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1. 发明申请

US20060034759A1 Production and use of novel peptide-based agents with bispecific antibodies 有权
公开(公告)号：US20060034759A1
公开(公告)日：2006-02-16
申请号：US11198846
申请日：2005-08-08
申请人： David Goldenberg , Hans Hansen , Shui-on Leung , William McBride , Zhengxing Qu
发明人： David Goldenberg , Hans Hansen , Shui-on Leung , William McBride , Zhengxing Qu
IPC分类号： A61K51/00 , C07K7/06 , C07K16/46
CPC分类号： A61K51/1048 , A61K47/665 , A61K47/6879 , A61K51/1063 , A61K2039/505 , B82Y5/00 , C07K5/0215 , C07K5/1016 , C07K5/1019 , C07K7/06 , C07K16/18 , C07K16/3007 , C07K16/3046 , C07K16/44 , C07K16/468 , C07K2317/12 , C07K2317/13 , C07K2317/24 , C07K2317/31 , C07K2317/55 , C07K2317/622 , C07K2317/64 , C07K2319/00
摘要： The present invention relates to a bi-specific antibody or antibody fragment having at least one arm that specifically binds a targeted tissue and at least one other arm that specifically binds a targetable construct. The targetable construct comprises a carrier portion which comprises or bears at least one epitope recognizable by at least one arm of said bi-specific antibody or antibody fragment. The targetable construct further comprises one or more therapeutic or diagnostic agents or enzymes. The invention provides constructs and methods for producing the bi-specific antibodies or antibody fragments, as well as methods for using them.

2. 发明申请

US20060104899A1 Production and use of novel peptide-based agents for use with bi-specific antibodies 有权
公开(公告)号：US20060104899A1
公开(公告)日：2006-05-18
申请号：US11216033
申请日：2005-09-01
申请人： Hans Hansen , Gary Griffiths , Shui-on Leung , William McBride , Zhengxing Qu
发明人： Hans Hansen , Gary Griffiths , Shui-on Leung , William McBride , Zhengxing Qu
IPC分类号： A61K51/00 , A61K39/395 , A61K49/16
CPC分类号： C07K16/468 , A61K47/6863 , A61K47/6899 , A61K51/1048 , A61K51/1063 , A61K2039/505 , B82Y5/00 , C07K16/18 , C07K16/30 , C07K16/3007 , C07K16/3046 , C07K16/44 , C07K2317/12 , C07K2317/13 , C07K2317/24 , C07K2317/31 , C07K2317/55 , C07K2317/622 , C07K2319/00
摘要： The present invention relates to a bi-specific antibody or antibody fragment having at least one arm that is reactive against a targeted tissue and at least one other arm that is reactive against a linker moiety. The linker moiety encompasses a hapten to which antibodies have been prepared. The antigenic linker is conjugated to one or more therapeutic or diagnostic agents or enzymes. The invention provides constructs and methods for producing the bispecific antibodies or antibody fragments, as well as methods for using them.

