- [heteroshikuridenasetoamido[heteroshikuridenasetoamido] derivative
-
The present invention provides, a novel method for producing a compound represented by formula (I) and a novel method for producing a compound represented by formula (B) or a salt thereof, which are intermediates in the production of formula (I).
- -
-
Paragraph 0298
(2021/02/18)
-
- Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain
-
In order to discover a novel type of analgesic, we investigated dual activity ligands with TRPV1 antagonism and mu-opioid receptor affinity with the goal of eliciting synergistic analgesia while avoiding the side effects associated with single targeting.
- Lee, Hobin,Ahn, Songyeon,Ann, Jihyae,Ha, Heejin,Yoo, Young Dong,Kim, Young Ho,Hwang, Ji-Young,Hur, Kwang-Hyun,Jang, Choon-Gon,Pearce, Larry V.,Esch, Timothy E.,Lewin, Nancy E.,Blumberg, Peter M.,Lee, Jeewoo
-
-
- Selective Catalytic Hydrogenation of Arenols by a Well-Defined Complex of Ruthenium and Phosphorus-Nitrogen PN3-Pincer Ligand Containing a Phenanthroline Backbone
-
Selective catalytic hydrogenation of aromatic compounds is extremely challenging using transition-metal catalysts. Hydrogenation of arenols to substituted tetrahydronaphthols or cyclohexanols has been reported only with heterogeneous catalysts. Herein, we demonstrate the selective hydrogenation of arenols to the corresponding tetrahydronaphthols or cyclohexanols catalyzed by a phenanthroline-based PN3-ruthenium pincer catalyst.
- Li, Huaifeng,Wang, Yuan,Lai, Zhiping,Huang, Kuo-Wei
-
p. 4446 - 4450
(2017/07/24)
-
- Tetrahydro-naphthols as orally available TRPV1 inhibitors
-
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
-
scheme or table
p. 3408 - 3411
(2012/06/29)
-
- SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
-
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)).
- -
-
Page/Page column 148; 150
(2010/11/18)
-
- Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
-
The synthesis and structure-activity relationships of a series of 5-monosubstituted and 4,5-disubstituted 2-arylaminooxazoles as novel antagonists of the transient receptor potential vanilloid 1 (TRPV1) receptor are described. The 7-hydroxy group of the t
- Perner, Richard J.,Koenig, John R.,Didomenico, Stanley,Gomtsyan, Arthur,Schmidt, Robert G.,Lee, Chih-Hung,Hsu, Margaret C.,McDonald, Heath A.,Gauvin, Donna M.,Joshi, Shailen,Turner, Teresa M.,Reilly, Regina M.,Kym, Philip R.,Kort, Michael E.
-
supporting information; experimental part
p. 4821 - 4829
(2010/08/06)
-
- TRPV1 ANTAGONISTS
-
Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
- -
-
Page/Page column 41
(2010/04/30)
-
- TRPV1 ANTAGONISTS
-
Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
- -
-
Page/Page column 39-40
(2010/04/30)
-
- TRPV1 ANTAGONISTS
-
Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV 1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using
- -
-
Page/Page column 12
(2009/05/28)
-
- ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
-
The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
- -
-
Page/Page column 13
(2008/12/06)
-
- ANTAGONISTS OF THE VANILLOID RECEPTOR SUBTYPE 1 (VR1) AND USES THEREOF
-
The present invention is directed to compounds of formula (I) (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.
- -
-
Page/Page column 41
(2008/06/13)
-
- TETRAHYDRO-NAPHTHALENE AND UREA DERIVATIVES
-
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 -
- -
-
-
- TETRAHYDRO-NAPHTHALENE AND UREA DERIVATIVES
-
This invention relates to a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q1a, Q2a, Q3a and Q4a are defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q1b, Q2b, Q3b, Q4b, Q5b, R1b, na, ma, Xa and Ra are defined.
- -
-
Page/Page column 40
(2008/06/13)
-
- Vanilloid receptor (VR) inhibitors for treatment of Human Immunodeficiency Virus (HIV)-mediated pain states
-
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
- -
-
-
- TETRAHYDRO-NAPHTHALENE DERIVATIVES AS VANILLOID RECEPTOR ANTAGONISTS
-
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
- -
-
-
- TETRAHYDRO-NAPHTHALENE DERIVATIVES
-
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
- -
-
-
- HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES
-
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
- -
-
-
- HYDROXY TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES
-
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
- -
-
Page/Page column 46
(2008/06/13)
-