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1. 发明申请

US20130190497A1 FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS 审中-公开
标题翻译：单色运输机荧光底物作为光学神经递质
公开(公告)号：US20130190497A1
公开(公告)日：2013-07-25
申请号：US13718832
申请日：2012-12-18
申请人： The Trustees of Columbia University in the City of New York
发明人： Niko Gert GUBERNATOR , Dalibor SAMES , David SULZER , Paul VADOLA
IPC分类号： C07D493/16 , C07D311/16 , C07D219/06 , C07D309/30
CPC分类号： C07D493/16 , C07D219/06 , C07D309/30 , C07D311/16 , C07D491/16
摘要： 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; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. 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.
摘要翻译：本发明涉及通式结构的化合物：其中Y是O，X是O，不存在α键，存在键β，或Y是H，X是CH，存在α键，键β不存在; 原子Z是碳并键合i，δ和γ存在，或是氮和键i，δ和γ不存在; R1是-H，-OH，-O-R7，-N（H）-R8，-N（H） - （CH2）n-NH2，-N（R9）（R10）或哌嗪阳离子; R 2与R 9共价结合或为-H，或与R3共价结合，形成取代或未取代的吡咯，或者R2与R 8或R 8或R 7共价键合; 或R 1和R 2共价连接形成芳香环; R3与R2共价结合形成吡咯，或者尤其是-H，-OH，烷基，或Z为氮时，R3为= O; R4尤其是-H，-OH或-R11NH2; R5尤其是-H，-OH或-R12NH2，R6与R10共价结合或为-H，或R6与R10或R8或R7共价键合。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。

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