Hoechst Roussel Pharmaceuticals

Hoechst Marion Roussel

Aventis Pharmaceuticals Inc.

Other

Aventis Hoklings Inc.

Frommer Lawrence & Huag Llp

Hoeschst-roussel Incorporated

Heochst-roussel Pharmaceuticals, Inc.

Nicholas J Hrib

John G Jurcak

Helen H Ong

Joseph R Perez

Gregory M Shutske

Kevin J Kapples

Brian S Freed

Gregory H Merriman

John Dick Tomer

Raymond W Kosley, Jr

John J Tegeler

Barbara S Rauckman

Kirk D Shoger

David Fink

George Lee

Joseph T Strupczewski

Kenneth J Bordeau

John D Tomer, Iv

Philip M Weintraub

Brian K Whiteley

Alexandre Gross

Ramalinga M Dharanipragada

James Hendrix

Kwon Yon Musick

Gregory Shutske

Jeffrey Stephen Sabol

Reda Hanna

Joseph T Klein

Abdul E Mutlib

The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl 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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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.

This invention discloses and claims a new class of indole derivatives for use in treating allergy, asthma, rhinitis, dermatitis, B-cell lymphomas, tumors and diseases associated with bacterial, rhinovirus or respiratory syncytial virus (RSV) infections. It has now been found that the compounds of this invention are capable of modulating T helper (Th) cells, Th1/Th2, and thereby capable of inhibiting the transcription of interleukin-4 (IL-4) message, IL-4 release or IL-4 production.

Indole derivatives as interleukin-4 gene expression inhibitors

There are disclosed compounds of the formula,

3-&lsqb;4-(1-substituted-4-piperazinyl)butyl&rsqb;-4-thiazolidinone and related compounds

4,5-Dihydronaphth�1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT.sub.3 antagonists. These compounds art useful for the treatment of anxiety, psychiatric disorders, nausea, vomiting and drug dependency.

4,5-dihydronaphth (1,2-c) isoxazoles and derivatives thereof

There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.

Substituted-4-amino-3-pyridonols

Substituted-4-amino-3-pyridinols

A compound selected from the following formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, m and n are as defined in the specification having antipsychotic activity.

3-�4-(1-substituted-4-piperazinyl)butyl!-4-thiazolidinone and related

This invention relates to compounds of the formula ##STR1## wherein X is halogen, hydroxy, (C.sub.1 -C.sub.6)alkoxy, amino or trifluoromethyl; and Y is --CN or --NR.sup.1 R.sup.2 ; where l is an integer of 0, 1 or 2; m is an integer of 0, 1 or 2; n is an integer of 2, 3 or 4, except when Y is CN, in which case n can also be 1; R.sup.1 is hydrogen, (C.sub.1 -C.sub.6)alkyl or (C.sub.1 -C.sub.6)alkylcarbonyl; R.sup.2 is hydrogen, (C.sub.1 -C.sub.10)alkylcarbonyl, (C.sub.3 -C.sub.12)cycloalkylcarbonyl, hydroxy-(C.sub.1 -C.sub.6)alkylcarbonyl, phenylcarbonyl, thienylcarbonyl or benzothienylcarbonyl; or

Substituted benzothienylpiperazines and their use

Novel 1-piperazinyl-2-butenes and -2-butynes, intermediates and processes for the preparation thereof, and methods of treating psychoses utilizing compounds or compositions thereof are disclosed.

1-piperazinyl-2-butenes and -2-butynes

There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

3-&lt;4-substituted-4-piperazinyl)buty]-4-thiazolidinone and related

Novel heteroarenylpiperazines, intermediates and processes for the preparation thereof, and methods for treating psychoses utilizing compounds or compositions thereof are disclosed.

Heteroarenylpiperazines

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Somerville, NJ, United States of America

Nicholas J Hrib