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    • 2. 发明授权
    • HYPOLIPIDAEMIC COMPOUNDS
    • 低分子量化合物
    • EP0683774B1
    • 2002-10-09
    • EP94906338.2
    • 1994-02-15
    • THE WELLCOME FOUNDATION LIMITED
    • BRIEADDY, Lawrence, EdwardHODGSON, Gordon, Lewis, Jr.
    • C07D285/36C07D513/04C07D281/10A61K31/55
    • C07D417/04C07D281/10C07D513/04
    • The invention provides a compound of formula (I), wherein 1 is an integer of from 0 to 4; n is an integer of from 0 to 2; X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; with the proviso that at least one of R, R?2, R4 and R5¿ is hydroxy or a group containing hydroxy; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic agents.
    • 本发明提供了式(I)的化合物,其中1是0至4的整数; n是0-2的整数; X是具有5至10个碳原子(包括形成部分硫氮杂环的两个碳原子)的芳族或非芳族单环或双环系统,其中任选地一个或多个碳原子被杂原子取代 )独立地选自氮,氧和硫; 条件是R 1,R 2,R 4和R 5'中至少一个是羟基或含羟基的基团; 以及它们的盐,溶剂合物和生理学功能衍生物,包含这些化合物的药物制剂,它们的制备方法以及它们在减少胆汁酸摄取中的用途以及因此作为降血脂剂。
    • 3. 发明授权
    • HYPOLIPIDAEMIC CONDENSED 1,4-THIAZEPINES
    • 降血脂,浓缩1,4-硫氮杂
    • EP0683773B1
    • 1997-09-17
    • EP94906323.4
    • 1994-02-15
    • THE WELLCOME FOUNDATION LIMITED
    • BRIEADDY, Lawrence, EdwardHODGSON, Gordon, Lewis, Jr.
    • C07D281/10C07D281/08C07D417/04C07D513/04A61K31/55
    • C07D417/04C07D281/08C07D281/10C07D513/04
    • The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R1 is hydrogen or C¿1-6?alkyl; R?2¿ is an atom or group selected from hydrogen, C¿1-6?alkyl (including cycloalkyl and cycloalkylalkyl), C1-4alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R?3¿ is hydrogen, OH, C¿1-6?alkyl, C1-6alkoxy or -OC1-6acyl; R?4¿ is a group independently selected from C¿1-6?alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl, and C2-6alkynyl which groups are optionally substituted; R?5¿ is a group independently selected from C¿2-6?alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl and C2-6alkynyl, which groups are optionally substituted; or R?4 and R5¿, together with the carbon atom to which they are attached, form a C¿3-7?spiro cycloalkyl group which is optionally substituted; R?6 and R7¿ are independently selected from hydrogen and C¿1-6?alkyl; and X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein optionally one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; or X is an aromatic or non-aromatic monocyclic or bicyclic ring system having from 5 to 10 carbon atoms (including the two carbon atoms forming part of the thiazepine ring) wherein one or more of the carbon atoms is/are replaced by heteroatom(s) independently selected from nitrogen, oxygen and sulphur; and salts, solvates and physiologically functional derivatives thereof, pharmaceutical formulations comprising such compounds, processes for their preparation and their use in reducing bile acid uptake and hence as hypolipidaemic compounds.