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US 8,946,231 B2Granted
P2X3, receptor antagonists for treatment of pain
AssigneeMerck Sharp & Dohme Corp.
InventorsChristopher S. Burgey, 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.
Claims6
A compound represented by structural formula II:
- or pharmaceutically acceptable salts and individual enantiomers and diastereomers thereof wherein:
- A is CH or N;
- Rb is C1-6 alkyl, or halogen;
- R2 represents H, C1-6 alkyl, CF3, OH;
- R3 represents (CHR2)nC5-10 heterocycle,said heterocyclyl substituted with 1 to 3 groups of Ra , wherein R2 in (CHR2)nC5-10 heterocycle is C1-6 alkyl which is methyl and n in (CHR2)nC5-10 heterocycle is 1 ;
- R6 represents C1-6 alkyl, (CHR2)nC6-10 aryl, (CHR2)nC5-10 heterocyclyl, said alkyl, aryl and heterocyclyl optionally substituted with 1 to 3 groups of Ra ;
- Ra represents C1-6 alkyl, halogen, OR2, (CH2)nCF3 , —O—, C3-6 cycloalkyl, C(O)N(R2)2, C(O)R2, CN, N(R2)2, C(O)OR2, SO2R2,(CHR2)nC5-10 heterocyclyl, or (CHR2)nC6-10 aryl, said 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 which is represented in Table 1:
- TABLE 1
- Example
- R3
- R7
- R6
- 1.1
- 1.2
- 1.3
- 1.4
- 1.5
- 1.6
- 1.7
- 1.8
- 1.9
- 1.10
- 1.11
- 1.12
- 1.13
- 1.14
- 1.15
- 1.16
- 1.17
- 1.18
- 1.19
- 1.20
- 1.21
- 1.22
- 1.23
- 1.24
- 1.25
- 1.26
- 1.27
- 1.28
- 1.29
- 1.30
- 1.31
- 1.32
- 1.33
- 1.34
- 1.35
- 1.36
- 1.37
- 1.38
- 1.39
- 1.40
- 1.41
- 1.42
- H
- 1.43
- 1.44
- 1.45
- 1.46
- 1.47
- 1.48
- 1.49
- 1.50
- 1.51
- 1.52
- 1.53
- 1.54
- 1.55
- 1.56
- 1.57
- 1.58
- 1.59
- 1.60
- 1.61
- 1.62
- 1.63
- 1.64
- 1.65
- 1.66
- 1.67
- 1.68
- 1.69
- 1.70
- 1.71
- 1.72
- 1.73
- 1.74
- 1.75
- 1.76
- 1.77
- 1.78
- 1.79
- 1.80
- 1.81
- 1.82
- 1.83
- 1.84
- 1.85
- 1.86
- 1.87
- 1.88
- 1.89
- 1.90
- 1.91
- 1.92
- 1.93
- 1.94
- 1.95
- 1.96
- 1.97
- 1.98
- 1.99
- 1.100
- 1.101
- 1.102
- 1.103
- 1.104
- 1.105
- 1.106
- 1.107
- 1.108
- 1.109
- 1.110
- 1.111
- 1.112
- 1.113
- 1.114
- 1.115
- 1.116
- 1.117
- 1.118
- 1.119
- 1.120
- 1.121
- 1.122
- 1.123
- 1.124
- 1.125
- 1.126
- 1.127
- 1.128
- 1.129
- 1.130
- 1.131
- 1.132
- 1.133
- 1.134
- 1.135
- 1.136
- 1.137
- 1.138
- 1.139
- 1.140
- 1.141
- 1.142
- 1.143
- 1.144
- 1.145
- 1.146
- 1.147
- 1.148
- 1.149
- 1.150
- or pharmaceutically acceptable salts and individual enantiomers and diastereomers thereof
154 more elements
Dependencies are inferred from the claim text.