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US 8,569,512 B2Granted
P2X3 receptor antagonists for treatment of pain
AssigneeMerck Sharp & Dohme Corp.
InventorsChristopher S. Burgey, Brendan M. Crowley, Zhengwu J. Deng, Daniel V. Paone, Craig M. Potteiger
Life of this patent
Estimating the term…
Abstract
The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
Claims11
A compound of structural formula III and VII:
- or pharmaceutically acceptable salts and individual enantiomers and diastereomers thereof wherein:
- R2 represents H, C1-6 alkyl, CF3, OH;
- R3 is selected from the group consisting of (CHRY)npyridyl, (CHRY)noxidopyridyl, (CHRY)npyrimidinyl, (CHRY)ntriazolyl, (CHRY)nphenyl, (CHRY)npyrazinyl, (CHRY)npyrazolyl, (CHRY)noxadiazolyl, (CHRY)nthiazolyl, (CHRY)nthiadiazolyl, (CHRY)nindazopyridyl, C1-6 alkyl, and (CHRY)nC3-6 cycloalkyl, wherein RY represents H, C1-6 alkyl optionally substituted with Ra, CF3, or OH
- or R2 and R3 can be combined with the nitrogen to which they are attached to form a C5-10 heterocyclyl optionally substituted with 1 to 3 groups of Ra;
- R6 represents hydrogen, OR2, (CH2)nCF3, halogen, C(R2)2OR2, C2-6 alkenyl, C2-6 alkynyl, (CH2)nC6-10 aryl, (CH2)nC5-10 heterocyclyl, said alkyl, cycloalkyl, aryl and heterocyclyl optionally substituted with 1 to 3 groups of Ra;
- R6a is R6;
- Ra represents C1-6 alkyl, halogen, hydroxyl, OR2 (CH2)nCF3, —O—, C3-6 cycloalkyl, NR2C(O)R2, C(O)N(R2)2, C(R2)2OR2, C(O)R2, O(CH2)nC(O)N(R2)2, O(CH2)nC(O)OR2, C(O)C5-10heterocyclyl, NO2, CN, N(R2)2, C(O)OR2, SO2R2, OR2, (CH2)nC5-10 heterocyclyl, or (CH2)nC6-10 aryl, said alkyl, heterocyclyl and aryl optionally substituted with 1 to 3 groups of C1-6 alkyl, halogen, hydroxyl, (CH2)nCF3, or CN;
- and
- n represents 0 to 4.
6 more elements
A compound represented by Tables 3 and 4 or pharmaceutically acceptable salts and individual enantiomers and diastereomers thereof.
Dependencies are inferred from the claim text.