CN111954532A - 杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途和蛋白质-药物分子复合物 - Google Patents

杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途和蛋白质-药物分子复合物 Download PDF

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CN111954532A
CN111954532A CN201880092312.6A CN201880092312A CN111954532A CN 111954532 A CN111954532 A CN 111954532A CN 201880092312 A CN201880092312 A CN 201880092312A CN 111954532 A CN111954532 A CN 111954532A
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alkyl
piperidinyl
piperazinyl
cancer
compound
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任瑞宝
吴敏
焦波
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Ruinjin Hospital Affiliated to Shanghai Jiaotong University School of Medicine Co Ltd
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Ruinjin Hospital Affiliated to Shanghai Jiaotong University School of Medicine 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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Abstract

一种作为微管抑制剂的杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途以及蛋白质‑药物分子复合物。从使用通过致癌RAS转化的细胞的高通量药物筛选，鉴定了阻断细胞增殖的先导杂芳基酰胺化合物。构效关系分析表明，该系列的骨架(以I‑28为示例)是肿瘤细胞生长的有效抑制剂。进一步分析表明，这种化合物在体外和体内都显示出抗肿瘤MDR的良好的药理学性质。总之，一种由I‑28代表的新型骨架，该骨架可以开发为癌症治疗剂，特别是对于肿瘤多重抗性。

Description

PCT国内申请，说明书已公开。

Claims (9)

  1. PCT国内申请，权利要求书已公开。
CN201880092312.6A 2018-04-13 2018-04-13 杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途和蛋白质-药物分子复合物 Pending CN111954532A (zh)

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PCT/CN2018/083043 WO2019196111A1 (zh) 2018-04-13 2018-04-13 杂芳基酰胺类化合物的抗肿瘤多药耐药性、治疗癌症的用途和蛋白质-药物分子复合物

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US10988439B2 (en) 2019-06-04 2021-04-27 King Abdulaziz University Cytotoxic compounds, pharmaceutical compositions thereof, and methods of treating cancer

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US20030144312A1 (en) * 2001-10-30 2003-07-31 Schoenhard Grant L. Inhibitors of ABC drug transporters in multidrug resistant cancer cells
CN1681489A (zh) * 2002-07-17 2005-10-12 蒂坦药物股份有限公司 增加抗肿瘤活性的化疗药物的联用
CN101939005A (zh) * 2007-12-14 2011-01-05 诺瓦提斯公司 作为癌症治疗剂的驱动蛋白抑制剂
US20150196560A1 (en) * 2014-01-15 2015-07-16 Southern Methodist University Inhibitors of Multidrug Resistance Transporter P-Glycoprotein
CN107847593A (zh) * 2015-04-20 2018-03-27 美侬米克国际有限公司 治疗抗体及其用途
CN110234357A (zh) * 2016-11-23 2019-09-13 梅尔莎纳医疗公司 用于抗体-药物缀合物的含肽接头
CN110431135A (zh) * 2017-01-06 2019-11-08 大连万春布林医药有限公司 微管蛋白结合化合物及其治疗用途

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PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
WO2006107756A1 (en) * 2005-04-04 2006-10-12 Osi Pharmaceuticals, Inc. Pyrrolo [2,3-d] imidazoles for the treatment of hyperproliferative disorders
TW200901969A (en) * 2007-06-06 2009-01-16 Smithkline Beecham Corp Chemical compounds
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US20030144312A1 (en) * 2001-10-30 2003-07-31 Schoenhard Grant L. Inhibitors of ABC drug transporters in multidrug resistant cancer cells
CN1681489A (zh) * 2002-07-17 2005-10-12 蒂坦药物股份有限公司 增加抗肿瘤活性的化疗药物的联用
CN101939005A (zh) * 2007-12-14 2011-01-05 诺瓦提斯公司 作为癌症治疗剂的驱动蛋白抑制剂
US20150196560A1 (en) * 2014-01-15 2015-07-16 Southern Methodist University Inhibitors of Multidrug Resistance Transporter P-Glycoprotein
CN107847593A (zh) * 2015-04-20 2018-03-27 美侬米克国际有限公司 治疗抗体及其用途
CN110234357A (zh) * 2016-11-23 2019-09-13 梅尔莎纳医疗公司 用于抗体-药物缀合物的含肽接头
CN110431135A (zh) * 2017-01-06 2019-11-08 大连万春布林医药有限公司 微管蛋白结合化合物及其治疗用途

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