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1. 发明公开

EP4349840A2 PYRAZOLOPYRIDINE DERIVATIVE HAVING GLP-1 RECEPTOR AGONIST EFFECT 审中-实审
公开(公告)号：EP4349840A2
公开(公告)日：2024-04-10
申请号：EP24154118.4
申请日：2017-09-26
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： YOSHINO, Hitoshi , TSUCHIYA, Satoshi , MATSUO, Atsushi , SATO, Tsutomu , NISHIMOTO, Masahiro , OGURI, Kyoko , OGAWA, Hiroko , NISHIMURA, Yoshikazu , FURUTA, Yoshiyuki , KASHIWAGI, Hirotaka , HORI, Nobuyuki , KAMON, Takuma , SHIRAISHI, Takuya , YOSHIDA, Shoshin , KAWAI, Takahiro , TANIDA, Satoshi , AOKI, Masahide
IPC分类号： C07D519/00
摘要： The present invention provides a a process for manufacturing a compound of formula (Ia), or a pharmaceutically acceptable salt thereof:

2. 发明授权

EP1852439B1 SPIROKETAL DERIVATIVE AND USE THEREOF AS DIABETIC MEDICINE 有权
标题翻译：螺缩酮衍生物和其作为糖尿病治疗
公开(公告)号：EP1852439B1
公开(公告)日：2016-03-23
申请号：EP06712450.3
申请日：2006-01-27
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： KOBAYASHI, Takamitsu , SATO, Tsutomu , NISHIMOTO, Masahiro
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07D311/96 , C07D491/153 , C07D493/10 , C07H19/01

3. 发明公开

EP1116726A1 ETHYLAMINE DERIVATIVES 审中-公开
标题翻译： ETHYLAMINDERIVATE
公开(公告)号：EP1116726A1
公开(公告)日：2001-07-18
申请号：EP99944808.7
申请日：1999-09-24
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： MATSUOKA, Hiroharu , SATO, Tsutomu
IPC分类号： C07K5/078 , A61K38/06
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/0827
摘要： The object of the present invention is to provide ethylamine derivatives that function as a motilin receptor antagonist and that are useful as medicines.
The invention provides compounds represented by the general formula (1):
wherein
R 1 represents a phenyl group or the like, R 2 represents a hydrogen atom and the like, R 3 represents a hydrogen atom and the like, R 4 represents a hydrogen atom and the like, R 5 represents an alkyl group and the like, R 7 represents a hydrogen atom and the like and R 8 represents a heterocyclic ring and the like; or a hydrate or pharmaceutically acceptable salt thereof and a medicine which comprises the above compound or a hydrate or pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明的目的是提供用作胃动素受体拮抗剂并可用作药物的乙胺衍生物。本发明提供由通式（1）表示的化合物：其中R 1表示苯基等，R 2表示氢原子等，R 3表示氢原子等，R 4表示氢原子， R 5表示烷基等，R 7表示氢原子等，R 8表示杂环等。或其水合物或药学上可接受的盐和包含上述化合物或其水合物或药学上可接受的盐作为活性成分的药物。

4. 发明公开

EP4134367A1 PYRAZOLOPYRIDINE DERIVATIVE HAVING GLP-1 RECEPTOR AGONIST EFFECT 无效
公开(公告)号：EP4134367A1
公开(公告)日：2023-02-15
申请号：EP22180270.5
申请日：2017-09-26
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： YOSHINO, Hitoshi , TSUCHIYA, Satoshi , MATSUO, Atsushi , SATO, Tsutomu , NISHIMOTO, Masahiro , OGURI, Kyoko , OGAWA, Hiroko , NISHIMURA, Yoshikazu , FURUTA, Yoshiyuki , KASHIWAGI, Hirotaka , HORI, Nobuyuki , KAMON, Takuma , SHIRAISHI, Takuya , YOSHIDA, Shoshin , KAWAI, Takahiro , TANIDA, Satoshi , AOKI, Masahide
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P25/16 , A61P25/28 , C07D519/00
摘要： The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

5. 发明公开

EP3517538A1 PYRAZOLOPYRIDINE DERIVATIVE HAVING GLP-1 RECEPTOR AGONIST EFFECT 有权
公开(公告)号：EP3517538A1
公开(公告)日：2019-07-31
申请号：EP17853220.6
申请日：2017-09-26
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： YOSHINO, Hitoshi , TSUCHIYA, Satoshi , MATSUO, Atsushi , SATO, Tsutomu , NISHIMOTO, Masahiro , OGURI, Kyoko , OGAWA, Hiroko , NISHIMURA, Yoshikazu , FURUTA, Yoshiyuki , KASHIWAGI, Hirotaka , HORI, Nobuyuki , KAMON, Takuma , SHIRAISHI, Takuya , YOSHIDA, Shoshin , KAWAI, Takahiro , TANIDA, Satoshi , AOKI, Masahide
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P25/16 , A61P25/28 , C07D519/00
摘要： The present invention provides a compound having the basic structure shown by Formula (I) in which the indole ring and the pyrazolopyridine structure is bound through a substituent, a salt thereof or a solvate of either the compound or a salt of the compound, as well as a preventative agent or a therapeutic agent for non-insulin-dependent diabetes mellitus (Type 2 diabetes) or obesity containing such compound, salt or solvate as an active ingredient.

