公开(公告)号：EP2669285A1

公开(公告)日：2013-12-04

申请号：EP12739093.8

申请日：2012-01-25

申请人： Kyorin Pharmaceutical Co., Ltd. ,  Kissei Pharmaceutical Co., Ltd.

发明人： SETO, Shigeki ,  UMEI, Kentaro ,  NISHIGAYA, Yosuke ,  TANIOKA, Asao ,  KONDO, Tatsuhiro ,  KONDO, Atsushi ,  TATANI, Kazuya ,  KAWAMURA, Naohiro

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/5377 ,  A61P13/02 ,  A61P43/00

CPC分类号： C07D471/04

摘要： A pyrazolopyridine derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof exhibits a strong EP 1 receptor antagonistic effect. Thus, the derivative or the pharmacologically acceptable salt is useful as a therapeutic agent for lower urinary tract symptoms (LUTS), particularly, overactive bladder syndrome (OABs), or a prophylactic agent therefor and furthermore, is also useful in the treatment, prevention, or suppression of various pathological conditions in which the EP 1 receptor is involved, such as inflammatory disease, pain disease, osteoporosis, and cancer.

[A is a benzene ring or the like, Y 1 is C 1-6 alkylene, R 1 is -C(=O)-OZ 1 or the like, Z 1 is H or the like, R 2 is a branched C 3-6 alkyl group or the like, R 3 is H or the like, R 4 is a hydrogen atom or the like, and R 5 is a hydrogen atom or the like].

摘要翻译： 由下式（I）表示的吡唑并吡啶衍生物或其药理学上可接受的盐表现出强烈的EP 1受体拮抗作用。 因此，衍生物或药理学上可接受的盐可用作下尿路症状（LUTS），特别是膀胱过度活动症（OAB）或其预防剂的治疗剂，此外，还可用于治疗，预防， 或抑制涉及EP 1受体的各种病理状况，例如炎性疾病，疼痛疾病，骨质疏松症和癌症。 [A是苯环等，Y 1是C 1-6亚烷基，R 1是-C（= O）-OZ 1等，Z 1是H等，R 2是支链C 3 -6烷基等，R 3为H等，R 4为氢原子等，R 5为氢原子等）。

公开(公告)号：EP2669271A1

公开(公告)日：2013-12-04

申请号：EP12739597.8

申请日：2012-01-24

申请人： Kissei Pharmaceutical Co., Ltd. ,  Kyorin Pharmaceutical Co., Ltd.

发明人： TATANI, Kazuya ,  KONDO, Atsushi ,  KONDO, Tatsuhiro ,  KAWAMURA, Naohiro ,  SETO. Shigeki ,  KOHNO, Yasushi

IPC分类号： C07D209/08 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/00 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

CPC分类号： C07D209/08 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K2300/00

摘要： The present invention provides a compound represented by the general formula (I) of the present invention, which has EP 1 receptor antagonism:

[wherein A represents a pyridine ring, a furan ring, or the like; Y 1 represents a C 1-6 alkylene group; Y 2 represents a single bond or the like; R 1 represents -C(=O)-NH-SO 2 -R 6 , an acidic 5-membered hetero ring group, or the like; R 2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R 3 represents a halogen atom, a C 1-6 alkoxy group, or the like; R 4 represents a hydrogen atom, a halogen atom, or the like; R 5 represents a hydrogen atom or the like; and R 6 represents a C 1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

摘要翻译： 本发明提供了具有EP1受体拮抗作用的由本发明通式（I）表示的化合物：[其中A表示吡啶环，呋喃环等; Y1表示C1-6亚烷基; Y2表示单键等; R 1表示-C（= O）-NH-SO 2 -R 6，酸性5元杂环基等; R2表示任选取代的苯基，任选取代的5元芳族杂环基团等; R3代表卤素原子，C1-6烷氧基等; R4代表氢原子，卤素原子等; R5代表氢原子等; 并且R6代表C1-6烷基等]及其药学上可接受的盐。 此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

公开(公告)号：EP2669272A1

公开(公告)日：2013-12-04

申请号：EP12739875.8

申请日：2012-01-24

申请人： Kissei Pharmaceutical Co., Ltd. ,  Kyorin Pharmaceutical Co., Ltd.

发明人： TATANI, Kazuya ,  KONDO, Atsushi ,  KONDO, Tatsuhiro ,  KAWAMURA, Naohiro ,  SETO, Shigeki ,  KOHNO, Yasushi

IPC分类号： C07D209/18 ,  A61K31/404 ,  A61K31/41 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/00 ,  A61P13/02 ,  A61P13/10 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D419/14

CPC分类号： A61K31/4245 ,  A61K31/404 ,  A61K31/41 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D209/18 ,  C07D401/06 ,  C07D401/14 ,  C07D403/10 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D419/14 ,  A61K2300/00

摘要： The present invention provides a compound represented by the general formula (I) of the present invention, which has EP 1 receptor antagonism:

[wherein A represents a benzene ring, a pyridine ring, or the like; Y 1 represents a C 1-6 alkylene group or the like; Y 2 represents a single bond or the like; Z represents -C(=O)-NHSO 2 R 6 , an acidic 5-membered hetero ring group, or the like; R 1 represents a hydrogen atom or the like; R 2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R 3 represents a halogen atom, a C 1-6 alkoxy group, or the like; R 4 represents a hydrogen atom, a halogen atom, or the like; R 5 represents a hydrogen atom or the like; and R 6 represents a C 1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

