42nd week of 2010 patent applcation highlights part 47 |
Patent application number | Title | Published |
20100267705 | PHARMACEUTICAL FORMULATION CONTAINING LIPOPHILIC DRUGS AND MILK AS A SOLUBILIZING/DISPENSING AGENT AND METHOD FOR THE PREPARATION THEREOF - The present invention relates to an improved pharmaceutical composition and in particular to a pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of a lipophilic active ingredient with milk as a solubilizing/dispersing agent and methods for the preparation thereof. | 2010-10-21 |
20100267706 | Compounds, Compositions and Methods Comprising Pyridazine Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1 or 2 or encompassed by formulas I, Ia, II, III, and IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2010-10-21 |
20100267707 | Tyrosine Kinase Inhibitors - The present invention relates to 4-indol-3-yl-N-phenylpyrimidin-2-amine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals. | 2010-10-21 |
20100267708 | GLUCOKINASE ACTIVATORS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT - The present invention relates to new compounds of formula (1) exhibiting excellent activity for glucokinase, and pharmaceutical compositions comprising the same as an active ingredient. | 2010-10-21 |
20100267709 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 2010-10-21 |
20100267710 | N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are compounds of the Formula I | 2010-10-21 |
20100267711 | METHOD OF ENHANCING CELLULAR PRODUCTION OF MOLECULAR CHAPERONE, HYDROXYLAMINE DERIVATIVES USEFUL FOR ENHANCING THE CHAPERONE PRODUCTION AND THE PREPARATION THEREOF - A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). | 2010-10-21 |
20100267712 | ISOINDOLINE COMPOUNDS FOR THE TREATMENT OF SPINAL MUSCULAR ATROPHY AND OTHER USES - Disclosed is a compound of Formula (I) in which W and R | 2010-10-21 |
20100267713 | 4,4-DISUBSTITUTED PIPERIDINES - The application relates to 4,4-disubstituted piperidines of the general formula (I) and their salts, preferably their pharmaceutically acceptable salts, in which R | 2010-10-21 |
20100267714 | MIF MODULATORS - The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression. | 2010-10-21 |
20100267715 | Polymorph Form II of Tanaproget - Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject. | 2010-10-21 |
20100267716 | METHODS OF TREATING INFLAMMATIONS AND INFECTIONS WITH PYRIDINIUM SALTS - Compounds of pyridinium salts and methods of their use in medicine, particularly in the prophylaxis and treatment of inflammatory conditions, infectious conditions, as well as immune disorders are disclosed. The present invention also relates to methods of controlling fungi and/or bacteria. | 2010-10-21 |
20100267717 | Novel Heterocyclic NF-kB Inhibitors - The present invention relates in one embodiment to compounds of formula (Ih) and/or a pharmaceutically acceptable salt thereof with an acid or a base, and/or a pharmaceutically acceptable prodrug and/or a stereoisomer thereof, | 2010-10-21 |
20100267718 | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them - The present invention relates to bicyclic heterocycles of general formula | 2010-10-21 |
20100267719 | Enhanced Indolinone Based Protein Kinase Inhibitors - Alpha-hydroxy-omega-(2-oxo-indolylidenemethyl-pyrrole-3′-carbonyl)amino alkanoic acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer. | 2010-10-21 |
20100267720 | Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate - The present invention relates to new crystalline forms of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]1H-indole-5-carbonitrile citrate, a Form D and a Form E, respectively, a process for their preparations, pharmaceutical formulations containing said compounds and to the use of said active compounds in therapy, and particularly to GSK3 related conditions and disorders. | 2010-10-21 |
20100267721 | Heterocyclic H3 Antagonists - Compound of formula (I) wherein W, X, Y, Z is —C(R′)═ or N; R | 2010-10-21 |
20100267722 | NOVEL PROLINE DERIVATIVES - The invention relates to a compound of formula (I) | 2010-10-21 |
20100267723 | Imidazole Substituted Pyrimidines - A compound of formula (I) | 2010-10-21 |
20100267724 | S-TRIAZOLE ALPHA-MERCAPTOACETANILIDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE - A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO | 2010-10-21 |
