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1. 发明申请

WO2004045642A1 USE OF MULTI-SPECIFIC, NON-COVALENT COMPLEXES FOR TARGETED DELIVERY OF THERAPEUTICS 审中-公开
标题翻译：多特异性非共价复合物的使用用于定向递送治疗药物
公开(公告)号：WO2004045642A1
公开(公告)日：2004-06-03
申请号：PCT/GB2003/004994
申请日：2003-11-17
申请人： IMMUNOMEDICS, INC. , MCCALL, John, Douglas , GRIFFITHS, Gary, L. , GOVINDAN, Serengulam, V. , HANSEN, Hans, J.
发明人： GRIFFITHS, Gary, L. , GOVINDAN, Serengulam, V. , HANSEN, Hans, J.
IPC分类号： A61K39/395
CPC分类号： B82Y5/00 , A61K45/06 , A61K47/6899 , C07K16/3007 , C07K16/44 , C07K2317/31 , C07K2317/54 , C07K2317/55
摘要： The invention relates to a method for treating target cells, tissues or pathogens in a subject, comprising administering a non-covalently bound complex which comprises a multispecific targeting protein and a hapten-enzyme covalent conjugate. The invention further relates to kits comprising the non-covalently bound complex or the components to prepare the complex.
摘要翻译：本发明涉及一种用于治疗受试者中靶细胞，组织或病原体的方法，包括施用包含多特异性靶向蛋白质和半抗原酶共价缀合物的非共价结合复合物。本发明还涉及包含非共价结合的复合物或组分以制备复合物的试剂盒。

2. 发明申请

WO0202150A8 STABLE RADIOIODINE CONJUGATES AND METHODS FOR THEIR SYNTHESIS 审中-公开
标题翻译：稳定的放射性素结合物及其合成方法
公开(公告)号：WO0202150A8
公开(公告)日：2003-01-16
申请号：PCT/US0120764
申请日：2001-06-29
申请人： IMMUNOMEDICS INC , GOVINDAN SERENGULAM V
发明人： GOVINDAN SERENGULAM V
IPC分类号： A61K51/04 , A61K51/08 , A61K51/10 , C07H3/04 , C07K1/107 , G01N33/543
CPC分类号： A61K51/088 , A61K51/0491 , A61K51/10 , A61K51/1093 , C07H3/04 , C07K1/1077 , G01N33/543
摘要： Methods are described for conjugating radioiodinated peptides to non-metabolizable carbohydrates with improved yields and qualities of conjugates. Radioiodinated residualizing antibody conjugates comprising a carbohydrate-appended peptide are also provided. The instant radioiodinated residualizing antibody conjugates are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
摘要翻译：描述了将放射性碘化肽与不可代谢的碳水化合物缀合的方法，其具有改善的缀合物的产率和质量。还提供了包含碳水化合物附加肽的放射性碘化残留抗体缀合物。瞬时放射性碘化残留抗体缀合物在体内特别稳定，并且适用于放射免疫检测和放射免疫治疗。

