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Kissei Pharmaceutical, Co. Ltd.

Kissei Pharmaceutical, Co. Ltd. Patent applications
Patent application numberTitlePublished
20120129890INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - A compound (I) of the present invention, which has an EP05-24-2012
20120122931INDOLE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - A compound represented by the general formula (I) of the present invention, which has an EP05-17-2012
20120064154SOLID DRUG FOR ORAL USE - The present invention provides a solid oral dosage form pharmaceutical for the treatment of dysuria, which comprises, as an active ingredient, an indoline compound having an α03-15-2012
20120015972INDOLIZINE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R01-19-2012
20110319464METHODS FOR TREATING BENIGN PROSTATIC HYPERPLASIA - Patients having symptoms associated with benign prostatic hyperplasia can be treated with a once daily composition containing silodosin or a pharmaceutically acceptable salt thereof.12-29-2011
20110230538PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS - The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di (lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R09-22-2011
20110230454(AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH09-22-2011
20110207935FUSED-RING DERIVATIVE AND MEDICAL APPLICATION OF SAME - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X08-25-2011
20110201815FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X08-18-2011
20110201793PROCESS FOR PRODUCTION OF GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE - The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like.08-18-2011
20110172208NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION - The present invention provides compounds represented by general formula (I):07-14-2011
20110092509Pharmaceutical Composition for Prevention or Treatment of Disease Associated with Tear Reduction - The present invention provides pharmaceutical compositions for the prevention or treatment of diseases associated with decrease in tear.04-21-2011
20110034679HEMIFUMARATE OF A PYRAZOLE DERIVATIVE - The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}-propylamino)-2,2-dimethylpropionamide hemifumarate dihydrate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.02-10-2011
20100280083NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION - The present invention provides compounds represented by general formula (I):11-04-2010
20100279962MONOSEBACATE OF PYRAZOLE DERIVATIVE - The present invention provides a novel form of 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide with improved storage stability. Since bis[3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide] monosebacate has extremely excellent storage stability, it is useful as a drug substance. Furthermore, it shows an extremely good crystalline property and can be purified by a convenient method, and therefore is suitable for the industrial preparation.11-04-2010
201002278645-MEMBERED HETEROCYCLIC DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH09-09-2010
20100172988SUSTAINED RELEASE PREPARATION AND METHOD FOR PRODUCTION THEREOF - Disclosed is a sustained release preparation which comprises an active ingredient having a higher release rate at pH 4 compared to that in pH 1.2 or pH 6.8 and exerts a controlled release of the active ingredient in a pH-independent manner. The sustained release preparation comprises ethyl (−)-2-[4-[2-[[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethyl-phenoxy]acetate hydrochloride as the active ingredient and a pH-independent gel-forming polymer and contains substantially no pH-controlling agent other than the polymer. The sustained release preparation can release the active ingredient in a pH-independent manner in the range from 1.2 to 6.8 and shows a constant release rate for a prolonged period of time. Therefore, the preparation is useful as a therapeutic agent for frequent urination/incontinence of urine which has a long-lasting effect.07-08-2010
20100137399PREVENTIVE AND/OR THERAPEUTIC AGENT FOR URINE COLLECTION DISORDER ACCOMPANYING LOWER URINARY TRACT OBSTRUCTION - An agent for the treatment of urine collection disorders associated with lower urinary tract obstructive disease, characterized by containing an indoline derivative represented by the following general formula (I):06-03-2010
20100130514FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I), pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; R05-27-2010
20100112090NITROGENATED FUSED RING DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USE OF THE SAME FOR MEDICAL PURPOSES - [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like.05-06-2010
