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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. 发明申请

US20050004134A1 Thiazole derivative and pharmaceutical use thereof 审中-公开
标题翻译：噻唑衍生物及其药物用途
公开(公告)号：US20050004134A1
公开(公告)日：2005-01-06
申请号：US10494033
申请日：2002-11-08
申请人： Hideo Tsutsumi , Seiichiro Tabuchi , Atsushi Akahane , Hironobu Yasuda , Hiroki Omori , Kiyoshi Temmaru , Atsuhiko Zanka
发明人： Hideo Tsutsumi , Seiichiro Tabuchi , Atsushi Akahane , Hironobu Yasuda , Hiroki Omori , Kiyoshi Temmaru , Atsuhiko Zanka
IPC分类号： C07D237/16 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/18 , A61P3/04 , A61P3/10 , A61P7/02 , A61P7/06 , A61P7/10 , A61P9/00 , A61P9/02 , A61P9/06 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/06 , A61P13/12 , A61P19/06 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P29/02 , A61P37/04 , A61P43/00 , C07D417/04 , C07D417/14 , C07D521/00 , C07D417/02
CPC分类号： C07D233/56 , C07D231/12 , C07D249/08 , C07D417/04 , C07D417/14
摘要： A thiazole derivative of the formula (I): wherein R is a 1-optionally substituted-6-oxo-1,6-dihydro-3-pyridazinyl, R′ is an optionally substituted phenyl, and R2 is hydrogen, a group of the formula (i): wherein R4 is hydrogen, lower alkyl or lower alkenyl, and R5 is hydrogen, optionally substituted lower alkyl, acyl, cyclo(lower)alkyl, lower alkenyl, optionally substituted aryl or heterocyclic, or a group of the formula (ii): wherein X is oxygen or sulfur, R8 is hydrogen or lower alkyl, R9 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, lower alkoxy or mono- or di-lower alkylamino or R8 and R9 may combine together to form optionally substituted saturated N-containing heterocyclic, or a salt thereof.
摘要翻译：式（I）的噻唑衍生物：其中R是1-任选取代的-6-氧代-1,6-二氢-3-哒嗪基，R'是任选取代的苯基，R 2是氢，式（i）的基团：其中R 4是氢，低级烷基或低级烯基，R 5是氢，任选取代的低级烷基，酰基，环（低级）烷基，低级烯基，任选取代的芳基或杂环或式（ⅱ）的基团：其中X为氧或硫，R 8为氢或低级烷基，R 9为氢，任选取代的低级烷基，环（低级）烷基，低级烷氧基或单 - 或二 - 低级烷基氨基或R 8和R 9可以结合在一起形成任选取代的饱和含氮杂环或其盐。

4. 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。

5. 发明申请

US20050043315A1 Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them 审中-公开
标题翻译：氨基嘧啶化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US20050043315A1
公开(公告)日：2005-02-24
申请号：US10498016
申请日：2002-12-27
申请人： Hideo Tsutsumi , Satoshi Yonishi , Atsushi Akahane
发明人： Hideo Tsutsumi , Satoshi Yonishi , Atsushi Akahane
IPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , C07D43/02 , A61K31/501
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14
摘要： An aminopyrimidine compound of the following formula (I) wherein Q is (a) or (b) in which R and R′ are each optionally substituted aryl or heterocyclic group,R5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R1 is hydrogen, optionally substituted lower alkyl or cyclo(lower) alkyl which may be interrupted by an oxygen atom; R2 and R3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R2 and R3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and 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：其中Q为（a）或（b）的下式（I）的氨基嘧啶化合物，其中R和R'各自为任选取代的芳基或杂环基，R 5为氢，卤素，低级烷基，任选取代的羟基，可以形成含氮杂环基的任选取代的氨基，任选取代的巯基，低级烷基亚磺酰基或低级烷基磺酰基，X是氧或硫; R 1是氢，任选取代的可被氧原子间隔的低级烷基或环（低级）烷基; R 2和R 3各自独立地为氢，低级烷基，酰基，芳基或杂环（低级）烷基，R 2和R 3可以与它们所连接的N原子一起形成含氮杂环基; 或其盐。本发明的氨基嘧啶化合物（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。

6. 发明授权

US5296490A Pharmaceutically useful pyrazolopyridines 失效
标题翻译：药学上有用的吡唑并吡啶
公开(公告)号：US5296490A
公开(公告)日：1994-03-22
申请号：US968664
申请日：1992-10-30
申请人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
发明人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
IPC分类号： A61K31/435 , A61P7/02 , A61P7/10 , A61P9/04 , A61P9/12 , A61P13/02 , A61P15/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The disclosure concerns pyrazolopyridine compounds of the formulawherein the variables are defined in the specification. The compounds are useful as a diuretic, anti-hypertensive agent, etc.
摘要翻译：本公开涉及下式的吡唑并吡啶化合物，其中变量在说明书中定义。该化合物可用作利尿剂，抗高血压剂等。

7. 发明授权

US4925849A Pharmaceutically useful pyrazolopyridines 失效
标题翻译：药学上有用的吡唑并吡啶
公开(公告)号：US4925849A
公开(公告)日：1990-05-15
申请号：US202526
申请日：1988-06-06
申请人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
发明人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
IPC分类号： A61K31/435 , A61P7/02 , A61P7/10 , A61P9/04 , A61P9/12 , A61P13/02 , A61P15/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The disclosure deals with a pyrazolopyridine compound of the formula ##STR1## wherein the variables are defined in the specification. The compounds are useful as a diuretic, antihypertensive agent, etc.

