- AMIDE DERIVATIVES
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The invention concerns amide derivatives of Formula (Ia) wherein X is -NHCO- or -CONH-; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group
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- Substituted anilino-quinazoline (or quinoline) compounds and use thereof
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The invention concerns amide derivatives of Formula (I), wherein: G is N or CH; R1is a group such as hydroxy, halo, trifluoromethyl, C1-6alkyl and C1-6alkoxy; each of R2and R3is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy and C3-7cycloalkyl, or R4is of the Formula (IC): —K—J, wherein J is aryl, heteroaryl or heterocyclyl and K is a bond or a group such as oxy and imino, R5is a group such as hydrogen, halo and trifluoromethyl: m is 1-3 and q is 0-4; or pharmaceutically acceptable salts or in vivo cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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- BEZAMIDE DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY CYTOKINES
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The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
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- Amide derivatives useful as inhibitors of the production of cytokines
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The invention concerns amide derivatives of formula (I) wherein R3is (1-6C)alkyl or halogeno; Q1is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as hydroxy, halogeno, trifluoromethyl, (1-6C)alkyl, (1-6C)alkoxy, hydroxy-(1-6C)alkyl, (1-6C)alkoxy-(1-6C)alkyl, hydroxy-(2-6C)alkoxy, amino-(2-6C)alkylamino, N-(1-6C)alkyl-(1-6C)alkylamino-(2-6C)alkylamino, aryl, heteroaryl and heterocyclyl; p is 0-2 and R2is a substituent such as hydroxy and halogeno; q is 0-4; and Q2includes optionally substituted aryl, cycloalkyl, heteroaryl and heterocyclyl; or pharmaceutically-acceptable salts or in vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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- Benzamide derivatives for the treatment of diseases mediated by cytokines
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The invention concerns amide derivatives of Formula (I) wherein: R1and R2include hydroxy, C1-6alkoxy, mercapto, C1-6akylthio, amino and heterocyclyl; m and p are independently 0-3; R3is halo, cyano or C1-6alkoxy; q is 0-4; and R4is aryl or cycloalkyl wherein R4is optionally substituted with up to 3 substituents having any value defined for each R1group; or a pharmaceutically-acceptable salt or in-vivo-cleavable ester thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
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- Amide derivatives for the treatment of diseases mediated by cytokines
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The invention concerns the use of amide derivatives of formula (I) wherein: R1and R2are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3is C1-4alkyl; q is 0-4; and R4is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines
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- Synthesis of meta-substituted aniline derivatives by nucleophilic substitution
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Substitution by amines of fluorobenzenes containing a meta- substituted electron withdrawing group (EWG), in DMSO at 100 °C over 60 h gave meta-substituted aniline derivatives in isolated yields of up to 98%. The scope of the reaction is explored in terms of reaction conditions and substrates. It is postulated that facile meta-substitutions are facilitated through field stabilisation of the intermediate anion by EWG substituents.
- Belfield, Andrew J.,Brown, George R.,Foubister, Alan J.,Ratcliffe, Paul D.
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p. 13285 - 13300
(2007/10/03)
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