Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

F. Hoffmann-la Roche Ag

Robert Stephen Wilhelm

Denis John Kertesz

Leyi Gong

David Bernard Smith

Francisco Xavier Talamas

Bradley E Loe

Bruce H Devens

Robert Alvarez

Ronnie L Chin

Sabine Axt

Paul Ross Fatheree

Michael Patrick Dillon

Alam Jahangir

Michael G Martin

Alfred Sui-Ting Lui

Donald Roy Hirschfeld

David Berard Smith

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein A, D, E, G, J, X, Y, Z R, Rand Rare as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2Xand/or a P2Xreceptor antagonist and methods of making the compounds.

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This invention relates to certain cyclic amine derivatives of Formula (I)that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Cyclic amine derivatives-CCR-3 receptor antagonists

This invention relates to certain cyclic amine derivatives of Formula (I)

Cyclic amine derivatives- CCR-3 receptor antagonists

This invention relates to certain piperidine quaternary salts of Formula (I) ##STR1## that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

4-aroylpiperidine derivatives-CCR-3 receptor antagonists

Benzo or pyridopyridazinones and pyridazinthiones of the formula ##STR1## wherein: X and Y are nitrogen or carbon, provided that at least one is carbon, and Z is oxygen or sulfur;

Benzopyridazinone and pyridopyridazinone compounds

The use of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines for treating atopic dermatitis, allograft rejection, graft-vs-host disease, and anti-autoimmune disease, and inducing immunosuppression, is disclosed.

Method of use of 8-phenylcyclopentenoquinoline and

The disclosed derivatives of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft, rejection agents, anti-graft-vs-host disease agents, anti-allergic agents, bronchodilation agents, anti-autoimmune agents, and analgetic agents.

8-phenylcyclopentenoquinoline and 8-phenylcyclohexenoquinoline

The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; and

8-phenyl-1,6-naphthyridin-5-ones

A compound of the formula ##STR1## wherein: R.sup.1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl, benzyl, arylmethyl, pyridylmethyl,

Optionally substituted 6,8-quinolines

The present invention relates to optionally substituted pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones or optionally substituted pyrido[2,3-d]pyrimidine-2(1H,3H)-ones, i.e., compounds of Formula I: ##STR1## wherein: Y is --CH.sub.2 -- or --C(O)--;

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Los Altos, CA, United States of America

Robert Stephen Wilhelm