Cyanomethylpyrazole carboxamides as Janus kinase inhibitors

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专利权人:

MERCK SHARP & DOHME CORP.

发明人:

BRUBAKER, Jason,CHILDERS, Matthew Lloyd,CHRISTOPHER, Matthew,CLOSE, Joshua,KATZ, Jason David,JUNG, Joon,PETERSON, Scott,SILIPHAIVANH, Phieng,SIU, Tony,SMITH, Graham Frank,TORRES, Luis,WOO, Hyun Chong

申请号：

ES12834379

公开号：

ES2670878T3

申请日:

2012.09.21

申请国别(地区):

ES

年份:

2018

代理人:

摘要：

A compound of formula I or a pharmaceutically acceptable salt or a stereoisomer thereof: ** Formula ** each of Ra and R4 is independently selected from hydrogen and C1-4 alkyl； A is selected from aryl and heteroaryl； n is independently 0, 1, 2, 3 or 4； p is 2 or 3； X is independently selected from C, N, O and S； each of R3 and R7 is independently selected from hydrogen, halogen, C1-10 alkyl, C2-10 alkenyl, C1-10 heteroalkyl, C0-10 arylalkylC0-10 alkyl, C3-8 cycloalkylC0-10 alkyl, heteroarylC0- alkyl 10, heterocycloalkyl (C3-8) C0-10 alkyl, and wherein each of R3 and R7 are independently substituted with 0, 1, 2, 3 or 4 substituents R5a； R5a is selected from: halogen, C1-10 alkyl (oxy) 0-1 (carbonyl) 0-1 C0-10 alkyl, C1-10 heteroalkyl 0-1 (carbonyl) 0-1 C0-10 alkyl, C2 alkenyl 10 (oxy) 0-1 (carbonyl) 0-1 C0-10 alkyl, C0-10 aryl (oxy) 0-1 (carbonyl) 0-1 C0-10 alkyl, C2-10 alkenyl (oxy) 0-1 ( carbonyl) 0-1 C0-10 alkyl, C2-10 aryl alkyl (oxy) 0-1 (carbonyl) 0-1 C0-10 alkyl, C3-8 cycloalkyl C0-10 alkyl (oxy) 0-1 (carbonyl) 0-1 alkyl C0-10, heteroarylalkyl C0-10 (oxy) 0-1 (carbonyl) 0-1alkyl C0-10, heterocycloalkyl (C3-8) alkyl C0-10 (oxy) 0-1 (carbonyl) 0-1alkyl C0-10, C1-10 alkyl (carbonyl) 0-1oxyC0-10 alkyl, C1-10 heteroalkyl (carbonyl) 0-1oxyC0-10 alkyl, C2-10 alkenyl (carbonyl) 0-1oxyC0-10 alkyl, C1-10 heteroalkyl (carbonyl ) 0-1oxy C0-10 alkyl, aryl C0-10 alkyl (carbonyl) 0-1oxy alkyl C0-10, cycloalkyl (C3-8) alkyl C0-10 (carbonyl) 0-1oxy alkyl C0-10, heteroarylalkyl C0-10 (carbonyl) 0-1oxyalkyl C0-10, heterocycloalkyl (C3-8) alkyl C0-10 (carbonyl) 0-1oxy alkyl C0-10, (alkyl (C0-10 )) 1-2-aminocarbonyloxy, heteroalkyl (C0-10) aminocarbonyloxy, arylalkyl (C0-10) aminocarbonyloxy, cycloalkyl (C3-8) alkyl (C0-10) aminocarbonyloxy, heteroarylalkyl (C0-10) aminocarbonyloxy, heterocycloalkyl (C3-8) (C0-10) aminocarbonyloxy, C0-10 alkyl amino (oxy) 0-1carbonylalkyl C0-10, heteroalkyl (C0-10) amino (oxy) 0-1carbonylalkylC0-10 alkyl, C3-8 alkyl C0-10 amino ( oxy) 0-1carbonyl

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