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1. 发明申请

WO1991011443A1 PROCESS FOR PRODUCING ISOXAZOLE DERIVATIVE 审中-公开
标题翻译：生产异噻唑衍生物的方法
公开(公告)号：WO1991011443A1
公开(公告)日：1991-08-08
申请号：PCT/JP1991000064
申请日：1991-01-22
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , TANAKA, Motoaki , HAGIWARA, Yuichi , KAJITANI, Makoto , YASUMOTO, Mitsugi
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D261/08
CPC分类号： C07D261/08
摘要： A process for producing an isoxazole derivative of general formula (II), wherein R?1 and R2¿ may be the same or different from each other and each represents hydrogen or lower alkoxy, and R3 represents cyano or alkoxycarbonyl, by oxidizing an α,β-unsaturated ketoxime derivative of general formula (I), wherein R?1, R2 and R3¿ are as defined above. The isoxazole derivative (II) is useful as an intermediate for the production of (3,4-diaryl-isoxazol-5-yl)acetic acid derivatives useful as an antiinflammatory, analgesic and antipyretic.

2. 发明申请

WO1991007374A1 'alpha','beta'-UNSATURATED KETONE AND KETOXIME DERIVATIVE 审中-公开
标题翻译：（ALPHA），（BETA） - 饱和酮和酮替代衍生物
公开(公告)号：WO1991007374A1
公开(公告)日：1991-05-30
申请号：PCT/JP1990001512
申请日：1990-11-19
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , TANAKA, Motoaki , HAGIWARA, Yuichi , KAJITANI, Makoto , YASUMOTO, Mitsugi
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07C69/738
CPC分类号： C07C69/738 , C07C251/48 , C07C255/40 , C07C255/64
摘要： An α,β-unsaturated ketone and ketoxime derivatives thereof represented by general formula (I), wherein Y is an oxygen atom or a hydroxyimino group, Z is a cyano group or an alkoxycarbonyl group, R?1 and R2¿ which may be the same or different are each a hydrogen atom or a lower alkoxy group. They are useful as an intermediate for a (3,4-diarylisoxazol-5-yl)acetate derivative useful as an anti-inflammatory agent, an analgesic and an antifebrile.

3. 发明申请

WO1991001306A1 OXOINDOLE DERIVATIVE 审中-公开
公开(公告)号：WO1991001306A1
公开(公告)日：1991-02-07
申请号：PCT/JP1990000945
申请日：1990-07-23
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , KAWAGUCHI, Akihiro , SATO, Atsushi , KAJITANI, Makoto , YASUMOTO, Mitsugi , YAMAMOTO, Junji
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D209/34
CPC分类号： C07D401/06 , C07D209/34 , C07D405/06
摘要： Oxoindole derivatives of general formula (1), remarkably useful for treating senile dementia, i.e., improving brain functions and activating and protecting brain metabolism. In the formula, R1 represents hydrogen, halogen, lower alkyl, or lower alkoxy; R2 represents hydrogen or lower alkyl; R3 represents -CH¿2-R?5, wherein R5 represents alkyl which may be cyclic, benzodioxanyl, or phenyl which may be substituted with a plurality of halogen, lower alkyl, lower alkoxy, hydroxy, diethylamino, trifluoromethyl, nitrile, nitro or benzyloxy; alternatively R?2 and R3¿ may be combined together to from =CH-R5, wherein R5 is as defined above; and R4 represents 1-propylbutyl, pyridyl, or phenyl which may be substituted with lower alkoxy, halogen, diethylamino, benzyloxy, trifluoromethyl, nitrile, nitro, or lower alkyl.

4. 发明申请

WO1991011434A1 BICYCLOLACTAM DERIVATIVE 审中-公开
标题翻译： BICYCLOLACTAM衍生物
公开(公告)号：WO1991011434A1
公开(公告)日：1991-08-08
申请号：PCT/JP1991000116
申请日：1991-01-30
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , KAWAGUCHI, Akihiro , SATOH, Atsushi , KAJITANI, Makoto , YASUMOTO, Mitsugi , YAMAMOTO, Junji
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D209/34
CPC分类号： C07D215/227 , C07D209/34 , C07D209/46 , C07D209/52 , C07D221/04
摘要： A bicyclolactam derivative of general formula (1), which is quite useful for treating senile dementia, or improving the brain function and activating and protecting the brain metabolism, wherein R represents benzoyl which may be substituted with halogen, lower alkyl, lower alkoxy, nitro, cyano or amino; 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.

5. 发明申请

WO1990007509A1 DIAZABICYCLOALKANE DERIVATIVES 审中-公开
公开(公告)号：WO1990007509A1
公开(公告)日：1990-07-12
申请号：PCT/JP1989001316
申请日：1989-12-27
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , HASEGAWA, Etsuo , KAWAGUCHI, Akihiro , KAJITANI, Makoto , YASUMOTO, Mitsugi , KASAHARA, Nobuo , YAMAMOTO, Junji
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides diazabicycloalkane derivatives of formula (1), wherein R1 represents a phenyl group optionally substituted by lower alkoxy, lower alkyl or halogen, a thiazolyl group or a furyl group, R2 represents oxygen or sulfur, m represents a number of 3 or 4, and n represents a number of 1 or 2, which are remarkably effective in treating senile dementia, namely, in improving cerebral functions and in activating and protecting cerebral metabolism.

