E.i. Dupont De Nemours and Company

The Dupont Merck Pharmaceutical Company

Dupont Pharmaceuticals Company

Jenrin Discovery, Inc.

Dupont Pharmaceuticals, Inc.

Bristol-myers Squibb Pharma Corporation

Parthasarathi Rajagopalan

Robert J Chorvat

Richard M Scribner

Penio Pennev

Richard Eric Olson

Paul Joseph Gilligan

Rajagopal Bakthavatchalam

John Francis McElroy

James Peter Beck

The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).

MAO-B inhibitors useful for treating obesity

Aryloxy- and arylthiosubstituted pyrimidines and triazines and derivatives thereof

The present invention provides novel compounds, and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsey, irritable bowl syndrome, immune supression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula:

Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae:

6-aryloxy and arylthiopurines

Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ##STR1## wherein R.sup.1, R.sup.13, X, Y, Z, G and Q are as defined herein.

Aryloxy- and arylthio- fused pyridines and pyrimidines and derivatives

This invention provides pyrido[4',3':2:3]indolo-[1,7-ab][1,5]benzodiazepines, pharmaceutical compositions containing these compounds, and methods of using these compounds to treat physiological or drug induced psychosis and/or dyskinesia.

Pyridoindolobenzodiazepines and derivatives as antipsychotics

Benzo-fused cycloalkane and oxa- and thia- cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.

Benzo-fused cycloalkane and oxa- and thia-, cycloalkane

Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetrahy dronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.

Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine

Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benezeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.

Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benzeneacetamide, and the pharmaceutically acceptable salts of N-oxides thereof, are useful as analgesics and/or diuretics.

Benoz-fused cycloalkane trans-1,2-diamine derivatives

Pyridoindolobenzodiazepines, including 1,2,3,4-tetrahydropyrido[4',3':2,3]indolo[1,7-ab][1,4]benzodiazepine-9(8H) -ones and 1,2,3,4,8,9-hexahydro- and 1,2,3,4,4a,8,9,14a-octahydropyrido[4',3':2,3]indolo[1,7-ab][1,4]benzodiaze pines, are useful as tranquilizers.

Pyridoindolobenzodiazepine tranquilizers

This invention relates to (.+-.)1,2,3,4,4a,5,10,10a-octahydro-5,10-o-benzenobenz[g]isoquinoline derivatives which are useful as antidepressants.

Growing community of inventors

Chennai, India

Parthasarathi Rajagopalan