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AR095464A1 - Compuestos de heteroarilo y usos de los mismos - Google Patents

Compuestos de heteroarilo y usos de los mismos

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Publication number
AR095464A1
AR095464A1 ARP140101067A ARP140101067A AR095464A1 AR 095464 A1 AR095464 A1 AR 095464A1 AR P140101067 A ARP140101067 A AR P140101067A AR P140101067 A ARP140101067 A AR P140101067A AR 095464 A1 AR095464 A1 AR 095464A1
Authority
AR
Argentina
Prior art keywords
ring
nitrogen
alkyl
independently selected
sulfur
Prior art date
Application number
ARP140101067A
Other languages
English (en)
Original Assignee
Celgene Avilomics Res Inc
Sanofi Sa
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
Application filed by Celgene Avilomics Res Inc, Sanofi Sa filed Critical Celgene Avilomics Res Inc
Publication of AR095464A1 publication Critical patent/AR095464A1/es

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    • 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
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
    • A61K49/0052—Small organic molecules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • 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
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/10—Protein-tyrosine kinases (2.7.10)
    • C12Y207/10001—Receptor protein-tyrosine kinase (2.7.10.1)

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente proporciona compuestos útiles como inhibidores de proteínas quinasas, composiciones farmacéuticamente aceptables de dichos compuestos y métodos de uso de dichos compuestos. Compuestos útiles para tratar diversas afecciones. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de dicho compuesto, en donde: X¹ es -NR⁴, N, -CR⁴R⁴ o -CR⁴; X² es -NR⁵, N, -CR⁵R⁵ o -CR⁵; X³ es N o CR⁶; X⁴ es N o CR⁷; X⁵ es N, C o CH; en donde al menos uno de X¹, X², X³, X⁴ o X⁵ es N; G es H, O, OR ó N(R)(R); el Anillo A es un grupo opcionalmente sustituido seleccionado de fenilo, un anillo carbocíclico de 3 - 8 miembros saturado o parcialmente insaturado, un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre, un anillo heterocíclico de 4 - 7 miembros saturado o parcialmente insaturado que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre, o un anillo de 7-10 miembros bicíclico saturado, parcialmente insaturado o anillo arilo; cada R es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, fenilo, un anillo carbocíclico de 3 - 8 miembros saturado o parcialmente insaturado, un anillo heterocíclico de 4 - 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre, o un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre; o dos grupos R en el mismo nitrógeno se toman junto con el átomo de nitrógeno al cual están unidos para formar un anillo heterocíclico de 4 - 7 miembros que tiene 0 - 2 heteroátomos adicionales independientemente seleccionados de nitrógeno, oxígeno o azufre, o un anillo heteroarilo de 4 - 7 miembros que tiene 0 - 4 heteroátomos adicionales independientemente seleccionados de nitrógeno, oxígeno o azufre; R¹ es un grupo ojiva; en donde R¹ está unido a un átomo adyacente al átomo donde está unido T; cada R² es independientemente -R, halógeno, -haloalquilo, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, - NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; R³ es hidrógeno, alquenilo C₂₋₆, -W-Cy o alquilo C₁₋₆, en donde el alquilo C₁₋₆ está opcionalmente sustituido con 1 - 3 grupos independientemente seleccionados de halógeno, -CN, oxo, -OR o -C(O)O(alquilo C₁₋₆); W