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1. 发明公开

EP2974730A1 DRUG FOR RESPIRATORY DISEASES 有权
标题翻译：药物治疗呼吸道疾病
公开(公告)号：EP2974730A1
公开(公告)日：2016-01-20
申请号：EP14763747.4
申请日：2014-03-13
申请人： Daiichi Sankyo Company, Limited
发明人： TAKAHASHI, Sakiko , DOMON, Yuki , KITANO, Yutaka , SHINOZUKA, Tsuyoshi
IPC分类号： A61K31/506 , A61P11/00 , A61P11/06 , A61P11/08 , A61P11/14
CPC分类号： A61K31/506 , A61K31/433 , A61K31/496
摘要： It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a pharmaceutical comprising a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof as an active ingredient:

Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group;
n: an integer of 1 to 3; and
the heteroaryl or aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group, and when the heteroaryl or aryl group has two such groups, the two groups are the same as or different from each other.
摘要翻译：旨在提供用于呼吸系统疾病或钠通道相关疾病的治疗剂和/或预防剂的治疗剂和/或预防剂。本发明提供药物，其含有下式（I）所示的化合物或其药理学上可接受的盐作为有效成分：Ar 1和Ar 2：杂芳基或芳基; R 1，R 2和R 3：氢原子，卤素原子，C 1 -C 6烷基，卤代C 1 -C 6烷基，羟基C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C7环烷基或氰基; R 4和R 5：氢原子，卤素原子，C 1 -C 6烷基，卤代C 1 -C 6烷基，羟基，羟基C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基， C3-C7环烷基或C1-C6烷氧基; n：1〜3的整数; 并且杂芳基或芳基任选具有一个或两个独立地选自卤素原子，C1-C6烷基，卤代C1-C6烷基，羟基，羟基C1-C6烷基，C1-C6烷基烷氧基C 1 -C 6烷基，C 3 -C 7环烷基，羧基，氰基，氨基，C 1 -C 3烷基氨基和二-C 1 -C 3烷基氨基，并且当杂芳基或芳基具有两个这样的组，两组彼此相同或不同。

2. 发明公开

EP2657219A1 Intermediate for producing bicyclic y-amino acid derivative 有权
标题翻译： Zwischenprodukt zur Herstellung eines bicyclischen y-Aminosäurederivats
公开(公告)号：EP2657219A1
公开(公告)日：2013-10-30
申请号：EP13177681.7
申请日：2008-09-25
申请人： Daiichi Sankyo Company, Limited
发明人： SHIMADA, Kousei , KAWAMURA, Asuka , ARAKAWA, Naohisa , DOMON, Yuki
IPC分类号： C07C49/627
CPC分类号： C07C229/32 , C07B2200/07 , C07C323/58 , C07C2601/04 , C07C2601/08 , C07C2602/20 , C07C2603/94
摘要： An intermediate represented by the general formula (1) is provided, useful for producing a bicyclic γ-amino acid derivative having excellent activity as an α 2 δ ligand:

wherein R 1 , R 2 , R 2' , R 4 , R 5 , R 8 and R 8' are each independently a hydrogen atom, and R 3 is a hydrogen atom, a methyl group, an ethyl group, a propyl group, or a butyl group.
摘要翻译：提供由通式（1）表示的中间体，其可用于制备作为±2'配体具有优异活性的双环-3-氨基酸衍生物：其中R 1，R 2，R 2'，R 4，R 5， R 8和R 8'各自独立地为氢原子，R 3为氢原子，甲基，乙基，丙基或丁基。

3. 发明授权

EP3144300B1 METHODS OF PRODUCING 4-CYCLOALKYLOXYBENZENESULFONAMIDES 有权
标题翻译：生产4-环烷氧基苯磺酰胺的方法
公开(公告)号：EP3144300B1
公开(公告)日：2017-12-20
申请号：EP16193142.3
申请日：2013-02-08
申请人： Daiichi Sankyo Company, Limited
发明人： SHINOZUKA, Tsuyoshi , KOBAYASHI, Hiroyuki , SUZUKI, Sayaka , TANAKA, Kyosuke , KIMOTO, Hiroko , DOMON, Yuki
IPC分类号： C07D285/08 , C07D417/12 , C07D403/12 , C07D401/12
CPC分类号： C07D403/12 , C07B2200/13 , C07D285/08 , C07D401/12 , C07D417/12 , Y02P20/55
摘要： It is intended to provide a therapeutic agent and/or a preventive agent for pain or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof: Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; n: an integer of 1 to 3; and the heteroaryl group or the aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-Cl-C3 alkylamino group, and when the heteroaryl group or the aryl group has two such groups, the two groups are the same as or different from each other.

