ANDREWS STEVEN WADE,CONDROSKI KEVIN RONALD,HAAS JULIA,JIANG YUTONG,KOLAKOWSKI GABRIELLE R.,SEO JEONGBEOB,YANG HONG WOON,ZHAO QIAN
申请号:
ARP110101715
公开号:
AR081919A1
申请日:
2011.05.19
申请国别(地区):
AR
年份:
2012
代理人:
摘要:
Trk inhibitors, compounds 1 for the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases: a compound of a common formula (1) or a salt acceptable for the drug, in which ring a is selected from the formula ring (A-1),The corrugation line 1 of (A-2) and (A-3) represents the connection point between ring a and ring B, and the corrugation line 2 represents the connection point between ring a and Ring w; X is n or CH; y is h or F; R1 is h, alcox c1-3 or halogen; ring B is selected from formula rings (B-1) and (b-2), in which the corrugation line marked with 3 represents a. The connection point of ring a and 4 corrugated line represents the connection point with pirazolo [1.5-A] piriminadine (1) of the formula ring;W is O, NH or CH2, when ring a is formula (A-2),So w is CH2, M is 0, 1 or 2, D is carbon, R2 and R2A are independent h, F, c1-3 tar or Oh (provided R2 and R2A are not the same oh),R3 and R3a are independent h, c1-3 tar or c1-3 hydrogen Xi tar, or D is carbon or nitrogen. R2 and R3 do not exist. R2A and R3a, together with the atoms to which they are attached, form a 5-6 heterocycle consisting of 1-2 ring atoms; Z is * - nr4ac (= O) -.-ONHC (3DO) --NR4bCH2- o -OC (3DO) -wherein the asterisk indicates the point of attachment of Z to the carbon that R3 carries; R4a is H, C1-6 alkyl, fluoro-C1-6 alkyl, difluoro-C1-6 alkyl, trifluoro-C1-6 alkyl, hydroxy (C1-6 alkyl) or dihydroxy (C2-6 alkyl);R4b is H, C1-6 alkyl, fluoro-C1-6 alkyl, difluoro-C1-6 alkyl, trifluoro-C1-6 alkyl, hydroxy (C1-6 alkyl),1. Dihydroxi (c2-6 tar);1. C1-6-c (o) tarcicloalquil C3-6-C (O) -Ar1C (O) -,That's what it means.C1-6-sulfur, cyclomethyleneglycol c3-6-sulfur, ar2 (SO2) -,HO2CCH2- o alquil C1-6-NH (CO) -AR1 is an optional phenyl substitute, which is replaced by one or more independent halogen, C1-6 tar and alcox C1-6 substitutes; ar2 is an optional phenyl substitute, which is replaced by one or more independent halogen, C1-6 tar and alcox C1-6 s