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1. 发明申请

WO2008124703A2 DEVELOPMENT OF MOLECULAR IMAGING PROBES FOR CARBONIC ANHYDRASE-IX USING CLICK CHEMISTRY 审中-公开
标题翻译：使用单一化学物质开发碳氢化合物IX的分子成像探针
公开(公告)号：WO2008124703A2
公开(公告)日：2008-10-16
申请号：PCT/US2008/059599
申请日：2008-04-07
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth C , WALSH, Joseph C. , KASI, Dhanalakshmi , MOCHARLA, Vani , WANG, Bing , GANGADHARMATH, Umesh B. , DUCLOS, Brian A. , CHEN, Kai , ZHANG, Wei , CHEN, Gang , PADGETT, Henry Clifton , KARIMI, Farhad , SCOTT, Peter J. H. , GAO, Zhiyong , LIANG, Qianwa , COLLIER, Thomas Lee , ZHAO, Tieming , XIA, Chunfang
发明人： KOLB, Hartmuth C , WALSH, Joseph C. , KASI, Dhanalakshmi , MOCHARLA, Vani , WANG, Bing , GANGADHARMATH, Umesh B. , DUCLOS, Brian A. , CHEN, Kai , ZHANG, Wei , CHEN, Gang , PADGETT, Henry Clifton , KARIMI, Farhad , SCOTT, Peter J. H. , GAO, Zhiyong , LIANG, Qianwa , COLLIER, Thomas Lee , ZHAO, Tieming , XIA, Chunfang
IPC分类号： C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D417/14 , A61P35/00 , A61K31/4192 , G01N33/532
CPC分类号： C07D417/04 , C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14 , C12Q1/485 , G01N2500/04 , G01N2500/10
摘要： The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
摘要翻译：本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。

2. 发明申请

WO1996020928A1 PIPERIDINE-BASED SIGMA RECEPTOR LIGANDS 审中-公开
标题翻译：基于哌啶的SIGMA受体配体
公开(公告)号：WO1996020928A1
公开(公告)日：1996-07-11
申请号：PCT/AU1995000885
申请日：1995-12-29
申请人： AUSTRALIAN NUCLEAR SCIENCE & TECHNOLOGY ORGANISATION , WATERHOUSE, Rikki, Noel , COLLIER, Thomas, Lee , O'BRIEN, Joanne, Christina
发明人： AUSTRALIAN NUCLEAR SCIENCE & TECHNOLOGY ORGANISATION
IPC分类号： C07D211/22
CPC分类号： C07D211/32 , A61K51/0455 , A61K2121/00 , A61K2123/00 , C07B59/002 , C07D211/22 , C07F7/2208
摘要： Compounds of formula (I) or pharmaceutically acceptable salts therof wherein X = O, CO or CHOH; R' is fluoroalkyl of 2 to 5 carbon atoms and 1 to 11 fluorine atoms; mono- and di-substituted benzyl wherein the substituents are selected from NO2, CN, I, Br, F, OH, OCH3 or OCH2OCH3 the substituents being at the meta or para positions; iodoalkenyl groups of 3 to 6 carbon atoms; bromoalkenyl groups of 3 to 6 carbon atoms; alkyl groups of 1 to 5 carbon atoms; or hydroxyalky containing 2 to 5 carbon atoms and 1 to 3 hydroxyl groups; R" is phenyl optionally substituted with one or two groups at the meta or para positions selected from methyl, ethyl, I, Br, CN, NO2, OH, CF3, OR wherein R is phenyl, 4-cyanophenyl, 4-nitrophenyl, CF3, methyl or ethyl; iodoalkenyl of 3 to 6 carbon atoms; bromoalkenyl of 3 to 6 carbon atoms; fluoroalkyl of 1 to 5 carbon atoms and 1 to 11 fluorine atoms; or alkyl groups of 1 to 5 carbon atoms as piperidine based sigma-1 receptor ligands suitable for use in diagnosis and therapy of diseases such as psychosis and cancer.
摘要翻译：式（I）化合物或其药学上可接受的盐，其中X = O，CO或CHOH; R'是2至5个碳原子的氟代烷基和1至11个氟原子; 单取代和二取代的苄基，其中取代基选自NO 2，CN，I，Br，F，OH，OCH 3或OCH 2 OCH 3，取代基在间位或对位; 3至6个碳原子的碘链烯基; 3至6个碳原子的溴链烯基; 1至5个碳原子的烷基; 或含有2至5个碳原子和1至3个羟基的羟基烷基; R“是在选自甲基，乙基，I，Br，CN，NO 2，OH，CF 3或OR的间位或对位，任选被一个或两个基团取代的苯基，其中R是苯基，4-氰基苯基，4-硝基苯基，CF 3 ，甲基或乙基; 3至6个碳原子的碘链烯基; 3至6个碳原子的溴链烯基; 1至5个碳原子和1至11个氟原子的氟代烷基;或1至5个碳原子的烷基，作为哌啶基的σ-1 受体配体适用于诊断和治疗疾病如精神病和癌症。

