公开(公告)号：US20040198962A1

公开(公告)日：2004-10-07

申请号：US10625047

申请日：2003-07-22

Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

Inventor： Claude F. Meares ,  Todd M. Corneillie

IPC: A61K039/395 ,  C07K016/46

CPC classification number: C07K16/1282 ,  C07K16/44 ,  C07K2317/31 ,  C07K2317/55 ,  G01N33/574

Abstract: The present invention provides antibodies comprising an antigen recognition domain that specifically binds to a metal chelate: mutant antibodies comprising a reactive site not present in the wild-type of the antibody, wherein the reactive site is in a position proximate to or within the antigen recognition domain; and methods of using such antibodies to diagnose and treat disease.

Abstract translation: 本发明提供了包含与金属螯合物特异性结合的抗原识别结构域的抗体：包含在野生型抗体中不存在的反应性位点的突变抗体，其中反应位点处于接近或在抗原识别内的位置 域; 以及使用这些抗体诊断和治疗疾病的方法。

公开(公告)号：US20040180054A1

公开(公告)日：2004-09-16

申请号：US10807732

申请日：2004-03-24

Applicant: Hanmi Pharm. Co., Ltd.

Inventor： Young-Min Kim ,  Dae-Jin Kim ,  Sung-Min Bae ,  Chang-Ki Lim ,  Se-Chang Kwon ,  Gwan-Sun Lee

IPC: A61K039/395 ,  C12P021/04 ,  C07K016/46

CPC classification number: C07K16/00 ,  A61K2039/505 ,  C07K2317/41

Abstract: A protein conjugate having a prolonged in vivo half-life of a physiological activity, comprising i) a physiologically active polypeptide, ii) a non-peptidic polymer, and iii) an immunoglobulin, is useful for the development of a polypeptide drug due to the enhanced in vivo stability and prolonged half-life in blood, while reducing the possibility of inducing an immune response.

Abstract translation: 具有延长的生理活性的体内半衰期的蛋白质缀合物，其包含i）生理活性多肽，ii）非肽聚合物和iii）免疫球蛋白，可用于开发多肽药物，因为 增强血液中的体内稳定性和延长的半衰期，同时降低诱导免疫反应的可能性。

公开(公告)号：US20040175824A1

公开(公告)日：2004-09-09

申请号：US10761593

申请日：2004-01-21

Inventor： Lee-Hwei K. Sun ,  Bill N. C. Sun ,  Cecily R. Y. Sun

IPC: C12N005/06 ,  C07K016/46

CPC classification number: C07K14/505 ,  A61K38/00 ,  C07K2317/52 ,  C07K2319/00 ,  C07K2319/30

Abstract: Fc fusion proteins of human EPO with high biological activities relative to rHuEPO on a molar basis are disclosed. The HuEPO-L-vFc fusion protein comprises HuEPO, a flexible peptide linker of about 20 or fewer amino acids, and a human IgG Fc variant. The Fc variant is of a non-lytic nature and shows minimal undesirable Fc-mediated side effects. A method is also disclosed to make or produce such fusion proteins at high expression levels. Such HuEPO-L-vFc fusion proteins exhibit extended serum half-life and increased biological activities, leading to improved pharmacokinetics and pharmacodynamics, thus fewer injections will be needed within a period of time.

Abstract translation: 公开了以摩尔计相对于rHuEPO具有高生物活性的人EPO的Fc融合蛋白。 HuEPO-L-vFc融合蛋白包含HuEPO，约20个或更少氨基酸的柔性肽接头和一个人IgG Fc变体。 Fc变体具有非溶解性质并且显示出最小的不期望的Fc介导的副作用。 还公开了以高表达水平制备或产生这种融合蛋白的方法。 这种HuEPO-L-vFc融合蛋白表现出延长的血清半衰期和增加的生物活性，导致改善的药代动力学和药效学，因此在一段时间内将需要更少的注射。

公开(公告)号：US20040171814A1

公开(公告)日：2004-09-02

申请号：US10713248

申请日：2003-11-13

Inventor： Jennie P. Mather ,  Ronghao Li ,  Tony W. Liang

IPC: C07K016/30 ,  C07K016/46 ,  A61K039/395

CPC classification number: C07K16/30 ,  C07K2317/73 ,  C07K2317/77

Abstract: Provided herein is disclosure about the identification and characterization of disease and cancer associated antigen PIPA. The invention also provides a family of monoclonal antibodies that bind to antigen PIPA, and methods of diagnosing and treating various human cancers and diseases that express PIPA.

