US 8,895,559 B2Granted

Quinoxalines derivatives and pharmaceutical compositions and kits

AssigneeMerck Patent GmbH

InventorsMarkus Klein, Ulrich Emde, Hans-Peter Buchstaller, Christina Esdar, Oliver Poeschke

Life of this patent

Estimating the term…

Abstract

A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.

Claims19

Dependent claims

A compound, which is one of the following compounds

A1 1-Methyl-1H-imidazole-4-sulfonic acid [3-(6-methoxybenzo-1,3-dioxo-4-ylamino)quinoxalin-2-yl] amide;
A2 4-Cyano-N{3-[2(3-dimethylaminopropyl)-3,5-dimethoxyphenylaminol]-quinoxalin-2-yl}benzene sulfonamide;
A3 4-Cyano-N-(3-{2-[3-(1,1-dioxo-1-lambda*6*-thiomorpholin-4-yl)propyl]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A4 1-Methyl-1H-imidazole-4-sulfonic acid (3-{2-[3-(1, 1-dioxo-1-lambda*6*-thiomorpholin-4-yl)propyl]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A5 1-Methyl-1H-imidazole-4-sulfonic acid[3-(2-hydroxymethyl-5-methoxy-2,3-dihydrobenzofuran-7-ylamino)quinoxalin-2-yl] amide;
A6 4-Cyano-N-{3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide;
A7 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A8 4-[3-(7-Methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A9 5-Methoxy-7-[3-(1-methyl- 1H-imidazole-4-sulfonylamino)quinoxalin-2-ylamino]benzofuran-2-carboxylic acid dimethyl amide;
A10 1-Methyl-1H-imidazole-4-sulfonic acid [3-(7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A11 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2,5-dimethoxy-3-methyl-phenylamino)quinoxalin-2-yl] amide;
A12 4-[3-(2,5-Dimethoxy-3-methylphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A13 4-[3-(2-Ethyl-3,5-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A14 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-ethyl-3,5-dimethoxyphenylamino)-quinoxalin-2-yl] amide;
A15 4-[3-(5-Methoxybenzofuran-7-ylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethyl-benzamide;
A16 1-Methyl-1H-imidazole-4-sulfonic acid [3-(5-methoxybenzofuran-7-ylamino)-quinoxalin-2-yl] amide;
A17 1-Methyl-1H-imidazole-4-sulfonic acid [3-(3-ethyl-2,5-dimethoxyphenylamino)-quinoxalin-2-yl] amide;
A18 4-[3-(3-Ethyl-2,5-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A19 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-bromo-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A20 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-chloro-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A21 Pyridine-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A22 Thiazole-5-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A23 1-(2-Dimethylaminoethyl)-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A24 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A25 N-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-methanesulfonamide;
A26 N-{3[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-2-methoxybenzenesulfonamide;
A27 2 -(4 {3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A28 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A29 1-Difluoromethyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A30 N-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide;
A31 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl] amide;
A32 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-2-methylpropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A33 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A34 Ethyl (4-{3[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}phenyl)carbamate;
A35 1,1-Dioxotetrahydro-1-lambda*6*-thiophene-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A36 3-Methanesulfonylpropan-1-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A38 4-Dimethylaminomethyl-N-{3[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A39 C,C,C-Trifluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}methanesulfonamide;
A40 C,C,C-Trifluoro-N-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl]methanesulfonamide;
A41 5-Cyanothiophene-2-sulfonic acid {3-[2-(2-methanesulfonylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A42 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A43 1-Methyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A44 1-Methyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A45 4-Cyano-N{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A46 2-Cyano-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A47 1-Methyl-1H-imidazole-4-sulfonic acid (3-{3,5-dimethoxy-2-[2-(2-methoxy-ethoxy)ethoxy]phenylamino}quinoxalin-2-yl) amide;
A48 4-Cyano-N-(3-{3,5-dimethoxy-2-[2-(2-methoxyethoxy)ethoxy]phenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A49 C,C,C-Trifluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)methanesulfonamide;
A50 N-(4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}phenyl)acetamide;
A51 5-Cyanothiophene-2-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A52 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-methanesulfinylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A53 4-Fluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A54 1-Methyl-1H-imidazole-4-sulfonic acid {3-[3,5-dimethoxy-2-(2-morpholin-4-yl-ethoxy)phenylamino]quinoxalin-2-yl} amide;
A55 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-methanesulfonylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A56 Propane-1-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A57 4-Dimethylaminomethyl-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A58 -N-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A59 5-Cyanothiophene-2-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A60 Thiophene-2-sulfonic acid [3-(2-{2-[(2-hydroxyethyl)methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A61 N-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)-4-methoxybenzenesulfonamide;
A62 N-[4-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-ylsulfamoyl)phenyll]acetamide;
A63 3-Cyano-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A64 Thiophene-2-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxy-phenylamino}quinoxalin-2-yl) amide;
