Eli Lilly and Company

Lilly Industries, Inc.

Charles A Bunnell

David Edward Tupper

Samuel Dean Larsen

Barry A Hendriksen

Thomas H Ferguson

Manuel V Sanchez-Felix

Terrence M Hotten

Douglas J Allen

Sharon L Shinkle

Norman D Brooks

Snehlata S Mascarenhas

Stuart J Garvin

Linda C Murray

Kurt D Dekemper

Gregory Alan Stephenson

James M Greene

Susan M Reutzel

John Richard Nichols

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

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.

The present invention provides a process for preparing olanzapine and intermediates therefor.

Intermediates and process for preparing olanzapine

The invention provides Form II, a pharmaceutically elegant, stable polymorph of olanzapine useful for treating a condition selected from the group consisting of a psychotic condition, mild anxiety and gastrointestinal conditions.

Olanzapine polymorph crystal form

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

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 solyates of olanzapine. The invention provides a method for using such solyates of olanzapine to prepare substantially pure anhydrous Form I 2-methyl-thieno-benzodiazepine.

An improved process for preparing trialkylsilyl ester and acid halide derivatives of carboxylic acids is provided along with novel trialkylsilyl ester intermediates of 2-(2-furyl)-2-methoximinoacetic acid.

Process for preparing acid halides

A process for preparing certain substituted benzyl esters of phenylacetic acids by esterification in a solvent in which the salt of the acid is insoluble, and in the presence of a phase transfer catalyst.

Synthesis of substituted benzyl esters

Cephalosporin sulfoxides are reduced to the corresponding cephalosporins in the presence of a halogen scavenger with triaryl phosphite-halogen complexes derived from the kinetically controlled reaction of selected triaryl phosphites and chlorine or bromine.

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Lafayette, IN, United States of America

Charles A Bunnell