http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2606949-C1

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http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04
filingDate 2015-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2017-01-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3fb9ba9a34cde200a47a28c6290cab22
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8eca59458109bf9236133e6020316b5d
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publicationDate 2017-01-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2606949-C1
titleOfInvention Substituted n-{3-[4-(1-methyl-1h-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides as modulators of egfr, applicable for treating cancer
abstract FIELD: chemistry. n SUBSTANCE: invention relates to novel substituted N-{3-[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}-amides of general formula 1 and pharmaceutically acceptable salts thereof, having properties of modulators of EGFR and suitable for treating cancer, for example small cell lung cancer. In general formula 1 n n n n n R 1 represents CH 2 =C(R 3 )-, R 3 CH=CH-; R 2 is (2-dimethylaminoethyl)-methylamino, 3-dimethylaminopiperidin-1-yl; R 3 is fluorine, trifluoromethyl, dimethylcarbamoyl; or R 2 is 3-dimethylaminopiperidin-1-yl; R 3 is H; or mesylate compound 1, where R 1 is C(CH3)≡C-, R 2 is (2-dimethylaminoethyl)-methylamino. Preferable compounds are N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-fluoro-acrylamide (1.2); N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-4,4,4-trifluorobut-2-enamide (1.6); (E)-3-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenylcarbamoyl}-N,N-dimethylacrylamide (1.8); N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11); mesylate N-{2-[(2-dimethylaminoethyl)-methylamino]-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-2-butynamide (1.14⋅CH 3 SO 3 H) or mesylate N-{2-(3-dimethylaminopiperidin-1-yl)-5-[4-(1-methyl-1H-indol-3-yl)-pyrimidin-2-ylamino]-4-methoxyphenyl}-acrylamide (1.11⋅CH 3 SO 3 H). Invention also relates to a method of producing compounds of formula 1. n EFFECT: method involves reacting a compound of formula 2 or its salt with activated derivative of corresponding organic acid, such as an acid, ester or organic acid anhydride. n 15 cl, 2 tbl, 14 ex
priorityDate 2015-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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