Entries |
Document | Title | Date |
20080200485 | Kinase Inhibitors - Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use, thereof. More particularly, disclosed are inhibitors of Aurora-2 (Aurora-A) protein kinase. Also disclosed are methods of treating diseases associated with protein kinases, especially diseases associated with Aurora-2, such as cancer. | 08-21-2008 |
20080207656 | Methods, compositions, and kits for organ protection during systemic anticancer therapy - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents. | 08-28-2008 |
20080214589 | Thrombin Inhibiting 2,4-Dioxo-3,4-Dihydropyrimidine Derivatives - There is provided a compound of formula I wherein R | 09-04-2008 |
20080214590 | Zalcitabine (Ddc) Boosted Lamivudine (3Tc) Compositions for Antiretroviral Therapy - Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound is a new therapeutic anti HIV option, in combination with another drug such as a NRTI or a protease inhibitor. It's heightened and sustained antiretroviral potency is due to the increased intracellular level of 3TC triphosphate, the active form of 3TC. This effect is obtained by combining 3TC, in usual doses, with a reduced dose of ddC, in the same pharmaceutical formulation. The product could be administered twice or even once daily, which is convenient, and does not increase the pill burden for the patient. The reduced ddC dosage prevents the occurrence of ddC related side effects. Other cytidine derivatives (racemic or negative enantiomers) could have the same effects as ddC and could probably be combined with 3TC, and have the same effect. On the other hand, low dose ddC may also increase the intracellular levels of other cytidine derivatives as it does for 3TC. Boosted cytidine analogue reverse transcriptase inhibitor antiretroviral compound could also be formulated in combination with another drug such as another NRTI (e.g. abacavir) or any protease inhibitor in the same capsule or tablet. This approach offers a dual anti-HIV therapy that is as efficacious as the routine triple therapy. In this way the HIV treatment cost could be significantly reduced which is imperative for resource-poor settings. This new formulation is convenient and well tolerated with no additional toxicity than that of the combining drug (NRTI or protease inhibitor) and 3TC. Moreover, this will enable a larger number of patients to benefit from the already known 3TC effects. It will also increase the 3TC effects in those organs or HIV sanctuaries with usually reduced 3TC concentrations or activity. It could be indicated in both the initial as well as in salvage HIV therapy. It could also be used for therapy optimization or simplification. Moreover, in combination with another NRTI such as abacavir, or even alone, it could be beneficial for reducing the HIV harm in resource-poor settings. | 09-04-2008 |
20080221140 | 1-[2',3' -Dideoxy-3' C-(Hydroxymethyl) - Beta-D-Erythro-Pentofuranosyl] Cytosine Derivatives as Hiv - Compounds of the formula (I) wherein: R | 09-11-2008 |
20080227798 | POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: | 09-18-2008 |
20080249118 | Silencing of Tumor-Suppressive Genes by Cpg-Methylation in Prostate Cancer - The present invention relates to method and kits for diagnosing and/or treating prostate cancer. The method and kit relate to the determination and/or modulation of the methylation degree of tumor suppressive genes in biological samples. More particularly, CpG-methylation of 14-3-3σ was found in all primary PCa samples analysed, but not in matching normal prostate epithelial cells or benign prostate hyperplasia (BPH). CpG-methylation was accompanied by a decrease or loss of 14-3-3σ protein expression in primary PCa and PCa cell lines. PCa-precursor lesions, known as prostatic intraepithelial neoplasia (PIN), also displayed decreased levels of 14-3-3σ expression, whereas normal prostate epithelial cells and BPH showed high levels of 14-3-3σ protein expression. The generality of CpG-methylation in PCa suggests that silencing of 14-3-3σ significantly contributes to the formation of PCa. Furthermore, the CpG-methylation of 14-3-3σ in PCa may be exploited for diagnostic purposes. | 10-09-2008 |
20080249119 | Homogemcitabines - The invention relates to homogemcitabines of general formula (2), with the meanings for the substituents as given in claim | 10-09-2008 |
20080255168 | METHODS FOR ADMINISTERING DPD INHIBITORS IN COMBINATION WITH 5-FU AND 5-FU PRODRUGS - Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient. Also provided are topical formulations comprising DPD, TP and/or UP inhibitors and methods of using same. | 10-16-2008 |
20080262005 | Uracil-Type Gonadotropin-Releasing Hormone Receptor Antagonists and Methods Related Thereto - Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R | 10-23-2008 |
20080262006 | Selective endothelin type-a antagonists - This invention relates to novel endothelin receptor antagonists that selectively inhibit the interaction between Endothelin-1 (ET-1) and endothelin type-A receptors, their derivatives, acceptable acid addition salts. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by endothelin receptor antagonists, particularly those diseases and conditions that are beneficially treated by selective inhibitors of endothelin type-A receptors. | 10-23-2008 |
20080269267 | KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Met kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a Raf kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof. | 10-30-2008 |
20080275071 | Radiotherapy Enhancer - The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions when used in combination with a cancer radiotherapy. A radiotherapy enhancer comprising (A) tegafur and (B) gimeracil. | 11-06-2008 |
20080275072 | WEEKLY ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 11-06-2008 |
20080280930 | Pyrimidinone Compounds and Preparation and Use Thereof - Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia. | 11-13-2008 |
20080280931 | POLYMORPHS OF SUCCINATE SALT OF 2-[6-(3-AMINO-PIPERIDIN-1-YL)-3-METHYL-2,4-DIOXO-3,4-DIHYDRO-2H-PYRIMIDIN-1-YLMETHY]-4-FLUOR-BENZONITRILE AND METHODS OF USE THEREFOR - Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: | 11-13-2008 |
20080287476 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 11-20-2008 |
20080300265 | ANTIVIRAL DRUGS FOR TREATMENT OF ARENAVRUS INFECTION - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever and Crimean-Congo hemorrhagic fever). | 12-04-2008 |
20080306098 | Pharmacokinetics of protease inhibitors and other drugs - A method for modulating at least one pharmacokinetic property of a protease inhibitor upon administration to a host is provided. One administers to the host an effective amount of a bifunctional compound of less than about 5000 daltons comprising the protease inhibitor or an active derivative thereof and a pharmacokinetic modulating moiety. The pharmacokinetic modulating moiety binds to at least one intracellular protein. The bifunctional compound has at least one modulated pharmacokinetic property upon administration to the host as compared to a free drug control that comprises the protease inhibitor. | 12-11-2008 |
20080312262 | ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The invention relates to a compound of formula (I): | 12-18-2008 |
20080318986 | Ddc Compositions - A composition comprising from 1% to 3% dDC which is aqueous and ophthalmically acceptable is disclosed herein. | 12-25-2008 |
20080318987 | METHODS FOR MODULATING BONE FORMATION AND MINERALIZATION - Methods and compositions for modulating bone formation and mineralization are described. | 12-25-2008 |
20090005405 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses. | 01-01-2009 |
20090012106 | Methods, compositions, and kits for organ protection during systemic anticancer therapy - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents. | 01-08-2009 |
20090023763 | Condensed Pyridine Derivatives Useful as A2B Adenosine Receptor Antagonists - New antagonists of the A | 01-22-2009 |
20090023764 | Use of Pyrimidinedione Derivative for Preventing or Treating Hepatitis C - A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus. | 01-22-2009 |
20090054473 | THERAPY FOR COMPLICATIONS OF DIABETES - A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ET | 02-26-2009 |
20090062319 | METHODS OF INHIBITING THE INTERACTION BETWEEN S100 AND THE RECEPTOR FOR ADVANCED GLYCATION END-PRODUCTS - A method of inhibiting an interaction between a S100 protein and the receptor for advanced glycation end-products is provided comprising administering to a subject a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. In some embodiments, the S100 protein is S100P. In some embodiments, the S100 protein is S100P. In addition, the present invention provides a method of treating a cancer comprising administering to a mammal a therapeutically effective amount of cromolyn, C5, or salt, hydrate, or solvate thereof. Additional methods are also provided. | 03-05-2009 |
20090069353 | DEUTERIUM-ENRICHED AMBRISENTAN - The present application describes deuterium-enriched ambrisentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090069354 | DEUTERIUM-ENRICHED GEMCITABINE - The present application describes deuterium-enriched gemcitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090069355 | Bicyclic pyrazolone cytokine inhibitors - The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states. | 03-12-2009 |
20090076045 | Non-nucleoside reverse transcriptase inhibitors - Compounds of formula I, wherein R | 03-19-2009 |
20090082376 | DEUTERIUM-ENRICHED ALOGLIPTIN - The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-26-2009 |
20090082377 | Matrix Metalloproteinase Inhibitors - The present invention relates to compounds of Formula (I): | 03-26-2009 |
20090082378 | DERIVATIVES OF 4-(2-AMINO-1-HYDROXIETHYL)PHENOL AS AGONISTS OF THE B2 ADRENERGIC RECEPTOR - This present disclosure relates to compounds of formula (I): | 03-26-2009 |
20090099218 | SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS - This invention provides a series of BPU analogues; their synthesis and evaluated biological activity. BPU sulfur analogues were found to possess up to 20 fold increased potency, when compared to compound 1, in various cancerous cell lines. | 04-16-2009 |
20090105286 | Low-molecular inhibitors of cytohesin-family guanine nucleotide exchange factors - The invention relates to drugs and the use thereof, wherein said drugs contain compounds selected from a group comprising general formulas (1), (2), (3) and (4) and/or enantiomers, diastereomers or the pharmaceutically acceptable salts thereof. Said drugs are used for treating autoimmune and tumoral diseases and/or for immunosuppresion. | 04-23-2009 |
20090118315 | Methods of Treatment Using Sapacitabine - A first aspect of the invention relates to a method of treating leukaemia or myelodysplastic syndromes (MDS), said method comprising administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, to a subject in accordance with a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 7 consecutive days every 21 days or 14 consecutive days every 21 days. | 05-07-2009 |