está ausente o es una cadena alquileno C₁₋₃ bivalente opcionalmente sustituida con uno o varios R y en donde una unidad de metileno de W está opcionalmente reemplazada con -O-, -S- o -NR-; cada R es independientemente hidrógeno o alquilo C₁₋₆; cada R es independientemente halógeno o alquilo C₁₋₆, en donde el alquilo C₁₋₆ está opcionalmente sustituido con 1 - 3 grupos independientemente seleccionados de halógeno, -CN, oxo o -OR; Cy es fenilo, cicloalquilo C₃₋₇, o un anillo de 3 - 7 miembros monocíclico o de 5 - 10 miembros bicíclico saturado, parcialmente insaturado, o heteroarilo, que tiene 1 - 3 heteroátomos independientemente seleccionados de nitrógeno, oxígeno o azufre, en donde Cy está opcionalmente sustituido con 1 - 3 Rˣ; cada Rˣ es independientemente H, -CN, oxo, -NH₂, alquilo C₁₋₆, halógeno, -OR, -N(R)₂, -NHC(O)(alquilo C₁₋₆), -C(O)N(R)₂, -C(O)O(alquilo C₁₋₆)-, -NHSO₂(alquilo C₁₋₆) o -SO₂N(R)₂; o R³ está ausente si no lo permite la valencia; cada uno de R⁴ y R⁴ es independientemente hidrógeno o un grupo opcionalmente sustituido seleccionado de alifático C₁₋₆, fenilo, un anillo carbocíclico de 3 - 8 miembros saturado o parcialmente insaturado que opcionalmente tiene puente, un anillo heterocíclico de 4 - 7 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxigeno o azufre, un anillo heteroarilo monocíclico de 5 - 6 miembros que tiene 1 - 4 heteroátomos independientemente seleccionados de nitrógeno, oxigeno o azufre, o un anillo de 7 - 10 miembros bicíclico saturado, parcialmente insaturado o anillo arilo, que opcionalmente tiene puente; cada uno de R⁵ y R⁵ es independientemente -R, halógeno, -O, -SR, -CN, - NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, -NRC(O)N(R)₂, -NRSO₂R o -N(R)₂; Y es O ó NRᵃ; Rᵃ es hidrógeno o un grupo alifático C₁₋₆ opcionalmente sustituido; T es un enlace covalente o una cadena de hidrocarburo C₁₋₆ bivalente recta o ramificada, saturada o insaturada, en donde una o varias unidades de metileno están opcionalmente reemplazadas con -O-, -S-, -N(R)-, -C(O)-, -OC(O)-, -C(O)O-, -C(O)N(R)-, -N(R)C(O)-, -N(R)C(O)N(R)-, -S(O)-, -SO₂-, -SO₂N(R)-, -N(R)SO₂- o -N(R)SO₂N(R)-; q es 0 - 6; y cada uno de R⁶ y R⁷ es independientemente -R, halógeno, -O, -SR, -CN, -NO₂, -SO₂R, -SOR, -C(O)R, -CO₂R, -C(O)N(R)₂, -NRC(O)R, - NRC(O)N(R)₂, -NRSO₂R o -N(R)₂.
ARP140101067A 2013-03-15 2014-03-14 Compuestos de heteroarilo y usos de los mismos AR095464A1 (es)

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US (5) US9321786B2 (es)
AR (1) AR095464A1 (es)
EC (1) ECSP15043696A (es)
TW (1) TWI647220B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
HUE055502T2 (hu) * 2012-07-11 2021-11-29 Blueprint Medicines Corp Fibroblaszt növekedési faktor receptor gátlók
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
KR102350704B1 (ko) 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
CN111793068A (zh) 2013-03-15 2020-10-20 西建卡尔有限责任公司 杂芳基化合物和其用途
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
CA2928042C (en) 2013-10-25 2022-05-10 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9828373B2 (en) 2014-07-26 2017-11-28 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido[2,3-D]pyrimidin-7(8H)-one derivatives as CDK inhibitors and uses thereof
EP3200786B1 (en) 2014-10-03 2019-08-28 Novartis AG Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016115412A1 (en) * 2015-01-18 2016-07-21 Newave Pharmaceutical Llc Dual-warhead covalent inhibitors of fgfr-4
WO2016128465A1 (en) 2015-02-11 2016-08-18 Basilea Pharmaceutica Ag Substituted mono- and polyazanaphthalene derivatives and their use
