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1. 发明授权

US09017724B2 Catalytic radiofluorination 有权
公开(公告)号：US09017724B2
公开(公告)日：2015-04-28
申请号：US12638606
申请日：2009-12-15
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K9/14 , C07F9/54 , A61K51/04 , C07D295/073 , A61B6/00 , C07B39/00
CPC分类号： A61K51/0459 , A61B6/507 , A61K51/04 , A61K51/0489 , C07B39/00 , C07B2200/05 , C07D295/073 , C07F9/5442
摘要： One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.

2. 发明授权

US08114379B2 Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process 有权
标题翻译：诊断和治疗烷基哌啶/哌嗪化合物和方法
公开(公告)号：US08114379B2
公开(公告)日：2012-02-14
申请号：US12100067
申请日：2008-04-09
申请人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
发明人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
IPC分类号： A61K51/04 , A61K49/22 , A61K31/4965 , A61K31/497
CPC分类号： C07D295/205 , C07D211/26 , C07D211/58 , C07D213/74 , C07D241/06 , C07D241/08 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/192 , C07D295/21 , C07D295/26
摘要： Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The compounds are characterized by the formulae: wherein: n is an integer of 1 to 6; X, Y, Z1 and Z2 can be the same or different and are hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6) alkoxy, N-alkyl, (C2-C6) acyloxy, N-alkylene, —SH, —SR, wherein R is from the same group as R1 and R2 and can be the same or different than R1 and R2, amino, nitro, cyano, hydroxy, C(═O)OR6, —C(═O)NR5R4, NR3R2, or S(═O)kR1 wherein k is 1 or 2, and R1 to R6 are independently hydrogen or (C1-C6) alkyl; R1, and R2 can be the same or different and are hydrogen, (C1-C6) alkyl, hydroxyalkyl or mercaptoalkyl, —C(═O)OR1, cyano, (C1-C6) alkenyl, (C2-C6) alkynyl, or 1,2,4-oxadiazol-5-yl optionally substituted at the 3-position by Z4 wherein any (C1-C6) alky, (C1-C6) alkanoyl, (C2-C6) alkenyl or (C2-C6) alkynyl can optionally be substituted by 1, 2 or 3 Z; R7 can be hydrogen, O or phenyl R8 can be hydrogen, phenyl, halophenyl, nitrophenyl, pyridyl, piperonyl or sulfoxonitrophenyl Z4 is (C1-C6) alkyl or phenyl, optionally substituted by 1, 2 or 3 Z1 W is O or S T is amino or C1-C6 aminoalkyl A is N or C T is C1-C6 alklyl or sulfonyl and V is alkyl (C0-C6), alkenyl, alkynyl, haloaryl, alkyl phenol, alkyl halophenyl, and R1 or R2 as indicated above and φ is phenyl, naphthyl, thienyl or pyridinyl.
摘要翻译：提供了可用于治疗特征在于缺乏多巴胺神经元活性或成像多巴胺神经元的神经变性疾病的哌啶或哌嗪化合物。该化合物的特征在于下式：其中：n为1至6的整数; X，Y，Z 1和Z 2可以相同或不同，为氢，卤素，卤代烷基，烷基，芳基，（C1-C6）烷氧基，N-烷基，（C2-C6）酰氧基，N-亚烷基， -SR，其中R是与R1和R2相同的基团，并且可以相同或不同于R1和R2，氨基，硝基，氰基，羟基，C（= O）OR6，-C（= O）NR5R4，NR3R2 或S（= O）kR1其中k为1或2，并且R 1至R 6独立地为氢或（C 1 -C 6）烷基; R 1和R 2可以相同或不同，为氢，（C 1 -C 6）烷基，羟烷基或巯基烷基，-C（= O）OR 1，氰基，（C 1 -C 6）烯基，（C 2 -C 6）炔基或其中任何（C 1 -C 6）烷基，（C 1 -C 6）烷酰基，（C 2 -C 6）烯基或（C 2 -C 6）炔基可以在3位上被Z 4任意取代在3位上的1,2,4-恶二唑-5-基，任选被1,2或3个Z取代; R7可以是氢，O或苯基R8可以是氢，苯基，卤代苯基，硝基苯基，吡啶基，胡椒基或磺基亚硝基苯基Z4是（C1-C6）烷基或苯基，任选被1,2或3取代，Z1是O或ST是氨基或C 1 -C 6氨基烷基A为N或CT为C 1 -C 6烷基或磺酰基，V为烷基（C 0 -C 6），链烯基，炔基，卤代芳基，烷基苯酚，烷基卤代苯基和如上所述的R 1或R 2，是苯基，萘基，噻吩基或吡啶基。

