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US 2013/0096130 A1Published application
CGRP Receptor Antagonists
AssigneeBristol-Myers Squibb Company
InventorsGuanglin Luo, Gene M. Dubowchik, John E. Macor, Ling Chen
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Abstract
The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD).
Claims15
A compound of Formula I
- such that ring A is selected from the group consisting of
- and wherein
- R1a is hydrogen, cyano, halo, alkyl, haloalkyl, alkoxy, amino, alkylamino, dialkylamino, azetidinyl, pyrrolidinyl, or piperidinyl;
- R1b is hydrogen, alkyl, or haloalkyl;
- R2 is piperidinyl substituted with 1 substituent selected from the group consisting of
- or R2 is
- R3 is hydrogen, halo, cyano, alkyl, haloalkyl, alkoxy, or haloalkoxy;
- R4 is hydrogen, halo, cyano, alkyl, haloalkyl, alkoxy, or haloalkoxy;
- R5 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, or dialkylamino;
- R6 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, or dialkylamino;
- R7 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, or dialkylamino;
- R8 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, or dialkylamino;
- R9 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, or dialkylamino;
- R10 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, dialkylamino, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, alkoxycarbonylamino, or benzyloxycarbonylamino;
- R11 is hydrogen, hydroxy, alkoxy, haloalkoxy, azido, amino, alkylamino, dialkylamino, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, alkoxycarbonylamino, or benzyloxycarbonylamino;
- or R10 and R11 taken together is O or N—OH;
- provided that at least one of R3, R6, R7, R8, R9, R10, or R11 is not hydrogen;
- Ar1 is phenyl substituted with 0-3 substituents selected from the group consisting of cyano, halo, alkyl, haloalkyl, alkoxy, haloalkoxy, and alkylSO2;
- X is O, CH2, or NH;
- and
- Y is a bond, O, CH2, or NH;
- or a pharmaceutically acceptable salt thereof.
19 more elements
Dependencies are inferred from the claim text.