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MX2018000777A - Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins. - Google Patents

Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins.

Info

Publication number
MX2018000777A
MX2018000777A MX2018000777A MX2018000777A MX2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A
Authority
MX
Mexico
Prior art keywords
inhibitors
compounds
hras
quinazoline compounds
mutant kras
Prior art date
Application number
MX2018000777A
Other languages
Spanish (es)
Other versions
MX388781B (en
Inventor
Li Liansheng
Liu Yuan
Liu Yi
Ren Pingda
Wu Tao
FENG Jung
Oliver Long Yu
Original Assignee
Araxes Pharma 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
Priority claimed from JOP/2016/0150A external-priority patent/JOP20160150B1/en
Application filed by Araxes Pharma Llc filed Critical Araxes Pharma Llc
Publication of MX2018000777A publication Critical patent/MX2018000777A/en
Publication of MX388781B publication Critical patent/MX388781B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)

Abstract

Se proveen compuestos que tienen actividad como inhibidores del mutante G12C de la proteína KRAS. Los compuestos tienen la siguiente estructura (I) (ver Fórmula) o una sal, estereoisómero o profármaco del mismo farmacéuticamente aceptable, en donde R, R1, R2a, R2b, R2C, A, B, L1 y E son como se define en la presente. También se proveen métodos asociados con la preparación y uso de los compuestos, composiciones farmacéuticas que comprenden los compuestos y métodos para modular la actividad del mutante G12C de la proteína KRAS para el tratamiento de trastornos, tales como cáncer.Compounds that have activity as inhibitors of the G12C mutant of the KRAS protein are provided. The compounds have the following structure (I) (see Formula) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R, R1, R2a, R2b, R2C, A, B, L1 and E are as defined in Present. Methods associated with the preparation and use of the compounds, pharmaceutical compositions comprising the compounds and methods for modulating the activity of the G12C mutant of the KRAS protein for the treatment of disorders, such as cancer, are also provided.

MX2018000777A 2015-07-22 2016-07-22 SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF KRAS, HRAS AND/OR NRAS MUTANT G12C PROTEINS. MX388781B (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562195636P 2015-07-22 2015-07-22
US201662342078P 2016-05-26 2016-05-26
GC201631750 2016-07-21
JOP/2016/0150A JOP20160150B1 (en) 2015-07-22 2016-07-21 Substituted quinazoline compounds and methods of use thereof
PCT/US2016/043568 WO2017015562A1 (en) 2015-07-22 2016-07-22 Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins

Publications (2)

Publication Number Publication Date
MX2018000777A true MX2018000777A (en) 2018-03-23
MX388781B MX388781B (en) 2025-03-20

Family

ID=57821530

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2018000777A MX388781B (en) 2015-07-22 2016-07-22 SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF KRAS, HRAS AND/OR NRAS MUTANT G12C PROTEINS.

Country Status (5)

Country Link
EP (1) EP3325447A1 (en)
JP (1) JP6869947B2 (en)
CA (1) CA2993013A1 (en)
MX (1) MX388781B (en)
WO (1) WO2017015562A1 (en)

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Also Published As

Publication number Publication date
WO2017015562A1 (en) 2017-01-26
EP3325447A1 (en) 2018-05-30
JP2018520195A (en) 2018-07-26
JP6869947B2 (en) 2021-05-12
CA2993013A1 (en) 2017-01-26
MX388781B (en) 2025-03-20

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