- Tetrahydro-naphthols as orally available TRPV1 inhibitors
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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
- 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
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scheme or table
p. 3408 - 3411
(2012/06/29)
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- SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
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Page/Page column 150
(2010/11/18)
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- Vanilloid receptor (VR) inhibitors for treatment of Human Immunodeficiency Virus (HIV)-mediated pain states
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The invention relates to the application of Vanilloid receptor (VR) 1 inhibitors for drug development and for the treatment of HIV-mediated neuropathies and neuropathic pain states. Further, the inventor identified a novel signaling cascade connecting the
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- TETRAHYDRO-NAPHTHALENE AND UREA DERIVATIVES
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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 -
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Page/Page column 100-101
(2015/05/06)
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- HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES
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This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excelle
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- TETRAHYDRO-NAPHTHALENE DERIVATIVES AS VANILLOID RECEPTOR ANTAGONISTS
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This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antago
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- TETRAHYDRO-NAPHTHALENE DERIVATIVES
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This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antago
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- HYDROXY TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES
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This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antago
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Page/Page column 46
(2008/06/13)
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