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61. 发明授权

US09643969B2 (aza)indolizine derivative and pharmaceutical use thereof 有权
公开(公告)号：US09643969B2
公开(公告)日：2017-05-09
申请号：US13824147
申请日：2011-09-28
申请人： Masato Iizuka , Kazuo Shimizu
发明人： Masato Iizuka , Kazuo Shimizu
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： (Aza)indolizine derivatives represented by 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 Formula (I), 0 to 2 of X1, X2, X3 and X4 are a nitrogen atom and the others are CR1; one of T1 and T2 represents cyano and the other represents a group represented by Formula (A), with the proviso that when T1 is cyano, at least one of X1 to X4 is a nitrogen atom; R1 independently represents a hydrogen atom, a halogen atom, a hydroxy group, C1-6 alkyl, C1-6 alkoxy or the like; ring U represents a benzene ring or the like; m represents integral number from 0 to 2; R2 independently represents a fluorine atom, a hydroxy group or the like.

62. 发明授权

US09585885B2 Substituted pyrido[2,3-g]quinazolines as dopamine D2 receptor agonists 有权
标题翻译：取代的吡啶并[2,3-g]喹唑啉作为多巴胺D2受体激动剂
公开(公告)号：US09585885B2
公开(公告)日：2017-03-07
申请号：US14650786
申请日：2013-12-06
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Toshihiro Nishimura , Yasunori Ueno , Kiyoshi Kasai , Masako Yoshida
IPC分类号： A61K31/519 , C07D487/14 , C07D471/04 , A61K45/06 , A61K31/55 , C12N15/09 , A61K31/13 , A61K31/198 , A61K31/423
CPC分类号： A61K31/519 , A61K31/13 , A61K31/198 , A61K31/423 , A61K31/55 , A61K45/06 , C07D471/04 , C12N15/09 , A61K2300/00
摘要： [Problem] To provide a novel compound that exhibits an agonistic effect on dopamine D2 receptors.[Solution] The present invention provides a compound represented by the general formula (I): in which R1 is C1-6 alkyl or the like; R2 is hydrogen or the like; R3 and R4 are each hydrogen, C1-6 alkyl, R10R11N—C1-6 alkyl, aralkyl, or the like; R5 and R6 are hydrogen or the like; and R7 is hydrogen or the like, or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same and uses for said compound/salt and composition. The compounds of the present invention exhibit potent dopamine D2 receptor simulating activities and thus are useful as a treating or preventing agent for Parkinson's disease and the like.
摘要翻译： [问题]提供对多巴胺D 2受体表现出激动作用的新化合物。 [溶液]本发明提供由通式（I）表示的化合物：其中R 1为C 1-6烷基等; R 2是氢等; R 3和R 4各自为氢，C 1-6烷基，R 10 R 11 N-C 1-6烷基，芳烷基等; R 5和R 6是氢等; 和R 7是氢等，或其药学上可接受的盐，含有该组合物的药物组合物和用于所述化合物/盐和组合物。本发明的化合物显示有效的多巴胺D 2受体模拟活性，因此可用作帕金森病等的治疗或预防剂。

63. 发明申请

US20160362368A1 NOVEL ANILINE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF 有权
标题翻译：新型苯胺衍生物，含有它们的药物组合物及其用途
公开(公告)号：US20160362368A1
公开(公告)日：2016-12-15
申请号：US15121522
申请日：2015-02-27
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Hitoshi Inoue , Kohsuke Ohno , Tetsuya Nakamura , Yusuke Ohsawa
IPC分类号： C07D205/04
CPC分类号： C07D205/04
摘要： [Problem] The present invention provides a novel compound having an S1P1 receptor antagonistic activity.[Solution] The present invention provides a compound represented by the general formula (I): (in the formula, R1, R2 and R3 are each a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group or the like, R4 is a C1-6 alkyl group or the like, R5 is a C1-6 alkyl group or the like, R6 is a C1-6 alkyl group or the like, R7 is a hydrogen atom, a halogen atom, a C1-6 alkyl group or the like, R8 is a halogen atom, a C1-6 alkyl group, a halo C1-6 alkyl group, a C1-6 alkoxy group or the like, and R9 is a hydrogen atom or a C1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent S1P1 receptor antagonistic activity and therefore are useful as an agent for the treatment or prevention of autoimmune diseases and the like.

