Tachykinin antagonists
AssigneeWarner-Lambert Company
InventorsDavid Christopher Horwell, William Howson, Martyn Clive Pritchard, Edward Roberts, David Charles Rees
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Abstract
The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.
Claims31
A compound of formula ##STR120## or a pharmaceutically acceptable salt thereof wherein R is phenyl or naphthalene each unsubstituted, mono-, di-, or trisubstituted by
- alkyl,
- hydroxy,
- alkoxy,
- NO.sub.2,
- halogen,
- NH.sub.2, or
- CF.sub.3 ;
- R.sup.1 and R.sup.2 are each independently hydrogen or alkyl of from 1 to 4 atoms;
- R and R.sup.2, when joined by a bond, can form a ring;
- X is ##STR121## wherein R.sup.11 is hydrogen or alkyl of from 1 to 3 carbon atoms;
- R.sup.3 is hydrogen or (CH.sub.2).sub.m R.sup.13 where m is an integer of from 1, to 6 and R.sup.13 is H, CN, NH.sub.2, N(CH.sub.3).sub.2, or NHCOCH.sub.3 ;
- n is an integer of from 1 to 2;
- R.sup.8 is phenyl or naphthalene each unsubstituted, or mono-, di-, or trisubstituted by
- alkyl,
- hydroxy,
- alkoxy,
- NO.sub.2,
- halogen,
- NH.sub.2, or
- CF.sub.3 ;
- Y is ##STR122## wherein R.sup.4 is hydrogen or alkyl of from 1 to 3 carbon atoms, --CO.sub.2 --,
- --COCH.sub.2 --,
- --CH.sub.2 O--,
- --CH.sub.2 NH--,
- --CH.dbd.CH--,
- --CH.sub.2 CH.sub.2 --,
- --CHOHCH.sub.2 --;
- R.sup.5 and R.sup.7 are each independently hydrogen or alkyl of from 1 to 4 carbon atoms;
- q is an integer of from 0 to 1;
- and
- R.sup.6 is phenyl or naphthalene each unsubstituted, or mono-, di-, or trisubstituted by
- alkyl,
- hydroxy,
- alkoxy,
- NO.sub.2,
- halogen,
- NH.sub.2, or
- CF.sub.3.
Dependencies are inferred from the claim text.