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    • 4. 发明申请
    • 5-ISOQUINOLINESULFONAMIDE DERIVATIVES AS PROTEIN KINASE INHIBITING AGENTS
    • 作为蛋白激酶抑制剂的5-异喹啉衍生物衍生物
    • WO1993013072A1
    • 1993-07-08
    • PCT/EP1992002869
    • 1992-12-11
    • ITALFARMACO S.P.A.LEVI, SilvioGROMO, GianniMAORET, TizianaSALA, Alberto
    • ITALFARMACO S.P.A.
    • C07D217/02
    • C07D217/02
    • 5-isoquinolinesulfonamide derivatives of formula (I) wherein R is the group alpha , where R1 and R2 are independently hydrogen, methyl, ethyl, straight or branched C3-C6 alkyl, benzyl, optionally substituted by at least one substituent selected from the group consisting of C1-C8 alkyl, halogen, hydroxy, C1-C6 alkoxy, nitro, amino, C1-C6 alkylamino di-C1-C6 alkylamino, aliphatic C2-C6 acylamino, C1-C6 carboxyamido, carbonyl, carboxyl, esterified carboxyl, cyano, methylenedioxy, and R3 is straight or branched (C2-C6)alkylene, optionally substituted by benzyl or benzyl substituted by at least one substituent selected from the group consisting of C1-C8 alkyl, halogen, hydroxy, C1-C6 alkoxy, nitro, amino, C1-C6 alkylamino di-C1-C6 alkylamino, aliphatic C2-C6 acylamino, C1-C6 carboxyamido, carbonyl, carboxyl, esterified carboxyl, cyano, methylenedioxy or C5-C8 cycloalkylene; or R is the bivalent residue beta where a and b are independently methylene, ethylene or propylene, optionally substituted by at least one C1-C4 alkyl group; X is an aromatic, partially or totally hydrogenated isoquinoline group, optionally substituted by at least one C1-C4 alkyl group, or the partially or totally hydrogenated naphthyl group and optionally substituted with at least one C1-C4 alkyl group; the salts with pharmaceutically acceptable acids thereof; said derivatives are useful as protein kinases inhibiting agents.
    • 式(I)的5-异喹啉磺酰胺衍生物,其中R是基团α,其中R 1和R 2独立地是氢,甲基,乙基,直链或支链C 3 -C 6烷基,苄基,任选地被至少一个选自以下的取代基 C 1 -C 8烷基,卤素,羟基,C 1 -C 6烷氧基,硝基,氨基,C 1 -C 6烷基氨基二-C 1 -C 6烷基氨基,脂族C 2 -C 6酰氨基,C 1 -C 6羧酰胺基,羰基,羧基,酯化羧基,氰基, 亚甲二氧基,R 3是直链或支链(C 2 -C 6)亚烷基,任选被苄基或被至少一个选自C 1 -C 8烷基,卤素,羟基,C 1 -C 6烷氧基,硝基,氨基 C 1 -C 6烷基氨基二-C 1 -C 6烷基氨基,脂族C 2 -C 6酰氨基,C 1 -C 6羧酰胺基,羰基,羧基,酯化羧基,氰基,亚甲二氧基或C 5 -C 8亚环烷基; 或R是二价残基β,其中a和b独立地是亚甲基,乙烯或丙烯,任选被至少一个C 1 -C 4烷基取代; X是任选被至少一个C 1 -C 4烷基或部分或全部氢化的萘基取代并任选被至少一个C 1 -C 4烷基取代的芳族部分或完全氢化的异喹啉基; 与其药学上可接受的酸的盐; 所述衍生物可用作蛋白激酶抑制剂。