BIMATOPROST CRYSTALLINE FORM I

• US 20110288179A1
• Filed: 05/23/2011
• Published: 11/24/2011
• Est. Priority Date: 08/29/2006
• Status: Abandoned Application

• Current Assignee: FineTech Pharmaceutical Ltd. (RxElite, Inc.)
• Original Assignee: FineTech Pharmaceutical Ltd. (RxElite, Inc.)
• Inventors: Rukhman, Igor, Tishin, Boris, Yudovich, Lev, Vilensky, Alexander, Pertsikov, Boris, Nisnevich, Gennady, GUTMAN, Arie
• Application Number:
  US13/113,136
• Publication Number:
  US 20110288179A1
• Time in Patent Office: Days
• US Class Current: 514/622
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: C07C 2601/08 the ring being saturated
• CPC Class Codes: C07C 405/00 Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
• CPC Class Codes: C07F 7/1804 Compounds having Si-O-C linkages Si-O-acyl linkages C07F7/1896

Abstract

The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.

Claims

1. A pure bimatoprost, wherein said bimatoprost contains (by HPLC) not more than (NMT) 2% of sum of all related impurities and 1% of 5-trans isomer.

2. The pure bimatoprost according to claim 1, wherein said bimatoprost contains (by HPLC) not more than (NMT) 1.5% of sum of all related impurities and 0.7% of 5-trans isomer.

3. The pure bimatoprost according to claim 1, wherein said bimatoprost contains (by HPLC) not more than (NMT) 1% of sum of all related impurities and 0.5% of 5-trans isomer.

4. The pure bimatoprost according to claim 1, wherein said bimatoprost is free of 5-trans and 15(R)-isomers of bimatoprost.

5. The pure bimatoprost according to claim 1, wherein said bimatoprost contains by LC not more than (NMT) 0.2% each of 5-trans isomer and 15(R) isomer.

6. The pure bimatoprost according to claim 1, wherein said bimatoprost contains by LC not more than (NMT) 0.1% each of 5-trans isomer and 15(R) isomer.

7. The pure bimatoprost according to claim 1, wherein said bimatoprost contains by LC not more than (NMT) 0.05% each of 5-trans isomer and 15(R) isomer.

8. A method for preparing a pharmaceutical or cosmetic composition by combining effective amount of said bimatoprost according to claim 1 with a pharmaceutical or cosmetic acceptable vehicle.

9. Use of crystalline form I of bimatoprost for the preparation of pure bimatoprost.