ECSP22033597A - Inhibidores de pequeñas moléculas de mutante g12c de kras - Google Patents

Inhibidores de pequeñas moléculas de mutante g12c de kras

Info

Publication number
ECSP22033597A
ECSP22033597A ECSENADI202233597A ECDI202233597A ECSP22033597A EC SP22033597 A ECSP22033597 A EC SP22033597A EC SENADI202233597 A ECSENADI202233597 A EC SENADI202233597A EC DI202233597 A ECDI202233597 A EC DI202233597A EC SP22033597 A ECSP22033597 A EC SP22033597A
Authority
EC
Ecuador
Prior art keywords
pharmaceutically acceptable
acceptable salts
compounds
small molecule
disclosure
Prior art date
Application number
ECSENADI202233597A
Other languages
English (en)
Inventor
Xiaoshen Ma
Thomas Graham
Ryan Otte
Yongxin Han
Anandan Palani
Symon Gathiaka
David Sloman
Timothy Henderson
Elisabeth Hennessy
Indu Bharathan
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of ECSP22033597A publication Critical patent/ECSP22033597A/es

Links

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
    • C07D471/02—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
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D471/22—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 systems contains four or more 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La divulgación proporciona compuestos de la fórmula (I) (conforme a figura constante en resumen de memoria técnica) o una de sus sales farmacéuticamente aceptables, en donde W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz y los subíndices m, n, q y r son como se describe en el presente documento. Los compuestos o sus sales farmacéuticamente aceptables pueden inhibir el mutante G12C de la proteína del sarcoma de rata de Kirsten (KRAS) y se espera que tengan utilidad como agentes terapéuticos, por ejemplo, para tratar el cáncer. La divulgación también proporciona composiciones farmacéuticas que comprenden compuestos de la fórmula (I) o sus sales farmacéuticamente aceptables. La divulgación también se refiere a métodos para el uso de los compuestos o sus sales farmacéuticamente aceptables en la terapia y profilaxis del cáncer y para preparar productos farmacéuticos para este propósito.
ECSENADI202233597A 2019-10-28 2022-04-27 Inhibidores de pequeñas moléculas de mutante g12c de kras ECSP22033597A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US202063030014P 2020-05-26 2020-05-26

Publications (1)

Publication Number Publication Date
ECSP22033597A true ECSP22033597A (es) 2022-05-31

Family

ID=73598936

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202233597A ECSP22033597A (es) 2019-10-28 2022-04-27 Inhibidores de pequeñas moléculas de mutante g12c de kras

Country Status (19)

Country Link
US (3) US11697657B2 (es)
EP (1) EP4051678A1 (es)
JP (2) JP7340100B2 (es)
KR (1) KR20220106980A (es)
CN (1) CN114867726B (es)
AU (1) AU2020372881A1 (es)
BR (1) BR112022007783A8 (es)
CA (1) CA3158793A1 (es)
CO (1) CO2022006858A2 (es)
CR (1) CR20220230A (es)
DO (1) DOP2022000090A (es)
EC (1) ECSP22033597A (es)
IL (1) IL292438A (es)
JO (1) JOP20220101A1 (es)
MX (1) MX2022005053A (es)
PE (1) PE20221253A1 (es)
TW (1) TW202130645A (es)
WO (1) WO2021086833A1 (es)
ZA (1) ZA202205938B (es)

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MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
CN114761012A (zh) 2019-09-24 2022-07-15 米拉蒂治疗股份有限公司 组合疗法
KR20220130126A (ko) 2019-12-20 2022-09-26 미라티 테라퓨틱스, 인크. Sos1 억제제
CN115003668A (zh) * 2020-01-21 2022-09-02 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
CN113248521B (zh) * 2020-02-11 2023-07-18 上海和誉生物医药科技有限公司 一种k-ras g12c抑制剂及其制备方法和应用
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CN116390919A (zh) * 2020-11-24 2023-07-04 杭州多域生物技术有限公司 一种芳香化合物、其制备方法及应用
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WO2022233316A1 (zh) * 2021-05-06 2022-11-10 南京明德新药研发有限公司 十二元大环类化合物
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2023018634A1 (en) * 2021-08-12 2023-02-16 Merck Sharp & Dohme Llc Dosage regimen for administration of belzutifan
WO2024040131A1 (en) 2022-08-17 2024-02-22 Treeline Biosciences, Inc. Pyridopyrimidine kras inhibitors
WO2024112654A1 (en) 2022-11-21 2024-05-30 Treeline Biosciences, Inc. Spirocyclic dihydropyranopyrimidine kras inhibitors
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