Cyclohexanecarboxylic acid compound

• US 7,691,894 B2
• Filed: 07/23/2004
• Issued: 04/06/2010
• Est. Priority Date: 07/24/2003
• Status: Expired due to Fees

• Current Assignee: Daiichi Pharmaceutical Company Limited (Daiichi Sankyo Company Limited)
• Original Assignee: Daiichi Pharmaceutical Company Limited (Daiichi Sankyo Company Limited)
• Inventors: Noguchi, Shigeru, Ono, Makoto
• Primary Examiner(s): Shameem; Golam M. M.
• Assistant Examiner(s): Loewe; Sun Jae Y
• Application Number:
  US10/562,122
• Publication Number:
  US 20070105936A1
• Time in Patent Office: 2,083 Days
• Field of Search: None
• US Class Current: 514/414
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 27/16 Otologicals
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/04 specific for metastasis
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 403/12 linked by a chain containing hetero atoms as chain links

Abstract

The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate.

Claims

1. Sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate, which is in the form of Type-II crystals having the full XRD pattern of FIG. 4.

2. A pharmaceutical composition comprising, as an active ingredient, a compound as described in claim 1 is in a form of a capsule.