Claims for Patent: 9,499,545
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Summary for Patent: 9,499,545
| Title: | Piperidinone carboxamide azaindane CGRP receptor antagonists |
| Abstract: | The present invention is directed to piperidinone carboxamide azaindane 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. |
| Inventor(s): | Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman |
| Assignee: | Merck Sharp and Dohme LLC |
| Application Number: | US14/485,259 |
| Patent Litigation and PTAB cases: | See patent lawsuits and PTAB cases for patent 9,499,545 |
| Patent Claims: |
1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein: X is —C(R8)═, wherein R8 is hydrogen, F or CN; 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 or more substituents as allowed by valence independently selected from the group consisting of: F and hydroxy; R2 is selected from hydrogen and methyl; and wherein: 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 with the proviso that 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 with the proviso that if R4 is methyl or Cl then R7 cannot be methyl or Cl. 2. A pharmaceutical composition which comprises an inert carrier and the compound of claim 1, or a pharmaceutically acceptable salt thereof. 3. A method of treating migraine in a mammalian patient in need of such treatment, which comprises administering to the patient a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof. |
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