169750-01-0Relevant articles and documents
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity
Arita, Tsuyoshi,Asano, Masayoshi,Domon, Yuki,Kubota, Kazufumi,Machinaga, Nobuo,Shimada, Kousei
, (2020/09/04)
We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic ac
2 -AMINO-PYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS
-
Page/Page column 54, (2009/07/03)
2-Aminopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2
Hudson, Sarah,Kiankarimi, Mehrak,Rowbottom, Martin W.,Vickers, Troy D.,Wu, Dongpei,Pontillo, Joseph,Ching, Brett,Dwight, Wesley,Goodfellow, Val S.,Schwarz, David,Heise, Christopher E.,Madan, Ajay,Wen, Jenny,Ban, William,Wang, Hua,Wade, Warren S.
, p. 4922 - 4930 (2007/10/03)
The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.