Rhone-poulenc Rorer Pharmaceuticals Inc.

Aventis Pharmaceuticals Inc.

Aventis Pharmaceuticals Products Inc.

Matthew R Powers

Michael K O'Brien

Adam W Sledeski

Walter Rodriguez

Raymond D Youssefyeh

Patrick Leon

Luc Grondard

James P Sherbine

Rick G Woodward

Gregory G Kubiak

Benoit J Vanasse

James J Mencel

Zofia J Chrzan

Robert C Liu

Daniel Robin

Jean-Paul Casimir

Vincent Windisch

David Toledo-Velasquez

Anthony J Gardetto

Narasimha M Vemuri

Diane C Salazar

John E Airey

Henry F Campbell

William L Studt

Donald E Kuhla

Scott I Klein

Ching T Tsuei

Tory H Powner

Frederick A Golec

Laurence Pailleres-Hubert

Benoit Viguier

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

This invention is directed to methods for stereospecifically preparing &lsqb;(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)&rsqb;-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.

Steroespecific preparation of chiral 1-aryl- and 1-heteroaryl-2-substituted ethyl-2-amines

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

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

This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.

Stereospecific preparation of chiral 1-aryl-and

The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by a stereospecific catalytic heteroannulation synthesis free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.

Process for preparing dibenzofurans via catalytic heteroannulation

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

The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by an intramolecular Heck stereospecific synthesis substantially free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.

Process for preparing chiral dibenzofurans via intramolecular heck

This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

Pharmaceutically useful dibenzofurancarboxamides of specific

This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.

Process for the preparation of optically pure amides

Growing community of inventors

Barto, PA, United States of America

Matthew R Powers