03rd week of 2010 patent applcation highlights part 49 |
Patent application number | Title | Published |
20100016286 | Anti-Inflammatory Agents - The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T | 2010-01-21 |
20100016287 | COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF" - Compounds of formula (I) | 2010-01-21 |
20100016288 | MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF - Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases. | 2010-01-21 |
20100016289 | Compounds Useful as Antagonists of CCR2 - The present invention provides compounds of general formula I: (I) or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R | 2010-01-21 |
20100016290 | AMORPHOUS POLYMORPH OF BAZEDOXIFENE ACETATE - The invention provides a novel polymorphic form C of bazedoxifene acetate, methods of preparing the polymorphic form, and compositions and methods of treatment using the polymorphic form. | 2010-01-21 |
20100016291 | MTP INHIBITING TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID DERIVATIVES - The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes. Formula (I). | 2010-01-21 |
20100016292 | INHIBITORS OF LETHAL FACTOR PROTEASE - The invention provides compounds that can efficiently and specifically inhibit bacterial toxins, such as inhibit the lethal factor (LF) protease activity of anthrax toxin and/or botulinum neurotoxin type A. The invention also provides methods for inhibiting proteases, such as lethal factor protease, as well as methods for treating bacterial infections, such as anthrax and botulinum. | 2010-01-21 |
20100016293 | Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use - Compounds that interact with the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of formula (I) wherein Q is CR | 2010-01-21 |
20100016294 | METHODS FOR REDUCING THE RISK OF AN ADVERSE DRUG INTERACTION IN A PATIENT SUFFERING FROM INSOMNIA - Disclosed herein is a method for treating a patient with Quazepam that reduces the risk of an adverse interaction between the Quazepam and drug that is a substrate of the cytochrome P450 enzyme isoform 2B6 (CYP2B6 substrate drug), e.g., Bupropion. The method includes determining if the patient to be treated with Quazepam is being treated with a CYP2B6 substrate drug, and prescribing or treating the patient with Quazepam based on the determination. | 2010-01-21 |
20100016295 | Preparation and Use of Biphenyl Amino Acid Derivatives for the Treatment of Obesity - This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases. | 2010-01-21 |
20100016296 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2010-01-21 |
20100016297 | ALKYL-SUBSTITUTED 3' COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 2010-01-21 |
20100016298 | Theramutein modulators - This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein. | 2010-01-21 |
20100016299 | Substituted benzoxepino-isoxazoles and use thereof - The present application relates to novel substituted benzoxepinoisoxazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis, restenosis and ischemias. | 2010-01-21 |
20100016300 | Imidazoacridine Compounds for Treating FLT3-Mediated Disorders - A method of treating a FLT3-mediated condition in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I), The conditions that can be treated by the compounds of the present invention and the definitions for the variables in formula (I) are provided herein. | 2010-01-21 |
20100016301 | Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyridine and 6-Phenyl-imidazo[1,2-b]pyridazine derivatives according to generic Formulae I-V: | 2010-01-21 |
20100016302 | Inhibitors of bruton's tyrosine kinase - This application discloses 6-Phenyl-imidazo[1,2-a]pyrazine derivatives according to generic Formulae I-V: | 2010-01-21 |
20100016303 | NOVEL PHENYLIMIDAZOLE DERIVATIVES AS PDE10A ENZYME INHIBITORS - This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. | 2010-01-21 |
20100016304 | GLUCOKINASE ACTIVATOR - A compound represented by the following formula (1): | 2010-01-21 |
20100016305 | novel use of activators and stimulators of soluble guanylate cyclase for the prevention or treatment of renal disorders - The present invention relates generally to a method for the treatment of renal failure or renal hypertension and, more particularly, for improving the recovery from acute renal failure or renal hypertension by treatment with activators of soluble guanylate cyclase or stimulators of guanylate cyclase. | 2010-01-21 |