A65 Pyridine-3-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxy-phenylamino}quinoxalin-2-yl) amide;
A66 Thiophene-2-sulfonic acid {3[2-(2-hydroxyethoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A67 Pyridine-3-sulfonic acid (3-{2-[2-(2-hydroxyethanesulfonyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A68 Pyridine-3-sulfonic acid [3-(2-{2-[(2-hydroxyethyl)-methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A69 4 -(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-ylsulfamoyl)-N,N-dimethylbenzamide;
A70 4-Cyano-N-{3-[3,5-dimethoxy-2-(2-morpholin-4-ylethoxy)phenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A71 3,4-Difluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A72 4-Cyano-N-(3-{2-[2-(2-hydroxyethanesulfinyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A73 3,4-Difluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A74 4-Cyano-N-{3-[2-(2,3-dihydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A75 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2,3-dihydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A76 4-Cyano-N-(3-{2-[2-(2-hydroxyethanesulfonyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A77 1 -Methyl-1H-imidazole-4-sulfonic acid (3-{2-[2-(2-hydroxyethanesulfonyl)-ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A78 4-Cyano-N-[3-(2-{2-[(2-hydroxyethyl)methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl]benzenesulfonamide;
A79 Pyridine-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A80 4-Cyano-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A81 1-Methyl-1H-imidazole-4-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A82 4-Cyano-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A83 1-Methyl-1H-imidazole-4-sulfonic acid [3-(5-difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A84 4-Cyano-N-[3-(5-difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-yl]-benzenesulfonamide;
A85 4-[3-(5-Difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A86 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A87 4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A88 4-{3-[2-(2-Hydroxyethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A89 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-hydroxyethoxy)-3,5-dimethoxy-phenylamino]quinoxalin-2-yl} amide;
A90 N,N-Dimethyl-4-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-benzamide;
A91 4-Cyano-N-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl]-benzenesulfonamide;
A92 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)-quinoxalin-2-yl] amide;
A93 N-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-methanesulfonamide;
A94 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A95 4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N-(2,2,2-trifluoroethyl)benzamide;
A96 2-Cyanoethanesulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A97 3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A98 4-(3,3-Difluoroazetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A99 N-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}methanesulfonamide;
A100 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A101 Thiazole-5-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A102 4-(Azetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A103 1-Difluoromethyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A 104
A105 3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N-(2,2,2-trifluoroethyl)benzamide;
A106 4-Aminomethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A107 3-(3,3-Difluoroazetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A108 3-(Azetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A109 3-Dimethylaminomethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A110 4-(3,3-Difluoroazetidin-1-ylmethyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A111 4-Azetidin-1-ylmethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A112 1-Methyl-1H-pyrazole-3-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A113 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2(4-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A114 C,C-Difluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}methanesulfonamide;
A115 C,C-Difluoro-N-{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}-methanesulfonamide;
A116 3-Azetidin-1-ylmethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A117 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A118 2,2-Difluoro-2-(3-{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A119 2,2-Difluoro-2-(3-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A120 2-(3-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A121 1-Methyl-1H-pyrazole-3-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)-quinoxalin-2-yl] amide;
A122 2-(3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A123 2-Diethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-butoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A124 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-hydroxymethyl-7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A125 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxy-3-methylbutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A126 2-Diethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-propoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A127 1-Methyl-1H-imidazole-4-sulfonic acid [3-(3-hydroxymethyl-7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A128 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2(3-hydroxy-3-methylbutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A129 1-(2-Dimethylaminoethyl)-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A130 1-(2-Dimethylaminoethyl)-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A131 N,N-Dimethyl-2-{3-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-pyrazol-1-yl}acetamide;
or
A132 N-(4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}benzyl)acetamide;
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.

