51st week of 2010 patent applcation highlights part 50 |
Patent application number | Title | Published |
20100323999 | Therapeutic Molecules and Methods-1 - Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) as defined herein, is provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as part of a combination therapy. Novel heterocyclic compounds are also provided for. | 2010-12-23 |
20100324000 | DERIVATIVES OF 4-(2-AMINO-1-HYDROXYETHYL)PHENOL AS AGONISTS OF THE BETA2 ADRENERGIC RECEPTORS - The present disclosure relates to 4-(2-amino-1-hydroxyethyl)phenol derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the β2 adrenergic receptor. | 2010-12-23 |
20100324001 | Novel Methods for the Treatment of Inflammatory Diseases - Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for. | 2010-12-23 |
20100324002 | Inhaled combination therapy - There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery. | 2010-12-23 |
20100324003 | AMINOOXIME DERIVATIVES OF 2- AND/OR 4-SUBSTITUTED ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS - New aminooxime derivatives at position 3 of 2- and/or 4-substituted androstanes and androstenes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application. | 2010-12-23 |
20100324004 | Method for Treating Diabetes - This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes. | 2010-12-23 |
20100324005 | METHOD FOR TREATMENT OF DISEASES - The invention provides a method of inhibiting vascular hyperpermeability in an animal in need thereof. The method comprises administering a vascular-hyperpermeability-inhibiting amount of a danazol compound to the animal. The invention also provides a method of modulating the cytoskeleton of an endothelial cell in an animal. The method comprises administering an effective amount of a danazol compound to the animal. | 2010-12-23 |
20100324006 | HORMONE DELIVERY SYSTEM AND METHOD - A hormone delivery system and method are provided for administering bio identical human hormones using a combination of modalities for the treatment of human physiological conditions. | 2010-12-23 |
20100324007 | ORAL SUSPENSION OF PREDNISOLONE ACETATE - The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation. | 2010-12-23 |
20100324008 | PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING - Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them. | 2010-12-23 |
20100324009 | Substituted Sulfonamide Compounds - Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states. | 2010-12-23 |
20100324010 | AMIDE COMPOUNDS AND USE OF THE SAME - A renin inhibitor comprising a compound represented by the formula: | 2010-12-23 |
20100324011 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324012 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324013 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324014 | AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324015 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324016 | HETEROAROMATIC AND AROMATIC PIPERAZINYL AZETIDINYL AMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS - Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: | 2010-12-23 |
20100324017 | ACYLGUANIDINE DERIVATIVE - An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT | 2010-12-23 |
20100324018 | PHARMACEUTICAL COMPOSITIONS HAVING IMPROVED DISSOLUTION PROFILES FOR POORLY SOLUBLE DRUGS - Pharmaceutical compositions having improved dissolution profiles for drugs therein is disclosed. | 2010-12-23 |
20100324019 | Use of Riboflavin in the Treatment of Hypertension - The invention provides the use of riboflavin in the manufacture of a medicament for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism. The invention also provides a pharmaceutical product for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism, comprising a pharmaceutically effective amount of an anti-hypertensive agent and riboflavin, and the invention further provides a method of treatment of such a subject comprising the administration of riboflavin. | 2010-12-23 |
20100324020 | Bicyclic [3.1.0] Heteroaryl Amides As Type 1 Glycine Transport Inhibitors - The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R | 2010-12-23 |
20100324021 | (DIHYDRO)IMIDAZOISO[5,1-A]QUINOLINES - The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I | 2010-12-23 |
20100324022 | NOVEL COMPOUNDS - Compounds of formula (I), pharmaceutical compositions thereof, and methods for treatment using the same. | 2010-12-23 |
20100324023 | IMIDAZOBENZAZEPINE CGRP RECEPTOR ANTAGONISTS - Compounds of Formula I: I (where variables R | 2010-12-23 |
20100324024 | Quinolizidinone M1 Receptor Positive Allosteric Modulators - The present invention is directed to compounds of formula (I) (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2010-12-23 |
