BR112022023462A2 - 2-amino-3-ciano tiofenos anulados e derivados para o tratamento de câncer - Google Patents

2-amino-3-ciano tiofenos anulados e derivados para o tratamento de câncer

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Publication number
BR112022023462A2
BR112022023462A2 BR112022023462A BR112022023462A BR112022023462A2 BR 112022023462 A2 BR112022023462 A2 BR 112022023462A2 BR 112022023462 A BR112022023462 A BR 112022023462A BR 112022023462 A BR112022023462 A BR 112022023462A BR 112022023462 A2 BR112022023462 A2 BR 112022023462A2
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BR
Brazil
Prior art keywords
treatment
thiophenes
cyan
deleted
cancer
Prior art date
Application number
BR112022023462A
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English (en)
Inventor
Abbott Jason
Broeker Joachim
Cui Jianwen
W Fesik Stephen
Gollner Andreas
Hodges Tim
Karolyi-Oezguer Jale
Little Andrew
Mantoulidis Andreas
Phan Jason
Sarkar Dhruba
Alan Paul Smethurst Christian
Sun Qi
Treu Matthias
Waterson Alex
Original Assignee
Boehringer Ingelheim Int
Univ Vanderbilt
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Application filed by Boehringer Ingelheim Int, Univ Vanderbilt filed Critical Boehringer Ingelheim Int
Publication of BR112022023462A2 publication Critical patent/BR112022023462A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three 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
    • 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
    • C07D471/08Bridged systems
    • 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems

Abstract

A presente invenção refere-se a compostos de fórmula (I) em que R1a, R1b, R2a, R2b, Z, R3 a R5, A, p, U, V, W, L e E têm os significados fornecidos nas reivindicações e especificações, seu uso como inibidores de proteínas mutantes da família Ras, composições farmacêuticas e preparações contendo tais compostos e seu uso como medicamentos/usos médicos, especialmente como agentes para tratamento e/ou prevenção de doenças oncológicas.
BR112022023462A 2020-06-02 2021-06-01 2-amino-3-ciano tiofenos anulados e derivados para o tratamento de câncer BR112022023462A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063033505P 2020-06-02 2020-06-02
EP20212067 2020-12-05
PCT/EP2021/064612 WO2021245051A1 (en) 2020-06-02 2021-06-01 Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer

Publications (1)

Publication Number Publication Date
BR112022023462A2 true BR112022023462A2 (pt) 2022-12-20

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BR112022023462A BR112022023462A2 (pt) 2020-06-02 2021-06-01 2-amino-3-ciano tiofenos anulados e derivados para o tratamento de câncer

Country Status (18)

Country Link
US (2) US11945812B2 (pt)
EP (2) EP4157837A1 (pt)
JP (2) JP2023528623A (pt)
KR (1) KR20230019462A (pt)
CN (2) CN116034106A (pt)
AU (1) AU2021285032A1 (pt)
BR (1) BR112022023462A2 (pt)
CA (1) CA3183656A1 (pt)
CL (1) CL2022003289A1 (pt)
CO (1) CO2022017049A2 (pt)
CR (1) CR20220614A (pt)
DO (1) DOP2022000266A (pt)
EC (1) ECSP22089077A (pt)
IL (1) IL298633A (pt)
MX (1) MX2022015260A (pt)
PE (1) PE20240493A1 (pt)
TW (1) TW202210474A (pt)
WO (2) WO2021245051A1 (pt)

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CN116234806A (zh) 2023-06-06
IL298633A (en) 2023-01-01
DOP2022000266A (es) 2023-01-15
JP2023528623A (ja) 2023-07-05
CR20220614A (es) 2023-05-08
MX2022015260A (es) 2023-01-11
KR20230019462A (ko) 2023-02-08
WO2021245051A1 (en) 2021-12-09
US11945812B2 (en) 2024-04-02
TW202210474A (zh) 2022-03-16
PE20240493A1 (es) 2024-03-15
US20210380574A1 (en) 2021-12-09
CL2022003289A1 (es) 2023-04-14
CO2022017049A2 (es) 2023-02-06
EP4157837A1 (en) 2023-04-05
ECSP22089077A (es) 2022-12-30
JP2023527891A (ja) 2023-06-30
CN116034106A (zh) 2023-04-28
AU2021285032A1 (en) 2022-12-08
CA3183656A1 (en) 2021-12-09
EP4157836A1 (en) 2023-04-05
WO2021245055A1 (en) 2021-12-09
US20230212164A1 (en) 2023-07-06

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