CN116113626A - 一种具有抗肿瘤活性的化合物及其用途 - Google Patents

一种具有抗肿瘤活性的化合物及其用途 Download PDF

Info

Publication number
CN116113626A
CN116113626A CN202180053993.7A CN202180053993A CN116113626A CN 116113626 A CN116113626 A CN 116113626A CN 202180053993 A CN202180053993 A CN 202180053993A CN 116113626 A CN116113626 A CN 116113626A
Authority
CN
China
Prior art keywords
amino
compound
hydrogen
independently
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN202180053993.7A
Other languages
English (en)
Inventor
党群
杨汉煜
李磐
蒋春华
尹洲
马建斌
付小旦
蔡欣
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Yishi Pharmaceutical Technology Co ltd
Original Assignee
Shanghai Yishi Pharmaceutical Technology Co ltd
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 Shanghai Yishi Pharmaceutical Technology Co ltd filed Critical Shanghai Yishi Pharmaceutical Technology Co ltd
Publication of CN116113626A publication Critical patent/CN116113626A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明提供了一种作为PRMT5抑制剂的具有全新结构的化合物、其化合物的制备方法及其治疗由PRMT5抑制剂介导的疾病方面的用途。实验证实这些化合物对PRMT5酶都具有较强的抑制作用，可作为治疗PRMT5抑制剂介导的疾病的前景化合物。此外，本发明研究了特定的合成方法，该合成方法工艺简单，操作便捷，利于规模化工业生产和应用。

Description

PCT国内申请，说明书已公开。

Claims (46)

  1. PCT国内申请，权利要求书已公开。
CN202180053993.7A 2020-09-04 2021-09-03 一种具有抗肿瘤活性的化合物及其用途 Pending CN116113626A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN202010921153 2020-09-04
CN2020109211535 2020-09-04
PCT/CN2021/116418 WO2022048631A1 (zh) 2020-09-04 2021-09-03 一种具有抗肿瘤活性的化合物及其用途

Publications (1)

Publication Number Publication Date
CN116113626A true CN116113626A (zh) 2023-05-12

Family

ID=80492224

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180053993.7A Pending CN116113626A (zh) 2020-09-04 2021-09-03 一种具有抗肿瘤活性的化合物及其用途

Country Status (5)

Country Link
EP (1) EP4209485A1 (zh)
JP (1) JP2023540548A (zh)
KR (1) KR20230047458A (zh)
CN (1) CN116113626A (zh)
WO (1) WO2022048631A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022237858A1 (zh) * 2021-05-13 2022-11-17 上海翊石医药科技有限公司 一种具有抗肿瘤活性的化合物及其用途
WO2024067433A1 (zh) * 2022-09-26 2024-04-04 上海湃隆生物科技有限公司 新型prmt5抑制剂及其应用
WO2024099411A1 (zh) * 2022-11-11 2024-05-16 石药集团中奇制药技术（石家庄）有限公司 一种杂环类抗肿瘤化合物的盐及其晶型

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015008052A (es) * 2012-12-21 2016-08-18 Epizyme Inc Inhibidores de prmt5 y sus usos.
CA2894130A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
CA2899363A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894126A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
JP2016511744A (ja) 2012-12-21 2016-04-21 エピザイム，インコーポレイティド Ｐｒｍｔ５を阻害する方法
WO2015200677A2 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US20170198006A1 (en) 2014-06-25 2017-07-13 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CN108570059B (zh) 2017-03-09 2022-02-08 中国科学院上海药物研究所 一种具有prmt5抑制活性的化合物及其制备和应用
GB201704327D0 (en) 2017-03-17 2017-05-03 Argonaut Therapeutics Ltd Compounds
IL274762B2 (en) 2017-11-24 2023-10-01 Jubilant Episcribe Llc Novel heterocyclic compounds as PRMT5 inhibitors
US11591326B2 (en) 2018-03-09 2023-02-28 Pharmablock Sciences (Nanjing), Inc. Inhibitors of protein arginine methyltransferase 5 (PRMT5), pharmaceutical products thereof, and methods thereof
US11993602B2 (en) * 2018-08-07 2024-05-28 Merck Sharp & Dohme Llc PRMT5 inhibitors
US20230108114A1 (en) * 2019-12-17 2023-04-06 Merck Sharp & Dohme Llc Prmt5 inhibitors
CA3160153A1 (en) * 2019-12-17 2021-06-24 Michelle Machacek Prmt5 inhibitors
CN111592522B (zh) * 2020-06-17 2022-09-09 郑州大学 一种精氨酸甲基化转移酶5小分子抑制剂及其制备方法和用途

Also Published As

Publication number Publication date
EP4209485A1 (en) 2023-07-12
KR20230047458A (ko) 2023-04-07
WO2022048631A1 (zh) 2022-03-10
JP2023540548A (ja) 2023-09-25

Similar Documents

Publication Publication Date Title
CN107530329B (zh) 用作CDK抑制剂的吡唑并[1，5-a][1，3，5]三嗪和吡唑并[1，5-a]嘧啶衍生物
CA2984586C (en) Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor
RU2632907C2 (ru) Дейтерированные диаминопиримидиновые соединения и фармацевтические композиции, содержащие такие соединения
AU2020446002A1 (en) Benzothiazolyl biaryl compound, and preparation method and use
EP3080100B1 (en) Inhibitors of lysine specific demethylase-1
AU2015317741B2 (en) MK2 inhibitors and uses thereof
IL293962A (en) Mutant kras protein inhibitors
JP2022081606A (ja) Ｅｈｍｔ１およびｅｈｍｔ２阻害剤としてのアミン置換アリールまたはヘテロアリール化合物
CN116113626A (zh) 一种具有抗肿瘤活性的化合物及其用途
EP3967695B1 (en) 1-(7-(quinazolin-4-yl)-2,7-diazaspiro[3.5]nonan-2-yl)prop-2-en-1-one derivatives as kras inhibitors for the treatment of cancer
JP2023528903A (ja) Ｋｒａｓ ｇ１２ｃタンパク質阻害剤およびその使用
JP2018507883A (ja) 抗がん剤としての置換２−ｈ−ピラゾール誘導体
AU2007338754A1 (en) 5-cyan0-4- (pyrrolo [2, 3B] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
EP4339193A1 (en) Compound having anti-tumor activity and use thereof
CN114430740A (zh) Egfr抑制剂、组合物及其制备方法
WO2020215998A1 (zh) 嘧啶并五元杂环类化合物及其作为突变型idh2抑制剂的用途
CN114072412B (zh) 三环化合物、药物组合物及其应用
EP3865488A1 (en) Macrocyclic compound as cdk inhibitor, preparation method therefor, and use thereof in medicine
CN114885607B (zh) 喹啉基膦氧化合物及其组合物和用途
CN109020957B (zh) 作为mnk抑制剂的杂环化合物
KR20230043955A (ko) 키나아제 억제 활성을 갖는 화합물
AU2020412779A1 (en) Ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) modulators and uses thereof
CA3043948C (en) Fgfr4 inhibitor and preparation method and use thereof
CN113004285B (zh) 杂环化合物及其药物组合物、制备方法、中间体和应用
TW202024057A (zh) 吡唑化合物及其藥物組合物及應用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40084497

Country of ref document: HK