3. 发明申请

US20060140858A1 Drug pre-targeting by means of bi-specific antibodies and hapten constructs comprising a carrier peptide and the active agent(s) 审中-公开
标题翻译：通过双特异性抗体和包含载体肽和活性剂的半抗原构建体的药物预靶向，
公开(公告)号：US20060140858A1
公开(公告)日：2006-06-29
申请号：US10514632
申请日：2003-05-16
申请人： David Goldenberg , Hans Hansen , Shui-on Leung , William McBride , Zhengxing Gu
发明人： David Goldenberg , Hans Hansen , Shui-on Leung , William McBride , Zhengxing Gu
IPC分类号： A61K49/14 , A61K51/00 , C07K7/06
CPC分类号： A61K51/1048 , A61K47/665 , A61K47/6879 , A61K51/1063 , A61K2039/505 , B82Y5/00 , C07K5/0215 , C07K5/1016 , C07K5/1019 , C07K7/06 , C07K16/18 , C07K16/3007 , C07K16/3046 , C07K16/44 , C07K16/468 , C07K2317/12 , C07K2317/13 , C07K2317/24 , C07K2317/31 , C07K2317/55 , C07K2317/622 , C07K2317/64 , C07K2319/00
摘要： The present invention relates to targetable constructs which may be bound by a bi-specific antibody or antibody fragment having at least one arm that specifically binds a targeted tissue and at least one other arm that specifically binds the targetable construct. The targetable construct comprises a carrier portion which comprises or bears at least one epitope recognizable by at least one arm of said bi-specific antibody or antibody fragment. The targetable construct further comprises one or more therapeutic or diagnostic agents or enzymes. The invention provides constructs and methods for producing the targetable constructs and bi-specific antibodies or antibody fragments, as well as methods for using them.
摘要翻译：本发明涉及可靶向的构建体，其可以由具有特异性结合靶组织的至少一个臂的双特异性抗体或抗体片段和至少一个特异性结合可靶向构建体的其它臂结合。可靶向构建体包含载体部分，其包含或携带至少一个可被所述双特异性抗体或抗体片段的至少一个臂识别的表位。可靶向构建物还包含一种或多种治疗剂或诊断剂或酶。本发明提供用于产生可靶向构建体和双特异性抗体或抗体片段的构建体和方法，以及使用它们的方法。

4. 发明申请

US20050100543A1 Multivalent carriers of bi-specific antibodies 审中-公开
标题翻译：双特异性抗体的多价载体
公开(公告)号：US20050100543A1
公开(公告)日：2005-05-12
申请号：US10882151
申请日：2004-07-01
申请人： Hans Hansen , William McBride , Zhengxing Qu
发明人： Hans Hansen , William McBride , Zhengxing Qu
IPC分类号： A61K20060101 , A61K39/395 , A61K47/48 , A61K51/08 , A61K51/10 , C07K16/28 , C07K16/30 , C07K16/44 , C12N9/00
CPC分类号： C07K16/2887 , A61K47/6897 , A61K51/1027 , A61K51/1048 , A61K51/109 , A61K2039/505 , B82Y5/00 , C07K16/3007 , C07K2317/31 , C07K2317/622 , C07K2319/00 , C07K2319/01
摘要： Provided herein are targetable constructs that are multivalent carriers of bi-specific antibodies, i.e., each molecule of a targetable construct can serve as a carrier of two or more bi-specific antibodies. Also provided are targetable complexes formed by the association of a targetable construct with two or more bi-specific antibodies. The targetable constructs and targetable complexes of the invention are incorporated into biosensors, kits and pharmaceutical compositions, and are used in a variety of therapeutic and other methods.
摘要翻译：本文提供作为双特异性抗体的多价载体的可靶向构建体，即可靶向构建体的每个分子可以用作两种或更多种双特异性抗体的载体。还提供了通过可靶向构建体与两种或更多种双特异性抗体缔合形成的可靶向复合物。将本发明的可靶向构建体和可靶向复合物掺入生物传感器，试剂盒和药物组合物中，并且以多种治疗和其它方法使用。

5. 发明申请

US20050261170A1 Folate conjugates and complexes 审中-公开
标题翻译：叶酸共轭物和复合物
公开(公告)号：US20050261170A1
公开(公告)日：2005-11-24
申请号：US11040114
申请日：2005-01-24
申请人： Hans Hansen , William McBride , David Goldenberg , Edmund Rossi , Chien-Hsing Chang
发明人： Hans Hansen , William McBride , David Goldenberg , Edmund Rossi , Chien-Hsing Chang
IPC分类号： A61K47/48 , A61K48/00 , C07H21/02 , C07K14/47 , C07K14/705 , C12N9/22
CPC分类号： C12N9/22 , A61K33/24 , A61K38/00 , A61K38/19 , A61K45/06 , A61K47/551 , C07K14/705 , Y02A50/401 , Y02A50/411 , Y02A50/473 , Y02A50/478 , A61K2300/00
摘要： Disclosed are conjugates and complexes that include a folate receptor ligand and one or more therapeutic molecules, such as onconase or a variant thereof such as rapLR1. The conjugates and complexes may be useful as primary therapeutic agents, which may be administered with additional therapeutic or diagnostic agents. Also disclosed are kits that include the conjugates and complexes.
摘要翻译：公开了包含叶酸受体配体和一种或多种治疗分子（例如onconase或其变体）如rapLR1的缀合物和复合物。缀合物和复合物可用作主要治疗剂，其可以与另外的治疗剂或诊断剂一起施用。还公开了包含缀合物和复合物的试剂盒。

