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11. 发明申请

US20040121405A1 Selective covalent-binding compounds having therapeutic diagnostic and analytical applications 审中-公开
标题翻译：具有治疗诊断和分析应用的选择性共价结合化合物
公开(公告)号：US20040121405A1
公开(公告)日：2004-06-24
申请号：US10474042
申请日：2003-10-15
发明人： Bernard S. Green
IPC分类号： G01N033/53 , C07K016/46 , C08B037/00
CPC分类号： G01N33/531 , G01N2600/00
摘要： Novel compounds are provided having enhanced affinity for a desired, preselected, target substance (a small molecule; a macromolecule such as a protein, a carbohydrate, a nucleic acid, a cell, a viral particle, etc.) by modification with chemical groups that allow these substances to form strong bonds, such as irreversible covalent bonds, with the desired target substance. These qualities of tight, specific binding are reminiscent of antibody-like affinity; hence the new substances are termed COBALT, an acronym for Covalent-Binding Antibody-Like Trap. The present invention includes a process wherein a target species is chosen and then, by synthetic chemical procedures and modifications, novel substances (COBALTs) are obtained that exhibit selective and covalent binding to the preselected target species. The applications of the COBALTs include diagnostic, analytical, therapeutic and industrial applications.
摘要翻译：通过用化学基团修饰，提供了对期望的，预选的靶物质（小分子，大分子如蛋白质，碳水化合物，核酸，细胞，病毒颗粒等）具有增强的亲和力的新型化合物，使这些物质与期望的目标物质形成强键，例如不可逆共价键。紧密，特异性结合的这些质量让人联想到抗体样亲和力; 因此新物质被称为COBALT，这是Covalent-Binding Antibody-Like Trap的缩写。本发明包括其中选择靶物种，然后通过合成化学方法和修饰获得与预选靶物种呈现选择性和共价结合的新物质（COBALT）的方法。 COBALT的应用包括诊断，分析，治疗和工业应用。

12. 发明申请

US20040120891A1 Compounds for intracellular delivery of therapeutic moieties to nerve cells 审中-公开
标题翻译：将治疗性部分细胞内递送给神经细胞的化合物
公开(公告)号：US20040120891A1
公开(公告)日：2004-06-24
申请号：US10655756
申请日：2003-09-05
发明人： Craig Hill , Stephen B. Kahl , Robert R. Webb , Constance A. McKee
IPC分类号： A61K051/00 , C12P019/14 , A61K039/395 , C07K014/52 , C07K016/46
CPC分类号： C07K14/48 , A61K47/6425 , A61K47/6807
摘要： The invention features compounds of the general formula: B-L-M where B is a binding agent capable of selectively binding to a nerve cell surface receptor and mediating absorption of the compound by the nerve cell; M is a moiety which performs a useful non-cytotoxic function when absorbed by a nerve cell, and can be a therapeutic moiety or an imaging moiety; and L is a linker coupling B to M. The invention also features methods of use of the compounds in, for example, treating conditions such as viral infections and pain, as well as in labeling nerve cells.
摘要翻译：本发明具有以下通式的化合物：B-L-M其中B是能够选择性结合神经细胞表面受体并介导神经细胞吸收化合物的结合剂; M是当被神经细胞吸收时可以执行有用的非细胞毒性功能的部分，并且可以是治疗部分或成像部分; 并且L是将B连接到M的接头。本发明还涉及在例如治疗病症如病毒感染和疼痛以及标记神经细胞中的化合物的使用方法。

13. 发明申请

US20040071711A1 Imaging, diagnosis and treatment of disease 有权
标题翻译：疾病的成像，诊断和治疗
公开(公告)号：US20040071711A1
公开(公告)日：2004-04-15
申请号：US10416090
申请日：2003-10-15
发明人： Roy Bicknell , Lukasz Huminiecki
IPC分类号： A61K039/395 , C07K016/46
CPC分类号： A61K9/127 , A61K2039/505 , C07K14/70503 , C07K16/2803 , C12Q1/6886 , C12Q2600/106 , C12Q2600/136
摘要： The present invention relates to endothelial cell-specific genes and encoded polypeptides and materials and uses thereof in the imaging, diagnosis and treatment of conditions involving the vascu lar endothelium.
摘要翻译：本发明涉及内皮细胞特异性基因和编码的多肽及其材料及其在成像，诊断和治疗涉及血管内皮的病症中的用途。

