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149 条记录 (耗时 0.032 秒)

    Enzyme activated self-immolative n-substituted nitrogen mustard prodrugs
    41.
    发明申请
    Enzyme activated self-immolative n-substituted nitrogen mustard prodrugs 有权
    酶活化的自消除性取代的氮芥前体药物

    公开(公告)号：US20060069154A1

    公开(公告)日：2006-03-30

    申请号：US10526173

    申请日：2003-09-01

    申请人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Dan Niculescu-Duvaz

    发明人： Caroline Springer ,  Ion Niculescu-Duvaz ,  Dan Niculescu-Duvaz

    IPC分类号： A61K31/325 ,  C07C275/40

    CPC分类号： B82Y5/00 ,  A61K47/67 ,  A61K47/6899 ,  C07C275/32

    摘要： This invention pertains to certain enzyme (CPG2) activated self-immolative nitrogen mustard prodrugs, which are useful in enzyme prodrug therapy (EPT), such as ADEPT and GDEPT, for the treatment of proliferative conditions, such as cancer, and which have the following formula: wherein: RN is independently C1-7alkyl; X1 is independently —I, —Br, or —Cl; X2 is independently —I, —Br, or —Cl; the group —N(CH2CH2X1)(CH2CH2X2) is independently attached at the 2-position or at the 4-position; each RG is independently —H or an ester substituent; n is independently an integer from 0 to 4; each RP, if present, is independently a phenyl substituent; m is independently an integer from 0 to 4; each RM, if present, is independently a mustard substituent; and pharmaceutically acceptable salts, solvates, amides, and esters thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds; such compounds and compositions for use in methods of treatment of the human or animal body by therapy; the use of such compounds and compositions for the manufacture of medicaments for the treatment of proliferative conditions; and the like.

    摘要翻译： 本发明涉及可用于酶前体药物治疗（EPT）如ADEPT和GDEPT中用于治疗增殖性疾病如癌症的某些酶（CPG2）活化的自褪色氮芥前药，并且具有以下 式：

    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors
    42.
    发明申请
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送至Gb3表达肿瘤的载体

    公开(公告)号：US20060008475A1

    公开(公告)日：2006-01-12

    申请号：US11046786

    申请日：2005-02-01

    申请人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    发明人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    IPC分类号： A61K39/095

    CPC分类号： A61K49/085 ,  A61K38/00 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/67 ,  A61K49/0008 ,  A61K49/14 ,  B82Y5/00 ,  C07K14/25 ,  C07K14/36

    摘要： The invention relates to new compounds for cancer therapy or diagnosis and to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein—STxB is the Shiga Toxin B subunit or a functional equivalent thereof, —Z(n) wherein n is 0 or 1, Z is an amino-acid residue devoid of sulfydryl groups, or is a polypeptide, —T is a molecule linked by a covalent bound to the S part of Cys, selected from: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, —Y(m) wherein m is 0 or 1, Y is a linker between T and Cys, which is either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into cells.

    摘要翻译： 本发明涉及用于癌症治疗或诊断的新化合物，以及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产品或药物的载体，具有下式：STxB -Z（n）-Cys-Y（m）-T其中-STxB是志贺毒素B亚基或其功能等同物，-Z（n）其中n为0或1，Z为不含 或者是多肽，-T是通过与Sys的S部分的共价结合连接的分子，其选自：用于体内诊断的试剂，细胞毒性剂，前药或用于将前药转化为药物的酶 -Y（m）其中m是0或1，Y是T和Cys之间的连接体，其在将杂化化合物内化为细胞后可以切割或不可切割以释放T。

    Formation of novel erythropoietin conjugates using transglutaminase
    44.
    发明申请
    Formation of novel erythropoietin conjugates using transglutaminase 失效
    使用转谷氨酰胺酶形成新型红细胞生成素缀合物

    公开(公告)号：US20040266690A1

    公开(公告)日：2004-12-30

    申请号：US10854854

    申请日：2004-05-27

    发明人： Chadler Pool

    IPC分类号： A61K038/18

    CPC分类号： B82Y5/00 ,  A61K47/543 ,  A61K47/544 ,  A61K47/60 ,  A61K47/665 ,  A61K47/67

    摘要： The invention provides biologically active erythropoietin (EPO) conjugate compositions wherein a transglutaminase reaction is employed to covalently and site specifically conjugate the EPO molecule to a non-antigenic hydrophilic polymer that can also be covalently linked to an organic molecule either of which modification increases the circulating serum half-life of the composition.

    Prodrugs activated by plasmin and their use in cancer chemotherapy
    45.
    发明申请
    Prodrugs activated by plasmin and their use in cancer chemotherapy 有权
    由纤溶酶活化的前体药物及其在癌症化疗中的应用

    公开(公告)号：US20040171562A1

    公开(公告)日：2004-09-02

    申请号：US10362958

    申请日：2003-10-31

    发明人： Andre Trouet ,  Vincent Dubois ,  Alexandre Passioukov

    IPC分类号： A61K048/00 ,  C07H021/04

    CPC分类号： B82Y5/00 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/65 ,  A61K47/67

    摘要： The product of the invention is a modified form of a therapeutic agent and comprises a therapeutic agent, an oligopeptide having a plasmin peptide substrate of 2-4 amino acids and mono- or di-peptide linkage, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by plasmin. Also disclosed are methods of making and using the prodrug compounds.

