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US 5,849,766 AGranted
Carbamoyl substituted heterocycles
AssigneeEli Lilly and Company
InventorsJoseph Anothony Jakubowski, Dale Eugene Mais, Kumiko Takeuchi
Life of this patent
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Abstract
This invention relates to carbamoyl substituted heterocycles which are .omega.-phenyl-.omega.-(3-pyridyl)-.omega.-alkenoic acid derivatives bearing a carbamoyl substituted oxazolyl or oxazolinyl group on the phenyl ring and which demonstrate utility for thromboxane receptor antagonism and/or thromboxane synthase inhibition, as well as pharmaceutical formulations containing them, methods for their use, and processes and intermediates for their preparation.
Claims31
A compound of Formula I ##STR36## in either the E-form, the Z-form or a mixture thereof, wherein
- n is 2, 3, 4 or 5;
- L is ortho-, meta- or para-phenylene;
- each R.sup.a is hydrogen or the two together form a double bond;
- and
- R is (3-12C)alkyl, (3-12C)alkenyl, (3-12C)alkynyl, 2-phenylcyclopropyl or R.sup.b -(1.varies.6C)alkyl in which R.sup.b is (3-8C)cycloalkyl, phenyl, tetrahydropyranyl, morpholino, piperidino or pyrrolidino wherein a phenyl group of the radical R may bear a 4-substituent selected from halo, (1-2C)alkyl and (1-2C)alkoxy;
- a cyclohexyl group of the radical R may bear a 4-substituent selected from (1-2C)alkyl and (1-2C)alkoxy;
- and in which one or two methylene groups of a (3-12C)alkyl, (3-12C)alkenyl, (3-12C)alkynyl, or the alkyl portion of R.sup.b -(1-6C)alkyl may be replaced by an oxy group;
- and further provided that at least two carbon atoms separate any oxygens or nitrogens in the residue --NHR;
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.