Eli Lilly and Company

Lilly Industries, Inc.

Lilly, Sa

David Edward Tupper

Terrence M Hotten

Jiban Kumar Chakrabarti

Charles A Bunnell

John M Schaus

Barry P Clark

John Fairhurst

Charles M Beasley, Jr

Graham H Timms

Thomas H Ferguson

Barry A Hendriksen

Manuel V Sanchez-Felix

Thomas Daniel Aicher

Vincent Patrick Rocco

Joseph H Krushinski, Jr

Zhaogen Chen

Samuel Dean Larsen

Maria I Fernandez

Douglas J Allen

Maria Isabel Fernandez Fernandez

Marta Maria Pineiro-Nunez

David C Horwell

Norman D Brooks

Sharon L Shinkle

Kevin Michael Ruley

Kurt D Dekemper

Stuart J Garvin

Linda C Murray

Snehlata S Mascarenhas

James Allen Monn

David T Wong

Margaret Mary Faul

Dennis C Thompson

Patrick Gianpietro Spinazze

Yvan Le Huerou

Ying Chen

Jingdan Hu

Lourdes Prieto

David Scott Coffey

Carlos Montero Salgado

Fionna Mitchell Martin

Stacy Jo Keding

Sandra Ginette Milutinovic

Yvan LeHuerou

Martine Keenan

Lesley Walton

Reba Chakrabarti

Teresa Tse Ki Man

John Mehnert Schaus

Joseph Herman Junior Krushinski

The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, and generalized anxiety disorder.

Bicyclo (3.1.0) hexane-2, 6-dicarboxylic acid derivatives as mGlu2 receptor agonist

Compounds and pharmaceutical compositions comprising compounds of the Formula as CBreceptor inverse agonists useful for reducing body weight in mammals, treating cognitive impairment associated with schizophrenia, and mitigating treatment emergent weight gain observed during treatment with antipsychotics.

1, 5-diphenyl-3-benzylamino-1, 5-dihydropyrrolidin-2-one as CB1 receptor modulators

Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C) alkylene or hydroxy substituted (C) alkylene; X is oxygen or sulfur; Ris hydrogen, (C) fluroalkyl, (C) cycloalkyl, or (C) alkyl, wherein the (C) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCHCHOH, or &#x2014;CN; Ris H, halogen, (C) fluoroalkyl, (C) cycloalkyl, OR, SR, NO, CN, COR, C(O)OR, CONRR, NRR, SONRR, NRCOR, NRSOR, optionally substituted aromatic, or (C) alkyl, wherein (C) alkyl is unsubstituted or substituted with a hydroxy group; Ris hydrogen (C) fluoroalkyl, (C) alkenyl, Ar, (C)alkyl-Ar, or (C) alkyl wherein (C) alkyly is unsubstituted or substituted with a phenyl; Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic, Ris hydrogen, (C) alkyl, (C) fluoroalkyl, or optionally substituted aromatic; Rand Rare independently hydrogen, (C) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Zand Zare independently selected from hydrogen, halogen, (C) alkyl, (C) fluoroalkyl, OR, SR, NO, CN, COR, CONRR, NRR, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I) 

Piperazine substituted aryl benzodiazepines

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure:

Process for preparing 2-methyl-thieno-benzodiazepine

The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.

2-methyl-thieno-benzodiazepine formulation

Described herein are antipyschotic compounds of formula (I) wherein,

Piperazine substituted aryl benzodiazepines and their use as dopamine receptor antagonists for the treatment of psychotic disorders

The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation or olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.

A pharmaceutical compound of formula (I) in which R and R are each hydrogen or C alkyl, or R and R together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C alkyl substituents, R is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.

3-bicycloaryl-2-aminomethyl bicycloalkanes as serotonine reuptake inhibitors

Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.

Thienobenzodiazepine compounds

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-[2,3-b][1,5]benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-�2,3-b!�1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of mental disorders. The compound has the following structure: ##STR1##

Mental disorders

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno -�2,3-b!�1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders of the central nervous system. The compound has the following structure: ##STR1##

Methods of treatment using a thieno-benzodiazepine

2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno-�2,3-b!�1,5!benzodiazepine, or an acid salt thereof, has pharmaceutical properties, and is of particular use in the treatment of disorders relating to the use of psychoactive substances. The compound has the following structure: ##STR1##

Psychoactive substance disorders

The invention provides lower alcohol solvates of 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno�2,3-b!�1,5!benzodiazepine (olanzapine) and a process for making such lower alcohol solvates of olanzapine. The invention provides a method for using such solvates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.

Process and solvate of 2-methyl-thieno-benzodiazepine

Growing community of inventors

Reading, United Kingdom

David Edward Tupper