摘要翻译： 本发明提供了具有EP1受体拮抗作用的由本发明通式（I）表示的化合物：[其中A表示苯环，吡啶环等; Y1表示C1-6亚烷基等; Y2表示单键等; Z表示-C（= O）-NHSO 2 R 6，酸性5元杂环基等; R1表示氢原子等; R2代表苯基，5元芳族杂环基团等; R3代表卤素原子，C1-6烷氧基等; R4代表氢原子，卤素原子等; R5代表氢原子等; 和R6代表C1-6烷基等]或其药学上可接受的盐。 此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

公开(公告)号：EP3459941A1

公开(公告)日：2019-03-27

申请号：EP17831063.7

申请日：2017-07-20

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： KONDO, Atsushi ,  MORITA, Naohide ,  ISHIKAWA, Takehiro ,  YOSHIDA, Masako ,  MORIYAMA, Akihiro ,  WANAJO, Isao

IPC分类号： C07D401/14 ,  A61K31/501 ,  A61K31/506 ,  A61P9/00 ,  A61P25/06 ,  A61P43/00 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： The present invention aims to provide a novel compound which has CGRP receptor antagonist activity and which is useful for the treatment of various diseases mediated by CGRP receptors. That is, the present invention relates to the pyrrolidine derivatives represented by the following formula (I) or a pharmaceutically acceptable salt thereof. In the formulae, W is ring, X is a carbon atom or the like, Y 1 to Y 4 are carbon atoms or the like, and R 1 to R 7 is alkyl or the like. The compounds of the present invention or a pharmaceutically acceptable salt thereof have an excellent CGRP receptor antagonist activity, and thus are useful as agents for the treatment of various diseases mediated by CGRP receptors.

公开(公告)号：EP2474530B1

公开(公告)日：2014-09-03

申请号：EP10804369.6

申请日：2010-07-26

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： KONDO, Tatsuhiro ,  KONDO, Atsushi ,  TATANI, Kazuya ,  KAWAMURA, Naohiro

IPC分类号： C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61P13/02 ,  A61P43/00

CPC分类号： A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

公开(公告)号：EP2474530A1

公开(公告)日：2012-07-11

申请号：EP10804369.6

申请日：2010-07-26

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： KONDO, Tatsuhiro ,  KONDO, Atsushi ,  TATANI, Kazuya ,  KAWAMURA, Naohiro

IPC分类号： C07D209/18 ,  A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61P13/02 ,  A61P43/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

CPC分类号： A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

摘要： A compound represented by the general formula (I) of the present invention, which has an EP 1 receptor antagonism:

[wherein A represents a benzene ring or the like; Y represents a C 1-6 alkylene group or the like; R N represents a hydrogen atom or a C 1-6 alkyl group; R 1 represents a hydrogen atom, a C 1-6 alkyl group or the like; R 2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like;R 3 represents a halogen atom, a C 1-6 alkoxy group or the like; R 4 represents a hydrogen atom or the like; and R 5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

摘要翻译： 本发明的通式（I）所示的化合物具有EP1受体拮抗作用，式中，A表示苯环等， Y表示C 1-6亚烷基等; RN代表氢原子或C1-6烷基; R1代表氢原子，C1-6烷基等; R 2表示可以具有取代基的苯基，可以具有取代基的5元芳族杂环基，可以具有取代基的6元芳族杂环基等; R 3表示卤素原子，C 1-6 烷氧基等; R4表示氢原子等; R5表示氢原子等]或其药学上可接受的盐。 此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

公开(公告)号：EP2460791A1

公开(公告)日：2012-06-06

申请号：EP10804370.4

申请日：2010-07-26

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： TATANI, Kazuya ,  KAWAMURA, Naohiro ,  KONDO, Tatsuhiro ,  KONDO, Atsushi

IPC分类号： C07D209/08 ,  A61K31/404 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  A61P13/02 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

CPC分类号： C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14

摘要： A compound (I) of the present invention, which has an EP 1 receptor antagonism:

[wherein A represents a benzene ring or the like; Y 1 represents a C 1-6 alkylene group; Y 2 represents a single bond or the like; R 1 represents a hydrogen atom, a C 1-6 alkyl group or the like; R 2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R 3 represents a halogen atom, a C 1-6 alkoxy group or the like; R 4 represents a hydrogen atom or the like; and R 5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

摘要翻译： 具有EP 1受体拮抗作用的本发明化合物（I）：其中A表示苯环等; Y 1表示C 1-6亚烷基; Y 2表示单键等; R 1表示氢原子，C 1-6烷基等; R 2表示可以具有取代基的苯基，可以具有取代基的5元芳香族杂环，可以具有取代基的6元芳族杂环等; R 3表示卤素原子，C 1-6烷氧基等; R 4表示氢原子等; 和R 5表示氢原子等]或其药学上可接受的盐。 此外，本发明的化合物（I）可以用作治疗或预防LUTS，特别是OAB的各种症状的药剂。

公开(公告)号：EP2460791B1

公开(公告)日：2014-04-02

申请号：EP10804370.4

申请日：2010-07-26

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： TATANI, Kazuya ,  KAWAMURA, Naohiro ,  KONDO, Tatsuhiro ,  KONDO, Atsushi

IPC分类号： C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  A61K31/422 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/427 ,  A61P13/02 ,  A61P43/00

CPC分类号： C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14