20100267725 | Compounds, Compositions and Methods Comprising 4N-Substituted Triazole Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or 2 or encompassed by formula I) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2010-10-21 |
20100267726 | 2-ARYL-ACETIC ACIDS, THEIR DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion. | 2010-10-21 |
20100267727 | PHARMACEUTICAL FORMULATIONS COMPRISING NEUROTROPHIN MIMETICS - Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75 | 2010-10-21 |
20100267728 | 3-SUBSTITUTED-1,2,3-TRIAZIN-4-ONE'S AND 3 SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES - This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment. | 2010-10-21 |
20100267729 | FUNGICIDAL HETEROCYCLIC AMINES - Disclosed are compounds of Formula 1, N-oxides, and salts thereof, | 2010-10-21 |
20100267730 | NOVEL COMPOUNDS - This invention relates to imidazopyridazine substituted piperidine derivatives and their use as pharmaceuticals. | 2010-10-21 |
20100267731 | USE OF TRANSFORMING GROWTH FACTOR-B RECEPTOR INHIBITORS TO SUPPRESS OCULAR SCARRING - A pharmaceutical composition useful in the prevention of subconjunctival scarring that may occur after GFS comprising an effective amount of an ALK-5 inhibitor. Also disclosed is a method of treating disorder or condition of other ocular scarring or fibrosis including corneal haze and PVR that may develop after ocular surgery or injury comprising applying an amount of a pharmaceutical composition including an ALK-5 inhibitor to a post-surgical or injury site. | 2010-10-21 |
20100267732 | Prognostic Molecular Markers for ET-743 Treatment - The present invention relates to the use of ecteinascidin 743 in human patients having certain molecular markers profile which has been associated with the outcome of ET-743 chemotherapy. In particular, the invention relates to the use of ecteinascidin 743 in patients having high expression levels of XPG mRNA or protein and/or having a “wild type” genotype for Asp1104His SNP of XPG gene. | 2010-10-21 |
20100267733 | Synergistic Modulation of Microglial Activation by Nicotine and THC - Treatment of microglial cells with nicotine and THC synergistically attenuate the microglial activation. Using microglial activation, the combination of THC and nicotine interact synergistically reduced LPS induced TNF-α release, showing that the combination of THC and nicotine clinically have greater efficacy in reducing neuroinflammation with less side effects than either drug given alone. CD40 signaling was found critically involved in pathological activation of microglial cells. This invention is also relevant to peripheral inflammation as well thru macrophages. In addition, other cannabinoids and other nicotinic-like medications currently in development are also covered under this discovery. | 2010-10-21 |
20100267734 | N-[(3,5-DICHLOROPHENYL)METHYL]-2-(4-METHYL-1-PIPERAZINYL)-2-(1-NAPHTHALENY- L)ETHANAMIDE AS GHRELIN RECEPTOR MODULATOR - The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, | 2010-10-21 |
20100267735 | METHODS AND COMPOSITIONS TO ENHANCE THE EFFICACY OF PHOSPHODIESTERASE INHIBITORS - Methods for treatment of sexual dysfunction in men and women using combination of phosphodiesterase (PDE) type 5 inhibitors and 1-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type5 inhibitors are also described. The methods comprise administering a therapeutically effect amount of 1-deprenyl or propargylamine compounds (also called monoamine oxidase [MAO] inhibitors) in combination with PDE inhibitors. Stimulation of nitric oxide production and vasodilation by 1-deprenyl and propargylamine compounds augments the actions of PDE inhibitors or other drugs and methods used in the treatment of sexual dysfunction. The composition described here enhances the actions of PDE inhibitors primarily by increasing the generation of cyclic GMP by stimulating the nitric oxide pathway and secondarily by providing several additional benefits such as enhanced dopamine activity. Methods of enhancing the efficacy of various PDE inhibitors in the treatment of a number of disorders other than sexual dysfunction are also disclosed. | 2010-10-21 |