6. 发明公开

EP2072522A1 THIOGLUCOSE SPIROKETAL DERIVATIVE AND USE THEREOF AS THERAPEUTIC AGENT FOR DIABETES 审中-公开
标题翻译：维生素D类药物治疗糖尿病 - 治疗
公开(公告)号：EP2072522A1
公开(公告)日：2009-06-24
申请号：EP07829669.6
申请日：2007-10-12
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： SATO, Tsutomu
IPC分类号： C07H7/06 , A61K31/7048 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/00 , A61P27/02 , A61P31/04 , A61P43/00
CPC分类号： C07H7/06
摘要： The present invention provides a compound represented by Formula (II):

wherein R 1 , R 2 , R 3 , and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and - C(=O)Rx; Rx is an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 is an optionally substituted aromatic carbocyclic ring, or an optionally substituted aromatic heterocyclic ring which may form a condensed ring; Q is - (CH 2 ) m -(L) p - or -(L) p -(CH 2 ) m -; m is an integer selected from 0 to 2, n is an integer selected from 1 and 2, and p is an integer selected from 0 and 1; L is -O-, -S- or -NR 5 -; A is an optionally substituted aryl group or an optionally substituted heteroaryl group; and a prodrug thereof and a pharmaceutically acceptable salt thereof, and a pharmaceutical agent or a pharmaceutical composition, which comprises the compound.
摘要翻译：本发明提供由式（II）表示的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，任选取代的C 1 -C 6烷基，任选取代的C 7〜14芳烷基和-C（= O）Rx; Rx是任选取代的C 1 -C 6烷基，任选取代的芳基，任选取代的杂芳基，任选取代的C 1 -C 6烷氧基或-NReRf; Ar 1是任选取代的芳族碳环，或可以形成稠环的任选取代的芳族杂环; Q是 - （CH 2）m - （L）p - 或 - （L）p - （CH 2）m - ; m是选自0至2的整数，n是选自1和2的整数，p是选自0和1的整数; L是-O - ， - S-或-NR 5 - ; A是任选取代的芳基或任选取代的杂芳基; 和其前药和药学上可接受的盐，以及包含该化合物的药物或药物组合物。

7. 发明公开

EP4349840A3 PYRAZOLOPYRIDINE DERIVATIVE HAVING GLP-1 RECEPTOR AGONIST EFFECT 审中-实审
公开(公告)号：EP4349840A3
公开(公告)日：2024-07-10
申请号：EP24154118.4
申请日：2017-09-26
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： YOSHINO, Hitoshi , TSUCHIYA, Satoshi , MATSUO, Atsushi , SATO, Tsutomu , NISHIMOTO, Masahiro , OGURI, Kyoko , OGAWA, Hiroko , NISHIMURA, Yoshikazu , FURUTA, Yoshiyuki , KASHIWAGI, Hirotaka , HORI, Nobuyuki , KAMON, Takuma , SHIRAISHI, Takuya , YOSHIDA, Shoshin , KAWAI, Takahiro , TANIDA, Satoshi , AOKI, Masahide
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5386 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P25/16 , A61P25/28 , C07D519/00 , C07D413/14
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/5386 , C07D519/00 , A61P1/16 , A61P3/06 , A61P3/04 , A61P9/10 , A61P25/16 , A61P25/28 , A61P3/10 , C07D471/04 , Y02A50/30 , C07D413/14
摘要： The present invention provides a a process for manufacturing a compound of formula (Ia), or a pharmaceutically acceptable salt thereof:

8. 发明公开

EP2048152A1 FUSED RING SPIROKETAL DERIVATIVE AND USE THEREOF AS DRUG FOR TREATING DIABETES 审中-公开
标题翻译： SPIROKETALDERIVATE稠环和其作为药物治疗糖尿病
公开(公告)号：EP2048152A1
公开(公告)日：2009-04-15
申请号：EP07791496.8
申请日：2007-07-27
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： SATO, Tsutomu , OHTAKE, Yoshihito , NISHIMOTO, Masahiro , EMURA, Takashi , KOBAYASHI, Takamitsu , YAMAGUCHI, Marina , TAKAMI, Kyouko
IPC分类号： C07H19/01 , A61K31/7048 , A61K31/7056 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07H19/01
摘要： Provided are a compound represented by Formula (I):

wherein R 1 , R 2 , R 3 , and R 4 are each independently selected from a hydrogen atom, a C 1-6 alkyl group which may be substituted, a C 7-14 aralkyl group which may be substituted and -C(=O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f).