130 more elements

Dependencies are inferred from the claim text.

Facts

Application: 13/879,416Filed 22 Sep 2011
Priority: DE 10 2010 048 80020 Oct 2010
Published: US 2013/0217670 A122 Aug 2013
Granted: 25 Nov 2014
Term ends: Not estimatedThe source records don’t support an estimate.

Classification26 codes

C07D 241/44
Benzopyrazines: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or…
A61P 1/18
Drugs for disorders of the alimentary tract or the digestive system: for pancreatic disorders, e.g. pancreatic enzymes
A61P 7/02
Drugs for disorders of the blood or the extracellular fluid: antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/00
Drugs for disorders of the cardiovascular system

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US 2013/0217670 A1Pre-grant publication · published 22 Aug 2013
US 8,895,559 B2This patent

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Abstract

A compound, which is one of the following compounds

A1 1-Methyl-1H-imidazole-4-sulfonic acid [3-(6-methoxybenzo-1,3-dioxo-4-ylamino)quinoxalin-2-yl] amide;
A2 4-Cyano-N{3-[2(3-dimethylaminopropyl)-3,5-dimethoxyphenylaminol]-quinoxalin-2-yl}benzene sulfonamide;
A3 4-Cyano-N-(3-{2-[3-(1,1-dioxo-1-lambda*6*-thiomorpholin-4-yl)propyl]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A4 1-Methyl-1H-imidazole-4-sulfonic acid (3-{2-[3-(1, 1-dioxo-1-lambda*6*-thiomorpholin-4-yl)propyl]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A5 1-Methyl-1H-imidazole-4-sulfonic acid[3-(2-hydroxymethyl-5-methoxy-2,3-dihydrobenzofuran-7-ylamino)quinoxalin-2-yl] amide;
A6 4-Cyano-N-{3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide;
A7 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A8 4-[3-(7-Methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A9 5-Methoxy-7-[3-(1-methyl- 1H-imidazole-4-sulfonylamino)quinoxalin-2-ylamino]benzofuran-2-carboxylic acid dimethyl amide;
A10 1-Methyl-1H-imidazole-4-sulfonic acid [3-(7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A11 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2,5-dimethoxy-3-methyl-phenylamino)quinoxalin-2-yl] amide;
A12 4-[3-(2,5-Dimethoxy-3-methylphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A13 4-[3-(2-Ethyl-3,5-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A14 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-ethyl-3,5-dimethoxyphenylamino)-quinoxalin-2-yl] amide;
A15 4-[3-(5-Methoxybenzofuran-7-ylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethyl-benzamide;
A16 1-Methyl-1H-imidazole-4-sulfonic acid [3-(5-methoxybenzofuran-7-ylamino)-quinoxalin-2-yl] amide;
A17 1-Methyl-1H-imidazole-4-sulfonic acid [3-(3-ethyl-2,5-dimethoxyphenylamino)-quinoxalin-2-yl] amide;
A18 4-[3-(3-Ethyl-2,5-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A19 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-bromo-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A20 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-chloro-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A21 Pyridine-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A22 Thiazole-5-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A23 1-(2-Dimethylaminoethyl)-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A24 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A25 N-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-methanesulfonamide;
A26 N-{3[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-2-methoxybenzenesulfonamide;
A27 2 -(4 {3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A28 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A29 1-Difluoromethyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A30 N-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-benzenesulfonamide;
A31 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl] amide;
A32 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-2-methylpropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A33 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A34 Ethyl (4-{3[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}phenyl)carbamate;
A35 1,1-Dioxotetrahydro-1-lambda*6*-thiophene-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A36 3-Methanesulfonylpropan-1-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A38 4-Dimethylaminomethyl-N-{3[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A39 C,C,C-Trifluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}methanesulfonamide;
A40 C,C,C-Trifluoro-N-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl]methanesulfonamide;