20100267736 | METHODS AND COMPOSITIONS TO ENHANCE THE EFFICACY OF PHOSPHODIESTERASE INHIBITORS - Methods for treatment of sexual dysfunction in men and women using combination of phosphodiesterase (PDE) type 5 inhibitors and 1-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type5 inhibitors are also described. The methods comprise administering a therapeutically effect amount of 1-deprenyl or propargylamine compounds (also called monoamine oxidase [MAO] inhibitors) in combination with PDE inhibitors. Stimulation of nitric oxide production and vasodilation by 1-deprenyl and propargylamine compounds augments the actions of PDE inhibitors or other drugs and methods used in the treatment of sexual dysfunction. The composition described here enhances the actions of PDE inhibitors primarily by increasing the generation of cyclic GMP by stimulating the nitric oxide pathway and secondarily by providing several additional benefits such as enhanced dopamine activity. Methods of enhancing the efficacy of various PDE inhibitors in the treatment of a number of disorders other than sexual dysfunction are also disclosed. | 2010-10-21 |
20100267737 | 4-PHENYLPIPERAZINE DERIVATIVES WITH FUNCTIONALIZED LINKERS AS DOPAMINE D3 RECEPTOR SELECTIVE LIGANDS AND METHODS OF USE | 2010-10-21 |
20100267738 | NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF - The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids. | 2010-10-21 |
20100267739 | TREATMENT OF AFFECTIVE DISORDERS BY THE COMBINED ACTION OF A NICOTINIC RECEPTOR AGONIST AND A MONOAMINERGIC SUBSTANCE - The use of the combined action of a nicotinic acetylcholine receptor agonist and a monoaminergic substance for the treatment of affective disorders, as well as pharmaceutical compositions comprising these substances and chemical substances for use in such treatment. | 2010-10-21 |
20100267740 | Oxadiazole Derivatives and Their Use as Metabotropic Glutamate Receptor Potentiators - 842 - Compounds of Formula (I) wherein R | 2010-10-21 |
20100267741 | Compounds, Compositions and Methods Comprising Pyrazole Derivatives - The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas Ia, Ib, IIa, and IIb) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease. | 2010-10-21 |
20100267742 | COMBINATION TARGETED THERAPY FOR LUNG CANCER - A combination of compounds is described that target protein kinases and is more effective than the individual compounds against cancer where EGFR is upregulated and c-met is activated, for example, epithelial cell tumors, and particularly, non small cell lung carcinomas (NSCLC). | 2010-10-21 |
20100267743 | 3-(PHENOXYPYRROLIDIN-3-YL-METHYL)HETEROARYL, 3-(PHENYLPYRROLIDIN-3-YLMETHOXY)HETEROARYL, AND 3-(HETEROARYLPYRROLIDIN-3-YLMETHOXY)HETEROARYL COMPOUNDS - In one aspect, the invention relates to compounds of formula I: | 2010-10-21 |
20100267744 | Pharmaceutical Compositions - Forms and formulations of VX-950 and uses thereof. | 2010-10-21 |
20100267745 | 3-Pyridinecarboxamide Derivatives as HDL-Cholesterol Raising Agents - The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula | 2010-10-21 |
20100267746 | ALIPHATIC PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS WITH BETA AGONIST ACTIVITY - The present invention provides sodium channel blockers possessing beta-adrenergic receptor agonist activity. | 2010-10-21 |
20100267747 | 5-(Arylsulfonyl)-Pyrazolopiperidines - The invention provides N-cyclic sulfonamido compounds of Formula I | 2010-10-21 |
20100267748 | HETEROCYCLIC COMPOUNDS USEFUL AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 1H-pyrido[1,2-a]pyrimidin-4(9aH)-one derivatives or 1H-pyrimido[1,2-a]pyrimidin-4(9aH)-one derivatives for use as inhibitors of stearoyl-CoA desaturase having the structure of Formula I: | 2010-10-21 |
20100267749 | TRISUBSTITUTED FUROPYRIMIDINES AND USE THEREOF - The invention relates to the novel 4,5,6-trisubstituted furo[2,3-d]pyrimidine derivatives of formula (I), to methods for their production, their use in the treatment and/or prophylaxis of diseases and their use in the production of drugs for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases. | 2010-10-21 |
20100267750 | METHODS AND COMPOSITIONS FOR TREATING PAIN - The present application relates to compounds and methods for treating pain, incontinence and other conditions. | 2010-10-21 |
