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1. 发明申请

WO1994026294A1 LIGAND PRECURSORS FOR INCORPORATION INTO PEPTIDES 审中-公开
标题翻译：配合入口的配对前列腺
公开(公告)号：WO1994026294A1
公开(公告)日：1994-11-24
申请号：PCT/US1994005403
申请日：1994-05-13
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , DUNN, T., Jeffrey , SRINIVASAN, Ananthachari
IPC分类号： A61K37/02
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 N3S, N2S2, 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。

2. 发明申请

WO1994021304A1 NOVEL HETEROCYCLE BASED NITROGEN-SULFUR LIGANDS USEFUL IN RADIOGRAPHIC IMAGING AGENTS 审中-公开
标题翻译：用于放射成像剂的新型基于氮的硫化物配体
公开(公告)号：WO1994021304A1
公开(公告)日：1994-09-29
申请号：PCT/US1994002601
申请日：1994-03-10
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , RAJAGOPALAN, Raghavan , SRINIVASAN, Ananthachari
IPC分类号： A61K49/02
CPC分类号： C07F13/005 , A61K51/0478 , A61K2123/00 , C07D295/13 , C07D309/08
摘要： The present invention relates particularly to novel heterocycle based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型基于杂环的氮 - 硫配体，并且可用作用于诊断目的的一般成像剂。

3. 发明申请

WO1993015771A1 LIGANDS FOR IMPROVING METAL CHELATE FORMATION KINETICS 审中-公开
标题翻译：用于改进金属烧结形成动力学的配体
公开(公告)号：WO1993015771A1
公开(公告)日：1993-08-19
申请号：PCT/US1993001013
申请日：1993-02-05
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , SRINIVASAN, Ananthachari
IPC分类号： A61K49/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/088 , A61K2121/00 , A61K2123/00 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555
摘要： Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include an amine to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to or conversion of the ligand to a thermodynamically stable amide-thiolate complex. In one embodiment of the invention, the amine is a tertiary amine, or its equivalent, strategically located to facilitate complex formation. In another embodiment of the invention, the amine is part of pyridine containing a lower alkoxy substituent in the 2 or 4 ring position. O-dealkylation occurs upon complexation causing the amine to become a vinylogous amide as part of a thermodynamically stable amide-thiolate complex. The amide-thiolate ligands of the present invention may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.
摘要翻译：公开了具有改进的金属螯合物形成动力学的酰胺 - 硫醇盐配体。配体包括胺以促进胺 - 酰胺 - 硫醇盐中间体络合物的快速形成，然后将金属转移到或将配体转化为热力学稳定的酰胺 - 硫醇盐复合物。在本发明的一个实施方案中，胺是一种叔胺或其等同物，其策略性定位以促进复合物形成。在本发明的另一个实施方案中，胺是在2或4环位置含有低级烷氧基取代基的吡啶的一部分。 O-脱烷基化在络合时发生，导致胺作为热力学稳定的酰胺 - 硫醇盐络合物的一部分而成为维仁酰胺。本发明的酰胺 - 硫醇酸酯配体可用于在诊断和治疗领域中用于生物物质的后成形标记。

4. 发明申请

WO1996040291A1 RADIOLABELED PEPTIDE COMPOSITIONS FOR SITE-SPECIFIC TARGETING 审中-公开
标题翻译：用于场地特异性靶向的无定形肽组合物
公开(公告)号：WO1996040291A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009384
申请日：1996-06-06
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , SRINIVASAN, Ananthachari , DYSZLEWSKI, Mary, Marmion , BUGAJ, Joseph, E.
IPC分类号： A61K51/00
CPC分类号： C07K14/6555 , A61K51/083 , A61K51/088
摘要： This invention relates to radiolabeled peptide compositions for radiopharmaceutical use and, more specifically, to radiolabeled peptides for diagnostic or therapeutic use having an unmodified carboxy terminal amino acid. The radiopharmaceutical composition may be used for targeting a selected biological site. The radiolabeled peptide is characterized by having its carboxy terminal amino acid in its carboxylic acid form and the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent. The radiopharmaceutical composition preferably comprises a radiolabeled peptide selected from the group consisting of somatostatin, an analog of somatostatin, a derivative of somatostatin and peptides capable of binding to the somatostatin receptor, where the peptide is coupled to a diagnostic or therapeutic radionuclide by a chelating agent has its carboxy terminal amino acid in its carboxylic acid form.
摘要翻译：本发明涉及用于放射性药物用途的放射性标记肽组合物，更具体地，涉及具有未修饰的羧基末端氨基酸的用于诊断或治疗用途的放射性标记肽。放射性药物组合物可以用于靶向选定的生物部位。放射性标记的肽的特征在于其羧基末端氨基酸为羧酸形式，肽通过螯合剂偶联至诊断或治疗放射性核素。放射性药物组合物优选包含选自生长抑素，生长抑素类似物，生长抑素衍生物和能够结合生长抑素受体的肽的放射性标记肽，其中肽通过螯合剂偶联至诊断或治疗放射性核素其羧基末端氨基酸呈羧酸形式。

5. 发明申请

WO1994020148A1 IMIDAZOLE BASED NITROGEN-SULFUR LIGANDS USEFUL IN RADIOGRAPHIC IMAGING AGENTS 审中-公开
标题翻译：基于咪唑基的氮素硫化物配合物可用于放射成像剂
公开(公告)号：WO1994020148A1
公开(公告)日：1994-09-15
申请号：PCT/US1994002483
申请日：1994-03-09
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , RAJAGOPALAN, Raghavan , SRINIVASAN, Ananthachari
IPC分类号： A61K49/02
CPC分类号： C07F13/005 , A61K51/0478 , A61K2123/00 , C07D233/64 , C07D405/12
摘要： The present invention relates particularly to novel imidazole based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型咪唑基氮硫配体，并且可用作用于诊断目的的一般成像剂。