    摘要翻译： 本发明的产品是治疗剂的修饰形式，并且包括治疗剂，具有2-4个氨基酸的纤溶酶肽底物和单 - 或二 - 肽键的寡肽，稳定基团和任选的接头 组。 该前体药物可被纤溶酶切割。 还公开了制备和使用前药化合物的方法。

    Cytotoxic drug therapy
    46.
    发明授权
    Cytotoxic drug therapy 失效
    细胞毒药物治疗

    公开(公告)号：US06299876B1

    公开(公告)日：2001-10-09

    申请号：US09353737

    申请日：1999-07-14

    申请人： Kenneth Dawson Bagshawe

    发明人： Kenneth Dawson Bagshawe

    IPC分类号： A61K39395

    CPC分类号： C07K16/40 ,  A61K47/665 ,  A61K47/67 ,  A61K47/6895 ,  A61K47/6899 ,  A61K2039/505 ,  B82Y5/00 ,  C07K16/30 ,  C07K16/3007 ,  C07K16/468 ,  C07K2317/31 ,  C07K2317/54 ,  Y10S424/809 ,  Y10S436/819

    摘要： A compound comprises a target cell-specific portion, such as an antibody specific to tumor cell antigens, and an inactivating portion, such as an enzyme, capable of converting a substance which in its native state is able to inhibit the effect of a cytotoxic agent into a substance which has less effect against said cytotoxic agent. The prolonged action of a cytotoxic agent at tumor sites is therefore possible while protecting normal tissues from the effects of the cytotoxic agent.

    摘要翻译： 化合物包含靶细胞特异性部分，例如对肿瘤细胞抗原特异的抗体，以及能够转化其天然状态能够抑制细胞毒性剂作用的物质的灭活部分，例如酶 成为对所述细胞毒性剂具有较小影响的物质。 因此，在保护正常组织免受细胞毒性作用的作用下，肿瘤部位的细胞毒性剂的延长作用是可能的。

    Enzyme catalyzed therapeutic agents
    47.
    发明授权
    Enzyme catalyzed therapeutic agents 有权
    酶催化治疗剂

    公开(公告)号：US06245750B1

    公开(公告)日：2001-06-12

    申请号：US09235809

    申请日：1999-01-22

    申请人： H. Michael Shepard

    发明人： H. Michael Shepard

    IPC分类号： A61K3170

    CPC分类号： C07H19/20 ,  A61K47/54 ,  A61K47/555 ,  A61K47/556 ,  A61K47/67 ,  B82Y5/00 ,  C07F9/6512 ,  C07H19/06 ,  C07H19/10

    摘要： This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expression as a result of selection by biologic or chemotherapy. This invention also provides methods and examples of molecules for selectively killing a pathological cell by contacting the cell with a prodrug that is a selective substrate for an endogenous, intracellular enzyme. The prodrug is subsequently converted to a cellular toxin. Further provided by this invention is a method for treating a pathology characterized by pathological, hyperproliferative cells in a subject by administering to the subject a prodrug that is a selective substrate for an endogenous, overexpressed, intracellular enzyme, and converted by the enzyme to a cellular toxin in the hyperproliferative cell.

    摘要翻译： 本发明提供了一种通过使靶细胞与候选治疗剂接触来鉴定潜在治疗剂的方法，所述候选治疗剂是细胞中的内源性细胞内酶的选择性底物，其作为通过生物或化疗选择的结果而增强其表达。 本发明还提供了通过使细胞与作为内源性细胞内酶的选择性底物的前药接触来选择性杀死病理细胞的分子的方法和实施例。 随后将前药转化为细胞毒素。 本发明进一步提供的是通过向受试者施用作为内源性，过表达的细胞内酶的选择性底物并由酶转化成细胞的前体药物来治疗受试者中病理学，过度增殖细胞特征的病理学的方法 毒素在过度增殖细胞中。

    PROTEIN-DRUG CONJUGATES COMPRISING CAMPTOTHECIN ANALOGS AND METHODS OF USE THEREOF
    48.
    发明公开
    PROTEIN-DRUG CONJUGATES COMPRISING CAMPTOTHECIN ANALOGS AND METHODS OF USE THEREOF 审中-公开

    公开(公告)号：US20240252661A1

    公开(公告)日：2024-08-01

    申请号：US18516454

    申请日：2023-11-21

    申请人： Regeneron Pharmaceuticals, Inc.

    发明人： Amy HAN

    IPC分类号： A61K47/64 ,  A61K47/55 ,  A61K47/66

    CPC分类号： A61K47/64 ,  A61K47/55 ,  A61K47/67

    摘要： Described herein are protein-drug conjugates and compositions thereof that are useful, for example, for target-specific delivery of therapeutic moieties, e.g., camptothecin analogs and/or derivatives. In certain embodiments, provided are specific and efficient methods for producing protein-drug constructs (e.g., antibody-drug conjugates) utilizing a combination of transglutaminase and 1,3-cycloaddition techniques. Camptothecin analogs, antibody-drug conjugates, and compositions which comprise glutaminyl-modified antibodies and camptothecin analog payloads and are provided.