405554-62-3Relevant academic research and scientific papers
The identification of potent and selective imidazole-based inhibitors of B-Raf kinase
Takle, Andrew K.,Brown, Murray J.B.,Davies, Susannah,Dean, David K.,Francis, Gerraint,Gaiba, Alessandra,Hird, Alex W.,King, Frank D.,Lovell, Peter J.,Naylor, Antoinette,Reith, Alastair D.,Steadman, Jon G.,Wilson, David M.
, p. 378 - 381 (2006)
A novel triarylimidazole derivative, SB-590885 (33), bearing a 2,3-dihydro-1H-inden-1-one oxime substituent has been identified as a potent and extremely selective inhibitor of B-Raf kinase.
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase
Takle, Andrew K.,Bamford, Mark J.,Davies, Susannah,Davis, Robert P.,Dean, David K.,Gaiba, Alessandra,Irving, Elaine A.,King, Frank D.,Naylor, Antoinette,Parr, Christopher A.,Ray, Alison M.,Reith, Alastair D.,Smith, Beverley B.,Staton, Penelope C.,Steadman, Jon G.A.,Stean, Tania O.,Wilson, David M.
scheme or table, p. 4373 - 4376 (2009/04/06)
Modification of the potent imidazole-based B-Raf inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in vivo to challenge the hypothesis that selective B-Raf inhibitors may be of value in the treatment of stroke.
Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H- indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management
Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Surowy, Carol S.,Honore, Prisca,Marsh, Kennan C.,Hannick, Steven M.,McDonald, Heath A.,Wetter, Jill M.,Sullivan, James P.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 392 - 395 (2008/09/17)
Vanilloid receptor TRPV1 is a cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of TRPV1 activation by selective antagonists is under investigation by several pharmaceutical companies in an effort to identify novel agents for pain management. Here we report that replacement of substituted benzyl groups by an indan rigid moiety in a previously described N-indazole-N′-benzyl urea series led to a number of TRPV1 antagonists with significantly increased in vitro potency and enhanced drug-like properties. Extensive evaluation of pharmacological, pharmacokinetic, and toxicological properties of synthesized analogs resulted in identification of (R)-7 (ABT-102). Both the analgesic activity and drug-like properties of (R)-7 support its advancement into clinical pain trials.
Prodrugs of compounds that inhibit TRPV1 receptor
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Page/Page column 33-34, (2010/11/27)
Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladd
Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Page 15, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
