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Thioether triazolopyrimidine and triazolopyridine myeloperoxidase inhibitors
专利权人:
Bristol-Myers Squibb Company
发明人:
VIET, Andrew Quoc,WURTZ, Nicholas R.
申请号:
ES15767392
公开号:
ES2688194T3
申请日:
2015.09.09
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
The compound according to formula (I) ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph or a solvate thereof, wherein:, ring A is independently phenyl substituted with 0- 1 R2 and 0-4 R3, or (a 5- to 6-membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from N, NRa, O and S (O) p, wherein said heterocycle is substituted with 0 -1 R2 and 0-3 R3); X is independently CH or N; And it is independently selected from: a hydrocarbon linker substituted with 0-1 R1, or a hydrocarbon-heteroatom linker substituted with 0-1 R1; wherein said hydrocarbon linker has one to six carbon atoms and can be linear or branched; and said hydrocarbon-heteroatom linker has one to four carbon atoms and a group selected from O, S, NH, N (C1-4 alkyl), CONH and NHCO; R1 is independently selected from: CN, OH, - (C1-4 alkyl substituted with 0-1 R18), C1-4 haloalkyl, Ph, Bn, COPh, CH (OH) Ph, CO2 (C1-4 alkyl) and CONHBn ; R2 is independently selected from: -CH (NH2) CF3, - (CH2) tOH, -O (CH2) 2-3N (C1-4 alkyl) 2, - (CH2) nR4 and - (CH2) n (X1) n (CH2) nR5; X1 is independently selected from: C (Me) 2, O, S, CO and SO2; R3 is, in each case, independently selected from: halogen, CN, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, C1-4 haloalkoxy, NO2, CONH2 and SO2 (C1-4 alkyl); alternatively, R2 and R3, together with the carbon atoms to which they are attached, combine to form a 5- to 6-membered heterocyclic or carbocyclic ring comprising carbon atoms and 0-3 heteroatoms selected from N, NRa, O and S (O) p; wherein said heterocycle is substituted with 0-2 R19; R4 is independently selected from: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, C1-4 haloalkoxy, haloalkylthio, CN, CO2 (C1-4 alkyl), NO2, NR6R7, CONR6R7 , COR10, -CONH (CH2) 1-2NR9R1030, SO2NR9R10 and S (O) pR8; R5 is independently selected from: C3-10 carbocycle substituted with 0-2 R11, phenyl substituted with 0-3 R11 and 0-1 R12, and 5-10 membered heterocycle comp
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