14. 发明申请

US20040063912A1 Central airway administration for systemic delivery of therapeutics 审中-公开
标题翻译：中枢气道管理系统性递送治疗
公开(公告)号：US20040063912A1
公开(公告)日：2004-04-01
申请号：US10622108
申请日：2003-07-17
申请人： The Brigham and Women's Hospital, Inc. , Children's Medical Center Corporation , Brandeis University , Syntonix Pharmaceuticals, Inc.
发明人： Richard S. Blumberg , Wayne I. Lencer , Neil E. Simister , Alan J. Bitonti
IPC分类号： C07K014/54 , C07K016/46
CPC分类号： A61K9/0073 , A61K9/0078 , C07K19/00 , C07K2319/00
摘要： The present invention relates to methods and products for the transepithelial systemic delivery of therapeutics. In particular, the invention relates to methods and compositions for the systemic delivery of therapeutics by administering an aerosol containing antibodies or conjugates of a therapeutic agent with an FcRn binding partner to epithelium of central airways of the lung. The methods and products are adaptable to a wide range of therapeutic agents, including proteins and polypeptides, nucleic acids, drugs, and others. In particular embodiments the conjugates are fusion proteins in which a therapeutic polypeptide is joined at its C terminal end through a peptide linker to the N terminal end of an immunoglobulin Fc gamma heavy chain, wherein the linker includes Glycine and Serine residues and is preferably 15 amino acids long. In one embodiment the fusion protein includes an interferon-alpha 2b (IFN-null2b) joined at its C terminal end through a peptide linker having a sequence Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser (SEQ ID NO:29) to the N terminal end of a human Fcnull1 heavy chain. The methods and products have the advantage of not requiring administration to the deep lung in order to effect systemic delivery.
摘要翻译：本发明涉及用于治疗的跨上皮系统递送的方法和产品。特别地，本发明涉及通过将含有治疗剂的抗体或缀合物与FcRn结合配偶体的气溶胶施用于肺的中央气道的上皮来全身递送治疗剂的方法和组合物。方法和产品适用于广泛的治疗剂，包括蛋白质和多肽，核酸，药物等。在具体实施方案中，缀合物是融合蛋白，其中治疗性多肽在其C末端通过肽接头连接到免疫球蛋白Fcγ重链的N末端，其中所述连接体包括甘氨酸和丝氨酸残基，并且优选为15个氨基酸长。在一个实施方案中，融合蛋白包括其C末端通过具有序列Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser-Gly-Gly-Gly-Gly-Ser- Gly-Gly-Gly-Gly-Ser（SEQ ID NO：29）至人Fcγm1重链的N末端。所述方法和产品具有不需要施用于深肺以实现系统递送的优点。

15. 发明申请

US20040048370A1 Cell targeting methods and compositions 有权
标题翻译：细胞靶向方法和组合物
公开(公告)号：US20040048370A1
公开(公告)日：2004-03-11
申请号：US10461887
申请日：2003-06-13
申请人： Case Western Reserve University
发明人： James E. Dennis , Arnold I. Caplan , Nir Cohen
IPC分类号： C12N005/08 , C07K016/46 , A61K045/00
CPC分类号： C12N5/0655 , A61K35/12 , C07K16/18 , C12N5/0006
摘要： In certain aspects, the invention relates to cell delivery compositions comprising a chondrogenic cell and a targeting moiety. Such compositions may be used, for example, in administering a targeted cell therapy to a subject.
摘要翻译：在某些方面，本发明涉及包含软骨形成细胞和靶向部分的细胞递送组合物。这样的组合物可以用于例如向受试者施用靶向细胞疗法。

16. 发明申请

US20040047865A1 Compositions and their uses 审中-公开
标题翻译：组合及其用途
公开(公告)号：US20040047865A1
公开(公告)日：2004-03-11
申请号：US10655405
申请日：2003-09-04
发明人： Richard Gareth Warner
IPC分类号： A61K039/395 , C07K016/46
CPC分类号： A61K47/643
摘要： A synthetic conjugate of a protein and a plurality of epitopes is useful in preventing hyperacute rejection of xenografts or at least in reducing the extent or the rate of rejection. It may also be useful in treating certain diseases.
摘要翻译：蛋白质和多个表位的合成缀合物可用于防止异种移植物的超急性排斥或至少在减少排斥程度或抑制率。它也可用于治疗某些疾病。