20100324025 | Antibacterial Agents - Antibacterial compounds of formula I are provided: | 2010-12-23 |
20100324026 | FUSED TRICYCLIC COMPOUNDS AS INHIBITORS OF TUMOR NECROSIS FACTOR-ALPHA - Compounds of formula 1: | 2010-12-23 |
20100324027 | DIAZAHOMOADAMANTANE DERIVATIVES AND METHODS OF USE THEREOF - The invention relates to compounds that are diazahomoadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions. | 2010-12-23 |
20100324028 | NOVEL COMPOUNDS - The present invention relates to new CGRP-antagonists of general formulae Ia and Ib | 2010-12-23 |
20100324029 | THERAPEUTIC AGENTS - The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed. | 2010-12-23 |
20100324030 | 5-Quinoline derivatives having an anti-bacterial activity - The present invention describes novel anti-bacterial compounds of the formula (I). | 2010-12-23 |
20100324031 | AQUEOUS PHARMACEUTICAL COMPOSITIONS CONTAINING BORATE-POLYOL COMPLEXES - The present invention is directed to the provision of multi-dose, ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP). The compositions include at two different polyols in conjunction with borate and a low concentration of benzalkonium chloride. | 2010-12-23 |
20100324032 | COMPOUNDS AND USES THEREOF IN MODULATING AMYLOID BETA - Novel compounds, compositions, and kits are provided. Methods of modulating Aβ levels, and methods of treating a disease associated with aberrant Aβ levels are also provided. | 2010-12-23 |
20100324033 | OXADIAZOANTHRACENE COMPOUNDS FOR THE TREATMENT OF DIABETES - The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, | 2010-12-23 |
20100324034 | Methods of Using SAHA for Treating HIV Infection - The present invention relates to pharmaceutical preparations and methods for treating individuals infected with the human immunodeficiency virus (HIV). The pharmaceutical preparations comprise SAHA and another anti-viral agent. The invention also relates to methods for treating HIV infected patients, particularly patients with persistent, latent HIV infection of CD4 | 2010-12-23 |
20100324035 | Carboxamide Compounds and Their Use - Chemokine receptor antagonists, in particular, compounds of Formula (I-A) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein. | 2010-12-23 |
20100324036 | SUBSTITUTED IMIDAZOPYRIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS - The present invention relates to substituted imidazopyridine derivatives as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin 4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression. | 2010-12-23 |
20100324037 | PHARMACOKINETICALLY IMPROVED COMPOUNDS - A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: | 2010-12-23 |
20100324038 | TETRAHYDROPYRIDOTHIOPHENES FOR THE TREATMENT OF PROLIFERATIVE DISEASES SUCH AS CANCER - The invention relates to compounds of formula I, wherein Ra is —C(O)OR1, in which R1 is 1-7C-alkyl, 3-7C-cycloalkyl, or 1-7C-alkyl substituted by one to four substituents independently selected from R2, Rb is -T-Q, in which T is 1-6C-alkylene or 3-7C-cycloalkylene, and either Q is optionally substituted by Rba and/or Rbb and/or Rbc, and is phenyl or naphthyl, or Q is optionally substituted by Rca and/or Rcb, and is Har, or Q is optionally substituted by Rda and/or Rdb, and is Het, or Q is optionally substituted by Rea and/or Reb, and is 3-7C-cycloalkyl, which are useful for the therapy of hyperproliferative diseases, in particular human cancer. | 2010-12-23 |
20100324039 | Substituted Indolealkanoic Acids - Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis. | 2010-12-23 |
20100324040 | 9-(PYRAZOL-3-YL)-9H-PURINE-2-AMINE AND 3-(PYRAZOL-3-YL) -3H-IMIDAZO[4,5-B] PYRIDIN-5- AMINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CANCER - The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer. | 2010-12-23 |
20100324041 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. Formula, (I). | 2010-12-23 |
20100324042 | HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS - The present invention relates to a heterocyclic compound of the general formula (I) | 2010-12-23 |
20100324043 | Bicyclic And Tricyclic Compounds As KAT II Inhibitors - Compounds of Formula X: | 2010-12-23 |
20100324044 | METABOTROPIC GLUTAMATE RECEPTOR ISOXAZOLE LIGANDS AND THEIR USE AS POTENTIATORS - Compounds in accord with Formula I: | 2010-12-23 |
20100324045 | CYCLIC UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih)1 (Ij), (Ik), (Il | 2010-12-23 |
20100324046 | 4-CARBOXYBENZYLAMINO DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo. | 2010-12-23 |
20100324047 | RAF KINASE MODULATORS AND METHODS OF USE - The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A | 2010-12-23 |