6. 发明申请

WO1989009767A1 CARBAMOYL-2-PYRROLIDINONE COMPOUNDS 审中-公开
标题翻译：卡巴酸-2-吡咯烷酮化合物
公开(公告)号：WO1989009767A1
公开(公告)日：1989-10-19
申请号：PCT/JP1989000401
申请日：1989-04-12
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , KAJITANI, Makoto , HASEGAWA, Etsuo , KAWAGUCHI, Akihiro , YAMAMOTO, Junji , TOIDE, Katsuo , HONNA, Takaji , YASUMOTO, Mitsugi , KASAHARA, Nobuo
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D207/26
CPC分类号： C07D207/27 , C07D207/26 , C07D207/273 , C07D401/12 , C07D417/12
摘要： Carbamoyl-2-pyrrolidinone compounds quite useful as an agent for treating senile dementia, or improving brain functions, or activating and protecting brain metabolism, which are represented by formula (2) (wherein R represents a hydrogen atom, a hydroxy group or an optionally hydroxy-substituted lower alkyl group, R represents a phenyl, tetrahydronaphthyl, pyridyl or thiazolyl group optionally substituted by a lower alkoxy group, a lower alkylamino group, a halogen atom or a halogenomethyl group) are disclosed. Also disclosed are novel carbamoyl-2-pyrrolidinone compounds represented by general formula (1), wherein R represents a hydrogen atom, a hydroxy group or an optionally hydroxy-substituted lower alkyl group, and R represents a phenyl, tetrahydronaphthyl, pyridyl or thiazolyl group optionally having a methoxy group or a lower alkylamino group as a substituent, provided that R does not represents an unsubstituted phenyl group when R represents a hydrogen atom or an unsubstituted lower alkyl group.
摘要翻译：氨基甲酰基-2-吡咯烷酮化合物作为治疗老年性痴呆或改善脑功能或激活和保护脑代谢的药剂，其由式（2）表示（其中R 1表示氢原子，羟基或任选羟基取代的低级烷基，R 3表示任选被低级烷氧基，低级烷基氨基，卤素原子或卤代甲基取代的苯基，四氢萘基，吡啶基或噻唑基。还公开了由通式（1）表示的新型氨基甲酰基-2-吡咯烷酮化合物，其中R 1表示氢原子，羟基或任选羟基取代的低级烷基，R 2表示苯基，四氢萘基，吡啶基或噻唑基，任选具有甲氧基或低级烷基氨基作为取代基，条件是当R 1表示氢原子或未取代的低级烷基时，R 2不表示未取代的苯基。

7. 发明申请

WO1987003881A1 2'-DEOXY-5-TRIFLUOROMETHYLURIDINE DERIVATIVES AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： 2'-脱氧-5-三氟甲基衍生物及其制备方法
公开(公告)号：WO1987003881A1
公开(公告)日：1987-07-02
申请号：PCT/JP1986000660
申请日：1986-12-26
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , UEDA, Toru , YASUMOTO, Mitsugi , YAMASHITA, Junichi , MATSUMOTO, Hiroshi , TADA, Yukio , KOBAYASHI, Kazuhiro , NOGUCHI, Kazuharu
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07H19/073
CPC分类号： C07H19/06
摘要： 2'-deoxy-5-trifluoromethyluridine derivatives represented by general formula (I), (wherein Tr represents a triphenylmethyl group and R represents a lower alkyl group or a benzyl group) and a process for their preparation. The derivatives are prepared by subjecting a 2'-deoxy-5-halogenuridine derivative represented by general formula (II), (wherein W represents an iodine atom or a bromine atom, Tr represents a triphenylmethyl group, and R represents a lower alkyl group or a benzyl group) to trifluoromethylation reaction with halogenotrifluoromethane in the presence of metallic copper.

