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Pyridine and pyrazine derivative for the treatment of cystic fibrosis (CF)
专利权人:
NOVARTIS AG
发明人:
BAETTIG, URS,BALA, KAMLESH JAGDIS,BUDD, EMMA,EDWARDS, LEE,HOWSHAM, CATHERINE,HUGHES, GLYN,LEGRAND, DARREN MARK,SPIEGEL, KATRIN
申请号:
ES11708490
公开号:
ES2552503T3
申请日:
2011.03.17
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of the formula I: ** Formula ** or pharmaceutically acceptable salts thereof, wherein: A is N or CR4a; R1 is H; alkyl of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; alkenyl of 2 to 8 carbon atoms; alkynyl of 2 to 8 carbon atoms; cycloalkyl of 3 to 10 carbon atoms; cycloalkenyl of 5 to 10 carbon atoms; -alkyl of 1 to 4 carbon atoms -cycloalkyl of 3 to 8 carbon atoms; alkoxy of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; halogen; SO2NR8R9; SO2R10; S-alkyl of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; S-aryl of 6 to 14 carbon atoms; CN; NR11R12; C (O) NR13R14; NR13SO2R15; NR13C (O) R15, CO2R15, - (alkyl of 0 to 4 carbon atoms) -aryl of 6 to 14 carbon atoms; or - (alkyl of 0 to 4 carbon atoms) - heterocyclic group of 3 to 14 members, wherein the heterocyclic group contains at least one heteroatom selected from N, O and S; wherein the cycloalkyl, cycloalkenyl, aryl, and heterocyclyl groups are each optionally substituted with one or more Z substituents; R2 is halo-alkyl of 1 to 4 carbon atoms; R3 and R4a are each independently H or alkyl of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; R4 is H, or alkyl of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; R5 is - (CH2) m-NR17R18, - (CH2) m-OR '; alkoxy of 1 to 8 carbon atoms optionally substituted with one or more halogen atoms; - (alkyl of 0 to 4 carbon atoms) -CO2R15; - (alkyl of 0 to 4 carbon atoms) -aryl of 6 to 14 carbon atoms or - heterocyclic group of 3 to 14 members, wherein the heterocyclic group contains at least one heteroatom selected from N, O and S; wherein the - (alkyl of 0 to 4 carbon atoms) - aryl of 6 to 14 carbon atoms, and - (alkyl of 0 to 4 carbon atoms) - heterocyclic group of 3 to 14 members, are each optionally substituted with one or more substituents Z; R6 is alkyl of 1 to 8 carbon atoms optionally substituted with one or more halogen atom
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