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    • 6. 发明授权
    • Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C
    • 蛋白激酶C的双 - (羟烷基氨基) - 蒽醌抑制剂
    • US5204370A
    • 1993-04-20
    • US609252
    • 1990-11-05
    • Jack B. JiangMary G. Johnson
    • Jack B. JiangMary G. Johnson
    • C07C225/34C07C225/36C07D303/36
    • C07C225/36C07C225/34C07D303/36
    • The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.
    • 本发明提供具有下式的新的取代的蒽醌:其中R1和R2独立地为H,C1-C10烷基,芳基,芳基烷基,烷基芳基; n和m独立地为1,2或3; A是卤素,OH,烷氧基,OCO(NR 3 R 4),S-C(NH 2)= NR 5,或当m = 1时,包含具有相邻氧原子的环氧乙烷环; R3,R4和R5独立地是H,烷基或芳基; X是H,OH,NR 6 R 7,Cl,Br,I,F,烷基,芳基,烷氧基,芳氧基,COOR 8或CONR 9 R 10; R 6,R 7,R 8,R 9和R 10独立地为可用于抑制蛋白激酶C的H,低级烷基或芳基,并且治疗与抑制蛋白激酶C特别是癌症肿瘤,炎性疾病,再灌注损伤有关或受其影响的条件 ,以及与再灌注损伤相关的心脏功能障碍。
    • 7. 发明授权
    • Substituted aurone derivatives
    • 取代的鸢尾衍生物
    • US06307070B1
    • 2001-10-23
    • US09122257
    • 1998-07-24
    • Wai-Lam Alex ChuFlemming R. JensenThomas B. JensenJames B. McAlpineBirgitte SøkildeAlexandra M. SantAna-SørensenSunil RatnayakeJack B. JiangCatharine NobleAngela M. Stafford
    • Wai-Lam Alex ChuFlemming R. JensenThomas B. JensenJames B. McAlpineBirgitte SøkildeAlexandra M. SantAna-SørensenSunil RatnayakeJack B. JiangCatharine NobleAngela M. Stafford
    • C07D30783
    • C07D307/82A61K31/343C07D307/83
    • A method for treating a fungal infection is disclosed. The method includes administering to a patient a pharmaceutical composition containing a compound of formula (IA): where each R is independently H, OH, Br, Cl, I, amino, thiol, nitro, C1-4 alkoxy, C1-4 alkenyloxy, C2-6 alkoxyalkyleneoxy, C1-4 alkylthio, C3-18 alkyl, or C3-18 alkenyl; or two adjacent R's, taken together, are a C2-18 bivalent moiety containing at least one oxgen atom, substituted or disubstituted with A or B or both, A being H, OH, Br, Cl, I, amino, or thiol, and B being H, C1-10 alkyl, C2-18 alkenyl, or C6-18 aryl; provided at least two Rs are not H; X is C4-10 alkyl, C4-20 alkenyl, or a C4-20 single, C6-20 bridged, or C6-20 fused ring moiety containing cycloalkyl, cycloalkenyl, aryl, heterocycle, or heteroaryl, where X is substituted with H, OH, Cl, Br, I, amino, cyano, nitro, alkyl, alkoxy, alkenyl, or alkenyloxy; provided that if X is a heteroaryl or heterocyclic moiety where two Rs are each OH and meta to each other, then the remaining R is H and ortho to each of the two hydroxyls, and Y and Z are each O and a ring atom of X is linked directly to the sp2 carbon atom adjacent to X, then substituted with H, OH, Cl, Br, I, amino, cyano, alkyl, alkoxy, alkenyl, or alkenyloxy; and each of Y and Z is independently selected from O, S, and NH; or a pharmaceutically acceptable salt or ester thereof.
    • 公开了一种治疗真菌感染的方法。 该方法包括向患者施用含有式(IA)化合物的药物组合物:其中每个R独立地为H,OH,Br,Cl,I,氨基,硫醇,硝基,C 1-4烷氧基,C 1-4链烯氧基, C 2-6烷氧基亚烷基氧基,C 1-4烷硫基,C 3-8烷基或C 3-8烯基; 或两个相邻的R一起是含有至少一个被A或B或两者取代或二取代的氧原子的C2-18二价部分,A是H,OH,Br,Cl,I,氨基或硫醇,以及 B是H,C 1-10烷基,C 2-8烯基或C 6-18芳基; 提供至少两个R不是H; X是C 4-10烷基,C 4-20链烯基,或含有环烷基,环烯基,芳基,杂环或碳原子的C 4-20单-C6-20桥环或C6-20稠环部分 杂芳基,其中X被H,OH,Cl,Br,I,氨基,氰基,硝基,烷基,烷氧基,烯基或烯氧基取代; 条件是如果X是杂芳基或杂环部分,其中两个R 5各自为OH并且彼此相互间隔,则剩余的R是H和两个羟基中的每一个的邻位,Y和Z各自为O,X为环原子 直接与X相邻的sp2碳原子连接,然后用H,OH,Cl,Br,I,氨基,氰基,烷基,烷氧基,烯基或烯氧基取代; Y和Z各自独立地选自O,S和NH; 或其药学上可接受的盐或酯。