851776-30-2Relevant academic research and scientific papers
Development of a scaleable synthesis of a partial nicotinic acid receptor agonist
Wilson, Robert D.,Cleator, Ed,Ashwood, Michael S.,Bio, Matthew M.,Brands, Karel M.J.,Davies, Antony J.,Dolling, Ulf-H,Emerson, Khateeta M.,Gibb, Andrew D.,Hands, David,McKeown, Arlene E.,Oliver, Steven F.,Reamer, Robert A.,Sheen, Faye J.,Stewart, Gavin W.,Zhou, George X.
experimental part, p. 543 - 547 (2010/04/22)
A practical and efficient synthesis of 1,4,5,6-tetrahydro-3-(1Htetrazol- 5-yl)cyclopenta[c]pyrazole, 1, is described. A new one-pot process has been developed, starting from the commercially available 1H-tetrazole-5-carboxylic acid-ethyl ester sodium salt which is reacted in a pseudo-Claisen condensation reaction with cyclopentanone, followed by the addition of hydrazine.
3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice
Semple, Graeme,Skinner, Philip J.,Gharbaoui, Tawfik,Shin, Young-Jun,Jung, Jae-Kyu,Cherrier, Martin C.,Webb, Peter J.,Tamura, Susan Y.,Boatman, P. Douglas,Sage, Carleton R.,Schrader, Thomas O.,Chen, Ruoping,Colletti, Steven L.,Tata, James R.,Waters, M. Gerard,Cheng, Kang,Taggart, Andrew K.,Cai, Tian-Quan,Carballo-Jane, Ester,Behan, Dominic P.,Connolly, Daniel T.,Richman, Jeremy G.
experimental part, p. 5101 - 5108 (2009/08/07)
The discovery and profiling of 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro- cyclopentapyrazole (5a, MK-0354), a partial agonist of GPR109a, is described. Compound 5a retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism,
COMPOSITIONS FOR TREATING FLUSHING AND LIPID-ASSOCIATED DISORDERS COMPRISING NIACIN RECEPTOR PARTIAL AGONISTS
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Page/Page column 79, (2010/11/30)
The invention provides a method of reducing flushing induced by niacin or a niacin analog in a subject, comprising administering to said subject an effective flush reducing amount of a niacin receptor partial agonist. In addition, the invention provides a
METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS
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Page/Page column 39, (2010/10/20)
A method of treating atherosclerosis, dyslipidemia and related conditions is disclosed wherein a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof is administered to the patient in combination with a DP receptor antagonist. T
TETRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF
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Page/Page column 60; 64, (2010/02/11)
The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present in