3. 发明申请

WO9808548A2 STABLE RADIOIODINE CONJUGATES AND METHODS FOR THEIR SYNTHESIS 审中-公开
标题翻译：稳定的放射性素结合物及其合成方法
公开(公告)号：WO9808548A2
公开(公告)日：1998-03-05
申请号：PCT/US9714998
申请日：1997-08-27
申请人： IMMUNOMEDICS INC , GOVINDAN SERENGULAM V , GRIFFITHS GARY L
发明人： GOVINDAN SERENGULAM V , GRIFFITHS GARY L
IPC分类号： A61K51/00 , A61K38/00 , A61K39/395 , A61K51/08 , A61P43/00 , C07H3/04 , C07K1/107
CPC分类号： A61K51/1069 , A61K51/1093 , C07H3/04 , C07K1/1077
摘要： Methods are described for conjugating radioiodinated peptides or carbohydrate structures to proteins with improved yields and qualities of conjugates. In one method, specially designed radioiodinated bifunctional peptides containing nonmetabolizable amide bonds are coupled to antibodies. In a second method, radioiodinated nonmetabolizable bifunctional peptides, which also contain aminopolycarboxylates, are coupled to antibodies. In a third method, radioiodinated bifunctional aminopolycarboxylates are coupled to antibodies. In a fourth method, a hydrazide-appended antibody is coupled to a radioiodinated carbohydrate, or a thiolated antibody is coupled to a hydrazide-appended and radioiodinated carbohydrate. In a fifth method, a monoderivatized cyanuric chloride is used to conjugate thiolated antibody. Radioiodinated residualizing antibody conjugates made by these methods are particularly stable in vivo and are suitable for radioimmunodetection and radioimmunotherapy.
摘要翻译：描述了将放射性碘化肽或碳水化合物结构与缀合物的产率和质量提高的蛋白质缀合的方法。在一种方法中，将特异设计的含有非代谢性酰胺键的放射性碘化双功能肽与抗体偶联。在第二种方法中，也含有氨基多羧酸盐的放射性碘化的不可代谢的双功能肽与抗体偶联。在第三种方法中，将放射性碘化双官能氨基多羧酸盐与抗体偶联。在第四种方法中，将酰肼附着的抗体与放射性碘化碳水化合物偶联，或硫醇化抗体与酰肼附着和放射性碘化碳水化合物偶联。在第五种方法中，使用monoderivatized氰尿酰氯来缀合硫醇化抗体。通过这些方法制备的放射性碘化残留抗体缀合物在体内特别稳定，适用于放射免疫检测和放射免疫治疗。

4. 发明申请

WO9930745A3 DOTA-BIOTIN DERIVATIVES 审中-公开
标题翻译： DOTA生物衍生物
公开(公告)号：WO9930745A3
公开(公告)日：2000-01-13
申请号：PCT/US9826579
申请日：1998-12-15
申请人： IMMUNOMEDICS INC , GRIFFITHS GARY L , HANSEN HANS , GOVINDAN SERENGULAM V
发明人： GRIFFITHS GARY L , HANSEN HANS , GOVINDAN SERENGULAM V
IPC分类号： A61K41/00 , A61K47/48 , A61K49/08 , A61K51/04 , A61K51/10 , G01N33/531 , G01N33/534 , G01N33/574 , G01N33/68 , A61K51/00
CPC分类号： A61K49/10 , A61K41/0095 , A61K47/665 , A61K47/6898 , A61K49/085 , A61K51/0497 , A61K51/1048 , A61K51/1093 , A61K2121/00 , A61K2123/00 , B82Y5/00 , G01N33/531 , G01N33/534 , G01N33/574 , G01N33/686
摘要： A radionuclide-chelator conjugate composition for detecting and/or treating lesions in a patient in a pre-targeting protocol which comprises pre-targeting the target cell, tissue, or pathogen with a substrate, using a targeting protein that specifically binds a marker substance on the target cell, tissue, or pathogen and to which the substrate is directly or indirectly bound; parenterally injecting the detection or therapeutic composition of the invention which comprises a chelate conjugate of biotin, a chelator, and a chelatable detection or therapeutic agent, and allowing the compsition to accrete at the targeted cell, tissue, or pathogen; wherein the chelate conjugate is purified by chromatography after chelate formation, or further comprises a blood transit-modifying linker or addend that is covalently bound within the chelate conjugate, or both; and using the detection or therapeutic agent to detect or treat the targeted cell, tissue, or pathogen.
摘要翻译： 1.一种放射性核素 - 螯合剂缀合物组合物，其用于在预靶向方案中检测和/或治疗患者的损伤，其包括使用特异性结合标记物质的靶向蛋白将靶标细胞，组织或病原体用靶基因靶细胞，组织或病原体，底物直接或间接结合在其上; 肠胃外注射本发明的检测或治疗组合物，其包含生物素的螯合缀合物，螯合剂和可螯合的检测或治疗剂，并允许该组合物在靶细胞，组织或病原体上进入; 其中所述螯合物缀合物在螯合形成之后通过色谱法纯化，或进一步包含共转运结合在螯合物缀合物内的血液转运修饰接头或加成物，或两者; 并使用检测或治疗剂来检测或治疗靶细胞，组织或病原体。