64. 发明授权

US09273085B2 Pyrazole derivative and use thereof for medical purposes 有权
标题翻译：吡唑衍生物及其用于医疗目的的用途
公开(公告)号：US09273085B2
公开(公告)日：2016-03-01
申请号：US14399093
申请日：2013-05-02
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Masayuki Isaji , Masaaki Takemura , Hidetoshi Isawa , Yukihiko Hotei , Itaru Miyashita
IPC分类号： A61K31/7056 , C07H17/02
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
摘要翻译：本发明提供了用于医疗目的的吡唑衍生物及其用途等。更具体地，本发明涉及可用于预防或治疗便秘的药物，其包含作为活性成分的3-（3- {4- [3 - （（R） - D-吡喃葡萄糖氧基）-5-异丙基-1H- 吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）-2,2-二甲基丙酰胺或其药学上可接受的盐。本发明的药物具有增加排便次数等的效果，对预防或治疗便秘是有用的。

65. 发明授权

US09040693B2 Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof 有权
标题翻译：稠合杂环衍生物，含有它们的药物组合物及其医药用途
公开(公告)号：US09040693B2
公开(公告)日：2015-05-26
申请号：US12089674
申请日：2006-10-17
申请人： Kohsuke Ohno , Takashi Miyagi , Tomonaga Ozawa , Nobuhiko Fushimi
发明人： Kohsuke Ohno , Takashi Miyagi , Tomonaga Ozawa , Nobuhiko Fushimi
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： 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; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.
摘要翻译：本发明提供了可用作预防或治疗性激素依赖性疾病等的药剂的化合物。也就是说，本发明提供由以下通式（I）表示的稠合杂环衍生物，含有该杂环衍生物的药物组合物，其医药用途等。在式（I）中，环A表示5元环状不饱和烃或5元杂芳基; 烷基，烯基，炔基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; 环B表示芳基或杂芳基; RB代表卤素，烷基，羧基，烷氧基，氨基甲酰基，烷基氨基甲酰基等; E1和E2表示氧原子等; U表示单键或亚烷基; X表示Y表示的基团，-SO 2 -Y，-O-（亚烷基）-Y，-O-Z，Y表示Z，氨基等; Z表示环烷基，杂环烷基，芳基，杂芳基等; 或类似物。

66. 发明申请

US20150141631A1 PYRAZOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
标题翻译：吡唑衍生物及其用于医疗用途
公开(公告)号：US20150141631A1
公开(公告)日：2015-05-21
申请号：US14399093
申请日：2013-05-02
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Masayuki Isaji , Masaaki Takemura , Hidetoshi Isawa , Yukihiko Hotei , Itaru Miyashita
IPC分类号： C07H17/02
CPC分类号： A61K31/7056 , C07H17/02
摘要： The present invention provides pyrazole derivatives, uses thereof for medical purposes and so on. More particularly, the present invention relates to pharmaceuticals useful for the prevention or treatment of constipation, which comprise as an active ingredient 3-(3-{4-[3-(β-D-glucopyranosyloxy)-5-isopropyl-1H-pyrazol-4-ylmethyl]-3-methylphenoxy}propylamino)-2,2-dimethylpropionamide, or a pharmaceutically acceptable salt thereof. The pharmaceuticals of the present invention exert an effect of increasing the frequency of bowel movement or the like, and are useful for the prevention or treatment of constipation.
摘要翻译：本发明提供了用于医疗目的的吡唑衍生物及其用途等。更具体地，本发明涉及可用于预防或治疗便秘的药物，其包含作为活性成分的3-（3- {4- [3 - （（R） - D-吡喃葡萄糖氧基）-5-异丙基-1H- 吡唑-4-基甲基] -3-甲基苯氧基}丙基氨基）-2,2-二甲基丙酰胺或其药学上可接受的盐。本发明的药物具有增加排便次数等的效果，对预防或治疗便秘是有用的。