6. 发明申请

US20050002945A1 Therapeutic and diagnostic conjugates for use with multispecific antibodies 有权
标题翻译：用于多特异性抗体的治疗和诊断缀合物
公开(公告)号：US20050002945A1
公开(公告)日：2005-01-06
申请号：US10776470
申请日：2004-02-11
申请人： William McBride , David Goldenberg , Carl Noren , Hans Hansen
发明人： William McBride , David Goldenberg , Carl Noren , Hans Hansen
IPC分类号： A61K47/48 , A61K51/04 , A61K51/08 , A61K51/10 , C07K7/06 , C07K16/18 , C07K16/30 , C07K16/44 , C07K16/46 , A61K39/00
CPC分类号： A61K51/0497 , A61K47/665 , A61K51/04 , A61K51/0455 , A61K51/048 , A61K51/1048 , A61K51/1063 , A61K2039/505 , B82Y5/00 , C07K5/06078 , C07K5/1013 , C07K5/1016 , C07K5/1019 , C07K7/06 , C07K16/18 , C07K16/3007 , C07K16/3046 , C07K16/44 , C07K16/468 , C07K2317/12 , C07K2317/13 , C07K2317/24 , C07K2317/31 , C07K2317/55 , C07K2317/622 , C07K2319/00
摘要： Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or combinations of DTPA and HSG. The compound also includes an effector molecule which may be conjugated to one or more of the haptens, the spacer/carrier, or both. The effector molecule may be conjugated by a number of linkages including an ester linkage, an imino linkage, an amino linkage, a sulfide linkage, a thiosemicarbazone linkage, a semicarbazone linkage, an oxime linkage, an ether linkage, or combinations of these linkages. Also disclosed are methods of synthesizing the compounds and/or precursors of the compounds.
摘要翻译：公开了包含两个或多个通过间隔物或载体缀合的半抗原的化合物。半抗原可以包括二亚乙基三胺五乙酸（DTPA），组氨酰胺 - 琥珀酰 - 谷氨酰胺（HSG）或DTPA和HSG的组合。化合物还包括效应分子，其可以与一个或多个半抗原，间隔物/载体或两者结合。效应分子可以通过多个键连接，包括酯键，亚氨基键，氨基键，硫键，硫代缩氨基脲键，缩氨基脲键，肟键，醚键或这些键的组合。还公开了合成化合物的化合物和/或前体的方法。

7. 发明申请

US20050136001A1 Fluorinated carbohydrate conjugates 有权
标题翻译：氟化碳水化合物共轭物
公开(公告)号：US20050136001A1
公开(公告)日：2005-06-23
申请号：US10901441
申请日：2004-07-29
申请人： William McBride , David Goldenberg
发明人： William McBride , David Goldenberg
IPC分类号： A61K47/48 , A61K49/04 , A61K51/04 , A61K51/08 , C07H3/00 , C07K16/30 , C07K16/44 , A61K51/00 , C07K16/46
CPC分类号： C07H3/00 , A61K47/64 , A61K47/6879 , A61K47/6897 , A61K49/0433 , A61K49/085 , A61K49/14 , A61K51/0491 , A61K51/088 , B82Y5/00 , C07K16/3007 , C07K16/44 , C07K2317/55
摘要： Disclosed are novel conjugates that include fluorinated carbohydrate molecules and methods for synthesizing the conjugates. The fluorinated carbohydrate molecule may include a radioisotope. The method of synthesizing the conjugate is useful for labeling selected molecules, and the conjugates may be useful in diagnostic or therapeutic methods. Particularly, the conjugates may be useful in diagnostic or therapeutic kits.
摘要翻译：公开了包括氟化碳水化合物分子的新型缀合物和用于合成缀合物的方法。氟化碳水化合物分子可以包括放射性同位素。合成缀合物的方法可用于标记所选择的分子，并且缀合物可用于诊断或治疗方法。特别地，缀合物可用于诊断或治疗试剂盒。

