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    • 8. 发明申请
    • 'DELTA'1,2BICYCLO[4,4,0] FUNCTIONAL DYES FOR CONTRAST ENHANCEMENT IN OPTICAL IMAGING
    • DELTA <1,2> BICYCLO [4,4,0]功能对比度增强光学成像
    • WO1997042978A1
    • 1997-11-20
    • PCT/US1997008385
    • 1997-05-09
    • MALLINCKRODT MEDICAL, INC.
    • MALLINCKRODT MEDICAL, INC.FUNG, Ella, Y.RAJAGOPALAN, Raghavan
    • A61K49/00
    • A61K49/0032
    • This invention provides functional dyes of general formula (1) wherein R , R , and R may be the same or different and are selected from the group consisting of hydrogen, C1-C10 alkyl, C1-C10 alkoxyl, hydroxyl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C1-C10 aryl, carboxyl, C1-C10 carboxylalkyl, halogen, nitro, C1-C10 alkoxycarbonyl, mercapto, C1-C10 mercaptoalkyl, C1-C10 alkylthio, sulfonate, and -(CH2)m-N(R )(R ) wherein R and R are independently hydrogen or C1-C10 alkyl, C1-C10 acyl, and R and R are capable of forming 5, 6, or 7 membered rings which may optionally be substituted with -O-, -NR , or -S-; R and R may be the same or different and are selected from the group consisting of C1-C10 alkyl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C1-C10 aryl, C1-C10 carboxylalkyl, C1-C10 alkyl sulfonate, mercaptoalkyl and -(CH2)m-N(R )(R ); W and W may be the same or different and are selected from the group consisting of -S-, -O-, -Se-, -Te-, -NR and C(R )(R ); and m is about 0-10; R is hydrogen, C1-C10 alkyl, C1-C10 alkoxy, C1-C10 mercaptoalkyl, hydroxyl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C1-C10 aryl, C1-C10 carboxylalkyl, C1-C10 alkoxycarbonyl, C1-C10 alkylthio, and -(CH2)m-N(R )(R ); R and R are independently hydrogen, C1-C10 alkyl, C1-C10 alkoxyl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C1-C10 carboxyalkyl, C1-C10 alkoxycarbonyl, and -(CH2)m-N(R )(R ); and A or B may be the same or different and are selected from the group consisting of -(CH2)m, -C(R )(R ), -(CH2)m-N(R )(R ), -O-, -S-, or -NR .
    • 本发明提供通式(1)的功能性染料,其中R 1,R 2和R 5可以相同或不同,并且选自氢,C1-C10烷基,C1- C10烷氧基,羟基,C1-C10羟基烷基,C1-C10烷氧基烷基,C1-C10芳基,羧基,C1-C10羧基烷基,卤素,硝基,C1-C10烷氧基羰基,巯基,C1-C10巯基烷基,C1-C10烷硫基, 和 - (CH 2)m N(R 6)(R 7)(R 7)其中R 6和R 7独立地是氢或C 1 -C 10烷基,C 1 -C 10酰基和R 6, 7>能够形成可以任选被-O-,-NR 8或-S-取代的5,6或7元环; R 3和R 4可以相同或不同,并且选自C1-C10烷基,C1-C10羟基烷基,C1-C10烷氧基烷基,C1-C10芳基,C1-C10羧基烷基,C1- C10烷基磺酸酯,巯基烷基和 - (CH 2)m N(R 6)(R 7); W 1和W 2可以相同或不同,并且选自-S-,-O-,-Se - , - Te-,-NR 8和C(R 9) >)(R <10>); m为约0-10; R 8是氢,C 1 -C 10烷基,C 1 -C 10烷氧基,C 1 -C 10巯基烷基,羟基,C 1 -C 10羟基烷基,C 1 -C 10烷氧基烷基,C 1 -C 10芳基,C 1 -C 10羧烷基,C 1 -C 10烷氧基羰基,C 1 -C 10烷硫基和 - (CH 2)m N(R 6)(R 7); R 9和R 10独立地是氢,C 1 -C 10烷基,C 1 -C 10烷氧基,C 1 -C 10羟基烷基,C 1 -C 10烷氧基烷基,C 1 -C 10羧基烷基,C 1 -C 10烷氧基羰基和 - (CH 2)m N [R <6>)(R <7>); 并且A或B可以相同或不同,并且选自 - (CH 2)m,-C(R 9)(R 10), - (CH 2)m N(R 6) (R 7),-O-,-S-或-NR 8。