8. 发明申请

WO1992020666A1 BENZOTHIADIAZINE DERIVATIVE 审中-公开
标题翻译：苯并噻嗪衍生物
公开(公告)号：WO1992020666A1
公开(公告)日：1992-11-26
申请号：PCT/JP1992000672
申请日：1992-05-22
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , OHNO, Tomoyasu , YANO, Shingo , FUJIWARA, Kosuke , AJIOKA, Hirofusa , YAMAMOTO, Noriyuki , YAMADA, Shozo , KAJITANI, Makoto
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D285/24
CPC分类号： C07D417/12 , C07D285/24
摘要： A benzothiadiazine derivative represented by general formula (I), a hydrate and acid addition salt thereof, and a remedy for peptic ulcer containing said derivative, said hydrate or said salt as an active ingredient. In formula (I) X represents methylene or a lower alkyl-substituted nitrogen atom; Y and Z represent each methylene or carbonyl; A represents phenylene which may be substituted by methoxycarbonyl; B represents lower alkylene or lower alkenylene; R1 represents hydrogen, acetoxyacetyl, cyclohexylmethyl, or benzyl wherein the benzene ring may be substituted by lower alkoxy, halogen, nitro, lower alkyl, methylenedioxy or hydroxyl; R2 represents lower alkyl or phenyl; and R3 represents hydrogen, halogen or lower alkoxy, provided that the case where X, Y and Z represent each methylene, A represents unsubstituted phenylene, B represents lower alkylene, and R1 represents hydrogen is excluded.
摘要翻译：由通式（I）表示的苯并噻二嗪衍生物，其水合物和酸加成盐，以及含有所述衍生物，所述水合物或所述盐作为活性成分的消化性溃疡的药物。在式（I）中，X表示亚甲基或低级烷基取代的氮原子; Y和Z代表每个亚甲基或羰基; A表示可被甲氧基羰基取代的亚苯基; B表示低级亚烷基或低级亚烯基; 卤素，硝基，低级烷基，亚甲基二氧基或羟基取代的苯环，其中R 1表示氢，乙酰氧基乙酰基，环己基甲基或苄基，其中苯环可被低级烷氧基， R2代表低级烷基或苯基; 并且R 3表示氢，卤素或低级烷氧基，条件是X，Y和Z表示各亚甲基的情况，A表示未取代的亚苯基，B表示低级亚烷基，R 1表示氢。

9. 发明申请

WO1989002432A1 THIENOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：三苯甲基衍生物
公开(公告)号：WO1989002432A1
公开(公告)日：1989-03-23
申请号：PCT/JP1988000935
申请日：1988-09-16
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , OGAWA, Kazuo , YAMAWAKI, Ichiro , MATSUSHITA, Yoichi , NOMURA, Naruo , OKAZAKI, Issei
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Thienopyrimidine derivatives represented by general formula (I), wherein R1 and R2, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a cyclic alkyl group or a phenyl group, or R1 and R2 may be bound to each other to form an alkylene chain for forming a ring, R3 represents a lower alkyl group or a group of formula (II) (wherein R4 represents a lower alkyl group, a lower alkoxy group or a halogen atom, m represents 0, 1 or 2 and R5 represents a hydrogen atom or a halogen atom) or pharmaceutically acceptable salts thereof, a pharmacological composition containing the same as effective ingredient, and an aldose reductase inhibitor are disclosed.
摘要翻译：由通式（I）表示的噻吩并嘧啶衍生物，其中可以相同或不同的R 1和R 2各自表示氢原子，卤素原子，低级烷基，环烷基或苯基，或R 1和 R2可以彼此结合以形成用于形成环的亚烷基链，R 3表示低级烷基或式（II）的基团（其中R 4表示低级烷基，低级烷氧基或卤素原子，m 表示0,1或2，R5表示氢原子或卤素原子）或其药学上可接受的盐，含有与有效成分相同的药理组合物和醛糖还原酶抑制剂。本发明提供式（I）的噻吩并嘧啶衍生物，其中R 1和R 2相同或不同，各自表示氢，卤素，低级烷基，环烷基或苯基，R 1 和R 2一起形成亚烷基链的环，R 3表示低级烷基或式CHEM的基团（其中R 4为低级烷基，低级烷氧基或卤素，m为0,1或2，R 5为氢或卤素），Z是氧或硫，或其药学上可接受的盐，含有它们作为活性成分的药物组合物和醛糖还原酶抑制剂。

10. 发明申请

WO1992004028A1 ANTINEOPLASTIC EFFECT POTENTIATOR AND ANTINEOPLASTIC AGENT 审中-公开
标题翻译：抗肿瘤药物和抗肿瘤药物
公开(公告)号：WO1992004028A1
公开(公告)日：1992-03-19
申请号：PCT/JP1991001187
申请日：1991-09-05
申请人： TAIHO PHARMACEUTICAL COMPANY, LIMITED , UCHIDA, Junji , OKABE, Hiroyuki , TAKECHI, Teiji , TAKEDA, Setsuo , YAMADA, Yuji
发明人： TAIHO PHARMACEUTICAL COMPANY, LIMITED
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , A61K2300/00
摘要： An antineoplastic effect potentiator for an antineoplastic agent containing tegafur in a therapeutically effective amount and uracil in an amount effective in potentiating the antineoplastic effect, containing as the active ingredient folinic acid or a pharmaceutically acceptable salt thereof in an amount effective in potentiating the antineoplastic effect; an antineoplastic agent containing tegafur in a therapeutically effective amount, uracil in an amount effective in potentiating the antineoplastic effect, and folinic acid or a pharmaceutically acceptable salt thereof in an amount effective in potentiating the antineoplastic effect; a method of potentiating the antineoplastic effect of an antineoplastic agent by administering said potentiator to patients; and a method fo treating cancers of mammals by administering said agent to patients.

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