20090131462 | Fungicidally Active Agent - The invention relates to a fungicidally active agent containing at least one other defined fungicide in addition to the fungicide N-[2-(1,3-dimethylbutyl)-3-thienyl]-1-methyl-3-(trifluormethyl)-1H-pyrazol-4-carboxamide (penthiopyrad). The invention also relates to a method for controlling pathogenic fungi using one such agent, and to the use of said agent for controlling pathogenic fungi. | 05-21-2009 |
20090149485 | PYRIMIDINEDIONES AS TYROSINE KINASE INHIBITORS - The present invention relates to a compound of formula (I) | 06-11-2009 |
20090149486 | 4,5-DIPHENYL-PYRIMIDINYL-OXY OR -MERCAPTO SUBSTITUTED CARBOXYLIC ACIDS, METHOD FOR THE PRODUCTION AND USE THEREOF AS MEDICAMENTS - This invention relates to a compound of formula I, | 06-11-2009 |
20090170883 | 3-ARYLPHENYL SULFIDE DERIVATIVE AND INSECTICIDE AND MITICIDE - 3-Arylphenyl sulfide derivatives represented by general formula (I): | 07-02-2009 |
20090176812 | HETEROMONOCYCLIC COMPOUND AND USE THEREOF - A compound represented by the formula (I): | 07-09-2009 |
20090186912 | ANTI-INFECTIVE AGENTS AND USES THEREOF - This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions. | 07-23-2009 |
20090186913 | Tetrahalogenated compounds useful as inhibitors of angiogenesis - Methods for inhibiting a neoplasm in a subject and methods of inhibiting undesired angiogenesis that include administering to a subject a therapeutically effective amount of at least one novel tetrahalogenated compound, or a pharmaceutically acceptable salt thereof. | 07-23-2009 |
20090192179 | CHROMAN DERIVATIVES - The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I | 07-30-2009 |
20090209563 | Pyridinoylpiperidines as 5-HT1F agonists - The present invention relates to compounds of formula I: | 08-20-2009 |
20090209564 | Glucagon Receptor Antagonist Compounds, Compositions Containing Such Compounds And Methods Of Use - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. | 08-20-2009 |
20090209565 | THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE - The present invention relates to a therapeutic agent for inflammatory bowel disease comprising 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof as an active ingredient. | 08-20-2009 |
20090215803 | Pyrimidinones as Casein Kinase II (CK2) Modulators - A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R | 08-27-2009 |
20090221617 | LEAD COMPOUND OF ANTI-HYPERTENSIVE DRUG AND METHOD FOR SCREENING THE SAME - A system for screening a small molecule library with 250,000 molecules to find out a compound of an anti-hypertensive drug aiming at human Angiotensin II type IA receptor is provided. The system includes a first database having a three-dimensional structure datum of a human Angiotensin II type IA receptor, a second database having molecular data of a plurality of small molecules, and a computer acquiring the three-dimensional structure datum and the molecular data from the first database and the second database respectively, wherein the computer has a molecular docking software for calculating a free energy of the human Angiotensin II type IA receptor bound to each of the plurality of small molecules, ranks the plurality of small molecules according to the respective free energy so as to select a top small molecule in the ranking as the compound of the drug. | 09-03-2009 |
20090221618 | AZABICYCLO (3, 1, 0) HEXAN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or a salt thereof: | 09-03-2009 |
20090239887 | Method of resolution and antiviral activity of 1,3-oxathiolane nucleoside enantiomers - A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (−)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner. | 09-24-2009 |
20090275600 | MODIFIED PYRIMIDINE GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a novel class of modified pyrimidine compounds and compositions and methods of using the compounds as glucocorticoid receptor modulators. | 11-05-2009 |
20090281132 | Pharmaceutical formulation for use in hiv therapy - The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules. | 11-12-2009 |
20090286818 | Pyridine Non-Classical Cannabinoid Compounds and Related Methods of Use | 11-19-2009 |
20090306111 | Pharmaceutical Comprising PPAR Agonist - An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. | 12-10-2009 |
20090306112 | ANTIVIRAL PROTEASE INHIBITORS - The invention is related to compounds of Formula I or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds. | 12-10-2009 |
20090306113 | PHARMACEUTICAL FORMULATION - The present invention provides enteric polymer coated tablet formulations for oral administration which comprise a phospholipase A2 enzyme Lipoprotein Associated Phospholipase A2 (Lp-PLA2) inhibitor, processes for preparing such formulations and their use in therapy, in particular the treatment of atherosclerosis. | 12-10-2009 |
20090306114 | Polymorphic and Other Crystalline Forms of Cis-FTC - Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B. | 12-10-2009 |
20090312352 | COMPOSITIONS AND METHODS FOR TREATMENT OF DISEASE CAUSED BY YERSINIA SPP INFECTION - The invention generally relates to compositions and methods for treatment of disease caused by | 12-17-2009 |
20090318482 | TABLET PREPARATION WITHOUT CAUSING A TABLETING TROUBLE - The present invention provides a tablet without causing a tableting trouble, which is superior in the tablet formability, dissolution property of pharmaceutically active ingredient, and the like. | 12-24-2009 |
20090318483 | Potentiators Of Glutamate Receptors - This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. | 12-24-2009 |
20090325988 | Glucocorticoid Mimetics, Methods of Making Them, Pharmaceutical Compositions and Uses Thereof - Compounds of Formula (I) | 12-31-2009 |
20100004273 | Compounds And Methods For Treating Disorders Related To Glucose Metabolism - The present invention relates to compounds and pharmaceutically acceptable salts thereof, and compositions comprising the same, that are useful in modulating lyn kinase activity, treating obesity, type II diabetes, metabolic syndrome, and in reducing blood glucose level, weight gain, or fat depot level, or treating a disease or condition associated with the same. | 01-07-2010 |
20100010024 | USE OF1,4-DIARYL-DIHYDROPYRIMIDINE-2-ON DERIVATIVES FOR TREATING PULMONARY ARTERIAL HYPERTENSION - The present application relates to the use of 1,4-diaryldihydropyrimidin-2-one derivatives of the formula (I) for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension, and to the use thereof for the manufacture of medicaments for the treatment and/or prophylaxis of pulmonary arterial hypertension and other types of pulmonary hypertension. | 01-14-2010 |
20100016343 | ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS - The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate α7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system. | 01-21-2010 |
20100022567 | Compositions containing pufa and/or uridine and methods of use thereof - This invention provides methods of enhancing brain development; increasing or enhancing intelligence; increasing or enhancing synthesis and levels of phospholipids, synapses, synaptic proteins, and synaptic membranes by a neural cell or brain cell, comprising contacting a subject or a pregnant or nursing mother thereof with a composition comprising an omega-3 fatty acid, an omega-6 fatty acid, and/or uridine, a metabolic precursor thereof, or a combination thereof. | 01-28-2010 |
20100022568 | ENDOTHELIN RECEPTOR ANTAGONISTS FOR EARLY STAGE IDIOPATHIC PULMONARY FIBROSIS - This present invention relates to the use of an endothelin receptor antagonist for the preparation of a medicament for the treatment of early stage idiopathic pulmonary fibrosis. | 01-28-2010 |
20100029699 | MATRIX METALLOPROTEINASE INHIBITORS - The present invention relates to compounds of Formula (I): | 02-04-2010 |
20100035905 | Hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)-pyr- imidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide - The present invention relates to hydrates of 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]-sulfonyl]benzamide. The invention also relates to a process for the preparation of these hydrates and to plant protection formulations which comprise hydrates of the phenyluracil I. | 02-11-2010 |
20100041685 | STAT3 INHIBITORS - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein. | 02-18-2010 |
20100041686 | 4,5-DIHYDRO-OXAZOL-2YL DERIVATIVES - The invention relates to compounds of formula I | 02-18-2010 |
20100048594 | USE OF CYTOHESIN INHIBITORS FOR CHEMICALLY INDUCING LONGEVITY - The invention relates to compounds selected from among the group comprising general formulas (1), (2), (3), and/or (4) and/or the enantiomers, diastereomers, and derivatives thereof, and the pharmaceutically acceptable salts thereof for producing a medicament used for therapeutically and/or preventively treating disease and pathological conditions linked to regulation of the insulin and/or insulin-like growth factor (IGF) signalling pathway and/or for chemically inducing longevity. | 02-25-2010 |
20100063078 | SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS - The present invention relates to novel compounds of formula (I) or salts thereof: | 03-11-2010 |
20100063079 | Pyrimidyl Sulphone Amide Derivatives as Chemokine Receptor Modulators - A compound of formula (I), pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof for the treatment of asthma, allergic rhinitis, COPD, inflammatory bowel disease, irritable bowel syndrome, osteoarthritis, osteoporosis, rheumatoid arthritis, psoriasis or cancer. | 03-11-2010 |
20100063080 | CXCR2 inhibitors - The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease. | 03-11-2010 |
20100069416 | Azabicyclo [3.1.0] Hexyl Derivatives as Modulators of Dopamine D3 Receptors - The present invention relates to certain azabicyclo compounds of formula (I)′: | 03-18-2010 |
20100105710 | SOLID PREPARATION COMPRISING 2-[[6-[(3R)-3-AMINO-1-PIPERIDINYL]-3,4-DIHYDRO-3-METHYL-2,4-DIOXO-1(2H)-P- YRIMIDINYL]METHYL]-4-FLUOROBENZONITRILE - The present invention provides a solid preparation containing 21[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active ingredient. Specifically, the present invention provides a solid preparation containing a granule composed of compound (A) or a salt thereof and an additive (excluding microcrystalline cellulose) and a tablet containing (a) a granule containing compound (A) or a salt thereof and microcrystalline cellulose, and (b) a tableting aid containing magnesium stearate and microcrystalline cellulose. | 04-29-2010 |
20100113491 | SYNTHESIS OF NOVEL TUBULIN POLYMERIZATION INHIBITORS: BENZOYLPHENYLUREA (BPU) SULFUR ANALOGS - A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM. | 05-06-2010 |
20100120806 | CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases. | 05-13-2010 |
20100125084 | DOSING REGIMENS FOR TREATMENT OF PROLIFERATIVE DISORDERS COMPRISING ADMINISTRATION OF SAPACITABINE - One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL). | 05-20-2010 |
