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

US6753409B1 · kind B1 · utility

Assignee

• Aventis Pharmaceuticals Inc. · US

Inventors

• Zofia J. Chrzan · Sellersville, US
• James J. Mencel · North Wales, US
• David Toledo-Velasquez · Lansdale, US
• Vincent Windisch · Green Lane, US
• Rick G. Woodward · Harleysville, US
• Diane C. Salazar · Carbondale, US
• Narasimha M. Vemuri · West Malling, GB
• Anthony J. Gardetto · Oley, US
• Matthew R. Powers · Barto, US
• Gregory G. Kubiak · Wilmington, US
• Robert C. Liu · Kankakee, US
• Benoit J. Vanasse · Collegeville, US
• James P. Sherbine · Voorhees, US
• Walter Rodriguez · Nazareth, US
• Adam W. Sledeski · Bound Brook, US

Key dates

• Filing date: Aug 15, 2000
• Grant date: Jun 22, 2004
• Expiry date: Nov 14, 2020

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

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)-&bgr;-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 wherein:A, B, Z, E1, E2, G, R, m, n, and p are as defined herein.