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1. 发明授权

US5447944A Carbamoyl-2-pyrrolidinone compounds 失效
标题翻译：氨基甲酰基-2-吡咯烷酮化合物
公开(公告)号：US5447944A
公开(公告)日：1995-09-05
申请号：US216244
申请日：1994-03-22
申请人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
发明人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
IPC分类号： C07D207/26 , C07D207/263 , C07D207/273 , C07D401/12 , C07D417/12 , A61K31/425 , A61K31/40 , A61K31/44 , C07D207/12
CPC分类号： C07D207/27 , C07D207/26 , C07D207/273 , C07D401/12 , C07D417/12
摘要： The present invention provides carbamoyl-2 -pyrrolidinone compounds useful as medicaments for improving cerebral functions and activating cerebral metabolism or protecting against anoxic brain damage.
摘要翻译：本发明提供了用作改善脑功能和激活脑代谢或防止缺氧性脑损伤的药物的氨基甲酰基-2-吡咯烷酮化合物。

2. 发明授权

US5229402A Carbamoyl-2-pyrrolidinone compounds 失效
标题翻译：卡巴酸-2-吡咯烷酮化合物
公开(公告)号：US5229402A
公开(公告)日：1993-07-20
申请号：US449923
申请日：1989-12-13
申请人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
发明人： Makoto Kajitani , Etsuo Hasegawa , Akihiro Kawaguchi , Junji Yamamoto , Katsuo Toide , Takaji Honna , Mitsugi Yasumoto , Nobuo Kasahara
IPC分类号： C07D207/26 , C07D207/263 , C07D207/273 , C07D401/12 , C07D417/12
CPC分类号： C07D207/27 , C07D207/26 , C07D207/273 , C07D401/12 , C07D417/12
摘要： The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.
摘要翻译： PCT No.PCT / JP89 / 00401 Sec。 371日期1989年12月13日第 102（e）日期1989年12月13日PCT提交1989年4月12日PCT公布。公开号WO89 / 09767 本发明提供具有下式（2）的氨基甲酰基-2-吡咯烷酮化合物，可用作治疗老年痴呆的药物，即作为脑功能改善剂和脑代谢激活剂或缺氧性脑（2）其中R1是氢原子，羟基或被羟基取代或未取代的低级烷基，R3是具有或没有低级烷氧基，低级烷基氨基，卤原子或卤代甲基的苯基，四氢萘基，吡啶基或噻唑基作为取代基。此外，本发明提供由式（1）表示的新型氨基甲酰基-2-吡咯烷酮化合物，其中R 1是氢原子，羟基或被羟基取代或未取代的低级烷基，R 2是苯基，四氢萘基，吡啶基或噻唑基具有或不具有甲氧基或低级烷基氨基作为取代基，条件是当R 1为氢原子或未取代的低级烷基时，R 2为未取代的苯基。

3. 发明授权

US5068235A Diazabicycloalkane derivative 失效
标题翻译： DIAZABICYCLOALKANE DERIVATIVE
公开(公告)号：US5068235A
公开(公告)日：1991-11-26
申请号：US566456
申请日：1990-08-16
申请人： Etsuo Hasegawa , Akihiro Kawaguchi , Makoto Kajitani , Mitsugi Yasumoto , Nobuo Kasahara , Junji Yamamoto
发明人： Etsuo Hasegawa , Akihiro Kawaguchi , Makoto Kajitani , Mitsugi Yasumoto , Nobuo Kasahara , Junji Yamamoto
IPC分类号： A61K31/415 , A61K31/425 , A61K31/435 , A61K31/505 , A61P25/28 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a diazabicycloalkane derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is phenyl group, thiazolyl group or furyl group, the phenyl group may have lower alkoxy, lower alkyl or halogen atom as a substituent, R.sup.2 is oxygen atom or sulfur atom, m is 3 or 4, n is 1 or 2.
摘要翻译： PCT No.PCT / JP89 / 01316 Sec。 371日期1990年8月16日 102（e）日期1990年8月16日PCT提交1989年12月27日PCT公布。公开号WO90 / 07509 日本1990年7月12日。本发明提供了具有下式的二氮杂双环烷烃衍生物，可用作治疗老年性痴呆的药物，即作为脑功能改善剂和脑代谢激活剂或缺氧性脑损伤保护剂。）其中R1是苯基，噻唑基或呋喃基，苯基可以具有低级烷氧基，低级烷基或卤原子作为取代基，R2是氧原子或硫原子，m是3或4，n是1或2。

4. 发明授权

US5206261A Oxindole derivative 失效
标题翻译： OXINDOLE DERIVATIVE
公开(公告)号：US5206261A
公开(公告)日：1993-04-27
申请号：US663960
申请日：1991-03-20
申请人： Akihiro Kawaguchi , Atsushi Sato , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
发明人： Akihiro Kawaguchi , Atsushi Sato , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
IPC分类号： A61K31/40 , A61K31/44 , C07D209/34 , C07D401/06 , C07D405/06
CPC分类号： C07D401/06 , C07D209/34 , C07D405/06
摘要： The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, nitrile group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.4 is 1-propylbutyl group; pyridyl group; or phenyl group which may be substituted by lower alkoxyl group, halogen atom, diethylamino group, benzyloxy group, trifluoromethyl group, nitrile group, nitro group or lower alkyl group.

