Carboxamide heterocyclic CGRP receptor antagonists
US-8993588-B2 · Mar 31, 2015 · US
US9850246B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9850246-B2 |
| Application number | US-201514854760-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 15, 2015 |
| Priority date | May 9, 2012 |
| Publication date | Dec 26, 2017 |
| Grant date | Dec 26, 2017 |
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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.
Opening claim text (preview).
What is claimed is: 1. 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. 2. 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 according to claim 1 having a DSC extrapolated onset melting temperature of about 144° C. and a DSC peak melting temperature of about 175° C. 3. 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 according to claim 1 having d-spacings determined by x-ray powder diffraction, Cu K alpha, of about 12.7, 8.9, 8.1, 7.4, 6.4, 5.2, 4.9, 4.8 and 4.0 angstroms.
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals · CPC title
Spiro-condensed systems · CPC title
polycyclic · CPC title
Ortho-condensed systems · CPC title
Crystalline forms, e.g. polymorphs · CPC title
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