Pseudopolymorphic forms of a HIV protease inhibitor

• US 7,700,645 B2
• Filed: 05/16/2003
• Issued: 04/20/2010
• Est. Priority Date: 05/16/2002
• Status: Active Grant

• Current Assignee: Janssen Sciences Ireland Unlimited Company (Johnson & Johnson)
• Original Assignee: Tibotec Pharmaceuticals (Johnson & Johnson)
• Inventors: Vermeersch, Hans Wim Pieter, Janssens, Luc Donne Marie-Louise, Thone, Daniel Joseph Christiaan
• Primary Examiner(s): Chang; Celia
• Application Number:
  US10/514,352
• Publication Number:
  US 20050250845A1
• Time in Patent Office: 2,531 Days
• Field of Search: 514/456, 549/396
• US Class Current: 514/456
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 31/18 for HIV
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 493/04 Ortho-condensed systems

Abstract

New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.

Claims

1. An ethanolate solvate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate, in which the ratio of compound to ethanol is about 1:

1.

2. A solvate having the formula:

3. A composition comprising an ethanolate solvate of the compound (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate, in which the ratio of compound to ethanol is about 1:

1, and an inert carrier.

4. The composition of claim 3 wherein the inert carrier is a pharmaceutically acceptable carrier.

5. The composition of claim 4 wherein the pharmaceutically acceptable carrier is a solid inert carrier.

6. A composition comprising a solvate having the formula:

7. The composition of claim 6 wherein the inert carrier is a pharmaceutically acceptable earner.

8. The composition of claim 7 wherein the pharmaceutically acceptable carrier is a solid inert carrier.