6. 发明申请

WO1993015770A1 RADIOLABELLED PEPTIDE COMPOUNDS 审中-公开
标题翻译：放射性肽化合物
公开(公告)号：WO1993015770A1
公开(公告)日：1993-08-19
申请号：PCT/US1993000939
申请日：1993-02-04
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , LYLE, Leon , RAJAGOPALAN, Raghavan , DEUTSCH, Karen , DUNN, Thomas, Jeffrey , SRINIVASAN, Ananthachari , VANDERHEYDEN, J., L.
IPC分类号： A61K49/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/083 , A61K51/088 , A61K2121/00 , A61K2123/00 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555
摘要： The present invention relates to novel ligands and labelling techniques. The present invention further relates to a diagnostic composition suitable for administration to a warm-blooded animal comprising somatostatin or hirudin or a molecule capable of interacting with the somatostatin receptor or with the hirudin receptor labeled with a radionuclide by means of a chelate ligand capable of administration to an animal to produce reliable visual imaging of tumors or therapeutic effects on tumors and blood clots.
摘要翻译：本发明涉及新的配体和标记技术。本发明还涉及一种适于给予温血动物的诊断组合物，其包含生长抑素或水蛭素或能够与生长抑素受体相互作用的分子，或与通过能够施用的螯合配体的放射性核素标记的水蛭素受体给动物产生肿瘤的可靠视觉成像或对肿瘤和血块的治疗作用。

7. 发明申请

WO1994026295A1 METAL CHELATES AS SPACER COMPOUNDS IN BIOLOGICALLY ACTIVE PEPTIDES 审中-公开
标题翻译：金属螯合物作为生物活性肽中的间隔化合物
公开(公告)号：WO1994026295A1
公开(公告)日：1994-11-24
申请号：PCT/US1994005412
申请日：1994-05-13
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , DUNN, T., Jeffrey , SRINIVASAN, Ananthachari , LYLE, Leon, R. , RAJAGOPALAN, Raghavan
IPC分类号： A61K37/02
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(CH2)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 - 甘氨酸 - 谷氨酸 - 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。

8. 发明申请

WO1996040292A1 A METHOD FOR PREPARING RADIOLABELED PEPTIDES 审中-公开
标题翻译：一种制备放射性肽的方法
公开(公告)号：WO1996040292A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009706
申请日：1996-06-07
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , SRINIVASAN, Ananthachari
IPC分类号： A61K51/00
CPC分类号： A61K51/088 , A61K51/083 , C07C227/18 , Y02P20/55 , C07C229/16 , C07C229/24
摘要： A method for radiolabelling peptides using polyaminocarboxylate ligands having suitable protecting groups such that they can be added to peptides by standard solid phase or solution phase peptide synthetic chemistry and can be deprotected using standard cleavage/deprotection reagents and produce the peptide/chelate conjugate as a high purity monoaddition product is provided. The cleaved and deprotected ligand-peptide molecules can then be labeled with lanthanide or actinide radionuclides. The protected polyaminocarboxylate ligands form mono-anhydrides or mono-active esters under solid phase or solution phase conditions and permit only the desired monoaddition chelate-peptide conjugate to be formed.
摘要翻译：使用具有合适的保护基的聚氨基羧酸盐配体放射性标记肽的方法，使得它们可以通过标准固相或溶液相肽合成化学物质加入到肽中，并且可以使用标准的切割/去保护试剂去保护，并产生高/低的肽/螯合物缀合物提供纯度单加成产物。然后可以用镧系元素或锕系元素放射性核素标记裂解和去保护的配体 - 肽分子。保护的多氨基羧酸盐配体在固相或溶液相条件下形成单酸酐或单官能酯，并且仅允许形成所需的单加成螯合物 - 肽缀合物。

9. 发明申请

WO1996003429A1 STABLE ANALOGS OF BIOACTIVE PEPTIDES CONTAINING DISULFIDE LINKAGES 审中-公开
标题翻译：含有不饱和链接的生物活性肽的稳定模拟
公开(公告)号：WO1996003429A1
公开(公告)日：1996-02-08
申请号：PCT/US1995009041
申请日：1995-07-18
申请人： MALLINCKRODT MEDICAL, INC.
发明人： MALLINCKRODT MEDICAL, INC. , SRINIVASAN, Ananthachari , LYLE, Leon, R. , RAJAGOPALAN, Raghavan
IPC分类号： C07K07/16
CPC分类号： C07K14/655 , C07K1/006 , C07K7/16 , C07K14/52 , C07K14/6555 , C07K14/70 , Y10S930/28
摘要： Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (-S-S-) is replaced with a monosulfide bond (-S-) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified side is a bifuctional effector molecule. In thioketal expansion, an alkylidene unit (-CR1R2-) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
摘要翻译：公开了含有二硫键的环肽的稳定类似物。二硫键通过四种方法之一进行改性：（a）硫化物收缩，（b）等排取代，（c）硫代缩酮扩展或（d）烷基化扩展。在硫化物收缩中，二硫键（-S-S-）用单硫键（-S-）代替，其中双功能效应分子如配体或化学毒性剂与新的肽键结合。在等排取代中，一个硫原子被碳原子取代，并且修饰侧的至少一个碳原子是双功能效应分子。在缩酮缩醛中，在两个硫原子之间插入亚烷基单元（-CR1R2-）。在烷基化扩展中，C2至C3的烷基部分插入在两个硫原子之间。

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