154257-76-8Relevant articles and documents
5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 76, (2010/11/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6 R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists
Nelson, Derek W.,Gregg, Robert J.,Kort, Michael E.,Perez-Medrano, Arturo,Voight, Eric A.,Wang, Ying,Grayson, George,Namovic, Marian T.,Donnelly-Roberts, Diana L.,Niforatos, Wende,Honore, Prisca,Jarvis, Michael F.,Faltynek, Connie R.,Carroll, William A.
, p. 3659 - 3666 (2007/10/03)
1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X? receptor. Structure-activity relationship (SAR) studies were conducted around both the benzyl and phenyl moieties. In addition, the importance of the regiochemical substitution
Process for the preparation of halogenated benzoic acids
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, (2008/06/13)
A process for the preparation of halogenated benzoic acids of formula (1): STR1 in which R1, R2, R3, R4 and R5 are hydrogen, fluorine, chlorine or bromine atoms or C1 -C6 -alkyl, C1 -C6 -alkoxy, nitro, cyano, trifluoromethyl, aidehyde, C1 -C4 -alkoxycarbonyl, -SO2 -C1 -C4 -alkyl, -SO2 -phenyl, -CONH2, -CON(C1 -C4 -alkyl)2, hydroxy, carboxy, -NH2 or -N(C1 -C4 - alkyl)2 groups, at least one of the substituents R1 -R5 being one of said halogen atoms, which comprises reacting 1 mol of a benzophenone, asymmetrically substituted on the benzene rings A and B, of general formula (2): STR2 in which R1 -R10 are as defined above for R1 -R5, with about 1 to about 10 mol of an oxidizing agent selected from the group comprising hydrogen peroxide, urea/hydrogen peroxide addition product, an alkali metal peroxide, ammonium, alkali metal or alkaline earth metal peroxodisulfates, pertungstates, perborates or percarbonates, ozone, alkyl- or aryl-percarboxylic acids, alkyl- or aryl-persulfonic acids or persulfuric acid, at temperatures from about -20° to about +100° C.