1334783-47-9Relevant academic research and scientific papers
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor
McClure, Kim F.,Jackson, Margaret,Cameron, Kimberly O.,Kung, Daniel W.,Perry, David A.,Orr, Suvi T.M.,Zhang, Yingxin,Kohrt, Jeffrey,Tu, Meihua,Gao, Hua,Fernando, Dilinie,Jones, Ryan,Erasga, Noe,Wang, Guoqiang,Polivkova, Jana,Jiao, Wenhua,Swartz, Roger,Ueno, Hirokazu,Bhattacharya, Samit K.,Stock, Ingrid A.,Varma, Sam,Bagdasarian, Victoria,Perez, Sylvie,Kelly-Sullivan, Dawn,Wang, Ruduan,Kong, Jimmy,Cornelius, Peter,Michael, Laura,Lee, Eunsun,Janssen, Ann,Steyn, Stefanus J.,Lapham, Kimberly,Goosen, Theunis
, p. 5410 - 5414 (2013)
The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine-piperidine inverse agonists of the ghrelin receptor is described. Decreased mAChR muscarinic M2 binding was achieved by use of a chiral indane in place of a substituted benzylic group. Compounds with desirable balance of human in vitro clearance and ex vivo central receptor occupancy were discovered by incorporation of heterocycles. Specifically, heteroaryl rings with nitrogen(s) vicinal to the indane linkage provided the most attractive overall properties.
2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES
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Page/Page column 58-59, (2011/10/10)
The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
