Bristol-myers Squibb Pharma Company

Dupont Pharmaceuticals Company

Britsol-myers Squibb Company

Jaan A Pesti

Jianguo Yin

Philip Ma

Shawn K Pack

James P Sherbine

Michael B Maurin

Robert E Yule

Kenneth C McNulty

Luigi Anzalone

Chiajen Lai

Robert Dicosimo

Joseph M Fortunak

David Kenneth Leahy

Lori Ann Spangler

Lucius Thomas Rossano

Gerard Crispino

Francis S Gibson

Lin-Hua Zhang

John E Thornton

Paul C Lobben

Zhongmin Xu

Goss S Kauffman

Robert P Discordia

George F Huhn

Thomas L LaPorte

Jale Muslehiddinoglu

Randall K Ward

David John Meloni

Lin Hua Zhang

Mourad Hamedi

The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula:  Compound I has been shown to be useful for the treatment of certain types of cancer.

Process for the preparation of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2, 1-F][1,2,4]triazin-6-yloxy]-1-methylethyl ester

The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression. 

Process for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof

The present invention provides novel processes and intermediates for preparing corticotropin releasing factor (CRF) receptor antagonists having the structure below which are useful in treating CRF-related disorders such as anxiety and depression 

Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof

The present invention relates to a process for the enantioselective enzymatic aminolysis of racemic 2-&lsqb;3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl&rsqb;acetate ((R/S)-I) by methyl N -Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluenesulfonic acid. More specifically, this invention pertains to a process for the enantioselective enzymatic aminolysis of racemic isobutyl 2-&lsqb;3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl&rsqb;-acetate by methyl N -Boc-L-&agr;,&bgr;-diaminoproprionate.p-toluene sulfonic acid to produce (R)-methyl-3-&lsqb;&lsqb;&lsqb;3-(4-cyanophenyl)-4,5-dihydro-5-isoxazolyl&rsqb;acetyl&rsqb;amino&rsqb;-N-(butoxycarbonyl)-L-alanine, an intermediate in the preparation of roxifiban, an isoxazoline-based platelet glycoprotein IIb/IIIa antagonist which has activity as an antithrombotic agent.

Enantioselective enzymatic aminolysis of a racemic 2-isoxazolylacetate alkyl ester

The potent platelet glycoprotein IIb/IIIa antagonist, roxifiban, is produced in crystalline form. Crystalline roxifiban exists in two polymorphic forms, designated Form 1 and Form 2. These polymorphic forms are characterized by x-ray powder diffraction and solid-state carbon NMR. Pharmaceutical compositions and methods for the treatment or prevention of diseases mediated by platelet aggregation are described.

Crystalline roxifiban

The present invention relates to processes for the synthesis of a crystalline polymorph of 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone in high purity. The product is useful in the synthesis of pharmaceutical compounds for the reduction of cholinergic system dysfunction.

Crystalline 10,10-Bis((2-fluoro-4-pyridinyl)methyl)-9(10H)-Anthracenone and an improved process for preparing the same

The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.

Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic

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Yardley, PA, United States of America

Jaan A Pesti