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Compounds based on pyrazolo [1,5-a] pyrimidine, compositions containing same and Methods of use
专利权人:
LEXICON PHARMACEUTICALS; INC.
发明人:
YINGZHI BI,KENNETH GORDON CARSON,GIOVANNI CIANCHETTA,MICHAEL ALAN GREEN,GODWIN KUMI,ALAN MAIN,YULIAN ZHANG,GLENN GREGORY ZIPP
申请号:
ARP130100765
公开号:
AR090292A1
申请日:
2013.03.11
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Compositions comprising these compounds and Methods for their use in the treatment, Control and / or prevention of diseases and disorders mediated by kinase activity associated with dual 1.Claim 1: a method to inhibit the activity of an associated kinase 1 (AAK1) adapter, which comprises contacting the AAK1 with a compound of the formula (1) or a pharmaceutically acceptable Salt thereof, wherein: r u00b9 is r u00b9a or hidrocarbilo c u2081 u208b u2081 u2082 or heterocarbilo 2 - 12 members, optionally substituted,Where the replacement is optional, with one or more of r u00b9a r u00b9a; each is independently or u00b9c -, - N (r u00b9c) u2082, - C (o) r u00b9c, - C (o) or u00b9c, - C (o) n ( u2082 r u00b9c), - N (C (or r u00b9c) or u00b9c), cyano, or hidrocarbilo c u2081 u208b u2081 u2082 or heterocarbilo Halo 2 - 12 members, optionally substituted, where their Optional is calculated with one or more of r u00b9b r u00b9b; each is independently or u00b9c -, - N (r u00b9c) u2082, - C (o) r u00b9c, - C (o) or u00b9c,- C (o) n ( u2082 r u00b9c), - N (r u00b9c) C (o) or u00b9c, cyano or Halo; each r u00b9c is independently Hydrogen or hidrocarbilo c u2081 u208b u2081 u2082 or heterocarbilo 2 - 12 members, optionally substituted, where the replacement is optional, with one or more cyano Halo, or hydroxyl; R u00b2 is nr u00b2ar u00b2b, Where R u00b2a is Hydrogen and r u00b2b is hidrocarbilo c u2081 u208b u2081 u2082 or heterocarbilo 2 - 12 members, optionally substituted,Where the replacement is optional, with one or more r u00b2c; or r u00b2a and r u00b2b are taken together to form a heterocycle of 4 - 7 members, optionally substituted with one or more r u00b2c r u00b2c; each is independently or u00b2d -, - N (r u00b2d) u2082, - C (o) r u00b2d, - C (o) or u00b2d, - C (o) n ( u2082 r u00b2d), - N (r u00b2d) C (o) or u00b2d, Ciano, Halo or hidrocarbilo c u2081 u208b u2081 u2082 or heterocarbilo 2 - 12 members, optionally substituted,Where the replacement is optional, with
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