RS54882B1 - Derivati piramidina kao fak inhibitori - Google Patents

Derivati piramidina kao fak inhibitori

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Publication number
RS54882B1
RS54882B1 RS20160420A RSP20160420A RS54882B1 RS 54882 B1 RS54882 B1 RS 54882B1 RS 20160420 A RS20160420 A RS 20160420A RS P20160420 A RSP20160420 A RS P20160420A RS 54882 B1 RS54882 B1 RS 54882B1
Authority
RS
Serbia
Prior art keywords
pyrimidin
ethyl
ylamino
phenyl
methyl
Prior art date
Application number
RS20160420A
Other languages
English (en)
Inventor
Timo Heinrich
Christina Esdar
Hartmut Greiner
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of RS54882B1 publication Critical patent/RS54882B1/sr

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Abstract

Jedinjenja izabrane iz grupe,,A1" N-(2-{2-[2-(4-Metansulfonil-fenilamino)-pirimidin-4-il]-etil}-fenil-N-rnetil-metansulfonamid,,A2" N-Metil-N-(2-{2-[2-(2-okso-1,2,3,4-tetrahidro-hinolin-6-ilamino)-pirimidin-4-il]-etil}-fenil-N-metansulfonamid,,A3" 6-{4-[2-(3-Metan sulfonil-fenil)-etil]-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on,,A4" (4-metansulfonil-fenil)-{4-[2-(3-metansulfonil-fenil)-etil]-pirimidin-2-il)-amin,,A5" N-Metil-N-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A6" N-Metil-N-(3-(2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid,,A7" N-Metil-N-(3-{2-[2-(2-okso-1,2,3,4-tetrahidro-hinolin-6-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid,,A8" N-(3-{2-[2-(4-metansulfonil-fenilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metilmetansulfonamid,,A9" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-acetonitril,,A10" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-acetamid,,A11" (4-Fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il}-fenil)-acetonitril„A12" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5 -ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-formamid,,A13" 1-(2{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril..A14" N- '2 (3-{2-[2-(2-okso-2,3-dihidro-1 H-indol 5- ilamino)-pirimidin-4-il]-etil}-piridin-2-ilamino)-formamid,,A15" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)-acetonitril,,A16" 3-(3-{2-(2okso-2.3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2 il)-azetidin-3-karbonitril,,A17" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)-acetonitril,,A18" (5-Fluor-2-{2-[2-(2-okso-2,3-dihidro-1 H-indol-5- ilamino)-pirimidin-4-il]-etil}-fenil)-acetonitril,,A19" 1-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-4- trifluorometil-fenil)-ciklobutankarbonitril,,A20" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-benzoksazol-6-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metanesulfonamidA21" N-Metil-N-(3-{2-[2-(1-metil-2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metanesulfonamid,,A22" N-(3-{2-[2-(3-cijan-fenilamino)-pirimidin-4-il]-etil}-piridin-2-il)-N-metil-metansulfonamid,,A24" N-Metil-N-[3-(2-{2-[(6-okso-1,6-dihidro-piradizin-3-ilmetil)-amino]-pirimidin-4-il}-piridin-2-il]-metansulfonamid,,A25" N-(3-{2-[2-(1,3-dimetil-2-okso-2,3-diidro-1-H-benzimidazol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-N-metil-metansulfonamid,,A26" N-(3-{[5-cijan-2-(2-okso-2,3-dihidro-benzoksazol-6-ilamino)-pirimidin-4-ilamino]-metil}-piridin-2-il)-N-metil-metansulfonamid,,A27" N-Metil-N-(2-{2-[(2-okso-2,3-dihidro-benzoksazo-6-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A28" N-(2-{2-[2-(3-cijan-fenilamino)-pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A29" N-(2-{2-[2-(3-cijan-4-fluor-fenilamino)-pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A30" N-Metil-N-(2-{2-[(2-okso-2,3-dihidro-benzotiazol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A31" N-(2-{2-(1-Acetil-2,3-dihidro-1H-indol-5-ilamino)- pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A32" 