CN111542324A - 细胞毒性剂及其偶联物、其制备方法及用途 - Google Patents

细胞毒性剂及其偶联物、其制备方法及用途 Download PDF

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Publication number
CN111542324A
CN111542324A CN201980006396.1A CN201980006396A CN111542324A CN 111542324 A CN111542324 A CN 111542324A CN 201980006396 A CN201980006396 A CN 201980006396A CN 111542324 A CN111542324 A CN 111542324A
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alkyl
formula
membered
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CN111542324B (zh
Inventor
肖亮
田强
宋帅
钟国庆
王川
唐祖建
刘登念
胡瑞斌
汪静
薛彤彤
蔡家强
王利春
王晶翼
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Sichuan Kelun Biotech Biopharmaceutical Co Ltd
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Sichuan Kelun Biotech Biopharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

一种新型细胞毒性剂(其为喜树碱衍生物)，其与靶向物的偶联物、所述细胞毒性剂和偶联物的制备方法，以及所述偶联物在预防和/或治疗与细胞活性异常相关的增殖性疾病(包括但不限于癌症疾病)中的用途。

Description

PCT国内申请，说明书已公开。

Claims (22)

  1. PCT国内申请，权利要求书已公开。
CN201980006396.1A 2018-02-11 2019-01-25 细胞毒性剂及其偶联物、其制备方法及用途 Active CN111542324B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810140073 2018-02-11
CN2018101400739 2018-02-11
PCT/CN2019/073148 WO2019154120A1 (zh) 2018-02-11 2019-01-25 细胞毒性剂及其偶联物、其制备方法及用途

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CN111542324A true CN111542324A (zh) 2020-08-14
CN111542324B CN111542324B (zh) 2023-09-12

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Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113286796A (zh) * 2019-01-30 2021-08-20 四川科伦博泰生物医药股份有限公司 喜树碱衍生物及其水溶性前药、包含其的药物组合物及其制备方法和用途
MX2022014332A (es) * 2020-05-15 2022-12-13 Sichuan Kelun Biotech Biopharmaceutical Co Ltd Conjugado anticuerpo-farmaco, metodo de preparacion del mismo y uso del mismo.

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US20060193865A1 (en) * 2002-12-13 2006-08-31 Immunomedics, Inc. Camptothecin-binding moiety conjugates
CN101824090A (zh) * 2002-06-14 2010-09-08 免疫医疗公司 人源化单克隆抗体hPAM4
WO2011068845A1 (en) * 2009-12-02 2011-06-09 Immunomedics, Inc. Combining radioimmunotherapy and antibody-drug conjugates for improved cancer therapy
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US20170014527A1 (en) * 2012-12-13 2017-01-19 Immunomedics, Inc. Antibody-drug conjugates and uses thereof
CN106999517A (zh) * 2014-10-07 2017-08-01 免疫医疗公司 抗体‑药物缀合物的新辅助剂用途
CN107206101A (zh) * 2014-12-03 2017-09-26 基因泰克公司 季铵化合物及其抗体‑药物缀合物
WO2017189279A1 (en) * 2016-04-27 2017-11-02 Immunomedics, Inc. Efficacy of anti-trop-2-sn-38 antibody drug conjugates for therapy of tumors relapsed/refractory to checkpoint inhibitors
CN107469089A (zh) * 2016-06-07 2017-12-15 北京键凯科技股份有限公司 一种peg连接子及配基药物偶联物
CN107735090A (zh) * 2012-12-13 2018-02-23 免疫医疗公司 具有cl2a接头的抗体‑sn‑38免疫缀合物
WO2018036438A1 (zh) * 2016-08-23 2018-03-01 四川科伦博泰生物医药股份有限公司 一种抗体-药物偶联物及其制备方法和应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101824090A (zh) * 2002-06-14 2010-09-08 免疫医疗公司 人源化单克隆抗体hPAM4
US20060193865A1 (en) * 2002-12-13 2006-08-31 Immunomedics, Inc. Camptothecin-binding moiety conjugates
CN102448494A (zh) * 2009-02-13 2012-05-09 免疫医疗公司 具有胞内可裂解的键的免疫共轭物
WO2011068845A1 (en) * 2009-12-02 2011-06-09 Immunomedics, Inc. Combining radioimmunotherapy and antibody-drug conjugates for improved cancer therapy
CN104755494A (zh) * 2012-10-11 2015-07-01 第一三共株式会社 抗体-药物偶联物
US20170014527A1 (en) * 2012-12-13 2017-01-19 Immunomedics, Inc. Antibody-drug conjugates and uses thereof
CN104837508A (zh) * 2012-12-13 2015-08-12 免疫医疗公司 功效改进且毒性降低的抗体与sn-38的免疫缀合物的剂量
CN107735090A (zh) * 2012-12-13 2018-02-23 免疫医疗公司 具有cl2a接头的抗体‑sn‑38免疫缀合物
CN105407891A (zh) * 2013-07-23 2016-03-16 免疫医疗公司 具有cl2a接头的抗体-sn-38免疫缀合物
WO2015148126A1 (en) * 2014-03-12 2015-10-01 Invictus Oncology Pvt. Ltd. Targeted drug delivery through affinity based linkers
CN106999517A (zh) * 2014-10-07 2017-08-01 免疫医疗公司 抗体‑药物缀合物的新辅助剂用途
CN107206101A (zh) * 2014-12-03 2017-09-26 基因泰克公司 季铵化合物及其抗体‑药物缀合物
WO2017189279A1 (en) * 2016-04-27 2017-11-02 Immunomedics, Inc. Efficacy of anti-trop-2-sn-38 antibody drug conjugates for therapy of tumors relapsed/refractory to checkpoint inhibitors
CN107469089A (zh) * 2016-06-07 2017-12-15 北京键凯科技股份有限公司 一种peg连接子及配基药物偶联物
WO2018036438A1 (zh) * 2016-08-23 2018-03-01 四川科伦博泰生物医药股份有限公司 一种抗体-药物偶联物及其制备方法和应用
CN108697809A (zh) * 2016-08-23 2018-10-23 四川科伦博泰生物医药股份有限公司 一种抗体-药物偶联物及其制备方法和应用

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Title
SERENGULAM V. GOVINDAN等: "Improving the Therapeutic Index in Cancer Therapy by Using Antibody-Drug Conjugates Designed with a Moderately Cytotoxic Drug", 《MOLECULAR PHARMACEUTICS》 *

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WO2019154120A1 (zh) 2019-08-15

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