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Bicyclic heterocycle derivatives for the treatment of pulmonary arterial hypertension
专利权人:
Novartis AG
发明人:
BRUCE, Ian,CHAMOIN, Sylvie,COLLINGWOOD, Stephen Paul,FURET, Pascal,FURMINGER, Vikki,LEWIS, Sarah,LOREN, Jon Christopher,MOLTENI, Valentina,SAUNDERS, Alex Michael,SHAW, Duncan,SVIRIDENKO, Lilya,THOMSON
申请号:
ES12772493
公开号:
ES2585048T3
申请日:
2012.08.31
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound represented by the formula (I) ** Formula ** or a pharmaceutically acceptable salt thereof, wherein, A is ** Formula ** R1 is C1-C4 alkyl; C1-C4 alkoxy optionally substituted by one or more halogen atoms; CN; or halogen; R1a is H, halogen, C1-C4 alkyl or C1-C4 haloalkyl; X is N or CH; R2 is H; C1-C8 alkyl optionally substituted by one or more OH, -NR9R11 or C1-C4 alkoxy; C1-C8 haloalkyl; C2-C8 alkynyl substituted by one or more halogen, OH, - NR9R11 or C1-C4 alkoxy; C3-C10 cycloalkyl; - (C1-C4 alkyl) -C3-C8 cycloalkyl; C1-C8 alkoxy optionally substituted by one or more halogen, -NR9R11 or OH; OH; CN; halogen; - (C0-C4 alkyl) -NR9R11; - (C0-C4 alkyl) -CO2R15; - (C0-C4 alkyl) -C (O) NR9R11; - (C0-C4 alkyl) -C6-C14 aryl; or - (C0-C4 alkyl) - 3- to 14-membered heterocyclyl; wherein the cycloalkyl, - (C0-C4 alkyl) -C6-C14 alkyl and - (C0-C4 alkyl) -heterocyclyl of 3 to 14 members are each optionally substituted by one or more Za substituents; R3 is H; C1-C8 alkyl optionally substituted by one or more OH, -NR9R11 or C1-C4 alkoxy; C1-C8 haloalkyl; C2-C8 alkynyl substituted by one or more halogen, OH, - NR9R11, or C1-C4 alkoxy; C3-C10 cycloalkyl; - (C1-C4 alkyl) -C3-C8 cycloalkyl; C1-C8 alkoxy optionally substituted by one or more halogen, -NR9R11 or OH; OH; CN; halogen; - (C0-C4 alkyl) -NR9R11; - (C0-C4 alkyl) -CO2R15; - (C0-C4 alkyl) -C (O) NR9R11; - (C0-C4 alkyl) -C6-C14 aryl; or - (C0-C4 alkyl) - 3- to 14-membered heterocyclyl; wherein the cycloalkyl, - (C0-C4 alkyl) -C6-C14 alkyl and - (C0-C4 alkyl) -heterocyclyl of 3 to 14 members are each optionally substituted by one or more Za substituents; each Za is independently OH; (C0-C4 alkyl) -C6 aryl; C6 O-aryl; C1-C4 alkyl optionally substituted by one or more OH, CN or -NR19aR21a; C1-C4 haloalkyl; C1-C4 alkoxy optionally substituted by one or more OH, -CO2R19a, - NR19aR21a or C1-C4 alkoxy; -NR18aC (O) R21a; -C (O) NR19aR21a; -NR18aC (O) NR19aR21a; -NR19aR21a; - (C0-C4 alkyl) -C (O) OR18a; - (C0-C4 alkyl) -C (O)
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