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1. 发明申请

WO2017049158A1 CARBOXYLIC DIARYLTHIAZEPINEAMINES AS MU-OPIOID RECEPTOR AGONISTS 审中-公开
标题翻译：羧甲基二胺嘧啶胺作为MU-OPIOID受体激动剂
公开(公告)号：WO2017049158A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/052250
申请日：2016-09-16
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , KRUEGEL, Andrew , SAMES, Dalibor , GASSAWAY, Madalee , JAVITCH, Jonathan, A.
发明人： KRUEGEL, Andrew , SAMES, Dalibor , GASSAWAY, Madalee , JAVITCH, Jonathan, A.
IPC分类号： A61K31/135 , A61K31/137 , A61K31/554 , C07D281/12 , C07D281/16 , C07D285/00
CPC分类号： A61K31/135 , A61K31/137 , A61K31/554 , C07D281/02
摘要： The present invention provides a compound having the structure of the instant invention or a pharmaceutically acceptable salt or ester thereof, methods of preparing the same, and methods of treating a subject with compounds of the instant invention in combination therapies.
摘要翻译：本发明提供具有本发明结构的化合物或其药学上可接受的盐或酯，其制备方法以及用本发明化合物在组合疗法中治疗受试者的方法。

2. 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。

3. 发明申请

WO2016086158A1 OPIOID RECEPTOR MODULATORS 审中-公开
标题翻译：阿片受体调节剂
公开(公告)号：WO2016086158A1
公开(公告)日：2016-06-02
申请号：PCT/US2015/062726
申请日：2015-11-25
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , KRUEGEL, Andrew, C. , GASSAWAY, Madalee, M. , JAVITCH, Jonathan, A. , SAMES, Dalibor
发明人： KRUEGEL, Andrew, C. , GASSAWAY, Madalee, M. , JAVITCH, Jonathan, A. , SAMES, Dalibor
IPC分类号： C07D491/18
CPC分类号： C07D491/18 , A61K9/0002 , A61K9/0073 , A61K9/7092 , A61K31/485 , A61K47/38 , A61P25/04 , A61P25/24 , C07D471/18 , C07D495/18
摘要： The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, 0, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.
摘要翻译：本发明提供具有以下结构的化合物，其中A是具有或不具有取代的环结构; X1是C或N; X2为N，0或S; Y1是H， - （烷基）， - （烯基）， - （炔基）， - （环烷基），（卤代烷基）， - （烷基）-O-（烷基）或 - （烷基） - （环烷基） Y 2是H， - （烷基）， - （烯基）， - （炔基）， - （环烷基），（卤代烷基）， - （烷基）-O-（烷基）或 - （烷基） - （环烷基） Y 3是H， - （烷基）， - （烯基）， - （炔基）， - （环烷基），（卤代烷基）， - （烷基）-O-（烷基）或 - （烷基） - Y 4是H， - （烷基）， - （烯基）， - （炔基）， - （环烷基），（卤代烷基）， - （烷基）-O-（烷基）或 - （烷基） - （环烷基） Y5是H， - （烷基）， - （烯基）， - （炔基）， - （环烷基），（卤代烷基）， - （烷基）-O-（烷基）或 - （烷基） - （环烷基） a和P各自存在或不存在，并且当存在时，每个都是键。

4. 发明申请

WO2015138791A1 A NEW CLASS OF MU-OPIOID RECEPTOR AGONISTS 审中-公开
标题翻译：一类新的MU-OPIOID受体激动剂
公开(公告)号：WO2015138791A1
公开(公告)日：2015-09-17
申请号：PCT/US2015/020273
申请日：2015-03-12
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , KRUEGEL, Andrew C. , HENKE, Adam , GASSAWAY, Madalee M. , RIVERS, Marie-laure , JAVITCH, Jonathan A. , SAMES, Dalibor
发明人： KRUEGEL, Andrew C. , HENKE, Adam , GASSAWAY, Madalee M. , RIVERS, Marie-laure , JAVITCH, Jonathan A. , SAMES, Dalibor
IPC分类号： A61K31/554 , C07D281/02
CPC分类号： C07D281/02 , A61K31/554 , A61K45/06 , C07D417/12 , C07D513/04 , A61K2300/00
摘要： The present invention provides a compound having the structure (I) or a pharmaceutically acceptable salt or ester thereof.
摘要翻译：本发明提供具有结构（I）的化合物或其药学上可接受的盐或酯。

