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1. 发明授权

US5464934A Metal chelates as spacer compounds in biologically active peptides 失效
标题翻译：金属螯合物作为生物活性肽中的间隔物化合物
公开(公告)号：US5464934A
公开(公告)日：1995-11-07
申请号：US63172
申请日：1993-05-14
申请人： T. Jeffrey Dunn , Ananthachari Srinivasan , Leon R. Lyle , Raghavan Rajagopalan
发明人： T. Jeffrey Dunn , Ananthachari Srinivasan , Leon R. Lyle , Raghavan Rajagopalan
IPC分类号： A61K51/00 , A61K49/04 , A61K49/14 , A61K51/08 , C07K1/04 , C07K5/10 , C07K7/04 , C07K14/815 , C07K5/00 , A61K49/00 , C07K7/00 , C07K17/00
CPC分类号： A61K49/14 , C07K1/04 , C07K14/815
摘要： Ligands that are capable of forming metal complexes are incorporated directly into peptides at nonbiologically active locations. The metal complex serves as a bifunctional agent and as a spacer molecule. In one aspect of the invention, the ligands are prepared by replacing a nonbiologically active peptide spacer sequence with either Cys-Gly-Gly-Glu(.gamma.-)CO- (SEQ ID NO:1) or Cys-Gly-Gly-Lys(.epsilon.-)NH-CO(CH.sub.2).sub.2 -CO- (SEQ ID NO:2). In these examples, unnatural peptide bonds are used to attach the ligand to the terminal end of the peptide. Peptides incorporating such ligands are also disclosed.Other spacer ligands which may be incorporated into peptides include the following natural peptide sequences: -Cys-Gly-His-, -Asp-Gly-Cys-, -Glu-Gly-Cys-, -Gly-Asp-Cys-, and -Gly-Glu-Cys-. Unnatural tripeptides which function as spacer ligands include: -Cys-Gly-(imidazolyl glycyl)-, -isoCys-Gly-(imidazolyl glycyl)-, and -isoCys-Gly-His-. When the above peptide sequences are present in a nonbiologically active peptide spacer, they are able to form metal complexes with desired metal ions, and the resulting complexes serve as bifunctional agents and as spacer molecules in the peptide.
摘要翻译：能够形成金属络合物的配体在非生物活性位置直接并入肽中。金属络合物用作双官能剂和间隔分子。在本发明的一个方面，通过用Cys-Gly-Gly-Glu（γ - ）CO-（SEQ ID NO：1）或Cys-Gly-Gly-Lys（SEQ ID NO：1）替代非生物活性肽间隔序列 ε-）NH-CO（CH 2）2 -CO-（SEQ ID NO：2）。在这些实施例中，使用非天然肽键将配体连接到肽的末端。还公开了掺入这种配体的肽。可以并入肽中的其它间隔配体包括以下天然肽序列：-Cys-Gly-His-，-Asp-Gly-Cys-，-Glu-Gly-Cys-，-Gly-Asp-Cys-和 - Gly-Glu-Cys-。用作间隔基配体的非天然三肽包括：-Cys-Gly-（咪唑基甘氨酰基） - ， - iSysys-Gly-（咪唑基甘氨酰基） - 和-i-Syysys-Gly-His-。当上述肽序列存在于非生物活性肽间隔物中时，它们能够与期望的金属离子形成金属络合物，并且所得复合物用作双功能试剂和肽中的间隔分子。

2. 发明授权

US5798444A Ligand precursors for incorporation into peptides 失效
公开(公告)号：US5798444A
公开(公告)日：1998-08-25
申请号：US711375
申请日：1996-09-05
申请人： T. Jeffrey Dunn , Ananthachari Srinivasan
发明人： T. Jeffrey Dunn , Ananthachari Srinivasan
IPC分类号： A61K51/00 , A61K49/04 , C07C271/22 , C07K1/02 , C07K1/04 , C07K1/06 , C07K1/107 , C07K4/00 , C07K5/09 , C07K5/093 , C07K1/00
CPC分类号： C07K1/1075 , C07K1/02 , C07K1/04 , C07K5/0815 , C07K5/0819 , Y02P20/55
摘要： Compositions and methods of incorporating ligand precursors and ligands at any location within a peptide during peptide synthesis are disclosed. Derivatives of 2,4,5-triaminopentanoic acid and .gamma.-aminoglutamic acid are selectively incorporated into the peptide during solid phase or liquid phase synthesis, depending upon the choice of protecting groups. Ligand synthesis may then be completed at a later time to produce N.sub.3 S, N.sub.2 S.sub.2, and EDTA type chelating agents.

