CN112601556A - 含有芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 - Google Patents
含有芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 Download PDFInfo
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- CN112601556A CN112601556A CN201980055709.2A CN201980055709A CN112601556A CN 112601556 A CN112601556 A CN 112601556A CN 201980055709 A CN201980055709 A CN 201980055709A CN 112601556 A CN112601556 A CN 112601556A
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- 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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- C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
- C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
- C07D207/448—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
- C07D207/452—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
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- C—CHEMISTRY; METALLURGY
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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- C07D233/94—Nitro radicals attached in position 4 or 5 with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to other ring members
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- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/42—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms with nitro or nitroso radicals directly attached to ring carbon atoms
- C07D333/44—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms with nitro or nitroso radicals directly attached to ring carbon atoms attached in position 5
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- C—CHEMISTRY; METALLURGY
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract
一种式I所示的含有芳硝基的连接子,还涉及含有所述连接子的抗体偶联药物,还涉及所述连接子的用途,还涉及包含所述抗体偶联药物的药物组合物,还涉及这些抗体偶联药物用于治疗和/或预防疾病的用途。
Description
PCT国内申请,说明书已公开。
Claims (21)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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CN2018110025592 | 2018-08-30 | ||
CN201811002559.2A CN110872339A (zh) | 2018-08-30 | 2018-08-30 | 含有芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 |
PCT/CN2019/103053 WO2020043129A1 (zh) | 2018-08-30 | 2019-08-28 | 含有芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 |
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CN112601556A true CN112601556A (zh) | 2021-04-02 |
CN112601556B CN112601556B (zh) | 2022-08-09 |
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CN201980055709.2A Active CN112601556B (zh) | 2018-08-30 | 2019-08-28 | 含有芳硝基的连接子、含连接子的抗体偶联药物及连接子的用途 |
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US (1) | US20210205464A1 (zh) |
EP (1) | EP3845251A4 (zh) |
JP (1) | JP2021535156A (zh) |
KR (1) | KR20210053934A (zh) |
CN (2) | CN110872339A (zh) |
WO (1) | WO2020043129A1 (zh) |
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CN114605367B (zh) * | 2020-12-03 | 2023-06-27 | 中国人民解放军军事科学院军事医学研究院 | 含香豆素的连接子及含该连接子的抗体偶联药物 |
CN115215780B (zh) * | 2022-04-22 | 2023-08-08 | 上海格苓凯生物科技有限公司 | 一种利用n,n-二琥珀酰亚胺基碳酸酯制备异双功能交联剂smcc的方法 |
Citations (7)
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WO2009151687A2 (en) * | 2008-03-12 | 2009-12-17 | The Regents Of The University Of Michigan | Dendrimer conjugates |
WO2016094505A1 (en) * | 2014-12-09 | 2016-06-16 | Abbvie Inc. | Antibody drug conjugates with cell permeable bcl-xl inhibitors |
CN106661123A (zh) * | 2014-06-20 | 2017-05-10 | 荷商台医(有限合伙)公司 | 抗‑cd22抗体‑药物缀合物及其使用方法 |
CN107189775A (zh) * | 2017-05-08 | 2017-09-22 | 中国科学技术大学 | 具有荧光发射性质的抗体‑药物/探针缀合物及其制备方法和应用 |
CN107417672A (zh) * | 2017-04-12 | 2017-12-01 | 华东师范大学 | 一种基于2,2‑二甲基‑3‑(2‑硝基咪唑基)丙酸的低氧激活前药 |
WO2017214301A1 (en) * | 2016-06-08 | 2017-12-14 | Abbvie Inc. | Anti-egfr antibody drug conjugates |
CN107789630A (zh) * | 2016-10-08 | 2018-03-13 | 四川百利药业有限责任公司 | 半胱氨酸改造的抗体‑毒素偶联物及其制备方法 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
-
2018
- 2018-08-30 CN CN201811002559.2A patent/CN110872339A/zh active Pending
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2019
- 2019-08-28 EP EP19853328.3A patent/EP3845251A4/en not_active Withdrawn
- 2019-08-28 CN CN201980055709.2A patent/CN112601556B/zh active Active
- 2019-08-28 JP JP2021510882A patent/JP2021535156A/ja active Pending
- 2019-08-28 US US17/271,882 patent/US20210205464A1/en active Pending
- 2019-08-28 KR KR1020217009506A patent/KR20210053934A/ko unknown
- 2019-08-28 WO PCT/CN2019/103053 patent/WO2020043129A1/zh unknown
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009151687A2 (en) * | 2008-03-12 | 2009-12-17 | The Regents Of The University Of Michigan | Dendrimer conjugates |
CN106661123A (zh) * | 2014-06-20 | 2017-05-10 | 荷商台医(有限合伙)公司 | 抗‑cd22抗体‑药物缀合物及其使用方法 |
WO2016094505A1 (en) * | 2014-12-09 | 2016-06-16 | Abbvie Inc. | Antibody drug conjugates with cell permeable bcl-xl inhibitors |
WO2017214301A1 (en) * | 2016-06-08 | 2017-12-14 | Abbvie Inc. | Anti-egfr antibody drug conjugates |
CN107789630A (zh) * | 2016-10-08 | 2018-03-13 | 四川百利药业有限责任公司 | 半胱氨酸改造的抗体‑毒素偶联物及其制备方法 |
CN107417672A (zh) * | 2017-04-12 | 2017-12-01 | 华东师范大学 | 一种基于2,2‑二甲基‑3‑(2‑硝基咪唑基)丙酸的低氧激活前药 |
CN107189775A (zh) * | 2017-05-08 | 2017-09-22 | 中国科学技术大学 | 具有荧光发射性质的抗体‑药物/探针缀合物及其制备方法和应用 |
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WO2020043129A1 (zh) | 2020-03-05 |
US20210205464A1 (en) | 2021-07-08 |
KR20210053934A (ko) | 2021-05-12 |
CN112601556B (zh) | 2022-08-09 |
EP3845251A4 (en) | 2022-05-04 |
EP3845251A1 (en) | 2021-07-07 |
CN110872339A (zh) | 2020-03-10 |
JP2021535156A (ja) | 2021-12-16 |
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