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1. 发明授权

US07407961B2 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：US07407961B2
公开(公告)日：2008-08-05
申请号：US10972340
申请日：2004-10-26
申请人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
发明人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): 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. 发明申请

US20050113387A1 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：US20050113387A1
公开(公告)日：2005-05-26
申请号：US10972340
申请日：2004-10-26
申请人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
发明人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
IPC分类号： A61K31/4965 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/497 , C07D43/02 , C07D43/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): 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

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。

4. 发明授权

US4460502A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4460502A
公开(公告)日：1984-07-17
申请号：US316653
申请日：1981-10-30
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Kada , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Kada , Masashi Hashimoto
IPC分类号： A61K38/00 , C07K5/02 , C07C103/52
CPC分类号： C07K5/0215 , A61K38/00 , Y02P20/55
摘要： The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms, having the structure ##STR1## wherein R.sup.1 is substituted or unsubstituted lower alkanoyl, or substituted or unsubstituted aralkanoyl,R.sup.2 and R.sup.3 are each carboxy or protected carboxy,R.sup.4 is hydrogen or an amino protective group, andR.sup.5 is hydrogen or lower alkyl, and their pharmaceutically acceptable salts.
摘要翻译：本发明涉及可用于治疗由病原微生物引起的感染性疾病的治疗性治疗的新型肽，其具有以下结构：其中R 1为取代或未取代的低级烷酰基或取代或未取代的芳烷酰基，R 2和R 3各自为羧基或被保护的羧基， R4是氢或氨基保护基，R5是氢或低级烷基，以及它们的药学上可接受的盐。

5. 发明授权

US5675011A Process for producing pyrrolidine derivative and salt thereof 失效
标题翻译：制备吡咯烷衍生物及其盐的方法
公开(公告)号：US5675011A
公开(公告)日：1997-10-07
申请号：US487521
申请日：1995-06-07
申请人： Kohji Kagara , Shunsuke Goto , Satoshi Yonishi , Muneharu Ikushima , Yukihisa Baba , Haruo Horiai
发明人： Kohji Kagara , Shunsuke Goto , Satoshi Yonishi , Muneharu Ikushima , Yukihisa Baba , Haruo Horiai
IPC分类号： C07D207/14 , C07D401/06
CPC分类号： C07D401/06 , C07D207/14
摘要： A process for producing a compound of the general formula: ##STR1## wherein R.sup.1 is heterocyclic(lower)alkyl, R.sup.2 is acyl, and R.sup.3 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, which is useful as a medicament or a salt thereof.
摘要翻译：制备通式如下的化合物的方法：其中R 1为杂环（低级）烷基，R 2为酰基，且R 3为羧基（低级）烷基或被保护的羧基（低级）烷基，其可用作药物或其盐。

6. 发明授权

US4497729A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4497729A
公开(公告)日：1985-02-05
申请号：US322902
申请日：1981-11-19
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno
IPC分类号： A61K38/00 , C07K5/02 , C07C103/52
CPC分类号： C07K5/0215 , A61K38/00
摘要： This invention relates to novel peptides, of pharmacological activity, of the formula: ##STR1## wherein R.sup.1 is heptanoyl, stearoyl, 2-hydroxypropionyl or 2-acetoxypropionyl,R.sup.2 is hydrogen or methyl,R.sup.3 is carboxy, benzyloxycarbonyl or hydroxymethyl,R.sup.4 is hydrogen or methyl,R.sup.5 is carboxy or hydroxymethyl,R.sup.6 is carboxy, methoxycarbonyl, 3-t-butoxycarbonylcarbazoyl or hydroxymethyl,R.sup.7 is hydrogen, 3-t-butoxycarbonyl or benzyloxycarbonyl, andn is an integer 0 or 1, with the proviso that when each of R.sup.3 and R.sup.6 is not simultaneously hydroxymethyl, then R.sup.5 is hydroxymethyl.
摘要翻译：本发明涉及具有下式的新颖的药物活性肽：其中R1是庚酰基，硬脂酰基，2-羟基丙酰基或2-乙酰氧基丙酰基，R2是氢或甲基，R3是羧基，苄氧羰基或羟甲基，R4是氢或甲基，R 5为羧基或羟甲基，R 6为羧基，甲氧基羰基，3-叔丁氧基羰基咔唑基或羟甲基，R7为氢，3-叔丁氧基羰基或苄氧基羰基，n为0或1的整数，条件是的R3和R6不同时为羟甲基，则R5为羟甲基。