5. 发明申请

WO1998004917A1 BORON NEUTRON CAPTURE THERAPY USING PRE-TARGETING METHODS 审中-公开
标题翻译：使用预定方法进行BORON NEUTRON CAPTURE治疗
公开(公告)号：WO1998004917A1
公开(公告)日：1998-02-05
申请号：PCT/US1997012558
申请日：1997-07-23
申请人： IMMUNOMEDICS INC. , GRIFFITHS, Gary, L. , GOVINDAN, Serengulam, V.
发明人： IMMUNOMEDICS INC.
IPC分类号： G01N33/53
CPC分类号： B82Y5/00 , A61K41/0095 , A61K47/665 , A61K47/6898 , A61K51/1078 , G01N33/534 , G01N33/574
摘要： The present invention provides a method for targeting boron atoms to tumor cells in a patient. The method comprises the steps of: (A) administering a targeting composition comprising a conjugate of a first member of a binding pair and an antibody, wherein the antibody selectively binds to antigens produced by or associated with the tumor cells, and allowing the conjugate to localize at said tumor cells; (B) optionally, administering a clearing composition, and allowing the clearing composition to clear non-localized conjugate from circulation; (C) administering a boron-containing compound comprising a conjugate comprising a complementary member of said binding pair and boron atoms, and allowing the compound to localize at the tumor cells. The method may further comprise the step of irradiating the boron atoms of the boron compound, thereby effecting BNCT of the tumor cells. Compositions and kits for carrying out the method also are provided.
摘要翻译：本发明提供了一种将硼原子靶向患者肿瘤细胞的方法。该方法包括以下步骤：（A）施用包含结合对的第一个成员和抗体的缀合物的靶向组合物，其中所述抗体选择性地结合由肿瘤细胞产生或与肿瘤细胞相关的抗原，并且允许缀合物在所述肿瘤细胞上定位; （B）任选地，施用清除组合物，并使清除组合物从循环中清除非局部缀合物; （C）施用含有包含所述结合对的互补成员和硼原子的缀合物的含硼化合物，并使化合物定位于肿瘤细胞。该方法还可以包括照射硼化合物的硼原子，从而实现肿瘤细胞的BNCT的步骤。还提供了用于实施该方法的组合物和试剂盒。

6. 发明申请

WO2010093395A1 IMMUNOCONJUGATES WITH AN INTRACELLULARLY-CLEAVABLE LINKAGE 审中-公开
标题翻译：免疫球蛋白与细胞内可清除的连接
公开(公告)号：WO2010093395A1
公开(公告)日：2010-08-19
申请号：PCT/US2009/066371
申请日：2009-12-02
申请人： IMMUNOMEDICS, INC. , GOVINDAN, Serengulam, V. , MOON, Sung-Ju , GOLDENBERG, David, M.
发明人： GOVINDAN, Serengulam, V. , MOON, Sung-Ju , GOLDENBERG, David, M.
IPC分类号： A61K39/44 , C12P21/08
CPC分类号： A61K47/6803 , A61K31/4745 , A61K45/06 , A61K47/6841 , A61K47/6849 , A61K47/6851 , A61K47/6853 , A61K47/6855 , A61K47/6857 , A61K47/6861 , A61K47/6889 , A61K2039/505 , A61N5/10 , C07D491/22 , C07K16/1063 , C07K16/18 , C07K16/2803 , C07K16/2833 , C07K16/2863 , C07K16/2887 , C07K16/30 , C07K16/303 , C07K16/3046 , C07K16/3076 , C07K16/3092 , C07K2317/21 , C07K2317/24 , C07K2317/31 , C07K2317/40 , C07K2317/52 , C07K2317/53 , C07K2317/94 , Y02A50/394 , Y02A50/401 , Y02A50/403 , Y02A50/412 , Y02A50/473 , Y02A50/478
摘要： The present invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a therapeutic moiety, and further relates to processes for making and using the conjugates.
摘要翻译：本发明涉及具有改善靶向各种含有靶向部分（例如抗体或抗体片段）的病变细胞，接头和治疗部分的能力的治疗性缀合物，还涉及制备和使用缀合物的方法。

