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1. 发明申请

US20060198786A1 Glycopeptide compositions 有权
标题翻译：糖肽组合物
公开(公告)号：US20060198786A1
公开(公告)日：2006-09-07
申请号：US11071975
申请日：2005-03-04
申请人： I-Chien Wei , David Yang , Dong-Fang Yu
发明人： I-Chien Wei , David Yang , Dong-Fang Yu
IPC分类号： A61K51/00 , C07K9/00
CPC分类号： A61K31/505 , A61K31/66 , A61K51/025
摘要： The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.
摘要翻译：本发明包括具有糖苷和通过酰胺键共价结合的肽的糖肽。糖肽还可以包括与糖肽结合的诊断或治疗剂。诸如放射性核素的金属也可以与糖肽螯合。本发明的具体实施方案涉及由聚（氨基酸）如聚（谷氨酸）或聚（天冬氨酸）共价结合的壳聚糖制成的糖肽。与糖肽缀合的诊断剂可以促进成像。可以与糖肽结合的特异性治疗剂包括抗癌药物，类风湿关节炎药物，抗凝血剂，抗血管生成药物，凋亡药物，骨质疏松症药物，类固醇和抗炎药物。一些药剂如放射性核素可能具有诊断和治疗作用。糖肽可以通过在碳二亚胺和酸基活化剂的存在下组合糖苷和肽来在糖苷和肽之间形成酰胺键来制备。

2. 发明授权

US09820986B2 Glycopeptide compositions 有权
公开(公告)号：US09820986B2
公开(公告)日：2017-11-21
申请号：US11071975
申请日：2005-03-04
申请人： I-Chien Wei , David J. Yang , Dong-Fang Yu
发明人： I-Chien Wei , David J. Yang , Dong-Fang Yu
IPC分类号： A61K31/505 , A61K31/66 , A61K51/02
CPC分类号： A61K31/505 , A61K31/66 , A61K51/025
摘要： The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.

3. 发明申请

US20110087003A1 GLYCOPEPTIDE COMPOSITIONS 审中-公开
标题翻译：糖精组合物
公开(公告)号：US20110087003A1
公开(公告)日：2011-04-14
申请号：US12970026
申请日：2010-12-16
申请人： I-Chien Wei , David J. Yang , Dong-Fang Yu
发明人： I-Chien Wei , David J. Yang , Dong-Fang Yu
IPC分类号： C07K2/00 , C07K1/113
CPC分类号： A61K31/505 , A61K31/66 , A61K51/025
摘要： The invention include glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.
摘要翻译：本发明包括具有糖苷和通过酰胺键共价键合的肽的糖肽。糖肽还可以包括与糖肽结合的诊断或治疗剂。诸如放射性核素的金属也可以与糖肽螯合。本发明的具体实施方案涉及由聚（氨基酸）如聚（谷氨酸）或聚（天冬氨酸）共价结合的壳聚糖制成的糖肽。与糖肽缀合的诊断剂可以促进成像。可以与糖肽结合的特异性治疗剂包括抗癌药物，类风湿关节炎药物，抗凝血剂，抗血管生成药物，凋亡药物，骨质疏松症药物，类固醇和抗炎药物。一些药剂如放射性核素可能具有诊断和治疗作用。糖肽可以通过在碳二亚胺和酸基活化剂的存在下组合糖苷和肽来在糖苷和肽之间形成酰胺键来制备。

