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Crystalline form of SLF

IP.com Disclosure Number: IPCOM000147748D
Publication Date: 2007-Mar-25
Document File: 2 page(s) / 79K

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Crystalline form of SLF

   (3R)-1-Azabicyclo[2.2.2]oct-3-yl-(1S)-1-phenyl-3,4-dihydroisoquinoline-2-(1H)- carboxylate (1(S)-Phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylic acid 3(R)- quinuclidinyl ester) is known as SLF. SLF has the molecular formula: C23H26O2, a

molecular weight of 362.4647 and the following chemical structure:

N

O N

               C23H26N2O2
Exact Mass: 362.1994
Mol. Wt.: 362.4647
m/e: 362.1994 (100.0%), 363.2028 (25.6%), 364.2061 (3.1%)

C, 76.21; H, 7.23; N, 7.73; O, 8.83

   SLF succinate is a urinary antispasmodic, acting as a selective antagonist to the M(3)-receptor. It is used for the treatment of symptoms of overactive bladder, such as urinary urgency and increased urinary frequency, as may occur in patients with overactive bladder syndrome ("OAB"). SLF succinate is currently marketed under the tradename VESICARE®. VESICARE® has been approved by the FDA for once daily treatment of OAB and is prescribed as 5 mg and 10 mg tablets.

   Sample of SLF succinate, prepared according to WO 2005/105795, was analyzed by X-Ray Powder diffraction and found to contain crystal Form of SLF. Pattern 1 is the XRD pattern of crystal Form SLF.

Pattern#1:

O

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SLF RR-713 with spin.raw

   According to pattern 1, the crystalline form of SLF succinate is characterized by X- ray powder diffraction (XRPD) ma...