5. 发明申请

WO2010025272A1 COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND TREATING OR PREVENTING DISEASES 审中-公开
标题翻译：用于减少毒性和治疗或预防疾病的化合物，组合物和方法
公开(公告)号：WO2010025272A1
公开(公告)日：2010-03-04
申请号：PCT/US2009/055221
申请日：2009-08-27
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , CHOU, Ting-Chao , LEI, Xiaoguang , YUN, Heedong , NG, Fay , HARTUNG, John , SAMES, Dalibor
发明人： DANISHEFSKY, Samuel, J. , CHOU, Ting-Chao , LEI, Xiaoguang , YUN, Heedong , NG, Fay , HARTUNG, John , SAMES, Dalibor
IPC分类号： A61K31/34
CPC分类号： C07C33/048 , A61K31/047 , A61K31/075 , A61K31/165 , A61K31/196 , A61K31/337 , A61K31/343 , A61K31/357 , A61K31/4192 , A61K31/427 , A61K31/661 , A61K31/675 , A61K31/7048 , A61K45/06 , C07B2200/07 , C07C33/05 , C07C33/14 , C07C33/30 , C07C43/315 , C07C49/24 , C07C2601/02 , C07C2601/14 , C07D249/04 , C07D317/16 , C07D317/18 , C07D317/20 , C07D317/22 , C07D317/24 , C07D317/26 , C07D317/28 , C07D317/30 , A61K2300/00
摘要： The present invention provides compounds of Formula (I), compositions comprising an effective amount of a Compound of Formula (I), optionally with chemotherapeutic drug, such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, for example chemotherapy agents, treating or preventing cancer or a neurotrophic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making Compounds of Formula (I).
摘要翻译：本发明提供式（I）化合物，包含有效量的式（I）化合物，任选地与化学治疗药物如微管蛋白结合药物组合的组合物，及其用于降低细胞毒性剂毒性的方法，例如化疗剂，治疗或预防癌症或神经营养障碍，诱导化学保护性II期酶，DNA或蛋白质合成，增强免疫系统，治疗炎症，改善和增强一般健康或健康，以及制备方法式（I）的化合物。

6. 发明申请

WO2009097144A1 MOLECULAR PROBES FOR PET-IMAGING OF DOPAMINE NEUROTRANSMISSION AND NEUROENDOCRINE PROCESSES IN VIVO 审中-公开
标题翻译：多巴胺神经递质和血管内皮细胞过程中PET成像的分子探针
公开(公告)号：WO2009097144A1
公开(公告)日：2009-08-06
申请号：PCT/US2009/000630
申请日：2009-01-30
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , SAMES, Dalibor , GUBERNATOR, Niko , VADOLA, Paul , HU, Gang , SULZER, David , SLIFSTEIN, Mark , ABI-DARGHAM, Anissa , LEUNG, David
发明人： SAMES, Dalibor , GUBERNATOR, Niko , VADOLA, Paul , HU, Gang , SULZER, David , SLIFSTEIN, Mark , ABI-DARGHAM, Anissa , LEUNG, David
IPC分类号： A61K31/54 , A61K31/535 , A61K31/497
CPC分类号： C07D491/052 , C07B59/002 , C07D311/16
摘要： The present invention relates to compounds of the general structure (I), wherein Y is O, X is O, bond alpha is absent and bond beta is present, or, Y is H, X is CH, bond alpha is present, and bond beta is is absent, atom Z is a carbon and bonds X, delta and gamma are present, or atom Z is a nitrogen and bonds X, delta and gamma are absent, or atom Z is a nitrogen and bonds X and delta are present and gamma is absent R1, R2, R3, R4, R5 and R6 are various subtitutents as described in the specification.
摘要翻译：本发明涉及通式（I）的化合物，其中Y为O，X为O，不存在α键且存在键β，或Y为H，X为CH，键α为键， β是不存在的，原子Z是碳并且键X，δ和γ存在，或者原子Z是氮并且键X，δ和γ不存在，或者原子Z是氮并键合X和δ存在， γ不存在R1，R2，R3，R4，R5和R6是说明书中所述的各种残基。

7. 发明申请

WO2022178099A1 OXA-IBOGAINE ANALOGUES FOR TREATMENT OF SUBSTANCE USE DISORDERS 审中-公开
公开(公告)号：WO2022178099A1
公开(公告)日：2022-08-25
申请号：PCT/US2022/016757
申请日：2022-02-17
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , HIGH POINT UNIVERSITY , SAMES, Dalibor , HEMBY, Scott , HAVEL, Vaclav
发明人： SAMES, Dalibor , HEMBY, Scott , HAVEL, Vaclav
IPC分类号： A61K31/407 , A61K31/55 , C07D491/04 , A61P25/00
摘要： The present invention provides a method of treating a subject afflicted with a substance use disorder (SUD) comprising administering to the subject an effective amount of a compound having the structure: [STRUCTURE], or a pharmaceutically acceptable salt or ester thereof, wherein A, X1, X2, Y1-Y6 and R1-R4 are as defined in the specification, so as to thereby treat the subject afflicted with the substance use disorder (SUD).

