Aventis Pharmaceuticals Products Inc.

Aventis Pharmaceuticals Inc.

Rhone-poulenc Rorer Pharmaceuticals Inc.

Walter Rodriguez

Matthew R Powers

Adam W Sledeski

James P Sherbine

Rick G Woodward

Benoit J Vanasse

Zofia J Chrzan

James J Mencel

Robert C Liu

Gregory G Kubiak

Vincent Windisch

David Toledo-Velasquez

Anthony J Gardetto

Diane C Salazar

Narasimha M Vemuri

Raymond D Youssefyeh

Michael K O'Brien

John E Airey

Diane C Salazar, Deceased

STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-&lsqb;N-&lsqb;N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL&rsqb;ASPARTYL&rsqb;-L-&bgr;-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES

The invention is directed to improved methods for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.

Process for preparing N6-substituted adenosine derivatives

The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.

Stable non-hygroscopic crystalline form of

Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT.sub.3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any significant D.sub.2 receptor binding affinity, therapeutic compositions and methods of treatment of disorders which result from 5-HT.sub.3 activity using said compounds. Processes for their preparation and the preparation of their intermediates are also disclosed.

2,6-methano-2H-1-benzoxocincarboxylic acids, esters and amides

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Douglasville, PA, United States of America

Walter Rodriguez