Anti-platelet aggregating 1,3-oxathiane derivatives, compositions, and method of use therefor
AssigneeImperial Chemical Industries PLC
InventorsVictor G. Matassa, Michael J. Smithers
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Abstract
The invention concerns novel [5,6]-cis-1,3-oxathiane derivatives of formula I in which R.sup.1 and R.sup.2 are variously defined as hydrogen, alkyl, trifluoromethyl or phenyl (as set out in the specification), n is 1 or 2, m is 2, 3 or 4, Y is vinylene and Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NH.SO.sub.2 R.sup.3 in which R.sup.3 is alkyl, phenyl or benzyl, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.
Claims10
A [5,6]-cis-1,3-oxathiane derivative of the formula I
- wherein R.sup.1 and R.sup.2 are independently hydrogen, trifluoromethyl or (1-6C)alkyl, provided that R.sup.1 and R.sup.2 together contain no more than 6 carbon atoms;
- or R.sup.1 is phenyl optionally bearing one or two substituents independently selected from halogeno, trifluoromethyl, cyano, nitro, (1-4C)alkyl and (1-4C)alkoxy, and R.sup.2 is hydrogen;
- n is 1 or 2;
- m is 2, 3 or 4;
- Y is vinylene;
- and Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NH.SO.sub.2.R.sup.3, wherein R.sup.3 is (1-6C)alkyl, benzyl or phenyl, the latter two of which may optionally bear a halogeno, (1-4C)alkyl, (1-4C)alkoxy, nitro, cyano or trifluoromethyl substituent;
- or a pharmaceutically acceptable salt thereof.
A compound selected from 5(Z)-7-(6-o-hydroxyphenyl-2,2-dimethyl-1,3-oxathian-cis-5-yl)heptenoic acid, 4(Z)-6-(6-o-hydroxyphenyl-2,2-dimethyl-1,3-oxathian-cis-5-yl)hexenoic acid , N-methanesulphonyl-5(Z)-7-(6-o-hydroxyphenyl-2,2-dimethyl-1,3-oxathian-ci s-5-yl)heptenamide, and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.