8. 发明授权

US5155114A Method of treatment using pyrazolopyridine compound 失效
标题翻译：使用吡唑并吡啶化合物治疗的方法
公开(公告)号：US5155114A
公开(公告)日：1992-10-13
申请号：US715460
申请日：1991-06-14
申请人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
发明人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04
摘要： The invention relates to a method for the prevention and/or treatment of renal toxicity, nephrosis or nephritis, which comprises administering a pyrazolopyridine compound of the formula: ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is unsaturated heterocyclic group which contains at least one heteroatom selected from the group consisting of N, O and S, which may have one or more suitable substituent(s), or a pharmaceutically acceptable salt thereof to a human being or an animal.
摘要翻译：本发明涉及一种用于预防和/或治疗肾毒性，肾病或肾炎的方法，其包括施用下式的吡唑并吡啶化合物：其中R1是芳基，R2是不饱和杂环基，其含有至少一个选自N，O和S的杂原子，其可以具有一个或多个合适的取代基或其药学上可接受的盐给人或动物。

9. 发明授权

US4985444A Pyrazolopyridine compound and processes for preparation thereof 失效
标题翻译：吡唑并吡啶化合物及其制备方法
公开(公告)号：US4985444A
公开(公告)日：1991-01-15
申请号：US466929
申请日：1990-01-18
申请人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
发明人： Youichi Shiokawa , Atsushi Akahane , Hirohito Katayama , Takafumi Mitsunaga
IPC分类号： A61K31/435 , A61K31/437 , A61K31/44 , A61K31/50 , A61K31/505 , A61P3/06 , A61P7/02 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P19/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P29/00 , A61P43/00 , C07D471/04 , C07D513/04 , C07D519/00 , C07D521/00
CPC分类号： C07D471/04
摘要： The invention relates to pyrazolopyridine compounds for the treatment of melancholia, heart failure, hypertension, renal insufficiency, edema, obesity, bronchial asthma, gout, hyperuricemia, sudden infant death syndrome, immunosuppression, diabetes, myocardiac infection, thrombosis, obstruction, arteriosclerosis obliterans, thrombophlebitis, cerebral infarction, transient ischemic attack or angina pectoris, said compounds being of the formula ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is unsaturated heterocyclic group which contains at least one heteroatom selected from the group consisting of N, O and S, which may have one or more suitable substituent(s),or a pharmaceutically acceptable salt thereof.

10. 发明授权

US4563455A Antiulcer fused imidazole compounds 失效
标题翻译：抗溃疡融合咪唑化合物
公开(公告)号：US4563455A
公开(公告)日：1986-01-07
申请号：US587981
申请日：1984-03-09
申请人： Ikuo Ueda , Masayuki Kato , Masanobu Nagano , Atsushi Akahane
发明人： Ikuo Ueda , Masayuki Kato , Masanobu Nagano , Atsushi Akahane
IPC分类号： A61K31/415 , A61P1/04 , C07D235/10 , C07D235/12 , C07D401/06 , C07D403/06 , C07D417/06 , C07D471/04 , C07D521/00 , A61K31/53
CPC分类号： C07D231/12 , C07D233/56 , C07D235/10 , C07D235/12 , C07D249/08 , C07D401/06 , C07D403/06 , C07D417/06 , C07D471/04
摘要： New fused imidazole compounds of the formula: ##STR1## wherein A is lower alkylene,R.sup.1 is hydrogen, lower alkyl, lower alkoxy or halogen,R.sup.2 is hydrogen, lower alkyl, cyclo(lower)alkyl, pyridyl, ar(lower)alkyl which may be substituted with halogen, or aryl which may be substituted with lower alkyl, lower alkoxy, hydroxy or halogen,R.sup.3 is N-containing unsaturated heterocyclic group which may be substituted with lower alkyl or amino, andY is .dbd.C-- or .dbd.N--,and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same.These derivatives and salts thereof are useful as antiulcer agents.
摘要翻译：其中A为低级亚烷基，R 1为氢，低级烷基，低级烷氧基或卤素，R 2为氢，低级烷基，环（低级）烷基，吡啶基，Ar（低级）烷基，可以被卤素取代，或可以被低级烷基，低级烷氧基，羟基或卤素取代的芳基，R3是可被低级烷基或氨基取代的含N不饱和杂环基，Y是=或= N - 及其药学上可接受的盐，及其制备方法和包含其的药物组合物。这些衍生物和其盐可用作抗溃疡剂。

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