CA3137458A1 - Fgfr inhibitors and methods of use thereof - Google Patents

Fgfr inhibitors and methods of use thereof Download PDF

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Publication number
CA3137458A1
CA3137458A1 CA3137458A CA3137458A CA3137458A1 CA 3137458 A1 CA3137458 A1 CA 3137458A1 CA 3137458 A CA3137458 A CA 3137458A CA 3137458 A CA3137458 A CA 3137458A CA 3137458 A1 CA3137458 A1 CA 3137458A1
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CA
Canada
Prior art keywords
nitrogen
oxygen
sulfur
independently selected
instance
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
CA3137458A
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English (en)
French (fr)
Inventor
Bakary-Barry Toure
Heike SCHOENHERR
Alexander M. Taylor
Fabrizio Giordanetto
Demetri T. Moustakas
Thomas H. MCLEAN
Brandi M. HUDSON
Mary M. Mader
Pelin AYAZ
Dina A. SHARON
Ravi Kurukulasuriya
Alessandro Boezio
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.)
DE Shaw Research LLC
Relay Therapeutics Inc
Original Assignee
DE Shaw Research LLC
Relay Therapeutics Inc
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Filing date
Publication date
Application filed by DE Shaw Research LLC, Relay Therapeutics Inc filed Critical DE Shaw Research LLC
Publication of CA3137458A1 publication Critical patent/CA3137458A1/en
Pending legal-status Critical Current

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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/53—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
    • 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
    • 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
    • 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
    • C07D487/22—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 four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA3137458A 2019-05-13 2020-05-12 Fgfr inhibitors and methods of use thereof Pending CA3137458A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962846991P 2019-05-13 2019-05-13
US62/846,991 2019-05-13
US202062993957P 2020-03-24 2020-03-24
US62/993,957 2020-03-24
US202063011469P 2020-04-17 2020-04-17
US63/011,469 2020-04-17
PCT/US2020/032474 WO2020231990A1 (en) 2019-05-13 2020-05-12 Fgfr inhibitors and methods of use thereof

Publications (1)

Publication Number Publication Date
CA3137458A1 true CA3137458A1 (en) 2020-11-19

Family

ID=73289291

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3137458A Pending CA3137458A1 (en) 2019-05-13 2020-05-12 Fgfr inhibitors and methods of use thereof

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US (3) US12522605B2 (cg-RX-API-DMAC10.html)
EP (2) EP4306529B1 (cg-RX-API-DMAC10.html)
JP (2) JP7527309B2 (cg-RX-API-DMAC10.html)
KR (2) KR102923990B1 (cg-RX-API-DMAC10.html)
CN (2) CN119874707A (cg-RX-API-DMAC10.html)
AU (2) AU2020274083B9 (cg-RX-API-DMAC10.html)
BR (1) BR112021022457A2 (cg-RX-API-DMAC10.html)
CA (1) CA3137458A1 (cg-RX-API-DMAC10.html)
CL (1) CL2021002882A1 (cg-RX-API-DMAC10.html)
ES (2) ES3065954T3 (cg-RX-API-DMAC10.html)
IL (2) IL287940B2 (cg-RX-API-DMAC10.html)
MX (1) MX428348B (cg-RX-API-DMAC10.html)
PE (1) PE20220573A1 (cg-RX-API-DMAC10.html)
PH (1) PH12021552862A1 (cg-RX-API-DMAC10.html)
SG (1) SG11202111327XA (cg-RX-API-DMAC10.html)
TW (2) TWI855070B (cg-RX-API-DMAC10.html)
WO (1) WO2020231990A1 (cg-RX-API-DMAC10.html)

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TW202304889A (zh) * 2021-04-03 2023-02-01 大陸商海南耀臻生物醫藥科技有限公司 作為fgfr抑制劑的雜環化合物及其應用
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CN120051471A (zh) * 2022-10-18 2025-05-27 首药控股(北京)股份有限公司 一种新型杂环化合物
CN115594682B (zh) * 2022-10-26 2024-03-15 苏州浦合医药科技有限公司 Fgfr2抑制剂
WO2024109799A1 (zh) * 2022-11-22 2024-05-30 西藏海思科制药有限公司 一种嘧啶衍生物及其在医药上的应用
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TW202442224A (zh) * 2023-03-20 2024-11-01 香港商英矽智能科技知識產權有限公司 Fgfr2與fgfr3之抑制劑及其用途
WO2024208315A1 (zh) * 2023-04-07 2024-10-10 中国医药研究开发中心有限公司 芳香杂环类化合物及其制备方法和医药用途
WO2024245193A1 (zh) * 2023-05-26 2024-12-05 上海艾力斯医药科技股份有限公司 杂芳环类化合物、其药物组合物及其应用
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CN117343068B (zh) * 2023-09-28 2026-04-28 上海相辉医药科技有限公司 一种FGFR2抑制剂Lirafugratinib(RLY-4008)的制备方法
KR20260115897A (ko) * 2023-11-17 2026-07-27 상하이 치루 파마슈티컬 리서치 앤 디벨롭먼트 센터 리미티드 질소 함유 헤테로아릴 유도체, 이의 제조 방법 및 의약학적 응용
CN120230109A (zh) * 2023-12-29 2025-07-01 广州科恩泰生物医药科技有限公司 一种亚砜亚胺类化合物的酸式盐的晶型及其制备方法和用途
WO2025149021A1 (zh) * 2024-01-10 2025-07-17 海思科医药集团股份有限公司 一种吡啶并吡咯衍生物及其在医药上的应用
WO2025237312A1 (zh) * 2024-05-15 2025-11-20 深圳福沃药业有限公司 一类含苯并异噁唑结构的高选择性fgfr2抑制剂及其制备方法和应用
CN121270563A (zh) * 2024-07-01 2026-01-06 北京鞍石生物科技股份有限公司 稠环化合物及其制备方法和应用
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CN120136834B (zh) * 2025-02-13 2026-02-03 浙江工业大学 一种手性吡喃环化合物及其合成方法和应用

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