N- (hetero) aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo [2,3-d] pyrimidines and pyrrol-3-yl-pyrrolo [2,3-d] pyrimidines as Janus kinase inhibitors

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专利权人:

INCYTE CORPORATION

发明人:

RODGERS, JAMES D.,SHEPARD, STACEY,ARVANITIS, ARGYRIOS G.,WANG, HAISHENG,STORACE, LOUIS,FOLMER, BEVERLY,SHAO, LIXIN,ZHU, WENYU,GLENN, JOSEPH P.

申请号：

ES10720113

公开号：

ES2487542T3

申请日:

2010.05.21

申请国别(地区):

ES

年份:

2014

代理人:

摘要：

A compound of formula I: or a pharmaceutically acceptable salt or N-oxide thereof； in which: X is cyano or halogen； Y is CH or N； Z is hydrogen, C1-4 alkyl, fluorinated C1-4 alkyl or fluorine； Ar is C6-14 aryl, C1-14 heteroaryl, C7-14 cycloalkyl-fused aryl, heterocycloalkyl C6-14-aryl condensed, cycloalkyl C2-14-heteroaryl fused or heterocycloalkyl C2-14-fused heteroaryl, each of which is optionally substituted with 1, 2, 3, 4, 5 or 6 independently selected R1 groups； each R1 is independently selected from halogen, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C3-14 cycloalkyl-C1-4 alkyl, C2- heterocycloalkyl 14, C2-14 heterocycloalkyl-C1-4 alkyl, C6-14 aryl, C6-14 aryl-C1-4 alkyl, C1-13 heteroaryl, C1-13 heteroaryl-C1-4 alkyl, -ORa, -SR3, -S (>； = O) Rb, -S (>； = O) 2Rb, -S (>； = O) NReRf, -C (>； = O) Rb, -C (>； = O) ORb, -C (>； = O) NReRf, -OC (>； = O) Rb, - OC (>； = O) NReRf, -NReRf, -NRcC (>； = O) Rd, -NRcC (>； = O) ORd, -NRcS (>； = O) 2Rd and -NRbS (>； = O) 2NReRf； wherein said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl and C2-6 alkynyl are each optionally substituted with independently selected 1, 2, 3 or 4 R1 to 30 groups； and wherein said C3-14 cycloalkyl, C3-14 cycloalkyl-C1-4 alkyl, C2-14 heterocycloalkyl, C2-14 heterocycloalkyl-C1-4 alkyl, C6-14 aryl, C6-14 aryl-C1-4 alkyl, C1-13 heteroaryl and C1-13 heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3 or 4 independently selected R2a groups； Each R1a is independently selected from halogen, cyano, nitro, hydroxyl, C1-4 alkoxy, C1-4 haloalkoxy, C1-4 alkylthio, C1-4 alkyl sulfinyl, C1-4 alkyl sulfonyl, amino, C1- alkyl 4-amino, di-C 1-4 alkyl-amino, C 1-4 alkylcarbonyl, carboxy, C 1-4 alkoxycarbonyl, C 1-4 alkylcarbonylamino, C 1-4 alkylcarbonylamino, C 1-4 alkoxy carbonylamino, C 1-4 alkoxycarbonyl- (C 1-4 alkyl) amino, carbamyl, C 1-4 alkylcarbamyl and diC 1-4 alkylcarbamyl； each R2a is independently selected from halogen, cyano,

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