Pirrolo [2,3-b] pyridines kinase inhibiting Chk1 and Chk2, Pharmaceutical compositions containing them and Process for preparing them and their use in the treatment and Prevention of cancer.
Ле Хюроу Івен,Блейк Джеймс Ф.,Ганвордана Індрані У.,Мор Пітер Дж.,Уоллес Ілай М.,Ван Бін,Чікареллі Марк,Лайон Майкл
申请号:
UAA201015012
公开号:
UA111933C2
申请日:
2009.05.13
申请国别(地区):
UA
年份:
2016
代理人:
摘要:
Claim 1: a selected Compound of Formula 1 and stereoisomers, pharmaceutically acceptable Salts and tautomeros them, where to choose: a direct link or crarb; r1 is selected from Hydrogen, halogen, alkyl of C1 CN, alquenilo C1 - 6, - 6, - (alkyl - or - C1, 6) s (alkyl C1 - 6 - 6), a heterocclico cycloalkyl C3, 4 to 6 members, phenylHeteroaryl and a 5 or 6 members, where the alquenilo, alkyl, cycloalkyl, heterocclico phenyl or heteroaryl substituted, optionally with one or m u00a0s groups selected from Halogen, CN, CF3, c1-3 alkyl or alkyl, - C1 - 3), and nrcrd alkyl; R2 is selected from C1 - 6 - (alkyl, or C1 - 6) - NH (alkyl, cycloalkyl, a C1 - C3 - 6) 6 partially saturated or unsaturated, phenylA heterocclico 4-6 members partially saturated or unsaturated, 5 or 6 members of a heteroaryl, aryl bicclico 8 to 10 members, a heterocclico bicclico 8 to 10 members and a heteroaryl bicclico 8 to 10 members, where the phenyl, alkyl, cycloalkyl, heteroccl Heteroarilos and aryl substituted, optionally with one or m u00a0s selected groups of Oh, CN,Halogen, oxo (except not in aryl or heteroaryl phenyl), NF3, ciclopropilo, ciclopropilmetilo so2ri, C1 -, alkyl - or 6 - (alkyl C1 - 6 S (alkyl) - C1 - 6), nrerf, where the phenyl and phenyl groups is replaced with one or m u00a0s selected Oh, CN, CF3, Halogen, alkyl of C1 - 3 - (c1-3 alkyl or,And nrgrh; R3 and R4 are independently Hydrogen or optionally substituted alkyl of C1 - 4 with Oh, F - (c1-3 alkyl or cycloalkyl - 6) or C3, R3 and R4 with the u00a0tomos est u00a0n which United to form a Ring of 5 or 6 members; R5 is selected Hydrogen and CH3, or to create B,Ra and RB are Hydrogen and R3 and R5 along with the u00a0tomos est u00a0n which United to form a Ring of 5 or 6 members; R6 is selected from Hydrogen, F, Oh, - OCH3, c1-3 alkyl or cycloalkyl, or is a direct link, r6a R6 and R3 is Hydrogen, and together with the u00a0tomos which United to form est u00a0n A Ring of 5 or 6 members; r6a is selected from Hydrogen, F, oh and