- Development of a scaleable synthesis of a partial nicotinic acid receptor agonist
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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.
- 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.
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experimental part
p. 543 - 547
(2010/04/22)
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- 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
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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,
- 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.
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experimental part
p. 5101 - 5108
(2009/08/07)
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- COMPOSITIONS FOR TREATING FLUSHING AND LIPID-ASSOCIATED DISORDERS COMPRISING NIACIN RECEPTOR PARTIAL AGONISTS
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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
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Page/Page column 75
(2010/11/30)
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- METHOD OF TREATING ATHEROSCLEROSIS, DYSLIPIDEMIAS AND RELATED CONDITIONS
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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
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Page/Page column 39
(2010/10/20)
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- TETRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF
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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
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Page/Page column 60
(2010/02/11)
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