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MX388781B - SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF KRAS, HRAS AND/OR NRAS MUTANT G12C PROTEINS. - Google Patents

SUBSTITUTED QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF KRAS, HRAS AND/OR NRAS MUTANT G12C PROTEINS.

Info

Publication number
MX388781B
MX388781B MX2018000777A MX2018000777A MX388781B MX 388781 B MX388781 B MX 388781B MX 2018000777 A MX2018000777 A MX 2018000777A MX 2018000777 A MX2018000777 A MX 2018000777A MX 388781 B MX388781 B MX 388781B
Authority
MX
Mexico
Prior art keywords
inhibitors
compounds
hras
kras
proteins
Prior art date
Application number
MX2018000777A
Other languages
Spanish (es)
Other versions
MX2018000777A (en
Inventor
Jun Feng
Li Liansheng
Pingda Ren
Tao Wu
Yi Liu
Yu Oliver LONG
Yuan Liu
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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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 are provided that have activity as inhibitors of the G12C mutant KRAS protein. 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 herein. Also provided are 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 KRAS protein for the treatment of disorders, such as cancer.

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 MX2018000777A (en) 2018-03-23
MX388781B true 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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