1214332-39-4Relevant articles and documents
Glutaminase inhibitors as well as compositions and applications thereof
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Paragraph 0634; 0687; 0688; 0689, (2018/01/09)
The invention provides a series of heterocyclic compounds expressed in a formula I. The compound comprises glutaminase inhibition activity, and can be used for treating diseases and symptoms related to dysfunction of glutaminase or raising activity of glutaminase.
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists
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
supporting information, p. 156 - 161 (2015/03/04)
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
Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate
Bhattacharya, Samit K.,Andrews, Kim,Beveridge, Ramsay,Cameron, Kimberly O.,Chen, Chiliu,Dunn, Matthew,Fernando, Dilinie,Gao, Hua,Hepworth, David,Jackson, V. Margaret,Khot, Vishal,Kong, Jimmy,Kosa, Rachel E.,Lapham, Kimberly,Loria, Paula M.,Londregan, Allyn T.,McClure, Kim F.,Orr, Suvi T. M.,Patel, Jigna,Rose, Colin,Saenz, James,Stock, Ingrid A.,Storer, Gregory,Vanvolkenburg, Maria,Vrieze, Derek,Wang, Guoqiang,Xiao, Jun,Zhang, Yingxin
supporting information, p. 474 - 479 (2014/06/09)
The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series is described. Examples from this series have promising in vivo pharmacokinetics and increase glucose-stimulated insulin secretion in human whole and dispersed islets. A physicochemistry-based strategy to increase lipophilic efficiency for ghrelin receptor potency and retain low clearance and satisfactory permeability while reducing off-target pharmacology led to the discovery of 16h. Compound 16h has a superior balance of ghrelin receptor pharmacology and off-target selectivity. On the basis of its promising pharmacological and safety profile, 16h was advanced to human clinical trials.
2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES
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Page/Page column 28-29, (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.