Neurogen Corporation

Bristol-myers Squibb Compnay

Other

Xi Chen

Jun Yuan

Andrew Y Thurkauf

Piyasena Hewawasam

John E Starrett, Jr

Jan William Wasley

Milind Deshpande

Atul Agarwal

Min Ding

Xiao-shu He

Michael F Summers

Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R, R, R, R, X, Y, Z, A, A, A, R, R, R, and Rare defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.

Inhibitors of HIV-1 capsid formation: substituted aryl aminomethyl thiazole ureas and analogues thereof

Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein:

1-phenyl-4-benzylpiperazines dopamine receptor subtype specific ligands

1-phenyl-4-benzlpiperazines: dopamine receptor subtype specific ligands

N-aminoalkyldibenzothiopencarboxamide receptor subtype specific ligands

The present invention provides novel carbamate oxadiazolone derivatives having the general formula

Carbamate derivatives of diaryl 1,3,4-oxadiazolone

1-(Benzothiazol-2-yl)-4-(1-phenylmethyl) piperazines: dopamine receptor subtype specific ligands

2-(2, 3-dihydrobenzofuran-5-yl)-4-aminomethylimidazoles: dopamine receptor subtype specific ligands

N-aminoalkyl-2-anthracenecarboxamides; new dopamine receptor subtype specific ligands

N-aminoalkyldibenzothiophenecarboxamides new dopamine receptor subtype specific ligands

1-phenyl-4-benzylpiperazines; dopamine receptor subtype specific ligands

Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R.sub.a represents ##STR2## where X, Y and Z are the same or different and represent CH or nitrogen;

2-Aryl-4-(1-[4-heteroaryl]piperazin-1-yl)methylimidazoles: dopamine      .

The present invention provides novel carbamate oxadiazolone derivatives having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.

Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; or

N-aminoalkyldibenzothiophenecarboxamides; new dopamine receptor subtype

Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable salts thereof wherein wherein: R.sub.1, R.sub.2, and and R.sub.4 independenlty represent hydrogen, halogen, alkyl, cyano, alkoxycarbonyl, trifluoromethoxy, SO.sub.2 NH.sub.2 or trifluoromethyl; R.sub.3 represents hydrogen, halogen, alkyl, alkoxy, alkylthio, hydroxy, amino, mono- or di(C.sub.1 -C.sub.6)alkylamino, cyano, alkoxycarbonyl, trifluoromethoxy, SO.sub.2 NH.sub.2 or trifluoromethyl; or R.sub.3 represents optionally substituted phenyl; X represents (CH.sub.2).sub.n where n is an integer; and m is 0 or an integer, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

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Clinton, CT, United States of America

Xi Chen