DEWDNEY, NOLAN JAMES,GABRIEL, TOBIAS,KONDRU, RAMA K.,LOU, YAN,SOTH, MICHAEL
申请号：
ES08805263
公开号：
ES2499017T3
申请日:
2008.10.14
申请国别(地区):
ES
年份:
2014
代理人:
摘要：
A compound of the formula I: ** Formula ** in which X1 is N； R1 is C (>； = O) NHR6, phenyl or heteroaryl, said heteroaryl is selected from the group consisting of pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl； pyrrolyl, furanyl, thiophenyl, imidazolyl, pyrazolyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, 2- (C1-6 alkyl) -pyridazin-3-on-6-yl, 2-benzyl-pyridazin-3-on-6-yl , 1,4,5,6-tetrahydro-pyrimidin-2-yl and 4,5-dihydro-1H-imidazol-2-yl； said phenyl and heteroaryl are optionally substituted independently from one to three times by moieties selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 heteroalkyl, C1-6 heteroalkoxy, C1-6 alkylsulfanyl, alkylsulfonyl C1-6, C1-6 heteroalkylsulfonyl and C1-6 heterocyclyl-alkoxy, said heterocyclyl is azetidinyl, pyrrolidinyl or piperidinyl, CONRaRb, CO2Rg, SO2NRaRb, NRaRb, NHSO2R7 or NHCOR7； wherein R 6 is hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 heteroalkyl, C 3-6 cycloalkyl, pyridinyl C 1-3 alkyl, phenyl or phenyl C 1-3 alkyl being said phenyl optionally substituted with C 1-6 alkyl 6, C1-6 alkoxy, C1-6 heteroalkoxy, halogen, CONRaRb or CO2R8； Ra and Rb (i) independently selected are hydrogen, C1-6 alkyl, C1-6 heteroalkyl, C1-3 alkoxy-C1-3 alkyl, carboxy-C1-3 alkyl, C3-6 cycloalkyl or heterocyclyl； (ii) together they are (CH2) mX2 (CH2) 2 where m is 2 or 3 and X2 is O, S (O) not NR8 and has a value of zero to two, and R8 is hydrogen, C1-6 alkyl, C1-6 hydroxyalkyl, or C1-3 acyl ,； or (iii) together with the nitrogen to which they are attached are piperidinyl or pyrrolidinyl, said piperidinyl or pyrrolidinyl are optionally substituted by hydroxy, C1-3 alkoxy, hydroxy C1-3 alkyl； Rg is hydrogen or C1-6 alkyl； R7 is C1-6 alkyl or C1-6 heteroalkyl； R2 is hydrogen or C1-6 alkyl； R3 and R4 are independently hydrogen, halogen, amino, C1-6 hydroxyalkyl, C1-6 alkyl or cyclopropyl； R5 is (i) phenyl, (ii) heteroaryl selected from the group consisting of pyridinyl, benzo [b] thiophene-2-yl, 4,5,6,7-tetr