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MY198534A (en) 2016-08-15 2023-09-04 Pfizer Pyridopyrimdinone cdk2/4/6 inhibitors
US20190192522A1 (en) * 2016-09-08 2019-06-27 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor 4 in combination with cyclin-dependent kinase inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
KR102382613B1 (ko) * 2020-01-15 2022-04-06 한국과학기술연구원 단백질 키나아제 저해 활성을 갖는 7-아미노-3,4-디히드로피리미도피리미딘-2-온 유도체 및 이를 포함하는 치료용 약학 조성물
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3213379A1 (en) * 2021-03-26 2022-09-29 Weiqiang Zhan Bicyclic heterocyclic fgfr4 inhibitor, pharmaceutical composition and preparation, and a use thereof
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2024242495A1 (ko) * 2023-05-25 2024-11-28 주식회사 매직불릿테라퓨틱스 단백질 키나아제 억제용 신규 화합물 및 이를 포함하는 약학조성물

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK281724B6 (sk) 1994-11-14 2001-07-10 Warner-Lambert Company 6-arylpyrido[2,3-d]pyrimidíny, ich použitie a farmaceutické prostriedky na ich báze
GB9508535D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivative
KR20000070751A (ko) 1997-02-05 2000-11-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 피리도[2,3-ｄ]피리미딘 및 4-아미노피리미딘
DE19802377A1 (de) 1998-01-22 1999-08-19 Max Planck Gesellschaft Verwendung von Inhibitoren für die Behandlung von RTK-Überfunktions-bedingten Störungen, insbesondere von Krebs
KR20010043829A (ko) 1998-05-26 2001-05-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 비시클릭 피리미딘 및 비시클릭3,4-디히드로피리미딘
HRP20010274A2 (en) 1998-10-23 2002-06-30 Hoffmann La Roche Bicyclic nitrogen heterocycles
KR100537241B1 (ko) 1999-10-21 2005-12-19 에프. 호프만-라 로슈 아게 Ｐ38 단백질 키나제의 억제제로서의 알킬아미노 치환된이중고리 질소 헤테로고리 화합물
WO2001029042A1 (en) 1999-10-21 2001-04-26 F. Hoffmann-La Roche Ag Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
JP2004519422A (ja) 2000-08-04 2004-07-02 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー ２−（４−ピリジル）アミノ−６−ジアルコキシフェニルピリド〔２，３−ｄ〕ピリミジン−７−オン
AU2001293784B2 (en) 2000-08-31 2007-08-30 F. Hoffmann-La Roche Ag 7-OXO pyridopyrimidines as inhibitors of a cellular proliferation
ES2243568T3 (es) 2000-08-31 2005-12-01 F. Hoffmann-La Roche Ag 7-oxo-piridopirimidinas.
US6506749B2 (en) 2000-08-31 2003-01-14 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (I)
US6518276B2 (en) 2000-08-31 2003-02-11 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (II)
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
PA8577501A1 (es) 2002-07-25 2004-02-07 Warner Lambert Co Inhibidores de quinasas
WO2004014869A2 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 5,6-fused 3,4-dihydropyrimidine-2-one derivatives as matrix metalloproteinase inhibitors
US7084270B2 (en) 2002-08-14 2006-08-01 Hoffman-La Roche Inc. Pyrimido compounds having antiproliferative activity
US7129351B2 (en) 2002-11-04 2006-10-31 Hoffmann-La Roche Inc. Pyrimido compounds having antiproliferative activity
TW200413381A (en) 2002-11-04 2004-08-01 Hoffmann La Roche Novel amino-substituted dihydropyrimido [4,5-d]pyrimidinone derivatives, their manufacture and use as pharmaceutical agents
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
EP1572682A4 (en) 2002-12-20 2008-01-23 Pharmacia Corp ACYCLIC PYRAZOLE COMPOUNDS
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
KR20050111636A (ko) 2003-04-10 2005-11-25 에프. 호프만-라 로슈 아게 피리미도 화합물
EP1620408A2 (en) 2003-04-16 2006-02-01 F. Hoffmann-La Roche Ag Quinazoline compounds
MXPA06001098A (es) 2003-07-29 2006-04-24 Irm Llc Compuestos y composiciones utiles como inhibidores de proteina cinasa.
