TW202308632A - 抑制ras的方法 - Google Patents

抑制ras的方法 Download PDF

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Publication number
TW202308632A
TW202308632A TW111112802A TW111112802A TW202308632A TW 202308632 A TW202308632 A TW 202308632A TW 111112802 A TW111112802 A TW 111112802A TW 111112802 A TW111112802 A TW 111112802A TW 202308632 A TW202308632 A TW 202308632A
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TW
Taiwan
Prior art keywords
optionally substituted
membered
alkyl
hydrogen
ras
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TW111112802A
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English (en)
Chinese (zh)
Inventor
萊恩 Ｂ 科克蘭
羅伯特 Ｊ 尼科爾斯
Original Assignee
美商綜合醫院股份有限公司
美商銳新醫藥有限公司
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Publication of TW202308632A publication Critical patent/TW202308632A/zh

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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Saccharide Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
TW111112802A 2021-04-02 2022-04-01 抑制ras的方法 TW202308632A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202163170292P 2021-04-02 2021-04-02
US63/170,292 2021-04-02
US202163192843P 2021-05-25 2021-05-25
US63/192,843 2021-05-25

Publications (1)

Publication Number Publication Date
TW202308632A true TW202308632A (zh) 2023-03-01

Family

ID=83456876

Family Applications (1)

Application Number Title Priority Date Filing Date
TW111112802A TW202308632A (zh) 2021-04-02 2022-04-01 抑制ras的方法

Country Status (12)

Country Link
US (1) US20240108630A1 (https=)
EP (1) EP4320143A4 (https=)
JP (1) JP2024512767A (https=)
KR (1) KR20240004436A (https=)
AU (1) AU2022249177A1 (https=)
BR (1) BR112023020182A2 (https=)
CA (1) CA3214155A1 (https=)
CR (1) CR20230500A (https=)
IL (1) IL307396A (https=)
MX (1) MX2023011608A (https=)
TW (1) TW202308632A (https=)
WO (1) WO2022212894A1 (https=)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023199180A1 (en) * 2022-04-11 2023-10-19 Novartis Ag Therapeutic uses of a krasg12c inhibitor
CN119301132A (zh) * 2022-06-01 2025-01-10 豪夫迈·罗氏有限公司 用于治疗癌症的卤代吲哚大环化合物
CN117720556A (zh) * 2022-09-19 2024-03-19 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物及其制备方法和用途
EP4582426A4 (en) * 2022-09-19 2025-12-24 Adlai Nortye Biopharma Co Ltd PAN-KRAS INHIBITOR COMPOUND
CN119522225A (zh) 2022-09-29 2025-02-25 广州嘉越医药科技有限公司 大环衍生物及其应用
WO2024104364A1 (zh) * 2022-11-16 2024-05-23 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
CN117534684A (zh) * 2022-11-29 2024-02-09 杭州阿诺生物医药科技有限公司 一种pan-KRAS抑制剂化合物
IL322278A (en) * 2023-02-06 2025-09-01 Bicara Therapeutics Inc Combined therapy and related methods
CR20250329A (es) 2023-02-14 2025-09-12 Hoffmann La Roche Compuestos tricíclicos para el tratamiento del cáncer
WO2024187174A2 (en) * 2023-03-09 2024-09-12 Aadigen, Llc Compositions for treating cancer with kras mutations and uses thereof
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
WO2025051241A1 (zh) * 2023-09-06 2025-03-13 劲方医药科技(上海)股份有限公司 大环化合物及其抗体-药物偶联物
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025087431A1 (zh) * 2023-10-27 2025-05-01 贝达药业股份有限公司 泛-kras抑制剂及其在医药上的应用
WO2025093625A1 (en) * 2023-11-01 2025-05-08 F. Hoffmann-La Roche Ag Macrocycle compounds for the treatment of cancer
WO2025119392A1 (zh) * 2023-12-08 2025-06-12 正大天晴药业集团股份有限公司 含有酰胺取代的大环类化合物
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025193628A2 (en) * 2024-03-09 2025-09-18 Aadigen, Llc Compositions for treating cancer with kras mutations and uses thereof
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025252241A1 (zh) * 2024-06-07 2025-12-11 杭州和正医药有限公司 一种大环衍生物及其用途
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
WO2026015745A1 (en) * 2024-07-11 2026-01-15 Treeline Biosciences, Inc. Macrocyclic ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101602876B1 (ko) * 2014-07-22 2016-03-11 아주대학교산학협력단 완전한 이뮤노글로불린 형태의 세포질 침투능을 갖는 항체를 이용하여 세포내 활성화된 ras를 억제하는 방법 및 그의 이용
KR20210116479A (ko) * 2018-12-21 2021-09-27 레볼루션 메디슨즈, 인크. 공동 결합에 참여하는 화합물 및 그의 용도
MX2023003060A (es) * 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.

Also Published As

Publication number Publication date
AU2022249177A1 (en) 2023-10-19
EP4320143A1 (en) 2024-02-14
MX2023011608A (es) 2023-12-14
IL307396A (en) 2023-12-01
KR20240004436A (ko) 2024-01-11
BR112023020182A2 (pt) 2023-12-12
WO2022212894A1 (en) 2022-10-06
CR20230500A (es) 2024-02-13
US20240108630A1 (en) 2024-04-04
CA3214155A1 (en) 2022-10-06
EP4320143A4 (en) 2025-02-19
JP2024512767A (ja) 2024-03-19

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