20100016306 | PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS - Thienopyrimidines of formula (Ia) or (Ib): | 2010-01-21 |
20100016307 | NOVEL COMPOUNDS - The present invention relates to compounds of formula (I): | 2010-01-21 |
20100016308 | Tetrahydroindole Derivatives for Treatment of Alzheimer's Disease - Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease. | 2010-01-21 |
20100016309 | 1,2,3,4-Tetrahydroisoquinoline Derivatives, Preparation Process therefor and Pharmaceutical Composition Containing the Same - The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I): | 2010-01-21 |
20100016310 | METHODS OF USING ARYL SULFONYL COMPOUNDS EFFECTIVE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are methods of using soluble epoxide hydrolase (sEH) inhibitors for treating diseases related to cardiovascular disease. | 2010-01-21 |
20100016311 | NOVEL MINOR GROOVE BINDERS - There is provided compounds of formula (I), wherein R | 2010-01-21 |
20100016312 | Substituted indolyl and indazolyl derivatives and uses thereof - This application discloses compounds of generic Formula I: | 2010-01-21 |
20100016313 | INTESTINAL ALKALINE PHOSPHATASE MODULATORS AND USES THEREOF - Disclosed are modulators, i.e., activators and inhibitors, of Intestinal Alkaline Phosphatase (IAP). Also disclosed are methods for treating bacterial infections of the intestinal tract and methods for maintaining the health of the intestinal tract using IAP activators. Further disclosed are methods to assist in weight gain of emaciated patients and those having reduced or negligible fat absorption using IAP inhibitors. | 2010-01-21 |
20100016314 | DERIVATIVES OF AZABICYCLO OCTANE, THE METHOD OF MAKING THEM AND THE USES THEREOF AS INHIBITORS OF DIPEPTIDYL PEPTIDASE IV - Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions. | 2010-01-21 |
20100016315 | Iminopyridine Derivative and Use Thereof - Provided are an iminopyridine derivative having a selective α | 2010-01-21 |
20100016316 | ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I) or (II): | 2010-01-21 |
20100016317 | HIV INHIBITING 6-SUBSTITUTED PYRIMIDINES - HIV replication inhibitors of formula | 2010-01-21 |
20100016318 | ANTHRANILAMIDE INHIBITORS OF AURORA KINASE - The present invention relates to a compound represented by the following formula: | 2010-01-21 |
20100016319 | ARYLMETHYLENE UREA DERIVATIVE AND USE THEREOF - This invention relates to a pharmaceutical comprising as an effective ingredient an arylmethylene urea exemplified by the following formula: | 2010-01-21 |
20100016320 | ARYL-SUBSTITUTED PYRAZOLE-AMIDE COMPOUNDS USEFUL AS KINASE INHIBITORS - The present invention relates to compounds having the formula, | 2010-01-21 |
20100016321 | DERIVATIVES OF ISOTHIAZOL-3(2H)-ONE 1,1-DIOXIDES AS LIVER X RECEPTOR MODULATOR - The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 2010-01-21 |
20100016322 | Water Dispersible Pharmaceutical Formulation and Process for Preparing The Same - Water dispersible compressed tablets and a process for preparing the same. The tablet comprising about 0.1 to 50% w/w of lamotrigine or its pharmaceutically acceptable salts, solvates, hydrates or polymorphs, about 5 to about 50% w/w of a water-soluble diluent(s), about 15 to about 70% w/w of a water swellable diluent(s), optionally one or more pharmaceutically acceptable adjuvants, wherein the ratio of water-soluble diluent(s) to water swellable diluents(s) is from about 0.6 to about 0.9 and said composition is essentially free of disintegrant, superdisintegrant and swellable clay. | 2010-01-21 |
20100016323 | 2-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS - The application claims a compound of the formula | 2010-01-21 |
20100016324 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF CELLULITE - There are disclosed pharmaceutical compositions for topical administration or for use in mesotherapy, containing a PDE3 inhibitor as active ingredient, and their use in the treatment of cellulite. | 2010-01-21 |