4. 发明申请

US20080300389A1 Metal-polysaccharide conjugates: compositions, synthesis and methods for cancer therapy 审中-公开
标题翻译：金属 - 多糖共轭物：用于癌症治疗的组合物，合成和方法
公开(公告)号：US20080300389A1
公开(公告)日：2008-12-04
申请号：US12009421
申请日：2008-01-18
申请人： David J. Yang , Dong-Fang Yu , I-Chien Wei
发明人： David J. Yang , Dong-Fang Yu , I-Chien Wei
IPC分类号： C07H15/00
CPC分类号： A61K33/24 , A61K31/282 , A61K47/61
摘要： The current disclosure, in one embodiment, includes a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid. According to another embodiment, the disclosure provides a method of synthesizing a polysaccharide conjugate by covalently bonding a monomeric amino acid having an O-group to a polysaccharide and by conjugating a metal to the O-group to form a polysaccharide conjugate. According to a third embodiment, the disclosure relates to a method of killing a cancer cell by administering to the cell an effective amount of a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid.
摘要翻译：在一个实施方案中，本公开内容包括多糖缀合物。该缀合物具有多糖和至少一个与多糖共价结合的具有O-基团的单体氨基酸。缀合物还具有至少一种由氨基酸的O-基缀合的金属。根据另一个实施方案，本公开提供了通过将具有O-基团的单体氨基酸与多糖共价键合并通过将金属与O基团缀合以形成多糖缀合物来合成多糖缀合物的方法。根据第三实施方案，本公开涉及通过向细胞施用有效量的多糖缀合物来杀死癌细胞的方法。该缀合物具有多糖和至少一个与多糖共价结合的具有O-基团的单体氨基酸。缀合物还具有至少一种由氨基酸的O-基缀合的金属。

5. 发明申请

US20070248537A1 Compositions and Methods for Cellular Imaging and Therapy 有权
标题翻译：细胞成像和治疗的组合和方法
公开(公告)号：US20070248537A1
公开(公告)日：2007-10-25
申请号：US11737694
申请日：2007-04-19
申请人： David Yang , Chang-Sok Oh , Dong-Fang Yu , Ali Azhdarinia , Saady Kohanim
发明人： David Yang , Chang-Sok Oh , Dong-Fang Yu , Ali Azhdarinia , Saady Kohanim
IPC分类号： A61K51/00 , A61K49/10 , C07F5/00 , C07K16/46
CPC分类号： C07F13/005 , A61K47/547 , A61K51/0474 , A61K51/0491
摘要： The present invention relates generally to the fields of chemistry and radionuclide imaging. More particularly, it concerns compositions, kits and methods for imaging and therapy involving N4 compounds and derivatives.
摘要翻译：本发明一般涉及化学和放射性核素成像领域。更具体地，涉及涉及N 4+化合物及其衍生物的成像，试剂盒和成像和治疗方法。

6. 发明申请

US20070122342A1 Ethylenedicysteine (EC)-Drug Conjugates Compositions and Methods for Tissue Specific Disease Imaging 有权
标题翻译：亚乙基半胱氨酸（EC） - 药物偶联物组合物和组织特异性疾病成像方法
公开(公告)号：US20070122342A1
公开(公告)日：2007-05-31
申请号：US11627299
申请日：2007-01-25
申请人： David Yang , Chun Liu , Dong-Fang Yu , E. Kim
发明人： David Yang , Chun Liu , Dong-Fang Yu , E. Kim
IPC分类号： A61K51/00
CPC分类号： A61K51/088 , A61K51/04 , A61K51/0478 , A61K51/0491 , A61K51/0497 , A61K51/087
摘要： The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.
摘要翻译：本发明在一般意义上提供了采用与乙二
氨酸（EC）螯合的99m Tc的新标记策略。 EC与各种配体缀合并螯合至99m Tc以用作组织特异性疾病的显像剂。本发明的药物缀合物也可用作预后工具或用作将治疗剂递送至哺乳动物体内特定部位的工具。还提供了用于组织特异性疾病成像的试剂盒。