3. 发明申请

US20080206135A1 Method for monitoring blood flow and metabolic uptake in tissue with radiolabeled alkanoic acid 有权
标题翻译：用放射性标记的链烷酸监测组织中血流和代谢摄取的方法
公开(公告)号：US20080206135A1
公开(公告)日：2008-08-28
申请号：US11974139
申请日：2007-10-11
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup
IPC分类号： A61K51/04
CPC分类号： A61K51/0402
摘要： The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.
摘要翻译：本发明涉及新的改性脂肪酸类似物，其中将正电子或γ发射标记物置于脂肪酸主链上的位置，有机取代基被置换在2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。这些新的脂肪酸类似物被设计成通过与天然脂肪酸相同的长链脂肪酸载体机制进入感兴趣的组织，然而，2,3中的官能取代基; 3,4; 4,5; 5,6和其他序列位置，阻断分解代谢途径，从而在感兴趣的组织中以几乎未修饰的形式捕获这些类似物。

4. 发明授权

US5716594A Biotin compounds for targetting tumors and sites of infection 失效
标题翻译：用于靶向肿瘤和感染部位的生物素化合物
公开(公告)号：US5716594A
公开(公告)日：1998-02-10
申请号：US725060
申请日：1996-10-02
申请人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup , John W. Babich
发明人： David R. Elmaleh , Alan J. Fischman , Timothy M. Shoup , John W. Babich
IPC分类号： A61K51/04 , A61K51/00 , A01N43/50 , A61K35/00 , C07D235/02
CPC分类号： A61K51/0497 , A61K47/48146 , A61K51/0495 , A61K2121/00 , A61K2123/00
摘要： Novel biotin amide analogs that are useful for targeting therapeutic and imaging agents to sites of infection and tumors in vivo are disclosed.
摘要翻译：公开了可用于将治疗和显像剂靶向感染部位和体内肿瘤的新型生物素酰胺类似物。

5. 发明授权

US08772319B2 Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process 失效
标题翻译：诊断和治疗烷基哌啶/哌嗪化合物和方法
公开(公告)号：US08772319B2
公开(公告)日：2014-07-08
申请号：US13396010
申请日：2012-02-14
申请人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
发明人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
IPC分类号： A61K31/445 , C07D401/12 , C07D211/18
CPC分类号： C07D295/205 , C07D211/26 , C07D211/58 , C07D213/74 , C07D241/06 , C07D241/08 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/192 , C07D295/21 , C07D295/26
摘要： Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
摘要翻译：本文描述了可用于治疗以缺乏多巴胺神经元活性为特征的神经变性疾病的哌啶和哌嗪化合物。这些化合物也可用于成像多巴胺神经元。

6. 发明申请

US20120208847A1 Diagnostic and Therapeutic Alkyl Piperidine/Piperazine Compounds and Process 失效
标题翻译：诊断和治疗烷基哌啶/哌嗪化合物和方法
公开(公告)号：US20120208847A1
公开(公告)日：2012-08-16
申请号：US13396010
申请日：2012-02-14
申请人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
发明人： David R. Elmaleh , Choi Sungwoon , Alan J. Fischman
IPC分类号： A61K31/454 , A61P25/36 , C07D401/12 , C07D211/26 , A61K31/445
CPC分类号： C07D295/205 , C07D211/26 , C07D211/58 , C07D213/74 , C07D241/06 , C07D241/08 , C07D295/088 , C07D295/096 , C07D295/135 , C07D295/192 , C07D295/21 , C07D295/26
摘要： Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
摘要翻译：本文描述了可用于治疗以缺乏多巴胺神经元活性为特征的神经变性疾病的哌啶和哌嗪化合物。这些化合物也可用于成像多巴胺神经元。