17. 发明申请

US20030198595A1 Use of bi-specific antibodies for pre-targeting diagnosis and therapy 有权
标题翻译：使用双特异性抗体进行预定位诊断和治疗
公开(公告)号：US20030198595A1
公开(公告)日：2003-10-23
申请号：US10150654
申请日：2002-05-17
申请人： IMMUNOMEDICS, INC.
发明人： David M. Goldenberg , Hans J. Hansen , Shui-On Leung , William J. McBride , Zhengxing Qu
IPC分类号： A61K051/00 , C07K016/46
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.
摘要翻译：本发明涉及具有特异性结合目标组织的至少一个臂的特异性抗体或抗体片段以及特异性结合可靶向构建体的至少一个其他臂。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。

18. 发明申请

US20030180305A1 Pharmaceuticals for the imaging of angiogenic disorders 失效
标题翻译：用于血管生成障碍成像的药物
公开(公告)号：US20030180305A1
公开(公告)日：2003-09-25
申请号：US10342081
申请日：2003-01-14
发明人： Milind Rajopadhye , D. Scott Edwards , John A. Barrett , Alan P. Carpenter JR. , Thomas D. Harris , Stuart J. Heminway , Shuang Liu , Prahlad R. Singh
IPC分类号： A61K039/395 , C07K016/46
CPC分类号： C07D401/14 , A61K38/00 , A61K45/06 , A61K49/0002 , A61K49/227 , A61K51/082 , A61K51/088 , C07D401/12 , C07K7/06 , C07K7/08 , C07K7/64
摘要： The present invention describes novel compounds of the formula:(Q)dnullLnnullCh,useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
摘要翻译：本发明描述了可用于癌症诊断和治疗的（Q）d-Ln-Ch的新型化合物，患者中肿瘤成像的方法和治疗患者癌症的方法。本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。药物由与血管发生期间上调的受体结合的靶向部分，任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。可成像部分是伽马射线或正电子发射放射性同位素，磁共振成像造影剂，X射线造影剂或超声造影剂。

19. 发明申请

US20030157056A1 Modified cytokines for use in cancer therapy 有权
公开(公告)号：US20030157056A1
公开(公告)日：2003-08-21
申请号：US10287811
申请日：2002-11-05
申请人： FONDAZIONE CENTRO SAN RAFFAELE DEL MONTE TABOR
发明人： Angelo Corti
IPC分类号： A61K048/00 , A61K038/19 , C07H021/04 , C07K016/46 , C07K014/525
CPC分类号： C07K5/1021 , A61K31/70 , A61K38/00 , A61K47/6813 , A61K47/6849 , C07K5/0819 , C07K14/525 , C07K14/57 , C07K2319/00
摘要： Cytokine derivatives capable of homing the tumoral vessels and the antigen presenting cells and the use thereof as antitumoral agents.

20. 发明申请

US20030152568A1 Methods for targeting cells that express fibroblast growth receptor-3 or -2 有权
标题翻译：靶向表达成纤维细胞生长受体-3或-2的细胞的方法
公开(公告)号：US20030152568A1
公开(公告)日：2003-08-14
申请号：US10354859
申请日：2003-01-29
发明人： James W. West
IPC分类号： A61K039/395 , C07K016/46
CPC分类号： C07K16/46
摘要： Fibroblast growth factor-18 (FGF-18) binds with FGF receptors-2 and -3. Compositions comprising an FGF-18 component can be used to target cells that express these receptors. Suitable targets include tumor cells that express constitutively activated forms of FGF receptors-2 and -3. For example, conjugates of FGF-18 and saporin can be used to target tumor cells that express FGF receptors-2 or -3, and to inhibit the proliferation of these cells.
摘要翻译：成纤维细胞生长因子-18（FGF-18）与FGF受体-2和-3结合。包含FGF-18组分的组合物可用于靶向表达这些受体的细胞。合适的靶标包括表达组成型活化形式的FGF受体-2和-3的肿瘤细胞。例如，FGF-18和saporin的缀合物可用于靶向表达FGF受体-2或-3的肿瘤细胞，并抑制这些细胞的增殖。

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