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    • 4. 发明申请
    • HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF
    • 恶唑罗丹明衍生物及其应用
    • WO2002079183A1
    • 2002-10-10
    • PCT/CA2002/000438
    • 2002-03-27
    • THERATECHNOLOGIES INC.HABI, AbdelkrimGRAVEL, DenisVILLENEUVE, LucFORTÉ, Jean-PierreSU, HongshengVAILLANCOURT, Marc
    • HABI, AbdelkrimGRAVEL, DenisVILLENEUVE, LucFORTÉ, Jean-PierreSU, HongshengVAILLANCOURT, Marc
    • C07D311/82
    • C07D311/82
    • Novel compounds of the formula (I) wherein: one of R1, R2, R3, R4, and (R10)n represents an halogen atom and each of the remaining R1, R2, R3, R4, and each of the remaining R10 group is independently selected in the group constituted by hydrogen, halogen atoms, an amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl group and by the corresponding substituted groups; - m = 0 - 1; n = 1-4, A is nil, O, or NH; R9 represents an alkylene group; -Z is H, amino, dialkylamino, or trialkylamino salt; X- is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4in combination with R7 or R8 represents an alkylene, alone or in association with a pharmaceutically acceptable carrier. These compounds, which are usefull as intermediate and as bactericides, as antiviral agent and in the treatment of immunologic disoders.
    • 式(I)的新型化合物其中:R 1,R 2,R 3,R 4和(R 10)中的一个表示卤素原子,剩余的R 1,R 2,R 3,R 4及其余R 10基中的每一个为 在由氢,卤素原子,氨基,酰氨基,二烷基氨基,环烷基氨基,氮杂环烷基,烷基环烷基氨基,芳酰氨基,二芳基氨基,芳基烷基氨基,芳烷基氨基,烷基烷基氨基,芳基芳基氨基,羟基,烷氧基,芳氧基,芳烷氧基,巯基, ,芳烷硫基,羧基,烷氧基羰基,芳氧基羰基,芳烷氧基羰基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,氰基,羟基磺酰基,酰氨基磺酰基,二烷基氨基磺酰基,芳基烷基氨基磺酰基,甲酰基,酰基,芳酰基,烷基,亚烷基,烯基,芳基,芳烷基,乙烯基,炔基 相应的取代基; - m = 0-1; n = 1-4,A为无,O或NH; R9表示亚烷基; -Z是H,氨基,二烷基氨基或三烷基氨基盐; X-是阴离子; R5,R6,R7和R8独立地是H或C1-C6烷基或R1与R5或R6组合,或R2与R5或R6组合,或R3与R7或R8组合,或R4in与R7或R8的组合表示 单独或与药学上可接受的载体结合的亚烷基。 这些化合物可用作中间体和杀菌剂,作为抗病毒剂和治疗免疫学解码器。
    • 5. 发明申请
    • HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF
    • 恶唑罗丹明衍生物及其应用
    • WO02079183A8
    • 2003-02-20
    • PCT/CA0200438
    • 2002-03-27
    • THERATECHNOLOGIES INCHABI ABDELKRIMGRAVEL DENISVILLENEUVE LUCSU HONGSHENGVAILLANCOURT MARC
    • HABI ABDELKRIMGRAVEL DENISVILLENEUVE LUCSU HONGSHENGVAILLANCOURT MARC
    • A61K31/352A61N5/06A61P31/00A61P31/04A61P31/12A61P35/00A61P35/02A61P37/00C07D311/82C07D493/10
    • C07D311/82
    • Novel compounds of the formula (I) wherein: one of R1, R2, R3, R4, and (R10)n represents an halogen atom and each of the remaining R1, R2, R3, R4, and each of the remaining R10 group is independently selected in the group constituted by hydrogen, halogen atoms, an amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl group and by the corresponding substituted groups; - m = 0 - 1; n = 1-4, A is nil, O, or NH; R9 represents an alkylene group; -Z is H, amino, dialkylamino, or trialkylamino salt; X- is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4in combination with R7 or R8 represents an alkylene, alone or in association with a pharmaceutically acceptable carrier. These compounds, which are usefull as intermediate and as bactericides, as antiviral agent and in the treatment of immunologic disoders.
    • 式(I)的新型化合物其中:R 1,R 2,R 3,R 4和(R 10)中的一个表示卤素原子,剩余的R 1,R 2,R 3,R 4及其余R 10基中的每一个为 在由氢,卤素原子,氨基,酰氨基,二烷基氨基,环烷基氨基,氮杂环烷基,烷基环烷基氨基,芳酰氨基,二芳基氨基,芳基烷基氨基,芳烷基氨基,烷基烷基氨基,芳基芳基氨基,羟基,烷氧基,芳氧基,芳烷氧基,巯基, ,芳烷硫基,羧基,烷氧基羰基,芳氧基羰基,芳烷氧基羰基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,氰基,羟基磺酰基,酰氨基磺酰基,二烷基氨基磺酰基,芳基烷基氨基磺酰基,甲酰基,酰基,芳酰基,烷基,亚烷基,烯基,芳基,芳烷基,乙烯基,炔基 相应的取代基; - m = 0-1; n = 1-4,A为无,O或NH; R9表示亚烷基; -Z是H,氨基,二烷基氨基或三烷基氨基盐; X-是阴离子; R5,R6,R7和R8独立地是H或C1-C6烷基或R1与R5或R6组合,或R2与R5或R6组合,或R3与R7或R8组合,或R4in与R7或R8的组合表示 单独或与药学上可接受的载体结合的亚烷基。 这些化合物可用作中间体和杀菌剂,作为抗病毒剂和治疗免疫学解码器。