CN109467538A - 环烯烃取代的杂芳环类化合物及其用途 - Google Patents

环烯烃取代的杂芳环类化合物及其用途 Download PDF

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Publication number
CN109467538A
CN109467538A CN201710801364.3A CN201710801364A CN109467538A CN 109467538 A CN109467538 A CN 109467538A CN 201710801364 A CN201710801364 A CN 201710801364A CN 109467538 A CN109467538 A CN 109467538A
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CN
China
Prior art keywords
compound
formula
alkyl
halogen
solvate
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Pending
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CN201710801364.3A
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English (en)
Chinese (zh)
Inventor
苏慰国
戴广袖
肖坤
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Hutchmed Ltd
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Hutchison Medipharma 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 Hutchison Medipharma Ltd filed Critical Hutchison Medipharma Ltd
Priority to CN201710801364.3A priority Critical patent/CN109467538A/zh
Priority to PE2020000280A priority patent/PE20200727A1/es
Priority to EP18853366.5A priority patent/EP3679020A4/en
Priority to CN202311040510.7A priority patent/CN117024363A/zh
Priority to CN201880057118.4A priority patent/CN111132967B/zh
Priority to SG11202001642WA priority patent/SG11202001642WA/en
Priority to PCT/CN2018/104531 priority patent/WO2019047909A1/en
Priority to CN202311036845.1A priority patent/CN117257809A/zh
Priority to NZ762447A priority patent/NZ762447B2/en
Priority to AU2018329047A priority patent/AU2018329047B2/en
Priority to JP2020513872A priority patent/JP7273030B6/ja
Priority to KR1020207009621A priority patent/KR102566237B1/ko
Priority to EA202090653A priority patent/EA202090653A1/ru
Priority to CN202311036787.2A priority patent/CN116999441A/zh
Priority to UAA202002089A priority patent/UA129118C2/uk
Priority to ARP180102548A priority patent/AR112794A1/es
Priority to US16/645,329 priority patent/US11414390B2/en
Priority to CN202311036829.2A priority patent/CN117797156A/zh
Priority to MX2020002505A priority patent/MX2020002505A/es
Priority to TW107131525A priority patent/TWI816693B/zh
Priority to BR112020004563-2A priority patent/BR112020004563B1/pt
Priority to CA3073782A priority patent/CA3073782A1/en
Publication of CN109467538A publication Critical patent/CN109467538A/zh
Priority to IL272923A priority patent/IL272923B2/en
Priority to PH12020500408A priority patent/PH12020500408A1/en
Priority to CL2020000553A priority patent/CL2020000553A1/es
Priority to ZA2020/01448A priority patent/ZA202001448B/en
Priority to US17/747,925 priority patent/US12234211B2/en
Priority to JP2023072737A priority patent/JP7603740B2/ja
Priority to US19/050,772 priority patent/US20250223267A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/48—Two nitrogen atoms
    • 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
    • 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
    • A61K31/53—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
    • 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
    • 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
    • C07D403/02—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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN201710801364.3A 2017-09-07 2017-09-07 环烯烃取代的杂芳环类化合物及其用途 Pending CN109467538A (zh)

Priority Applications (29)

