Showing papers by "Kunzer Aaron R published in 2010"

Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Sulfonamide derivatives as bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases

Abstract: Disclosed are compounds (I) which inhibit the activity of anti-apoptotic Bc1-2 or Bc1 xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti apoptotic Bc1-2 protein.

ortho-Selectivity in SNAr Substitutions of 2,4-Dihaloaromatic Compounds. Reactions with Anionic Nucleophiles.

Abstract: Optimized conditions are developed for an ortho-selective nucleophilic substitution, which avoid the concomitant formation of disubstituted products.

Agents inducing apoptosis for the treatment of cancer and immune and autoimmune diseases

Abstract: A compound or a therapeutically acceptable salt, where the compound is selected from the group consisting of: - Group 1: 4- [4- (3,3-diphenylprop-2-enyl) piperazin-1-yl] -N- [ (3-nitrophenyl) sulfonyl] benzamide N - [(2-bromophenyl) sulfonyl] -4- (4 - {[2- (4-chlorophenyl) cyclohex-1-en-1-yl] methyl} piperazin-1-yl )benzamide; N - [(3-bromophenyl) sulfonyl] -4- (4 - {[2- (4-chlorophenyl) cyclohex-1-en-1-yl] methyl} piperazin-1-yl) benzamide; N - [(4-bromophenyl) sulfonyl] -4- (4 - {[2- (4-chlorophenyl) cyclohex-1-en-1-yl] methyl} piperazin-1-yl) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N- (phenylsulfonyl) benzamide; 2- (benzyloxy) -4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -NN - [(3-nitrophenyl) sulfonyl] -2- (2-phenylethoxy) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] -2-phenoxybenzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl-2-phenoxy-N- (phenylsulfonyl) benzamide; N - [(4-bromophenyl) sulfonyl] -4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} benzamide; 4- [4- (1,1'-Biphenyl-4-ylmethyl) -3-isopropylpiperazin-1-yl] -N- (phenylsulfonyl) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] -2- (phenylthio) benzamide; 2- (benzylamino) -4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] benzamide; 2-benzyl-4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-nitrophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-hydroxyphenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] -2- (2-phenylethyl) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-fluorophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-fluorophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] -2- (phenylsulfinyl) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-nitrophenyl) sulfonyl] -2-phenoxybenzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-fluorophenyl) sulfonyl] -2-phenoxybenzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-fluorophenyl) sulfonyl] -2-phenoxybenzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -2-methoxy-N - [(3-nitrophenyl) sulfonyl] benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-nitrophenyl) sulfonyl] -2- (phenylsulfonyl) benzamide; 4- {4 - [(4'-chloro-1,1'-biphenyl-2-yl) methyl] piperazin-1-yl} -N - [(4-chloro-3-nitrophenyl) sulfonyl] -2-phenoxy -benzamide; 4- [4 - ({4'-chloro-3- [2- (dimethylamino) ethoxy] -1,1'-biphenyl-2-yl} methyl) piperazin-1-yl] -2- (1H-indole- 4-yloxy) -N - [(3-nitrophenyl) -ulfonyl] benzamide; and 4- [4 - ({4'-chloro-3- [2- (dimethylamino) ethoxy] -1,1'-biphenyl-2-yl} methyl) piperazin-1-yl] -2- (1H-indole -4-yloxy) -N- (phenylsulfonyl) -benzamide; and - Group 2: 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -2- (1H-indole- 5-yloxy) -N - [(3-nitrophenyl) -ulfonyl] benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -2- (1H-indole-5-yloxy) - N- (phenylsulfonyl) -benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -N - [(3-cyanophenyl) sulfonyl] -2 - (1H-indole-5-yloxy) benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -N - [(3-chlorophenyl) sulfonyl] -2 - (1H-indole-5-yloxy) benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -N - [(3-fluorophenyl) sulfonyl] -2 - (1H-indole-5-yloxy) benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -2- (1H-indole-5-yloxy) - N- (2-naphthylsulfonyl) -benzamide; 4- (4 - {[2- (4-chlorophenyl) -4,4-dimethylcyclohex-1-en-1-yl] methyl} piperazin-1-yl) -2- (1H-indole-5-yloxy) - N- (isoquinolin-5-ylsulfonyl) benzamide; 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - [(2-chloropyridin-3-yl) sulfonyl] benzamide; 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - [(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl ) sulfonyl] benzamide; 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - [(6-chloro-1,1-dioxide-2H-1,2,4-benzothiadiazin-7 -yl) sulfonyl] -benzamide; 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - ({5- [ethyl (trifluoroacetyl) amino] -1-naphthyl} sulfonyl) benzamide; 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - [(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2 -yl) sulfonyl] -benzamide; and 4- {4 - [(4'-chlorobiphenyl-2-yl) methyl] piperazin-1-yl} -N - [(2-oxo-2H-chromen-6-yl) sulfonyl] benzamide.

(hetero)aryl substituted sulfonyl-2-(1h-pyrrolo[2,3-b]pyridine-5-oxy) benzamide compounds and their use as apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Dérivés de sulfonamide comme agents induisant l'apoptose sélectifs à l'égard de bcl-2 pour le traitement du cancer et de maladies immunes

Abstract: L'invention concerne des composes (I) qui inhibent l'activite des proteines anti-apoptotiques Bcl-2 ou Bcl xL, des compositions contenant ces composes et des methodes de traitement de maladies dans lesquelles la proteine Bcl-2 anti-apoptotique est exprimee.

Agents induisant l'apoptose pour le traitement du cancer et de maladies immunes et auto-immunes

Abstract: L'invention concerne des composes qui inhibent l'activite de proteines Bcl-2 anti-apoptotiques, des compositions contenant ces composes et des methodes de traitement de maladies dans lesquelles la proteine Bcl-2 anti-apoptotique est exprimee.