A41 5-Cyanothiophene-2-sulfonic acid {3-[2-(2-methanesulfonylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A42 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A43 1-Methyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A44 1-Methyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A45 4-Cyano-N{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A46 2-Cyano-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A47 1-Methyl-1H-imidazole-4-sulfonic acid (3-{3,5-dimethoxy-2-[2-(2-methoxy-ethoxy)ethoxy]phenylamino}quinoxalin-2-yl) amide;
A48 4-Cyano-N-(3-{3,5-dimethoxy-2-[2-(2-methoxyethoxy)ethoxy]phenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A49 C,C,C-Trifluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)methanesulfonamide;
A50 N-(4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}phenyl)acetamide;
A51 5-Cyanothiophene-2-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A52 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-methanesulfinylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A53 4-Fluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A54 1-Methyl-1H-imidazole-4-sulfonic acid {3-[3,5-dimethoxy-2-(2-morpholin-4-yl-ethoxy)phenylamino]quinoxalin-2-yl} amide;
A55 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-methanesulfonylethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A56 Propane-1-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A57 4-Dimethylaminomethyl-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A58 -N-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A59 5-Cyanothiophene-2-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A60 Thiophene-2-sulfonic acid [3-(2-{2-[(2-hydroxyethyl)methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A61 N-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)-4-methoxybenzenesulfonamide;
A62 N-[4-(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-ylsulfamoyl)phenyll]acetamide;
A63 3-Cyano-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A64 Thiophene-2-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxy-phenylamino}quinoxalin-2-yl) amide;
A65 Pyridine-3-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxy-phenylamino}quinoxalin-2-yl) amide;
A66 Thiophene-2-sulfonic acid {3[2-(2-hydroxyethoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A67 Pyridine-3-sulfonic acid (3-{2-[2-(2-hydroxyethanesulfonyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A68 Pyridine-3-sulfonic acid [3-(2-{2-[(2-hydroxyethyl)-methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A69 4 -(3-{2-[2-(2-Hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-ylsulfamoyl)-N,N-dimethylbenzamide;
A70 4-Cyano-N-{3-[3,5-dimethoxy-2-(2-morpholin-4-ylethoxy)phenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A71 3,4-Difluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A72 4-Cyano-N-(3-{2-[2-(2-hydroxyethanesulfinyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A73 3,4-Difluoro-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A74 4-Cyano-N-{3-[2-(2,3-dihydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A75 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2,3-dihydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A76 4-Cyano-N-(3-{2-[2-(2-hydroxyethanesulfonyl)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl)benzenesulfonamide;
A77 1 -Methyl-1H-imidazole-4-sulfonic acid (3-{2-[2-(2-hydroxyethanesulfonyl)-ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A78 4-Cyano-N-[3-(2-{2-[(2-hydroxyethyl)methylamino]ethoxy}-3,5-dimethoxyphenylamino)quinoxalin-2-yl]benzenesulfonamide;
A79 Pyridine-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A80 4-Cyano-N-(3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}-quinoxalin-2-yl)benzenesulfonamide;
A81 1-Methyl-1H-imidazole-4-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A82 4-Cyano-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A83 1-Methyl-1H-imidazole-4-sulfonic acid [3-(5-difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-yl] amide;
A84 4-Cyano-N-[3-(5-difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-yl]-benzenesulfonamide;
A85 4-[3-(5-Difluoromethoxy-2,3-dimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-N,N-dimethylbenzamide;
A86 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A87 4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A88 4-{3-[2-(2-Hydroxyethoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A89 1-Methyl-1H-imidazole-4-sulfonic acid {3-[2-(2-hydroxyethoxy)-3,5-dimethoxy-phenylamino]quinoxalin-2-yl} amide;
A90 N,N-Dimethyl-4-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-benzamide;
A91 4-Cyano-N-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-yl]-benzenesulfonamide;
