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    • 8. 发明授权
    • Biaryl-pyridoquinazolinone derivatives as anti-cancer agents
    • 二芳基吡啶并喹唑啉酮衍生物作为抗癌剂
    • US5914327A
    • 1999-06-22
    • US965552
    • 1997-11-06
    • Michael P. TrovaNan ZhangDouglas B. Kitchen
    • Michael P. TrovaNan ZhangDouglas B. Kitchen
    • C07D471/04A61K31/505A61K31/55
    • C07D471/04
    • This invention provides a compound having the formula: ##STR1## wherein: (A) n=2-4;(B) R.sub.1 and R.sub.2 are the same or different and selected from the group consisting of H, (C.sub.1 -C.sub.3)alkyl, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 NH.sub.2, and --CH.sub.2 CH.sub.2 N(CH.sub.3).sub.2 or R.sub.1 and R.sub.2 are alkyl moieties which may taken together to form a 4- to 7-membered ring;(C) R.sub.3 is selected from H, --CH.sub.3, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 NH.sub.2 ;(D) X is located at the 2-, or 3-position and is selected from the group consisting of 2-naphthyl, 1-naphthyl, 1-phenanthrenyl, 2-phenanthrenyl, 3-phenanthrenyl, 4-phenanthrenyl, 9-phenanthrenyl, phenyl, and mono- or polysubstituted phenyl wherein the substituents are selected from the group consisting of --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3) alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.3 H, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 H, --CO.sub.2 R.sub.4, and phenyl;R.sub.4 is H or (C.sub.1 -C.sub.4)alkyl;R.sub.5 and R.sub.6 are the same or different and are selected from H, or (C.sub.1 -C.sub.4)alkyl, or R.sub.5 and R.sub.6 are alkyl groups which may be taken together to form a 4-7 membered ring;(E) W is selected from H, --OR.sub.4, --NR.sub.5 R.sub.6, (C.sub.1 -C.sub.3)alkyl, --CF.sub.3, F, Cl, Br, I, --NO.sub.2, --CN, --SO.sub.2 NR.sub.5 R.sub.6, --CO.sub.2 R.sub.4 ; or a pharmacologically acceptable salt thereof which is useful as an antineoplastic agent.
    • 本发明提供具有下式的化合物:其中:(A)n = 2-4; (B)R 1和R 2相同或不同,选自H,(C 1 -C 3)烷基,-CH 2 CH 2 OH,-CH 2 CH 2 NH 2和-CH 2 CH 2 N(CH 3)2或R 1和R 2是可以被取代的烷基部分 一起形成4-至7-元环; (C)R 3选自H,-CH 3,-CH 2 CH 3,-CH 2 CH 2 NH 2; (D)X位于2-或3-位,并且选自2-萘基,1-萘基,1-菲基,2-菲基,3-菲基,4-菲基,9-菲基 ,苯基和单取代或多取代的苯基,其中取代基选自-OR4,-NR5R6,(C1-C3)烷基,-CF3,F,Cl,Br,I,-NO2,-CN, SO 3 H,-SO 2 NR 5 R 6,-CO 2 H,-CO 2 R 4和苯基; R4是H或(C1-C4)烷基; R5和R6相同或不同并且选自H或(C1-C4)烷基,或R5和R6是可以一起形成4-7元环的烷基; (E)W选自H,-OR4,-NR5R6,(C1-C3)烷基,-CF3,F,Cl,Br,I,-NO2,-CN,-SO2NR5R6,-CO2R4; 或其药理学上可接受的盐,其可用作抗肿瘤剂。
    • 10. 发明授权
    • Substituted 3-cyano quinolines
    • US6002008A
    • 1999-12-14
    • US49718
    • 1998-03-27
    • Allan WissnerBernard D. JohnsonMarvin F. ReichMiddleton B. Floyd, Jr.Douglas B. KitchenHwei-Ru Tsou
    • Allan WissnerBernard D. JohnsonMarvin F. ReichMiddleton B. Floyd, Jr.Douglas B. KitchenHwei-Ru Tsou
    • C07D215/54C07D215/56C07D401/04C07D401/12C07D409/12A01N43/42C07D215/16C07D215/38
    • C07D401/04C07D215/54C07D215/56C07D401/12C07D409/12
    • This invention provides compounds having the formula: ##STR1## wherein: X is cycloalkyl which may be optionally substituted; or is a pyridinyl, pyrimidinyl, or phenyl ring; wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionally substituted;n is 0-1;Y is --NH--, --O--, --S--, or --NR--;R is alkyl of 1-6 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl, alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl, alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido, hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl, phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino, alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, ##STR2## R.sub.5 is alkyl which may be optionally substituted, or phenyl which may be optionally substituted;R.sub.6 is hydrogen, alkyl, or alkenyl;R.sub.7 is chloro or bromoR.sub.8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl, alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl+, chloro, fluoro, or bromo;Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino, piperazino, N-alkylpiperazino, or pyrrolidino;m=1-4,q=1-3, and p=0-3;any of the substituents R.sub.1, R.sub.2, R.sub.3, or R.sub.4 that are located on contiguous carbon atoms can together be the divalent radical --O--C(R.sub.8).sub.2 --O--;or a pharmaceutically acceptable salt thereof with the proviso that when Y is --NH--, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen, and n is 0, X is not 2-methylphenyl, which are inhibitors of protein tyrosine kinase.