7. 发明授权

US5543525A Process for producing pyrrolidine derivative and salt thereof 失效
标题翻译：制备吡咯烷衍生物及其盐的方法
公开(公告)号：US5543525A
公开(公告)日：1996-08-06
申请号：US360679
申请日：1994-12-30
申请人： Kohji Kagara , Shunsuke Goto , Satoshi Yonishi , Muneharu Ikushima , Yukihisa Baba , Haruo Horiai
发明人： Kohji Kagara , Shunsuke Goto , Satoshi Yonishi , Muneharu Ikushima , Yukihisa Baba , Haruo Horiai
IPC分类号： C07D207/14 , C07D401/06
CPC分类号： C07D401/06 , C07D207/14
摘要： A process for producing a compound of the general formula: ##STR1## wherein R.sup.1 is heterocyclic(lower)alkyl,R.sup.2 is acyl, andR.sup.3 is carboxy(lower)alkyl orprotected carboxy (lower) alkyl, which is useful as a medicament or a salt thereof.
摘要翻译： PCT No.PCT / JP93 / 00886 Sec。 371日期1994年12月30日第 102（e）日期1994年12月30日PCT提交1993年6月29日PCT公布。出版物WO94 / 01400 日本1994年1月20日制备通式如下的化合物的方法：其中R1是杂环（低级）烷基，R2是酰基，R3是羧基（低级）烷基或保护的羧基（低级）烷基，其是可用作药物或其盐。

8. 发明授权

US4493794A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4493794A
公开(公告)日：1985-01-15
申请号：US328997
申请日：1981-12-09
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Okada , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Okada , Masashi Hashimoto
IPC分类号： C07D263/44 , A61K31/195 , A61K31/22 , A61K31/27 , A61K38/00 , A61P31/04 , A61P35/00 , A61P37/04 , C07C231/02 , C07C237/10 , C07C237/12 , C07C237/22 , C07C271/22 , C07K5/02 , C07C103/52
CPC分类号： C07K5/0215 , A61K38/00 , Y02P20/55
摘要： The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms, having the structure: ##STR1## wherein R.sup.1 is hydrogen, substituted or unsubstituted alkanoyl, or substituted or unsubstituted aralkanoyl,R.sup.2 is carboxy or protected carboxy,R.sup.3 is carboxy, protected carboxy, carbamoyl, or carboxy or protected carboxy(lower)alkylcarbamoyl,R.sup.4 is carboxy, protected carboxy or carbamoyl, andR.sup.5 is hydrogen or an amino protective group, with proviso that at least one of R.sup.3 and R.sup.4 is always carbamoyl and their pharmaceutically acceptable salts.
摘要翻译：本发明涉及可用于治疗由病原微生物引起的感染性疾病的新型肽，其具有以下结构：其中R 1为氢，取代或未取代的烷酰基或取代或未取代的芳烷酰基，R 2为羧基或被保护的羧基，R 3 羧基，保护的羧基，氨基甲酰基或羧基或受保护的羧基（低级）烷基氨基甲酰基，R4是羧基，保护的羧基或氨基甲酰基，R5是氢或氨基保护基，条件是R3和R4中的至少一个总是氨基甲酰基及其药学上可接受的盐。

9. 发明授权

US4476050A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4476050A
公开(公告)日：1984-10-09
申请号：US341057
申请日：1982-01-20
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Okada , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Satoshi Yonishi , Hidekazu Takeno , Satoshi Okada , Masashi Hashimoto
IPC分类号： C07K1/113 , A61K38/00 , A61P31/04 , A61P37/04 , C07K5/02 , C07C103/52
CPC分类号： C07K5/0215 , A61K38/00 , Y02P20/55
摘要： The invention deals with novel peptides useful in the therapeutic treatment of infectious diseases caused by pathogenic microorganisms having the structure: ##STR1## wherein, R.sup.1 is hydrogen or acyl,R.sup.2 is lower alkyl,R.sup.3 is carboxy or protected carboxy,R.sup.4 is hydrogen or lower alkyl,R.sup.5 is hydrogen, alkyl or ar(lower)alkyl,R.sup.6 is carboxy or protected carboxy, andR.sup.7 is hydrogen or an amino protective group,and their pharmaceutically acceptable salts.
摘要翻译：本发明涉及用于治疗由具有以下结构的病原微生物引起的感染性疾病的新型肽：其中R1为氢或酰基，R2为低级烷基，R3为羧基或被保护的羧基，R4为氢或低级烷基，R 5为氢，烷基或芳（低级）烷基，R 6为羧基或被保护的羧基，R 7为氢或氨基保护基，及其药学上可接受的盐。

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