WO2021136462A1 - Dérivés furane et leur application en médecine - Google Patents

Dérivés furane et leur application en médecine Download PDF

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Publication number
WO2021136462A1
WO2021136462A1 PCT/CN2020/141860 CN2020141860W WO2021136462A1 WO 2021136462 A1 WO2021136462 A1 WO 2021136462A1 CN 2020141860 W CN2020141860 W CN 2020141860W WO 2021136462 A1 WO2021136462 A1 WO 2021136462A1
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WO
WIPO (PCT)
Prior art keywords
methyl
alkyl
chloro
dihydro
amino
Prior art date
Application number
PCT/CN2020/141860
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English (en)
Chinese (zh)
Inventor
魏用刚
许学珍
楚洪柱
何吕学
孟详玉
王建成
晏婕
孙毅
Original Assignee
成都百裕制药股份有限公司
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Application filed by 成都百裕制药股份有限公司 filed Critical 成都百裕制药股份有限公司
Publication of WO2021136462A1 publication Critical patent/WO2021136462A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • 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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/30—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/40—Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne une classe de dérivés furane et leur application en médecine ; l'invention concerne plus particulièrement des dérivés furane qui se rapportent à des dérivés pyrimidine représentés par la formule générale (I'), ou des stéréo-isomères, des solvates, des promédicaments, des métabolites, des produits deutérés, des sels pharmaceutiquement acceptables ou des cristaux eutectiques de ceux-ci, une composition pharmaceutique comprenant ceux-ci et une utilisation des composés ou de la composition dans la préparation d'un inhibiteur de protéine kinase dépendante de l'ADN (ou ADN-PK), la définition de chaque substituant dans la formule générale (I') étant la même que la définition associée dans la description.
PCT/CN2020/141860 2019-12-31 2020-12-30 Dérivés furane et leur application en médecine WO2021136462A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201911410949 2019-12-31
CN201911410949.8 2019-12-31
CN202010154743.X 2020-03-11
CN202010154743 2020-03-11

Publications (1)

Publication Number Publication Date
WO2021136462A1 true WO2021136462A1 (fr) 2021-07-08

Family

ID=76686500

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2020/141860 WO2021136462A1 (fr) 2019-12-31 2020-12-30 Dérivés furane et leur application en médecine

Country Status (2)

Country Link
CN (1) CN113121538B (fr)
WO (1) WO2021136462A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022135555A1 (fr) * 2020-12-24 2022-06-30 江苏恒瑞医药股份有限公司 Composé de purinone, son procédé de préparation et son application pharmaceutique
WO2022135360A1 (fr) * 2020-12-21 2022-06-30 江苏恒瑞医药股份有限公司 Dérivé de purinone, son procédé de préparation et son utilisation en médecine
WO2022199547A1 (fr) * 2021-03-22 2022-09-29 成都赜灵生物医药科技有限公司 Dérivé de 7,9-dihydropurine et son usage pharmaceutique

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022017368A1 (fr) * 2020-07-20 2022-01-27 首药控股(北京)股份有限公司 Inhibiteur sélectif de dna-pk, son procédé de préparation et son utilisation

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103649085A (zh) * 2011-05-25 2014-03-19 阿尔米雷尔有限公司 用作治疗骨髓增生性疾病、移植排斥、免疫介导性疾病和炎性疾病的药剂的吡啶-2(1h)-酮衍生物
CN105246883A (zh) * 2013-03-12 2016-01-13 沃泰克斯药物股份有限公司 Dna-pk抑制剂
CN110177791A (zh) * 2016-12-20 2019-08-27 阿斯利康(瑞典)有限公司 氨基-三唑并吡啶化合物及其在治疗癌症中的用途
CN110386932A (zh) * 2018-04-20 2019-10-29 艾科思莱德制药公司 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂
WO2019238929A1 (fr) * 2018-06-15 2019-12-19 Astrazeneca Ab Composés de purinone et leur utilisation dans le traitement du cancer

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105384695B (zh) * 2014-08-22 2019-12-20 四川海思科制药有限公司 嘧啶衍生物及其制备方法和在医药上的应用
WO2019201283A1 (fr) * 2018-04-20 2019-10-24 Xrad Therapeutics, Inc. Inhibiteurs doubles d'atm et d'adn-pk pour une utilisation en thérapie antitumorale

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103649085A (zh) * 2011-05-25 2014-03-19 阿尔米雷尔有限公司 用作治疗骨髓增生性疾病、移植排斥、免疫介导性疾病和炎性疾病的药剂的吡啶-2(1h)-酮衍生物
CN105246883A (zh) * 2013-03-12 2016-01-13 沃泰克斯药物股份有限公司 Dna-pk抑制剂
CN110177791A (zh) * 2016-12-20 2019-08-27 阿斯利康(瑞典)有限公司 氨基-三唑并吡啶化合物及其在治疗癌症中的用途
CN110386932A (zh) * 2018-04-20 2019-10-29 艾科思莱德制药公司 用于抗肿瘤疗法中的双重atm和dna-pk抑制剂
WO2019238929A1 (fr) * 2018-06-15 2019-12-19 Astrazeneca Ab Composés de purinone et leur utilisation dans le traitement du cancer

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022135360A1 (fr) * 2020-12-21 2022-06-30 江苏恒瑞医药股份有限公司 Dérivé de purinone, son procédé de préparation et son utilisation en médecine
WO2022135555A1 (fr) * 2020-12-24 2022-06-30 江苏恒瑞医药股份有限公司 Composé de purinone, son procédé de préparation et son application pharmaceutique
WO2022199547A1 (fr) * 2021-03-22 2022-09-29 成都赜灵生物医药科技有限公司 Dérivé de 7,9-dihydropurine et son usage pharmaceutique

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Publication number Publication date
CN113121538B (zh) 2023-04-21
CN113121538A (zh) 2021-07-16

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