20100130521 | METHOD OF TREATMENT USING FUSED AROMATIC COMPOUNDS HAVING ANTI-DIABETIC ACTIVITY - Fused aromatic compounds of Formula I are PPAR gamma agonists or partial agonists and are useful for weekly dosing in the treatment or control of type II diabetes, including hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes. | 05-27-2010 |
20100137344 | INDUCTION OF ANALGESIA IN NEUROPATHIC PAIN - The present invention relates to agents which are capable of inducing analgesia in chronic neuropathic pain, associated methods and uses thereof. In particular, the present invention provides compounds capable of activating the TRPM8 receptor for the treatment of chronic neuropathic pain. | 06-03-2010 |
20100137345 | PROPHYLACTIC AND THERAPEUTIC USE OF SIRTUIN INHIBITORS IN TNF-ALPHA MEDIATED PATHOLOGIES - The invention relates to the use of sirtuin inhibitors for reducing TNF-alpha production by cells and organisms. The invention also concerns prophylactic and therapeutic applications of sirtuin inhibitors in TNF-alpha mediated pathologies, such as various inflammatory and autoimmune disorders. | 06-03-2010 |
20100144770 | Pyrimidinones as Casein Kinase II (CK2) Modulators - A compound having Formula I: or a pharmaceutically acceptable salt thereof, wherein X, R, R and R are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof. The compounds of Formula I are inhibitors of Casein kinase II (CK2) pathways. | 06-10-2010 |
20100144771 | Novel Hydantoin Derivatives for the Treatment of Obstructive Airway Diseases - The invention provides compounds of formula (I): | 06-10-2010 |
20100152215 | METHODS OF IDENTIFYING ACTIVATORS OF LYN KINASE - The present invention relates to methods of identifying activators of lyn kinase by preincubating a test compound in the presence of lyn kinase; adding ATP and substrate to the lyn kinase and test compound; incubating the test compound, lyn kinase, ATP, and substrate; and measuring phosphorylation level of the substrate, whereby an increase in the phosphorylation of the substrate indicates that the test compound is an activator of lyn kinase. | 06-17-2010 |
20100152216 | MONOCYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: | 06-17-2010 |
20100152217 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years. | 06-17-2010 |
20100173921 | Antiretroviral Solid Oral Composition - The present invention provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with one or more excipients. The invention provides a composition which is smaller for a given amount of said active substance and possesses taste masking property and a process for preparing the composition. The present invention also provides an antiretroviral solid oral composition comprising one or more antiretroviral drugs, for example protease inhibitors such as lopinavir, ritonavir or a combination thereof with at least one water insoluble polymer, wherein the ratio of drug to polymer in the composition ranges from about 1:1 to about 1:6, and a process for preparing the composition. | 07-08-2010 |
20100173922 | Polymorphisms for Predicting Disease and Treatment Outcome - The invention provides compositions and methods for determining the increased risk for recurrence of certain cancers and the likelihood of successful treatment with one or both of chemotherapy and radiation therapy. The methods comprising determining the type of genomic polymorphism present in a predetermined region of the gene of interest isolated from the subject or patient. Also provided are nucleic acid probes and kits for determining a patient's cancer risk and treatment response. | 07-08-2010 |
20100184788 | HETEROCYCLIC DERIVATIVES - The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction, and heart failure development. | 07-22-2010 |
20100190810 | COMPOSITION AND METHOD FOR TREATMENT OF WARTS - Provided is a composition comprising 5-FU and salicylic acid. This composition is useful as a treatment for warts. As opposed to conventional compositions and methods, this composition need only be applied once a day. Also provided are methods for the preparation and use of the composition for treatment of warts. | 07-29-2010 |
20100197710 | Methods Of Activating IRS-1 And AKT - The present invention provides methods of activating IRS-1 and/or AKT and methods of treating or preventing IRS-1- and/or AKT-related disease, condition, or disorder. | 08-05-2010 |
20100197711 | BENZOTHIAZOLE COMPOUNDS - The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival. | 08-05-2010 |
20100204253 | Ribosome Structure and Protein Synthesis Inhibitors - The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism. | 08-12-2010 |
20100216826 | Polymorphisms in Voltage-Gated Sodium Channel Alpha 1-Subunit as Markers for Therapy Selection - A method for determining whether a patient in need thereof will respond to chemotherapy by screening a suitable sample isolated from the patient for a pre-selected polymorphism present in the VGSC gene. | 08-26-2010 |
20100222372 | THERAPEUTIC AGENT FOR INFLAMMATORY BOWEL DISEASE COMPRISING URACIL DERIVATIVE AS ACTIVE INGREDIENT - To provide a therapeutic agent for inflammatory bowel disease. | 09-02-2010 |
20100234405 | PYRIMIDINE NUCLEOSIDE DERIVATIVES AND SALTS THEREOF - A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents: | 09-16-2010 |
20100240685 | 2-S-Benzyl Substituted Pyrimidines As CRTH2 Antagonists - Provided herein are 2-S-benzyl pyrimidine compounds having CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity, useful for the prophylaxis and treatment of diseases associated with CRTH2 activity, including the treatment of allergic diseases, eosinophil-related diseases and basophil-related diseases. | 09-23-2010 |
20100249163 | RENIN INHIBITORS - The present invention relates to piperidinyl-based renin inhibitor compounds having the formula | 09-30-2010 |
20100280055 | Flavoring Systems for Pharmaceutical Compositions and Methods of Making Such Compositions - A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and/or mixtures thereof. Pharmaceutical compositions of the invention include a flavoring system of the invention, a solvent system, and at least one pharmaceutically active agent, such as lopinavir or derivatives thereof, ritonavir or derivatives thereof, or mixtures thereof. Methods for making such liquid pharmaceutical compositions are also disclosed. | 11-04-2010 |
20100286178 | COMPOUNDS AND USES THEREOF | 11-11-2010 |
20100286179 | EGFR POLYMORPHISMS PREDICT GENDER-RELATED TREATMENT - The invention provides compositions and methods for identifying a gender-specific cancer patient suitable for treatment with various treatment regimens available to cancer patients. After determining if a patient is suitable for therapy, the invention also provides methods for treating these patients. | 11-11-2010 |
20100292261 | QUORUM SENSING ANTAGONIST, METHOD OF PREVENTING A BIOFILM FORMATION USING THE QUORUM SENSING ANTAGONIST AND METHOD OF REDUCING A BACTERIAL CONTAMINATION USING THE QUORUM SENSING ANTAGONIST - In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well. | 11-18-2010 |
20100298363 | Use of carboxyamidotriazole (CAI) orotate in macular degeneration - Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases. | 11-25-2010 |
20100305145 | Substituted Aminobutyric Derivatives as Neprilysin Inhibitors - The present invention provides a compound of formula I′; | 12-02-2010 |
20100311773 | NOVEL ANABASEINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - Disclosed are novel anabaseine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds. | 12-09-2010 |
20100311774 | Combination Comprising Paclitaxel for Treating Ovarian Cancer - The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer. | 12-09-2010 |
20110009438 | SUBSTITUTED ISOXAZOLINE COMPOUND AND PEST CONTROL AGENT - There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted isoxazoline compound of General Formula (1): | 01-13-2011 |
20110015216 | Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 01-20-2011 |
20110028502 | DIHYDROPYRIMIDONE AMIDES AS P2X7 MODULATORS - Compounds of the formula I: | 02-03-2011 |
20110034488 | METHOD OF ASSAYING 5-FU - The present invention provides methods, compositions, devices and kits for assaying 5-FU. | 02-10-2011 |
20110034489 | SOLID DOSAGE FORMS OF HIV PROTEASE INHIBITORS - The present invention relates to a solid dosage form comprising a solid dispersion composition of at least one HIV protease inhibitor and water soluble polymer having a glass transition temperature (Tg) of at least about 50° C. in an amount of less than 50% by weight of the dosage form. It also relates to a process of preparation of such solid dosage forms. | 02-10-2011 |
20110034490 | N1-acyl-5-fluoropyrimidinone derivatives - This present disclosure is related to the field of N1-acyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 02-10-2011 |
20110034491 | 5-FLUORO-2-OXOPYRIMIDINE- 1(2H)-CARBOXYLATE DERIVATIVES - This present disclosure is related to the field of 5-fluoro-2-oxopyrimidine-1-(2H)-carboxylates and their derivatives and to the use of these compounds as fungicides. | 02-10-2011 |
20110034492 | N1-SUBSTITUTED-5-FLUORO-2-OXOPYRIMIDINONE-1(2H)-CARBOXAMIDE DERIVATIVES - This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides. | 02-10-2011 |
20110034493 | N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 02-10-2011 |
20110039872 | DEUTERIUM-ENRICHED CAPECITABINE - The present application describes deuterium-enriched capecitabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 02-17-2011 |
20110046169 | FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF - The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof. | 02-24-2011 |
20110053965 | SULFONATED PRECURSORS OF THYMIDINE FOR THE TREATMENT OF EPITHELIAL HYPERPLASIAS - This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration. | 03-03-2011 |
20110053966 | SYNERGISTIC FUNGICIDAL COMPOSITIONS CONTAINING A 5-FLUOROPYRIMIDINE DERIVATIVE FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula IA and/or IB and (b) at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, chlorothalanil, isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-[(3-isobutyryloxymethoxy-4-methoxypyridine-2-carbonyl)-amino]-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester, and (5,8-difluoroquinazolin-4-yl)-{2-[2-fluoro-4-(4-trifluoromethylpyridin-2-yloxy)-phenyl]-ethyl}-amine provides synergistic control of selected fungi. | 03-03-2011 |
20110053967 | (POLY) AMINOACETAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN THEIR PROCESS OF PREPARATION AND THEIR APPLICATIONS IN THERAPEUTICS AS ANTICANCER AGENTS - The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents. | 03-03-2011 |
20110065739 | NOVEL ISOXAZOLE DRIVATIVE - Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an agonistic activity on GPR120 and is therefore useful for the treatment of diabetes, obesity or hyperlipemia. [In formula (I), the A represents a phenyl group which may be substituted by a lower alkoxy group or the like; the 13 represents a bivalent group produced by removing two hydrogen atoms from a benzene ring which may be substituted by a halogen atom or the like; X represents a lower alkylene group having 2 to 4 carbon atoms in its main chain or the like, wherein a carbon atom constituting the main chain may be substituted by an oxygen atom or the like; and Y represents a hydrogen atom or the like.] | 03-17-2011 |
