Hoechst Marion Roussel

Hoechst Roussel Pharmaceuticals

Aventis Pharmaceuticals Inc.

John D Tomer, Iv

Gregory M Shutske

Kevin J Kapples

Brian S Freed

R Richard Hamer

David M Fink

Barbara E Kurys

Richard C Effland

Lawrence L Martin

Joseph T Klein

Nicholas J Hrib

John G Jurcak

James Hendrix

Gregory Shutske

Reda Hanna

The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as Dantagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of Dreceptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

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There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antienmtics, and for the treatment of personality disorders such as obsessive compulsive disorder.

Substituted pyridylamino indoles

Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.

Pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles

Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Aminoalkyloximers

Pyridiniminyl-1,2-benzisothiazoles

Aminoalkyloximes

Aminoalkyloximes for treating depression and affective disorders

Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.

Aminoalkyloximes useful in the treatment of depression and obsessive

Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.

Certain 6,7-dihydro-3(2-nitrophenyl)-1,2-benzisoxazol-4(5H)-ones as

There are disclosed novel pyrazolo[4,3-c]pyridines of the formula ##STR1## where Ar and R.sub.1 are as defined in the specification, which are useful as serotonin reuptake inhibitors and as such may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.

Pharmaceutically useful

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Perkasie, PA, United States of America

John D Tomer, Iv