CA3219236A1 - Exatecan derivatives and antibody-drug conjugates thereof - Google Patents

Exatecan derivatives and antibody-drug conjugates thereof Download PDF

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Publication number
CA3219236A1
CA3219236A1 CA3219236A CA3219236A CA3219236A1 CA 3219236 A1 CA3219236 A1 CA 3219236A1 CA 3219236 A CA3219236 A CA 3219236A CA 3219236 A CA3219236 A CA 3219236A CA 3219236 A1 CA3219236 A1 CA 3219236A1
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CA
Canada
Prior art keywords
group
antibody
3alkyl
lig
c2alkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3219236A
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English (en)
French (fr)
Inventor
Marija VRLJIC
Peter Strop
Janica Cheuk-ying WONG
Jaume Pons
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
ALX Oncology Inc
Original Assignee
ALX Oncology Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ALX Oncology Inc filed Critical ALX Oncology Inc
Publication of CA3219236A1 publication Critical patent/CA3219236A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero 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
    • A61K31/435—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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
    • 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
    • A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • 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
    • 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
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA3219236A 2021-05-07 2022-05-06 Exatecan derivatives and antibody-drug conjugates thereof Pending CA3219236A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202163185736P 2021-05-07 2021-05-07
US63/185,736 2021-05-07
US202163248705P 2021-09-27 2021-09-27
US63/248,705 2021-09-27
US202263321187P 2022-03-18 2022-03-18
US63/321,187 2022-03-18
PCT/US2022/028193 WO2022236136A1 (en) 2021-05-07 2022-05-06 Exatecan derivatives and antibody-drug conjugates thereof

Publications (1)

Publication Number Publication Date
CA3219236A1 true CA3219236A1 (en) 2022-11-10

Family

ID=81851425

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3219236A Pending CA3219236A1 (en) 2021-05-07 2022-05-06 Exatecan derivatives and antibody-drug conjugates thereof

Country Status (15)

Country Link
US (1) US20250101032A1 (https=)
EP (1) EP4334322A1 (https=)
JP (1) JP2024518438A (https=)
KR (1) KR20240036506A (https=)
AU (1) AU2022269073A1 (https=)
BR (1) BR112023023276A2 (https=)
CA (1) CA3219236A1 (https=)
CL (1) CL2023003304A1 (https=)
CO (1) CO2023016939A2 (https=)
GE (1) GEAP202416409A (https=)
IL (1) IL308246A (https=)
MX (1) MX2023013118A (https=)
PE (1) PE20241299A1 (https=)
TW (1) TW202309042A (https=)
WO (1) WO2022236136A1 (https=)

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KR20240038138A (ko) 2020-07-13 2024-03-22 리제너론 파마슈티칼스 인코포레이티드 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도
MX2023003778A (es) 2020-09-30 2023-04-26 Duality Biologics Suzhou Co Ltd Compuesto antitumoral, metodo de preparacion y uso del mismo.
CN114805377A (zh) * 2021-01-29 2022-07-29 明慧医药（杭州）有限公司 适用于抗体-药物偶联物的毒素分子
AU2022375634A1 (en) 2021-10-25 2024-06-06 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
EP4434548A1 (en) 2021-11-15 2024-09-25 Systimmune, Inc. Bispecific antibody-camptothecin drug conjugate and pharmaceutical use thereof
US11814394B2 (en) 2021-11-16 2023-11-14 Genequantum Healthcare (Suzhou) Co., Ltd. Exatecan derivatives, linker-payloads, and conjugates and thereof
CA3241734A1 (en) * 2022-01-12 2023-07-20 Amy Han Camptothecin analogs conjugated to a glutamine residue in a protein, and their use
EP4489790A1 (en) * 2022-03-10 2025-01-15 Vivasor, Inc. Antibody-drug conjugates and uses thereof
CN118696048A (zh) * 2022-05-09 2024-09-24 同宜医药（苏州）有限公司 一种喜树碱衍生物，基于其的抗体-药物偶联物和药物组合物，及其应用
KR20250075560A (ko) 2022-07-15 2025-05-28 진콴텀 헬스케어 (쑤저우) 씨오., 엘티디. 항-trop2 항체 및 이의 접합체
KR20250049293A (ko) * 2022-07-27 2025-04-11 밍훼이 파마슈티컬 (항저우) 리미티드 항체-약물 접합체 및 이의 용도
CN117510515A (zh) * 2022-07-28 2024-02-06 明慧医药（杭州）有限公司 适用于抗体-药物偶联物的毒素分子
CN117024438A (zh) * 2022-07-29 2023-11-10 杭州爱科瑞思生物医药有限公司 依沙替康衍生物及其应用
JP2025511436A (ja) * 2022-09-02 2025-04-16 メルク・シャープ・アンド・ドーム・エルエルシー エキサテカン由来トポイソメラーゼ－１阻害薬医薬組成物及びその使用
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IL321193A (en) * 2022-12-28 2025-07-01 Adcendo Aps Antibody-drug conjugates targeting UPARAP including extacan derivatives
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CN116063311B (zh) * 2023-03-01 2025-09-26 金麦安博生物制药(苏州)有限公司 一种依喜替康衍生物及其制备方法
CN120916790A (zh) * 2023-03-27 2025-11-07 台湾浩鼎生技股份有限公司 Trop2耦合生物分子、医药组合物及方法
TW202438069A (zh) * 2023-03-30 2024-10-01 大陸商上海齊魯製藥研究中心有限公司 依喜替康衍生物及其抗體藥物偶聯物
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CN119080792A (zh) * 2023-09-15 2024-12-06 杭州爱科瑞思生物医药有限公司 依沙替康羟胺衍生物及其应用
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CN117417347A (zh) * 2023-09-28 2024-01-19 杭州爱科瑞思生物医药有限公司 卤素取代的依沙替康的酰胺衍生物及其制备方法和应用
CN117645608A (zh) * 2023-11-30 2024-03-05 昆山新蕴达生物科技有限公司 抗体药物偶联物及其应用
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WO2025167722A1 (zh) * 2024-02-06 2025-08-14 四川科伦博泰生物医药股份有限公司 稠环化合物及其制备方法和应用
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MX2023013118A (es) 2024-02-27
CO2023016939A2 (es) 2024-05-10
US20250101032A1 (en) 2025-03-27
TW202309042A (zh) 2023-03-01
EP4334322A1 (en) 2024-03-13
JP2024518438A (ja) 2024-05-01
GEAP202416409A (en) 2024-02-26
AU2022269073A1 (en) 2023-11-23
KR20240036506A (ko) 2024-03-20
CL2023003304A1 (es) 2024-04-19
WO2022236136A1 (en) 2022-11-10
PE20241299A1 (es) 2024-06-24
BR112023023276A2 (pt) 2024-01-30
IL308246A (en) 2024-01-01

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