717906-56-4Relevant academic research and scientific papers
Discovery of SB-705498: A potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development
Rami, Harshad K.,Thompson, Mervyn,Stemp, Geoffrey,Fell, Steve,Jerman, Jeffrey C.,Stevens, Alexander J.,Smart, Darren,Sargent, Becky,Sanderson, Dominic,Randall, Andrew D.,Gunthorpe, Martin J.,Davis, John B.
, p. 3287 - 3291 (2007/10/03)
Small molecule antagonists of the vanilloid receptor TRPV1 (also known as VR1) are disclosed. Pyrrolidinyl ureas such as 8 and 15 (SB-705498) emerged as lead compounds following optimisation of the previously described urea SB-452533. Pharmacological studies using electrophysiological and FLIPR-Ca2+-based assays showed that compounds such as 8 and 15 were potent antagonists versus the multiple chemical and physical modes of TRPV1 activation (namely capsaicin, acid and noxious heat). Furthermore, 15 possessed suitable developability properties to enable progression of this compound into in vivo studies and subsequently clinical development.
ANILINE DERIVATIVES
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Page/Page column 34, (2010/11/25)
The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds represented by the formulas (A), (B), (C), (E) and (H) : wherein each symbol is as defined in the specification, or a pharmac
UREA COMPOUNDS ACTIVE AS VANILLOID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF PAIN
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Page 13-14, (2010/02/06)
Certain compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, P, P', n, p, q, r and s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.