8. 发明申请

US20060228357A1 Methods for generating stably linked complexes composed of homodimers, homotetramers or dimers of dimers and uses 有权
公开(公告)号：US20060228357A1
公开(公告)日：2006-10-12
申请号：US11389358
申请日：2006-03-24
申请人： Chien Chang , David Goldenberg , William McBride , Edmund Rossi
发明人： Chien Chang , David Goldenberg , William McBride , Edmund Rossi
IPC分类号： C12Q1/70 , G01N33/574 , A61K39/395 , C07K14/82 , C07K16/30 , C07K14/415 , A61K39/00 , C07K16/46
CPC分类号： C12N9/12 , B82Y5/00 , B82Y10/00 , C07K16/18 , C07K16/2803 , C07K16/2887 , C07K16/3007 , C07K16/3092 , C07K2317/31 , C07K2317/55 , C07K2319/00 , C07K2319/70 , C12Y207/11011
摘要： The present invention concerns methods and compositions for stably tethered structures of defined compositions, which may have multiple functionalities and/or binding specificities. Particular embodiments concern homodimers comprising monomers that contain a dimerization and docking domain attached to a precursor. The precursors may be virtually any molecule or structure, such as antibodies, antibody fragments, antibody analogs or mimetics, aptamers, binding peptides, fragments of binding proteins, known ligands for proteins or other molecules, enzymes, detectable labels or tags, therapeutic agents, toxins, pharmaceuticals, cytokines, interleukins, interferons, radioisotopes, proteins, peptides, peptide mimetics, polynucleotides, RNAi, oligosaccharides, natural or synthetic polymeric substances, nanoparticles, quantum dots, organic or inorganic compounds, etc. Other embodiments concern tetramers comprising a first and second homodimer, which may be identical or different. The disclosed methods and compositions provide a facile and general way to obtain homodimers, homotetramers and heterotetramers of virtually any functionality and/or binding specificity.

9. 发明申请

US20070086942A1 Methods and compositions for generating bioactive assemblies of increased complexity and uses 有权
标题翻译：用于生成增加复杂性和用途的生物活性组件的方法和组合物
公开(公告)号：US20070086942A1
公开(公告)日：2007-04-19
申请号：US11478021
申请日：2006-06-29
申请人： Chien Chang , David Goldenberg , William McBride , Edmund Rossi
发明人： Chien Chang , David Goldenberg , William McBride , Edmund Rossi
IPC分类号： A61K51/00 , C12Q1/68 , G01N33/53 , G01N33/554 , C07K16/46
CPC分类号： A61K47/48438 , A61K31/00 , A61K38/00 , A61K47/48415 , A61K47/48484 , A61K47/485 , A61K47/48538 , A61K47/48546 , A61K47/48561 , A61K47/48569 , A61K47/6811 , A61K47/6817 , A61K47/6829 , A61K47/6833 , A61K47/6843 , A61K47/6845 , A61K47/6849 , A61K47/6851 , A61K2039/505 , B82Y5/00 , B82Y10/00 , B82Y15/00 , C07K14/475 , C07K16/18 , C07K16/22 , C07K16/28 , C07K16/2803 , C07K16/2833 , C07K16/2851 , C07K16/2863 , C07K16/2881 , C07K16/2887 , C07K16/2896 , C07K16/3007 , C07K16/3092 , C07K16/32 , C07K2317/31 , C07K2317/55 , C07K2317/76 , C07K2319/30 , C07K2319/35 , C07K2319/70 , C07K2319/74 , C12N9/12 , C12N9/22 , C12N9/96 , C12Y207/11001 , G01N33/54353 , G01N33/588 , Y02A50/491
摘要： The present invention concerns methods and compositions for making and using bioactive assemblies of defined compositions, which may have multiple functionalities and/or binding specificities. In particular embodiments, the bioactive assembly is formed using dock-and-lock (DNL) methodology, which takes advantage of the specific binding interaction between dimerization and docking domains (DDD) and anchoring domains (AD) to form the assembly. In various embodiments, one or more effectors may be attached to a DDD or AD sequence. Complementary AD or DDD sequences may be attached to an adaptor module that forms the core of the bioactive assembly, allowing formation of the assembly through the specific DDD/AD binding interactions. Such assemblies may be attached to a wide variety of effector moieties for treatment, detection and/or diagnosis of a disease, pathogen infection or other medical or veterinary condition.
摘要翻译：本发明涉及用于制备和使用具有多种功能和/或结合特异性的限定组合物的生物活性组合物的方法和组合物。在特定的实施方案中，生物活性组件使用对接和锁定（DNL）方法形成，其利用二聚化和对接结构域（DDD）和锚定结构域（AD）之间的特异性结合相互作用形成组件。在各种实施方案中，一个或多个效应物可以连接到DDD或AD序列。互补AD或DDD序列可以连接到形成生物活性组件核心的适配器模块，从而允许通过特定的DDD / AD结合相互作用形成组装体。这些组合物可以连接到各种各样的效应部分，用于治疗，检测和/或诊断疾病，病原体感染或其他医学或兽医病症。

