(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: A Wingless β-Catenin Agonist That Increases Bone Formation Rate
摘要:
A high-throughput screening campaign to discover small molecule leads for the treatment of bone disorders concluded with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-catenin cellular messaging system. Hit-to-lead in vitro optimization for target activity and molecular properties led to the discovery of (1-(4-(naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine (5, WAY-262611). Compound 5 has excellent pharmacokinetic properties and showed a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration.
NAPHTHYLPYRIMIDINE, NAPHTHYLPYRAZINE AND NAPHTHYLPYRIDAZINE ANALOGS AND THEIR USE AS AGONISTS OF THE WNT-BETA-CATENIN CELLULAR MESSAGING SYSTEM
申请人:Pelletier Jeffrey Claude
公开号:US20090054392A1
公开(公告)日:2009-02-26
The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-β-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.
Ester diol alkoxylate based alkyd resins and compositions containing them
申请人:UNION CARBIDE CORPORATION
公开号:EP0040979A2
公开(公告)日:1981-12-02
An alkyd resin characterised in that it comprises the reaction product of (A) an ester diol alkoxylate of the formula
wherein m is an integer having a value of from 2 to 4, n is an integer having a value of from 1 to 5, x and y are integers each having a value of from 1 to 20, and R is an unsubstituted or substituted alkyl group having from 1 to 8 carbon atoms with (B) a polyol and (C) a polycarboxylic acid or anhydride thereof.
A coating composition comprising such a resin and the coating composition when cured.