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Inhibitors of serine / Threonine Kinase
专利权人:
GENENTECH; INC.
发明人:
申请号:
ARP140104549
公开号:
AR098647A1
申请日:
2014.12.05
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
Formula compound (1) is an inhibitor of ERK cyclase. It also describes the components and methods of treatment for diffuse disorders. Claim 1: a formula compound (1), characterized by: X1 is n or CH; X2 is NR 749191;O o s; X3 is (cr.8308;]CH₂NRᵇ,it is life.C (= O) nr7495o o (= O) or the condition is: X3 is ch8322; nr74955;The other three cycle formula (1) is 6.7.8, 9-tetrahydro-1, 2, 2A1, 6.8-pentaazabenzo [CD] azoleno, while X3 is C (= O) n74955;The other three cycle equation (1) is 8.9-dihydro-1, 2, 2A1, 6.8-pentaazabenzo [CD] azulen-7 (6h) - ona, while X3 is ch8322; (= O),the tricyclic residue of formula (1) is an 8,9-dihydro-1,2,2a¹, 6-tetraazabenzo [cd] azulen-7 (6H) -one and when X³ is C (= O) O, the tricyclic residue of formula (1) is a 6H-8-oxa-1,2,2a¹, 6-tetraazabenzo [cd] azulen-7 (9H) -one; X⁴ is CR²R³ or NR³ with the proviso that when X⁴ is NR³,X2 is No. 7491, X3 is C (= O);R1 is a heterocyclic compound of (I) 4 to 7 saturated or partially unsaturated members, or (II) 5 to 6 optional replacement members; R2 is selected from the following groups: (a) c83218331; (8320a);(B) alquenilo C (c) haloalquilo C(d) C₃₋₇ cycloalkyl or C₃₋₇ cycloalkyl-C₁₋₆ alkyl;(E) halocicloalquilo C o halocicloalquilo C -alquilo C(f) C₁₋₁₀ hydroxyalkyl or C₁₋₁₀ dihydroxyalkyl;(G) alcoxi C -alquilo C(h) C₁₋₃-alkylthio-C₁₋₆-alkyl;(I) cianoalquilo C(j) Phenyl, phenyl tar c833218331s 83323; e. Phenyl or phenyl pitch c832131;(k) heteroaryl, heteroaryl-C₁₋₃-alkyl or heteroaryloxy wherein said heteroaryl moiety is selected from the group consisting of pyrazolyl, imidazolyl, oxazolyl, isoazolyl, thiazolyl, isothiazolyl, pyridinyl, pyrid-2 (1H) -one and 1- alkylpyrid-2 (1H) -one and each said heteroaryl is independently and optionally substituted with one or more groups selected from the group consisting of halogen, hydroxyl, oxide, C₁₋₆-alkoxy,haloalkoxy C₁₋₆,cyano, C₃₋₆ cycloalkyl and C₁₋₆ alkyl wherein said C₁₋₆ alkyl is optionally and independently substituted with one or more groups in
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