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1. 发明申请

WO1992007557A1 BIS-(HYDROXYALKYLAMINO)-ANTHRAQUINONE INHIBITORS OF PROTEIN KINASE C 审中-公开
标题翻译：蛋白激酶C（BIS-（羟基喹啉）） - 氨基丁酸酯抑制剂
公开(公告)号：WO1992007557A1
公开(公告)日：1992-05-14
申请号：PCT/US1991008026
申请日：1991-10-30
申请人： SPINX PHARMACEUTICALS CORPORATION , JIANG, Jack, B. , JOHNSON, Mary, George
发明人： SPINX PHARMACEUTICALS CORPORATION
IPC分类号： A61K31/045
CPC分类号： C07D303/36 , C07C225/34 , C07C225/36 , C07C229/74 , C07C271/12 , C07C335/32 , C07C2603/24
摘要： The present invention provides novel substituted anthraquinones having formula ( alpha ), wherein R1 and R2 are independently H, C1-C10 alkyl, aryl, arylalkyl, alkylaryl, or R1 and R2 taken together with the adjacent nitrogen atom N form a substituted or unsubstituted cyclic ring which may contain additional heteroatoms; n and m are independently 1, 2, or 3; A is halogen, OH, alkoxy, OCO(NR3R4), S-C(NH2)=NR5, or when m = 1, comprises an oxirane ring with the adjacent oxygen atom; R3, R4, and R5 are independently H, alkyl, or aryl; X is H, OH, NR6R7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR8, or CONR9R10; and R6, R7, R8, R9, and R10 are independently H, lower alkyl, or aryl useful 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.
摘要翻译：本发明提供具有式（α）的新的取代的蒽醌，其中R 1和R 2独立地为H，C 1 -C 10烷基，芳基，芳基烷基，烷基芳基或R 1和R 2与相邻的氮原子N一起形成取代或未取代的环状可能含有其他杂原子的环; 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，以及与再灌注损伤相关的心脏功能障碍。

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