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1. 发明申请

WO2006026368A3 DEVELOPMENT OF FLUOROGENIC SUBSTRATES FOR MONOAMINE OXIDASES (MAO-A AND MAO-B) 审中-公开
标题翻译：单胺氧化物（MAO-A和MAO-B）的荧光底物的开发
公开(公告)号：WO2006026368A3
公开(公告)日：2006-08-31
申请号：PCT/US2005030276
申请日：2005-08-25
申请人： F NEW YORK THE TRUSTEES OF COL , CHEN GONG , YEE DOMINIC J , GUBERNATOR NIKO , SAMES DALIBOR
发明人： CHEN GONG , YEE DOMINIC J , GUBERNATOR NIKO , SAMES DALIBOR
IPC分类号： A61K31/436 , A61K31/352 , A61K31/404 , C07D311/16 , C07D311/18 , C07D405/04 , C07D491/052 , C07D491/06 , C12Q1/26
CPC分类号： C07D491/04 , C07D311/20
摘要： The present invention relates to compounds useful for detecting the activity of monoamine oxidases, compounds useful for competitively inhibiting monoamine oxidases, for determining inhibitors of monoamine oxidases and compounds useful for treating monoamine oxidase-related nervous system pathologies, as well as pharmaceutical compositions and methods of manufacture thereof.
摘要翻译：本发明涉及可用于检测单胺氧化酶的活性的化合物，用于竞争性抑制单胺氧化酶的化合物，用于确定单胺氧化酶抑制剂的化合物和用于治疗单胺氧化酶相关神经系统病理学的化合物，以及药物组合物和方法制造。

2. 发明申请

WO2008013997A3 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：WO2008013997A3
公开(公告)日：2008-11-27
申请号：PCT/US2007017014
申请日：2007-07-27
申请人： UNIV COLUMBIA , GUBERNATOR NIKO GERT , SAMES DALIBOR , SULZER DAVID , VADOLA PAUL
发明人： GUBERNATOR NIKO GERT , SAMES DALIBOR , SULZER DAVID , VADOLA PAUL
IPC分类号： A61K31/4738 , C07D491/12
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 a is absent and bond ß is present, or Y is H, X is CH, bond a is present, and bond ß is absent; atom Z is a carbon and bonds ?, d and ? are present, or is a nitrogen and bonds ?, d and ? 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 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。

3. 发明申请

WO2006023821A3 LIGANDS FOR ALDOKETOREDUCTASES 审中-公开
标题翻译： ALDOKETOREDUCTASES的配偶
公开(公告)号：WO2006023821A3
公开(公告)日：2009-04-02
申请号：PCT/US2005029722
申请日：2005-08-19
申请人： UNIV COLUMBIA , YEE DOMINIC J , BALSANEK VOJTECH , SAMES DALIBOR
发明人： YEE DOMINIC J , BALSANEK VOJTECH , SAMES DALIBOR
IPC分类号： A61K31/136 , C07C211/58
CPC分类号： A61K31/4745
摘要： The present invention relates to compounds useful for detecting the activity of human aldoketoreductase 1Cs, compounds useful for competitively inhibiting human aldoketoreductase 1Cs and compounds useful for treating human aldoketoreductase 1C-related cancers, as well as pharmaceutical compositions and methods of manufacture thereof.
摘要翻译：本发明涉及可用于检测人醛糖还原酶1C的活性的化合物，可用于竞争性抑制人醛糖还原酶1c的化合物和可用于治疗人醛糖还原酶1C相关癌症的化合物，以及药物组合物及其制备方法。

4. 发明申请

WO2004069394A3 SYNTHETIC METHOD FOR DIRECT ARYLATION OF HETEROCYCLIC ARENES 审中-公开
标题翻译：用于直接聚合芳烃的合成方法
公开(公告)号：WO2004069394A3
公开(公告)日：2005-08-25
申请号：PCT/US2004003215
申请日：2004-02-03
申请人： UNIV COLUMBIA , SAMES DALIBOR , SEZEN BENGU , LANE BENJAMIN S
发明人： SAMES DALIBOR , SEZEN BENGU , LANE BENJAMIN S
IPC分类号： B01F20060101 , C07D207/32 , C07D207/323 , C07D209/04 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/18 , C07D231/12 , C07D233/54 , C07D235/18 , C07D263/32 , C07D263/56 , C07D263/57 , C07D277/20 , C07D277/22 , C07D401/04 , C07D471/04 , C07D473/00
CPC分类号： C07D207/323 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/18 , C07D231/12 , C07D233/56 , C07D235/18 , C07D263/32 , C07D263/57 , C07D277/22 , C07D401/04 , C07D471/04 , C07D473/00
摘要： Methods for the direct, selective arylation of carbon-hydrogen sites on various heteroaromatic compounds are disclosed. A method of the present invention includes contacting the heteroaromatic compound with a basic compound to form a first mixture, adding a second mixture comprising a catalyst to the first mixture to form a third mixture, and adding an Ar-X compound to the third mixture, wherein Ar comprises an aryl species and X comprises a leaving group.
摘要翻译：公开了在各种杂芳族化合物上直接选择性芳基化碳 - 氢位点的方法。本发明的方法包括使杂芳族化合物与碱性化合物接触以形成第一混合物，向第一混合物中加入包含催化剂的第二混合物以形成第三混合物，并向第三混合物中加入Ar-X化合物，其中Ar包含芳基，X包括离去基团。

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