10. 发明申请

US20070142296A1 D-amino acid peptides 有权
标题翻译： D-氨基酸肽
公开(公告)号：US20070142296A1
公开(公告)日：2007-06-21
申请号：US11640557
申请日：2006-12-18
申请人： William McBride , David Goldenberg
发明人： William McBride , David Goldenberg
IPC分类号： A61K38/08 , C07K7/06 , A61K31/7048 , A61K31/704
CPC分类号： C07K5/0815 , A61K38/00 , A61K47/6897 , A61K49/0002 , A61K51/109 , B82Y5/00 , C07K5/1008 , C07K5/1016 , C07K5/1019 , C07K5/1021 , C07K7/06 , Y02A50/411
摘要： The present invention provides compounds of the formula X—R1-D-[Dpr, Orn or Lys](A)-R2(Z)-D-[Dpr, Orn or Lys](B)—R3(Y)—NR4R5; or R1(X)-D-[Dpr, Orn or Lys](A)-R2(Z)-D-[Dpr, Orn or Lys](B)—R3(Y)—NR4R5, in which X is a hard acid cation chelator, a soft acid cation chelator or Ac—, R1, R2 and R3 are independently selected from a covalent bond or one or more D-amino acids that can be the same or different, Y is a hard acid cation chelator, a soft acid cation chelator or absent, Z is a hard acid cation chelator, a soft acid cation chelator or absent, and A and B are haptens or hard acid cation chelators and can be the same or different, and R4 and R5 are independently selected from the group consisting of hard acid cation chelators, soft acid cation chelators, enzymes, therapeutic agents, diagnostic agents and H. The present invention also provides methods of using these compounds and kits containing the compounds.
摘要翻译：本发明提供式XR 1 -D- [Dpr，Orn或Lys]（A）-R 2（Z）-D- [Dpr，Orn 或Lys]（B）-R 3（Y）-NR 4 R 5; （X）-D- [Dpr，Orn或Lys]（A）-R 2（Z）-D- [Dpr，Orn或Lys]（ B）-R 3（Y）-NR 4 R 5，其中X是硬酸阳离子螯合剂，软酸阳离子螯合剂或Ac-，R 1，R 2和R 3独立地选自共价键或一个或多个D氨基酸，其可以 Y是硬酸阳离子螯合剂，软酸阳离子螯合剂或不存在，Z是硬酸阳离子螯合剂，软酸阳离子螯合剂或不存在，A和B是半抗原或硬酸阳离子螯合剂， R 4和R 5可以相同或不同，R 4和R 5独立地选自硬酸阳离子螯合剂，软酸阳离子螯合剂，酶，治疗剂，诊断剂和H.本发明还提供使用这些化合物和含有化合物的试剂盒的方法。

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