Crystalline form of (3R,4R)-4-[3-(S)-hydroxy-3-(6 methoxyquinolin-4-propyl]-1-[2-2-thienylthio)ethyl] piperidine-3-carboxylic acid

US6939970B2 · kind B2 · utility

Assignee

• AVENTIS PHARMA S.A. · FR

Inventors

• Jacques Bourget · Vitry-sur-Seine, FR
• Marc-Antoine Perrin · Jouy-en-Josas, FR
• Bernd Janocha · Frankfurt am Main, DE
• Carole Neves · Paris, FR
• Pascal Billot · Paris, FR
• Sylvaine Lafont · Yssingeaux, FR

Key dates

• Filing date: Dec 18, 2003
• Grant date: Sep 6, 2005
• Expiry date: Dec 23, 2023

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D409/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention comprises monohydrated form C of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, represented by the structure and as herein defined by powder X-ray diffraction, processes for preparing monohydrated form C from amorphorous (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid or form A of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, pharmaceutical compositions comprising monohydrated form C and form A or form B of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, pharmaceutical compositions comprising monohydrated form C, form A and form B, methods for treating bacterial infection with monohydrated form C, methods for treating bacterial infection with monohydrated form C and form A or form B, methods for treating bacterial infection with monohydrated form C, form A and form B, and a process for the preparation of form A from monohydrated form C.