2-[3-(4-{2-[2-(Metansulfonil-metil-amino)-fenil]-etil}-pirimidin-2-ilamino)-fenil]-N-metil-acetamid,,A33" N-Metil-N-[2-(2-{2-[4-(3-okso-morfoln-4-il)-fenilamino]-pirimidin-4-il}-etil)-fenil)-metansulfonamid,,A34" N-[4-(4-{2-[2-(Metansulfonil-metil-amino)-fenil]-etil}-pirimidin-2-ilamino)-fenil]-nikotinamid,,A35" N-Metil-N-[2-(2-{2-[4-(2-okso-pirolidin-1-il)-fenilamino-]-pirimidin-4-il}-etil]-metansulfonamid,,A36" N-[2-(2-{2-[3,5-dihlor-4-(2-okso-pirolidin-1-il)-fenilamino]-pirimidin-4-il}-etil]-fenil]-N-metil-metansulfonamid,,A37" N-[2-(2-{2-[3-cijan-4-(2-okso-piperidin-1-il)-fenilamino]-pirimidin-4-il}-etil]-fenil]-N-metil-metansulfonamid,,A38" N-[2-(2-{2-[4-(1,3-diokso-1,3-dihidro-izoindol-2-il)- fenilamino]-pirimidin-4-N}-etil]-fenil]-N-metil-metansulfonamid,,A39" N-Metil-N-[3-(2-{2-[4-(2-okso-pirolidin-1-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-metansulfonamid,,A40" N-[4-(4-{2-[2-(Metansulfonil-metil-amino)-piridin-3-il]-etil}-pirimidin-2-ilamino)-fenil]-nikotinamid,A41" N-Metil-N-[3-(2-{2-[4-(2-okso-morfolin-4-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-metansuifonamid,A42" N-[3-(2-{2-[3-cijan-4-(2-okso-piperidin-1-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-N-metil-metansulfonamid,,A43" N-[3-(2-{2-[4-(1,3-diokso-1,3-dihidro-izoindol-2-il) fenilamino]-pirimidin-4-il}-etil)-piridin-2-il)-N-metil-metansulfonamid,,A44" N-Metil-N-(5-metil-3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid 1-(4-fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril,,A46" 1-(5-fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril,,A47" 1-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)- ciklobutankarbonitril,,A48" (5-Fluor-4-fenetil-pirimidin-2-il)-fenil-amin,,A49" (5-Metil-4-fenetil-pirimidin-2-il)-fenil-amin,,A50" (5-fenetil-5-trifluormetil-pirimidin-2-il)-fenil-amin,,A52" (5-Brom-4-fenetil-pirimidin-2-il)-fenil-amin,,A56" 6-{5-Fluor-4-[2-(4-fluor-fenil)-etil]-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on,,A65" 6-{4-[2-(4-fluor-fenil)-etil]-5-metil-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on,,A71" [5-(1-Metil-1H-pirazol-4-il)-4-fenetil-pirimidin-2-il]-fenil-amin,,A74" [5-{4-[2-(4-Fluor-fenil)-etil]-5-trifluormetil-pirimidin-2-ilamino}-1,3-dihidro-indol-2-on,,A77" 6-{4-[2-(4-Fluor-fenil)-etil]-5-trifluormetil-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on„A101" 6-(5-Brom-4-fenetil-pirimidin-2-ilamino(-3,4-dihidro-1H-hinolin-2-on„A102" 5-(4-fenetil-5-trifluormetil-pirimidin-2-ilamino)-1,3-dihidro-indol-2-on„A103" 6-(4-fenetil-5-trifluormetil-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A104" 6-(5-metii-4-{2-[3-(propan-1-sulfonil)-fenil]-etil}-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A105" 6-(5-Fluor-4-{2-[3-(propan-1-sulfonil)-fenil]-etil}-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A106" [6-(4-terc.-Butil-fenoksi)-piridin-3-il]-(5-fluor-4-fenetil-pirimidin-2-il)-amin„A107" (5-Fluor-4-fenetil-pirimidin-2-il)-(6-trifluormetil-piridin-3-il)-amin„A108" (5-Fluor-4-fenetil-pirimidin-2-il)-(6-fluor-piridin-3-il)-amin„A109" 5-(5-Fluor-4-fenetil-pirimidin-2-ilamino)-piridin-2-karbonitril„A110" N-[5-(5-Fluor-fenetil-pirimidin-2-ilamino)-piridin-2-il]-acetamid„A111" N-Metil-N-(2-{2-[2-(2-okso-2,3 dihidro-1H-indol-5-ilamino)-5-trifluormetil-pirimidin-4-il]etil)-fenil)-metansulfonamidkao i farmaceutski primenjene soli, tautomera i stereoizomera, uključujući njihove smese u svim odnosima.Prijava sadrži još 2 patentna zahteva.
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