Hypolipidaemic condensed 1, 4-thiazepines

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 281/08 (2006.01) A61K 31/55 (2006.01) C07D 281/10 (2006.01) C07D 417/00 (2006.01) C07D 417/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2156184

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 C1-6alkyl; R2 is an atom or group selected from hydrogen, C1-6alkyl (including cycloalkyl and cycloalkylalkyl), C1-4alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R3 is hydrogen, OH, C1-6alkyl, C1-6alkoxy or -OC1-6acyl; R4 is a group independently selected from C1-6alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl and C2-6alkynyl which groups are optionally substituted; R5 is a group independently selected from C2-6alkyl (including cycloalkyl and cycloalkylalkyl), C2-6alkenyl and C2-6alkynyl which groups are optionally substituted; or R4 and R5, together with the carbon atom to which they are attached, form a C3-7spiro cycloalkyl group which is optionally substituted; R6 and R7 are independently selected from hydrogen and C1-6alkyl; 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 use and their use in reducing bile acid uptake and hence as hypolipidaemic compounds.

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