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US 7,888,394 B2Granted
Synthesis, polymorphs, and pharmaceutical formulation of FAAH inhibitors
AssigneeN.V. Organon
InventorsDavid Putman, Olivier Dasse
Life of this patent
Estimating the term…
Abstract
Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.
Claims17
A process for preparing of the alkylcarbamic acid aryl ester of Formula (I):
- comprising the steps of:
- (a) reacting cyclohexyl isocyanate with 3′-hydroxybiphenyl-3-carboxamide in the presence of an amine base in a suitable non-aromatic solvent;
- and
- (b) isolating the alkylcarbamic acid aryl ester KDS-4103.
1 more element
A crystalline form of the compound KDS-4103
- having D-spacings determined by x-ray powder diffraction, Cu-K alpha of
- D spacing
- 2-Theta
- (angstroms)
- 2.672
- 33.035
- 5.299
- 16.665
- 7.943
- 11.122
- 10.598
- 8.341
- 13.253
- 6.675
- 15.925
- 5.561
- 16.911
- 5.239
- 17.559
- 5.047
- 17.898
- 4.952
- 18.412
- 4.815
- 18.987
- 4.67
- 19.356
- 4.582
- 20.079
- 4.419
- 20.537
- 4.321
- 21.1
- 4.207
- 21.375
- 4.153
- 22.374
- 3.97
- 23.147
- 3.839
- 23.905
- 3.719
- 24.623
- 3.613
- 25.039
- 3.553
- 25.784
- 3.452
- 26.756
- 3.329
- 27.974
- 3.187
- 29.157
- 3.06
- 30.712
- 2.909
- 31.871
- 2.806
- 33.076
- 2.706
- 33.935
- 2.639
- 34.695
- 2.583.
61 more elements
Dependencies are inferred from the claim text.