JP7542613B2 - Axlとc-Metキナーゼ阻害活性を有する化合物およびその製造と使用 - Google Patents

Axlとc-Metキナーゼ阻害活性を有する化合物およびその製造と使用 Download PDF

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JP7542613B2
JP7542613B2 JP2022514985A JP2022514985A JP7542613B2 JP 7542613 B2 JP7542613 B2 JP 7542613B2 JP 2022514985 A JP2022514985 A JP 2022514985A JP 2022514985 A JP2022514985 A JP 2022514985A JP 7542613 B2 JP7542613 B2 JP 7542613B2
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fluorophenyl
dioxo
substituted
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ドゥアン,ウェンフー
ゲン,メイユ
チャン,へーフェン
ディン,ジアン
アイ,ジン
ペン,シア
ジ,インチュン
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Shanghai Institute of Materia Medica of CAS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
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    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (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)
  • Plural Heterocyclic Compounds (AREA)
JP2022514985A 2019-09-06 2020-09-03 Axlとc-Metキナーゼ阻害活性を有する化合物およびその製造と使用 Active JP7542613B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910843097 2019-09-06
CN201910843097.5 2019-09-06
PCT/CN2020/113265 WO2021043217A1 (zh) 2019-09-06 2020-09-03 具有Axl与c-Met激酶抑制活性的化合物及其制备和应用

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JP2022547915A JP2022547915A (ja) 2022-11-16
JP2022547915A5 JP2022547915A5 (https=) 2023-10-30
JP7542613B2 true JP7542613B2 (ja) 2024-08-30

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US (1) US12479850B2 (https=)
EP (1) EP4029862A4 (https=)
JP (1) JP7542613B2 (https=)
KR (1) KR102826937B1 (https=)
CN (2) CN112457295B (https=)
AU (1) AU2020342108B2 (https=)
WO (1) WO2021043217A1 (https=)

Families Citing this family (5)

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Publication number Priority date Publication date Assignee Title
JP2022551422A (ja) * 2019-09-26 2022-12-09 エグゼリクシス, インコーポレイテッド ピリドン化合物およびタンパク質キナーゼの調節における使用の方法
BR112022019517A2 (pt) 2020-03-30 2022-12-06 Hutchison Medipharma Ltd Compostos de amida e usos dos mesmos
IT202100022682A1 (it) * 2021-09-01 2023-03-01 Luigi Frati Derivati pirimidinici e loro uso nel trattamento di tumori
CN114573553B (zh) * 2022-01-27 2023-11-10 广州六顺生物科技有限公司 杂芳环类衍生物及其制备方法和应用
US12421207B2 (en) * 2022-02-16 2025-09-23 Cmg Pharmaceutical Co., Ltd. Pyrimidinedione-based compounds as AXL, c-MET, and Mer inhibitors and methods of use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014533287A (ja) 2011-11-14 2014-12-11 セファロン、インク. AXLおよびc−METキナーゼ阻害剤としてのウラシル誘導体
CN106543145A (zh) 2016-10-28 2017-03-29 山西医科大学 c‑Met激酶抑剂3‑(4‑氟苯基)嘧啶酮‑5‑甲酸酰胺衍生物、制备方法与应用
WO2019101178A1 (zh) 2017-11-24 2019-05-31 南京明德新药研发股份有限公司 作为c-MET/AXL抑制剂的尿嘧啶类化合物
CN110041316A (zh) 2018-01-17 2019-07-23 南京药捷安康生物科技有限公司 Tam家族激酶/和csf1r激酶抑制剂及其用途

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TW201422592A (zh) 2012-08-27 2014-06-16 Boehringer Ingelheim Int β-分泌酶抑制劑
AU2014370186A1 (en) 2013-12-26 2016-07-14 Ignyta, Inc. Pyrazolo[1,5-a]pyridine derivatives and methods of their use
KR102483020B1 (ko) 2016-03-28 2023-01-04 인사이트 코포레이션 Tam 저해제로서의 피롤로트리아진 화합물
CA3114987A1 (en) 2018-08-27 2020-03-05 Beijing Yuezhikangtai Biomedicines Co., Ltd. Multi-substituted pyridone derivatives and medical use thereof
UY38349A (es) * 2018-08-30 2020-03-31 Array Biopharma Inc Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014533287A (ja) 2011-11-14 2014-12-11 セファロン、インク. AXLおよびc−METキナーゼ阻害剤としてのウラシル誘導体
CN106543145A (zh) 2016-10-28 2017-03-29 山西医科大学 c‑Met激酶抑剂3‑(4‑氟苯基)嘧啶酮‑5‑甲酸酰胺衍生物、制备方法与应用
WO2019101178A1 (zh) 2017-11-24 2019-05-31 南京明德新药研发股份有限公司 作为c-MET/AXL抑制剂的尿嘧啶类化合物
CN110041316A (zh) 2018-01-17 2019-07-23 南京药捷安康生物科技有限公司 Tam家族激酶/和csf1r激酶抑制剂及其用途

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CN112457295A (zh) 2021-03-09
CA3153600A1 (en) 2021-03-11
KR20220058931A (ko) 2022-05-10
KR102826937B1 (ko) 2025-07-01
CN116283916B (zh) 2024-06-11
JP2022547915A (ja) 2022-11-16
AU2020342108B2 (en) 2024-03-07
US12479850B2 (en) 2025-11-25
US20220324869A1 (en) 2022-10-13
EP4029862A1 (en) 2022-07-20
WO2021043217A1 (zh) 2021-03-11
EP4029862A4 (en) 2023-10-04
CN116283916A (zh) 2023-06-23
CN112457295B (zh) 2022-07-26
AU2020342108A1 (en) 2022-04-21

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