5. 发明授权

US5214039A Bicyclolactam derivative for improving cerebral function 失效
标题翻译：双环内酰胺衍生物用于改善脑功能
公开(公告)号：US5214039A
公开(公告)日：1993-05-25
申请号：US925047
申请日：1992-08-05
申请人： Akihiro Kawaguchi , Atsushi Satoh , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
发明人： Akihiro Kawaguchi , Atsushi Satoh , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
IPC分类号： C07D209/34 , C07D209/46 , C07D209/52 , C07D215/22 , C07D215/227 , C07D221/04
CPC分类号： C07D215/227 , C07D209/34 , C07D209/46 , C07D209/52 , C07D221/04
摘要： The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.
摘要翻译：本发明提供了具有下式的双环内酰胺衍生物，可用作治疗老年痴呆的药物，即作为脑功能改善剂和脑代谢激活剂或缺氧性脑损伤保护剂。（1）其中R是苯甲酰基，可以被卤素原子，低级烷基，低级烷氧基，硝基，氰基或氨基取代; l为1或2; m为0或1; 并且n为0,1或2，条件是m和n不同时为0。

6. 发明授权

US5185344A Pharmaceutically useful bicyclolactam derivative 失效
标题翻译：药物有用的双酚A衍生物
公开(公告)号：US5185344A
公开(公告)日：1993-02-09
申请号：US768074
申请日：1991-10-01
申请人： Akihiro Kawaguchi , Atsushi Satoh , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
发明人： Akihiro Kawaguchi , Atsushi Satoh , Makoto Kajitani , Mitsugi Yasumoto , Junji Yamamoto
IPC分类号： A61K31/40 , C07D209/34 , C07D209/46 , C07D209/52 , C07D215/22 , C07D215/227 , C07D217/24 , C07D221/04 , C07D223/16
CPC分类号： C07D215/227 , C07D209/34 , C07D209/46 , C07D209/52 , C07D221/04
摘要： The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.
摘要翻译： PCT No.PCT / JP91 / 00116 Sec。 371日期1991年10月1日 102（e）1991年10月1日PCT 1991年1月30日PCT PCT。公开号WO91 / 11434 日本1991年8月8日。本发明提供具有下式的双环内酰胺衍生物，可用作治疗老年痴呆的药物，即作为脑功能改善剂和脑代谢活化剂或缺氧性脑损伤保护剂。）其中R是可以被卤素原子，低级烷基，低级烷氧基，硝基，氰基或氨基取代的苯甲酰基; l为1或2; m为0或1; 并且n为0,1或2，条件是m和n不同时为0。

7. 发明授权

US4696929A Derivative of piperazine having anti-allergic and anti-inflammatory action 失效
标题翻译：具有抗过敏和抗炎作用的哌嗪衍生物
公开(公告)号：US4696929A
公开(公告)日：1987-09-29
申请号：US809876
申请日：1985-12-17
申请人： Ichiro Yamawaki , Kazuo Ogawa , Naohiko Ono , Takaji Honna , Sekio Nagayama , Mitsugi Yasumoto
发明人： Ichiro Yamawaki , Kazuo Ogawa , Naohiko Ono , Takaji Honna , Sekio Nagayama , Mitsugi Yasumoto
IPC分类号： C07D405/12 , A61K31/495 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/28 , C07D403/12 , C07F7/18 , C12N9/99
CPC分类号： C07D209/28 , Y02P20/55
摘要： A piperazine derivative represented by the formula (I) below ##STR1## wherein R.sup.1 is lower alkyl or phenyl, R.sup.2 is hydrogen or lower alkyl, n is an integer of 2 to 10, is useful as an effective component of anti-inflammatory agent or antiallergic agent.
摘要翻译：由下式（I）表示的哌嗪衍生物，其中R 1为低级烷基或苯基，R 2为氢或低级烷基，n为2至10的整数，可用作抗 - 抗炎剂或抗过敏剂。

