- Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists
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Several polar heteroaromatic acetic acids and their piperidine amides were synthesized and evaluated as ghrelin or type 1a growth hormone secretagogue receptor (GHS-R1a) inverse agonists. Efforts to improve pharmacokinetic and safety profile was achieved
- Orr, Suvi T. M.,Beveridge, Ramsay,Bhattacharya, Samit K.,Cameron, Kimberly O.,Coffey, Steven,Fernando, Dilinie,Hepworth, David,Jackson, Margaret V.,Khot, Vishal,Kosa, Rachel,Lapham, Kimberly,Loria, Paula M.,McClure, Kim F.,Patel, Jigna,Rose, Colin,Saenz, James,Stock, Ingrid A.,Storer, Gregory,Von Volkenburg, Maria,Vrieze, Derek,Wang, Guoqiang,Xiao, Jun,Zhang, Yingxin
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supporting information
p. 156 - 161
(2015/03/04)
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- 2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES
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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.
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Page/Page column 31
(2011/10/10)
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