LABADIE, SHARADA SHENVI,LIN, CLARA JEOU JEN,TALAMAS, FRANCISCO XAVIER,WEIKERT, ROBERT JAMES
申请号：
ES09710988
公开号：
ES2377280T3
申请日:
2009.02.05
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
A compound of the formula I (I) X2 A2 in which: A1 is phenylene or pyridinylene； A2 is phenyl or pyridinyl optionally substituted by 1-3 groups independently selected from the group consisting of halogen, C1-6 alkyl, C1-6 haloalkyl, cyano and C1-6 alkoxy； R1 is hydrogen, C1-10 alkyl, C3-7 cycloalkyl, C1-10 alkoxy or halogen； Y is NR2R3, C1-6 hydroxyalkyl, C1-6 acyl or heteroaryl chosen from the group consisting of pyrrolyl, pyrazolyl isoxazolyl, said heteroaryl is optionally substituted by one or two groups selected from C1-3 alkyl, C1-3 haloalkyl, C1 alkoxy -3, halogen or pyrrolidinyl, in which the nitrogen atom is optionally substituted by C1-6 acyl or C1-6 alkylsulfonyl； wherein (i) R2 is (a) hydrogen, (b) C1-10 alkyl, (c) C1-10 alkyl substituted one to four times by moieties independently selected from hydroxy, NR7bR8b, C1-3 alkoxy, halogen and cyano； (d) R11S (= O) m [C (R5) 2] 1-6 in which R11 is C1-6 alkyl or NR7cR8c； (e) (C1-3 alkyl) -S (= O) 2NH- [C (R5) 2] 1-6； (f) R7bR8bNC (= O) - [C (R5) 2] 1-6； (g) C3-6 cycloalkyl optionally substituted by -OH, C1-3 alkoxy or -NR7bR8b； (h) heterocyclyl； (i) heterocyclyl-C 1-6 alkyl； (j) heteroaryl-C 1-6 alkyl； (k) C 1-6 acyl optionally substituted by C 1-6 alkylsulfonyl； (1) (CH2) pCOX3 in which p is a number from one to six and X3 is hydroxy, C1-6 alkoxy or NR7cR8c； wherein said heterocyclyl moiety is oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, azetidinyl, pyrrolidinyl or piperidinyl, oxazolidin -2-on-4-yl and said heteroaryl moiety is pyridinyl or pyrimidinyl and said heterocyclyl or heteroaryl groups are optionally substituted by optionally substituted by -OH, C13 alkoxy, C1-3 alkyl or -NR7bR8b； R3 is hydrogen, C1-10 alkyl, S (= O) 2R6, S (= O) 2NR7aR8a, C1-6 acyl or C (= O) NR7aR8a； or (ii) R2 and R3 together are (CH2) 2X1 (CH2) 2, (CH2) 3-4S (= O) 2, (CH2) 2-3NR10S (= O) 2； R4 and R5 are independently hydrogen, C1-6 alkyl or C3-7 cycloalkyl； R 6 is C 1-6 alkyl or C 3-7 cycloalkyl； R7a and R8a are (i) independen
