WO2020119739A1 - Composé de 2-aminopyrimidine et son utilisation - Google Patents

Composé de 2-aminopyrimidine et son utilisation Download PDF

Info

Publication number
WO2020119739A1
WO2020119739A1 PCT/CN2019/124686 CN2019124686W WO2020119739A1 WO 2020119739 A1 WO2020119739 A1 WO 2020119739A1 CN 2019124686 W CN2019124686 W CN 2019124686W WO 2020119739 A1 WO2020119739 A1 WO 2020119739A1
Authority
WO
WIPO (PCT)
Prior art keywords
substituted
unsubstituted
alkyl
halogen
pharmaceutically acceptable
Prior art date
Application number
PCT/CN2019/124686
Other languages
English (en)
Chinese (zh)
Inventor
丁克
丁健
陆小云
耿美玉
李姗
谢华
陈灏
童林江
任小梅
冯芳
Original Assignee
暨南大学
中国科学院上海药物研究所
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 暨南大学, 中国科学院上海药物研究所 filed Critical 暨南大学
Priority to CN201980077663.4A priority Critical patent/CN113166110B/zh
Publication of WO2020119739A1 publication Critical patent/WO2020119739A1/fr

Links

Classifications

    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

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

Abstract

La présente invention concerne un composé de 2-aminopyrimidine et son utilisation. La structure du composé de 2-aminopyrimidine est représentée en I; le composé peut inhiber de manière efficace l'activité de mutants résistant aux médicaments de protéine kinase EGFR (tels que EGFRT790M et EGFRT790M/C797S), et peut surmonter la résistance clinique aux médicaments de patients tumoraux ayant un cancer du poumon non à petites cellules et similaire induit par des inhibiteurs de petites molécules EGFRT790M sélectifs de troisième génération existants tels que Osimertinib (AZD9291), Olmutinib (HM6171) et Rociletinib (CO-1686).
PCT/CN2019/124686 2018-12-12 2019-12-11 Composé de 2-aminopyrimidine et son utilisation WO2020119739A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201980077663.4A CN113166110B (zh) 2018-12-12 2019-12-11 2-氨基嘧啶类化合物及其应用

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201811517594 2018-12-12
CN201811517594.8 2018-12-12

Publications (1)

Publication Number Publication Date
WO2020119739A1 true WO2020119739A1 (fr) 2020-06-18

Family

ID=71076798

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2019/124686 WO2020119739A1 (fr) 2018-12-12 2019-12-11 Composé de 2-aminopyrimidine et son utilisation

Country Status (2)

Country Link
CN (1) CN113166110B (fr)
WO (1) WO2020119739A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113264920A (zh) * 2021-05-10 2021-08-17 中国药科大学 一种嘧啶苯并六元环母核的cdk6抑制剂及其制备方法和应用
US11174252B2 (en) 2018-02-15 2021-11-16 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
CN115785134A (zh) * 2022-10-28 2023-03-14 浙大城市学院 一种含氮杂环的硼酸化合物及制备方法和应用

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220011663A (ko) * 2019-05-22 2022-01-28 상하이 한서 바이오메디컬 컴퍼니 리미티드 인돌 유도체-함유 억제제, 이의 제조 방법 또는 이의 적용
KR20230056331A (ko) * 2021-10-20 2023-04-27 한미약품 주식회사 급성 골수성 백혈병의 치료를 위한 FLT3 저해제와 Bcl-2 저해제의 치료 유효적 조합

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060183900A1 (en) * 2004-10-29 2006-08-17 Shenlin Huang Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US20100105655A1 (en) * 2008-10-29 2010-04-29 Astrazeneca Ab Novel compounds 515
CN101723936A (zh) * 2008-10-27 2010-06-09 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
US20100267707A1 (en) * 2006-06-22 2010-10-21 Merck Sharp & Dohme Corp. Tyrosine Kinase Inhibitors
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US20170121326A1 (en) * 2015-10-28 2017-05-04 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
WO2017200016A1 (fr) * 2016-05-17 2017-11-23 公益財団法人がん研究会 Agent thérapeutique pour le cancer bronchique ayant acquis une résistance à egfr-tki
CN107382974A (zh) * 2017-06-08 2017-11-24 扬州市三药制药有限公司 一种嘧啶胺类化合物作为周期蛋白依赖性激酶4/6抑制剂的应用
WO2019190259A1 (fr) * 2018-03-30 2019-10-03 한미약품 주식회사 Nouveau dérivé de sulfonamide ayant un effet inhibiteur sur la mutation du récepteur du facteur de croissance épidermique

