86162-89-2Relevant academic research and scientific papers
TRPV1 vanilloid receptor antagonists with a bicyclic portion
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Page/Page column 23; 33, (2011/11/01)
The invention discloses compounds of formula I wherein Y s selected from a group of formula and W, Q, n, R1, R2, R3, U1-U5 have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1. 1.
Identification of potent, highly constrained CGRP receptor antagonists
Stump, Craig A.,Bell, Ian M.,Bednar, Rodney A.,Fay, John F.,Gallicchio, Steven N.,Hershey, James C.,Jelley, Richard,Kreatsoulas, Constantine,Moore, Eric L.,Mosser, Scott D.,Quigley, Amy G.,Roller, Shane A.,Salvatore, Christopher A.,Sharik, Steven S.,Theberge, Cory R.,Zartman, C. Blair,Kane, Stefanie A.,Graham, Samuel L.,Selnick, Harold G.,Vacca, Joseph P.,Williams, Theresa M.
scheme or table, p. 2572 - 2576 (2010/07/13)
A novel series of potent CGRP receptor antagonists containing a central quinoline ring constraint was identified. The combination of the quinoline constraint with a tricyclic benzimidazolinone left hand fragment produced an analog with picomolar potency (
HETEROCYCLICALLY SUBSTITUTED PENTANOL DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS ANTI-INFLAMMATORY AGENTS
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Page/Page column 88, (2010/02/10)
The invention relates to pentanol derivatives of general formula (I), which are substituted by quinazoline, quinoxaline, cinnoline, indazole, phthalazine, naphthyridine, benzothiazole, dihydroindolone, dihydroisoindolone, benzimidazole, or indole, a method for the production thereof, and the use thereof as anti-inflammatory agents.
1-AMINO-2-OXY-SUBSTITUTED TETRAHYDRONAPHTALENE DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, AND THEIR USE AS ANTIPHLOGISTICS
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Page/Page column 73, (2010/02/11)
The invention relates to polysubstituted tetrahydronaphtalene derivatives of formula (I), to methods for the production thereof, and to their use as antiphlogistics. The substituents are defined in Claim 1.
Synthesis of 2-(2,6-dinitrophenyl)malonates, -acetates and acetonitrile by copper-mediated vicarious nucleophilic substitution
Haglund,Nilsson
, p. 242 - 243 (2007/10/02)
A regioselective, vicarious nucleophilic substitution of 1,3- dinitrobenzene with α-bromo- and iodocarbanions proceeds in the presence of copper(1) tert-butoxide and pyridine giving 2,6-dinitrophenylmalonates, 2,6- dinitrophenylacetates or 2,6-dinitrophenylacetonitrile as the only isomers from bromomalonate esters, bromoacetate esters, iodoacetate esters or iodoacetonitrile, respectively. Without copper(I) tert-butoxide, the 4- substituted isomer is the only product. We believe that the reaction proceeds via a σ-adduct of 1,3-dinitrobenzene and halocarbanion from which hydrogen and halogen are eliminated. This elimination is dependent upon the concentration of copper(I) tert-butoxide.
Ring-Chain Tautomerism in Anions Derived from Substituted (Arylideneamino)toluenes and (Arylideneamino)oxindoles
Goetz, Frederick J.,Hirsch, Jerry A.,Augustine, Robert L.
, p. 2468 - 2472 (2007/10/02)
Intramolecular nucleophilic attack by carbon and nitrogen anions on imine and enone double bonds, respectively, has been investigated as a synthetic route to fused five-membered azacycles.In both (arylideneamino)toluenes and (arylideneamino)oxindoles, cyc