20100112053GASTRIC RETENTION-TYPE SUSTAINED-RELEASE LEVODOPA PREPARATION - The present invention is to provide a levodopa preparation which is able to persistently release levodopa in the stomach, has a sufficient gastric residence time, is in an easily ingestible size and is able to be easily manufactured industrially with an object of maintaining a sustained concentration of levodopa in blood. It is a gastric retentive preparation for levodopa, characterized in that, the preparation contains a gastric resident layer showing a sufficient retentive property due to a high mechanical strength in the stomach and showing a good disintegrating property in an intestinal tract in addition to a drug releasing layer containing levodopa.05-06-2010
20100081674FUSED HETEROCYCLIC DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides fused heterocyclic derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A is 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; R04-01-2010
20100056521(AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES - The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH03-04-2010
20100029919PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE IN PRODUCING THE SAME - The present invention provides pyrazole derivatives represented by the general formula:02-04-2010
20100009939CONCURRENT DRUGS - The present invention provides a combination drug which is useful for the prevention or treatment of thromboembolism. A pharmaceutical agent comprising an antiplatelet agent in combination with a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula:01-14-2010
20090325900FUSED HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF - The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; R12-31-2009
20090311321ORAL DISINTEGRATING TABLET HAVING MASKED BITTER TASTE AND METHOD FOR PRODUCTION THEREOF - The present invention provides an orally disintegrating tablet containing mitiglinide calcium hydrate. The tablet has reduced bitterness and quickly disintegrates in the mouth, while exhibiting rapid dissolution in the digestive tract. The bitterness-masked orally disintegrating tablet comprises: (a) mitiglinide calcium hydrate; (b) microcrystalline cellulose; (c) at least one masking agent selected from the group consisting of aminoalkyl methacrylate copolymer E, polyvinylacetal diethylaminoacetate, an ethyl acrylate-methyl methacrylate copolymer, and ethyl cellulose; (d) a sugar or a sugar alcohol; and (e) at least one selected from corn starch and partially pregelatinized starch.12-17-2009
20090306396NITROGENATED HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention relates to novel compounds having a xanthine oxidase inhibitory effect and an uricosuric effect and pharmaceutical compositions comprising the same as an active ingredient. That is, the present invention relates nitrogen-containing heterocyclic compounds represented by the following general formula (I):12-10-2009
20090286751PROGRESSION INHIBITOR FOR DISEASE ATTRIBUTED TO ABNORMAL ACCUMULATION OF LIVER FAT - The present invention provides pharmaceutical compositions useful as agents for the inhibition of progression of diseases associated with abnormal accumulation of liver lipids. In particular, the pharmaceutical compositions of the present invention which comprise as an active ingredient a sodium/glucose co-transporter 2 inhibitor are highly suitable as an agent for the inhibition of progression of not only common fatty liver but also non-alcoholic fatty liver disease (NAFL), non-alcoholic steatohepatitis (NASH), hypernutritive fatty liver, diabetic fatty liver, alcoholic fatty liver disease toxic fatty liver or the like.11-19-2009
20090275626PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF NEUROGENIC PAIN - The purpose of the present invention is to provide agents useful for the prevention or treatment of a neuropathic pain. That is, the present invention provides agents for the prevention or treatment of neuropathic pain such as painful diabetic neuropathy, postherpetic neuralgia, trigeminal neuralgia, or postoperative or posttraumatic chronic pain or the like, which comprises a β11-05-2009
20090247781SYNTHESIS OF PHENOXYACETIC ACID DERIVATIVES - The present invention relates to an improved process for the preparation of substituted 2-(4-carbonylmethoxy-optionally 2,5-disubstituted-phenyl-acetaldehydes, in particular 2-(4-alkoxycarbonylmethoxy-optionally 2,5-disubstituted-phenyl)-acetaldehydes and their use in the synthesis of optionally substituted 2-[4-[2-[[-2-hydroxy-2-(4-hydroxyphenyl)-10-01-2009
20090203633PYRAZOLE DERIVATIVES, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF - The present invention provides pyrazole derivatives represented by the general formula:08-13-2009
20090163571PHARMACEUTICAL FOR USE IN THE TREATMENT OF URETEROLITHIASIS - The present invention provides pharmaceutical compositions useful for relieving pain caused by ureteral calculi, facilitating exclusion of ureteral calculi or the like. That is, the present invention provides a pharmaceutical composition for the treatment of ureteral lithiasis, which comprises as an active ingredient an indoline derivative represented by the following general formula (I) or a salt thereof. In the formula, R represents saturated or unsaturated aliphatic acyl which may have a substituent; hydroxyalkyl; aliphatic acyloxyalkyl; lower alkyl which has as a substituent lower alkoxy, carboxy, lower alkoxycarbonyl, aryl-substituted lower alkoxycarbonyl, carbamoyl, mono or di(lower alkyl)-substituted carbamoyl or cyano; optionally substituted aromatic acyl; furoyl or pyridylcarbonyl; R06-25-2009
