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    • 10. 发明申请
    • FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS
    • 单色运输机荧光底物作为光学神经递质
    • WO2008013997A2
    • 2008-01-31
    • PCT/US2007/017014
    • 2007-07-27
    • THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKGUBERNATOR, Niko, GertSAMES, DaliborSULZER, DavidVADOLA, Paul
    • GUBERNATOR, Niko, GertSAMES, DaliborSULZER, DavidVADOLA, Paul
    • C07D491/14
    • C07D493/16C07D219/06C07D309/30C07D311/16C07D491/16
    • The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ , δ and γ are present, or is a nitrogen and bonds χ , δ and γ are absent; R 1 is -H, -OH, -O-R 7 , -N(H) -R 8 , -N (H) - (CH 2 ) n -NH 2 , -N(R 9 ) (R 10 ), or a piperazine cation; R 2 is either covalently bound to R 9 , or is -H, or is covalently bound to R 3 so as to form a substituted or unsubstituted pyrrole or R 2 is covalently bound to R 9 or R 8 or R 7 ; or R 1 and R 2 are covalently joined to form an aromatic ring; R 3 is either covalently bound to R 2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R 3 is =O; R 4 is, inter alia, -H, -OH, or -R 11 NH 2 ; R 5 is, inter alia, -H, -OH, or -R 12 NH 2 , and R 6 is either is covalently bound to R 10 or is -H, or R 6 is covalently bound to R 10 or R 8 or R 7 . This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
    • 本发明涉及通式结构的化合物:其中Y为O,X为O,不存在键a,键ß存在,或Y为H,X为CH,存在键a,键ß不存在; 原子Z是碳并键合α,d和? 是否存在,或是氮并键合?,d和? 不存在 R 1是-H,-OH,-OR 7,-N(H)-R 8,-N(H) - ( CH 2 N 2,-N(R 9)(R 10) SUB>)或哌嗪阳离子; R 2与R 9共价结合,或者是-H,或者共价键合到R 3,以便形成取代或未取代的 未取代的吡咯或R 2 2共价键合到R 9或R 8或R 7上。 或R 1和R 2 2共价连接形成芳香环; R 3共价结合到R 2上,以便形成吡咯,或者尤其是-H,-OH,烷基或当Z是氮时R 3 = O; 其中R 4尤其是-H,-OH或-R 11 NH 2; 特别地,R 5是-H,-OH或-R 12 NH 2,和R 6 N 2 >与R 10共价结合或为-H,或R 6共价结合R 10或R 8 或者R 7 。 本发明还提供了制备该化合物的方法以及通过使用该化合物来监测单胺转运蛋白的活性或治疗单胺转运蛋白相关疾病的方法。