20100324048 | DISUBSTITUTED PHTHALAZINE HEDGEHOG PATHWAY ANTAGONISTS - The present invention provides novel 1,4-disubstituted phthalazine hedgehog pathway antagonists useful in the treatment of cancer. | 2010-12-23 |
20100324049 | DIARYL KETIMINE DERIVATIVE HAVING ANTAGONISM AGAINST MELANIN-CONCENTRATING HORMONE RECEPTOR - [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. | 2010-12-23 |
20100324050 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2010-12-23 |
20100324052 | NOVEL PIPERIDINE CARBOXYLIC ACID AMINE DERIVATIVES - The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin. | 2010-12-23 |
20100324053 | TRISUBSTITUTED 1,2,4 TRIAZOLES - The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). | 2010-12-23 |
20100324054 | AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES - The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved. | 2010-12-23 |
20100324055 | SOLID STATES FORMS OF VARENICLINE SALTS AND PROCESSES FOR PREPARATION THEREOF - Salts and crystalline forms of several salts of Varenicline, i.e., Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, methods of preparing the solid states of Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, and processes for preparing Varenicline base from those Varenicline salts are provided. | 2010-12-23 |
20100324056 | BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2010-12-23 |
20100324057 | THERAPEUTIC AGENT OR PROPHYLACTIC AGENT FOR INFLAMMATORY BOWEL DISEASE COMPRISING AMINO ALCOHOL DERIVATIVE AS ACTIVE INGREDIENT - A novel therapeutic agent or prophylactic agent for an inflammatory bowel disease is provided. An amino alcohol derivative represented by the general formula (1): | 2010-12-23 |
20100324058 | THROMBIN FUNCTION COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS BASED ON THEM - This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research. | 2010-12-23 |
20100324059 | PHARMACEUTICAL COMPOSITIONS USEFUL FOR TREATING HCV - This invention relates to combinations of Compound 1 and Compound 2 which are useful for treating hepatitis C virus infection. | 2010-12-23 |
20100324060 | PHARMACEUTICAL COMPOSITIONS USEFUL FOR TREATING HCV - This invention relates to combinations of Compound 1 and Compound 2 which are useful for treating hepatitis C virus infection. | 2010-12-23 |
20100324061 | ENANTIOMERICALLY PURE AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS - Enantiomerically pure compound of formula 1 | 2010-12-23 |
20100324062 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKKα, IR, JNK2α2, Lck, Met, MKK6, MST2, p70S6K, PDGFRα, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases. | 2010-12-23 |
20100324063 | JAK2 TYROSINE KINASE INHIBITION - The present invention provides methods for inhibiting JAK2 tyrosine kinase. Further, the present invention also provides methods of treating or preventing myeloproliferative disorders. | 2010-12-23 |
20100324064 | NOVEL ANALOGS OF CHOLINE FOR NEUROPROTECTION AND COGNITIVE ENHANCEMENT IN NEURODEGENERATIVE DISORDERS - The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected. Compounds according to the present invention are effective to alleviate and/or reverse the effects of a neurodegenerative condition, prevent further deterioration and/or enhance cognition and memory in patients suffering from neurodegenerative disorders, especially Alzheimer's disease. | 2010-12-23 |
20100324065 | Compounds and methods for development of Ret Modulators - Compounds active on Ret are described, as well as methods of using such compounds. Also described are crystal structures of Ret surrogates that were determined using X-ray crystallography. The use of such Ret surrogate crystals and structural information can, for example, be used for identifying molecular scaffolds and for developing ligands that bind to and modulate Ret and for identifying improved ligands based on known ligands. | 2010-12-23 |
20100324066 | CRYSTALLINE FORMS OF 4-[(2,4-DICHLORO-5-METHOXYPHENYL)AMINO]-6-METHOXY-7-[3-(4-METHYL-1-PIPERA- ZINYL)PROPOXY]-3-QUINOLINECARBONITRILE AND METHODS OF PREPARING THE SAME - This invention is directed to a crystalline 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 2θ angles (°) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33, 23.96, 24.95, 25.29, 25.84, 26.55, 27.61, and 29.51, and a transition temperature of about 109° C. to about 115° C. | 2010-12-23 |
20100324067 | TETRACYCLIC DIPYRANO-COUMARIN COMPOUNDS WITH ANTI-HIV AND ANTI-MYCOBACTERIUM TUBERCULOSIS ACTIVITIES - The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti- | 2010-12-23 |
20100324068 | CHEMICAL COMPOUNDS 785 - DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 2010-12-23 |