3. 发明授权

US5734011A Ligand precursors for incorporation into peptides 失效
标题翻译：用于掺入肽的配体前体
公开(公告)号：US5734011A
公开(公告)日：1998-03-31
申请号：US469028
申请日：1995-06-06
申请人： T. Jeffrey Dunn , Ananthachari Srinivasan
发明人： T. Jeffrey Dunn , Ananthachari Srinivasan
IPC分类号： A61K51/00 , A61K49/04 , C07C271/22 , C07K1/02 , C07K1/04 , C07K1/06 , C07K1/107 , C07K4/00 , C07K5/09 , C07K5/093 , A61K38/03
CPC分类号： C07K1/1075 , C07K1/02 , C07K1/04 , C07K5/0815 , C07K5/0819 , Y02P20/55
摘要： Compositions and methods of incorporating ligand precursors and ligands at any location within a peptide during peptide synthesis are disclosed. Derivatives of 2,4,5-triaminopentanoic acid and .gamma.-aminoglutamic acid are selectively incorporated into the peptide during solid phase or liquid phase synthesis, depending upon the choice of protecting groups. Ligand synthesis may then be completed at a later time to produce N.sub.3 S, N.sub.2 S.sub.2, and EDTA type chelating agents.
摘要翻译：公开了在肽合成期间将配体前体和配体掺入肽内的任何位置的组合物和方法。取决于保护基团的选择，2,4,5-三氨基戊酸和γ-氨基谷氨酸的衍生物在固相或液相合成期间选择性地掺入肽中。随后可以在稍后完成配体合成以产生N 3 S，N 2 S 2和EDTA型螯合剂。

4. 发明授权

US5071965A Novel TC-99M complexes 失效
标题翻译：新型TC-99M复合
公开(公告)号：US5071965A
公开(公告)日：1991-12-10
申请号：US315168
申请日：1989-02-24
申请人： T. Jeffrey Dunn , Dennis Nosco , Steven Woulfe , Richard Dean , Dennis Wester
发明人： T. Jeffrey Dunn , Dennis Nosco , Steven Woulfe , Richard Dean , Dennis Wester
IPC分类号： A61K51/00 , A61K51/04 , C07C211/13 , C07C215/50 , C07C217/42 , C07C251/08 , C07C251/24 , C07F5/02 , C07F5/04 , C07F9/50 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0478 , C07C211/13 , C07C215/50 , C07C217/42 , C07C251/08 , C07C251/24 , C07F9/5013 , A61K2123/00
摘要： Complexes useful as radiopharmaceutical imaging agents comprise technetium bonded to a ligand which generally can be described by the formula: ##STR1## wherein Z is N, C, B or P;the three Y groups can be the same or different, each characterized by the general formula ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, W, and X are further defined herein.
摘要翻译：可用作放射性药物成像剂的复合物包含与配体结合的锝，其通常可以由下式描述：其中Z是N，C，B或P; 三个Y基团可以相同或不同，各自以通式“IMAGE”为特征，R1，R2，R3，R4，W和X在本文中进一步定义。

5. 发明授权

US5565184A Functionalized tripodal ligands for x-ray & radioactive imaging applications 失效
标题翻译：用于x射线和放射性成像应用的功能化三齿配体
公开(公告)号：US5565184A
公开(公告)日：1996-10-15
申请号：US310514
申请日：1994-09-22
申请人： T. Jeffrey Dunn , Dennis A. Moore , Muthunadar P. Periasamy , Milorad M. Rogic , Rebecca A. Wallace , David H. White , Steven R. Woulfe
发明人： T. Jeffrey Dunn , Dennis A. Moore , Muthunadar P. Periasamy , Milorad M. Rogic , Rebecca A. Wallace , David H. White , Steven R. Woulfe
IPC分类号： G01R33/28 , A61B5/055 , A61K49/00 , A61K49/06 , C07C59/125 , C07C229/16 , C07C229/76 , C07C237/08 , C07C309/07 , C07C309/13 , C07F5/00 , C07F9/38 , C07F9/94 , C07F13/00 , A61K49/04
CPC分类号： C07C229/76 , A61K49/06 , C07C229/16 , C07C237/08 , C07C59/125 , C07F5/003 , Y10S514/836 , Y10T436/24
摘要： The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## wherein A is N or CR.sub.1, R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, where the alkyl or aryl group may be optionally substituted with one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.2, --CONR.sub.3 R.sub.4, or NR.sub.3 R.sub.4 ; R.sub.2 -R.sub.7 are as defined within; g, h, i, j, k and m may be the same or different and are an integer from one to about six; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH.Methods for imaging including MRI, X-ray and radiation diagnosis using compositions of the invention are also provided.
摘要翻译：本发明提供新的和结构上不同的组合物，其包含以下通式的化合物：其中A是N或CR 1，R 1是氢，C 1 -C 8烷基或C 6 -C 10芳基，其中烷基或芳基可以是任选的被一个或多个羟基，C 1 -C 8烷基，C 1 -C 8羟烷基，C 1 -C 8烷氧基，C 6 -C 10芳基，C 6 -C 10羟基芳基，C 6 -C 10芳氧基，-CO 2 R 2，-CONR 3 R 4或NR 3 R 4取代; R2-R7如上所定义; g，h，i，j，k和m可以相同或不同，为1〜6的整数; X是-CO 2 H，-PO 3 H 2，-SO 3 H或-CONHOH。还提供了使用本发明的组合物进行MRI，X射线和放射线诊断的成像方法。

