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Tetrahidroquinolinas Condensed with cycloalkyl crth receptor modulators
专利权人:
MERCK SHARP & DOHME CORP.
发明人:
申请号:
ARP120102111
公开号:
AR086931A1
申请日:
2012.06.14
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Pharmaceutical compositions comprising such compounds and Methods of using the compounds for the treatment of diseases or conditions associated with the uncontrolled or inappropriate Stimulation of the role of CRTH2.Claim 1: a compound of the formula (1) or a pharmaceutically acceptable Salt or Ester thereof, wherein R1 is H (i), (ii) c1-4 alkyl, (iii) alquenilo c2-4, cycloalkyl C3 - 7 (iv), (V) - 3 - (alquileno C1 R9) - that is, the R9 cycloalkyl C3 - 7, phenyl or heteroaryl 5 to 6 Member 1 to 2 s containing hetero Atoms selected from the group consisting of N, o and S, (VI), phenyl(vii) - C (o) - R5, which is 6 R5 C1 - C3 alkyl, cycloalkyl, phenyl - 6 (viii) or a group of the formula (2), in which V is 1, 2 or 3; R2 is (i) - Q - W - V in which q is - C (o) -, - C (o) o -, - C (o) n (H) -, - C (o) n (C1 - 6 alkyl) -, - CH2 -, or - S (o) 2 - (W) is alquileno; C1 - 8, in which W is said alquileno Without a substitute or substituted with 1 to 2 Fluorine; (b) - ch = CH -, or (c) a phenylene of formula (3),In which the phenylene is no substitute or substituted with 1 to 2 Halo; V is CO2H - (a), (b) or (c) tetrazolilo, a group of the formula (4), in which RV1 is selected from the group consisting of C1 - C3 alkyl and cycloalkyl - 6 6 phenyl; (II) - M - CO2H, in which M is selected from the group of F u00f3rmulas (5), in which W is 0, 1,2 or 3; Xa is s u o; XB is n or C (H); under the condition that when R1 is - C (o) - R2 R5, then is - CH2 - W - V, and - C (o) -, - S (OR) 2 - or group of the formula (6), in the XA1 is s u o; and XB1 is n or C (H); Z is absent (i), (ii) - alquileno C1 - 6 -, - O -, (iii) (iv) - or - (alquileno C1 - - 6) in the di (alquileno Cho - or - C1 - 6) - Z is no substitute or substituted with 1 to 3 Fluorine, (V) - N (H) -,(VI) or a group of the formula (7), in which R is 1, 2, 3 or 4; and (i), (ii) phenyl, naphthyl, (iii) tetrahidronaftilo indanilo, (iv), (V) mono - or bicyclic heteroaryl containing 5 to 10 members of one to three heteroatoms sel
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