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US 2014/0005214 A1Published application
Piperidinone carboxamide spirohydantoin cgrp receptor antagonists
OwnerIan M. Bell, Mark E. Fraley +3inventors
InventorsIan M. Bell, Mark E. Fraley, Steven N. Gallicchio, Helen J. Mitchell, Cheng Wang
Life of this patent
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Abstract
The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Claims19
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is selected from the group consisting of:
- C1-4alkyl, cyclopropylmethyl, cyclobutylmethyl and [1-(trifluoromethyl)cyclopropyl]methyl, each of which is optionally substituted with one to four substituents as allowed by valence independently selected from the group consisting of hydroxyl and F;
- R2 is hydrogen or methyl;
- when R2 is hydrogen then
- R3 is selected from hydrogen, F or Cl;
- R4 is selected from hydrogen, F or Cl;
- R5 is hydrogen;
- R6 is selected from hydrogen or F;
- and
- R7 is selected from hydrogen, F or Cl;
- except that at least two of R3, R4, R6 and R7 must be F or Cl, unless R3 is F in which case R4, R6 and R7 may all be hydrogen;
- and if R4 is Cl then R7 cannot be Cl;
- when R2 is methyl then
- R3 is selected from hydrogen, methyl, F, Cl, or Br;
- R4 is selected from hydrogen, methyl, F or Cl;
- R5 is selected from hydrogen or F;
- R6 is selected from hydrogen or F;
- and
- R7 is selected from hydrogen, methyl, F or Cl;
- except that if R5 is F then at least three of R3, R4, R6 and R7 must be F;
- and if R4 is methyl or Cl then R7 cannot be methyl or Cl;
- and
- R8 is selected from the group consisting of:
- hydrogen, C1-4cyclopropylmethyl, and cyclobutylmethyl, each of which is optionally substituted with one to three fluoro substituents as allowed by valence.
22 more elements
-20. (canceled)
Dependencies are inferred from the claim text.