Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

Klaus K Weinhardt

Robin D Clark

Colin C Beard

Jacob Berger

William L Smith

Richard M Eglen

Michael Marx

Charles Alois Dvorak

Adolph P Roszkowski

Joseph M Muchowski

Francisco Javier Lopez-Tapia

Jim W Li

Counde O'Yang

Terrence Joseph Connolly

Chris Richard Melville

Dov Nitzan

Paul Francis Keitz

Eun Kyung Lee

Fernando Padilla

Patrick Finbar McGarry

Marshall B Wallach

Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R', Rand Rare as defined herein.

Arylamine-substituted quinazolinone compounds useful as alpha 1A/B adrenergic receptor antagonists

The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;

Tricyclic 5-HT.sub.3 receptor antagonists

Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;

Tricyclic compounds acting at serotonin receptor subtypes

.alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.

Serotonergic alpha-oxoacetamides

1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;

1,9-alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines

Certain 1,4,5,6-tetrahydropyrimidine compounds which are substituted with an amino, amido or carbamate at the 2-position, with an optionally substituted phenyl at the 5-position or at the 4-position when there is no alkyl at the 1-position and optionally a lower alkyl at the 1-position when the phenyl is at the 5-position are useful as CNS agents and as antihypertensives.

4-Phenyl-and 5-phenyl-1,4,5,6-tetrahydro-pyrimidine derivatives

4-Phenyl-and 5-phenyl-1,4,5,6-tetrahydropyrimidine derivatives

4,5-Dihydro-2-lower alkoxycarbonylamino-4-phenylimidazole, and substituted phenyl derivatives thereof, and pharmaceutically acceptable salts thereof, and methods of preparing such compounds. In one method, the compounds can be prepared by treating the corresponding .beta.-amino-.beta.-(phenyl or substituted phenyl)-ethylamine with the desired 1,3-bis(alkoxycarbonyl)-S-methylisothiourea or 1-alkoxycarbonyl-S-methylisothiourea. The compounds can also be prepared by treating the corresponding 2-amino-4,5-dihydro-4-(phenyl or substituted phenyl)-imidazole with the desired dialkylcarbonate. The subject compounds are useful as psychotherapeutic agents for treating, preventing or palliating abnormal conditions, in mammals, which are related to the central nervous system.

4,5-Dihydro-2-lower alkoxycarbonylamino-4-phenylimidazoles and

Compounds represented by the formula ##STR1## wherein R is hydrogen or alkyl of 1-4 carbons, R.sup.1 is alkyl of 1-6 carbons and the naphthyl group is attached to the imidazole ring at the 1 or 2 positions of the naphthyl ring and the pharmaceutically acceptable salts thereof are useful as centrally acting skeletal muscle relaxants.

Imidazole-2-carbamates

1-Lower alkyl-4,5-dihydro-5-phenyl-2-lower alkoxycarbonylaminoimidazoles, and substituted phenyl derivatives thereof, and pharmaceutically acceptable salts thereof, and methods of preparing such compounds. In one method, the compounds can be prepared by treating the corresponding .beta.-lower alkylamino-.beta.-(phenyl or substituted phenyl)-ethylamine with the desired 1,3-bis (alkoxycarbonyl)-S-methylisothiourea or 1-alkoxycarbonyl-S-methylisothiourea. The compounds can also be prepared by treating the corresponding 1-lower alkyl-2-amino-4,5-dihydro-5-(phenyl or substituted phenyl)-imidazole with the desired dialkylcarbonate. The subject compounds are useful as psychotherapeutic agents in treating or palliating abnormal conditions, in mammals, which involve the central nervous system.

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San Francisco, CA, United States of America

Klaus K Weinhardt