3. 发明申请

WO2008124703A3 DEVELOPMENT OF MOLECULAR IMAGING PROBES FOR CARBONIC ANHYDRASE-IX USING CLICK CHEMISTRY 审中-公开
标题翻译：使用单一化学物质开发碳氢化合物IX的分子成像探针
公开(公告)号：WO2008124703A3
公开(公告)日：2009-02-05
申请号：PCT/US2008059599
申请日：2008-04-07
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , WALSH JOSEPH C , KASI DHANALAKSHMI , MOCHARLA VANI , WANG BING , GANGADHARMATH UMESH B , DUCLOS BRIAN A , CHEN KAI , ZHANG WEI , CHEN GANG , PADGETT HENRY CLIFTON , KARIMI FARHAD , SCOTT PETER J H , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , ZHAO TIEMING , XIA CHUNFANG
发明人： KOLB HARTMUTH C , WALSH JOSEPH C , KASI DHANALAKSHMI , MOCHARLA VANI , WANG BING , GANGADHARMATH UMESH B , DUCLOS BRIAN A , CHEN KAI , ZHANG WEI , CHEN GANG , PADGETT HENRY CLIFTON , KARIMI FARHAD , SCOTT PETER J H , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , ZHAO TIEMING , XIA CHUNFANG
IPC分类号： C07D249/04 , A61K31/4192 , A61P35/00 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D417/14 , G01N33/532
CPC分类号： C07D417/04 , C07D249/04 , C07D249/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14 , C12Q1/485 , G01N2500/04 , G01N2500/10
摘要： The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.
摘要翻译：本申请公开了使用点击化学法鉴定对碳酸酐酶IX（CA-IX）酶具有高结合亲和力的抑制剂的方法，并将其候选用作正电子发射断层摄影（PET）成像剂。

4. 发明申请

WO2008124651A3 NITRO-IMIDAZOLE HYPOXIA IMAGING AGENTS 审中-公开
公开(公告)号：WO2008124651A3
公开(公告)日：2008-10-16
申请号：PCT/US2008/059505
申请日：2008-04-04
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , KOLB, Hartmuth C , WALSH, Joseph C. , GANGADHARMATH, Umesh B. , KARIMI, Farhad , PADGETT, Henry Clifton , KASI, Dhanalakshmi , GAO, Zhiyong , LIANG, Qianwa , COLLIER, Thomas Lee , DUCLOS, Brian A. , ZHAO, Tieming
发明人： KOLB, Hartmuth C , WALSH, Joseph C. , GANGADHARMATH, Umesh B. , KARIMI, Farhad , PADGETT, Henry Clifton , KASI, Dhanalakshmi , GAO, Zhiyong , LIANG, Qianwa , COLLIER, Thomas Lee , DUCLOS, Brian A. , ZHAO, Tieming
IPC分类号： C07D403/06 , C07D403/12 , C07B59/00 , A61K31/4192
摘要： The present invention relates to novel radioactively labeled bioreducible tracers of Formula (I) useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.

5. 发明申请

WO2008124651A2 NITRO-IMIDAZOLE HYPOXIA IMAGING AGENTS 审中-公开
标题翻译： NITRO-IMIDAZOLE HYPOXIA成像剂
公开(公告)号：WO2008124651A2
公开(公告)日：2008-10-16
申请号：PCT/US2008059505
申请日：2008-04-04
申请人： SIEMENS MEDICAL SOLUTIONS , KOLB HARTMUTH C , WALSH JOSEPH C , GANGADHARMATH UMESH B , KARIMI FARHAD , PADGETT HENRY CLIFTON , KASI DHANALAKSHMI , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , DUCLOS BRIAN A , ZHAO TIEMING
发明人： KOLB HARTMUTH C , WALSH JOSEPH C , GANGADHARMATH UMESH B , KARIMI FARHAD , PADGETT HENRY CLIFTON , KASI DHANALAKSHMI , GAO ZHIYONG , LIANG QIANWA , COLLIER THOMAS LEE , DUCLOS BRIAN A , ZHAO TIEMING
CPC分类号： C07D403/06 , C07B59/002 , C07D403/12
摘要： The present invention relates to novel radioactively labeled bioreducible tracers of Formula (I) useful for detecting hypoxic tumors or ischemic tissue in vivo. In one embodiment, the tracers consist of a 2-nitroimidazole moiety, a triazole, metabolically stable linker with pharmacokinetics enhancing substituents, and a radioisotope. The preferred in vivo imaging modality is positron emission tomography.
摘要翻译：本发明涉及用于体内检测缺氧性肿瘤或缺血组织的式（I）的新型放射性标记生物可还原示踪剂。在一个实施方案中，示踪剂由2-硝基咪唑部分，三唑，具有药代动力学增强取代基的代谢稳定接头和放射性同位素组成。优选的体内成像模式是正电子发射断层摄影。

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