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1. 发明授权

US4668677A 4-phenylphthalazine derivatives, their preparation and their use as pharmaceuticals 失效
标题翻译： 4-苯基酞嗪衍生物，它们的制备及其作为药物的用途
公开(公告)号：US4668677A
公开(公告)日：1987-05-26
申请号：US722304
申请日：1985-04-11
申请人： Yasuhiro Morinaka , Katsuhiko Iseki , Toshiji Kanayama , Toshiaki Watanabe , Hiroyoshi Nishi
发明人： Yasuhiro Morinaka , Katsuhiko Iseki , Toshiji Kanayama , Toshiaki Watanabe , Hiroyoshi Nishi
IPC分类号： A61K31/50 , A61K31/502 , A61P7/02 , A61P9/00 , C07D237/34 , C07D237/30
CPC分类号： C07D237/34
摘要： Certain new 1-alkylamino-4-phenylphthalazine derivatives, 1-neopentylamino-4-phenylphthalazine and 1-(1-ethylpropylamino)-4-phenylphthalazine, having prominent activity to ameliorate circulatory disorders and prepared from the corresponding phthalazinones.
摘要翻译：某些新的1-烷基氨基-4-苯基酞嗪衍生物，1-新戊基氨基-4-苯基酞嗪和1-（1-乙基丙基氨基）-4-苯基酞嗪，具有改善循环障碍并由相应的2,3-二氮杂萘酮制备的活性。

2. 发明授权

US4857542A Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
标题翻译：循环障碍的预防和治疗组合物及治疗方法
公开(公告)号：US4857542A
公开(公告)日：1989-08-15
申请号：US122516
申请日：1987-11-19
申请人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Sakurai
发明人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Sakurai
IPC分类号： C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28 , C07D231/56
CPC分类号： C07D231/56 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28
摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms; or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group,or a pharmaceutically acceptable salt thereof as an acitve ingredient.The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor agaisnt lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
摘要翻译：一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基。或R 1和R 2一起表示具有3至5个碳原子的亚烷基; R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基，未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基，总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为acitve成分。本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抑制剂脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

3. 再颁专利

USRE35801E Prophylactic and therapeutic composition for circulatory disorders and method of treatment 失效
标题翻译：循环障碍的预防和治疗组合物及治疗方法
公开(公告)号：USRE35801E
公开(公告)日：1998-05-19
申请号：US309558
申请日：1994-09-20
申请人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Nakajima (nee Sakurai)
发明人： Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Yasuhiro Morinaka , Katsuhiko Iseki , Hiroko Nakajima (nee Sakurai)
IPC分类号： C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28 , C07D231/56 , A61K31/415
CPC分类号： C07D231/56 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/28
摘要： A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 5 to 7 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, a benzyl group, a naphthyl group, or a phenyl group which is unsubstituted or substituted with 1 to 3 substituents which are the same or different selected from the group consisting of alkyl groups having 1 to 5 carbon atoms, alkoxy groups having 1 to 5 carbon atoms, hydroxyalkyl groups having 1 to 3 carbon atoms, alkoxycarbonyl groups having total carbon number of 2 to 5, alkylmercapto groups having 1 to 3 carbon atoms, alkylamino groups having 1 to 4 carbon atoms, dialkylamino groups having total carbon number of 2 to 8, halogen atoms, trifluoromethyl group, carboxyl group, cyano group, hydroxyl group, nitro group, amino group and acetamide group, or a pharmaceutically acceptable salt thereof as an active ingredient. The agent of the present invention is useful as a prophylactic and therapeutic agent for circulatory disorders, particularly as an inhibitor against lipid peroxidation and/or an agent for normalizing cerebral dysfunctions.
摘要翻译：一种循环系统疾病的预防和治疗剂，其包含下式的吡唑啉酮衍生物：其中R 1表示氢原子，芳基，具有1至5个碳原子的烷基或具有总碳数的烷氧基羰基烷基 3至6; R 2表示氢原子，芳氧基，芳基巯基，碳原子数1〜5的烷基或碳原子数1〜3的羟烷基，或者R 1和R 2一起表示碳原子数3〜5的亚烷基。 R3表示氢原子，碳原子数1〜5的烷基，碳原子数5〜7的环烷基，碳原子数1〜3的羟烷基，苄基，萘基或苯基，未取代或被1〜3个选自碳原子数1〜5的烷基，碳原子数为1〜5的烷氧基，碳原子数1〜3的烷氧基，碳原子数1〜3的烷氧基，烷氧基羰基，总碳数为2至5，具有1至3个碳原子的烷基巯基，具有1至4个碳原子的烷基氨基，总碳数为2至8的二烷基氨基，卤素原子，三氟甲基，羧基，氰基，羟基基团，硝基，氨基和乙酰胺基，或其药学上可接受的盐作为活性成分。本发明的药剂可用作循环障碍的预防和治疗剂，特别是作为抗脂质过氧化作用的抑制剂和/或用于使脑功能障碍正常化的药剂。

4. 发明授权

US4990619A Pyrazoline derivatives 失效
标题翻译：吡唑啉衍生物
公开(公告)号：US4990619A
公开(公告)日：1991-02-05
申请号：US451526
申请日：1989-12-18
申请人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
发明人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
IPC分类号： A61K31/415 , A61K31/44 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , A61K31/415 , A61K31/44 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14
摘要： A lipid-peroxide formation inhibitor useful as a preventive medicine and/or therapeutic medicine against various ischemic diseases and accompanying diseases such as various brain diseases, heart diseases and peripheral circulatory diseases and novel pyrazolone derivatives having such inhibitory activity and their pharmaceutically acceptable salts.

