Abstract: The present invention provides a heterodimeric compound possessing bradykinin and neurokinin receptor antagonist activities useful in the treatment of asthma and other inflammatory diseases especially those involving the airway or pulmonary system. The present invention is also useful in the treatment of pain and inflammation.
Type:
Grant
Filed:
August 1, 1994
Date of Patent:
March 11, 1997
Assignee:
Cortech, Inc.
Inventors:
Val S. Goodfellow, Eric T. Whalley, Francine E. Wincott
Abstract: A bradykinin antagonist of the formulaX(BKA).sub.nwherein BKA is the peptide chain of a bradykinin antagonist peptide, X is a linking group and n is a whole number greater than 1. The BKA substituents may be the same or different. Monomeric antagonists of the formula X(BKA) are also disclosed.
Type:
Grant
Filed:
January 8, 1993
Date of Patent:
May 16, 1995
Assignee:
Cortech, Inc.
Inventors:
John C. Cheronis, Eric T. Whalley, Khe T. Nguyen, Shadrach R. Eubanks, Lisa G. Allen
Abstract: Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are selected from the group consisting of hydrogen, alkyl of 1-6 carbons, cycloalkyl of 3 to 6 carbons, alkenyl of 2-6 carbons, or together represent methylene groups --(CH.sub.2).sub.n --where n is a whole number from 1 to 6, provided that R.sub.1 and R.sub.2 or R.sub.3 and R.sub.4 are not both hydrogen;R.sub.5 and R.sub.6, which may be the same or different, are selected from the group consisting of hydrogen, halogen, nitro or --S(O).sub.n R.sub.7 where n is 0, 1 or 2 and R.sub.7 is an optionally substituted alkyl of 1-12 carbons atoms; and both Ar substituents are optionally substituted heteroaromatic rings or one Ar is such heteroaromatic ring and the other is optionally substituted phenyl, the optional substitution for Ar being halogen, nitro or --S(O).sub.n R.sub.7 where n and R.sub.7 have the value given above. The compounds are useful as inhibitors of human neutrophil elastase.
Type:
Grant
Filed:
December 19, 1991
Date of Patent:
June 1, 1993
Assignee:
Cortech, Inc.
Inventors:
Jozef Oleksyszyn, Gary P. Kirschenheuter