IP Library Granted Patent US 9,409,875
Granted Patent B2
US 9,409,875 · App. 14/920,080 · Granted Aug 9, 2016

Crystal modifications of elobixibat

Inventors: Martin Bohlin (Johanneshov, SE); Erica Tjerneld (Enskede, SE); Andreas Vestermark (Stockholm, SE); Ingvar Ymen (Saltsjo-boo, SE)
Assignee: Elobix AB
C07D281/02C07D281/10
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Quick Facts
Patent No.
US 9,409,875
App. No.
14/920,080
Granted
Aug 9, 2016
Kind
B2
Abstract

The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.

Claims (6)

1. Crystal modification IV of elobixibat, having an XRPD pattern, obtained with CuKα1-radiation, with peaks at °2θ positions 6.3±0.2 and 19.4±0.2.

2. The crystal modification according to claim 1 , having an XRPD pattern, obtained with CuKα1-radiation, with peaks at °2θ positions 6.3±0.2 and 19.4±0.2 and one or more of the characteristic peaks: 10.2±0.2, 10.5±0.2, 9.4±0.2, 9.5±0.2, 12.5±0.2, 14.6±0.2, 15.6±0.2, and 23.3±0.2.

3. Crystal modification IV of elobixibat according to claim 1 , having an XRPD pattern, obtained with CuKα1-radiation, as shown in FIG. 1 .

4. Crystal modification I of elobixibat, having an XRPD pattern, obtained with CuKα1-radiation, with peaks at °2θ position 5.2±0.2 and 10.0±0.2.

5. Crystal modification I of elobixibat according to claim 4 , having an XRPD pattern, obtained with CuKα1-radiation, as shown in FIG. 4 .

6. The crystal modification according to claim 4 , having an XRPD pattern, obtained with CuKα1-radiation, with characteristic peaks at °2θ positions: 5.2±0.2 and 10.0±0.2 and one or more of the characteristic peaks: 4.9±0.2, 6.0±0.2, 7.6±0.2, 10.5±0.2, 11.3±0.2, 18.8±0.2, 20.4±0.2, and 22.9±0.2.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 15, 2015
From: BOHLIN, MARTIN; TJERNELD, ERICA; VESTERMARK, ANDREAS; YMEN, INGVAR
To: ELOBIX AB
Reel/Frame 037291/0080 →
Priority Claims (1)
SE 1350517 · Apr 26, 2013 · national
Continuity (2)
Continuation PCTEP2014058432 · Apr 25, 2014
Related Publication 20160039777A1 · Feb 11, 2016