20110077259 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses. | 03-31-2011 |
20110077260 | METHODS, COMPOSITIONS, AND KITS FOR ORGAN PROTECTION DURING SYSTEMIC ANTICANCER THERAPY - Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents. | 03-31-2011 |
20110082162 | SYNERGISTIC FUNGICIDAL COMPOSITION CONTAINING 5-FLUOROCYTOSINE FOR FUNGAL CONTROL IN CEREALS - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, chlorothalonil and isobutyric acid (3S,6S,7R,8R)-8-benzyl-3-[(3-isobutyryloxymethoxy-4-methoxypyridine-2-carbonyl)-amino]-6-methyl-4,9-dioxo-[1,5]dioxonan-7-yl ester provides synergistic control of selected fungi. | 04-07-2011 |
20110082163 | NOVEL URACIL COMPOUND OR SALT THEREOF HAVING HUMAN DEOXYURIDINE TRIPHOSPHATASE INHIBITORY ACTIVITY - Provided is a uracil compound or a salt thereof, which has potent human dUTPase inhibitory activity and is useful as, for example, an antitumor drug. | 04-07-2011 |
20110098313 | POSITIVE ALLOSTERIC MODULATORS (PAM) - The present invention relates to phenylethynyl compounds of formula I | 04-28-2011 |
20110112123 | Compositions for Intratumoral Administration - The present disclosure describes compositions for intratumoral administration which include a tissue-stabilizing agent and a therapeutic agent. | 05-12-2011 |
20110112124 | FUNGICIDAL COMPOSITIONS - A method of controlling phytopathogenic diseases on useful plants or on propagation material thereof, which comprises applying to the useful plants, the locus thereof or propagation material thereof a combination of components A) and B) in a synergistically effective amount, wherein component A) is a compound of formula (I) wherein R | 05-12-2011 |
20110124668 | NOVEL INDOLE DERIVATIVE HAVING, CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP - The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKKβ inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKKβ. In the formula, R | 05-26-2011 |
20110152300 | 2-ALDOXIMINO-5-FLUOROPYRIMIDINE DERIVATIVES - This present disclosure is related to the field of 2-aldoximino-5-fluoropyrimidines and their derivatives and to the use of these compounds as fungicides. | 06-23-2011 |
20110152301 | Compounds that Inhibit HIV Particle Formation - The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV. | 06-23-2011 |
20110160235 | TRIAZOLYL TROPANE DERIVATIVES - This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor. | 06-30-2011 |
20110172257 | (POLY) AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS - The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. Formula (1) wherein: —R represents hydrogen or C | 07-14-2011 |
20110178110 | Genotype and Expression Analysis for Use in Predicting Outcome and Therapy Selection - The invention provides compositions and methods for determining the likelihood of successful treatment with a various treatment regimens available to gastrointestinal cancer patients. After determining if a patient is likely to be successfully treated, the invention also provides methods for treating these patients. | 07-21-2011 |
20110184006 | METHOD AND COMPOSITION FOR THERMALLY STABILIZING VITAMIN C WITHIN NANO LAYERS OF MONTMORILLONITE CLAY - A thermally stable Vitamin C composition containing montmorillonite, an organic acid containing L-ascorbic acid or a derivative thereof, a divalent cation present within nanolayers of the montmorillonite, wherein the organic acid is combined with the divalent cation within the nanolayers to form an organic acid-montmorillonite chelate. | 07-28-2011 |
20110190326 | IMIDAZO[1,5]NAPHTHYRIDINE COMPOUNDS, THEIR PHARMACEUTICAL USE AND COMPOSITIONS - The present invention is directed to compounds of Formula (I), | 08-04-2011 |
20110201634 | DIHYDROPYRIDIMIDINONE COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASES AND PROCESS FOR PREPARING THE SAME - The present invention relates to a dihydropyrimidinone compound of formula (I) wherein X represents O, S, etc. and R′ represents alkyl, alkoxy, thioalkyl, thioalkyloxy, phenyl, substituted phenyl, phenyloxy, substituted phenyloxy, amino, monosubstitutedamino, disubstitutedamino, aryl, heteroaryl, aryloxy, heteroaryloxy, halo; R″ represents alkoxy, phenyloxy, substituted phenyloxy, aryloxy, heteroaryloxy, halo, NR | 08-18-2011 |
20110212981 | Method of Determining a Chemotherapeutic Regimen Based on ERCC1 and TS Expression - The present invention relates to prognostic methods which are useful in medicine, particularly cancer chemotherapy. The object of the invention to provide a method for assessing TS and/or ERCC1 expression levels in fixed or fixed and paraffin embedded tissues and prognosticate the Probable resistance of a patient's tumor to treatment with 5-FU and oxaliplatin-based therapies by examination of the amount of TS and/or ERCC1 mRNA in a Patient's tumor cells and comparing it to a predetermined threshold expression level for those genes. More specifically, the invention provides to oligonucleotide prither pairs ERCC1 and TS and methods comprising their use for detecting levels of ERCC1 and TS mRNA, respectively. | 09-01-2011 |
20110212982 | Administration of Dipeptidyl Peptidase Inhibitors - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions. | 09-01-2011 |
20110245282 | Compounds - The invention provides a compound according to formula (I): wherein: X is O or S; Y is O or S; each Ar and Ar′ is independently a mono-, bi- or tricyclic aryl or heteroaryl group optionally substituted with one or more substituents selected from halo, alkyl, aryl, heteroaryl, hydroxyl, nitro, amino, alkoxy, alkylthio, cyano, thio, ester, acyl and amido; each R | 10-06-2011 |
20110251220 | Pharmaceutical compositions comprising gamma secretase modulators - The present invention relates to pharmaceutical compositions comprising gamma secretase modulators as well as to the use of gamma secretase modulators for treating renal disorders, cancer, neurodegenerative disorders as well as related disorders. | 10-13-2011 |
20110257210 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX - The present application discloses novel benzimidazole derivatives of general formula (I) or an N-oxide thereof, any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein R represents a pyridyl or pyrimidyl group; which pyridyl or pyrimidyl group is optionally substituted with one or more substituents independently selected from the group consisting of: halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, alkyl, hydroxy, hydroxyalkyl and alkoxy, and their use as modulators of the GABA | 10-20-2011 |
20110263626 | NOVEL BRADYKININ B1-ANTAGONISTS - The present invention relates to compounds of general formula I | 10-27-2011 |
20110263627 | N3-SUBSTITUTED-N1-SULFONYL-5-FLUOROPYRIMIDINONE DERIVATIVES - This present disclosure is related to the field of N3-substituted-N1-sulfonyl-5-fluoropyrimidinones and their derivatives and to the use of these compounds as fungicides. | 10-27-2011 |
20110269785 | Substituted 2-Aminoacetamides and the Use Thereof - The invention is directed to substituted 2-aminoacetamides represented by formula (II): | 11-03-2011 |
20110281900 | Crystalline Pharmaceutical - New crystalline forms of lopinavir are disclosed. | 11-17-2011 |
20110294839 | NOVEL POLYMORPHS OF LOPINAVIR - The present invention provides a novel cyclohexane solvate form of lopinavir, and a process for its preparation thereof. The present invention also provides a novel desolvated crystalline form of lopinavir, process for its preparation and to pharmaceutical composition containing it. Thus, for example, lopinavir cyclohexane solvate was heated at 100° C. for 10 hours to give lopinavir desolvated crystalline form H1. | 12-01-2011 |
20110306624 | GLUCAGON RECEPTOR ANTAGONIST COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE - Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included. | 12-15-2011 |
20110312983 | DEUTERIUM-ENRICHED ALOGLIPTIN - The present application describes deuterium-enriched alogliptin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 12-22-2011 |
20110312984 | STAT3 INHIBITORS - Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein. | 12-22-2011 |
20110319437 | IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition. | 12-29-2011 |
20110319438 | NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I) | 12-29-2011 |
20110319439 | AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - MCHR1 antagonists are provided having the following Formula I: | 12-29-2011 |
20120004252 | NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. | 01-05-2012 |
20120010227 | FORMULATION FOR NAIL AND NAIL BED DISEASES - The invention relates to a pharmaceutical composition with a content in active ingredient that can be an antimycotic, so that the composition is suitable for the treatment of onychomycoses, in particular severe onychomycoses. The inventive formulation is an ointment-like thermogel at body temperature and an inviscid thermogel at lower temperatures and facilitates the permeation of sufficient active ingredient quantities through human fingernails and toenails, in order to also treat severe onychomycoses. | 01-12-2012 |
20120015966 | PPAR ACTIVE COMPOUNDS - Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ. | 01-19-2012 |
20120022087 | AMORPHOUS AMBRISENTAN - The invention relates to amorphous ambrisentan, preferably together with a surface stabiliser in the form of a stable intermediate. The invention further relates to methods of producing stable amorphous ambrisentan and pharmaceutical formulations containing stable amorphous ambrisentan. | 01-26-2012 |
20120022088 | PHARMACEUTICAL COMBINATION OF 5-FLUOROURACIL AND DERIVATE OF 1,4-DIHYDROPYRIDINE AND ITS USE IN THE TREATMENT OF CANCER - New compounds of 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid ester type having general formula I | 01-26-2012 |
20120022089 | Solid Pharmaceutical Dosage Form - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 01-26-2012 |
20120029000 | PROCESS FOR THE PREPARATION OF ALOGLIPTIN - The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV). | 02-02-2012 |
20120035196 | CARBOXYLIC ACID COMPOUND | 02-09-2012 |
20120041009 | PYRIMIDINE COMPOUND AND ITS USE IN PEST CONTROL - A pyrimidine compound represented by below formula (I) has excellent control activity against pests and is useful as an active ingredient of a pest controlling agent. | 02-16-2012 |
20120083503 | METHOD FOR PREDICTING THERAPEUTIC EFFICACY OF CHEMOTHERAPY ON NON-SMALL-CELL LUNG CANCER - This invention relates to an antitumor agent comprising carboplatin and a combination drug of tegafur/gimeracil/oteracil potassium to be administered to a cancer patient selected according to an expression level of thymidylate synthase gene. | 04-05-2012 |
20120088783 | CHROMAN DERIVATIVES - The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I | 04-12-2012 |
20120108616 | SUBSTITUTED OXAZOLE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors. | 05-03-2012 |
