18650-38-9Relevant articles and documents
DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE AND PHARMACEUTICALS CONTAINING THE SAME
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Paragraph 1328, (2016/01/30)
The present invention provides a dihydropyridazine-3,5-dione derivative or a salt thereof, or a solvate of the compound or the salt, a pharmaceutical drug, a pharmaceutical composition, a sodium-dependent phosphate transporter inhibitor, and a preventive and/or therapeutic agent for hyperphosphatemia, secondary hyperparathyroidism, chronic renal failure, chronic kidney disease, and arteriosclerosis associated with vascular calcification comprising the compound as an active ingredient, and a method for prevention and/or treatment.
Design and Synthesis of (R)-1-Arylsulfonylpiperidine-2-carboxamides as 11β-Hydroxysteroid Dehydrogenase Type1 Inhibitors
Xia, Guangxin,Liu, Lin,Liu, Haiyan,Yu, Jianxin,Xu, Zhenmin,Chen, Qian,Ma, Chen,Li, Ping,Xiong, Bing,Liu, Xuejun,Shen, Jingkang
supporting information, p. 577 - 581 (2013/08/22)
R adamantly beats S: 11β-HSD1 is a target for treating metabolic syndrome. The Risomer 5 was selected as a starting point for optimization and SAR studies. Inhibitor 8w emerged after several rounds of optimization, showing cross-species inhibition of human and mouse 11β-HSD1. It also displays a good DMPK profile invitro, and was advanced to PK/PD evaluations invivo. The results confirmed its dose-dependent activity in mice.
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists
Lamb, Jeffrey P.,Engers, Darren W.,Niswender, Colleen M.,Rodriguez, Alice L.,Venable, Daryl F.,Conn, Jeffrey P.,Lindsley, Craig W.
scheme or table, p. 2711 - 2714 (2011/06/20)
This Letter describes a chemical lead optimization campaign directed at a weak mGlu5 NAM discovered while developing SAR for the mGlu 5 PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu5 NAMs, mGlu5 PAMs as well as mGlu5 partial antagonists.
Electrochemical deallylation of α-allyl cyclic amines and synthesis of optically active quaternary cyclic amino acids
Kirira, Peter G.,Kuriyama, Masami,Onomura, Osamu
experimental part, p. 3970 - 3982 (2010/07/04)
Electrochemical oxidation of α-allylated and α-betizylated N-acylated cyclic amines by using a graphite anode easily affords the corresponding α-methoxylated products with up to 76% yield. Ease of oxidation was affected by the type of electrode, the size
Synthesis of (D)- And (L)-forms of differentially protected 2-piperidinemethanamine
Perumattam, John,Shearer, Barry G.,Confer, William L.,Mathew, Rose M.
, p. 7183 - 7186 (2007/10/02)
(D)- and (L)-isomers of pipecolic acid were converted into (D)- and (L)-2-piperidinemethanamine using an efficient sequence. The amino groups were selectively protected for further functionalization.
ENANTIOSELECTIVE REDUCTIONS OF KETONES WITH OXAZABOROLIDINES DERIVED FROM (R) AND (S)-α,α-DIPHENYL-2-PIPERIDINE METHANOL
Rao, A. V. Rama,Gurjar, M. K.,Sharma, P. A.,Kaiwar, Vijay
, p. 2341 - 2344 (2007/10/02)
Oxazaborolidnes obtained from (R) and (S)-α,α-diphenyl-2-piperidine methanol have been used as catalysts in the enantioselective reductions of ketones with borane.
