IL287940B2 - FGFR inhibitors and methods of using them - Google Patents

FGFR inhibitors and methods of using them

Info

Publication number
IL287940B2
IL287940B2 IL287940A IL28794021A IL287940B2 IL 287940 B2 IL287940 B2 IL 287940B2 IL 287940 A IL287940 A IL 287940A IL 28794021 A IL28794021 A IL 28794021A IL 287940 B2 IL287940 B2 IL 287940B2
Authority
IL
Israel
Prior art keywords
cancer
compound
pharmaceutical composition
disorder
pharmaceutically acceptable
Prior art date
Application number
IL287940A
Other languages
English (en)
Hebrew (he)
Other versions
IL287940B1 (en
IL287940A (en
Original Assignee
Relay Therapeutics Inc
De Shaw Res Llc
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 Relay Therapeutics Inc, De Shaw Res Llc filed Critical Relay Therapeutics Inc
Publication of IL287940A publication Critical patent/IL287940A/en
Publication of IL287940B1 publication Critical patent/IL287940B1/en
Publication of IL287940B2 publication Critical patent/IL287940B2/en

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Classifications

    • 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
    • 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
    • C07D487/02—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
    • 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)
IL287940A 2019-05-13 2020-05-12 FGFR inhibitors and methods of using them IL287940B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962846991P 2019-05-13 2019-05-13
US202062993957P 2020-03-24 2020-03-24
US202063011469P 2020-04-17 2020-04-17
PCT/US2020/032474 WO2020231990A1 (en) 2019-05-13 2020-05-12 Fgfr inhibitors and methods of use thereof

Publications (3)

Publication Number Publication Date
IL287940A IL287940A (en) 2022-01-01
IL287940B1 IL287940B1 (en) 2025-11-01
IL287940B2 true IL287940B2 (en) 2026-03-01

Family

ID=73289291

Family Applications (2)

Application Number Title Priority Date Filing Date
IL287940A IL287940B2 (en) 2019-05-13 2020-05-12 FGFR inhibitors and methods of using them
IL323675A IL323675A (en) 2019-05-13 2025-09-29 FGFR inhibitors and methods of using them

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL323675A IL323675A (en) 2019-05-13 2025-09-29 FGFR inhibitors and methods of using them

Country Status (17)

Country Link
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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ES3065954T3 (en) * 2019-05-13 2026-05-08 Relay Therapeutics Inc Fgfr inhibitors and methods of use thereof
JP2021017595A (ja) * 2019-07-18 2021-02-15 花王株式会社 アニオン変性セルロース
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
AU2021263914B2 (en) 2020-04-29 2026-07-23 D.E. Shaw Research, Llc PI3K-α inhibitors and methods of use thereof
TWI924727B (zh) 2020-11-18 2026-05-11 美商傳達治療有限公司 Ｆｇｆｒ抑制劑及其製造及使用方法
CN115160319B (zh) * 2021-04-01 2023-12-26 西安新通药物研究股份有限公司 含1,3-苯并二氧戊环结构的化合物及其制备方法与用途
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
WO2023011581A1 (zh) * 2021-08-04 2023-02-09 江苏恒瑞医药股份有限公司 含氮杂环化合物、其制备方法及其在医药上的应用
CA3231948A1 (en) * 2021-09-23 2023-03-30 Jingyu Hu Fgfr inhibitors and methods of use thereof
WO2023104035A1 (zh) * 2021-12-06 2023-06-15 英矽智能科技(上海)有限公司 取代的单环或双环杂环化合物，其制法与医药上的用途
WO2023151560A1 (en) * 2022-02-08 2023-08-17 Etern Biopharma (Shanghai) Co., Ltd. Bicyclic heteroaryl compounds and uses thereof
US20260152503A1 (en) * 2022-03-31 2026-06-04 Acerand Therapeutics (Hong Kong) Limited Spirobicyclic compounds
WO2023202625A1 (zh) * 2022-04-20 2023-10-26 深圳福沃药业有限公司 Fgfr2抑制剂及使用方法
US20250313524A1 (en) * 2022-05-10 2025-10-09 Relay Therapeutics, Inc. Pi3k-alpha inhibitors and methods of use thereof
JP2025523588A (ja) * 2022-06-29 2025-07-23 インシリコ メディスン アイピー リミテッド Ｆｇｆｒ２及びｆｇｆｒ３の阻害剤並びにその使用
CN119421872A (zh) * 2022-06-29 2025-02-11 上海翰森生物医药科技有限公司 杂环类衍生物抑制剂、其制备方法和应用
CN117402161A (zh) * 2022-07-06 2024-01-16 上海科恩泰生物医药科技有限公司 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途
CA3266687A1 (en) * 2022-09-07 2024-03-14 Eli Lilly And Company PYRAZOLO[1,5-A]PYRIDINE AND IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS FGFR3 INHIBITORS FOR CANCER TREATMENT
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
WO2024175121A1 (zh) * 2023-02-24 2024-08-29 希格生科（深圳）有限公司 α，β-不饱和酰胺类化合物及其应用
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
KR20260009912A (ko) 2023-06-05 2026-01-20 캉바이다 (시추안) 바이오테크놀로지 씨오. 엘티디. 피롤로피리미딘 유도체 및 의약물 제조에서 이의 용도
WO2025067484A1 (en) * 2023-09-28 2025-04-03 Acerand Therapeutics (Hong Kong) Limited Crystal forms and salts of spirobicyclic compound
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
WO2026119036A1 (zh) * 2024-12-04 2026-06-11 康百达（四川）生物医药科技有限公司 一种吡咯并嘧啶衍生物的晶型及其制备方法
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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