20100267751 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF TREATING DRY EYE DISORDERS - Inhibitors of Janus kinase-3 (“Jak3”) are useful for treating dry eye disorders and other disorders requiring the wetting of the eye. Jak3 inhibitors useful for treating eye disorders include the compound 3-{(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo [2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile. | 2010-10-21 |
20100267752 | 3-HYDROQUINAZOLIN-4-ONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS - The present invention discloses 3-hydroquinazolin-4-one derivatives for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cancer, cardiovascular disease, diabetes, obesity, metabolic syndrome and the like. | 2010-10-21 |
20100267753 | METHODS OF TREATING DISORDERS ASSOCIATED WITH PROTEIN KINASE CK2 ACTIVITY - The invention provides methods for the treatment or amelioration of disorders associated with undesired activity of protein kinase CK2, using compounds of Formula (I) | 2010-10-21 |
20100267754 | INTEGRIN EXPRESSION INHIBITOR - The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, | 2010-10-21 |
20100267755 | PYRIMIDINE DERIVATIVES - The invention provides the compounds of formula (I) | 2010-10-21 |
20100267756 | PHARMACEUTICAL PREPARATION FOR TREATING DEMYELINATING DISEASES OF THE NERVOUS SYSTEM; PREPARATION PROMOTING RESTORATION OF THE MYELIN SHEATH OF NERVE FIBERS; AND A METHOD FOR TREATING DEMYELINATING DISEASES OF THE NERVOUS SYSTEM - The invention relates to a pharmaceutical remedy used to treat demyelinating diseases of the nervous system, said remedy containing stephaglabrin sulfate that contributes to the restoration of the myelin sheath of nerve fibers, and to a method for treating demyelinating diseases of the nervous system. | 2010-10-21 |
20100267757 | AMINOTHIAZOLES AND THEIR USES - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 2010-10-21 |
20100267758 | PHARMACEUTICAL FORMULATION - Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided. | 2010-10-21 |
20100267759 | INHIBITORS OF Akt ACTIVITY - Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis. | 2010-10-21 |
20100267760 | Methods of and Combination Therapies for Treating or Delaying the Onset of Dyskinesia - Methods of treating or delaying onset of levodopa-induced dyskinesia in an individual comprise administering to the individual an effective amount of mammalian target of rapamycin (mTOR) inhibitor. Methods of treating or delaying onset of dyskinesia in an individual, wherein the dyskinesia is induced by administration of a drug causing abnormal protein expression in striatal medium-size spiny neurons (MSNs), comprise administering to the individual an effective amount of mTOR inhibitor. Further, a combination therapy for an individual having Parkinson's Disease comprises levodopa or a precursor or functional analogue thereof and mTOR inhibitor. | 2010-10-21 |
20100267761 | 7-Azaindole Derivatives as Selective 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors - The present invention relates to 7-azaindole derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions. | 2010-10-21 |
20100267762 | NOVEL P2X7R ANTAGONISTS AND THEIR USE - The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity. | 2010-10-21 |
20100267763 | Method of Decreasing Pro-ADAM10 Secretase and/or Beta Secretase Levels - The present invention provides a method of decreasing the level of pro-ADAM10 and/or BACE protein in a subject, the method comprising administering a heterocyclic compound or a pharmaceutically acceptable salt, hydrate or prodrug thereof to a subject in need thereof. | 2010-10-21 |
20100267764 | 8-Aza-Bicyclo[3.2.1]Octane Derivatives and Their Use as Monoamine Neurotransmitter Re-Uptake Inhibitors - This invention relates to novel 8-aza-bicyclo[3.2.1]octane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 2010-10-21 |
20100267765 | Pharmaceutical Compositions and Methods for CCR5 Antagonists - The present invention relates to a CCR5 antagonist compound for elevating high density lipoprotein (HDL) particles in a patient, improving plasma lipid profile in a patient or reducing triglycerides in a patient. The invention also relates to a pharmaceutical composition comprising a CCR5 antagonist compound, an HMG-CoA reductase inhibitor compound and a pharmaceutically acceptable carrier. The invention also relates to a pharmaceutical composition comprising a CCR5 antagonist compound, a cholesteryl ester transfer protein (CETP) inhibitor compound and a pharmaceutically acceptable carrier. | 2010-10-21 |