20100016325 | TETRAHYDROCINNOLINE DERIVATIVES - Provided herein are compounds of formula (I): | 2010-01-21 |
20100016326 | CONCENTRATED METHOTREXATE SOLUTIONS - Concentrated methotrexate solutions are described which are suitable for the use of an active substance in the production of a parenterally administered medicament for the treatment of inflammatory autoimmune diseases. The methotrexate is added to a pharmaceutically acceptable solvent at a concentration of more than 25 mg/ml. The invention also relates to a ready-made syringe and a carpule containing such a pharmaceutical solution formulation, as well as a pen injector comprising such a carpule and/or a ready-made syringe. | 2010-01-21 |
20100016327 | QUINOLINE COMPOUNDS - [Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. | 2010-01-21 |
20100016328 | PTERIN ANALOGS - Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by administration of the analog. These analogs are contemplated for use wherever tetrahydrobiopterin is currently used to treat conditions responsive to tetrahydrobiopterin therapies. | 2010-01-21 |
20100016329 | XANTHINE-BASED CYCLIC GMP-ENHANCING RHO-KINASE INHIBITOR INHIBITS PHYSIOLOGICAL ACTIVITIES OF LUNG EPITHELIAL CELL LINE - The present invention provides a pharmaceutical composition including a compound of 7-[2-[4-(2-chlorophenyl)piperazinyl]-ethyl]-1,3-dimethylxanthine (KMUP-1), wherein the compound is a Rho-kinase inhibitor, and the pharmaceutical composition inhibits a physiological activity of a lung epithelial cell. | 2010-01-21 |
20100016330 | Novel Derivatives - The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca | 2010-01-21 |
20100016331 | NOVEL COMPOUNDS - The present invention provides compounds of formula (I): | 2010-01-21 |
20100016332 | POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE - The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine, crystaline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl) butyl]-4-(2-carbomyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation. | 2010-01-21 |
20100016333 | Once-a-day (RNA-Polymerase Inhibiting or phenazine) - dihydropteroate synthase inhibiting - dihydrofolate reductase inhibiting antibiotic pharmaceutical product, formulation thereof, and use thereof in treating infection caused by Methicillin-Resistant Staphylococcus aureus - Disclosed are once-a-day antibiotic products for treating Methicillin-Resistant | 2010-01-21 |
20100016334 | PHARMACEUTICAL FORMULATIONS CONTAINING DOPAMINE RECEPTOR LIGANDS - The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described. | 2010-01-21 |
20100016335 | NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION - The present invention relates to a compound of formula I: | 2010-01-21 |
20100016336 | HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE - The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-β) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-β) inhibitors, and to methods for regulating angiogenesis. | 2010-01-21 |
20100016337 | HETEROARYL-SUBSTITUTED CARBOXAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to heteroaryl-substituted carboxamides of the formula I, | 2010-01-21 |
20100016338 | 5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1-arylquinolin-2-ones, a Process for their Production and their Use as Anti-inflammatory Agents - The present invention relates to compounds of formula I, | 2010-01-21 |
20100016339 | FUNGICIDAL COMPOUNDS AND COMPOSITIONS - The present invention relates, inter alia, to a compound having the formula (I):—wherein (R)n is selected from the group consisting of 4-Br, 4-OCH | 2010-01-21 |
20100016340 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds of the formula (I): | 2010-01-21 |
20100016341 | ASPARTYL PROTEASE INHIBITORS CONTAINING A TRICYCLIC RING SYSTEM - Disclosed are compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof or wherein R | 2010-01-21 |
20100016342 | SOLID FORMS COMPRISING 3-(2,5-DIMETHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, COMPOSITIONS COMPRISING THE SAME, AND METHODS OF USING THE SAME - Provided herein are solid forms comprising 3-(2,5-dimethyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione. Pharmaceutical compositions comprising the solid forms and methods for treating, preventing and managing various disorders are also disclosed. | 2010-01-21 |
