12-05-2016 дата публикации
Номер: US20160130273A1
The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine. 111-. (canceled)12. Crystalline (S)—N-((3S ,5S ,6R)-6-methyl-2-oxo-1-(2 ,2 ,2-trifluoroethyl)-5-(2 ,3 ,6-trifluorophenyl)piperidin-3-yl)-2′-oxo-1′ ,2′ ,5 ,7-tetrahydrospiro[cyclopenta[b]pyridine-6 ,3′-pyrrolo[2 ,3-b]pyridine]-3-carboxamide monohydrate.13. Crystalline (S)—N-((3S claim 12 ,5S claim 12 ,6R)-6-methyl-2-oxo-1-(2 claim 12 ,2 claim 12 ,2-trifluoroethyl)-5-(2 claim 12 ,3 claim 12 ,6-trifluorophenyl)piperidin-3-yl)-2′-oxo-1′ claim 12 ,2′ claim 12 ,5 claim 12 ,7-tetrahydrospiro[cyclopenta[b]pyridine-6 claim 12 ,3′-pyrrolo[2 claim 12 ,3-b]pyridine]-3-carboxamide monohydrate according to having a DSC extrapolated onset melting temperature of about 144° C. and a DSC peak melting temperature of about 175° C.14. Crystalline (S)—N-((3S claim 12 ,5S claim 12 ,6R)-6-methyl-2-oxo-1-(2 claim 12 ,2 claim 12 ,2-trifluoroethyl)-5-(2 claim 12 ,3 claim 12 ,6-trifluorophenyl)piperidin-3-yl)-2′-oxo-1′ claim 12 ,2′ claim 12 ,5 claim 12 ,7-tetrahydrospiro[cyclopenta[b]pyridine-6 claim 12 ,3′-pyrrolo[2 claim 12 ,3-b]pyridine]-3-carboxamide monohydrate according to having d-spacings determined by x-ray powder diffraction claim 12 , Cu K alpha claim 12 , of about 12.7 claim 12 , 8.9 claim 12 , 8.1 claim 12 , 7.4 claim 12 , 6.4 claim 12 , 5.2 claim 12 , 4.9 claim 12 , 4.8 and 4.0 angstroms.15. Crystalline (S)—N-((3S claim 12 ,5S claim 12 ,6R)-6-methyl-2-oxo-1-(2 claim 12 ,2 claim 12 ,2-trifluoroethyl)-5-(2 claim 12 ,3 claim 12 ,5-trifluorophenyl)piperidin-3-yl)-2′-oxo-1′ claim 12 ,2′ claim 12 ,5 claim 12 ,7-tetrahydrospiro[cyclopenta[b]pyridine-6 claim 12 ,3′-pyrrolo[2 claim 12 ,3-b]pyridine]-3-carboxamide. The official copy of the Sequence Listing is submitted concurrently with the specification as an ASCII formatted text file via EFS-Web, with a file name of “23236USPSP-SEQLIST-09MAY2012”, a ...
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