7. 发明申请

US20060246005A1 Poly(peptide) as a chelator: methods of manufacture and uses 审中-公开
标题翻译：聚（肽）作为螯合剂：制造和使用方法
公开(公告)号：US20060246005A1
公开(公告)日：2006-11-02
申请号：US11394664
申请日：2006-03-31
申请人： David Yang , Dong-Fang Yu , Chang Oh , Saady Kohanim , E. Kim , Ali Azhdarinia
发明人： David Yang , Dong-Fang Yu , Chang Oh , Saady Kohanim , E. Kim , Ali Azhdarinia
IPC分类号： A61K51/00
CPC分类号： A61K51/088 , A61K47/64 , A61K51/0478 , A61K51/0497
摘要： Novel compositions for imaging that include (a) a polypeptide that includes two or more consecutive amino acids that will function to non-covalently bind valent metal ions and (2) a valent metal ion chelated to at least one of the two consecutive amino acids, are disclosed. Also disclosed are methods of imaging using these novel compositions, such as methods of imaging a tumor within a subject. Methods of synthesizing an imaging agent and kits for preparing an imaging agent are also disclosed. Methods for determining the effectiveness of a candidate substance as an imaging agent that involve conjugating or chelating the candidate substance with a polypeptide that includes two or more consecutive amino acids that will function to non-covalently bind valent metal ions.
摘要翻译：用于成像的新型组合物包括（a）包含两个或更多个连续氨基酸的多肽，所述两个或多个连续的氨基酸将用于非共价结合价金属离子，和（2）螯合至两个连续氨基酸中的至少一个的价金属离子，被披露。还公开了使用这些新型组合物成像的方法，例如在受试者内成像肿瘤的方法。还公开了合成显影剂的方法和用于制备显影剂的试剂盒。用于确定作为显像剂的候选物质的有效性的方法，所述显像剂涉及使候选物质与包含两个或更多个连续氨基酸的多肽共轭或螯合候选物质，所述多个连续的氨基酸将用于非共价结合价金属离子。

8. 发明申请

US20050227910A1 LOCAL REGIONAL CHEMOTHERAPY AND RADIOTHERAPY USING IN SITU HYDROGEL 有权
标题翻译：当地区域化疗和放射治疗在现代水文中的应用
公开(公告)号：US20050227910A1
公开(公告)日：2005-10-13
申请号：US10024678
申请日：2001-12-18
申请人： David Yang , Dong-Fang Yu , Ali Azhdarinia , Tommy Lee , E. Kim
发明人： David Yang , Dong-Fang Yu , Ali Azhdarinia , Tommy Lee , E. Kim
IPC分类号： A61K47/30 , A61K9/00 , A61K9/16 , A61K31/337 , A61K31/555 , A61K31/7048 , A61K31/717 , A61K31/718 , A61K31/721 , A61K31/722 , A61K31/728 , A61K31/729 , A61K35/76 , A61K36/00 , A61K38/00 , A61K38/22 , A61K47/02 , A61K47/04 , A61K47/18 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/48 , A61K48/00 , A61K51/00 , A61K51/06 , A61K51/12 , A61M37/00 , A61P31/00 , A61P35/00
CPC分类号： A61K51/1255 , A61K9/0024 , A61K9/1652 , A61K31/717 , A61K31/718 , A61K31/721 , A61K31/722 , A61K31/728 , A61K31/729 , A61K47/183 , A61K47/36 , A61K47/38 , A61K47/6903 , A61K51/06 , A61K51/1213
摘要： Methods regarding local regional treatment in situ for an individual, such as of a tumor, are provided herein. A hydrogel composition is generated in situ in the tumor by administering a polymer, such as a polysaccharide or a polyamino acid, with a therapeutic agent, such as a radionuclide or a drug, and administering a cross-linking agent. The hydrogel/therapeutic agent composition is retained in the tumor for safe and efficient tumor therapy. Alternatively, a hydrogel composition is generated in situ in an artery which nourishes a tumor to occlude the artery.
摘要翻译：本文提供了关于个体如肿瘤的原位局部局部治疗的方法。通过使用诸如多糖或多氨基酸的聚合物与治疗剂如放射性核素或药物一起在肿瘤中原位产生水凝胶组合物，并施用交联剂。水凝胶/治疗剂组合物保留在肿瘤中用于安全和有效的肿瘤治疗。或者，在动脉中产生水凝胶组合物，该动脉会滋养肿瘤以闭塞动脉。

