14347-25-2Relevant articles and documents
Development of an enabling route to PF-00610355: A novel inhaled β2-adrenoreceptor agonist
De Koning, Pieter D.,Gladwell, Iain R.,Moses, Ian B.,Panesar, Maninder S.,Pettman, Alan J.,Thomson, Nicholas M.
, p. 1247 - 1255 (2012/01/19)
The initial route used to prepare PF-00610355 (8) for early clinical development is described. Through careful choice of solvent, an efficient, telescoped route to carboxylic acid 23 was developed, affording this late-stage intermediate in 80% yield over 4 steps. Deprotection of 23 to give sodium salt 24a and coupling with amine 6·HCl afforded the desired API. Effective synthetic routes to two of the starting materials, chiral bromide 1 and amine 6, are also described.
4-Aminopiperidine ureas as potent selective agonists of the human β3-Adrenergic receptor
Ashwell, Mark A,Solvibile Jr., William R,Han, Stella,Largis, Elwood,Mulvey, Ruth,Tillet, Jeffrey
, p. 3123 - 3127 (2007/10/03)
The preparation and structure-activity relationships (SARs) of potent agonists of the human β3-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human β3-AR potency with selectivity over human β1-AR and/or human β2-AR agonism. Compound 29s was identified as a potent (EC50 = 1 nM) and selective (greater than 400-fold over β1- with no β2-AR agonism) full β3-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.
CATECHOLAMINE SURROGATES USEFUL AS BETA 3 AGONISTS
-
, (2008/06/13)
Compounds of the formula STR1 and pharmaceutically acceptable salts thereof. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.
