Process for making CGRP receptor antagonists

US9850246B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9850246-B2
Application numberUS-201514854760-A
CountryUS
Kind codeB2
Filing dateSep 15, 2015
Priority dateMay 9, 2012
Publication dateDec 26, 2017
Grant dateDec 26, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

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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.

First claim

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.

Assignees

Inventors

Classifications

  • Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals · CPC title

  • C07D471/20Primary

    Spiro-condensed systems · CPC title

  • polycyclic · CPC title

  • Ortho-condensed systems · CPC title

  • Crystalline forms, e.g. polymorphs · CPC title

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What does patent US9850246B2 cover?
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.
Who is the assignee on this patent?
Merck Sharp & Dohme
What technology area does this patent fall under?
Primary CPC classification C07D471/20. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Dec 26 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).