9. 发明申请

US20050208138A1 Local regional chemotherapy and radiotherapy using in situ hydrogel 审中-公开
标题翻译：局部局部化疗和放疗使用原位水凝胶
公开(公告)号：US20050208138A1
公开(公告)日：2005-09-22
申请号：US11036580
申请日：2005-01-14
申请人： David Yang , Dong-Fang Yu , Ali Azhdarinia , Tommy Lee , E. Kim
发明人： David Yang , Dong-Fang Yu , Ali Azhdarinia , Tommy Lee , E. Kim
IPC分类号： A61K47/30 , A61K9/00 , A61K9/16 , A61K31/337 , A61K31/555 , A61K31/7048 , A61K31/717 , A61K31/718 , A61K31/721 , A61K31/722 , A61K31/728 , A61K31/729 , A61K35/76 , A61K36/00 , A61K38/00 , A61K38/22 , A61K47/02 , A61K47/04 , A61K47/18 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/48 , A61K48/00 , A61K51/00 , A61K51/06 , A61K51/12 , A61M37/00 , A61P31/00 , A61P35/00 , A61K9/14 , A61M31/00
CPC分类号： A61K51/1255 , A61K9/0024 , A61K9/1652 , A61K31/717 , A61K31/718 , A61K31/721 , A61K31/722 , A61K31/728 , A61K31/729 , A61K47/183 , A61K47/36 , A61K47/38 , A61K47/6903 , A61K51/06 , A61K51/1213
摘要： Methods regarding local regional treatment in situ for an individual, such as of a tumor, are provided herein. A hydrogel composition is generated in situ in the tumor by administering a polymer, such as a polysaccharide or a polyamino acid, with a therapeutic agent, such as a radionuclide or a drug, and administering a cross-linking agent. The hydrogel/therapeutic agent composition is retained in the tumor for safe and efficient tumor therapy. Alternatively, a hydrogel composition is generated in situ in an artery which nourishes a tumor to occlude the artery.
摘要翻译：本文提供了关于个体如肿瘤的原位局部局部治疗的方法。通过使用诸如多糖或多氨基酸的聚合物与治疗剂如放射性核素或药物一起在肿瘤中原位产生水凝胶组合物，并施用交联剂。水凝胶/治疗剂组合物保留在肿瘤中用于安全和有效的肿瘤治疗。或者，在动脉中产生水凝胶组合物，该动脉会滋养肿瘤以闭塞动脉。

10. 发明申请

US20050129619A1 N2S2 chelate-targeting ligand conjugates 有权
标题翻译： N2S2螯合靶向配体缀合物
公开(公告)号：US20050129619A1
公开(公告)日：2005-06-16
申请号：US10732919
申请日：2003-12-10
申请人： David Yang , Dong-Fang Yu , Chang-Sok Oh , Jerry Bryant
发明人： David Yang , Dong-Fang Yu , Chang-Sok Oh , Jerry Bryant
IPC分类号： A61K51/04 , A61K51/08 , A61K51/10 , A61K49/00 , A61K51/00 , C07F5/00 , C07K16/46
CPC分类号： A61K51/1093 , A61K51/0497 , A61K51/088
摘要： The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, a COX-2 inhibitor, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.
摘要翻译：本发明在一般意义上提供了使用与靶向配体缀合的N 2 S 2 N 2螯合物的化合物的新标记策略，其中靶向配体是疾病细胞周期靶向化合物，肿瘤血管生成靶向配体，肿瘤凋亡靶向配体，疾病受体靶向配体，氨磷汀，血管抑素，单克隆抗体C225，单克隆抗体CD31，单克隆抗体CD40，卡培他滨，COX-2抑制剂，脱氧胞苷，富勒烯，赫赛汀，人血清白蛋白，乳糖，促黄体激素，吡哆醛，喹唑啉，沙利度胺，转铁蛋白或三甲基赖氨酸。本发明还涉及使用目的化合物的试剂盒，以及使用本发明化合物评价感兴趣剂的药理学的方法。

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