8. 发明授权

US5182284A Piperazine compounds, processes for preparation thereof and medical uses thereof 失效
标题翻译：哌嗪化合物，其制备方法及其医疗用途
公开(公告)号：US5182284A
公开(公告)日：1993-01-26
申请号：US761974
申请日：1991-09-25
申请人： Masahiro Suzuki , Kenji Nozaki , Makoto Kajitani , Mitsugi Yasumoto , Naohiko Ono , Takashi Shindo
发明人： Masahiro Suzuki , Kenji Nozaki , Makoto Kajitani , Mitsugi Yasumoto , Naohiko Ono , Takashi Shindo
IPC分类号： C07D295/084 , C07D295/125 , C07D295/13 , C07D295/185 , C07D317/60 , C07F9/6509
CPC分类号： C07D295/185 , C07D295/092 , C07D295/125 , C07D295/13 , C07D317/60 , C07F9/650958
摘要： Disclosed are a piperazine compound of the formula below or a pharmaceutically acceptable salt thereof, medical uses thereof, and processes for preparing the same: ##STR1## wherein each of R and R' is --OH, a lower alkoxy, a halo, H, a di(lower alkyl) hydrogenphosphate residue or a group --OR" (R" is an aralkyl group, etc.), etc., Y is --CH.dbd.CH-- or --(CH.sub.2).sub.m -- (m is 0, 1 or 2), and Y.sub.1 is a group of the formula ##STR2## (wherein A is --NH-- or --O--, A.sub.1 is a methylene or a carbonyl, n is 6-20, X is --OH, H or a lower alkoxycarbonyl, and X.sub.1 is an optionally halo-substituted phenyl or H) or a group of the formula ##STR3## (wherein X and n are as defined above), provided that when Y.sub.1 is the group of the formula (3), each of R and R' is an --OH group.

9. 发明授权

US5310926A Process for producing isoxazole derivatives 失效
标题翻译：异恶唑衍生物的制备方法
公开(公告)号：US5310926A
公开(公告)日：1994-05-10
申请号：US121557
申请日：1993-09-16
申请人： Yu-ichi Hagiwara , Motoaki Tanaka , Makoto Kajitani , Mitsugi Yasumoto
发明人： Yu-ichi Hagiwara , Motoaki Tanaka , Makoto Kajitani , Mitsugi Yasumoto
IPC分类号： C07D261/08
CPC分类号： C07D261/08
摘要： The present invention provides a process for producing isoxazole derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each a hydrogen atom or lower alkoxyl, and R.sup.3 is cyano or alkoxycarbonyl, the process being characterized by oxidizing an .alpha., .beta.-unsaturated ketoxime derivative represented by the formula ##STR2## wherein R.sup.1 , R.sup.2 and R.sup.3 are as defined above. The isoxazole derivatives (II) to be produced by the process of the present invention are useful as intermediates for preparing (3,4-diarylisoxazol-5-yl) acetic acid derivatives which are useful as anti-inflammatory agents, analgesics and antipyretics.
摘要翻译：本发明提供一种制备由式（II）表示的异恶唑衍生物的方法，其中R 1和R 2相同或不同，各自为氢原子或低级烷氧基，R 3为氰基或烷氧基羰基，该方法的特征在于通过氧化由式（I）表示的α，β-不饱和酮肟衍生物，其中R 1，R 2和R 3如上所定义。通过本发明的方法生产的异恶唑衍生物（II）可用作制备（3,4-二芳基异恶唑-5-基）乙酸衍生物的中间体，其可用作抗炎剂，止痛剂和解热药。

10. 发明授权

US5142091A .alpha., .beta.-unsaturated ketones and ketoxime derivatives 失效
标题翻译：（ALPHA），（BETA） - 饱和的酮和酮替代衍生物
公开(公告)号：US5142091A
公开(公告)日：1992-08-25
申请号：US690939
申请日：1991-07-10
申请人： Motoaki Tanaka , Yu-ichi Hagiwara , Makoto Kajitani , Mitsugi Yasumoto
发明人： Motoaki Tanaka , Yu-ichi Hagiwara , Makoto Kajitani , Mitsugi Yasumoto
IPC分类号： C07D261/08 , C07C69/738 , C07C251/48 , C07C255/37 , C07C255/40 , C07C255/62 , C07C255/64
CPC分类号： C07C69/738 , C07C251/48 , C07C255/40 , C07C255/64
摘要： The present invention provides an .alpha., .beta.-unsaturated ketone and ketoxime derivative represented by the formula ##STR1## wherein Y is oxygen atom or hydroxyimino group, Z is cyano or alkoxycarbonyl group, R.sup.1 and R.sup.2 are the same or different and are each hydrogen atom or lower alkoxyl group.The .alpha., .beta.-unsaturated ketones and ketoxime derivatives of the invention are useful as an intermediate for preparing a (3,4-diarylisoxazol-5-yl)acetic acid derivatives which is useful as an anti-inflammatory agent, analgesic and antipyretic.
摘要翻译： PCT No.PCT / JP90 / 01512 Sec。 371日期：1991年7月10日 102（e）日期1991年7月10日PCT 1990年11月19日PCT PCT。公开号WO91 / 07374 日本1991年5月30日。本发明提供由式（I）表示的+60，β-不饱和酮和酮肟衍生物，其中Y是氧原子或羟基亚氨基，Z是氰基或烷氧基羰基，R1和R2 相同或不同，为氢原子或低级烷氧基。本发明的α，β-不饱和酮和酮肟衍生物可用作制备（3,4-二芳基异恶唑-5-基）乙酸衍生物的中间体，其可用作抗炎剂，镇痛和解热。

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