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    • 2. 发明申请
    • POLYHYDROXYLATED DIBENZ (C,E) AZEPINES AS PROTEIN KINASE C INHIBITORS
    • 作为蛋白激酶C抑制剂的聚甲氧基二苯胺(C,E)
    • WO1993020695A1
    • 1993-10-28
    • PCT/US1993000193
    • 1993-01-11
    • SPHINX PHARMACEUTICALS CORPORATIONJIANG, Jack, B.HUGHES, Philip, F.
    • SPHINX PHARMACEUTICALS CORPORATION
    • A01N43/46
    • C07D223/18
    • The invention provides compounds having formula (I) wherein: R1, R2, R3, R4, R5 and R6, independently, are H, halo, methoxy or hydroxyl, provided that at least one of R1, R2, R3, R4, R5 and R6 is hydroxyl, R7 and R8 are H or taken together form a carbonyl; R12 and R13 are H or taken together form a carbonyl; A is H or CR9R10R11; R9 and R10 are H or taken together form a carbonyl; R11 is H, C1 - C17 alkyl, C1 - C17 alkenyl, C1 - C17 alkynyl, or aryl; and, R14 and R15, independently are H, halo, methoxy or hydroxyl when at least 5 of R1 - R6 are hydroxyl, and H when less than 5 of R1 - R6 are hydroxyl. The compounds are useful for inhibiting protein kinase C, and treating conditions affected by protein kinase C activity, particularly cancer tumors, inflammatory disease, reperfusion injury and cardiac dysfunctions related to reperfusion injury.
    • 本发明提供具有式(I)的化合物,其中:R 1,R 2,R 3,R 4,R 5和R 6独立地是H,卤素,甲氧基或羟基,条件是R 1,R 2,R 3,R 4,R 5和 R6是羟基,R7和R8是H或一起形成羰基; R 12和R 13是H或一起形成羰基; A为H或CR9R10R11; R9和R10是H或一起形成羰基; R 11是H,C 1 -C 17烷基,C 1 -C 17烯基,C 1 -C 17炔基或芳基; 当R 1至R 5中的至少5个为羟基时,R 14和R 15独立地为H,卤素,甲氧基或羟基,当小于5的R 1 -R 6为羟基时,R 14和R 15独立地为H。 这些化合物可用于抑制蛋白激酶C,以及治疗受蛋白激酶C活性,特别是癌症肿瘤,炎性疾病,再灌注损伤和与再灌注损伤相关的心脏功能障碍的影响。
    • 5. 发明申请
    • BIS-(HYDROXYALKYLAMINO)-ANTHRAQUINONE INHIBITORS OF PROTEIN KINASE C
    • 蛋白激酶C(BIS-(羟基喹啉)) - 氨基丁酸酯抑制剂
    • WO1992007557A1
    • 1992-05-14
    • PCT/US1991008026
    • 1991-10-30
    • SPINX PHARMACEUTICALS CORPORATIONJIANG, Jack, B.JOHNSON, Mary, George
    • SPINX PHARMACEUTICALS CORPORATION
    • A61K31/045
    • C07D303/36C07C225/34C07C225/36C07C229/74C07C271/12C07C335/32C07C2603/24
    • 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.
    • 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。