20100324069 | OXAZOLONE AND PYRROLIDINONE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2010-12-23 |
20100324070 | INDOLE, INDAZOLE AND BENZIMIDAZOLE ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS - Compounds of the formula I: | 2010-12-23 |
20100324071 | NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME - Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure | 2010-12-23 |
20100324072 | PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS - This invention relates to novel compounds having the structural formula I below: (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 2010-12-23 |
20100324073 | Pyrazolo [1,5-A] Pyrimidine Compounds - This invention relates generally to pyrazolo[1,5- | 2010-12-23 |
20100324074 | Protein Kinase Inhibitors - The present invention is directed to low molecular weight and orally bioavailable 3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the tyrosine kinase MET. The invention is also directed to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2010-12-23 |
20100324075 | THERAPEUTIC USE OF CARBOXYL ESTER LIPASE INHIBITORS - Compounds, pharmaceutical compositions, and their methods of use in raising serum HDL levels in subjects in need thereof are provided. Also provided are compounds, pharmaceutical compositions, and their methods of use in increasing reverse cholesterol transport in subjects in need thereof. Finally, methods for treating disease by raising serum HDL levels and increasing reverse cholesterol transport are provided. | 2010-12-23 |
20100324076 | Novel sEH Inhibitors and their Use - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 2010-12-23 |
20100324077 | COMBINATIONS OF ANILINOPYRIMIDINES AND PYRION COMPOUNDS - The present invention relates to combinations of an anilinopyrimidine, or a salt thereof, and a pyrion compound, or a salt thereof, which provide an improved biocidal effect. More particularly, the present invention relates to compositions comprising a combination of an anilinopyrimidine, or a salt thereof, selected from the group consisting of pyrimethanil, cyprodinil or mepanipyrim, together with a pyrion compound selected from 1-hydroxy-2-pyridinone, ciclopirox, ciclopirox olamine, piroctone, piroctone olamine, rilopirox, pyrion disulfide, sodium pyrithione and zinc pyrithione in respective proportions to provide a synergistic biocidal effect. Compositions comprising these combinations are useful for the protection of any living or non-living material, such as crops, plants, fruits, seeds, objects made of wood, thatch or the like, engineering material, biodegradable material and textiles against deterioration due to the action of microorganisms such as bacteria, fungi, yeasts, algae, virusses, and the like. | 2010-12-23 |
20100324078 | Crystalline Forms of Naltrexone Methobromide - The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions. | 2010-12-23 |
20100324079 | Medicament for prophylaxis and treatment of Alzheimer disease - A medicament effective for inhibiting onset of Alzheimer disease via intracellular aggregation mechanism is provided. A medicament for prophylaxis and treatment of Alzheimer disease comprising as an active ingredient apomorphine hydrochloride wherein cell death dependent upon intracellularly accumulated amyloid β proteins and/or p53 is inhibited; and/or wherein a level of intracellularly accumulated amyloid β proteins and/or phosphorylated tau proteins is lowered to improve energy production, protein metabolism and synaptic function of neurons so as to ameliorate the recognition capacity such as defects of memory. A medicament for prophylaxis and treatment of Alzheimer disease according to the present invention may allow for eradicative treatment of Alzheimer disease due to its inhibition of intracellular coagulation and accumulation of amyloid β proteins and intracellular activation of proteasome, and even prior to occurrence of massive neuronal death, may improve the function per se of neurons by reducing intracellularly accumulated amyloid β proteins to thereby contribute amelioration of the recognition function of Alzheimer disease patients. | 2010-12-23 |
20100324080 | Benzomorphan Compounds - The invention relates to Benzomorphan Compounds of Formula (I): wherein X, R | 2010-12-23 |
20100324081 | PREVENTIVE, INHIBITOR OR REMEDY FOR CEREBRAL ANEURYSM COMPRISING IBUDILAST AS AN ACTIVE INGREDIENT - Herein provided is an agent for the prevention of cerebral aneurysm, for the control of the formation thereof or for the treatment thereof, which comprises Ibudilast as an effective component. | 2010-12-23 |
