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1. 发明授权

US5132454A Oxamic acid compounds and pharmaceutical compositions for use in improvement of damaged cerebral functions of brain 失效
标题翻译：用于改善脑损伤的神经功能的含氧化合物和药物组合物
公开(公告)号：US5132454A
公开(公告)日：1992-07-21
申请号：US662192
申请日：1991-02-28
申请人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
发明人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
IPC分类号： A61K31/19 , A61P9/00 , A61P25/28 , C07C231/12 , C07C233/36 , C07C233/56
CPC分类号： C07C233/56
摘要： A method of inhibiting the abnormal postnatal axial growth of the eye of a maturing animal during conditions ordinarily leading to said abnormal growth, which comprises (1) determining the neurochemical present in the retina of said eye, e.g., dopamine, the concentration of which is reduced during said conditions, and (2) administering to said eye during postnatal maturation effective amounts of said neurochemical, its agonist or its antagonist.

2. 发明授权

US5066677A Novel oxamic acid compounds and pharmaceutical composition for use in improvement of damaged cerebral functions of brain 失效
标题翻译：新型含氧化合物和药物组合物用于改善脑损伤的神经功能
公开(公告)号：US5066677A
公开(公告)日：1991-11-19
申请号：US489358
申请日：1990-07-06
申请人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
发明人： Yasuo Sato , Shinsuke Kato , Takako Taniguchi , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
IPC分类号： A61K31/19 , A61P9/00 , A61P25/28 , C07C231/12 , C07C233/36 , C07C233/56
CPC分类号： C07C233/56
摘要： Novel N-(dialkylaminoalkyl)-substituted derivatives or N-(dialkylaminoalkyl)-N-alkyl-substituted derivatives of oxamic acid are now synthetized and found to exhibit the cerebral protective effect against cerebral anoxia in brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain.

3. 发明授权

US5232947A Oxamic acid compounds and pharmaceutical composition for use in improvement of damaged cerebral functions of brain 失效
标题翻译：用于改善脑损伤脑功能的恶唑酸化合物和药物组合物
公开(公告)号：US5232947A
公开(公告)日：1993-08-03
申请号：US754393
申请日：1991-09-04
申请人： Yasuo Sato , Shinsuke Katoh , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
发明人： Yasuo Sato , Shinsuke Katoh , Kunio Atsumi , Mitsugu Hachisu , Seiji Shibahara
IPC分类号： A61K31/19 , C07C233/56
CPC分类号： C07C233/56 , A61K31/19 , Y10S514/921
摘要： New N,N-di-alkyl- or alkenyl-substituted derivatives of oxamic acid of which the two alkyl or alkenyl groups are different from each other are now produced and found to exhibit the cerebral protective effect against cerebral anoxia in the brain of a mammalian animal, including human, and to be useful as an agent for improving or ameliorating the damaged or disturbed functions of the brain. Some known N,N-di-alkyl-substituted derivatives of oxamic acid or which the two alkyl groups are identical to each other are now also found to have similar, cerebral protective effect against cerebral anoxia and to be useful as an agent for improving the damaged functions of the brain.
摘要翻译：现在产生两个烷基或链烯基彼此不同的新的N，N-二 - 烷基 - 或链烯基取代的衍生物，并发现它们在哺乳动物脑中表现出对脑缺氧的脑保护作用动物，包括人类，并且可用作改善或改善大脑受损或紊乱功能的药剂。现在还发现一些已知的氧杂酸的N，N-二烷基取代的衍生物或两个烷基彼此相同，对脑缺氧具有相似的脑保护作用，并且可用作改善损坏大脑功能。

4. 发明授权

US4929633A Actinonin derivatives having physiological activities 失效
标题翻译：猕猴桃衍生物具有生理活性
公开(公告)号：US4929633A
公开(公告)日：1990-05-29
申请号：US203888
申请日：1988-06-08
申请人： Seiji Shibahara , Yukiko Takahashi , Yuji Matsuhashi , Mitsugu Hachisu , Shinichi Kondo , Tomio Takeuchi , Takaaki Aoyagi
发明人： Seiji Shibahara , Yukiko Takahashi , Yuji Matsuhashi , Mitsugu Hachisu , Shinichi Kondo , Tomio Takeuchi , Takaaki Aoyagi
IPC分类号： A61K31/40 , A61P25/28 , C07D207/08
CPC分类号： C07D207/08
摘要： As new compounds are provided a class of derivatives of actinonin represented by the general formula ##STR1## where R is a hydrogen or a lower alkyl group, which can exhibit the enzyme-inhibitory activities to a limited range of peptidases and show a remarkable enzyme-specificity, and which are effective to treat a cycloheximide-induced experimental amnesia in mice and are expectable to be useful to treat an amnesia in a mammalian animal, including human.