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. | 2010-01-21 |
20100016344 | AMINO HETEROCYCLIC LINKED PYRIMIDINE DERIVATIVES - Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein. | 2010-01-21 |
20100016345 | PYRIMIDINYL SULFONAMIDE COMPOUNDS WHICH INHIBIT LEUKOCYTE ADHESION MEDIATED BY VLA-4 - Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis. | 2010-01-21 |
20100016346 | ELASMOBRANCH-REPELLING DOMPOUNDS AND METHODS OF USE - Compounds for repelling elasmobranch having an aldehyde or derivative, a carboxylic acid a derivative, a ketone or a derivative thereof, a di-ketone or a derivative thereof, a pyridine or derivative thereof, or an antipyrine or a derivative thereof and methods of use thereof. | 2010-01-21 |
20100016347 | SERIES OF SKIN WHITENING (LIGHTENING) COMPOUNDS - The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin. | 2010-01-21 |
20100016348 | ORALLY DISINTEGRATIVE DOSAGE FORM - The present invention features an orally disintegrating dosage form including from about 5% to about 40%, by weight, of at least one hydrated salt and a pharmaceutically active agent, wherein the at least hydrated salt has a dehydration temperature of from about 20 to about 120° C. | 2010-01-21 |
20100016349 | PSEUDOAZULENYL NITRONES - Disclosed herein are pseudoazulenyl nitrone compounds and methods of using these compounds to trap free radicals and to treat, prevent, or ameliorate various diseases associated with free radicals. | 2010-01-21 |
20100016350 | NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R | 2010-01-21 |
20100016351 | NICOTINIC ALPHA-7 RECEPTOR LIGANDS AND PREPARATION AND USES THEREOF - The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds which act as ligands for the α7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof. | 2010-01-21 |
20100016352 | COMPOUNDS AND METHODS FOR TREATING ESTROGEN RECEPTOR-RELATED DISEASES - Provided herein in certain embodiments are compounds, pharmaceutical compositions and methods for modulating the functions of estrogen receptor alpha 36, for preventing and/or treating diseases mediated by estrogen receptor alpha 36, for preventing and/or treating osteoporosis, for inducing cell death and/or inhibiting cell proliferation and for preventing and/or treating diseases involving abnormal cell proliferation such as cancers. | 2010-01-21 |
20100016353 | BENZOIMIDAZOLE DERIVATIVES USEFUL AS ANTIPROLIFERATIVE AGENTS - The invention relates to substantially pure compounds of the formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R, R | 2010-01-21 |
20100016354 | NOVEL OXADIAZOLE DERIVATIVES AND THIADIAZOLE DERIVATIVES HAVING NEOVASCULARIZATION INHIBITORY ACTIVITY - The present invention relates to Compounds represented by the formula (I) or salts thereof. In the formula (I), the ring A represents a benzene ring, a thiophene ring, or a pyridine ring; R | 2010-01-21 |
20100016355 | ALPHA-2B ADRENERGIC RECEPTOR AGONIST AND SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITOR COMPOSITIONS FOR TREATING CHRONIC PAIN - Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed. | 2010-01-21 |
20100016356 | METHOD FOR TREATING THROMBOSIS AND INHIBITING PLATELET AGGREGATION WITH 21-(S)-ARGATROBAN - A method for inhibiting coagulation including administering to a patient in need thereof a pharmaceutical composition having 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for inhibiting coagulation having 21-(S)-Argatroban and/or a pharmaceutically acceptable salt thereof. Compared with 21 (R) Argatroban, 21-(S)-Argatroban significantly prolongs coagulation time of whole blood (CT), recalcification time (RT), kaolin partial thromboplastin time (APTT), pro-time prothrombin time (PT), thrombin time (TT), and reduces platelet adhesion rate and platelet aggregation rate in healthy dogs. Therefore, 21-(S)-Argatroban has a stronger effect of inhibiting coagulation and reducing therapeutically effective dose and is suitable for treatment and/or prevention of thrombosis and inhibiting platelet aggregation. | 2010-01-21 |
