Pfizer Corporation

Other

Willard M Welch, Jr

Charles A Harbert

Bertrand Leo Chenard

Gene M Bright

Phoebe Chiang

William A Novomisle

Yuhpyng Liang Chen

Allen R Kraska

B Kenneth Koe

Angel Guzman-Perez

Frank S Menniti

Ravi Shanker Garigipati

Kevin K Liu

Paul Andrew Dasilva-Jardine

Mark Leonard Elliott

Compounds of Formula (IC) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HTreceptors in animals are described herein.

5-HT receptor ligands and uses thereof

Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HTreceptors in animals are described herein

Compounds of Formula (IA) that act as 5-HT receptor ligands and their uses in the treatment of diseases linked to the activation of 5-HT receptors in animals are described herein.

The present invention relates to novel atropisomers of 2,3-disubstituted-(5,6)-heteroarylfused-pyrimidin-4-ones, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones

The present invention relates to novel 2,3 disubstituted-4(3H)-quinazolinone compounds of the formula I:

2,3 disubstituded-4(3H)-quinazolinones

Methods of administering CRF antagonists

The invention relates to a method of treating dyskinesias associated with dopamine agonist therapy in a mammal which comprises administering to said mammal a compound, as defined herein, which is an antagonist of the AMPA receptor. Dopamine agonist therapy, as referred to in the present invention, is generally used in the treatment of a central nervous system disorder such as Parkinson's disease.

Methods of administering AMPA receptor antagonists to treat dyskinesias

The present invention relates to novel quinazolin-4-one derivatives of the formula I, as defined in the specification, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

Quinazoline-4-one AMPA antagonists

Substituted pyrazoles as corticotropin-releasing factor (CRF) antagonists

The present invention relates to novel compounds of the formula I, described above, and their pharmaceutically acceptable salts, and pharmaceutical compositions and methods of treating neurodegenerative and CNS-trauma related conditions.

2,3 Disubstituted- (5,6)-heteroarylfused-pyrimidine-4-ones

The compounds of the formula wherein A, R.sub.1, R.sub.3, X.sub.1, Y and Z are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Substituted pyrazoles as CRF antagonists

Compounds of the formula ##STR1## wherein B, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein with reference to formula IX have corticotropin-releasing factor antagonist activity and as such are of use in the treatment of panics, phobias and other stress-related disorders.

A novel process for preparing various 2-substituted-5-aryl-1,2,3,4-tetrahydro-.gamma.-carboline derivatives is provided, which involves (1) condensing a corresponding 2-unsubstituted compound with formaldehyde and an appropriate acetylenic derivative in the presence of cuprous chloride or cuprous bromide, followed by (2) reduction of the corresponding unsaturated intermediate to yield the desired final product. The latter compounds are known to be useful as tranquilizing agents, with 2-[4-(p-fluorophenyl)-4-hydroxybutyl]-5-(p-fluorophenyl)-8-fluoro-1,2,3,4- tetrahydro-.gamma.-carboline representing a preferred final product. The aforesaid unsaturated intermediates are all novel compounds.

Certain

Novel trans-isomeric derivatives of 4-phenyl-1,2,3,4-tetrahydro-1-naphthalenamine are useful as antidepressant agents. These novel compounds act to block the synaptosomal uptake of norepinephrine and serotonin (5-hydroxy-tryptamine), thereby alleviating abnormalities at central receptor sites. The preferred embodiment is the enantiomer trans-(1R)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalen amine and its pharmaceutically acceptable acid addition salts.

Growing community of inventors

Mystic, CT, United States of America

Willard M Welch, Jr