20100267766 | DERIVATIVES OF PYRROLIZINE, INDOLIZINE AND QUINOLIZINE, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to a compound of formula (I): | 2010-10-21 |
20100267767 | NUCLEAR RECEPTOR BINDING AGENTS - The present invention relates to methods for prevention and/or treatment of metabolic disorders, post-menopausal obesity and conditions associated with high fat diet consumption including, obesity, body weight gain, fat mass formation, bone mineral content reduction, white adipose tissue weight gain, increased cholesterol levels, increased leptin levels, insulin resistance, type II diabetes, increased blood glucose levels, inflammatory diseases, cardiovascular diseases, fatty liver condition (accumulation of fat in the liver), decreased uncoupling protein-1 (UCP-1) levels and increased lipogenesis. | 2010-10-21 |
20100267768 | PROCESS FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The invention provides a process for the preparation of a compound of Formula 1, | 2010-10-21 |
20100267769 | Substituted Bicyclocarboxyamide Compounds - This invention provides a compound of the formula | 2010-10-21 |
20100267770 | PIPERIDINE DERIVATIVES AND COSMETIC COMPOSITIONS THEREOF - The present invention provides piperidine derivatives of formula (I): | 2010-10-21 |
20100267771 | AUTOMATED IMMUNOSSAY APPARATUS WITH FLEXIBLE PICK-UP ARM - An automated sample handling apparatus is disclosed having a pipette mechanism ( | 2010-10-21 |
20100267772 | Combination of a Serotonin Reuptake Inhibitor and Agomelatine - The present invention relates to the use of a combination of agomelatine and a serotonin reuptake inhibitor (SRIs), or any other compound, which causes an elevation in the level of extracellular serotonin, for the treatment of depression and other affective disorders. | 2010-10-21 |
20100267773 | ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF - The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject. | 2010-10-21 |
20100267774 | P38 MAP KINASE INHIBITORS - Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: formula (I) wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R | 2010-10-21 |
20100267775 | OXADIAZOLIDINEDIONE COMPOUND - A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. | 2010-10-21 |
20100267776 | ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 2010-10-21 |
20100267777 | TREATMENT OF CANCERS WITH ACQUIRED RESISTANCE TO KIT INHIBITORS - The present invention provides compositions and uses thereof for treating cancers which have acquired resistance to a KIT inhibitor by administering effective amounts of DAST (4{4-[3-(4-chloro-3-trifluoromethylphenyf)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide.) | 2010-10-21 |
20100267778 | Diphenyl ether compound, process for producing the same, and use - The present invention relates to a compound represented by formula (I): | 2010-10-21 |
20100267779 | Novel Compounds and Methods of Using Them - Described herein are novel HDAC inhibitors, formulations containing them and methods of using them. In some embodiments, the HDAC inhibitors possess specific stereochemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders. | 2010-10-21 |
20100267780 | BICYCLIC ARYL AND HETEROARYL RECEPTOR MODULATORS - Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity. | 2010-10-21 |
20100267781 | NAPHTHALENE-BASED INHIBITORS OF ANTI-APOPTOTIC PROTEINS - Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: | 2010-10-21 |
20100267782 | SODIUM CHANNEL INHIBITORS - Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. | 2010-10-21 |
20100267783 | PHARMACEUTICAL COMPOSITION CONTAINING OPTICALLY ACTIVE COMPOUND HAVING THROMBOPOIETIN RECEPTOR AGONIST ACTIVITY, AND INTERMEDIATE THEREFOR - An optically active 4-phenylthiazole derivative having a thrombopoietin receptor agonist activity and a pharmaceutical composition containing the present compound as an active ingredient are created, and a platelet production regulating agent which can be orally administered is provided. | 2010-10-21 |
20100267784 | NOVEL 4,5-DIHYDROISOXAZOLES WITH ESTROGENIC ACTIVITY - This invention relates to novel 4,5-dihydroisoxazoles of formula (I), to their use as estrogen receptor modulators, and to methods of their preparation. | 2010-10-21 |
