发明公开
EP0238973A2 Diphenyl-methane derivative, pharmaceutical composition and use
失效
二苯甲烷衍生物，药物Zusammensetzung und Verwendung。
- 专利标题： Diphenyl-methane derivative, pharmaceutical composition and use
- 专利标题（中）： 二苯甲烷衍生物，药物Zusammensetzung und Verwendung。
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申请号： EP87103834.5申请日： 1987-03-17
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公开(公告)号： EP0238973A2公开(公告)日： 1987-09-30
- 发明人: Yamagishi, Youji , Akasaka, Kozo , Suzuki, Takeshi , Miyamoto, Mitsuaki , Nakamoto, Kouji , Okano, Kazuo , Abe, Shinya , Ikuta, Hironori , Hayashi, Kenji , Yoshimura, Hiroyuki , Fujimori, Tohru , Harada, Koukichi , Yamatsu, Isao
- 申请人： Eisai Co., Ltd.
- 申请人地址： 6-10, Koishikawa 4-chome Bunkyo-ku Tokyo 112 JP
- 专利权人： Eisai Co., Ltd.
- 当前专利权人： Eisai Co., Ltd.
- 当前专利权人地址： 6-10, Koishikawa 4-chome Bunkyo-ku Tokyo 112 JP
- 代理机构： Hansen, Bernd, Dr.rer.nat.
- 优先权： JP57061/86 19860317; JP65963/86 19860326
- 主分类号： C07C251/00
- IPC分类号： C07C251/00 ; C07C311/15 ; C07C235/42 ; C07C255/37 ; C07C233/65 ; C07D213/75 ; C07C257/00 ; C07C257/06 ; C07C327/00 ; C07C59/64 ; A61K31/15
摘要：
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative.
in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is =CXY or =N-O-W,
X is hydrogen, cyano or -COR6, R6 being hydroxyl or an amino, Y is -R10-COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, -CO-NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, -CH2-NHSO2-C6H5 or -C(R8)=NR7, R7 being a lower alkoxy or an aryl, R8 is -VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,
W is -CH2-CO-CH2-C00R13, R13 being hydrogen or a lower alkyl, -CH2-C(=NOR14)-CH2-COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, -CH(CN)-(CH2)q-COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or -(CH2)p-Z, Z being -SH, -SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
A pharmaceutical composition containing compounds of formula (XX) or their pharmaceutically acceptable salts as active ingredients, and the use of compounds of formula (XX) or their pharmaceutically acceptable salts in the preparation of a medicament for treatment of diseases caused by blood stream disorders are also disclosed.
in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is =CXY or =N-O-W,
X is hydrogen, cyano or -COR6, R6 being hydroxyl or an amino, Y is -R10-COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, -CO-NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, -CH2-NHSO2-C6H5 or -C(R8)=NR7, R7 being a lower alkoxy or an aryl, R8 is -VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,
W is -CH2-CO-CH2-C00R13, R13 being hydrogen or a lower alkyl, -CH2-C(=NOR14)-CH2-COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, -CH(CN)-(CH2)q-COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or -(CH2)p-Z, Z being -SH, -SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
A pharmaceutical composition containing compounds of formula (XX) or their pharmaceutically acceptable salts as active ingredients, and the use of compounds of formula (XX) or their pharmaceutically acceptable salts in the preparation of a medicament for treatment of diseases caused by blood stream disorders are also disclosed.
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