119981-04-3Relevant articles and documents
ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE
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, (2008/06/13)
There are disclosed compounds of formula (I) STR1 and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Pyridine compounds which are useful in treating a disease state characterized by an excess of platelet activating factors
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, (2008/06/13)
The invention relates to compounds of the formula STR1 wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH2)n --(X)s --(CH2)r ----, X is O, S or --CH=CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R1 and R2, independently, are lower alkyl, lower alkenyl or aryl, or one of R1 or R2 is hydrogen and the other is STR2 wherein W is STR3 --CH2 --CH2 --, --CH2 --, O, S, or STR4 and X1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X2, X3 and X4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R3 is hydrogen, lower alkyl or aryl, R4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R5 is hydrogen or lower alkyl, R6 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 6-membered heteroaromatic radical containing one or two nitrogen atoms, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R5 and R6 are different, their enantiomers and racemic mixtures thereof, when R1 and R2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof.
Pentadieneamides
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, (2008/06/13)
Compounds of the formula STR1 Y is O ir S, *A is paraphenylene or *----(CH2)n----(X)m --(CH2)r ----, X is O, S or --CH=CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R1 and R2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R3, R4 and R8, independently, are hydrogen, lower alkyl, aryl, R5 and R6, independently, are hydrogen or lower alkyl, R7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment, and when R6 and R7 are different, their enantiomers and racemic mixtures thereof, when R1 and R2 are different, their geometric isomers, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characerized by excess platelet activating factor or for the prevention and treatment of cardiovascular disease, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.