Claims
- 1. A compound of the formula: ##STR209## u is 0 to 2; y is 1 to 3;
- with the proviso that no more than one R.sub.c is other than H in the ##STR210## moiety; each R.sub.c is independently H, C.sub.1 -C.sub.6 alkyl, hydroxy(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl or H.sub.2 NC(O)-(C.sub.1 C.sub.6)alkyl;
- each R.sub.1 and R.sub.2 is independently H, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.2 F.sub.5, Cl, Br, I, ##STR211## or when R.sub.1 and R.sub.2 are on adjacent carbons on a ring, they can form ##STR212## wherein n' is 1 or 2; each R.sub.3 is independently H, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.2 F.sub.5, ##STR213## Cl, Br, I, or F, OR.sub.a, OCF.sub.3 or phenyl; each R.sub.a and R.sub.b is independently selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, phenyl, benzyl, allyl, ##STR214## or R.sub.a and R.sub.b together are C.sub.2 -C.sub.6 alkylene and are attached to the same nitrogen, so that R.sub.a and R.sub.b, together with the nitrogen to which they are attached, join to form a 4 to 7 membered ring;
- Ar.sub.1 is ##STR215## m.sub.1 =0 to 1; n.sub.3 is 0 to 4;
- each R.sub.e and R.sub.f is independently selected from the group consisting of H, C.sub.1 -C.sub.6 alkyl, phenyl, benzyl, allyl, ##STR216## or R.sub.e and R.sub.f taken together with the carbon to which they are attached can also form a carbonyl group, with the proviso that no more than one carbonyl group is in the ##STR217## moiety; R.sub.6 is H, C.sub.3 -C.sub.6 cycloalkyl, ##STR218## heteroaryl, substituted heteroaryl, or, provided that Re,R.sub.f taken together with the carbon atom to which they are attached form a carbonyl group and n.sub.3 is R1, R.sub.6 is OR.sub.a wherein R.sub.a is not H;
- wherein heteroaryl is selected from the group consisting of imidazolyl, oxadiazolyl, thiadiazolyl, benzimidazolyl, indolyl, thiazolyl, thienyl, pyrrolyl, furyl, pyridyl, isoxazolyl, pyrimidyl and quinolyl; and wherein substituted heteroaryl are heteroaryl rings substituted with R.sub.1, R.sub.2 and R.sub.3 ;
- or a pharmaceutically acceptable salt thereof.
- 2. A compound according to claim 1 wherein y is 1.
- 3. A compound according to claim 2 wherein u is 0.
- 4. A compound according to claim 1 wherein y is 1 and u is 0.
- 5. A compound according to claim 4 wherein R.sub.6 is ##STR219##
- 6. A compound according to claim 1 selected from the group consisting of ##STR220##
- 7. A composition comprising a neurokinin antagonistic effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier material.
- 8. A method for treating asthma and bronchospasm which comprises administering a therapeutically effective amount of a compound according to claim 1.
CROSS REFERENCE TO RELATED APPLICATIONS
This application is a continuation-in part of International Application No. PCT/US96/05660, filed May 1, 1996, which is a continuation-in-part of U.S. Provisional Application No. 60/003048, filed Aug. 31, 1995, and a continuation-in-part of U.S. Ser. No. 08/432,739, filed May 2, 1995now U.S. Pat. No. 5,719,156.
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
432739 |
May 1995 |
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