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MX2016006119A - Derivados de 1-(5-terc-butil-2-aril-pirazol-3-il)-3-[2-fluoro-4-[( 3-oxo-4h-pirido[2,3 b]piracin-8-il)oxi]fenil]urea como inhibidores de raf para el tratamiento del cancer. - Google Patents

Derivados de 1-(5-terc-butil-2-aril-pirazol-3-il)-3-[2-fluoro-4-[( 3-oxo-4h-pirido[2,3 b]piracin-8-il)oxi]fenil]urea como inhibidores de raf para el tratamiento del cancer.

Info

Publication number
MX2016006119A
MX2016006119A MX2016006119A MX2016006119A MX2016006119A MX 2016006119 A MX2016006119 A MX 2016006119A MX 2016006119 A MX2016006119 A MX 2016006119A MX 2016006119 A MX2016006119 A MX 2016006119A MX 2016006119 A MX2016006119 A MX 2016006119A
Authority
MX
Mexico
Prior art keywords
disorders
braf
craf
compounds
inhibition
Prior art date
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MX2016006119A
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English (en)
Other versions
MX372942B (es
Inventor
Joy Springer Caroline
Marais Richard
Girotti Romina
Niculescu-Duvaz Dan
Niculescu-Duvaz Ion
Zambon Alfonso
Original Assignee
Cancer Res Tech Ltd
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Application filed by Cancer Res Tech Ltd filed Critical Cancer Res Tech Ltd
Publication of MX2016006119A publication Critical patent/MX2016006119A/es
Publication of MX372942B publication Critical patent/MX372942B/es

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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
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  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Immunology (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención trata generalmente del campo de los compuestos terapéuticos. Más específicamente, la presente invención trata de ciertos compuestos de 1-(5-terc-butil-2-aril-pi razol-3-il)-3-[2-fluoro-4-[(3-oxo-4H-pirido[2,3-b]piracin-8-il)ox i]fenil]urea (denominados en la presente "compuestos de TBAP") que, entre otras cosas, inhiben RAF (p. ej., BRAF, CRAF, etc.). La presente invención también trata de composiciones farmacéuticas que comprenden tales compuestos y del uso de tales compuestos y composiciones, tanto in vitro como in vivo, para inhibir RAF (p. ej., BRAF, CRAF, etc.); y para tratar trastornos incluyendo: trastornos proliferativos; cáncer (incluyendo, p. ej., melanoma maligno, carcinoma colorrectal, adenocarcinoma pancreático); inflamación; trastornos inmunológicos; infecciones virales; trastornos fibróticos; trastornos asociados con una forma mutada de RAF (p. ej., BRAF, CRAF, etc.); trastornos mejorados por la inhibición de RAF (p. ej., BRAF, CRAF, etc.); trastornos mejorados por la inhibición de BRAF mutante; trastornos mejorados por la inhibición de BRAF y CRAF; trastornos asociados con mutaciones en RAS y/o la activación de la ruta de MAPK; trastornos mejorados por la inhibición de SRC, p38, FGFRA, VEGFR-2 (KDR), y/o LCK; etc.
MX2016006119A 2013-11-25 2014-11-25 Derivados de 1-(5-terc-butil-2-aril-pirazol-3-il)-3-[2-fluoro-4-[(3-oxo-4h-pirido[2,3 b]piracin-8-il)oxi]fenil]urea como inhibidores de raf para el tratamiento del cancer. MX372942B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1320729.5A GB201320729D0 (en) 2013-11-25 2013-11-25 Therapeutic compounds and their use
PCT/GB2014/053490 WO2015075483A1 (en) 2013-11-25 2014-11-25 1 -(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4h-pyrido[2, 3-b]pyrazin-8-yl)oxy]phenyl]urea derivatives as raf inhibitors for the treatment of cancer

Publications (2)

Publication Number Publication Date
MX2016006119A true MX2016006119A (es) 2016-12-14
MX372942B MX372942B (es) 2020-04-03

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US (2) US9725447B2 (es)
EP (1) EP3074396B1 (es)
JP (1) JP6389529B2 (es)
KR (1) KR102327096B1 (es)
CN (1) CN105793260B (es)
AU (1) AU2014351571B2 (es)
BR (1) BR112016011078B1 (es)
CA (1) CA2928009C (es)
DK (1) DK3074396T3 (es)
EA (1) EA034216B1 (es)
ES (1) ES2740325T3 (es)
GB (1) GB201320729D0 (es)
HU (1) HUE045596T2 (es)
IL (1) IL245062B (es)
MX (1) MX372942B (es)
PL (1) PL3074396T3 (es)
PT (1) PT3074396T (es)
SA (1) SA516371189B1 (es)
WO (1) WO2015075483A1 (es)

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CA2928009A1 (en) 2015-05-28
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WO2015075483A1 (en) 2015-05-28
CA2928009C (en) 2022-08-30
IL245062B (en) 2019-09-26
DK3074396T3 (da) 2019-07-29
AU2014351571A1 (en) 2016-05-19
SA516371189B1 (ar) 2018-06-30
US9725447B2 (en) 2017-08-08
PL3074396T3 (pl) 2019-11-29
EP3074396B1 (en) 2019-05-01
CN105793260B (zh) 2018-04-10
PT3074396T (pt) 2019-08-06
BR112016011078A8 (pt) 2020-04-22
KR20160079792A (ko) 2016-07-06
BR112016011078B1 (pt) 2022-12-06
GB201320729D0 (en) 2014-01-08
HUE045596T2 (hu) 2020-01-28
EA201690531A1 (ru) 2016-08-31
MX372942B (es) 2020-04-03
US10167282B2 (en) 2019-01-01
EP3074396A1 (en) 2016-10-05
KR102327096B1 (ko) 2021-11-16
ES2740325T3 (es) 2020-02-05
CN105793260A (zh) 2016-07-20
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IL245062A0 (en) 2016-06-30
US20160355510A1 (en) 2016-12-08

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