8. 发明申请

WO2022020352A1 IBOGAINE ANALOGS AS THERAPEUTICS FOR NEUROLOGICAL AND PSYCHIATRIC DISORDERS 审中-公开
公开(公告)号：WO2022020352A1
公开(公告)日：2022-01-27
申请号：PCT/US2021/042370
申请日：2021-07-20
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , SAMES, Dalibor , HAVEL, Vaclav , HWU, Christopher
发明人： SAMES, Dalibor , HAVEL, Vaclav , HWU, Christopher
IPC分类号： C07D401/14 , C07D471/04
摘要： The present invention provides a compound having the structure: formula wherein X1 is H or alkyl; Y1 is H, -alkyl, -alkenyl, -alkynyl, alkylaryl, -cycloalkyl, - aryl, heteroaryl, -alkyl-Y3 or -alkyl-C(O)Y4, and Y2 is H, -alkyl, -alkenyl, -alkynyl, alkylaryl, -cycloalkyl, - aryl, heteroaryl, -alkyl-Yg or -alkyl-C(O)Y4, wherein each Y3 is, independently, -OH, -O(alkyl), -NH2, - NH(alkyl) or halogen, and each Y4 is, independently, -OH, -O(alkyl), -NH2, -NH(alkyl) or -N(alkyl)2; Z1 is H, -alkyl, -alkenyl, -alkynyl, alkylaryl, -aryl, heteroaryl, -alkyl-Zg or -alkyl-C(O)Z4, and Z2 is H, -alkyl, -alkenyl, -alkynyl, alkylaryl, -aryl, heteroaryl, -alkyl-Zg or -alkyl-C(O)Z4, wherein each Z3 is, independently, -OH, -O(alkyl), -NH2, - NH(alkyl) or halogen, and each Z4 is, independently, -OH, -O(alkyl), -NH2, -NH(alkyl) or -N(alkyl)2; R1, R2, R3 and R4 are each, independently, -H, -F, -Cl, -Br, -I, -NO2, -CN, -CF3, -CF2H, -OCF3, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -OH, -OAc, -O-(alkyl), -O-(alkenyl), - O-(alkynyl), -O-(aryl), -O-(heteroaryl), -SH, -S-(alkyl), S (alkenyl), -S-(alkynyl), -S-(aryl), -S-(heteroaryl), -NH2, -NH- (alkyl), -NH-(alkenyl), -NH-(alkynyl), -NH-(aryl), -NH- (heteroaryl), -C(0)R5, -S(O)R5, -SO2R5, -NHSO2R5, -0C(0)R5, SC(0)R5, -NHC(O)R6 or -NHC(S)R6, wherein each R5 is, independently, -(alkyl), -(aryl), (heteroaryl), -OH, -O(alkyl), -NH2, -NH(alkyl) or N(alkyl)2, and wherein each R6 is, independently, -(alkyl), -(aryl), -O- (alkyl), -S-(alkyl), -S-(aryl), -NH2, -NH(alkyl) or N(alkyl)2, wherein the compound is other than any of ibogaine, ibogamine, N- methyl-ibogaine, N-methyl-noribogaine, N-ethyl-noribogaine, N-methyl- ibogamine or 10-ethoxy-ibogamine, or a pharmaceutically acceptable salt of the compound, and methods of using the composition to treat pain, depressive disorders, mood disorders, anxiety disorders, substance use disorders, opioid use disorders, and opioid withdrawal symptoms.

9. 发明申请

WO2020037136A1 MITRAGYNINE ANALOGS FOR THE TREATMENT OF PAIN, MOOD DISORDERS AND SUBSTANCE USE DISORDERS 审中-公开
公开(公告)号：WO2020037136A1
公开(公告)日：2020-02-20
申请号：PCT/US2019/046677
申请日：2019-08-15
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , THE RESEARCH FOUNDATION FOR MENTAL HYGIENE, INC. , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , KRUEGEL, Andrew, C. , SAMES, Dalibor , BHOWMIK, Srijita , HAVEL, Václav , JAVITCH, Jonathan, A. , MAJUMDAR, Susruta , GALETA, Juraj
发明人： KRUEGEL, Andrew, C. , SAMES, Dalibor , BHOWMIK, Srijita , HAVEL, Václav , JAVITCH, Jonathan, A. , MAJUMDAR, Susruta , GALETA, Juraj
IPC分类号： A61K31/437 , A61P25/04 , C07D471/04
摘要： The present invention provides a compound having the structure (I): or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.

10. 发明申请

WO2022170268A1 OXA-IBOGAINE INSPIRED ANALOGUES FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS 审中-公开
公开(公告)号：WO2022170268A1
公开(公告)日：2022-08-11
申请号：PCT/US2022/015681
申请日：2022-02-08
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , SAMES, Dalibor , HAVEL, Vaclav , BECHAND, Benjamin , LANKRI, David
发明人： SAMES, Dalibor , HAVEL, Vaclav , BECHAND, Benjamin , LANKRI, David
IPC分类号： A61K31/407 , A61K31/55 , C07D491/04 , A61P25/00
摘要： The present invention provides a compound having the structure: [STRUCTURE}, wherein D,E,F,X1, X2 and R1-R14 are as defined herein; a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier; and a method of treating a subject afflicted with a substance use disorder, opioid withdrawal symptoms, a depressive disorder, a mood disorder, an anxiety disorder, Parkinson's disease, traumatic brain injury, a headache, a migraine, or of altering the psychological state or enhancing the effect of psychotherapy, comprising administering to the subject an effective amount of said compound or a pharmaceutically acceptable salt thereof.

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