Abstract translation: 本文提供关于疾病和癌症相关抗原PIPA的鉴定和表征的公开。 本发明还提供了结合抗原PIPA的单克隆抗体家族，以及诊断和治疗表达PIPA的各种人类癌症和疾病的方法。

公开(公告)号：US20040166058A1

公开(公告)日：2004-08-26

申请号：US10703405

申请日：2003-11-07

Applicant: Board of Regents, The University of Texas System ,  Cell>Point LLC

Inventor： David J. Yang ,  Dong-Fang Yu ,  Chang-Sok Oh ,  Jerry L. Bryant JR.

IPC: A61K051/00 ,  C07K016/46 ,  C07F005/00

CPC classification number: C07F13/005 ,  A61K51/04 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0487 ,  A61K51/0491 ,  A61K51/08 ,  A61K51/081 ,  A61K51/088 ,  A61K51/1027 ,  A61K51/1093

Abstract: 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, COX-2, 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.

Abstract translation: 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，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， ，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。

公开(公告)号：US20040142451A1

公开(公告)日：2004-07-22

申请号：US10746678

申请日：2003-12-23

Applicant: Nanogen Recognomics GmbH

Inventor： Christian Miculka ,  Norbert Windhab ,  Albert Eschenmoser ,  Stefan Scherer ,  Gerhard Quinkert

IPC: C12N007/01 ,  C07K014/705 ,  C07K016/46

CPC classification number: C12Q1/68

Abstract: The invention relates to conjugates including at least one linker, a biomolecule coupled to the linker, and cyclohexane derivatives of the following formula: 1 and oligomers thereof

Abstract translation: 本发明涉及包含至少一个接头，与接头连接的生物分子和下式的环己烷衍生物的共轭物：及其低聚物

公开(公告)号：US20040121405A1

公开(公告)日：2004-06-24

申请号：US10474042

申请日：2003-10-15

Inventor： Bernard S. Green

IPC: G01N033/53 ,  C07K016/46 ,  C08B037/00

CPC classification number: G01N33/531 ,  G01N2600/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20040120891A1

公开(公告)日：2004-06-24

申请号：US10655756

申请日：2003-09-05

Inventor： Craig Hill ,  Stephen B. Kahl ,  Robert R. Webb ,  Constance A. McKee

IPC: A61K051/00 ,  C12P019/14 ,  A61K039/395 ,  C07K014/52 ,  C07K016/46

CPC classification number: C07K14/48 ,  A61K47/6425 ,  A61K47/6807

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20040071711A1

公开(公告)日：2004-04-15

申请号：US10416090

申请日：2003-10-15

Inventor： Roy Bicknell ,  Lukasz Huminiecki

IPC: A61K039/395 ,  C07K016/46

CPC classification number: A61K9/127 ,  A61K2039/505 ,  C07K14/70503 ,  C07K16/2803 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/136

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20040063912A1

公开(公告)日：2004-04-01

申请号：US10622108

申请日：2003-07-17

Applicant: The Brigham and Women's Hospital, Inc. ,  Children's Medical Center Corporation ,  Brandeis University ,  Syntonix Pharmaceuticals, Inc.

Inventor： Richard S. Blumberg ,  Wayne I. Lencer ,  Neil E. Simister ,  Alan J. Bitonti

IPC: C07K014/54 ,  C07K016/46

CPC classification number: A61K9/0073 ,  A61K9/0078 ,  C07K19/00 ,  C07K2319/00

Abstract: 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.

Abstract translation: 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。