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1. 发明申请

US20050222159A1 Pyrazine derivatives and pharmaceutical use thereof 失效
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：US20050222159A1
公开(公告)日：2005-10-06
申请号：US11087761
申请日：2005-03-24
申请人： Hideo Tsutsumi , Seiichiro Tabuchi , Masatoshi Minagawa , Atsushi Akahane
发明人： Hideo Tsutsumi , Seiichiro Tabuchi , Masatoshi Minagawa , Atsushi Akahane
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/14 , C07D487/04 , C07D498/08 , A61K31/501 , C07D43/04
CPC分类号： C07D417/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D487/04
摘要： A pyrazine derivative of the following formula (I): wherein R1 is hydrogen or optionally substituted lower alkyl; X is hydrogen, halogen, hydroxy, cyano, acyl, or amino, aryl, heterocyclic group or the like; Y is hydrogen, halogen, hydroxy, acyl, amino, or the like; Z is aryl or heteroaryl, each of which is optionally substituted; or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物：其中R 1是氢或任选取代的低级烷基; X是氢，卤素，羟基，氰基，酰基或氨基，芳基，杂环基等; Y是氢，卤素，羟基，酰基，氨基等; Z是芳基或杂芳基，其各自任选被取代; 或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

2. 发明授权

US07265120B2 Pyrazine derivatives and pharmaceutical use thereof 失效
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：US07265120B2
公开(公告)日：2007-09-04
申请号：US11087761
申请日：2005-03-24
申请人： Hideo Tsutsumi , Seiichiro Tabuchi , Masatoshi Minagawa , Atsushi Akahane
发明人： Hideo Tsutsumi , Seiichiro Tabuchi , Masatoshi Minagawa , Atsushi Akahane
IPC分类号： C07D403/04 , C07D403/14 , A61K31/497 , A61P25/24
CPC分类号： C07D417/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D487/04
摘要： A pyrazine derivative of the following formula (I): wherein R1 is hydrogen or optionally substituted lower alkyl; X is hydrogen, halogen, hydroxy, cyano, acyl, or amino, aryl, heterocyclic group or the like; Y is hydrogen, halogen, hydroxy, acyl, amino, or the like; Z is aryl or heteroaryl, each of which is optionally substituted; or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物：其中R 1是氢或任选取代的低级烷基; X是氢，卤素，羟基，氰基，酰基或氨基，芳基，杂环基等; Y是氢，卤素，羟基，酰基，氨基等; Z是芳基或杂芳基，其各自任选被取代; 或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

3. 发明授权

US06346527B1 Guanidine derivatives 失效
标题翻译：胍衍生物
公开(公告)号：US06346527B1
公开(公告)日：2002-02-12
申请号：US09674006
申请日：2000-10-24
申请人： Kohei Takenaka , Yoshikazu Inoue , Masatoshi Minagawa , Atsushi Akahane
发明人： Kohei Takenaka , Yoshikazu Inoue , Masatoshi Minagawa , Atsushi Akahane
IPC分类号： C07D31308
CPC分类号： C07D313/08
摘要： A compound of the formula: wherein R1 is hydrogen or halogen, R2 is hydroxy, acyl(lower)alkoxy, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkylthio(lower)alkyl, mono(or di or tri)halo(lower)alkyl, (ethoxycarbonyl)amino, sulfamoylamino, (dimethylsulfamoyl)amino, N,N-di(lower)alkylamino(lower)alkyl, hydroxyimino(lower)alkyl, lower alkoxyimino(lower)alkyl, acyl, lower alkoxycarbonyl, carbamoyl, di(lower)alkylcarbamoyl, (amino(lower)alkyl)carbamoyl, N,N-di(lower)alkylamino(lower)alkylcarbamoyl, guanidinocarbonyl, morpholinylsulfonyl, sulfamoyl, lower alkylsulfamoyl, (lower alkylsulfonyl)(lower)alkyl, guanidinocarbonyl(lower)alkenyl, lower alkylthio, cyano, acyl(lower)alkyl, acyl(lower)alkenyl, aryl which has one or more substituent(s) or a heterocyclic group which has one or more substituent(s), and X is —O—, or a salt thereof.
摘要翻译：下式化合物：其中R 1是氢或卤素，R 2是羟基，酰基（低级）烷氧基，羟基（低级）烷基，低级烷氧基（低级）烷基，低级烷硫基（低级）烷基，单（或二或三）卤素（低级）烷基，（乙氧基羰基）氨基，氨磺酰基氨基，（二甲基氨磺酰基）氨基，N，N-二（低级）烷基氨基（低级）烷基，羟基亚氨基（低级）烷基，低级烷氧基亚氨基（低级）烷基，酰基，低级烷氧基羰基，（低级）烷基氨基甲酰基，（氨基（低级）烷基）氨基甲酰基，N，N-二（低级）烷基氨基（低级）烷基氨基甲酰基，胍基羰基，吗啉基磺酰基，氨磺酰基，低级烷基氨磺酰基，（低级烷基磺酰基）（低级）烷基，胍基羰基低级）烯基，低级烷硫基，氰基，酰基（低级）烷基，酰基（低级）烯基，具有一个或多个取代基的芳基或具有一个或多个取代基的杂环基，X是-O- ，或其盐。

4. 发明授权

US06812235B2 Beta-alanine derivatives and their use as receptor anatgonists 失效
标题翻译： β-丙氨酸衍生物及其作为受体拮抗剂的用途
公开(公告)号：US06812235B2
公开(公告)日：2004-11-02
申请号：US10182909
申请日：2002-08-02
申请人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Masatoshi Minagawa , Toshiaki Aoki , Kayoko Harada , Jiro Seki
发明人： Mitsuru Ohkubo , Satoru Kuroda , Hideko Nakamura , Masatoshi Minagawa , Toshiaki Aoki , Kayoko Harada , Jiro Seki
IPC分类号： A61K31445
CPC分类号： C07K5/0202 , A61K38/00 , C07D211/60 , Y02P20/55
摘要： A beta-alanine derivative of the formula (I) wherein R1 is hydrogen atom or an amino protective group; A is a lower alkylene group or a lower alkenylene group; R2 is hydrogen atom or an amino group which may be substituted with an acyl group; R3 is hydrogen atom or an aryl or aralkyl group which may be substituted with one or more of hydroxy and/or lower alkoxy, a moiety represented by the formula (II), which is a bivalent N-containing 6- to 8-membered heterocyclic group, or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的β-丙氨酸衍生物，其中R 1是氢原子或氨基保护基; A是低级亚烷基或低级亚烯基; R 2是氢原子或可被酰基取代的氨基; R 3是氢原子或可以被一个或多个羟基和/或低级烷氧基取代的芳基或芳烷基，即由式（II）表示的部分，其是二价含N的6-8 杂环基或其药学上可接受的盐。

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