, or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供由式（I）表示的化合物：其中R 1，R 2，R 3，和R 4各自独立地选自氢原子，可被取代的C 1-6烷基团，一个C 7-14 可被取代的芳烷基和基团-C（= O）的Rx; n表示选自1和2选择的整数; 和环Ar为从由下式（A）至（f）表示的基团。或其前药或其药学上可接受的盐以及药物制剂和含有寻求的化合物或其前药的药物组合物，或其药学上可接受的盐。

9. 发明公开

EP1852439A1 SPIROKETAL DERIVATIVE AND USE THEREOF AS DIABETIC MEDICINE 有权
标题翻译： SPIROKETAL-DERIVAT UND DESSEN VERWENDUNG ALS DIABETES-HEILMITTEL
公开(公告)号：EP1852439A1
公开(公告)日：2007-11-07
申请号：EP06712450.3
申请日：2006-01-27
申请人： CHUGAI SEIYAKU KABUSHIKI KAISHA
发明人： KOBAYASHI, Takamitsu , SATO, Tsutomu , NISHIMOTO, Masahiro
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07D311/96 , C07D491/153 , C07D493/10 , C07H19/01
摘要： The present invention provides a compound of Formula (I):

wherein R 1 , R 2 , R 3 and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and -C(=O)Rx; Rx represents an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents -(CH 2 ) m -(L) p - or -(L)p-(CH 2 ) m -; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents -O-, -S- or -NR 5 -; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.
摘要翻译：本发明提供式（I）的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，任选取代的C 1 -C 6烷基，任选取代的C 7 - C 14芳烷基和-C（= O）Rx; Rx表示任选取代的C 1 -C 6烷基，任选取代的芳基，任选取代的杂芳基，任选取代的C 1 -C 6烷氧基或-NReRf; Ar 1表示任选取代的芳族碳环或任选单取代的芳族杂环; Q表示 - （CH 2）m - （L）p - 或 - （L）p-（CH 2）m - ; m表示选自0至2的整数，n表示选自1和2的整数，p表示选自0和1的整数; L表示-O - ， - S-或-NR 5 - ; A表示任选取代的芳基或任选取代的杂芳基，其前药及其药学上可接受的盐以及包含这种化合物的药物组合物或药物组合物。

10. 发明公开

EP3072897A1 SPIROKETAL DERIVATIVES AND USE THEREOF AS DIABETIC MEDICINE 有权
标题翻译： DEREN VERWENDUNG ALS DIABETES-HEILMITTEL的SPIROKETAL-DERIVATE
公开(公告)号：EP3072897A1
公开(公告)日：2016-09-28
申请号：EP16161071.2
申请日：2006-01-27
申请人： Chugai Seiyaku Kabushiki Kaisha
发明人： KOBAYASHI, Takamitsu , SATO, Tsutomu , NISHIMOTO, Masahiro
IPC分类号： C07H19/01 , A61K31/7048 , A61P3/04 , A61P3/10 , A61P43/00
CPC分类号： C07D311/96 , C07D491/153 , C07D493/10 , C07H19/01
摘要： The present invention provides a compound of Formula (I):

wherein R 1 , R 2 , R 3 and R 4 are each independently selected from a hydrogen atom, an optionally substituted C 1 -C 6 alkyl group, an optionally substituted C 7 -C 14 aralkyl group and -C(=O)Rx; Rx represents an optionally substituted C 1 -C 6 alkyl group, an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted C 1 -C 6 alkoxy group or -NReRf; Ar 1 represents an optionally substituted aromatic carbocyclic ring or an optionally mono-substituted aromatic heterocyclic ring; Q represents -(CH 2 ) m -(L) p - or -(L) p -(CH 2 ) m -; m represents an integer selected from 0 to 2, n represents an integer selected from 1 and 2, and p represents an integer selected from 0 and 1; L represents -O-, -S- or -NR 5 -; and A represents an optionally substituted aryl group or an optionally substituted heteroaryl group, a prodrug thereof and a pharmaceutically acceptable salt thereof, as well as a pharmaceutical preparation or pharmaceutical composition comprising such a compound.
摘要翻译：本发明提供式（I）的化合物：其中R 1，R 2，R 3和R 4各自独立地选自氢原子，任选取代的C 1 -C 6烷基，任选取代的C 7 - C 14芳烷基和-C（= O）Rx; Rx表示任选取代的C 1 -C 6烷基，任选取代的芳基，任选取代的杂芳基，任选取代的C 1 -C 6烷氧基或-NReRf; Ar 1表示任选取代的芳族碳环或任选单取代的芳族杂环; Q表示 - （CH 2）m - （L）p - 或 - （L）p - （CH 2）m - m表示选自0至2的整数，n表示选自1和2的整数，p表示选自0和1的整数; L表示-O - ， - S-或-NR 5 - ; A表示任选取代的芳基或任选取代的杂芳基，其前药及其药学上可接受的盐以及包含这种化合物的药物组合物或药物组合物。

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