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

US8481737B2 · kind B2 · utility

Assignee

• Millennium Pharmaceuticals, Inc. · US

Inventors

• Carole Neves · Paris, FR
• Aurelia Chevalier · Dreux, FR
• Pascal Billot · Paris, FR

Key dates

• Filing date: May 26, 2011
• Grant date: Jul 9, 2013
• Expiry date: May 26, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D491/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.