6. 发明授权

US5405601A Functionalized tripodal ligands for imaging applications 失效
标题翻译：用于成像应用的功能化三齿配体
公开(公告)号：US5405601A
公开(公告)日：1995-04-11
申请号：US87837
申请日：1993-07-02
申请人： T. Jeffrey Dunn , Dennis A. Moore , Muthanadar Periasamy , Milorad M. Rogic , Rebecca A. Wallace , David H. White , Steven R. Woulfe
发明人： T. Jeffrey Dunn , Dennis A. Moore , Muthanadar Periasamy , Milorad M. Rogic , Rebecca A. Wallace , David H. White , Steven R. Woulfe
IPC分类号： G01R33/28 , A61B5/055 , A61K49/00 , A61K49/06 , C07C59/125 , C07C229/16 , C07C229/76 , C07C237/08 , C07C309/07 , C07C309/13 , C07F5/00 , C07F9/38 , C07F9/94 , C07F13/00 , C07C55/00 , C07C59/245
CPC分类号： C07C229/76 , A61K49/06 , C07C229/16 , C07C237/08 , C07C59/125 , C07F5/003 , Y10S514/836 , Y10T436/24
摘要： The present invention provides new and structurally diverse compositions for diagnostic imaging comprising compounds of the general formula: ##STR1## wherein A is N or CR.sub.1, R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, where the alkyl or aryl group may be optionally substituted with one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.2, --CONR.sub.3 R.sub.4, or NR.sub.3 R.sub.4 ; D is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O--, or NR.sub.5 ; E is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.6 ; F is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.7 ; R.sub.2 -R.sub.7 are as defined within; g, h, i, j, k and m may be the same or different and are an integer from one to about six; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH.
摘要翻译：本发明提供用于诊断成像的新的和结构不同的组合物，其包含以下通式的化合物：其中烷基或芳基可以任选地被一个或多个羟基，C 1 -C 8烷基，C 1 -C 8羟基烷基，C 1 -C 8烷氧基，C 6 -C 10芳基，C 6 -C 10羟基芳基，C 6 -C 10芳氧基，-CO 2 R 2，-CONR 3 R 4或NR 3 R 4; D是O，-O（CH 2）2 O-，-O（CH 2）3 O-或NR 5; E是O，-O（CH 2）2 O-，-O（CH 2）3 O-或NR 6; F是O，-O（CH 2）2 O-，-O（CH 2）3 O-或NR 7; R2-R7如上所定义; g，h，i，j，k和m可以相同或不同，为1〜6的整数; X是-CO 2 H，-PO 3 H 2，-SO 3 H或-CONHOH。

7. 发明授权

US5264204A Hydrophilic free radicals for magnetic resonance imaging 失效
标题翻译：用于磁共振成像的亲水自由基
公开(公告)号：US5264204A
公开(公告)日：1993-11-23
申请号：US876548
申请日：1992-04-30
申请人： William P. Cacheris , T. Jeffrey Dunn , Lynn deLearie , Youlin Lin , Jeffrey A. Levine
发明人： William P. Cacheris , T. Jeffrey Dunn , Lynn deLearie , Youlin Lin , Jeffrey A. Levine
IPC分类号： A61K49/20 , C07D207/46 , G01R33/28 , G01N24/08 , A61K31/40 , A61K31/415
CPC分类号： G01R33/5601 , A61K49/20 , C07D207/46 , Y10T436/24
摘要： Methods and compositions are disclosed for enhancing magnetic resonance imaging which utilize hydrophilic free radical compounds as magnetic resonance contrast media. Typical magnetic resonance contrast media within the scope of the present invention include stable hydrophilic free radicals having a hydrophilic moiety, such as polyhydroxyalkyl groups and heterocyclic amino-alcohols such as dihydroxypyrrolidine, dihydroxypiperidine, and trihydroxypiperidine, and a stable free radical moiety, such as a nitroxide, phenoxy, or phenoxazinyl free radical moiety.
摘要翻译：公开了用于增强使用亲水性自由基化合物作为磁共振造影剂的磁共振成像的方法和组合物。在本发明范围内的典型磁共振造影剂包括具有亲水部分的稳定的亲水性自由基，例如聚羟基烷基和杂环氨基醇，例如二羟基吡咯烷，二羟基哌啶和三羟基哌啶，以及稳定的自由基部分，例如硝基氧，苯氧基或吩恶嗪基自由基部分。

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