20100267785 | CANDESARTAN CILEXETIL - Candesartan cilexetil-containing granules which include a sugar alcohol and a binder and which are produced by granulation with an alcoholic granulating liquid. The granules are suitable for producing tablets in which the candesartan cilexetil is present in a form stabilized with regard to decomposition. | 2010-10-21 |
20100267786 | DUAL ACTING PHARMACEUTICAL COMPOSITIONS BASED ON SUPERSTRUCTURES OF ANGIOTENSIN RECEPTOR ANTAGONIST/BLOCKER (ARB) AND NE UTRAL ENDOPEPTIDASE (EP) INHIBITOR - Solid oral dosage forms, especially tablets, of a pharmaceutical composition comprising a supramolecular complex can be formed from a direct compression process or a compaction process such as roller compaction. Such solid oral dosage forms feature an immediate release profile that allows for fast release of the therapeutic agent. A particularly useful supramolecular complex is trisodium [3-((1S,3R)-1-biphenyl-4-ylmethyl-3-ethoxycarbonyl-1-butylcarbamoyl)propionate-(S)-3′-methyl-2′-(pentanoyl{2″-(tetrazol-5-ylate)biphenyl-4′-ylmethyl}amino)butyrate]hemipentahydrate. | 2010-10-21 |
20100267787 | Pharmaceutical Compositions - Provided are compositions comprising aqueous solutions of valsartan suitable for oral administration, preferably in pediatric and geriatric populations. Methods for making such compositions and methods for their stabilization are provided. | 2010-10-21 |
20100267788 | DUAL-ACTING ANTIHYPERTENSIVE AGENTS - The invention is directed to compounds of formula I: | 2010-10-21 |
20100267789 | TABLET FORMULATIONS COMPRISING VALSARTAN - The invention relates to solid oral dosage forms comprising pharmacologically effective amounts of valsartan or a pharmaceutically acceptable salt thereof or hydrate thereof. The compositions are at least 1.2 times more bioavailable than conventional valsartan capsule. | 2010-10-21 |
20100267790 | Method, Use and Agent for Protecting a Plant Against Phakopsora - The present invention relates to a method for protecting a plant against a phytopathogen selected from the genus | 2010-10-21 |
20100267791 | Method for Preventing Growth of Microorganisms, and a Combination for the Prevention of Microbial Growth - According to the invention, a method for the prevention of microbial growth in process waters is provided, wherein first a peracid compound, and thereafter a halogenated dialkyl hydantoin are dosed into said process water. Further, according to the invention, a combination for the prevention of microbial growth is provided, said combination comprising compounds to be dosed separately, said compounds being a peracid compound to be dosed first, and a halogenated dialkyl hydantoin to be dosed after the peracid compound, the weight ratio of the peracid compound to the halogenated dialkyl hydantoin being at least 2:1, wherein the amount of the peracid compound is calculated as active agent, while the amount of halogenated dialkyl hydantoin is calculated as active chlorine. | 2010-10-21 |
20100267792 | Topical Compositions Containing Desthiobiotin and its Derivatives and a Method of Treating Skin - Topical compositions and methods of use to treat symptoms of reduced skin elasticity are provided comprising desthiobiotin and certain desthiobiotin analogues. These compounds are effective in stimulating LOXL-1 activity and can thus increase elastin remodeling and improve appearance of fine lines, wrinkles, skin sagging and other symptoms of reduced elastin function. | 2010-10-21 |
20100267793 | METHOD OF TREATMENT USING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS - Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula | 2010-10-21 |
