Eli Lilly and Company

Thomas M Wilson

Charles J Barnett

Michael Edward Kobierski

John M Schaus

Michael J Martinelli

Marlene L Cohen

Dennis C Thompson

Steven Swanson

John T Catlow

Scott Allan May

Bret Anthony Astleford

Paul Leslie Ornstein

Tony Yantao Zhang

Bret E Huff

Ana Maria Escribano

Thomas John Bleisch

Andrew Michael Ratz

Julie Kay Bush

Susan Marie Reutzel-Edens

Ana Isabel Mateo Herranz

Michael E Kopach

Michael Edward LeTourneau

Jose Antonio Martinez-Perez

Michael O Martinelli

Darrell Robert Hutchison

The disclosure provides process developments and novel routes for the preparation of the NK-1 receptor antagonist, Compound (I) and intermediates in those routes. 

Process development of a pyridine-containing NK-1 receptor antagonist

The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).

Excitatory amino acid receptor antagonists

The present invention relates to a one-pot process for preparing a compound of formula I: I; by reacting a compound of formula II with a compound of formula III: in the presence of a suitable solvent, a suitable base, a palladium catalyst and a suitable ligand.

Synthesis of 2-aryl-1-naphthol derivatives via a tandem palladium catalyzed arylation and dehydrogenation

This invention provides a process to prepare (2R)-anti-5-&lcub;3-&lsqb;4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl&rsqb;-2-hydroxypropoxy&rcub;quinoline.

Process for preparing a 10,11-methanodibenzosuberane derivative

This invention provides a process to prepare 10,11-(optionally substituted)methanodibenzosuberane derivatives. The invention also provides an intermediate in this process.

Process for preparing 10,11-methanobenzosuberane derivatives

The compounds are of the class of pyrrolo&lsqb;2,3-d&rsqb;pyrimidines useful for inhibiting sPLA mediated release of fatty acids for treatment of diseases such as septic shock.

Bicyclic sPLA2 inhibitors

This invention provides a process for preparing a compound of formula III ##STR1## wherein R.sup.1 is bromo, iodo or COOR.sup.2 ;

Cyclization for preparing antifolate compounds

The invention provides a method of preparing compounds of formula I and VIII: ##STR1## which are useful intermediates to compounds that are used as antagonists and partial agonists for the serotonin receptor 5-HT.sub.4.

Process for preparing 3-substituted indazoles

Processes for preparing 5-substituted pyrrolo�2,3-d!pyrimidines which are useful as intermediates for the preparation of pyrrolo�2,3-d!pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.

Process for preparing 5-substituted pyrrolo-�2,3-d!pyrimidines

Indazolecarboxamides are used as antagonists and partial agonists for the serotonin receptor 5-HT.sub.4 and provide therapeutic methods for treatment of disorders caused by or affected by dysfunction of the 5-HT.sub.4 receptor.

Indazolecarboxamides

Processes for preparing 5-substituted pyrrolo[2,3-d]pyrimidines which are useful as intermediates for the preparation of pyrrolo[2,3-d]pyrimidine antineoplastic agents or as antineoplastic agents themselves are provided.

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Speedway, IN, United States of America

Thomas M Wilson