CO2021000942A2 - Compuestos 1h-pyrazolo [4,3-d]pirimidina como agonistas del receptor 7 tipo toll (tlr7) y métodos y usos de los mismos - Google Patents

Compuestos 1h-pyrazolo [4,3-d]pirimidina como agonistas del receptor 7 tipo toll (tlr7) y métodos y usos de los mismos

Info

Publication number
CO2021000942A2
CO2021000942A2 CONC2021/0000942A CO2021000942A CO2021000942A2 CO 2021000942 A2 CO2021000942 A2 CO 2021000942A2 CO 2021000942 A CO2021000942 A CO 2021000942A CO 2021000942 A2 CO2021000942 A2 CO 2021000942A2
Authority
CO
Colombia
Prior art keywords
tlr7
toll
agonists
receptor
pyrazolo
Prior art date
Application number
CONC2021/0000942A
Other languages
English (en)
Inventor
Christine M Tarby
Yam B Poudel
Sanjeev Gangwar
Liqi He
Prasanna Sivaprakasam
Matthias Broekema
Naidu S Chowdari
Matthew Cox
Qian Zhang
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CO2021000942A2 publication Critical patent/CO2021000942A2/es

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    • 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
    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K39/3955—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de acuerdo con la Fórmula I son útiles como agonistas del receptor 7 tipo Toll (TLR7). Dichos compuestos pueden usarse en el tratamiento del cáncer, especialmente en combinación con un agente de inmunoterapia contra el cáncer, o como un adyuvante de vacuna.
CONC2021/0000942A 2018-08-03 2021-01-28 Compuestos 1h-pyrazolo [4,3-d]pirimidina como agonistas del receptor 7 tipo toll (tlr7) y métodos y usos de los mismos CO2021000942A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862714238P 2018-08-03 2018-08-03
PCT/US2019/044575 WO2020028608A1 (en) 2018-08-03 2019-08-01 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS AND METHODS AND USES THEREFOR

Publications (1)

Publication Number Publication Date
CO2021000942A2 true CO2021000942A2 (es) 2021-02-17

Family

ID=67742964

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2021/0000942A CO2021000942A2 (es) 2018-08-03 2021-01-28 Compuestos 1h-pyrazolo [4,3-d]pirimidina como agonistas del receptor 7 tipo toll (tlr7) y métodos y usos de los mismos

Country Status (19)

Country Link
US (3) US11554120B2 (es)
EP (2) EP3830089B1 (es)
JP (4) JP7337907B2 (es)
KR (2) KR20210039410A (es)
CN (2) CN112513046A (es)
AR (1) AR115885A1 (es)
AU (1) AU2019314444A1 (es)
BR (1) BR112021001503A2 (es)
CA (1) CA3108512A1 (es)
CL (1) CL2021000216A1 (es)
CO (1) CO2021000942A2 (es)
EA (1) EA202190442A1 (es)
ES (2) ES2941520T3 (es)
IL (1) IL280473A (es)
MX (1) MX2021001311A (es)
PE (1) PE20211812A1 (es)
SG (1) SG11202101031XA (es)
TW (1) TW202019933A (es)
WO (2) WO2020028610A1 (es)

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US20230140430A1 (en) * 2020-01-27 2023-05-04 Bristol-Myers Squibb Company 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS
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JP2023512230A (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Ｃ３置換１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物
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JP2023512208A (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
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US20230219962A1 (en) * 2020-06-04 2023-07-13 Merck Sharp & Dohme Llc 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
CN115337406B (zh) * 2021-05-13 2025-10-03 清华大学 一种抗体药物偶联物及其制备方法和应用
WO2024238735A1 (en) * 2023-05-18 2024-11-21 Merck Sharp & Dohme Llc Compounds and formulations useful as vaccine adjuvants
US20240390471A1 (en) * 2023-05-18 2024-11-28 Merck Sharp & Dohme Llc Compounds and adjuvant formulations useful in pneumococcal vaccines
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
CN119462640A (zh) * 2023-07-24 2025-02-18 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
US20250282786A1 (en) * 2024-03-05 2025-09-11 Bristol-Myers Squibb Company Tricyclic TLR7 Agonists and Uses Thereof

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