7. 发明授权

US08092782B2 Polybiotin compounds of magnetic resonance imaging and drug delivery 有权
标题翻译：用于磁共振成像和药物递送的多生物素化合物
公开(公告)号：US08092782B2
公开(公告)日：2012-01-10
申请号：US12208025
申请日：2008-09-10
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman
IPC分类号： A61B5/055 , A61B5/05 , C07F5/00 , C07D255/02 , C07D235/02
CPC分类号： C07D519/00 , A61B5/0059 , A61B5/055 , A61B5/412 , A61B5/4839 , A61K47/557 , A61K49/085 , A61K49/10 , A61K49/106 , A61K49/124 , A61K51/0446 , A61K51/0497 , G01R33/5601
摘要： The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.
摘要翻译：本发明一般涉及可用作成像剂和药物递送剂的含生物素的化合物。本发明的另一方面涉及上述与金属原子螯合的化合物。在优选的实施方案中，金属原子是钆。本发明的另一方面涉及包含三个生物素部分和共价结合到杂环核心的药剂的化合物。在某些实施方案中，药剂是抗生素，抗病毒剂或放射性核素。本发明的另一方面涉及一种治疗涉及将哺乳动物施用本发明化合物的疾病的方法。本发明的另一方面涉及使用本发明化合物获得磁共振图像的方法。

8. 发明申请

US20110236308A1 Aryl Bidentate Isonitriles and Their Uses 审中-公开
标题翻译：芳基二异丁腈及其用途
公开(公告)号：US20110236308A1
公开(公告)日：2011-09-29
申请号：US12297513
申请日：2007-04-17
申请人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman , Bhaskar C. Das
发明人： David R. Elmaleh , Timothy M. Shoup , Alan J. Fischman , Bhaskar C. Das
IPC分类号： A61K51/04 , C07C255/33 , C07C255/51 , C07F13/00 , A61K47/48 , A61P43/00
CPC分类号： A61K51/0478 , A61K49/0002 , A61K49/0019
摘要： The present invention relates generally to chelation compounds, radionuclide metal chelate compounds, i.e., complexes, and radiolabeled targeting moieties, i.e., conjugates, formed therefrom, and methods of using these compounds, complexes and conjugates for diagnostic and therapeutic purposes. This invention is more particularly related to aryl bidentate isonitrile metal complexes generated by a chemical interaction of a metal salt oxide or weak complex of the metal with aryl isonitrile bidentate ligands.
摘要翻译：本发明一般涉及螯合化合物，即放射性核素金属螯合物，即络合物和放射性标记的靶向部分，即由其形成的缀合物，以及用于诊断和治疗目的的这些化合物，复合物和缀合物的使用方法。本发明更特别涉及通过金属盐氧化物或金属与芳基异腈二齿配体的弱络合物的化学相互作用产生的芳基二齿异腈金属络合物。

9. 发明申请

US20090117032A1 Imaging Agents for Early Detection and Monitoring of Cardiovascular Plaque 审中-公开
标题翻译：用于早期检测和监测心血管斑块的成像剂
公开(公告)号：US20090117032A1
公开(公告)日：2009-05-07
申请号：US12210760
申请日：2008-09-15
申请人： David R. Elmaleh , Alan J. Fischman , John W. Babich
发明人： David R. Elmaleh , Alan J. Fischman , John W. Babich
IPC分类号： A61K51/00 , C12N5/00 , C07K14/00 , C07K16/00
CPC分类号： A61K51/088
摘要： The present invention relates in part to imaging agents comprised of a targeting moiety and a label, such as a radionuclide or paramagnetic contrast agent, and methods of use thereof.
摘要翻译：本发明部分涉及由靶向部分和标记（例如放射性核素或顺磁造影剂）组成的成像剂及其使用方法。

10. 发明授权

US5587398A Meta substituted arylalkylamines and therapeutic and diagnostic uses therefor 失效
标题翻译：元取代的芳基烷基胺及其治疗和诊断用途
公开(公告)号：US5587398A
公开(公告)日：1996-12-24
申请号：US461577
申请日：1995-06-02
申请人： David R. Elmaleh , Alan J. Fischman
发明人： David R. Elmaleh , Alan J. Fischman
IPC分类号： A61K31/40 , A61K31/135 , A61K31/403 , A61K31/404 , A61P3/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07C211/27 , C07C211/29 , C07C211/30 , C07C225/16 , C07D209/08 , C07C15/04
CPC分类号： C07C211/27 , C07C211/29 , C07C211/30 , Y10S514/909
摘要： Novel meta substituted arylakylamine compounds are disclosed. These compounds can be administered as small molecule drugs to treat diseases or conditions associated with insufficient serotonin mediated nerve transmission (e.g. depression and obesity).
摘要翻译：公开了新的间位取代的芳基芳胺化合物。这些化合物可以作为小分子药物施用以治疗与5-羟色胺介导的神经传递不足（例如抑郁症和肥胖症）有关的疾病或病症。

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