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Tricyclic compounds to inhibit the CFTR channel
专利权人:
Novartis AG
发明人:
AHMED, Mahbub,ASHALL-KELLY, Alexander,GUERITZ, Louisa,MCKENNA, Jeffrey,MCKENNA, Joseph,MUTTON, Simon,PARMAR, Rakesh,SHEPHERD, Jon,WRIGHT, Paul
申请号:
ES13826625
公开号:
ES2628369T3
申请日:
2013.12.17
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of the formula (I) or a pharmaceutically acceptable salt thereof: ** Formula ** in which R1 represents phenyl, cycloalkenyl (C4-C7) or Het1, whose group R1 may be unsubstituted or substituted in one or two carbon atoms by the substituents Ra and may also be substituted on a nitrogen atom with a substituent Ra1; each Ra independently represents (C1-C4) alkyl, halo, halo (C1-C4) alkyl, cyano, hydroxyalkyl (C1-C4), alkoxy (C1-C4), haloalkoxy (C1-C4), alkoxy (C1-C4) alkyl (C1-C4), R6OC (O) -, or R6OC (O) (C1-C4) alkyl -; Ra1 represents (C1-C4) alkyl, hydroxy (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkylamino (C1-C4) alkyl, di [(C1-C4) alkyl ] amino (C1-C4) alkyl-, aryl (C1-C4) alkyl or R6OC (O) (C1-C4) alkyl; R2 represents (C1-C6) alkyl, (C3-C7) cycloalkyl, (C4-C7) cycloalkenyl, phenyl, furanyl, thiazolyl or thienyl, R2 which may be unsubstituted or substituted on one to three carbon atoms with Rb substituents; each Rb independently represents (C1-C4) alkyl, halo, halo (C1-C4) alkyl, cyano, (C1-C4) alkylamino (C1-C4) alkyl, di [(C1-C4) alkyl] (C1-C4) aminoalkyl -, (R6) 2NC (O) (C1-C4) alkyl or R6OC (O) (C1-C4) alkyl; X represents S, Z represents CHR4a and n represents 1; or X represents CHR4b, Z represents NR5 and n represents 1 or 2; or X represents CHR4b, Z represents CHR4a and n represents 0, 1 or 2; or X represents C (>; = CH2), CF2 or C (CH3) 2, Z represents CHR4a and n represents 0 or 1; each R3 independently represents methyl or ethyl; when X represents S, R4 represents hydrogen, (C1-C4) alkyl, halo (C1-C4) alkyl, hydroxy (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) aminoalkyl, (C1-C4) alkylamino (C1-C4) alkyl, di [(C1-C4) alkyl] amino (C1-C4) alkyl -, phenyl, Het1alkyl (C1-C4), Het2alkyl (C1-C4), alkyl (C1 -C4) S (O) 2N (C1-C4) alkyl -, or R7C (O) NH (C1-C4) alkyl -; when X represents CHR4b, each R4 independently represents hydrogen, hydroxy, (C1-C4) alkyl, (C1-C4) alkoxy, halo (C1-C4) alkyl, hydroxy (C1-C4) alkyl, (C1-C4) alkox
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