20120115894 | IMIDAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH AND AS FAAH IMAGING AGENTS - The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease. | 05-10-2012 |
20120122907 | Novel Pyrazole Derivatives and their use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors - The present invention relates to novel compounds of Formula (I), wherein M, P, X | 05-17-2012 |
20120129878 | TABLET - Provided is a tablet having a high content of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof as a pharmaceutically active component. A tablet containing compound (A) or a salt thereof, and a fluidizer, which has a compound (A) content of 35-50 weight %. | 05-24-2012 |
20120136017 | USE OF 4'-THIO-2'-DEOXYNUCLEOSIDES AS ANTI ORTHOPOXVIRUS AGENTS - Compound represented by the formulae: | 05-31-2012 |
20120142716 | 4-PYRIMIDINESULFAMIDE DERIVATIVE - The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound. | 06-07-2012 |
20120142717 | COMPOUNDS - The present invention relates to novel compounds that inhibit Lp-PLA | 06-07-2012 |
20120149723 | 5-METHYL-PIPERIDINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS FOR THE TREATMENT OF SLEEP DISORDER - This invention relates to heteroaryloxy 5-methyl substituted piperidine derivatives and their use as pharmaceuticals. | 06-14-2012 |
20120157485 | SYNERGISTIC FUNGICIDAL INTERACTIONS OF 5-FLUOROCYTOSINE AND OTHER FUNGICIDES - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, pentiopyrad, fluopyram, boscalid, mancozeb, and pyrimethanil provides synergistic control of selected fungi. | 06-21-2012 |
20120157486 | SYNERGISTIC FUNGICIDAL INTERACTIONS OF AMINOPYRIMIDINES AND OTHER FUNGICIDES - A fungicidal composition containing a fungicidally effective amount of a) a compound of Formula I and (b) at least one fungicide selected from the group consisting of myclobutanil, fenbuconazole, difenoconazole, trifloxystrobin, penthiopyrad, fluopyram, boscalid, mancozeb, pyrimethanil, and bixafen provides synergistic control of selected fungi. | 06-21-2012 |
20120157487 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 06-21-2012 |
20120184573 | PROCESS FOR THE PREPARATION OF AMBRISENTAN AND NOVEL INTERMEDIATES THEREOF - The invention relates to improved processes for the preparation of ambrisentan. The invention also relates to a novel intermediate useful in the preparation of ambrisentan and a process for the preparation of the intermediate. The invention also relates to new polymorphic form of ambrisentan. In particular, it relates to a polymorphic form, designated as Form I of ambrisentan and a process for the preparation of the Form I. | 07-19-2012 |
20120190699 | PYRIDONES USEFUL AS INHIBITORS OF KINASES - The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes. | 07-26-2012 |
20120196884 | UREA SUBSTITUTED SULPHONAMIDE DERIVATIVES - The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially α2β1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I′). | 08-02-2012 |
20120214831 | METHOD FOR DETERMINATION OF SENSITIVITY TO ANTI-CANCER AGENT - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. | 08-23-2012 |
20120220612 | PHARMACEUTICAL COMPRISING PPAR AGONIST - An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye. | 08-30-2012 |
20120220613 | METHOD FOR DETERMINING SENSITIVITY TO AN ANTICANCER AGENT - To provide a marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker. | 08-30-2012 |
20120220614 | SUBSTITUTED BIARYL DERIVATIVES AND METHODS OF USE THEREOF - The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient. | 08-30-2012 |
20120232103 | NOVEL 5-FLUOROURACIL DERIVATIVE - The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: | 09-13-2012 |
20120232104 | NOVEL SULFONAMIDES AS L-CPT1 INHIBITORS - The invention is concerned with novel sulfonamide derivatives of formula (I) | 09-13-2012 |
20120245188 | METHODS OF TREATING MEMORY LOSS AND ENHANCING MEMORY PERFORMANCE - The present invention provides methods and compositions for enhancing working memory impaired due to aging, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), Parkinson's disease, alcoholism or alcohol withdrawal or Huntington's disease using p38 MAPK inhibitor such as SB239063. | 09-27-2012 |
20120252829 | TIVOZANIB AND CAPECITABINE COMBINATION THERAPY - A method of treating a tumor in a subject using a combination of tivozanib and capecitabine is disclosed. | 10-04-2012 |
20120252830 | Substituted Aminobutyric Derivatives as Neprilysin Inhibitors - The present invention provides a compound of formula I′; | 10-04-2012 |
20120258978 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. | 10-11-2012 |
20120270890 | Methods of Pancreatic Beta Cell Regeneration - Disclosed are new methods for pancreatic β-cell regeneration and the methods for identifying adult pancreatic endocrine stem cells and the methods for identifying the existence of differentiation processes from adult pancreatic endocrine stem cells toward pancreatic β-cell fate and a new animal model for pancreatic β-cell regeneration. The present invention can be utilized in screening and development of new medicines and therapy protocols for diabetes. | 10-25-2012 |
20120283281 | NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS - The present invention relates to new derivatives of epipodophyllotoxin 4-substituted with an optionally substituted (poly)aminoalkylaminoalkylamide, or alkyl-urea or alkyl-sulfonamide chain, a process for preparing them and their use as a medicine as an anticancer agent. | 11-08-2012 |
20120289526 | IMIDAZOLIDINEDIONE DERIVATIVES - The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy. | 11-15-2012 |
20120295929 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Additionally, and surprisingly compositions including uracil or a metabolite thereof are effective for treating or preventing various dermatoses. | 11-22-2012 |
20120295930 | NOVEL PROCESS FOR THE PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE - The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients. | 11-22-2012 |
20120309777 | SUBSTITUTED 2-IMIDAZOLIDONES AND ANALOGS - Compounds of formula (I): wherein R | 12-06-2012 |
20120329820 | Pyridinoylpiperidines As 5-HT1F Agonists - The present invention relates to compounds of formula I: | 12-27-2012 |
20120329821 | PESTICIDAL COMPOSITIONS - The invention disclosed in this document is related to field of pesticides and their use in controlling pests. | 12-27-2012 |
20130005756 | METHOD FOR TREATING PULMONARY DISEASES USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions of the lungs associated with excessive cell proliferation, remodeling, inflammation, vasoconstriction, bronchoconstriction, airway hyperreactivity and edema. Particularly, this invention is directed to methods of treating pulmonary diseases such as asthma; chronic obstructive pulmonary disease; respiratory tract illness caused by respiratory syncytial virus; pulmonary arterial hypertension; acute respiratory distress syndrome and ventilator induced lung injury; cystic fibrosis; bronchiectasis; alpha-1-antitrypsin deficiency; rhinitis; rhinosinusitis; primary ciliary dyskinesia; pneumonia; bronchiolitis caused by agents other than respiratory syncytial virus; and interstitial lung disease including lymphangioleiomyomatosis; idiopathic pulmonary fibrosis; obliterative bronchiolitis or bronchiolitis obliterans organizing pneumonia due to lung transplantation or HSCT; nonspecific interstitial pneumonia; cryptogenic organizing pneumonia; acute interstitial pneumonia; respiratory bronchiolitis-associated interstitial lung disease; or pulmonary sarcoidosis. The method comprises administering to a subject an effective amount of a rho kinase inhibitor compound to treat the disease. | 01-03-2013 |
20130012530 | New Positive allosteric modulators of nicotinic acetylcholine receptor - The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor. | 01-10-2013 |
20130035351 | Oximes For Treatment Of Peripheral And Central Nervous System Exposure To Acetyl Cholinesterase Inhibitors - The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates. | 02-07-2013 |
20130045984 | 5-FLUORO-4-IMINO-3,4-DIHYDROPYRIMIDIN-2-(1H)-ONES DERIVATIVES - This present disclosure is related to the field of 5-fluoro-4-imino-3-(substituted)-3,4-dihydropyrimidin-2(1H)ones and their derivatives and to the use of these compounds as fungicides. | 02-21-2013 |
20130045985 | N-(5-FLUORO-2-((4-METHYLBENZYL)OXY)PYRIMIDIN-4-YL)BENZAMIDE DERIVATIVES - This present disclosure is related to the field of N-(5-fluoro-2-((4-methylbenzyl)oxy)pyrimidin-4-yl)benzamides and their derivatives and to the use of these compounds as fungicides. | 02-21-2013 |
20130059872 | POLYMORPHS OF ALOGLIPTIN BENZOATE - The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes. | 03-07-2013 |
20130072508 | SOLID PHARMACEUTICAL DOSAGE FORM - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 03-21-2013 |
20130079361 | NOVEL IODO PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS - Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound. | 03-28-2013 |
20130079362 | CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES - Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases. | 03-28-2013 |
20130109707 | FLUOROURACIL DERIVATIVES | 05-02-2013 |
20130109708 | Chemical Compounds | 05-02-2013 |
20130116269 | CYCLIC N,N'-DIARYLTHIOUREAS AND N,N'-DIARYLUREAS - ANDROGEN RECEPTOR ANTAGONISTS, ANTICANCER AGENT, METHOD FOR PREPARATION AND USE THEREOF - The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. | 05-09-2013 |
20130123288 | POLYSUBSTITUTED DERIVATIVES OF 2-HETEROARYL-6-PHENYLIMIDAZO[1,2-a]PYRIDINES, AND PREPARATION AND THERAPEUTIC USE THEREOF - Compounds of formula (I): | 05-16-2013 |
20130131091 | HARMFUL ORGANISM CONTROL AGENT - The present invention provides a composition for use as a harmful organism control agent comprising as an active ingredient one or more of compounds represented by formula (I) or salts thereof and an agriculturally or zootechnically acceptable carrier. | 05-23-2013 |
20130131092 | NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein X | 05-23-2013 |
20130131093 | Novel Dihydropyrimidin-2(1H)-One Compounds As Neurokinin-3 Receptor Antagonists - The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same. | 05-23-2013 |
20130143907 | PYRAZOLOQUINOLINE DERIVATIVES - A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. | 06-06-2013 |
20130150392 | IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition. | 06-13-2013 |
20130158055 | Prevention Of Pancreatic Beta Cell Degeneration - The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in methods of preventing pancreatic beta cell degeneration or methods of treating a disorder associated with pancreatic beta cell degeneration, such as type I diabetes. | 06-20-2013 |
20130158056 | ALKOXY PYRIMIDINE PDE10 INHIBITORS - The present invention is directed to 2-alkoxy pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction. | 06-20-2013 |
20130165460 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 06-27-2013 |
