THERAVANCE BIOPHARMA R&D IP LLC; LLC;Theravance Biopharma R&D IP
发明人:
FLEURY, Melissa,GENDRON, Roland,HUGHES, Adam D.,FLEURY MELISSA,FLEURY, MELISSA,GENDRON ROLAND,GENDRON, ROLAND,HUGHES ADAM D,HUGHES, ADAM D.
申请号：
ES12708194
公开号：
ES2582640T3
申请日:
2012.02.16
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound of the formula I: ** Formula ** where: R1 is selected from -OR7 and -NR8R9； R2a is selected from -CH2OH, -10 CH2OP (O) (OH) 2 and -CH2OC (O) CH (R37) NH2； or R2a is taken together with R7 to form -CH2O-CR18R19-； R2b is selected from H and -CH3； Z is selected from -CH- and -N-； X is a C1-9 heteroaryl； R3 is absent or is selected from H； halo； -C0-5-OH alkylene； -NH2； -C 1-6 alkyl； -CF3； -C3-7 cycloalkyl； -C0-2-O-C 1-6 alkyl； -C (O) R20； -C0-1-COOR21 alkylene； -C (O) NR22R23； -NHC (O) R24； >； = O； -NO2； -C (CH3)>； = N (OH)； phenyl optionally substituted with one or two groups independently selected from halo, -OH, -CF3, -OCH3, -NHC (O) CH3 and phenyl； naphthalenyl； pyridinyl； pyrazinyl； pyrazolyl optionally substituted with methyl； thiophenyl optionally substituted with methyl or halo； furanyl； and -CH2-morpholinyl； and R3, when present, is attached to a carbon atom； R4 is absent or is selected from H； -OH； -C 1-6 alkyl； -C1-2-COOR35 alkylene； -CH2OC (O) CH (R36) NH2； -OCH2OC (O) CH (R36) NH2； -OCH2OC (O) CH3； -CH2O P (O) (OH) 2； -CH2CH (OH) CH2OH； -CH [CH (CH3) 2] -NHC (O) C1-6alkyl； pyridinyl； and phenyl or benzyl optionally substituted with one or more groups selected from halo, -COOR35, -OCH3, -OCF3 and -SCF3； and R4, when present, is attached to a carbon or nitrogen atom； or R3 and R4 are taken together to form -phenylene-O- (CH2) 1-3- or -phenylene-O-CH2-CHOH-CH2-； a is 0 or 1； R5 is selected from halo, -CH3, -CF3 and -CN； b is 0 or an integer from 1 to 3； each R6 is independently selected from halo, -OH, -CH3, -OCH3 and -CF3； R7 is selected from H, -C1-8 alkyl, -C3-10 alkylene-C6-10 aryl, -C3-3-alkylene-C1-9 heteroaryl, -C3-7 cycloalkyl, - [(CH2) 2O] 1- 3CH3, -C1-6-OC alkylene (O) R10, -C1-6 alkylene-NR12R13, -C1-6-C alkylene (O) R31, -C0-6-morpholinyl alkylene, -C 1-6-SO2 alkylene C 1-6 alkyl； ** Formula ** R 10 is selected from -C 1-6 alkyl, -O-C 1-6 alkyl, -C 3-7 cycloalkyl, -O-C 3-7 cycloalkyl, phenyl, -O-phenyl, -NR12R13, -CH [CH (CH3) 2] -N
