Hoechst Roussel Pharmaceuticals

Aventis Pharmaceuticals Inc.

Hoechst Marion Roussel

Sanofi-A Ventis Deutschland Gmbh

Aventis Hoklings Inc.

Hoescht Roussel Pharmaceuticals Inc.

Gregory H Merriman

Brian S Freed

Barbara S Rauckman

John J Tegeler

Russell R Hamer

Russell R Harner

Nicholas J Hrib

Brian K Whiteley

Alexandre Gross

Jeffrey Stephen Sabol

Joseph T Klein

Raymond W Kosley, Jr

Siegfried Stengelin

Kenneth J Bordeau

Matthias Gossel

Thomas Klabunde

Daniel Gerard McGarry

Martin Smrcina

Pavel Safar

David Fink

George Lee

Carolina Lanter

Liang Ma

David Rampe

Patrick Shum

Francis A Volz

James Spoonamore

Garth E Ringheim

Zhaoxia Yang

Russell R Harmer

John G Jurcak

Stefanie Flohr

Philip M Weintraub

David M Fink

Barbara E Kurys

Petra Lennig

Ramalinga M Dharanipragada

Kwon Yon Musick

Petra Stahl

Russell Richard Lee Hamer

Russell R Hanner

Daniel G Mcgarry

Alexandre 245 Eighth Street Gross

The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments.

Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids

The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R, R, R, R, R, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.

Heterocyclic compounds as P2X7 ion channel blockers

Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for the preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Nitrogen-substituted hexahydropyrazino[1,2-A]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments

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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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

Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.

1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino 1,3-propanediols and related compounds

Novel N-(pyridinylamino)isoindolines and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the N-(pyridinylamino)isoindolines and related compounds, the intermediates or compositions thereof are disclosed.

N-(pyridinylamino) isoindolines and related compounds

1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino- 1,3-propanediols and

This invention relates to 3-aryl-2-(1-substituted-4-piperidinyl)-1,1-dioxo-3H-benzo[d]isothiazoles and related compounds of the formula, ##STR1## where X and Y are independently halogen, loweralkyl, loweralkoxy, arylloweralkoxy, acyl, hydroxy, nitro, amino, trifluoromethyl and hydrogen; n, p and q are independently integers of 1 or 2; R is hydrogen, loweralkyl, aryloweralkyl, acyl, --(CH.sub.2).sub.m --OR.sub.1,--(CH.sub.2)NHR.sub.1, ##STR2## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, acyl and loweralkoxycarbonyl; Z is hydrogen, halogen, loweralkyl, loweralkoxy and acyl; m is an integer of 2 to 4; is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof and the optical isomers thereof where such isomers exist.

3-aryl-2-(1-substituted 4-piperidinyl)-1,1-dioxo-3H-benzo[D]isothiazoles

1-alkyl-,1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and

1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and

1-Alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and

Growing community of inventors

Fairfield, OH, United States of America

Gregory H Merriman