860434-15-7Relevant academic research and scientific papers
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines as potent melanin-concentrating hormone receptor 1 antagonists
Giordanetto, Fabrizio,Karlsson, Olle,Lindberg, Jan,Larsson, Lars-Olof,Linusson, Anna,Evertsson, Emma,Morgan, David G.A.,Inghardt, Tord
, p. 4232 - 4241 (2008/12/21)
We herein report the optimization of cyclopentane- and cyclohexane-1,3-diamine derivatives as novel and potent MCH-R1 antagonists. Structural modifications of the 2-amino-quinoline and thiophene moieties found in the initial lead compound served to improve its metabolic stability profile and MCH-R1 affinity, and revealed unprecedented SAR when compared to other 2-amino-quinoline-containing MCH-R1 antagonists.
THERAPEUTIC AGENTS I
-
Page/Page column 39, (2010/02/12)
Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
