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公开(公告)号:US08466282B2
公开(公告)日:2013-06-18
申请号:US12999428
申请日:2009-06-17
申请人: Takanobu Kuroita , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
发明人: Takanobu Kuroita , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
IPC分类号: C07D413/00 , A61K31/535
CPC分类号: C07D401/12 , C07D233/90 , C07D401/14 , C07D405/14 , C07D407/12 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D495/04
摘要: Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
摘要翻译: 由式(I)(II)表示的化合物,其中各符号如说明书中所定义,其前药具有优异的肾素抑制活性,可用作预防或治疗高血压的药剂,可归因于 高血压等。
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公开(公告)号:US20110178057A1
公开(公告)日:2011-07-21
申请号:US12999428
申请日:2009-06-17
申请人: Takanobu Kuroita , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
发明人: Takanobu Kuroita , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
IPC分类号: A61K31/454 , C07D413/14 , C07D471/04 , C07D401/14 , C07D401/12 , A61K31/5377 , A61K31/4545 , A61P9/12 , A61P9/00
CPC分类号: C07D401/12 , C07D233/90 , C07D401/14 , C07D405/14 , C07D407/12 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D495/04
摘要: Compounds represented by the formulas (I) (II) wherein each symbol is as defined in the specification, and a pro-drug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
摘要翻译: 由式(I)(II)表示的化合物,其中各符号如说明书中所定义,其前药具有优异的肾素抑制活性,可用作预防或治疗高血压,各种器官损伤的药剂 归因于高血压等。
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公开(公告)号:US20120264733A1
公开(公告)日:2012-10-18
申请号:US13446408
申请日:2012-04-13
申请人: Takanobu KUROITA , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
发明人: Takanobu KUROITA , Yasuhiro Imaeda , Kouichi Iwanaga , Naohiro Taya , Hidekazu Tokuhara , Yoshiyuki Fukase
IPC分类号: A61K31/454 , A61K31/5377 , C07D471/04 , C07D495/04 , C07D405/14 , A61P9/12 , A61K31/4545 , C07D401/14 , C07D487/08 , A61K31/553 , A61K31/538 , A61P9/00 , C07D413/14 , C07D401/12
CPC分类号: C07D401/12 , C07D233/90 , C07D401/14 , C07D405/14 , C07D407/12 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D495/04
摘要: Compounds represented by the formulas wherein each symbol is as defined in the specification, and a prodrug thereof have a superior renin inhibitory activity, and are useful as agents for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
摘要翻译: 由式表示的化合物,其中各符号如说明书中所定义,其前药具有优异的肾素抑制活性,可用作预防或治疗高血压,高血压等各种器官损害的药剂。
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公开(公告)号:US20090227560A1
公开(公告)日:2009-09-10
申请号:US12216874
申请日:2008-07-11
申请人: Takanobu Kuroita , Tsuneo Oda , Yasutomi Asano , Naohiro Taya , Kouichi Iwanaga , Hidekazu Tokuhara , Yoshiyuki Fukase
发明人: Takanobu Kuroita , Tsuneo Oda , Yasutomi Asano , Naohiro Taya , Kouichi Iwanaga , Hidekazu Tokuhara , Yoshiyuki Fukase
IPC分类号: A61K31/496 , C07D403/06 , C07D403/14 , C07D413/14 , A61K31/5377 , A61P9/12
CPC分类号: C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
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公开(公告)号:US20090156612A1
公开(公告)日:2009-06-18
申请号:US12081917
申请日:2008-04-23
申请人: Takanobu Kuroita , Tsuneo Oda , Yasutomi Asano , Naohiro Taya , Kouichi Iwanaga , Hidekazu Tokuhara , Yoshiyuki Fukase
发明人: Takanobu Kuroita , Tsuneo Oda , Yasutomi Asano , Naohiro Taya , Kouichi Iwanaga , Hidekazu Tokuhara , Yoshiyuki Fukase
IPC分类号: A61K31/497 , C07D403/06 , A61P9/12
CPC分类号: C07D403/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension, and the like.
摘要翻译: 本发明涉及由下式表示的化合物:其中每个符号如说明书中所定义,或其盐或其前药。 本发明的化合物具有优异的肾素抑制活性,因此可用作预防或治疗高血压,高血压引起的各种器官损害等。
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公开(公告)号:US08329691B2
公开(公告)日:2012-12-11
申请号:US12734150
申请日:2008-10-14
IPC分类号: A61K31/5377 , A61K31/506 , C07D413/14 , C07D239/20
CPC分类号: C07D401/12 , C07D239/42 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
摘要翻译: 一种肾素抑制剂,其包含由下式表示的化合物:其中每个符号如说明书中所定义,或其盐或其前药。 本发明的化合物具有优异的肾素抑制活性,因此可用作预防或治疗高血压,高血压等各种器官损害的药剂。
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公开(公告)号:US20100324010A1
公开(公告)日:2010-12-23
申请号:US12734150
申请日:2008-10-14
IPC分类号: A61K31/506 , A61K31/553 , A61K31/55 , A61K31/551 , A61K31/541 , A61K31/4709 , A61K31/4545 , A61K31/4439 , C07D413/14 , C07D405/14 , C07D417/14 , C07D401/14 , A61P9/12
CPC分类号: C07D401/12 , C07D239/42 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.
摘要翻译: 一种肾素抑制剂,其包含由下式表示的化合物:其中每个符号如说明书中所定义,或其盐或其前药。 本发明的化合物具有优异的肾素抑制活性,因此可用作预防或治疗高血压,高血压等各种器官损害的药剂。
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公开(公告)号:US09156837B2
公开(公告)日:2015-10-13
申请号:US14235992
申请日:2012-07-27
申请人: Satoshi Yamamoto , Junya Shirai , Atsuko Ochida , Yoshiyuki Fukase , Yoshihide Tomata , Ayumu Sato , Shotaro Miura , Kazuko Yonemori , Ryokichi Koyama
发明人: Satoshi Yamamoto , Junya Shirai , Atsuko Ochida , Yoshiyuki Fukase , Yoshihide Tomata , Ayumu Sato , Shotaro Miura , Kazuko Yonemori , Ryokichi Koyama
IPC分类号: C07D277/30 , C07D277/56 , C07D211/90 , C07D417/12 , C07D471/04 , C07D401/12 , C07D277/24 , C07D401/04 , C07D417/04 , C07D417/14 , C07D491/107
CPC分类号: C07D471/04 , C07D417/04 , C07D417/14 , C07D491/107
摘要: A heterocyclic compound having an RORγt inhibitory activity, which is a compound of formula (I) or a salt thereof is provided. The compound has ring A, which is an optionally substituted cyclic group and is bound to a pyrazole ring though Q. Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene. R1 is a substituent. Ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2. R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group.
摘要翻译: 提供具有RORγt抑制活性的杂环化合物,其为式(I)化合物或其盐。 该化合物具有环A,其为任选取代的环状基团,并且通过Q键合至吡唑环。Q为键,任选取代的C 1-10亚烷基,任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基。 R1是取代基。 环B是噻唑环,异噻唑环或二氢噻唑环,除了R2之外,它们各自任选进一步被取代基取代。 R 2是任选取代的环羰基-C 1-6烷基,任选取代的氨基羰基-C 1-6烷基,任选取代的环C 1-6烷基,任选取代的环C 1-6烷基氨基羰基, 任选取代的氨基羰基-C 2-6烯基,任选取代的C 1-6烷基羰基氨基-C 1-6烷基,任选取代的环 - 氨基羰基,任选取代的环羰基或任选取代的非芳族杂环基。
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公开(公告)号:US07803822B2
公开(公告)日:2010-09-28
申请号:US11887936
申请日:2006-04-06
申请人: Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
发明人: Keiji Kubo , Mamoru Tobisu , Eiji Honda , Takahiko Taniguchi , Yoshiyuki Fukase , Masaki Kawamura , Masaharu Nakayama
IPC分类号: A61K31/41 , C07D249/00
CPC分类号: C07D249/06 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D411/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D487/04
摘要: The present invention relates to a thrombin receptor antagonist containing a compound represented by the formula (I) wherein R1a, R1b and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted alkoxy, R3 is a group represented by the formula —NHCOR4, —NHSO2R5, —NHCON(R6a)(R6b), —NHCOOR7 or —CONHR8 wherein R4, R5, R6a, R6b, R7 and R8 are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group and the like), ring A is monocyclic aromatic ring optionally further having substituent(s), R1a and R1b are optionally bonded to each other to form an optionally substituted nitrogen-containing non-aromatic heterocycle, or a salt thereof or a prodrug thereof. The thrombin receptor antagonist of the present invention has a thrombin receptor (particularly PAR-1) antagonistic action and is useful for the prophylaxis or treatment of PAR-1 mediated pathological condition or disease.
摘要翻译: 本发明涉及含有式(I)表示的化合物的凝血酶受体拮抗剂,其中R1a,R1b和R2各自为氢原子,任选取代的烃基,任选取代的杂环基或任选取代的烷氧基,R 3 是由式-NHCOR4,-NHSO2R5,-NHCON(R6a)(R6b),-NHCOOR7或-CONHR8表示的基团,其中R4,R5,R6a,R6b,R7和R8各自为氢原子,任选取代的烃基 ,任选取代的杂环基等),环A是任选进一步具有取代基的单环芳环,R 1a和R 1b任选地彼此键合以形成任选取代的含氮非芳族杂环或盐 或其前药。 本发明的凝血酶受体拮抗剂具有凝血酶受体(特别是PAR-1)拮抗作用,可用于预防或治疗PAR-1介导的病理状态或疾病。
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公开(公告)号:US20140163001A1
公开(公告)日:2014-06-12
申请号:US14235992
申请日:2012-07-27
申请人: Satoshi Yamamoto , Junya Shirai , Atsuko Ochida , Yoshiyuki Fukase , Yoshihide Tomata , Ayumu Sato , Shotaro Miura , Kazuko Yonemori , Ryokichi Koyama
发明人: Satoshi Yamamoto , Junya Shirai , Atsuko Ochida , Yoshiyuki Fukase , Yoshihide Tomata , Ayumu Sato , Shotaro Miura , Kazuko Yonemori , Ryokichi Koyama
IPC分类号: C07D491/107 , C07D417/04 , C07D471/04 , C07D417/14
CPC分类号: C07D471/04 , C07D417/04 , C07D417/14 , C07D491/107
摘要: Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): wherein ring A is an optionally substituted cyclic group, Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene, R1 is a substituent, ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2, and R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group, or a salt thereof.
摘要翻译: 提供具有RORγt抑制活性的杂环化合物。 由式(I)表示的化合物:其中环A是任选取代的环状基团,Q是键,任选取代的C 1-10亚烷基,任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基,R 1是 取代基,环B是噻唑环,异噻唑环或二氢噻唑环,其中R 2独立地任选被取代基任意地进一步被R 2取代,R 2是任选取代的环羰基-C 1-6烷基,任选地 取代的氨基羰基-C 1-6烷基,任选取代的环烷基-C 1-6烷基,任选取代的环基-C 1-6烷基氨基 - 羰基,任选取代的氨基羰基-C 2-6链烯基,任选取代的C 1-6 烷基羰基氨基-C 1-6烷基,任选取代的环 - 氨基羰基,任选取代的环羰基或任选取代的非芳族杂环基,或其盐。
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