DEWDNEY, NOLAN JAMES,GABRIEL, TOBIAS,KONDRU, RAMA K.,LOU, YAN,SOTH, MICHAEL
申请号：
ES11184324
公开号：
ES2444144T3
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, in which: ** Formula ** in which X1 is CH or N； R1 is C (>； = O) NHR6, where R6 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C1-6 heteroalkyl, C3-6 cycloalkyl, pyridinyl-C1-3 alkyl, phenyl-C1-3 alkyl , said phenyl is optionally substituted by C1-6 alkyl, C1-6 alkoxy, C1-6 heteroalkoxy, halogen, CONRaRb or CO2Rg； Ra and Rb (i) are independently selected from 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 the number 2 or 3 and X2 is O, S (O) not NR8 and n is a number from zero to two and R8 is hydrogen, C1- alkyl 6, C1-6 hydroxyalkyl or C1-3 acyl； or (iii) together with the nitrogen atom to which they are attached are piperidinyl opirrolidinyl, said piperidinyl or pyrrolidinyl are optionally substituted by hydroxy, C1-3 alkoxy, C1-3 hydroxyalkyl； Rg is hydrogen or C1-6 alkyl； 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-tetrahydro-benzo [b] thiophene-2-yl, thiophenyl , 1 ', 2', 3 ', 4', 5 ', 6'-hexahydro- [2,4'] bipyridin-5-yl and (C1-3 alkyl) -indolyl optionally substituted by one or two C1-6 alkyl or halogen； (iii) azetidin-1-yl, pyrrolidin-2-yl, piperidin-1-yl, azepan-1-yl or 2,3-dihydro-1H-isoindolin-2-yl, or 6,7-dihydro-5H-pyrrolo [ 3,4-b] pyridine； (iv) NRcRd, in which Rc and Rd together are (CH2) or X2 (CH2) p, in which oyp are independently the number 1 or 2, and X2 has the meaning defined above, or Rc and Rd independently are hydrogen , C1-10 alkyl or C1-10 hydroxyalkyl.Un compuesto de la fórmula I, en la que:**Fórmula** en la que X1 es CH o N； R1 es C(>；=O)NHR6, en donde R6 es hidrógeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, cicloalquilo C3-6, piridinil-alquilo C1-3, fenilo ofenil-alquilo C1-3,
