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Patent

Hypolipidaemic condensed 1,4-thiazepines

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TLDR
In this article, the authors provided a compound of formula (I) wherein n is an integer of from 0 to 2; R is an optional substituent; R 1 is hydrogen or C?1-6?alkyl; R?2? is an atom or group selected from hydrogen, C? 1-6?alkyl (including cycloalkyl and cyclo-alkylalkyl), C1-4alkoxy, pyrryl, pypyryl, thienyl, polycyclohexyl and pyridyl,
Abstract
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.

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Citations
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References
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Journal ArticleDOI

Suppression of atherosclerosis in cholesterol-fed rabbits by diltiazem injection.

TL;DR: It is concluded that diltiazem administered intraperitoneally suppresses the plasma total and LDL cholesterol elevation induced by the cholesterol diet and inhibits experimentally-induced atherosclerosis.
Patent

Hypolipidaemic benzothiazepine compounds

TL;DR: In this article, the present invention relates to compounds of the formula (I) wherein 1 is an integer between 0 and 4; m represente un entier compris entre 0 and 5; m represents an integer in the range of 0 and 3; n represents an entier in the ranges of 0 to 2; and R5 is C2-6 alkyl law.
Journal ArticleDOI

Synthesis and spectroscopic investigations of 1,4-benzothiazepine derivatives

TL;DR: In this article, the reaction of sodium 3,4-dimethoxythiophenolate (1) with 2-bromoethylamine (2) gave 2′-aminoethyl-3,4dimethoxy-phenyl sulfide hydrochloride (3) and corresponding nitrile.
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