Crystalline form of a quinolinone-carboxamide compound

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S126000

Reexamination Certificate

active

07728004

ABSTRACT:
The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4receptor activity, and processes useful for preparing such crystalline salt forms.

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Kirk-Othmer Encyclopedia of Chemical technology p. 95-147 (2002).
Suzuki et al., “Synthesis and Evaluation of Novel 2-Oxo-1,2-dihydro-3-quinolinecarboxamide Derivatives as Potent and Selective Serotonin 5-HT4Receptor Agonists”, Chem. Pharm. Bull., 49(1), pp. 29-39 (2001).
Suzuki et al., “A Practical Procedure for Preparation ofN-(endo-8-3-hydroxy)propyl-8-azabicyclo[3.2.1]oct-3-yl)-1-isopropyl-2-oxo-1,2-dihydro-3-quinoline-carboxamide (TS-951)”, Heterocycles, vol. 53, No. 11, pp. 2471-2485 (2000).

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