7. 发明申请

WO2009100194A3 CAMPTOTHECIN-BINDING MOIETY CONJUGATES 审中-公开
公开(公告)号：WO2009100194A3
公开(公告)日：2009-08-13
申请号：PCT/US2009/033182
申请日：2009-02-05
申请人： IMMUNOMEDICS, INC. , GOVINDAN, Serengulam V. , GOLDENBERG, David M. , MOON, Sung-ju
发明人： GOVINDAN, Serengulam V. , GOLDENBERG, David M. , MOON, Sung-ju
IPC分类号： A61K39/00
摘要： The invention relates to therapeutic conjugates with improved ability to target various diseased cells containing a targeting moiety (such as an antibody or antibody fragment), a linker and a camptothecin as a therapeutic moiety, and further relates to processes for making and using the said conjugates.

8. 发明申请

WO2005084179A2 IMPROVED METHOD FOR PREPARING CONJUGATES OF PROTEINS AND CHELATING AGENTS 审中-公开
标题翻译：制备蛋白质和螯合剂结合物的改进方法
公开(公告)号：WO2005084179A2
公开(公告)日：2005-09-15
申请号：PCT/US2004/040046
申请日：2004-12-01
申请人： IMMUNOMEDICS, INC. , GRIFFITHS, Gary L. , GOVINDAN, Serengulam V.
发明人： GRIFFITHS, Gary L. , GOVINDAN, Serengulam V.
IPC分类号： A61K51/00 , A61K51/10 , C07K14/52 , C07K14/525 , C07K14/54 , C07K16/46
CPC分类号： A61K51/1027 , A61K51/0482 , A61K51/1045
摘要： Improved synthesis methods are provided for preparing conjugates of proteins and chelating agents. In the synthesis methods, non-stable bonds are hydrolyzed after the conjugate is synthesized, for example by treating the conjugate with a quenching agent. The synthesis method provides conjugates that are substantially free of non-stable bonds between the protein and the chelating agent, such that the chelating agent is less likely to dissociate with the conjugate after the conjugate has been stored for extended periods. The conjugate may be useful for therapeutic or diagnostic methods.
摘要翻译：提供改进的合成方法用于制备蛋白质和螯合剂的缀合物。在合成方法中，在合成共轭物后，例如通过用猝灭剂处理缀合物，非稳定键被水解。合成方法提供基本上不含蛋白质和螯合剂之间非稳定键的缀合物，使得螯合剂在缀合物长时间储存后不太可能与缀合物解离。缀合物可用于治疗或诊断方法。

