The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.

Hypolipidemic 1,4-benzothiazepine-1,1-dioxides

Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications

Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors

Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Benzothiepines having activity as inhibitors of ileal bile acid transport and taurocholate uptake

The present invention provides combinations of cardiovascular
therapeutic compounds for the prophylaxis or treatment of
cardiovascular disease including hypercholesterolemia,
atherosclerosis, or hyperlipidemia. Combinations disclosed
include an ileal bile acid transport inhibitor combined with
a fibric acid derivative.

Combinations of ileal bile acid transport inhibitors and fibric acid derivatives for cardiovascular indications

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.

Gordon Lewis Hodgson

Papers

Hypolipidaemic condensed 1,4-thiazepines