20130172377 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions and methods comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile or a pharmaceutically acceptable salt thereof administered once weekly. | 07-04-2013 |
20130190336 | STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE-SULFAMIDE - The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof | 07-25-2013 |
20130190337 | SOLID DOSAGE FORMS OF HIV PROTEASE INHIBITORS - The present invention relates to a solid dosage form comprising a solid dispersion composition of at least one HIV protease inhibitor and a water-soluble polymer having a glass transition temperature (Tg) of at least about 50° C. in an amount of less than 50% by weight of the dosage form. It also relates to a process of preparation for such solid dosage forms. | 07-25-2013 |
20130190338 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 07-25-2013 |
20130203790 | SULFUR-CONTAINING COMPOUNDS AS ANTI-PROLIFERATIVE AGENTS - Novel sulphur-containing compounds and pharmaceutically acceptable salts thereof are disclosed, which have utility as anti-proliferative agents against mammalian cells. The invention provides a method for synthesizing the sulphur-containing compounds. | 08-08-2013 |
20130203791 | Tablets and Preparation Thereof - The present invention features processes of making tablets having reduced internal fractures. In one aspect, the processes comprise the steps of (1) compressing a pre-tabletting material in a die to form a tablet, where an internal surface of the die is lubricated with at least one lubricant, and the pre-tabletting material comprises at least one therapeutic agent and at least one pharmaceutically acceptable polymer; and (2) ejecting said tablet from said die. In another aspect, the processes employ a granular or powdery pre-tabletting material which comprises at least one therapeutic agent and at least one pharmaceutically acceptable polymer, wherein 90% of the particles in the pre-tabletting material are smaller than 400 μm. | 08-08-2013 |
20130225619 | SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR DISEASE TREATMENT - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. | 08-29-2013 |
20130237552 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 09-12-2013 |
20130245051 | CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia) and (Ib), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, j which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell Or the inhibition of the conversion of cortisone to Cortisol in a cell. | 09-19-2013 |
20130252984 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 09-26-2013 |
20130252985 | Flavoring Systems for Pharmaceutical Compositions and Methods of Making Such Compositions - A flavoring system for a liquid pharmaceutical composition and pharmaceutical compositions containing such flavoring systems are disclosed. Flavoring systems of the invention include at least one sweetening agent, at least two flavored ingredients, and at least one flavor modifier selected from the group consisting of citric acid, sodium citrate, sodium chloride, and mixtures thereof. At least two of the flavored ingredients are selected from the group consisting of a vanilla flavored ingredient, a peppermint flavored ingredient, a menthol flavored ingredient, a cotton candy flavored ingredient, and mixtures thereof. The one or more sweetening agents comprise glycerin, monoammonium glycyrrhizinate, saccharin sodium, acesulfame potassium, high fructose corn syrup, and/or mixtures thereof. Pharmaceutical compositions of the invention include a flavoring system of the invention, a solvent system, and at least one pharmaceutically active agent, such as lopinavir or derivatives thereof, ritonavir or derivatives thereof, or mixtures thereof. Methods for making such liquid pharmaceutical compositions are also disclosed. | 09-26-2013 |
20130252986 | COMPOUNDS - The present invention relates to novel compounds that inhibit Lp-PLA | 09-26-2013 |
20130267547 | PRODRUGS UTILIZING A TRANSPORTER-DIRECTED UPTAKE MECHANISM - Prodrugs comprising a lipophilic drug linked to a transport moiety that can be taken up by a fatty acid transporter are provided. The transport moiety comprises a lipid chain connected to a hydrophilic group (e.g. a carboxylic acid, a phosphate, or a sphingosine-like moiety). Due to the presence of the transport moiety, the prodrugs are substrates for endogenous fatty acid transporter systems. The transport moiety thus serves as a carrier or targeting moiety to facilitate uptake of the entire prodrug complex by endogenous fatty acid transporter systems, thereby moving the prodrug into cells and tissues where drug distribution and effects are desired. Hydrolysis of the chemical linkage between the lipid-like moiety and the lipophilic drug releases the drug in an active form within the cells or tissues. | 10-10-2013 |
20130296351 | 2-Thiopyrimidinones - Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions. | 11-07-2013 |
20130296352 | PYRAZOLOQUINOLINE DERIVATIVES - A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. | 11-07-2013 |
20130310406 | MIR-193A-3P AND ASSOCIATED GENES PREDICT TUMORIGENESIS AND CHEMOTHERAPY OUTCOMES - The disclosure provides a correlation between the expression level of the miR-193a gene, which can be regulated by its methylation status, and both tumorigenesis of and the resistance of a cancer cell to a pyrimidine antimetabolite (5-FU) based chemotherapy. In addition to the methylation status and the expression of miR-193a, its downstream genes, such as E2F1, SRSF2, and apoptotic genes such as caspase 2, are also involved and can serve as useful markers for cancer therapy prognosis and for therapy selection. | 11-21-2013 |
20130310407 | COMBINATIONS COMPRISING MACITENTAN FOR THE TREATMENT OF GLIOBLASTOMA MULTIFORME - The invention relates to the use of macitentan in combination with a cytotoxic therapy agent (such as temozolomide or paclitaxel), with radiotherapy or with both a cytotoxic therapy agent and radiotherapy, in the treatment of malignant glioma, in particular glioblastoma multiforme. | 11-21-2013 |
20130317048 | COMBINATION COMPRISING PACLITAXEL FOR TREATING OVARIAN CANCER - The invention relates to the combination of an endothelin receptor antagonist of formula (I) | 11-28-2013 |
20130324566 | PYRIMIDINE COMPOUNDS INHIBITING THE FORMATION OF NITRIC OXIDE AND PROSTAGLANDIN E2, METHOD OF PRODUCTION THEREOF AND USE THEREOF - The invention provides pyrimidine compounds of general formula (I), which reduce simultaneously the production of nitric oxide (NO) and prostaglandin E2 (PGE2). They have no negative effect on the viability of cells in concentrations decreasing the production of these factors by up to 50%; they are not cytotoxic. Furthermore, a method of preparation of the pyrimidine compounds of general formula (I), carrying 2-formamido group, a pharmaceutical composition comprising the substituted pyrimidine compounds according to the invention, and the use of these compounds for the treatment of inflammatory and cancer diseases are provided. | 12-05-2013 |
20130338178 | SIRTUIN MODULATORS AS INHIBITORS OF CYTOMEGALOVIRUS - Agents and methods of inhibiting or improving the growth of viruses are provided. | 12-19-2013 |
20130345244 | LOCAL TREATMENT OF NEUROFIBROMAS - A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed. | 12-26-2013 |
20140011824 | N1-SUBSTITUTED-5-FLUORO-2-OXOPYRIMIDINONE-1(2H)-CARBOXAMIDE DERIVATIVES - This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides. | 01-09-2014 |
20140024665 | GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO - GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: | 01-23-2014 |
20140024666 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) | 01-23-2014 |
20140031376 | IMINOPROPENE COMPOUND AND USE THEREOF - The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition. | 01-30-2014 |
20140045872 | 17a-HYDROXYLASE/C17,20-LYASE INHIBITORS - The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R | 02-13-2014 |
20140045873 | NOVEL MICROBIOCIDES - The present invention provides compounds of formula (I) wherein A | 02-13-2014 |
20140066468 | AMORPHOUS FORM OF LOPINAVIR AND RITONAVIR MIXTURE - The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it. | 03-06-2014 |
20140073658 | Dipyridylamine Derivative - Disclosed herein are compounds, or pharmacologically acceptable salts thereof, having glucokinase activating activity. In various aspects, the compounds are represented by general formula (I), or pharmacologically acceptable salts thereof: | 03-13-2014 |
20140088125 | USE OF 3-CARBOXY-N-ETHYL-N,N-DIMETHYLPROPAN-1-AMINIUM SALTS IN THE TREATMENT OF CARDIOVASCULAR DISEASE - Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease. | 03-27-2014 |
20140094479 | Process For Producing A Solid Dispersion Of An Active Ingredient - A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts ( | 04-03-2014 |
20140107139 | HYDANTOIN DERIVATIVES AS KV3 INHIBITORS - The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders. | 04-17-2014 |
20140107140 | COMPOSITIONS AND METHODS FOR TREATMENT OF GULF WAR ILLNESS - Pharmaceutical compositions and methods for the treatment of Gulf War Illness in human patients comprising administering a central nervous system (CNS) stimulant in a daily low-dosage amount, and micronutrients acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha-lipoic acid. The CNS stimulant and micronutrient components may be in admixture for convenient daily oral administration of a low dosage CNS stimulant and micronutrients in the range of about 60-250 mg acetyl L-carnitine, 50-200 mg L-tyrosine, 60-250 mg N-acetyl cysteine, and 25-100 mg alpha-lipoic acid per day. | 04-17-2014 |
20140113921 | FORMULATIONS OF PYRIMIDINEDIONE DERIVATIVE COMPOUNDS - The present disclosure relates to pharmaceutical compositions of pyrimidinedione derivative compounds and methods of preparing and uses thereof. The disclosure also relates to methods of enhancing bioavailability of pyrimidinedione derivative compounds in pharmaceutical compositions administered to a subject and methods of reducing the amount of a pyrimidinedione derivative compound in a pharmaceutical composition while achieving the same bioavailability in a subject. | 04-24-2014 |
20140113922 | COMPOUNDS - The present invention relates to novel compounds that inhibit Lp-PLA | 04-24-2014 |
20140155420 | INHIBITORS OF EYA2 - The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject. | 06-05-2014 |
20140163054 | Methods And Formulations For Modulating Lyn Kinase Activity And Treating Related Disorders - The present invention relates to compounds and pharmaceutically acceptable salts thereof and formulations comprising the compounds or a pharmaceutically acceptable salts thereof that are useful in modulating lyn kinase activity. In particular, the compounds or a pharmaceutically acceptable salts thereof are useful for treating or preventing a disease or disorder including cardiovascular disease, dyslipidemia, dyslipoproteinemia, a disorder of glucose metabolism, metabolic syndrome (i.e., Syndrome X), a peroxisome proliferator activated receptor-associated disorder, septicemia, a thrombotic disorder, type II diabetes, obesity, pancreatitis, hypertension, renal disease, inflammation, or impotence. | 06-12-2014 |