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060183900A1 (en) * 2004-10-29 2006-08-17 Shenlin Huang Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US20100267707A1 (en) * 2006-06-22 2010-10-21 Merck Sharp & Dohme Corp. Tyrosine Kinase Inhibitors
CN101723936A (zh) * 2008-10-27 2010-06-09 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
US20100105655A1 (en) * 2008-10-29 2010-04-29 Astrazeneca Ab Novel compounds 515
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US20170121326A1 (en) * 2015-10-28 2017-05-04 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
WO2017200016A1 (fr) * 2016-05-17 2017-11-23 公益財団法人がん研究会 Agent thérapeutique pour le cancer bronchique ayant acquis une résistance à egfr-tki
CN107382974A (zh) * 2017-06-08 2017-11-24 扬州市三药制药有限公司 一种嘧啶胺类化合物作为周期蛋白依赖性激酶4/6抑制剂的应用
WO2019190259A1 (fr) * 2018-03-30 2019-10-03 한미약품 주식회사 Nouveau dérivé de sulfonamide ayant un effet inhibiteur sur la mutation du récepteur du facteur de croissance épidermique

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY STN; 14 October 2011 (2011-10-14), Database accession no. RN1335498-99-1 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11174252B2 (en) 2018-02-15 2021-11-16 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
CN113264920A (zh) * 2021-05-10 2021-08-17 中国药科大学 一种嘧啶苯并六元环母核的cdk6抑制剂及其制备方法和应用
CN115785134A (zh) * 2022-10-28 2023-03-14 浙大城市学院 一种含氮杂环的硼酸化合物及制备方法和应用
CN115785134B (zh) * 2022-10-28 2023-08-29 浙大城市学院 一种含氮杂环的硼酸化合物及制备方法和应用

Also Published As

Publication number Publication date
CN113166110B (zh) 2023-08-11
CN113166110A (zh) 2021-07-23

Similar Documents

Publication Publication Date Title
AU2015353210B2 (en) 2-aminopyrimidine compound and pharmaceutical composition and use thereof
WO2020119739A1 (fr) Composé de 2-aminopyrimidine et son utilisation
TWI726968B (zh) Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑
JP6517928B2 (ja) キナーゼ阻害剤として有用なインドールカルボキシアミド
KR101614572B1 (ko) 디아미노 헤테로환 카르복사미드 화합물
JP5756518B2 (ja) 複素環アルキニルベンゼン化合物と、その医療用組成物および使用
TWI221470B (en) Pyrimidine derivatives and pharmaceutical compositions containing the same
WO2017028797A1 (fr) Composition pharmaceutique et application remplaçant un dérivé de quinolone, sel pharmaceutiquement acceptable, ou stéréoisomère
CN103012399B (zh) 7-氧代吡啶并嘧啶类化合物及其药用组合物和应用
TW200924776A (en) Heteroaryl compounds and uses thereof
WO2016026445A1 (fr) Composés indazole utilisés comme inhibiteurs de la fgfr kinase, préparation et utilisation associées
NZ538617A (en) Azaarene derivatives
TW200819439A (en) 2-amino-5-substituted pyrimidine inhibitors
WO2018018986A1 (fr) Composé de diphénylaminopyrimidine et de triazine, composition pharmaceutique et utilisation de celui-ci
CN105518001A (zh) Bet蛋白抑制性的改性的二氢喹喔啉酮类化合物和二氢吡啶并吡嗪酮类化合物
CN110305161A (zh) 2-氨基嘧啶类化合物及其应用
PT3013814T (pt) Compostos de tetrahidrocarbazol e carbazol carboxamida substituídos úteis como inibidores de quinases
CN103539784A (zh) 杂环苯甲酰胺类化合物、药用组合物及其应用
JP2022530097A (ja) がんを処置するためのアシルスルホンアミド類
TW201623239A (zh) 新穎２－胺基－吡啶及２－胺基－嘧啶衍生物及其醫藥用途
WO2020135210A1 (fr) Composé aryle substitué, procédé de préparation correspondant et utilisation associée
WO2021088859A1 (fr) Composé d'indazole, composition pharmaceutique de celui-ci et ses applications
WO2022213932A1 (fr) Composé de pyrrolopyrimidinone et son utilisation
IL277671B1 (en) Quinoline (QUINOLINE) and quinazoline (QUINAZOLINE) compounds and their applications
CN112313213B (zh) 3-氨基吡唑类化合物及其应用

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 19895988

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 19895988

Country of ref document: EP

Kind code of ref document: A1