67. 发明授权

US08829040B2 (aza)indole derivative and use thereof for medical purposes 有权
标题翻译：（氮杂）吲哚衍生物及其用于医疗目的的用途
公开(公告)号：US08829040B2
公开(公告)日：2014-09-09
申请号：US14193911
申请日：2014-02-28
申请人： Kissei Pharmaceutical Co., Ltd.
发明人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
IPC分类号： A61K31/404 , C07D209/30 , C07D209/42
CPC分类号： C07D209/30 , A61K31/165 , A61K31/404 , A61K31/407 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D209/42 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/12 , C07D417/04 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： 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, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.
摘要翻译：本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐其中。在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

68. 发明申请

US20140179932A1 (AZA)INDOLE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES 有权
标题翻译：（AZA）INDOLE DERIVATIVE及其用于医疗用途
公开(公告)号：US20140179932A1
公开(公告)日：2014-06-26
申请号：US14193911
申请日：2014-02-28
申请人： KISSEI PHARMACEUTICAL CO., LTD.
发明人： Kazuo Shimizu , Yasushi Takigawa , Hideki Fujikura , Masato Iizuka , Masahiro Hiratochi , Norihiko Kikuchi
IPC分类号： C07D209/42
CPC分类号： C07D209/30 , A61K31/165 , A61K31/404 , A61K31/407 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D209/42 , C07D401/04 , C07D405/04 , C07D405/10 , C07D409/12 , C07D417/04 , C07D471/04 , C07D491/056 , A61K2300/00
摘要： 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, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.
摘要翻译：本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐其中。在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

69. 发明授权

US08263622B2 Fused-ring derivative and medical application of same 有权
标题翻译：融合环衍生物和医疗应用相同
公开(公告)号：US08263622B2
公开(公告)日：2012-09-11
申请号：US13124345
申请日：2009-10-14
申请人： Kazuo Shimizu , Masato Iizuka , Hideki Fujikura , Yasushi Takigawa , Masahiro Hiratochi
发明人： Kazuo Shimizu , Masato Iizuka , Hideki Fujikura , Yasushi Takigawa , Masahiro Hiratochi
IPC分类号： A61K31/426 , A61K31/433 , A61K31/4709 , A61K31/4725 , C07D215/16 , C07D239/72 , C07D277/24
CPC分类号： C07C255/57 , A61K31/192 , A61K31/415 , A61K31/426 , A61K31/44 , A61K31/47 , C07C255/54 , C07D213/79 , C07D215/50 , C07D231/14 , C07D277/20 , C07D277/56
摘要： 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), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.
摘要翻译：本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前药，其盐或类似物。在式（I）中，X 1和X 2表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

70. 发明授权

US07998975B2 Nitrogenous fused-ring derivatives, medicinal compositions containing the derivatives, and use thereof as drugs 有权
标题翻译：含氮稠环衍生物，含有衍生物的药物组合物及其作为药物的用途
公开(公告)号：US07998975B2
公开(公告)日：2011-08-16
申请号：US12032411
申请日：2008-02-15
申请人： Nobuhiko Fushimi , Hirotaka Teranishi , Kazuo Shimizu , Shigeru Yonekubo , Fumiaki Ito , Masayuki Isaji
发明人： Nobuhiko Fushimi , Hirotaka Teranishi , Kazuo Shimizu , Shigeru Yonekubo , Fumiaki Ito , Masayuki Isaji
IPC分类号： A61K31/44 , A61K31/405 , A01N43/38
CPC分类号： A61K31/7056 , A61K31/706 , C07H17/02
摘要： The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, an alkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.
摘要翻译：本发明提供由以下通式表示的含氮稠环衍生物或其药学上可接受的盐或其前药，其在人SGLT中表现出优异的抑制活性，并且可用作预防或治疗疾病的药剂与糖尿病，餐后高血糖症，葡萄糖耐量降低，糖尿病并发症或肥胖症等高血糖相关，在式R 1中表示H，任选取代的烷基，烯基等; R2表示H，卤素原子或烷基; R3和R4代表H，OH，卤素原子，任选取代的烷基等; Y表示CH或N; Q表示亚烷基，亚烯基等; 环A表示芳基或杂芳基; G表示由以下通式（G-1）或（G-2）表示的基团（其中E1表示H，F或OH; E2表示H，F，甲基等）和药物组合物包括它们的药物用途。

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