1123620-89-2Relevant articles and documents
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy
McCoull, William,Bailey, Andrew,Barton, Peter,Birch, Alan M.,Brown, Alastair J. H.,Butler, Hayley S.,Boyd, Scott,Butlin, Roger J.,Chappell, Ben,Clarkson, Paul,Collins, Shelley,Davies, Robert M. D.,Ertan, Anne,Hammond, Clare D.,Holmes, Jane L.,Lenaghan, Carol,Midha, Anita,Morentin-Gutierrez, Pablo,Moore, Jane E.,Raubo, Piotr,Robb, Graeme
, p. 3187 - 3197 (2017/04/19)
GPR120 agonists have therapeutic potential for the treatment of diabetes, but few selective agonists have been reported. We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency. Furthermore, we identified a (S,S)-cyclopropylcarboxylic acid structural motif which gave selectivity against GPR40. Good oral exposure was obtained with some compounds displaying unexpected high CNS penetration. Increased MDCK efflux was utilized to identify compounds such as 33 with lower CNS penetration, and activity in oral glucose tolerance studies was demonstrated. Differential activity was observed in GPR120 null and wild-type mice indicating that this effect operates through a mechanism involving GPR120 agonism.
Crystalline Form Of A Cyclopropyl Benzamide Derivative
-
, (2011/09/14)
The present invention relates to a crystalline form of compound (I), 4-{(1S,2S)-2-[(4-cyclobutylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide, pharmaceutical formulations containing said compound and to the use of said active compound in therapy.
Solid Forms Comprising A Cyclopropyl Amide Derivative
-
, (2011/09/14)
This disclosure relates to at least one solid form of 4-{(1S, 2S)-2-[((R)-4-cyclobutyl-2-methylpiperazin-1-yl)carbonyl]-cyclopropyl}-benzamide. This disclosure also relates to at least one pharmaceutical composition comprising at least one solid form described herein, methods of using the solid forms and pharmaceutical compositions comprised thereof, and processes of manufacturing the solid forms.
Cyclopropyl Amide Derivatives
-
Page/Page column 53-54, (2010/09/05)
Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
4-OXO-1-(3-SUBSTITUTED PHENYL-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXAMIDE PHOSPHODIESTERASE-4 INHIBITORS
-
Page 43, (2010/02/07)
Compounds represented by Formula (I):or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition.