公开(公告)号：US20080214851A1

公开(公告)日：2008-09-04

申请号：US11973926

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： C07C51/00

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 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. Theses 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发射标记置于脂肪酸主链上的位置，有机取代基被置换为2,3; 3,4; 4,5; 5,6和脂肪酸骨架的其他序列位置。 这些新型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。

公开(公告)号：US07381822B2

公开(公告)日：2008-06-03

申请号：US10814118

申请日：2004-03-31

申请人： David R. Elmaleh ,  Choi Songwoon ,  Alan J. Fischman

发明人： David R. Elmaleh ,  Choi Songwoon ,  Alan J. Fischman

IPC分类号： C07D401/12 ,  C07D241/10

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(αO)k R1 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.

公开(公告)号：US06548041B1

公开(公告)日：2003-04-15

申请号：US09568106

申请日：2000-05-10

申请人： Peter C. Meltzer ,  Paul Blundell ,  Bertha K. Madras ,  Alan J. Fischman ,  Alun G. Jones ,  Ashfaq Mahmood

发明人： Peter C. Meltzer ,  Paul Blundell ,  Bertha K. Madras ,  Alan J. Fischman ,  Alun G. Jones ,  Ashfaq Mahmood

IPC分类号： A61K5100

CPC分类号： A61K31/46 ,  A61B6/506 ,  A61K51/0448 ,  A61K51/0478 ,  A61K51/0497 ,  C07D451/02 ,  C07F13/005

摘要： Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

摘要翻译： 公开了放射性药物化合物。 托烷化合物通过8-位的N原子连接到能够络合锝或铼的螯合配体，以产生中性标记的复合物，其以比例为10或更高的比例选择性地结合血清素转运蛋白上的多巴胺转运蛋白。 这些化合物可以制备成单独的非对映异构体以及非对映异构体的混合物。 还公开了用于制备标记的放射性药物化合物的放射性药物试剂盒。

公开(公告)号：US6004990A

公开(公告)日：1999-12-21

申请号：US265512

申请日：1994-06-24

申请人： David R. Elmaleh ,  Alan J. Fischman

发明人： David R. Elmaleh ,  Alan J. Fischman

IPC分类号： C07C211/27 ,  C07C211/29 ,  C07C211/30 ,  A61K31/405 ,  C07D209/04

CPC分类号： C07C211/27 ,  C07C211/29 ,  C07C211/30

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, such as 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的疾病或病症，例如抑郁症和肥胖症。

公开(公告)号：US08900550B2

公开(公告)日：2014-12-02

申请号：US13602810

申请日：2012-09-04

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： A61K51/00 ,  A61M36/14 ,  C07F9/54 ,  A61K51/04 ,  C07C211/64 ,  C07C381/12 ,  C07D241/04 ,  A61K49/04 ,  A61K9/00

CPC分类号： A61K51/04 ,  A61B6/507 ,  A61K9/0021 ,  A61K49/0433 ,  A61K51/00 ,  A61K51/0459 ,  A61K51/0489 ,  C07B2200/05 ,  C07C209/74 ,  C07C211/64 ,  C07C381/12 ,  C07D241/04 ,  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 arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium 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.

摘要翻译： 本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。 在优选的实施方案中，使用氟化钾-18。 本发明的另一方面涉及可用作成像剂的含氟-18的芳基铵化合物。 在某些实施方案中，铵化合物是四芳基铵盐。 本发明的另一方面涉及可用作成像剂的含有氟-18的芳基锍化合物。 在某些实施方案中，锍化合物是三芳基锍盐。 本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

公开(公告)号：US08871179B2

公开(公告)日：2014-10-28

申请号：US13595546

申请日：2012-08-27

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： A61K51/00 ,  A61M36/14 ,  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。

公开(公告)号：US20130115168A1

公开(公告)日：2013-05-09

申请号：US13602810

申请日：2012-09-04

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： A61K51/04 ,  A61B6/507 ,  A61K9/0021 ,  A61K49/0433 ,  A61K51/00 ,  A61K51/0459 ,  A61K51/0489 ,  C07B2200/05 ,  C07C209/74 ,  C07C211/64 ,  C07C381/12 ,  C07D241/04 ,  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 arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium 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.

摘要翻译： 本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。 在优选的实施方案中，使用氟化钾-18。 本发明的另一方面涉及可用作成像剂的含氟-18的芳基铵化合物。 在某些实施方案中，铵化合物是四芳基铵盐。 本发明的另一方面涉及可用作成像剂的含有氟-18的芳基锍化合物。 在某些实施方案中，锍化合物是三芳基锍盐。 本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

公开(公告)号：US20130052129A1

公开(公告)日：2013-02-28

申请号：US13595546

申请日：2012-08-27

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 ,  A61K51/10 ,  A61K51/08

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.

公开(公告)号：US20120207677A1

公开(公告)日：2012-08-16

申请号：US11506603

申请日：2006-08-18

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 ,  C07C211/64

CPC分类号： A61K51/04 ,  A61B6/507 ,  A61K9/0021 ,  A61K49/0433 ,  A61K51/00 ,  A61K51/0459 ,  A61K51/0489 ,  C07B2200/05 ,  C07C209/74 ,  C07C211/64 ,  C07C381/12 ,  C07D241/04 ,  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 arylammonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the ammonium compound is a tetraaryl ammonium salt. Another aspect of the invention relates to arylsulfonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the sulfonium compound is a triaryl sulfonium 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.

摘要翻译： 本发明的一个方面涉及制备放射氟化取代的烷基，环烷基，芳基和链烯基化合物的方法。 在优选的实施方案中，使用氟化钾-18。 本发明的另一方面涉及可用作成像剂的含氟-18的芳基铵化合物。 在某些实施方案中，铵化合物是四芳基铵盐。 本发明的另一方面涉及可用作成像剂的含有氟-18的芳基锍化合物。 在某些实施方案中，锍化合物是三芳基锍盐。 本发明的另一方面涉及一种获得哺乳动物正电子发射图像的方法，包括以下步骤：向哺乳动物施用本发明的化合物，并获得哺乳动物的正电子发射光谱。

公开(公告)号：US07858803B2

公开(公告)日：2010-12-28

申请号：US12110686

申请日：2008-04-28

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： C07D417/12

CPC分类号： C07D277/66 ,  A61K51/0446 ,  A61K51/0453

摘要： The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4′-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.

摘要翻译： 本发明涉及用于成像和治疗阿尔茨海默病或淀粉样变性相关病理状况的化合物和方法，其利用新型淀粉样蛋白成像示踪剂来检测患有这些病症的受试者中的淀粉样蛋白沉积物。 在某些实施方案中，本发明涉及[N-2 [18F]氟丙基] -2-（4' - （甲基氨基） - 苯基）-6-羟基苯并噻唑（F-18MHT）及其二聚体。