5. 发明授权

US5206384A Actinonin derivatives and pharmaceutically acceptable salts thereof 失效
标题翻译： ACTINONIN衍生物及其药物可接受的盐
公开(公告)号：US5206384A
公开(公告)日：1993-04-27
申请号：US754543
申请日：1991-09-04
申请人： Seiji Shibahara , Yoshiyuki Koyama , Shigeharu Inoue , Mitsugu Hachisu , Shinichi Kondo , Takaaki Aoyagi , Tomio Takeuchi
发明人： Seiji Shibahara , Yoshiyuki Koyama , Shigeharu Inoue , Mitsugu Hachisu , Shinichi Kondo , Takaaki Aoyagi , Tomio Takeuchi
IPC分类号： A61K31/40 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07D207/08 , C07D207/16 , C07K5/06 , C07K14/81 , C12N9/99
CPC分类号： C07D207/08 , C07D207/16
摘要： A novel actinonin derivative and a salt thereof are provided, which are useful as enzyme inhibitors and particularly have strong inhibitory activities against enkephalinase and angiotensin-converting enzymes. This actinonin derivative is represented by general formula (I): ##STR1## wherein R.sup.1 is sulfoxymethyl or carboxyl or a substituted carboxyl group selected from carboxamide, hydroxyaminocarbonyl and alkoxycarbonyl groups; and R.sup.2 is hydroxyl, alkoxy, hydroxyamino or sulfoxyamino group.

6. 发明授权

US06451800B1 Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
标题翻译：苯基哌嗪衍生物作为整合素α2β拮抗剂
公开(公告)号：US06451800B1
公开(公告)日：2002-09-17
申请号：US09601176
申请日：2000-07-28
申请人： Keiichi Ajito , Shoichi Murakami , Minoru Ishikawa , Mikio Yamamoto , Dai Kubota , Shuichi Gomi , Mitsugu Hachisu , Kiyoaki Katano
发明人： Keiichi Ajito , Shoichi Murakami , Minoru Ishikawa , Mikio Yamamoto , Dai Kubota , Shuichi Gomi , Mitsugu Hachisu , Kiyoaki Katano
IPC分类号： A61K31497
CPC分类号： C07D239/42 , C07D235/30 , C07D239/14
摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.
摘要翻译：本发明的目的是提供具有整合素α2拮抗活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基，卤素等; Q表示> C = O，> CH2等; R6表示H，烷基，芳烷基等; R 7表示H，炔基等; R8表示H，取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

7. 发明授权

US4418070A Cardiotonic agents 失效
标题翻译：强心剂
公开(公告)号：US4418070A
公开(公告)日：1983-11-29
申请号：US345672
申请日：1982-02-04
申请人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
发明人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
IPC分类号： A61K31/425 , A61K31/426 , A61P9/04 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40
CPC分类号： A61K31/425 , C07D277/34
摘要： A 5-phenylthiazole derivative represented by the formula: ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a hydroxyl group, an amino group or a mercapto group, or a pharmaceutically acceptable salt thereof shows a cardiac effect and a low toxicity to a human or animal with little influence on atrium rhythms.
摘要翻译：其中R表示氢原子，低级烷基，羟基，氨基或巯基的5-苯基噻唑衍生物或其药学上可接受的盐显示心脏效应和低对人或动物的毒性，对心房节律几乎没有影响。

8. 发明授权

US4719231A 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives and an analgesic agent comprising the same 失效
标题翻译： 3- [N-（巯基酰基）]氨基-4-芳基丁酸衍生物和包含其的止痛剂
公开(公告)号：US4719231A
公开(公告)日：1988-01-12
申请号：US735643
申请日：1985-05-20
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Masao Hirayama , Shinjiro Murata , Shunzo Fukatsu
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Masao Hirayama , Shinjiro Murata , Shunzo Fukatsu
IPC分类号： A61K31/165 , A61K31/195 , A61K31/215 , A61P25/04 , C07C67/00 , C07C313/00 , C07C323/60 , C07C327/32 , C07C153/017 , C07C149/41 , C07C149/43 , C07C153/023
CPC分类号： C07C323/60
摘要： New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).
摘要翻译：现在提供新的3- [N-（巯基乙酰基）]氨基-4-芳基丁酸衍生物，其显示镇痛活性并且有效增强已知镇痛化合物[D-ala2，met5] - 脑啡肽（DAME）诱导的镇痛）。

9. 发明授权

US4229448A 5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same 失效
标题翻译： 5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物
公开(公告)号：US4229448A
公开(公告)日：1980-10-21
申请号：US23504
申请日：1979-03-23
申请人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
发明人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
IPC分类号： C07D213/65 , C07D213/79 , C07D213/81 , A61K31/455
CPC分类号： C07D213/79 , C07D213/65 , C07D213/81
摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.
摘要翻译：由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基：其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基，酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基，制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

10. 发明授权

US4198416A 5-Alkoxy-picolinic esters and anti-hypertensive composition containing 5-alkoxy-picolinic esters 失效
标题翻译： 5-烷氧基 - 吡啶甲酸酯和含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物
公开(公告)号：US4198416A
公开(公告)日：1980-04-15
申请号：US944683
申请日：1978-09-22
申请人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
发明人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
IPC分类号： C07D213/65 , C07D213/79 , A61K31/44
CPC分类号： C07D213/79 , C07D213/65
摘要： 5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.
摘要翻译：由式（I）表示的5-烷氧基 - 吡啶甲酸酯：其中R表示具有1至6个碳原子的烷基，R 1表示未取代的苯基; 被一个或多个具有1至4个碳原子的烷基或乙酰基取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷氧基烷基; 茚满基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等），基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等原子）或其中烷基部分具有1〜3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸酯的方法和含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物。

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