20100324082 | ENANTIOMERIC COMPOSITIONS OF 2-AMINO-1-(2-ISOPROPYLPYRAZOLO[1,5-a]PYRIDIN-3-YL)PROPAN-1-ONE AND RELATED METHODS - Enantiomerically pure (S)-2-amino-1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one, (S)-AV1013, is a candidate therapeutic for treating neuroathic pain, addiction behavior and drug withdrawal symptoms. Also described are methods for preparing and using (S)-AV1013, its pharmaceutically acceptable salts as well as pharmaceutically acceptable formulations of the same. | 2010-12-23 |
20100324083 | Combinations of Organic Compounds - The invention provides a pharmaceutical combination comprising:
| 2010-12-23 |
20100324084 | UREA DERIVATIVES OF TROPANE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION - The present invention is related to a compound of formula (I) | 2010-12-23 |
20100324085 | AZABICYCLIC CARBAMATES AND THEIR USE AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The invention relates to novel benzothiophene-, benzofuran-, and indole ureas and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning, and/or memory. | 2010-12-23 |
20100324086 | COMPOUNDS AND METHODS - A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer. | 2010-12-23 |
20100324087 | COMBINED USE OF ANGIOGENESIS INHIBITOR AND TAXANE - The problems of the present invention are to find a pharmaceutical composition and a method for treating cancer that exhibit excellent anti-tumor effect. Excellent anti-tumor effect is achieved when 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, an analogous compound thereof, a pharmacologically acceptable salt thereof or a solvate thereof is used in combination with taxane. | 2010-12-23 |
20100324088 | Fused Pyridone M1 Receptor Positive Allosteric Modulators - The present invention is directed to fused pyridone compounds of formula (I) (I) that are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 2010-12-23 |
20100324089 | Anti-inflammatory composition - The invention relates to 3-(2′,2′-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and its use for preparing a medicament intended to prevent or treat inflammatory disorders. | 2010-12-23 |
20100324090 | COMPOSITIONS OF TOLPERISONE - The present disclosure is directed to methods for providing tolperisone having extremely low levels of 4-MMPPO (2-methyl-1-(4-methylphenyl)-propenone), as well as related compositions. The invention further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO, among other features. | 2010-12-23 |
20100324091 | Pyrazolone Derivative - A pyrazolone derivative represented by formula (I) below: | 2010-12-23 |
20100324092 | PYRIDYL AND PYRIMIDINYL DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS - The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the pyridyl and pyrimidinyl derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the pyridyl and pyrimidinyl derivatives vivo. | 2010-12-23 |
20100324093 | CCR9 INHIBITORS AND METHODS OF USE THEREOF - The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods. | 2010-12-23 |
20100324094 | Conformationally Restrained Epothilone Analogues as Anti-Leukemic Agents - A method for synthesizing anti-leukemic epothilone analogues includes rigidifying a region between the macrolactone ring and the aromatic side-chain. The anti-leukemic compositions are non-naturally occurring epothilone analogue that are rigidified between the macrolactone ring and the aromatic side-chain. | 2010-12-23 |
20100324095 | PHARMACEUTICAL COMPOSITION FOR INHIBITING AMYLOID-BETA PROTEIN ACCUMULATION - The present invention provides: a pharmaceutical composition for inhibiting amyloid-β protein accumulation comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient; a method for inhibiting amyloid-β protein accumulation, comprising a step of administering an effective amount of the compound of the formula (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-β protein-related disease; and so on. | 2010-12-23 |
20100324096 | Whitening Agent And Skin External Preparation - The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof: | 2010-12-23 |
20100324097 | Method of Providing Pirfenidone Therapy to a Patient - The invention relates to methods for decreasing adverse events associated with pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. The invention discloses an optimized dose escalation scheme that results in the patient having increased tolerance to adverse events associated with the administration of pirfenidone. The invention also discloses a starter pack that may be used in conjunction with the dose escalation scheme. | 2010-12-23 |
20100324098 | SUSTAINED RELEASE AMINOPYRIDINE COMPOSITIONS - A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases. | 2010-12-23 |
20100324099 | SUSTAINED RELEASE AMINOPYRIDINE COMPOSITIONS - A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases. | 2010-12-23 |