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Tetrahydroquinolines condensed with cycloalkyl as modulators of the CRTH2 receptor
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
PALANI, Anandan,HUANG, Xianhai,BRUBAKER, Jason,PETERSON, Scott,BUTCHER, John,CLOSE, Joshua,MARTINEZ, Michelle,MACCOSS, Rachel,JUNG, Joon,SILIPHAIVANH, Phieng,ZHANG, Hongjun,ASLANIAN, Robert,BIJU, Pura
申请号:
ES12799914
公开号:
ES2613644T3
申请日:
2012.06.14
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a pharmaceutically acceptable salt or ester thereof, wherein R1 is (i) H, (ii) C1-C4 alkyl, (iii) C2-C4 alkenyl, (iv) C3-C7 cycloalkyl, (v) - (C1-C3 alkylene) -R9 wherein R9 is C3-C7 cycloalkyl, phenyl or a 5- to 6-membered heteroaryl containing 1 to 2 heteroatoms selected from the group consisting of N, O and S, (vi) phenyl, (vii) -C (O) -R5, wherein R5 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl, (viii) or a group of the formula ** Formula ** in which v is 1, 2 or 3; R2 is (i) -QWV, where Q is -C (O) -, -C (O) O-, -C (O) N (H) -, -C (O) N (C1-C6 alkyl) -, -CH2- or -S (O) 2-; W is (a) C1-C8 alkylene, wherein said W alkylene is unsubstituted or substituted with 1 to 2 fluorine; (b) -CH>; = CH-, or (c) a phenylene of the formula ** Formula ** in which said phenylene is unsubstituted or substituted with 1 to 2 halos; V is (a) -CO2H, (b) tetrazolyl, or (c) a group of the formula ** Formula ** in which RV1 is selected from the group consisting of C1-C6 alkyl, C3-C6 cycloalkyl and phenyl ; (ii) -M-CO2H, in which M is ** Formula ** in which w is 0, 1, 2 or 3; XA is S or O; XB is N or C (H); with the proviso that when R1 is -C (O) -R5, then R2 is -CH2-W-V; Y is -C (O) -, -S (O) 2-, or a group of the formula ** Formula ** in which XA1 is S or O; and XB1 is N or C (H); Z is or is (i) absent, (ii) -alkylene (C1-C6) -, (iii) -O-, (iv) -O- (C1-C6 alkylene) -, wherein said -O- ( C1-C6 alkylene) - of Z is unsubstituted or substituted with 1 to 3 fluorine, (v) -N (H) -, or (vi) a group of the formula ** Formula ** in which r is 1, 2, 3 or 4; E is (i) phenyl, (ii) naphthyl, (iii) tetrahydronaphthyl, (iv) indanyl, (v) 5- or 10-membered mono or bicyclic heteroaryl containing from one to three heteroatoms selected from the group consisting of N, O and S, (vi) 5 to 10 membered mono or bicyclic heterocyclynyl containing from one to three heteroatoms selected from the group consisting of N, O and S, wherein said phenyl, naphthyl, tetrahydronaphth
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