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US 5,633,381 AGranted
(Z,Z), (Z,E) and (E,Z) isomers of substituted bis(phenylmethylene)cycloketones
AssigneeBerlex Laboratories, Inc.
InventorsJerry L. Dallas, William J. Guilford, Sunil K. Koovakkat, Michael M. Morrissey, Kenneth J. Shaw
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Abstract
This invention relates to novel (Z,Z), (Z,E) and (E,Z) olefin isomers of substituted benzylidene cycloketones and their pharmaceutically acceptable salts. The compounds of the invention are potent factor Xa inhibitors thereby acting as anticoagulants useful in a number of thrombotic disease states. Pharmaceutical compositions are proposed for the compounds.
Claims23
A compound of one of the following formulae:
- ##STR7## wherein R, R.sub.1 are the same or independently ##STR8## R.sub.2, R.sub.3 are the same or independently hydrogen, loweralkyl or halogen;
- R.sub.4 are the same or independently hydrogen, loweralkyl, aryl or arylloweralkyl;
- R.sub.5 are the same or independently hydrogen, loweralkyl, aryl, arylloweralkyl ##STR9## R.sub.6 is loweralkyl, aryl or arylloweralkyl;
- X is (CHR.sub.7).sub.n O, S, SO, SO.sub.2 or NR.sub.8 ;
- R.sub.7 is independently hydrogen, --COOH or (--CH.sub.2).sub.p --COOH;
- R.sub.8 is hydrogen, loweralkyl, arylloweralkyl or ##STR10## Y is loweralkyl or aryl;
- n is the integers 1, 2, 3, 4 or 5;
- p is the integers 1, 2, 3 or 4 and the pharmaceutically acceptable salts thereof;
- with the provisos:
- a) both R and R.sub.1 must be in the meta or para positions,
- b) R and R.sub.1 cannot both be --CON(R.sub.4).sub.2,
- c) only one of R.sub.5 can be ##STR11## and d) only one of R.sub.7 can be --COOH or (--CH.sub.2).sub.p --COOH.
9 more elements
Dependencies are inferred from the claim text.