20140179721 | SOLID PHARMACEUTICAL DOSAGE FORM - A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 5° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10. | 06-26-2014 |
20140213602 | ANTITUMOR AGENT AND THERAPEUTIC EFFECT PREDICTION METHOD FOR PATIENTS WITH KRAS-MUTATED COLORECTAL CANCER - This invention provides a method for predicting a therapeutic effect of chemotherapy that uses an antitumor agent comprising α,α,α-trifluorothymidine and 5-chloro-6-(1-(2-iminopyrrolidinyl) methyl)uracil hydrochloride at a molar ratio of 1:0.5 on a colorectal cancer patient, | 07-31-2014 |
20140221409 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): | 08-07-2014 |
20140221410 | Fluorinated 3-(2-Oxo-3-(3-Arylpropyl)Imidazolidin-1-yl)-3-Arylpropanoic Acid Derivatives - The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described. | 08-07-2014 |
20140235659 | DELTA-TOCOTRIENOL TREATMENT AND PREVENTION OF PANCREATIC CANCER - Methods are disclosed for treating neoplastic disorders, such as pancreatic cancer, using tocotrienols; namely, gamma-tocotrienol and delta tocotrienol. The antitumorogenic effects of these compounds are shown both in vitro and in vivo using several human pancreatic cancer cell lines and MIA-PACA2 human pancreatic cancer cells xenografted in nude mice. Also disclosed are methods of testing the efficacy of potential chemotherapeutic agents by measuring their effect on surrogate endpoint biomarkers, such as Ki-67 and p27. Associated compounds are also disclosed. | 08-21-2014 |
20140235660 | COMPOUNDS AND COMPOSITIONS AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS - The present invention relates to compounds of formula I: | 08-21-2014 |
20140235661 | NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. | 08-21-2014 |
20140256757 | ADMINISTRATION OF DIPEPTIDYL PEPTIDASE INHIBITORS - Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof in combination with metformin and in combination with pioglitazone. | 09-11-2014 |
20140288105 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 09-25-2014 |
20140288106 | CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula 1 | 09-25-2014 |
20140288107 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 09-25-2014 |
20140288108 | PROCESS FOR THE PREPARATION OF SOLID DISPERSION OF LOPINAVIR AND RITONAVIR - An extrusion process for preparation of solid dispersion of lopinavir and ritonavir carried out in twin screw extruder. | 09-25-2014 |
20140315935 | GENE SIGNATURES FOR LUNG CANCER PROGNOSIS AND THERAPY SELECTION - The invention provides for molecular classification of disease and, particularly, molecular markers for lung cancer prognosis and therapy selection and methods and systems of use thereof. | 10-23-2014 |
20140315936 | APRICITABINE AND PI COMBINATION THERAPY - The present invention provides a method of treating HIV-1 infection in a subject. The method comprises administering to the subject a combination of anti-HIV-1 agents wherein the combination comprises an effective dose of Apricitabine and an effective dose of Atazanavir. | 10-23-2014 |
20140323507 | MYCOPHENOLIC ACID ANALOGUES AS ANTI-TUMOR CHEMOSENSITIZING AGENTS - In some embodiments, the present invention provides methods of treating a tumor in a subject. In some embodiments, the methods may include a step of administering to the subject a therapeutic composition that comprises: (a) mycophenolic acid, an analogue thereof, or a derivative thereof; and (b) at least one anti-neoplastic agent. In some embodiments, the antineoplastic agent may include at least one of 5-fluouracil (5-FU), paclitaxel, oxaliplatin, doxorubicin, etoposide, irinotecan, bleomycin, imiquimod, 13-cis-retinoic acid, and combinations thereof. In some embodiments, the relative concentrations of the mycophenolic acid, the analogue thereof, or the derivative thereof, and the at least one anti-neoplastic agent correspond to their respective IC50 values. In some embodiments, the methods of the present invention may be used to treat tumors associated with at least one of an oral cancer, a skin cancer, a breast cancer, a prostate cancer, precancerous lesions thereof, hyperplastic lesions thereof, and benign tumors thereof. | 10-30-2014 |
20140323508 | NOVEL COMPOUNDS - The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders. | 10-30-2014 |
20140336209 | NITROGEN-CONTAINING SIX-MEMBERED AROMATIC RING DERIVATIVES AND PHARMACEUTICAL PRODUCTS CONTAINING THE SAME - Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): | 11-13-2014 |
20140336210 | ARYL UREA COMPOUNDS IN COMBINATION WITH OTHER CYTOSTATIC OR CYTOTOXIC AGENTS FOR TREATING HUMAN CANCERS - This invention relates to aryl urea compounds in combination with cytotoxic or cytostatic agents for use in treating raf kinase mediated diseases such as cancer. | 11-13-2014 |
20140343084 | IMIDAZOPYRROLIDINONE COMPOUNDS - The invention relates to compounds of formula (I): | 11-20-2014 |
20140378490 | Formulations of Phenyl Uracil Compounds - A pharmaceutical product comprising at least one phenyl uracil-based pharmaceutically active agent or an agent of related structural type and processes for obtaining such product. | 12-25-2014 |
20140378491 | CYCLOALKYL-SUBSTITUTED PYRIMIDINEDIONE COMPOUNDS - The present invention provides novel cycloalkyl-substituted pyrimidine dione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease. | 12-25-2014 |
20140378492 | SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS - The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. | 12-25-2014 |
20150018377 | IMIDAZOLIDINEDIONE DERIVATIVES - The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy. | 01-15-2015 |
20150025094 | COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE - The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related dis | 01-22-2015 |
20150031714 | METHODS AND COMPOSITIONS FOR PREVENTION OF ALLERGIC REACTION - Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1′,2-dihydroxy-1,2′-binaphthalen-4′-yl)-4-methoxybenzenesulfonamide. | 01-29-2015 |
20150031715 | INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4 - The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4. | 01-29-2015 |
20150038522 | COMBINED ANTICANCER DRUG SENSITIVITY-DETERMINING MARKER - To provide an anti-cancer agent sensitivity determination marker, which marker can determine whether or not the patient has a therapeutic response to the anti-cancer agent, and novel cancer therapeutic means employing the marker. | 02-05-2015 |
20150045378 | AROMATIC RING COMPOUND - Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): | 02-12-2015 |
20150051233 | METHODS AND COMPOSITIONS FOR TREATMENT OF FIBROSIS - Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3. | 02-19-2015 |
20150051234 | THERAPY FOR COMPLICATIONS OF DIABETES - A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelia A (ET | 02-19-2015 |
20150057300 | SUBSTITUTED PIPERIDINES AS SODIUM CHANNEL BLOCKERS - The present disclosure provides substituted piperidines or pyrrolidines having Formula IA: | 02-26-2015 |
20150065531 | COMPOUNDS FOR USE IN CANCER THERAPY - Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds. | 03-05-2015 |
20150065532 | PYRIMIDINE CYCLOHEXYL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators. | 03-05-2015 |
20150073003 | NOVEL SYNTHETIC ANALOGS OF SPHINGOLIPIDS - The present invention provides new ceramide analogs indicated as the compounds of formula (II). These novel analogs exhibit a significant anti cancerous effect and are therefore provided as a pharmaceutical composition for treating cell proliferative diseases, neurodegenerative disorders, metabolism-associated conditions, infectious diseases, and immune-related disorders. The invention further provides combined compositions and kits combining the novel ceramide analogs of formula (II) with an additional therapeutic agent. | 03-12-2015 |
20150073004 | SUBSTITUTED B-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS - The present invention relates to compounds of formula 1 | 03-12-2015 |
20150080420 | AMORPHOUS FORM OF LOPINAVIR AND RITONAVIR MIXTURE - The present invention relates to a novel amorphous Form of lopinavir and ritonavir mixture in the ratio of 3.8:1.2 to 4.2:0.8, process for its preparation and pharmaceutical compositions comprising it. | 03-19-2015 |
20150111909 | DOSAGE FORM COMPRISING NON-CRYSTALLINE LOPINAVIR AND CRYSTALLINE RITONAVIR - The present invention relates to an oral dosage form comprising non-crystalline lopinavir and crystalline ritonavir. The invention further relates to methods of preparing said oral dosage forms containing the above pharmaceutical active agents. | 04-23-2015 |
20150111910 | TRIAZOLES AS KV3 INHIBITORS - Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders. | 04-23-2015 |
20150111911 | TREATING BAX(DELTA)2-POSITIVE CANCER WITH CHEMOTHERAPIES TARGETING CASPASE 8 - Discovery of a new Bax isoform, BaxΔ2, in cancer cell lines and primary tumors is described. The BaxΔ2 isoform resulted from combination of Bax microsatellite mutation and alternative splicing Bax exon 2. It is also discovered that BaxΔ2 renders cancer cells sensitive to certain chemotherapeutic drugs that target caspase 8. Also provided are methods for treating colorectal cancer by administering to a colorectal cancer patient a chemotherapeutic agent that is capable of activating caspase 8, wherein the patient contains a cancer cell that expresses a BaxΔ2 protein (SEQ ID NO. 2). | 04-23-2015 |
20150133477 | Methods for Reducing Uric Acid Levels Using Barbiturate Derivatives - Methods for reducing uric acid levels in blood or serum of a subject employing metabolites of merbarone as active agents. Methods for treating or preventing disorders of uric acid metabolism are also provided. The metabolites can be formulated as pharmaceutical compositions comprising the metabolites and a pharmaceutically acceptable carrier for use in these methods. | 05-14-2015 |
20150141447 | SOLID PREPARATION - The present invention provides a solid preparation excellent in disintegration property and preservation stability. The present invention relates to a solid preparation containing (1) 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile (compound (A)) or a salt thereof, (2) a saccharide, and (3) sodium stearyl fumarate. In addition, the present invention relates to a solid preparation containing (1) compound (A) or a salt thereof, (2) a saccharide, and (3) stearic acid or talc in a naked tablet part. | 05-21-2015 |
20150148359 | SELECTIVE INHIBITORS OF UNDIFFERENTIATED CELLS - Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells. | 05-28-2015 |
20150297526 | PHARMACEUTICAL COMPOSITION FOR TREATMENT OF HIV INFECTION - The invention is a pharmaceutical composition for the treatment of HIV infection; containing at least one HIV protease inhibitor as an active ingredient, as well as pharmaceutically acceptable excipients with a specific quantitative component ratio. Additionally, the invention belongs to the process of its production and to a treatment method. The inventive pharmaceutical composition has increased bioavailability and improved technological properties, such as durability, plasticity, disintegration, compared to the prototype drug. | 10-22-2015 |
