573676-05-8Relevant articles and documents
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists
Blum, Charles A.,Caldwell, Timothy,Zheng, Xiaozhang,Bakthavatchalam, Rajagopal,Capitosti, Scott,Brielmann, Harry,De Lombaert, Stéphane,Kershaw, Mark T.,Matson, David,Krause, James E.,Cortright, Daniel,Crandall, Marci,Martin, William J.,Murphy, Beth Ann,Boyce, Susan,Jones, A. Brian,Mason, Glenn,Rycroft, Wayne,Perrett, Helen,Conley, Rachael,Burnaby-Davies, Nicola,Chenard, Bertrand L.,Hodgetts, Kevin J.
experimental part, p. 3330 - 3348 (2010/09/07)
The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a nonselective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antago
Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution
Blum, Charles A.,Zheng, Xiaozhang,Brielmann, Harry,Hodgetts, Kevin J.,Bakthavatchalam, Rajagopal,Chandrasekhar, Jayaraman,Krause, James E.,Cortright, Daniel,Matson, David,Crandall, Marci,Ngo, Chu K.,Fung, Lawrence,Day, Marta,Kershaw, Mark,De Lombaert, Stephane,Chenard, Bertrand L.
scheme or table, p. 4573 - 4577 (2009/04/06)
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflammator
From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist
Zheng, Xiaozhang,Hodgetts, Kevin J.,Brielmann, Harry,Hutchison, Alan,Burkamp, Frank,Brian Jones,Blurton, Peter,Clarkson, Robert,Chandrasekhar, Jayaraman,Bakthavatchalam, Rajagopal,De Lombaert, Stephane,Crandall, Marci,Cortright, Daniel,Blum, Charles A.
, p. 5217 - 5221 (2007/10/03)
Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1 anta
SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES
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, (2008/06/13)
Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor
SUBSTITUTED CINNOLIN-4-YLAMINES
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Page/Page column 37, (2008/06/13)
Substituted cinnolin-4-ylamines are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activityin vivo or in vitro, and are particularly useful in the treatmen
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
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Page/Page column 17, (2010/02/14)
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions assoc
SUBSTITUTED BIPHENYL-4-CARBOXYLIC ACID ARYLAMIDE ANALOGUES
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, (2008/06/13)
Substituted bipheny1-4-carboxylic acid arylamide analogues capable of modulating receptor activity, are provided. Such ligands may be used to modulate receptor activity in viva or in vitro, and are particularly useful in the treatment of pain and other co