4. 发明授权

EP2813491B1 CYCLOALKANE DERIVATIVE 有权转让
标题翻译： CYCLO的烷衍生物
公开(公告)号：EP2813491B1
公开(公告)日：2016-11-02
申请号：EP13746373.3
申请日：2013-02-08
申请人： Daiichi Sankyo Company, Limited
发明人： SHINOZUKA, Tsuyoshi , KOBAYASHI, Hiroyuki , SUZUKI, Sayaka , TANAKA, Kyosuke , KIMOTO, Hiroko , DOMON, Yuki
IPC分类号： C07D285/08 , C07D417/12 , C07D403/12 , C07D401/12 , A61K31/433 , A61K31/427 , A61K31/506 , A61P29/00 , A61P25/00
CPC分类号： C07D403/12 , C07B2200/13 , C07D285/08 , C07D401/12 , C07D417/12 , Y02P20/55
摘要： It is intended to provide a therapeutic agent and/or a preventive agent for pain or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof: Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; n: an integer of 1 to 3; and the heteroaryl group or the aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-Cl-C3 alkylamino group, and when the heteroaryl group or the aryl group has two such groups, the two groups are the same as or different from each other.

5. 发明授权

EP2657219B1 Intermediate for producing bicyclic y-amino acid derivative 有权
标题翻译： Zwischenprodukt zur Herstellung eines bicyclischen y-Aminosäurederivats
公开(公告)号：EP2657219B1
公开(公告)日：2014-12-10
申请号：EP13177681.7
申请日：2008-09-25
申请人： Daiichi Sankyo Company, Limited
发明人： SHIMADA, Kousei , KAWAMURA, Asuka , ARAKAWA, Naohisa , DOMON, Yuki
IPC分类号： C07C49/627 , C07C323/58 , C07C229/32
CPC分类号： C07C229/32 , C07B2200/07 , C07C323/58 , C07C2601/04 , C07C2601/08 , C07C2602/20 , C07C2603/94

6. 发明授权

EP2974730B1 DRUG FOR RESPIRATORY DISEASES 有权
标题翻译：药物治疗呼吸道疾病
公开(公告)号：EP2974730B1
公开(公告)日：2018-01-31
申请号：EP14763747.4
申请日：2014-03-13
申请人： Daiichi Sankyo Company, Limited
发明人： TAKAHASHI, Sakiko , DOMON, Yuki , KITANO, Yutaka , SHINOZUKA, Tsuyoshi
IPC分类号： A61K31/506 , A61P11/00 , A61P11/06 , A61P11/08 , A61P11/14
CPC分类号： A61K31/506 , A61K31/433 , A61K31/496
摘要： It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a pharmaceutical comprising a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; n: an integer of 1 to 3; and the heteroaryl or aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group, and when the heteroaryl or aryl group has two such groups, the two groups are the same as or different from each other.

7. 发明公开

EP3144300A1 METHODS OF PRODUCING 4-CYCLOALKYLOXYBENZENESULFONAMIDES 有权
标题翻译：生产4-环烷氧基苯磺酰胺的方法
公开(公告)号：EP3144300A1
公开(公告)日：2017-03-22
申请号：EP16193142.3
申请日：2013-02-08
申请人： Daiichi Sankyo Company, Limited
发明人： SHINOZUKA, Tsuyoshi , KOBAYASHI, Hiroyuki , SUZUKI, Sayaka , TANAKA, Kyosuke , KIMOTO, Hiroko , DOMON, Yuki
IPC分类号： C07D285/08 , C07D417/12 , C07D403/12 , C07D401/12
CPC分类号： C07D403/12 , C07B2200/13 , C07D285/08 , C07D401/12 , C07D417/12 , Y02P20/55
摘要： A method of producing a compound of formula (I) or a pharmacologically acceptable salt thereof, useful as a therapeutic agent and/or a preventive agent for pain or for a sodium channel associated disease:

Ar 1 and Ar 2 : a heteroaryl group or an aryl group, each optionally substituted; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; and n: an integer of 1 to 3, comprising a step of removing a protecting group P from the compound of formula (VI):

or a step of reacting a compound of formula (X) and a compound of formula (XI) :

wherein X represents a halogen atom.
摘要翻译：制备用作疼痛或钠通道相关疾病的治疗剂和/或预防剂的式（I）化合物或其药理学上可接受的盐的方法：Ar 1和Ar 2：杂芳基或芳基，各自任选被取代; R 1，R 2和R 3：氢原子，卤素原子，C 1 -C 6烷基，卤代C 1 -C 6烷基，羟基C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C7环烷基或氰基; R 4和R 5：氢原子，卤素原子，C 1 -C 6烷基，卤代C 1 -C 6烷基，羟基，羟基C 1 -C 6烷基，C 1 -C 6烷氧基C 1 -C 6烷基， C3-C7环烷基或C1-C6烷氧基; 并且n为1至3的整数，所述方法包括从式（VI）化合物除去保护基团P的步骤或使式（X）化合物与式（XI）化合物反应的步骤：其中 X代表卤素原子。

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