5. 发明授权

US5089515A Lipid-peroxide formation inhibiting composition and novel compounds useful therefor 失效
标题翻译：脂肪过氧化物形成抑制组合物和有用的新型化合物
公开(公告)号：US5089515A
公开(公告)日：1992-02-18
申请号：US606829
申请日：1990-10-31
申请人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
发明人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
IPC分类号： A61K31/415 , A61K31/44 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , A61K31/415 , A61K31/44 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14
摘要： A lipid-peroxide formation inhibitor useful as a preventive medicine and/or therapeutic medicine against various ischemic diseases and accompanying diseases such as various brain diseases, heart diseases and peripheral circulatory diseases and novel pyrazolone derivatives having such inhibitory activity and their pharmaceutically acceptable salts.

6. 发明授权

US4906644A Lipid-peroxide formation inhibiting composition and novel compounds useful therefor 失效
标题翻译：脂肪过氧化物形成抑制组合物及其有用的新化合物
公开(公告)号：US4906644A
公开(公告)日：1990-03-06
申请号：US123237
申请日：1987-11-20
申请人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
发明人： Yasuhiro Morinaka , Hiroyoshi Nishi , Toshiaki Watanabe , Satoshi Yuki , Hiroko Sakurai , Yoshio Hayashi , Nobuko Fukushima
IPC分类号： A61K31/415 , A61K31/44 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14 , C07D521/00
CPC分类号： C07D231/12 , A61K31/415 , A61K31/44 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D405/04 , C07D405/14 , C07D417/14
摘要： A lipid-peroxide formation inhibitor useful as a preventive medicine and/or therapeutic medicine against various ischemic diseases and accompanying diseases such as various brain diseases, heart diseases and peripheral circulatory diseases and novel pyrazolone derivatives having such inhibitory activity and their pharmaceutically acceptable salts.
摘要翻译：一种脂过氧化物形成抑制剂，其可用作预防药物和/或治疗各种缺血性疾病和伴随疾病如各种脑疾病，心脏病和周围循环系统疾病以及具有这种抑制活性的新型吡唑啉酮衍生物及其药学上可接受的盐。

7. 发明授权

US5116858A 4-imidazoline derivatives 失效
标题翻译： 4-咪唑啉衍生物
公开(公告)号：US5116858A
公开(公告)日：1992-05-26
申请号：US514832
申请日：1990-04-26
申请人： Yoshio Hayashi , Yasuhiro Morinaka , Masaki Shinoda , Hiroyoshi Nishi , Kazutoshi Watanabe , Nobuko Fukushima
发明人： Yoshio Hayashi , Yasuhiro Morinaka , Masaki Shinoda , Hiroyoshi Nishi , Kazutoshi Watanabe , Nobuko Fukushima
IPC分类号： A61K31/415 , A61P25/28 , A61P43/00 , C07D233/70
CPC分类号： C07D233/70
摘要： 4-Imidazoline derivatives represented by the formula (I) and/or formula (II): ##STR1## wherein R.sup.1 represents C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; R.sup.2 and R.sup.3 independently represent hydrogen, C.sub.3 -C.sub.20 alkyl, C.sub.3 -C.sub.20 alkenyl, C.sub.3 -C.sub.20 alkynyl, C.sub.3 -C.sub.20 alkoxy, C.sub.3 -C.sub.20 alkenyloxy, C.sub.3 -C.sub.20 alkynyloxy, C.sub.3 -C.sub.8 cyloalkyl, C.sub.1 -C.sub.10 alkylthio, or optionally substituted aralkyl or aralkyloxy; R.sup.4 represents C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; provided that R.sup.2 and R.sup.3 cannot be hydrogen at the same time, and pharmaceutically acceptable salts thereof. A pharmaceutical formulation containing the compound is also provided.

8. 发明授权

US4016193A Novel substituted phenylacetic acid derivatives and a process for preparing thereof 失效
标题翻译：新型取代苯乙酸衍生物及其制备方法
公开(公告)号：US4016193A
公开(公告)日：1977-04-05
申请号：US592946
申请日：1975-07-03
申请人： Toshihiko Kobayashi , Hidetoshi Hiranuma , Susumu Mizogami , Hiroyoshi Nishi , Mamoru Higuchi , Masatoshi Onoya
发明人： Toshihiko Kobayashi , Hidetoshi Hiranuma , Susumu Mizogami , Hiroyoshi Nishi , Mamoru Higuchi , Masatoshi Onoya
IPC分类号： A61K31/19 , A61K31/195 , A61K31/21 , A61K31/215 , C07C67/00 , C07C201/00 , C07C205/56 , C07C205/59 , C07C79/46
CPC分类号： C07C255/00 , C07C205/56
摘要： Novel substituted phenylacetic acid derivatives having the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or lower alkyl radical and R.sub.3 represents an alkenyl or alkynyl radical having 3 - 4 carbon atoms with excellent anti-inflammatory and analgesic activities.
摘要翻译：具有下式的新型取代的苯乙酸衍生物：其中R 1表示氢原子或低级烷基，R 3表示具有3-4个碳原子的烯基或炔基，具有优异的抗炎和止痛活性。

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