581812-77-3Relevant academic research and scientific papers
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists
Drizin, Irene,Gomtsyan, Arthur,Bayburt, Erol K.,Schmidt, Robert G.,Zheng, Guo Zhu,Perner, Richard J.,DiDomenico, Stanley,Koenig, John R.,Turner, Sean C.,Jinkerson, Tammie K.,Brown, Brian S.,Keddy, Ryan G.,McDonald, Heath A.,Honore, Prisca,Wismer, Carol T.,Marsh, Kennan C.,Wetter, Jill M.,Polakowski, James S.,Segreti, Jason A.,Jarvis, Michael F.,Faltynek, Connie R.,Lee, Chih-Hung
, p. 4740 - 4749 (2007/10/03)
Novel 5,6-fused heteroaromatic ureas were synthesized and evaluated for their activity as TRPV1 antagonists. It was found that 4-aminoindoles and indazoles are the preferential cores for the attachment of ureas. Bulky electron-withdrawing groups in the para-position of the aromatic ring of the urea substituents imparted the best in vitro potency at TRPV1. The most potent derivatives were assessed in in vivo inflammatory and neuropathic pain models. Compound 46, containing the indazole core and a 3,4-dichlorophenyl group appended to it via a urea linker, demonstrated in vivo analgesic activity upon oral administration. This derivative also showed selectivity versus other receptors in the CEREP screen and exhibited acceptable cardiovascular safety at levels exceeding the therapeutic dose.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity, wherein X1, X2, X3, X4, X5, R5, R6, R7, R8a, R8b, R9, Z1, Z2 and L are as defined in the description.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
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Page/Page column 37, (2010/02/11)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
-
, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
-
, (2008/06/13)
Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
