Aventis Pharma S.a.

Other

Millennium Pharmaceuticals Limited

Carole Neves

Pascal Billot

Aurelia Chevalier

Jacques Bourget

Marc Antoine Perrin

Bernd Janocha

Sylvaine Lafont

Serge Mignani

Michel Tabart

Michel Cheve

The citrate salt of (S)-4-(4-Chloro-phenyl)-1-{3-[7-(1-hydroxy-1-methyl-ethyl)-11H-10-oxa-1-aza-dibenzo[a,d]cyclohepten-5-ylidene]-propyl}-3,3-dimethyl-piperidin-4-ol, which may be used in pharmaceutical applications, is disclosed. The crystalline Citrate Salt, including particular single crystal forms and combinations of the single crystalline forms, are also discussed. Mixtures for forming the crystalline salts are discussed. As well, methods of producing the Citrate Salt, and crystalline forms thereof, and using such Citrate Salt, and crystalline forms thereof, in treating diseases associated with aberrant leukocyte recruitment, activation, or recruitment and activation are also discussed.

Solid forms of a chemokine receptor antagonist and methods of use thereof

The present invention comprises crystalline forms 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 characterized herein by powder X-ray diffraction patterns as form A and form B, processes for preparing form A from the purified amorphous form of (3R,4R)-4-[3-(S)-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-[2-(2-thienylthio)ethyl]piperidine-3-carboxylic acid, a processes for preparing form A by heating 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, a pharmaceutical composition comprising form A, a pharmaceutical composition comprising form A and form B or monohydrated form C, a pharmaceutical composition comprising form A, form B and monohydrated form C, a method for treating a bacterial infection with form A, a method for treating a bacterial infection with form A and form B or monohydrated form C, and a method for treating a bacterial infection with form A and form B and monohydrated form C.

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

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 structureand 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.

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

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Paris, France

Carole Neves