20100267794 | ANTI-FATIGUE AGENT COMPRISING AMINO ACID COMPOSITION - Conventional amino acid compositions are primarily intended to improve athletic performance or to promote fat-burning. Provided is an anti-fatigue agent which can prevent both of muscle fatigue and nerve strain concurrently. An anti-fatigue agent which comprises an amino acid composition composed of specific amino acids in specified amounts can prevent both of muscle fatigue and nerve strain concurrently. As for the types and the ratio of the amounts of the amino acids contained in the amino acid composition, the amino acid composition preferably contains 30 to 200 parts by weight of proline, 60 to 140 parts by weight of glycine, 50 to 260 parts by weight of alanine, 50 to 130 parts by weight of lysine, 30 to 75 parts by weight of tryptophan and 20 to 40 parts by weight of histidine, more preferably further comprises 3 to 75 parts by weight of tyrosine and 15 to 45 parts by weight of arginine, still more preferably further contains 30 to 55 parts by weight of valine, 35 to 60 parts by weight of leucine and 25 to 60 parts by weight of isoleucine. | 2010-10-21 |
20100267795 | NITROSUBSTITUTED ARYLOXYALKYLIMIDAZOLINES FOR USE AS PESTICIDES - The present invention relates to imidazoline derivatives and their use as insecticidal and acaricidal agents. The invention also extends to insecticidal and acaricidal compositions comprising such imidazoline derivatives, and to methods of using such derivatives and/or compositions to combat and control insect and acarine pests. In particular the present invention relates to phenoxy-imidazoline derivatives wherein the phenoxy moiety is substituted with a nitro group. A method of combating and/or controlling an insect or acarid pest, which comprises applying to said pest, or to the locus of said pest, or to a plant susceptible to attack by said pest, a compound of formula (I): or salt or N-oxide thereof. | 2010-10-21 |
20100267796 | THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME - The present invention provides a therapeutic agent for irritable bowel syndrome which comprises, as an active ingredient, a compound having an adenosine uptake inhibitory activity, a therapeutic agent for irritable bowel syndrome which comprises, as an active ingredient, a tricyclic compound represented by formula (I) | 2010-10-21 |
20100267797 | Use of Tetramic Acid Derivatives for Controlling Pests by Watering or Droplet Application - Compounds of the formulae (I) and (II) | 2010-10-21 |
20100267798 | PHARMACEUTICAL FORMULATIONS AND USE THEREOF IN THE PREVENTION OF STROKE, DIABETES AND/OR CONGESTIVE HEART FAILURE - The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF). | 2010-10-21 |
20100267799 | Orodispersible pharmaceutical composition of perindopril - The invention relates to a solid orodispersible pharmaceutical composition of perindopril, characterised in that it comprises perindopril or a pharmaceutically acceptable salt thereof and granules consisting of co-dried lactose and starch. | 2010-10-21 |
20100267800 | N-Alkyl-Hydroxamic Acid-Isoindolyl Compounds and Their Pharmaceutical Uses - The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4. | 2010-10-21 |
20100267801 | CYCLOHEXYL SULPHONES FOR TREATMENT OF CANCER - Sulphones of formula (I) are disclosed for use in treatment of cancer. | 2010-10-21 |
20100267802 | DELIVERY METHOD - The present invention relates, in general, to RNA silencing and, in particular, to a method of effecting targeted delivery of an RNA silencing moiety using a targeting moiety that binds to a cell surface receptor and mediates internalization of the RNA silencing moiety to be accessible to Dicer. Also provided is a chimeric nucleic acid molecule comprised of a targeting moiety and an RNA silencing moiety, wherein the targeting moiety is an aptamer and the RNA silencing moiety comprises a Dicer substrate. | 2010-10-21 |
20100267803 | Regulators Of Fat Metabolism As Anti-Cancer Targets - Embodiments of the invention provide methods of identifying agents that reduce or prevent the proliferation of breast cancer cells, or kill them, in particular by interfering with the expression of the transcription factors NR1D1 and PPARγ or the expression of genes whose transcription they activate or the activity of the proteins translated from those transcripts. | 2010-10-21 |
20100267804 | DIFFERENTIAL EXPRESSION OF MICRORNAS IN NONFAILING VERSUS FAILING HUMAN HEARTS - The present invention discloses specific miRNAs as novel biomarkers and therapeutic targets in the treatment of heart failure. Methods of treating or preventing heart failure in a subject by administering mimics or inhibitors of these particular miRNAs are disclosed. A method of diagnosing or prognosing heart failure in a subject by determining the level of expression of one or more miRNAs is also described. | 2010-10-21 |