CN112513046A - 作为TOLL样受体7(TLR7)激动剂的2H-吡唑并[4,3-d]嘧啶化合物及其方法和用途 - Google Patents

作为TOLL样受体7(TLR7)激动剂的2H-吡唑并[4,3-d]嘧啶化合物及其方法和用途 Download PDF

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CN112513046A
CN112513046A CN201980051044.8A CN201980051044A CN112513046A CN 112513046 A CN112513046 A CN 112513046A CN 201980051044 A CN201980051044 A CN 201980051044A CN 112513046 A CN112513046 A CN 112513046A
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alkyl
cancer
compound
antibody
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Y·B·波德尔
S·冈沃
何立崎
P·西瓦帕卡萨姆
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Bristol Myers Squibb Co
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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CN201980051044.8A 2018-08-03 2019-08-01 作为TOLL样受体7(TLR7)激动剂的2H-吡唑并[4,3-d]嘧啶化合物及其方法和用途 Pending CN112513046A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862714238P 2018-08-03 2018-08-03
US62/714,238 2018-08-03
PCT/US2019/044578 WO2020028610A1 (en) 2018-08-03 2019-08-01 2H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS AND METHODS AND USES THEREFOR

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CN112513046A true CN112513046A (zh) 2021-03-16

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CN201980062888.2A Pending CN112752759A (zh) 2018-08-03 2019-08-01 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物及其方法与用途

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US (3) US11554120B2 (https=)
EP (2) EP3830089B1 (https=)
JP (4) JP7337909B2 (https=)
KR (2) KR20210039411A (https=)
CN (2) CN112513046A (https=)
AR (1) AR115885A1 (https=)
AU (1) AU2019314444A1 (https=)
BR (1) BR112021001503A2 (https=)
CA (1) CA3108512A1 (https=)
CL (1) CL2021000216A1 (https=)
CO (1) CO2021000942A2 (https=)
EA (1) EA202190442A1 (https=)
ES (2) ES2941768T3 (https=)
IL (1) IL280473A (https=)
MX (1) MX2021001311A (https=)
PE (1) PE20211812A1 (https=)
SG (1) SG11202101031XA (https=)
TW (1) TW202019933A (https=)
WO (2) WO2020028610A1 (https=)

Cited By (2)

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CN115337406A (zh) * 2021-05-13 2022-11-15 清华大学 一种抗体药物偶联物及其制备方法和应用
WO2025021106A1 (zh) * 2023-07-24 2025-01-30 北京森妙生物科技有限公司 吡啶[3,2-d]嘧啶-2-胺衍生物及其制备方法和应用

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US11554120B2 (en) * 2018-08-03 2023-01-17 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor
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JP2023512204A (ja) * 2020-01-27 2023-03-24 ブリストル－マイヤーズ スクイブ カンパニー トール様受容体７（ＴＬＲ７）アゴニストとしての１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物
US20230348468A1 (en) * 2020-01-27 2023-11-02 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US20230131192A1 (en) 2020-01-27 2023-04-27 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
US12485123B2 (en) 2020-01-27 2025-12-02 Bristol-Myers Squibb Company 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists
KR20220132601A (ko) * 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
CN115151546A (zh) * 2020-01-27 2022-10-04 百时美施贵宝公司 作为Toll样受体7(TLR7)激动剂的C3-取代的1H-吡唑并[4,3-d]嘧啶化合物
WO2021154663A1 (en) 2020-01-27 2021-08-05 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
KR20220132589A (ko) * 2020-01-27 2022-09-30 브리스톨-마이어스 스큅 컴퍼니 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물
US20230144824A1 (en) 2020-01-27 2023-05-11 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
AR122043A1 (es) * 2020-05-12 2022-08-03 Bristol Myers Squibb Co Dosificación y administración del anticuerpo anti-ctla-4 activable
WO2021247809A1 (en) * 2020-06-04 2021-12-09 Merck Sharp & Dohme Corp. PYRAZOLO[4,3-d]PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF CELLULAR PROLIFERATIVE DISORDERS
CN115119508B (zh) * 2021-01-20 2024-05-24 上海维申医药有限公司 大环tlr7激动剂、其制备方法、药物组合物及其用途
AU2024271872A1 (en) * 2023-05-18 2025-12-18 Merck Sharp & Dohme Llc Compounds and adjuvant formulations useful in pneumococcal vaccines
PE20260293A1 (es) * 2023-05-18 2026-02-10 Merck Sharp And Dohme Llc Compuestos y formulaciones utiles como adyuvantes de vacunas
WO2024250985A1 (zh) * 2023-06-07 2024-12-12 上海维申医药有限公司 Toll样受体激动剂杂环类衍生物及其制备和应用
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