20090148480SUSTAINED RELEASE PREPARATION - The invention provides a preparation which shows a satisfactory gastric residence time, has such a size that allows for easy ingestion, can quickly disintegrate after expelled from the stomach, and can be prepared readily in an industrial scale. A gastric retentive preparation having a gastric resident layer and a drug release layer is provided, wherein the gastric resident layer does not disintegrate in the stomach and disintegrates in the intestine. Preferably, the gastric resident layer has a minimum diameter of 7 mm or more as measured after stirring the preparation in the first fluid at 200 rpm at 37° C. for 15 hours under the conditions of the paddle method in the dissolution test in accordance with Japanese Pharmacopoeia and has a maximum diameter of 6 mm or less as measured after further stirring the preparation in the second fluid at 200 rpm at 37° C. for 9 hours under the same conditions.06-11-2009
20090093419GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVES AND USE THEREOF IN MEDICINES - The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula:04-09-2009
200900747381-SUBSTITUTED-3-BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO-CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME - A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D-glycopyranosyl) nitrogen-containing heterocyclic compound represented by the general formula (I), a prodrug thereof, or a pharmaceutically acceptable salt thereof, or a hydrate or a solvate thereof; an SGLT inhibitor containing the same; a pharmaceutical composition containing the same and a combination pharmacy of them. In the formula, A represents an alkylene group or alkenylene group; B represents a single bond, —O—, —S— or —NH—; C represents an optionally substituted aryl or heteroaryl group; Q independently represents a carbon atom which a hydrogen atom or a substituent binds to, or a nitrogen atom.03-19-2009
20090069421CRYSTAL POLYMORPH OF HYDROXYNOREPHEDRIN DERIVATIVE HYDROCHLORIDE - The present invention provides a novel crystal polymorph of ethyl (−)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate hydrochloride which can be determined by characteristic diffraction peaks of the powder X-ray diffraction or the like, and obtained from ethyl (−)-2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethyl]-2,5-dimethylphenoxyacetate by a specific method.03-12-2009
20090062518PROCESS FOR PRODUCTION OF GLUCOPYRANOSYLOXYPYRAZOLE DERIVATIVE - The present invention relates to a method for preparing the glucopyranosyloxypyrazole derivatives which are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications, obesity or the like.03-05-2009
200900543561-SUBSTITUTED-7-(B-D-GLYCOPYRANOSYLOXY)(AZA)INDOLE COMPOUND AND PHARMACEUTICAL CONTAINING THE SAME - [Objective] The present invention provides a compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity or the like. 02-26-2009
20090043110Asymmetric Reduction Method - The present invention is to provide a novel method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid which is useful as a therapeutic agent for diabetes. The present invention relates to a method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid, which is characterized in that 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid is subjected to a catalytic reduction reaction in the presence of an asymmetric catalyst prepared from a pyrrolidinebisphosphine compound (I) represented by the following general formula (I):02-12-2009
20090030218Method For Producing Aminoalcohol Derivative Having Biphenyl Group - The present invention provides an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method.01-29-2009
20090018181DRUG COMPOSITION FOR PREVENTION OR INHIBITION OF ADVANCE OF DIABETIC COMPLICATION - The present invention provides pharmaceutical compositions which can achieve good state of glycemic control and correct postprandial hyperglycemia and early morning fasting hyperglycemia. The present pharmaceutical composition is for administration before meal to prevent or inhibit the progression of diabetic complication, which comprises 5 to 45 mg, as a single dose, of mitiglinide or a pharmaceutically acceptable salt thereof, or a hydrate thereof (for example, mitiglinide calcium salt hydrate). And said compositions are extremely useful for prevention or inhibition of progression of, for example, diabetic microvascular complications and arteriosclerotic diseases, because the frequency of adverse drug reactions such as hypoglycemic symptoms and gastrointestinal disorders is low.01-15-2009
20080312153PYRAZOLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF, AND INTERMEDIATE FOR PRODUCTION THEREOF - The present invention provides pyrazole derivatives represented by the general formula:12-18-2008

Patent applications by Kissei Pharmaceutical, Co. Ltd.