A92 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)-quinoxalin-2-yl] amide;
A93 N-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}-methanesulfonamide;
A94 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A95 4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N-(2,2,2-trifluoroethyl)benzamide;
A96 2-Cyanoethanesulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A97 3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N,N-dimethylbenzamide;
A98 4-(3,3-Difluoroazetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A99 N-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}methanesulfonamide;
A100 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A101 Thiazole-5-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl} amide;
A102 4-(Azetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A103 1-Difluoromethyl-1H-pyrazole-4-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A 104
A105 3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}-N-(2,2,2-trifluoroethyl)benzamide;
A106 4-Aminomethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}benzenesulfonamide;
A107 3-(3,3-Difluoroazetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A108 3-(Azetidine-1-carbonyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A109 3-Dimethylaminomethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A110 4-(3,3-Difluoroazetidin-1-ylmethyl)-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A111 4-Azetidin-1-ylmethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A112 1-Methyl-1H-pyrazole-3-sulfonic acid (3-{2-[2-(2-hydroxyethoxy)ethoxy]-3,5-dimethoxyphenylamino}quinoxalin-2-yl) amide;
A113 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2(4-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A114 C,C-Difluoro-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}methanesulfonamide;
A115 C,C-Difluoro-N-{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-yl}-methanesulfonamide;
A116 3-Azetidin-1-ylmethyl-N-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl}benzenesulfonamide;
A117 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(4-hydroxybutyl)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A118 2,2-Difluoro-2-(3-{3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A119 2,2-Difluoro-2-(3-{3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]-quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A120 2-(3-{3-[2-(3-Hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A121 1-Methyl-1H-pyrazole-3-sulfonic acid [3-(2,3,5-trimethoxyphenylamino)-quinoxalin-2-yl] amide;
A122 2-(3-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}pyrazol-1-yl)-N,N-dimethylacetamide;
A123 2-Diethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-butoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A124 1-Methyl-1H-imidazole-4-sulfonic acid [3-(2-hydroxymethyl-7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A125 1-Methyl-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxy-3-methylbutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A126 2-Diethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2-(3-hydroxy-propoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A127 1-Methyl-1H-imidazole-4-sulfonic acid [3-(3-hydroxymethyl-7-methoxy-2,3-dihydrobenzo-1,4-dioxin-5-ylamino)quinoxalin-2-yl] amide;
A128 2-Dimethylaminomethyl-1-methyl-1H-imidazole-4-sulfonic acid {3-[2(3-hydroxy-3-methylbutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A129 1-(2-Dimethylaminoethyl)-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxybutoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A130 1-(2-Dimethylaminoethyl)-1H-pyrazole-3-sulfonic acid {3-[2-(3-hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-yl} amide;
A131 N,N-Dimethyl-2-{3-[3-(2,3,5-trimethoxyphenylamino)quinoxalin-2-ylsulfamoyl]-pyrazol-1-yl}acetamide;
or
A132 N-(4-{3-[2-(3-Hydroxypropoxy)-3,5-dimethoxyphenylamino]quinoxalin-2-ylsulfamoyl}benzyl)acetamide;
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.

130 more elements

Facts

Application

13/879,416Filed 22 Sep 2011

Priority

DE 10 2010 048 80020 Oct 2010

Published

US 2013/0217670 A122 Aug 2013

Granted

25 Nov 2014

Term ends

Not estimatedThe source records don’t support an estimate.

Classification26 codes

C07D 241/44
Benzopyrazines: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or…
A61P 1/18
Drugs for disorders of the alimentary tract or the digestive system: for pancreatic disorders, e.g. pancreatic enzymes
A61P 7/02
Drugs for disorders of the blood or the extracellular fluid: antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
A61P 9/00
Drugs for disorders of the cardiovascular system