- DIHYDROPYRIDAZINE-3,5-DIONE DERIVATIVE AND PHARMACEUTICALS CONTAINING THE SAME
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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.
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Paragraph 1328
(2016/01/30)
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- Design and Synthesis of (R)-1-Arylsulfonylpiperidine-2-carboxamides as 11β-Hydroxysteroid Dehydrogenase Type1 Inhibitors
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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.
- Xia, Guangxin,Liu, Lin,Liu, Haiyan,Yu, Jianxin,Xu, Zhenmin,Chen, Qian,Ma, Chen,Li, Ping,Xiong, Bing,Liu, Xuejun,Shen, Jingkang
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supporting information
p. 577 - 581
(2013/08/22)
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- 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
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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.
- Lamb, Jeffrey P.,Engers, Darren W.,Niswender, Colleen M.,Rodriguez, Alice L.,Venable, Daryl F.,Conn, Jeffrey P.,Lindsley, Craig W.
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scheme or table
p. 2711 - 2714
(2011/06/20)
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- Electrochemical deallylation of α-allyl cyclic amines and synthesis of optically active quaternary cyclic amino acids
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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
- Kirira, Peter G.,Kuriyama, Masami,Onomura, Osamu
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experimental part
p. 3970 - 3982
(2010/07/04)
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- Synthesis of (D)- And (L)-forms of differentially protected 2-piperidinemethanamine
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(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.
- Perumattam, John,Shearer, Barry G.,Confer, William L.,Mathew, Rose M.
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p. 7183 - 7186
(2007/10/02)
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- ENANTIOSELECTIVE REDUCTIONS OF KETONES WITH OXAZABOROLIDINES DERIVED FROM (R) AND (S)-α,α-DIPHENYL-2-PIPERIDINE METHANOL
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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.
- Rao, A. V. Rama,Gurjar, M. K.,Sharma, P. A.,Kaiwar, Vijay
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p. 2341 - 2344
(2007/10/02)
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