20100016357 | Use of Beta-Aminoalcohols for the Treatment of Inflammatory Disorders and Pain - Compounds that may be used for the treatment or prevention of a condition associated with T-cell proliferation or that is mediated by pro-inflammatory cytokines are of formula (I): wherein at least one of R1, R2 or R3 is not H and each is independently H, alkyl, CF | 2010-01-21 |
20100016358 | GAMMA-GLOBIN INDUCER - The present invention is directed to a γ-globin inducer, to a prophylactic and/or therapeutic agent for sickle cell disease, and to a prophylactic and/or therapeutic agent for β-thalassemia, each containing, as an active ingredient, 4-[N-(4-methoxyphenyl)-N-[[5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]methyl]amino]-1-[[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl]piperidine, a salt thereof, or a solvate of either of these. | 2010-01-21 |
20100016359 | METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY - The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses. | 2010-01-21 |
20100016360 | 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. | 2010-01-21 |
20100016361 | ARYL CARBOXYLIC ACID CYCLOHEXYL AMIDE DERIVATIVES - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: (I) wherein the variants R and X are defined in the specification. | 2010-01-21 |
20100016362 | STABILIZED PHARMACEUTICAL COMPOSITION CONTAINING DONEPEZIL, PROCESS OF PRODUCING SAME AND METHOD FOR STABILIZATION - An object of the present invention is to provide a novel pharmaceutical composition containing donepezil, which is already used as a remedy for the treatment of dementia (cognitive impairment), in order to increase options for administration methods and improve patient compliance. The present invention provides a pharmaceutical composition containing donepezil or a pharmaceutically acceptable salt thereof and a naturally-occurring polymer, the pharmaceutical composition further containing at least one of edetate, sulfite, dibutylhydroxytoluene and butylhydroxyanisole. | 2010-01-21 |
20100016363 | Fixed Combination Dosage Forms for the Treatment of Migraine - Therapeutic regimens and dosage forms are disclosed for the treatment of migraine headache. The regimens preferably combine a serotonin receptor agonist, such as sumatriptan, eletriptan or almotriptan, with a fast acting formulation of diclofenac potassium. | 2010-01-21 |
20100016364 | METHOD OF PREDICTIVE DETERMINATION OF RESPONSIVENESS TO PHARMACOLOGICAL INTERVENTION - A diagnostic test for determining the efficacy of 5HT | 2010-01-21 |
20100016366 | Novel Compounds Active as Muscarinic Receptor Antagonists - The invention relates to compounds of formula | 2010-01-21 |
20100016367 | BIS-PYRINIDIUM COMPOUNDS - A method of treating, inhibiting, or preventing an infection in a subject is described. The method comprises administering to the subject an effective amount of at least one bis-pyridinium compound. The bis-pyridinium compound comprises two aromatic ring structures. Each of the ring structures comprises a pyridine ring, and the ring structures are linked by a linker group of at least 8 atoms in length, said linker group being attached to the nitrogen atoms of the pyridine rings. At least one substituent on at least one of the ring structures is an alkyl group having at least 2 carbon atoms, and no substituent on either of the ring structures is —OH, —SH or an amine group. | 2010-01-21 |
20100016368 | AMINOTETRAHYDROINDAZOLOACETIC ACIDS - The invention is concerned with the compounds of formula I: | 2010-01-21 |
20100016369 | AMINOTETRAHYDROINDAZOLOACETIC ACIDS - The invention is concerned with the compounds of formula I: | 2010-01-21 |
20100016370 | PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE MAGNESIUM IN A STABLE FORM - There is provided a process for preparing purified esomeprazole magnesium, comprising the steps of: providing esomeprazole magnesium; contacting said esomeprazole magnesium with a non-solvent comprising an aqueous component up to a maximum content defined by water saturation in the non-solvent; and recovering purified esomeprazole magnesium formed from the contacting step. The process is particularly suitable to obtain esomeprazole magnesium dihydrate, especially form A. The esomeprazole magnesium obtained is remarkably pure, stable and is resistant to form interchangeability. | 2010-01-21 |