20150313898 | COMPOUNDS THAT INHIBIT HUMAN DNA LIGASES AND METHODS OF TREATING CANCER - Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases. | 11-05-2015 |
20150313901 | COMPOSITIONS AND METHODS FOR TREATING AND PREVENTING DERMATOSES - The invention encompasses protectant agents including uracil or a metabolite thereof that effectively treat the cutaneous toxicities and dermatological side-effects associated with chemotherapeutic agents. Specifically, and surprisingly, the compositions of the invention including uracil or a metabolite thereof are effective for treating various dermatoses including atopic dermatitis, irritant contact dermatitis, radiation-induced dermatitis, dry skin dermatitis, papulopustular rashes, xerosis, pruritus, actinic keratosis, and genital warts. | 11-05-2015 |
20150315157 | PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) | 11-05-2015 |
20150322044 | PYRROLIDINE GPR40 MODULATORS - The present invention provides compounds of Formula (I): | 11-12-2015 |
20150342188 | 1-(SUBSTITUTED-BENZOYL)-5-FLUORO-4-IMINO-3-METHYL-3,4-DIHYDROPYRIMIDIN-2(1- H)-ONE DERIVATIVES - This present disclosure is related to the field of 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less. The present disclosure relates to 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-one compounds and their use as fungicides. The compounds of the present disclosure may offer protection against fungi and fungi like organisms including ascomycetes, basidiomycetes, deuteromycetes, and oomycetes. | 12-03-2015 |
20150353506 | N-(SUBSTITUTED)-5-FLUORO-4-IMINO-3-METHYL-2-OXO-3,4-DIHYDROPYRIMIDINE-1(2H- )-CARBOXAMIDE DERIVATIVES - This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-di-hydropyrimidine-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/746,837 filed Dec. 28, 2012, which is expressly incorporated by reference herein. Background and Summary of the Invention Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less. | 12-10-2015 |
20150359225 | 3-ALKYL-5-FLUORO-4-SUBSTITUTED-IMINO-3,4-DIHYDROPYRIMIDIN-2(1H)-ONE DERIVATIVES AS FUNGICIDES - This present disclosure is related to the field of 3-alkyl-5-fluoro-4-substituted-imino-3,4-5 dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Also provided are methods of controlling a fungal disease such as | 12-17-2015 |
20150366867 | METHODS OF TREATING ATHEROSCLEROSIS OR MYELOPROLIFERATIVE NEOPLASMS BY ADMINISTERING A LYN KINASE ACTIVATOR - This invention provides a method of treating a subject suffering from atherosclerosis or a myeloproliferative neoplasm which comprises administering to the subject an amount of a Lyn kinase activator effective to activate Lyn kinase so as to thereby treat the subject. | 12-24-2015 |
20150368207 | METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES - Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I: | 12-24-2015 |
20150368232 | LAMIVUDINE SALTS - The present disclosure relates to novel crystalline salt forms of lamivudine, methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of viruses such as Human Immunodeficiency Virus (HIV) infection. | 12-24-2015 |
20150376178 | Pyridinoylpiperidines As 5-HT1F Agonists - The present invention relates to compounds of formula I: | 12-31-2015 |
20150376180 | DIHYDROQUINOLINE-2-ONE DERIVATIVES - The invention provides novel compounds having the general formula (I) | 12-31-2015 |
20160017437 | MIR-193A-3P AND ASSOCIATED GENES PREDICT TUMORIGENESIS AND CHEMOTHERAPY OUTCOMES - The disclosure provides a correlation between the expression level of the miR-193a gene, which can be regulated by its methylation status, and both tumorigenesis of and the resistance of a cancer cell to a pyrimidine antimetabolite (5-FU) based chemotherapy. In addition to the methylation status and the expression of miR-193a, its downstream genes, such as E2F1, SRSF2, and apoptotic genes such as caspase 2, are also involved and can serve as useful markers for cancer therapy prognosis and for therapy selection. | 01-21-2016 |
20160022678 | THERAPEUTIC COMPOSITIONS CONTAINING MACITENTAN - The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having prostacyclin receptor (IP) agonist properties, or a pharmaceutically acceptable salt thereof. | 01-28-2016 |
20160031862 | CYCLOALKYL-SUBSTITUTED PYRIMIDINEDIONE COMPOUNDS - The present invention provides novel cycloalkyl-substituted pyrimidine dione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM) and conditions associated with left ventricular hypertrophy or diastolic dysfunction. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease. | 02-04-2016 |
20160045502 | THERAPEUTIC BENEFIT OF SUBOPTIMALLY ADMINISTERED CHEMICAL COMPOUNDS - The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to mustard-based alkylating agents such as uracil mustard and analogs, derivatives, or prodrugs thereof, including 6-methyluracil mustard and 6-ethyluracil mustard. | 02-18-2016 |
20160058737 | IMIDAZOLIDINEDIONE DERIVATIVES - The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy. | 03-03-2016 |
20160060226 | INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE - The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD | 03-03-2016 |
20160060229 | N-HYDROXYLAMINO-BARBITURIC ACID DERIVATIVES - The present disclosure provides N-hydroxylamino-barbituric acid compounds of formulae (1)-(4), pharmaceutical compositions and kits comprising them, and methods of using such compounds or pharmaceutical compositions. The present disclosure provides methods of using such compounds or pharmaceutical compositions for treating heart failure. | 03-03-2016 |
20160075689 | POLYMERASE, ENDONUCLEASE, AND HELICASE INHIBITORS AND METHODS OF USING THEREOF - Inhibitors of DNA damage polymerases, endonucleases, and helicases are provided. In particular, compounds comprising Formula (I) are described. | 03-17-2016 |
20160089370 | TREATMENT OR PREVENTION OF AUTISM DISORDERS USING MENTHOL, LINALOOL AND/OR ICILIN - Compositions for treatment or prevention of autism disorders are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Linalool, Icilin and combinations thereof. Methods for treatment or prevention of autism disorders are also provided, and the methods include administering such compositions. | 03-31-2016 |
20160095859 | COMBINATION THERAPIES FOR OVERCOMING RESISTANCE TO MITOTIC AGENTS DURING CHEMOTHERAPY - This disclosure relates to the uses of compounds that target an interaction between CHFR and PARP1. In certain embodiments, the disclosure relate to treating cancer by administering a mitotic inhibitor such as a taxane and a vinca alkaloid in combination with a compound that inhibits CHFR and PARP1 interactions, such as 5-((1-benzyl-1H-indol-3-yl)methylene)-1-(3,4-dimethylphenyl)pyrimidine-2,4,6(1H,3H,5H)-trione, derivatives or salts thereof, optionally in further combination with a third anti-cancer agent. | 04-07-2016 |
20160096843 | PYRAZOLO-PYRROLIDIN-4-ONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the pyrazolo-pyrrolidin-4-one derivatives, and their use as BET inhibitors for the treatment of conditions or diseases such as cancer. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 04-07-2016 |
20160106749 | FATTY LIVER DISEASE TREATMENT USING GLUCOCORTICOID AND MINERALOCORTICOID RECEPTOR ANTAGONISTS - The present invention provides treatment of fatty liver disease using a class of pyrimidinedione cyclohexyl compounds. | 04-21-2016 |
20160106849 | FORMULATIONS OF PHENYL URACIL COMPOUNDS - A pharmaceutical product comprising at least one phenyl uracil-based pharmaceutically active agent or an agent of related structural type and processes for obtaining such product. | 04-21-2016 |
20160108004 | TREATMENT OR PREVENTION OF NEURODEGENERATIVE DISORDERS USING MENTHOL, LINALOOL AND/OR ICILIN - Compositions for treatment or prevention of neurodegenerative disorders are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Linalool, Icilin and combinations thereof. Methods for treatment or prevention of neurodegenerative disorders are also provided, and the methods include administering such compositions. | 04-21-2016 |
20160108005 | TREATMENT OR PREVENTION OF DEPRESSION USING MENTHOL AND/OR ICILIN - Compositions for treatment or prevention of depression are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Icilin and combinations thereof. Methods for treatment or prevention of depression are also provided, and the methods include administering such compositions. | 04-21-2016 |
20160120980 | REGIONAL CANCER THERAPY - This invention relates to compositions and methods of treating cancers, and more particularly to regional delivery of cancer therapy compositions on surrounding internal tissues after surgery to remove or ablate cancer cells. The composition of the present invention can comprise an antineoplastic agent, such as, 5-Fluorouracil (“5-FU”) in an aqueous fluid, and a transcellular transport agent. An example of a composition of an embodiment of the present invention is 5-fluorouracil in an aqueous solution with polyethylene glycol and isopropanol. | 05-05-2016 |
20160130270 | FLUORINATED 3-(2-OXO-3-(3-ARYLPROPYL)IMIDAZOLIDIN-1-YL)-3-ARYLPROPANOIC ACID DERIVATIVES - The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described. | 05-12-2016 |
20160136163 | STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING A PYRIMIDINE-SULFAMIDE - The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof | 05-19-2016 |
20160145241 | STABLE CRYSTAL FORM OF TIPIRACIL HYDROCHLORIDE AND CRYSTALLIZATION METHOD FOR THE SAME - An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2θ±0.1°) in powder X-ray diffraction. | 05-26-2016 |
20160151371 | COMPOSITION FOR REGULATING IMMUNOLOGICAL ACTIVITY IN INTESTINE AND USE THEREOF | 06-02-2016 |
20160159755 | TETRAZOLINONE COMPOUND AND USE THEREOF - A tetrazolinone compound represented by formula (1): | 06-09-2016 |
20160166570 | TREATMENT OR PREVENTION OF NON-INFLAMMATORY NEURONAL DAMAGE FROM BRAIN TRAUMA AND STROKES USING MENTHOL, LINALOOL AND/OR ICILIN | 06-16-2016 |
20160185772 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 06-30-2016 |
20160192653 | N-(SUBSTITUTED)-5-FLUORO-4-IMINO-3-METHYL-2-OXO-3,4-DIHYDROPYRIMIDINE-1(2H- )-CARBOXYLATE DERIVATIVES | 07-07-2016 |
20160193197 | USE OF 6-HYDROXY-2-PYRIDONES AND DERIVATIVES THEREOF FOR PREPARING A PHARMACEUTICAL COMPOSITION THAT ACTS BY INHIBITING THE HUMAN URIDINE PHOSPHORYLASE ENZYME | 07-07-2016 |
20160194290 | DIHYDROPYRIMIDIN-2-ONE COMPOUNDS AND MEDICAL USE THEREOF | 07-07-2016 |
20160194303 | HETEROCYCLES CAPABLE OF MODULATING T-CELL RESPONSES, AND METHODS OF USING SAME | 07-07-2016 |
20160198711 | N-(SUBSTITUTED)-5-FLUORO-4-IMINO-3-METHYL-2-OXO-3,4-DIHYDROPYRIMIDINE-1(2H- )-CARBOXAMIDE DERIVATIVES | 07-14-2016 |
20180021336 | IMIDAZOLIDINEDIONE DERIVATIVES | 01-25-2018 |
20180021337 | SALT OF A PYRIMIDO[6,1-A]ISOQUINOLIN-4-ONE COMPOUND | 01-25-2018 |
20180022712 | NEGATIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 3 | 01-25-2018 |
20190144458 | ETHYNYL DERIVATIVES | 05-16-2019 |