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7h pyrrolo [2,3-d] pyrimidines 4 - (substituted amino) as inhibitors of LRRK2
专利权人:
PFIZER INC.
发明人:
申请号:
ARP130102325
公开号:
AR091628A1
申请日:
2013.06.28
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
It is also directed to pharmaceutical compositions comprising the compounds of formula (1) and to the use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy, LRRK2 is an active 86 kDa protein kinase. Claim 1: A compound of the formula the formula (1) or a pharmaceutically acceptable salt thereof, wherein each of R¹ and R² are independently hydrogen, C₁₋₆-alkyl,cycloalkyl C₃₋₇,a four to seven membered heterocycloalkyl containing one to three heteroatoms selected from N, O, and S; or a five to six membered heteroaryl containing one to four heteroatoms selected from N, O, and S, wherein the C₁₋₆ alkyl,cycloalkyl C₃₋₇,a. Heterosexuality of four to seven members or five to six members may be changed to one to three r8310 optionally;O R1 and R2, combined with the added nitrogen, are a four to seven member heterocyclic propene, optionally containing one to two additional heteroatoms selected from n, O and s, and optionally two links; 1. Heterosexuality consisting of 6 to 11 members, optionally including 1 to 2 extra heterosexual atoms selected from n, O and S; or heterosexuality consisting of 6 to 12 members, optionally including 1 to 2 extra heterosexual atoms selected from n, O and S; There, heterosexuals have four or seven members,The isomerization dechlorination of 6 to 11 members or the isomerization dechlorination of 6 to 12 members can optionally be replaced by 1 to 3 r8311;R³ is phenyl or a five to ten membered heteroaryl containing from one to four heteroatoms selected from N, O and S; wherein the five to ten membered phenyl and heteroaryl are optionally substituted with one to three R⁹ and where the phenyl is optionally fused with a C₅₋₆ cycloalkyl or a five to six membered heterocycloalkyl containing one to three selected heteroatoms starting with N, O and S and which is optionally substituted with oxo; R⁴ and R⁵ are each
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