20100016371 | Indole Compounds - The present application relates to compounds of formula (I) or a pharmaceutically acceptable derivative thereof; wherein X, R | 2010-01-21 |
20100016372 | Benzimidazole Derivatives - Novel compounds of the formula I (I), in which R | 2010-01-21 |
20100016373 | IMIDAZOLE CARBOXAMIDES - The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same and processes for preparing the same. | 2010-01-21 |
20100016374 | Compounds Which Inhibit the Glycine Transporter and Uses Thereof - Compounds of formula (I) and salts and solvates are provided: | 2010-01-21 |
20100016375 | 1,5-DIPHENYL-3-PYRIDINYLAMINO-1,5-DIHYDROPYRROLIDIN-2-ONE AS CB1 RECEPTOR MODULATOR - Compound and pharmaceutical compositions of Formula by blockade of the CB | 2010-01-21 |
20100016376 | CASPASE INHIBITORS BASED ON PYRIDONE SCAFFOLD - The present invention relates to a pyridone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same. | 2010-01-21 |
20100016377 | Use of a p38 Kinase Inhibitor for Treating Psychiatric Disorders - The use of 6-(S-Cyclopropylcarbamoyl-S-fluoro-2-methyl-phenyl)-N-(2,2-dimethylproyl)-nicotinamide, which is known in the art as a p38 kinase inhibitor in the treatment or prophlaxis of one or more psychiatric disorders. | 2010-01-21 |
20100016378 | Method of preventing dihydropyridine compound from degradation - As the addition of water to dihydropyridine compounds such as amlodipine accelerates their degradation into the pyridine form, either immediately or following the formation of unstable hydrates, methods for producing pharmaceutical compositions that contain dihydropyridine compounds are limited to methods in which no water is added, such as methods in which dihydropyridine compounds are added in the form of powder, but these methods are unsuitable for wet granulation in which tablet moldability, hardness, disintegration, or the like can be readily adjusted and the homogeneity of the ingredients can be readily ensured by modifying the granulating conditions. According to the present invention, the co-presence of a methylated cellulose-based polymer during wet processing of dihydropyridine compounds prevents the formation of dihydropyridine compound hydrates and/or the degradation of the dihydropyridine compounds. | 2010-01-21 |
20100016379 | Terephthalamate Compounds and Compositions, and Their Use as HIV Integrase Inhibitors - Described herein are compounds having a terephthalamate structural feature. Also described herein, are methods of making such compounds, methods of using such compounds to modulate the activity of HIV integase, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology of AIDS or infection with HIV. | 2010-01-21 |
20100016380 | TNF-alpha production inhibitors - A compound having the following formula | 2010-01-21 |
20100016381 | STABLE EMULSION COMPOSITION - The present invention provides an emulsion composition comprising (A) a compound stable in an acidic range, and (B) a buffer, wherein the pH is adjusted from about 3.7 to about 5.5. | 2010-01-21 |
20100016382 | PHARMACEUTICAL COMPOSITION - The present invention provides a solid pharmaceutical composition superior in the stability and dissolution property, wherein the drug dissolution property of a solid dosage form containing a fat and oil-like substance having a low melting point is improved. | 2010-01-21 |
20100016383 | 4-(3,3-DIHALO-ALLYLOXY)PHENOL DERIVATIVES HAVING PESTICIDAL PROPERTIES - Compounds of formula | 2010-01-21 |
20100016384 | PESTICIDAL COMPOSITION AND METHOD FOR CONTROLLING A PEST - A pesticidal composition containing 4-methoxymethyl-2,3,5,6-tetrafluorobenzyl 3-(2-cyano-1-propenyl)-2,2-dimethylcyclopropanecarboxylate and 1-(2-chloro-1,3-thiazolyl)methyl-3-methyl-2-nitroguanidine has a high pesticidal activity. | 2010-01-21 |
20100016385 | PROCESS AND FORMULATION CONTAINING EPOTHILONES AND ANALOGS THEREOF - A process for formulating certain epothilones and analogs thereof for parenteral administration is provided wherein the pH of the formulation for administration can be controlled to enhance the stability and thus, potency of the epothilone, or analog thereof. | 2010-01-21 |
20100016386 | SELECTIVE GLYCOSIDASE INHIBITORS AND USES THEREOF - The invention provides compounds of formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc | 2010-01-21 |