CN118900838A - 杂环化合物、其组合物及其治疗方法 - Google Patents

杂环化合物、其组合物及其治疗方法 Download PDF

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Publication number
CN118900838A
CN118900838A CN202380028687.7A CN202380028687A CN118900838A CN 118900838 A CN118900838 A CN 118900838A CN 202380028687 A CN202380028687 A CN 202380028687A CN 118900838 A CN118900838 A CN 118900838A
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China
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substituted
unsubstituted
compound
fluoro
methoxy
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CN202380028687.7A
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English (en)
Chinese (zh)
Inventor
喻超
陈捷
孙汉资
刘华庆
王策
王志伟
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Beone Pharmaceutical Suzhou Co Ltd
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Beigene Ltd
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Publication of CN118900838A publication Critical patent/CN118900838A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/537Heterocyclic 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 spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
CN202380028687.7A 2022-03-24 2023-03-23 杂环化合物、其组合物及其治疗方法 Pending CN118900838A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2022082722 2022-03-24
CNPCT/CN2022/082722 2022-03-24
PCT/CN2023/083294 WO2023179703A1 (en) 2022-03-24 2023-03-23 Heterocyclic compounds, compositions thereof, and methods of treatment therewith

Publications (1)

Publication Number Publication Date
CN118900838A true CN118900838A (zh) 2024-11-05

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Family Applications (1)

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CN202380028687.7A Pending CN118900838A (zh) 2022-03-24 2023-03-23 杂环化合物、其组合物及其治疗方法

Country Status (5)

Country Link
US (1) US20250101028A1 (https=)
EP (1) EP4499639A1 (https=)
JP (1) JP2025510656A (https=)
CN (1) CN118900838A (https=)
WO (1) WO2023179703A1 (https=)

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EP4373822A2 (en) 2021-07-23 2024-05-29 Theras Inc. Compositions and methods for inhibition of ras
JP2024543879A (ja) * 2021-11-24 2024-11-26 メルク・シャープ・アンド・ドーム・エルエルシー Kras変異型タンパク質の小分子阻害剤
JP2025525938A (ja) * 2022-08-05 2025-08-07 セラス, インコーポレイテッド Krasの阻害のための組成物及び方法
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
AU2024323424A1 (en) 2023-08-17 2026-03-05 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
AU2024337913A1 (en) 2023-09-08 2026-03-26 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
TW202528315A (zh) 2023-09-21 2025-07-16 美商樹線生物科學公司 螺環二氫哌喃并吡啶KRas抑制劑
US20250114339A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor
AU2024357850A1 (en) 2023-10-09 2026-04-23 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025090811A1 (en) * 2023-10-25 2025-05-01 Kumquat Biosciences Inc. Methods of modulating cell proliferation
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025245127A1 (en) 2024-05-21 2025-11-27 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026035945A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload
WO2026035947A1 (en) 2024-08-07 2026-02-12 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026064520A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload
WO2026064527A1 (en) 2024-09-19 2026-03-26 Tesseract Medicines Us, Llc Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

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EP4192585A4 (en) * 2020-08-04 2024-08-21 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2022132200A1 (en) * 2020-12-15 2022-06-23 Mirati Therapeutics, Inc. Azaquinazoline pan-kras inhibitors
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CN115304623A (zh) * 2021-04-30 2022-11-08 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用
WO2022247760A1 (zh) * 2021-05-22 2022-12-01 上海科州药物研发有限公司 作为kras抑制剂的杂环化合物,及其制备和治疗用途
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EP4373822A2 (en) * 2021-07-23 2024-05-29 Theras Inc. Compositions and methods for inhibition of ras
WO2023020521A1 (en) * 2021-08-18 2023-02-23 Jacobio Pharmaceuticals Co., Ltd. Pyridine fused pyrimidine derivatives and use thereof
CN117858878A (zh) * 2021-08-18 2024-04-09 北京加科思新药研发有限公司 N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途
WO2023056951A1 (zh) * 2021-10-08 2023-04-13 杭州德睿智药科技有限公司 芳基取代并杂环化合物
WO2023061294A1 (zh) * 2021-10-13 2023-04-20 再鼎医药(上海)有限公司 含氮杂环类衍生物调节剂、其制备方法及应用
WO2023072188A1 (zh) * 2021-10-29 2023-05-04 贝达药业股份有限公司 Kras g12d抑制剂及其在医药上的应用
TW202334138A (zh) * 2021-11-05 2023-09-01 美商新領域醫藥公司 癌症治療方法

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Publication number Publication date
EP4499639A1 (en) 2025-02-05
US20250101028A1 (en) 2025-03-27
WO2023179703A1 (en) 2023-09-28
JP2025510656A (ja) 2025-04-15

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Effective date of registration: 20251022

Address after: 215002 Jiangsu Province Suzhou City China (Shanghai) Pilot Free Trade Zone Suzhou Area Suzhou Industrial Park Jinhai Road 29.NO

Applicant after: Baiji Shenzhou (Suzhou) Biotechnology Co.,Ltd.

Country or region after: China

Address before: 94 sonaris Avenue, kamana Bay, grand caiman, British Isles

Applicant before: BEIGENE, Ltd.

Country or region before: Cayman Islands

TA01 Transfer of patent application right