BR112022007783A8 - Composto, composição farmacêutica, e, métodos para inibir proteína g12c de kras e para tratar câncer - Google Patents

Composto, composição farmacêutica, e, métodos para inibir proteína g12c de kras e para tratar câncer

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Publication number
BR112022007783A8
BR112022007783A8 BR112022007783A BR112022007783A BR112022007783A8 BR 112022007783 A8 BR112022007783 A8 BR 112022007783A8 BR 112022007783 A BR112022007783 A BR 112022007783A BR 112022007783 A BR112022007783 A BR 112022007783A BR 112022007783 A8 BR112022007783 A8 BR 112022007783A8
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methods
protein
treat cancer
pharmaceutically acceptable
compound
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BR112022007783A
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English (en)
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BR112022007783A2 (pt
Inventor
Bharathan Indu
Gathiaka Symon
H Graham Thomas
Han Yongxin
Henderson Timothy
Hennessy Elisabeth
Ma Xiaoshen
Otte Ryan
Palani Anandan
L Sloman David
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Merck Sharp & Dohme
Merck Sharp & Dohme Llc
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Publication of BR112022007783A2 publication Critical patent/BR112022007783A2/pt
Publication of BR112022007783A8 publication Critical patent/BR112022007783A8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/519Pyrimidines; 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • 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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

COMPOSTO, COMPOSIÇÃO FARMACÊUTICA, E, MÉTODOS PARA INIBIR PROTEÍNA G12C DE KRAS E PARA TRATAR CÂNCER. A descrição provê compostos da Fórmula (I) ou um sal farmaceuticamente aceitável dos mesmos, em que W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Ry, Rz e os subscritos m, n, q e r são como aqui descritos. Os compostos ou seus sais farmaceuticamente aceitáveis podem inibir o mutante G12C da proteína do sarcoma de rato Kirsten (KRAS) e são esperados ter utilidade como agentes terapêuticos, por exemplo, para tratar câncer. A descrição também provê composições farmacêuticas que compreendem compostos da Fórmula (I) ou sais farmaceuticamente aceitáveis do mesmo. A descrição também se refere aos métodos para o uso dos compostos ou seus sais farmaceuticamente aceitáveis na terapia e profilaxia de câncer e para preparar produtos farmacêuticos para este propósito.
BR112022007783A 2019-10-28 2020-10-27 Composto, composição farmacêutica, e, métodos para inibir proteína g12c de kras e para tratar câncer BR112022007783A8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926879P 2019-10-28 2019-10-28
US202063030014P 2020-05-26 2020-05-26
PCT/US2020/057496 WO2021086833A1 (en) 2019-10-28 2020-10-27 Small molecule inhibitors of kras g12c mutant

Publications (2)

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BR112022007783A2 BR112022007783A2 (pt) 2022-07-05
BR112022007783A8 true BR112022007783A8 (pt) 2023-04-11

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Country Status (19)

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

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