Cyclopropylpropenamides

Details Cyclopropylpropenamides Cyclopropylpropenamides

1987-07-10

1988-11-22

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514351, 514352, 514357, 546291, 546300, 546301, 546302, 546303, 546304, 546305, 546309, 546329, 546331, 546334, 546153, 546156, 546159, 546162, 546255, 546257, 548471, 548172, 548325, 548333, 548339, 548341, 548215, 548225, 548233, 549 62, 549 63, 549475, 549480, 549 68, 549 75, 549491, 544322, 544335, A61K 3144, C07D41300

Patent

active

047866462

ABSTRACT:
The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.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, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.7 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 their enantiomers, diastereomers and racemic mixtures thereof, as well as when *E is ##STR3## their geometric isomers, and pharmaceutically acceptable acid addition salts thereof.
The compounds of formula I exhibit activity as platelet activating factor (PAF) antagonists and are, therefore, useful in disease states characterized by excess platelet activating factor or for the prevention and treatment of cardiovascular diseases, pulmonary diseases, immunological disorders, inflammatory diseases, dermatological disorders, shock or transplant rejection.

REFERENCES:
patent: 3072649 (1963-01-01), Semb et al.
patent: 4542145 (1985-09-01), Wright, Jr. et al.
patent: 4568685 (1986-02-01), Wright, Jr. et al.
patent: 4568687 (1986-02-01), Wright, Jr. et al.
Chemical Abstracts 104:168177c, 1986.
Chemical Abstracts 107:154084v, 1987.
Chemical Abstracts 105:226649s, 1986.
Chemical Abstracts 97:6167j, 1982.
Chemical Abstracts 96:178,218x, 1982.

Affiliated with

Also associated with

Rating

Cyclopropylpropenamides does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Cyclopropylpropenamides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclopropylpropenamides will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-435590