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Derivatives of pyridin - 2 - one with Inhibitory activity of Ezh2
专利权人:
EPIZYME; INC.
发明人:
KEILHACK HEIKE,KLAUS C. - DUNCAN KENNETH W.,KUNTZ KEVIN WAYNE,WARHOLIC NATALIE,CHESWORTH RICHARD
申请号:
ARP120101289
公开号:
AR086839A1
申请日:
2012.04.13
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
2. Pyrethroids, including drugs of its components and their use in cancer treatment. Require 1: formula (1) or compounds of salts acceptable to its drugs, wherein X1 is n or cr11; X2 is n or Cr13; X3 is n or C, X3 is n, R6 is not; Z is nr7r8, or7, s (o) Ar7 or cr7r8r14 A is 0, 1 or 2; each R1, R5, R9 and R10 is h or C1-6 tar and can be replaced by one or more alternatives selected from C1-6 halogenation, hydroxyl, COOH, C (o) or tar, cyanogen, C1-6 toxicology, c1-6-amino, di-c1-6-amino, di tar, c1-6-amino, cyclo-8, arilo-c6-10.1.4 to 12 members of isopropyl carbinol and 5 to 6 members of isopropyl carbinol; each R2, R3 and R4 is a separate es-q1-t1, wherein Q1 is the link or link of optional c1-3 tar, replaced by halogen, cyanogen, hydroxy or alcoxi C1-6 and T1 as h, halogen, hydroxy, library, cyanogen, azido or RS1, RS1 as c1-3, alquen2-6 tar, C1-6, C1-6, C (o) or - pitch C1-6, C3-8, arilo C6-10, ammonia, c1-6-amino, c1-6-amino, di-acquil c1-6-amino, 4-12 isoprene or 5-6 member isoprene, RS1 is replaced by one or more alternatives selected from halogen, hydroxyl, oxo, COH.C (O) O-C1-6alkyl, cyano, C1-6alkoxy, amino, mono-C1-6alkyl-amino, di-C1-6alkyl-amino, C3-8cycloalkyl, C6-10 aryl, heterocycloalkyl of 4-12 members and 5- or 6-membered heteroaryl; R6 is H, halo, cyano, azido, ORa, -NRaRb, -C (O) Ra, -C (O) ORa, -C (O) NRaRb, -NRbC (O) Ra, -S (O) bRa, -S (O) bNRaRb or RS2, where RS2 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl or 4- to 12-membered heterocycloalkyl, b is 0, 1 or 2, each of Ra and Rb, independently is H or RS3 and RS3 is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C6-10 aryl, 4- to 12-membered heterocycloalkyl or 5-heteroaryl or 6 members; or Ra and Rb,together with the N atom to which they are attached, they form a 4- to 12-membered heterocycloalkyl ring having 0 or 1 additional heteroatoms; and each of RS2, RS3 and the 4- to 12-membered heterocycloalkyl ring formed by Ra and Rb, is optionally substituted with one or more
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