851266-39-2Relevant academic research and scientific papers
Tetrahydro-naphthols as orally available TRPV1 inhibitors
Urbahns, Klaus,Yura, Takeshi,Gupta, Jang B.,Tajimi, Masaomi,Fujishima, Hiroshi,Masuda, Tsutomu,Yamamoto, Noriyuki,Ikegami, Yuka,Marumo, Makiko,Yasoshima, Kayo,Yoshida, Nagahiro,Moriwaki, Toshiya,Madge, David,Chan, Fiona,Mogi, Muneto
scheme or table, p. 3408 - 3411 (2012/06/29)
Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lead's phenol structure whilst maintai
TETRAHYDRO-NAPHTHALENE AND UREA DERIVATIVES
-
Page/Page column 85-87, (2015/05/06)
This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD). BHC 03 2 001-Foreign-Countries - 66 - BHC 03 2 001-Foreign-Countries - 65 -