9. 发明申请

WO2008088658A3 POLYMERIC CARRIERS OF THERAPEUTIC AGENTS AND RECOGNITION MOIETIES FOR ANTIBODY-BASED TARGETING OF DISEASE SITES 审中-公开
标题翻译：治疗药物的聚合物载体和基于抗病基因治疗疾病的认可机构
公开(公告)号：WO2008088658A3
公开(公告)日：2008-11-20
申请号：PCT/US2007088308
申请日：2007-12-20
申请人： IMMUNOMEDICS INC , GOVINDAN SERENGULAM V , MOON SUNG-JU , GOLDENBERG DAVID M , CHANG CHIEN-HSING
发明人： GOVINDAN SERENGULAM V , MOON SUNG-JU , GOLDENBERG DAVID M , CHANG CHIEN-HSING
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/556 , A61K47/61 , A61K47/6425 , A61K47/645 , A61K47/65 , A61K47/665 , A61K47/6835 , A61K47/6897 , A61K47/6951
摘要： The present invention concerns methods and compositions for delivery of therapeutic agents to target cells, tissues or organisms. In preferred embodiments, the therapeutic agents are delivered in the form of therapeutic-loaded polymers that may comprise many copies of one or more therapeutic agents. In more preferred embodiments, the polymer may be conjugated to a peptide moiety that contains one or more haptens, such as HSG. The agent-polymer-peptide complex may be delivered to target cells by, for example, a pre-targeting technique utilizing bispecific or multispecific antibodies or fragments, having at least one binding arm that recognizes the hapten and at least a second binding arm that binds specifically to a disease or pathogen associated antigen, such as a tumor associated antigen. Methods for synthesizing and using such therapeutic-loaded polymers and their conjugates are provided.
摘要翻译：本发明涉及用于将治疗剂递送至靶细胞，组织或生物体的方法和组合物。在优选的实施方案中，治疗剂以治疗负荷聚合物的形式递送，其可以包含许多拷贝的一种或多种治疗剂。在更优选的实施方案中，聚合物可以与含有一种或多种半抗原如HSG的肽部分缀合。药剂 - 聚合物 - 肽复合物可以通过例如利用双特异性或多特异性抗体或片段的预靶向技术递送至靶细胞，所述双特异性或多特异性抗体或片段具有识别半抗原的至少一个结合臂和至少一个结合的结合臂具体涉及疾病或病原体相关抗原，例如肿瘤相关抗原。提供了合成和使用这种治疗负载型聚合物及其共轭物的方法。

10. 发明申请

WO2008088658A2 POLYMERIC CARRIERS OF THERAPEUTIC AGENTS AND RECOGNITION MOIETIES FOR ANTIBODY-BASED TARGETING OF DISEASE SITES 审中-公开
标题翻译：治疗药物的聚合物载体和用于基于抗体的疾病靶点瞄准的识别时机
公开(公告)号：WO2008088658A2
公开(公告)日：2008-07-24
申请号：PCT/US2007/088308
申请日：2007-12-20
申请人： IMMUNOMEDICS, INC. , GOVINDAN, Serengulam V. , MOON, Sung-ju , GOLDENBERG, David M. , CHANG, Chien-hsing
发明人： GOVINDAN, Serengulam V. , MOON, Sung-ju , GOLDENBERG, David M. , CHANG, Chien-hsing
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/556 , A61K47/61 , A61K47/6425 , A61K47/645 , A61K47/65 , A61K47/665 , A61K47/6835 , A61K47/6897 , A61K47/6951
摘要： The present invention concerns methods and compositions for delivery of therapeutic agents to target cells, tissues or organisms. In preferred embodiments, the therapeutic agents are delivered in the form of therapeutic-loaded polymers that may comprise many copies of one or more therapeutic agents. In more preferred embodiments, the polymer may be conjugated to a peptide moiety that contains one or more haptens, such as HSG. The agent-polymer-peptide complex may be delivered to target cells by, for example, a pre-targeting technique utilizing bispecific or multispecific antibodies or fragments, having at least one binding arm that recognizes the hapten and at least a second binding arm that binds specifically to a disease or pathogen associated antigen, such as a tumor associated antigen. Methods for synthesizing and using such therapeutic-loaded polymers and their conjugates are provided.
摘要翻译：本发明涉及用于将治疗剂递送至靶细胞，组织或生物体的方法和组合物。在优选的实施方案中，治疗剂以可包含一种或多种治疗剂的许多拷贝的治疗负荷聚合物的形式递送。在更优选的实施方案中，聚合物可以缀合至含有一种或多种半抗原如HSG的肽部分。可通过例如利用双特异性或多特异性抗体或片段的预靶向技术将试剂 - 聚合物 - 肽复合物递送至靶细胞，所述双特异性或多特异性抗体或片段具有至少一个识别半抗原的结合臂和至少第二个结合臂，具体涉及疾病或病原体相关抗原，如肿瘤相关抗原。提供了用于合成和使用这种负载治疗的聚合物及其偶联物的方法。

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