Application Number Priority Date Filing Date Title
CN201710801364.3A CN109467538A (zh) 2017-09-07 2017-09-07 环烯烃取代的杂芳环类化合物及其用途
US16/645,329 US11414390B2 (en) 2017-09-07 2018-09-07 Cycloolefin substituted heteroaromatic compounds and their use
ARP180102548A AR112794A1 (es) 2017-09-07 2018-09-07 Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso en el tratamiento de enfermedades inducidas por mutaciones idh
CN202311040510.7A CN117024363A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN201880057118.4A CN111132967B (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
SG11202001642WA SG11202001642WA (en) 2017-09-07 2018-09-07 Cycloolefin substituted heteroaromatic compounds and their use
PCT/CN2018/104531 WO2019047909A1 (en) 2017-09-07 2018-09-07 HETEROAROMATIC COMPOUNDS SUBSTITUTED WITH CYCLOOLEFINS AND THEIR USE
CN202311036845.1A CN117257809A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
NZ762447A NZ762447B2 (en) 2018-09-07 Cycloolefin substituted heteroaromatic compounds and their use
AU2018329047A AU2018329047B2 (en) 2017-09-07 2018-09-07 Cycloolefin substituted heteroaromatic compounds and their use
JP2020513872A JP7273030B6 (ja) 2017-09-07 2018-09-07 シクロオレフィン置換複素芳香族化合物およびそれらの使用
KR1020207009621A KR102566237B1 (ko) 2017-09-07 2018-09-07 사이클로올레핀 치환된 헤테로방향족 화합물 및 그의 용도
EA202090653A EA202090653A1 (ru) 2017-09-07 2018-09-07 Циклоолефиновые замещённые гетероароматические соединения и их применение
CN202311036787.2A CN116999441A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
UAA202002089A UA129118C2 (uk) 2017-09-07 2018-09-07 Циклоолефінозаміщені гетероароматичні сполуки та їх використання
PE2020000280A PE20200727A1 (es) 2017-09-07 2018-09-07 Compuestos heteroaromaticos sustituidos con cicloolefinas y su uso
CA3073782A CA3073782A1 (en) 2017-09-07 2018-09-07 Cycloolefin substituted heteroaromatic compounds and their use
CN202311036829.2A CN117797156A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
MX2020002505A MX2020002505A (es) 2017-09-07 2018-09-07 Compuestos heteroaromaticos sustituidos con cicloolefinas y su uso.
TW107131525A TWI816693B (zh) 2017-09-07 2018-09-07 環烯烴取代的雜芳環類化合物及其用途
BR112020004563-2A BR112020004563B1 (pt) 2017-09-07 2018-09-07 Compostos heteroaromáticos substituídos por ciclo-olefina e seu uso
EP18853366.5A EP3679020A4 (en) 2017-09-07 2018-09-07 CYCLOOLEFIN SUBSTITUTED HETEROAROMATIC COMPOUNDS AND THEIR USES
IL272923A IL272923B2 (en) 2017-09-07 2020-02-26 Disubstituted cycloolefin heteroaromatic compounds and their uses
PH12020500408A PH12020500408A1 (en) 2017-09-07 2020-02-28 Cycloolefin substituted heteroaromatic compounds and their use
CL2020000553A CL2020000553A1 (es) 2017-09-07 2020-03-05 Compuestos heteroaromáticos sustituidos con cicloolefinas y su uso.
ZA2020/01448A ZA202001448B (en) 2017-09-07 2020-03-06 Cycloolefin substituted heteroaromatic compounds and their use
US17/747,925 US12234211B2 (en) 2017-09-07 2022-05-18 Cycloolefin substituted heteroaromatic compounds and their use
JP2023072737A JP7603740B2 (ja) 2017-09-07 2023-04-26 シクロオレフィン置換複素芳香族化合物およびそれらの使用
US19/050,772 US20250223267A1 (en) 2017-09-07 2025-02-11 Cycloolefin substituted heteroaromatic compounds and their use

Applications Claiming Priority (1)

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CN201710801364.3A CN109467538A (zh) 2017-09-07 2017-09-07 环烯烃取代的杂芳环类化合物及其用途

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CN109467538A true CN109467538A (zh) 2019-03-15

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Family Applications (6)

Application Number Title Priority Date Filing Date
CN201710801364.3A Pending CN109467538A (zh) 2017-09-07 2017-09-07 环烯烃取代的杂芳环类化合物及其用途
CN201880057118.4A Active CN111132967B (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036845.1A Pending CN117257809A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036829.2A Pending CN117797156A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036787.2A Pending CN116999441A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311040510.7A Pending CN117024363A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途

Family Applications After (5)

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CN201880057118.4A Active CN111132967B (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036845.1A Pending CN117257809A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036829.2A Pending CN117797156A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311036787.2A Pending CN116999441A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途
CN202311040510.7A Pending CN117024363A (zh) 2017-09-07 2018-09-07 环烯烃取代的杂芳环类化合物及其用途

Country Status (19)

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US (3) US11414390B2 (https=)
EP (1) EP3679020A4 (https=)
JP (2) JP7273030B6 (https=)
KR (1) KR102566237B1 (https=)
CN (6) CN109467538A (https=)
AR (1) AR112794A1 (https=)
AU (1) AU2018329047B2 (https=)
CA (1) CA3073782A1 (https=)
CL (1) CL2020000553A1 (https=)
EA (1) EA202090653A1 (https=)
IL (1) IL272923B2 (https=)
MX (1) MX2020002505A (https=)
PE (1) PE20200727A1 (https=)
PH (1) PH12020500408A1 (https=)
SG (1) SG11202001642WA (https=)
TW (1) TWI816693B (https=)
UA (1) UA129118C2 (https=)
WO (1) WO2019047909A1 (https=)
ZA (1) ZA202001448B (https=)

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CN111132967A (zh) * 2017-09-07 2020-05-08 和记黄埔医药（上海）有限公司 环烯烃取代的杂芳环类化合物及其用途
WO2022095756A1 (zh) * 2020-11-09 2022-05-12 贝达药业股份有限公司 突变型idh1和idh2抑制剂及其应用
WO2023134686A1 (zh) * 2022-01-11 2023-07-20 正大天晴药业集团股份有限公司 一种1,3,5-三嗪衍生物的制备方法

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KR102917509B1 (ko) 2017-09-07 2026-01-26 오거스타 유니버시티 리서치 인스티튜트, 인크. 특이적 akt3 활성제 및 이의 용도

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