JP4758349B2 (ja) 2003-10-08 2011-08-24 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
WO2005066211A2 (en) * 2003-12-19 2005-07-21 Five Prime Therapeutics, Inc. Fibroblast growth factor receptors 1, 2, 3, and 4 as targets for therapeutic intervention
EP2260849A1 (en) 2004-01-21 2010-12-15 Emory University Compositions and methods of use for tyrosine kinase inhibitors to treat pathogenic infection
WO2005105097A2 (en) 2004-04-28 2005-11-10 Gpc Biotech Ag Pyridopyrimidines for treating inflammatory and other diseases
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
RU2007111757A (ru) 2004-08-31 2008-10-10 Ф.Хоффманн-Ля Рош Аг (Ch) Амидные производные 3-фенилдигидропиримидо [4,5-d] пиримидинонов, их получение и использованиев качестве фармацевтических агентов
MX2007002089A (es) 2004-08-31 2007-03-29 Hoffmann La Roche Derivados de amida de 7-amino-3-fenil-dihidropirimido[4,5-d]pirimidonas, su fabricacion y su uso como inhibidores de proteina cinasa.
US20090118261A1 (en) 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
WO2006038112A1 (en) 2004-10-01 2006-04-13 Warner-Lambert Company Llc Use of kinase inhibitors to promote neochondrogenesis
EP1828186A1 (en) 2004-12-13 2007-09-05 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
US7906522B2 (en) 2005-04-28 2011-03-15 Kyowa Hakko Kirin Co., Ltd 2-aminoquinazoline derivatives
MX2007015610A (es) 2005-06-10 2008-02-21 Irm Llc Compuestos que mantienen la fluripotencia de las celulas totipotentes embrionarias.
WO2006137421A1 (ja) 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
EP2083081A1 (en) * 2005-07-22 2009-07-29 Five Prime Therapeutics, Inc. Compositions and methods of treating disease with FGFR fusion proteins
WO2007014250A2 (en) 2005-07-26 2007-02-01 Vertex Pharmaceuticals Incorporated Abl kinase inhibition
KR100832594B1 (ko) 2005-11-08 2008-05-27 한미약품 주식회사 다중저해제로서의 퀴나졸린 유도체 및 이의 제조방법
US7618982B2 (en) 2005-12-19 2009-11-17 Nerviano Medical Sciences S.R.L. Heteroarylpyrrolopyridinones active as kinase inhibitors
BRPI0620408B8 (pt) 2005-12-21 2021-05-25 Novartis Ag derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica
WO2007134259A2 (en) 2006-05-11 2007-11-22 Irm Llc Compounds and compositions as protein kinase inhibitors
EP2018167A4 (en) 2006-05-15 2010-07-14 Irm Llc COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES
US8063225B2 (en) * 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
WO2008150260A1 (en) 2007-06-06 2008-12-11 Gpc Biotech, Inc. 8-oxy-2-aminopyrido (2, 3-d) pyrimidin-7-one derivatives as kinase inhibitors and anticancer agents
EP1914234A1 (en) 2006-10-16 2008-04-23 GPC Biotech Inc. Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors
AU2007311480A1 (en) 2006-10-16 2008-04-24 Forma Therapeutics, Inc. Pyrido [2, 3-d] pyrimidines and their use as kinase inhibitors
CA2668731A1 (en) 2006-11-09 2008-05-15 Tobias Gabriel Kinase inhibitors and methods for using the same
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
MX2009006706A (es) 2006-12-22 2009-07-02 Astex Therapeutics Ltd Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos.
RS51655B (sr) 2006-12-27 2011-10-31 Sanofi-Aventis Derivati izohinolina i izohinolinona supstituisani cikloalkilaminom
JP5313919B2 (ja) 2006-12-27 2013-10-09 サノフイ 新規な置換イソキノリン及びイソキノリノン誘導体
HRP20161536T1 (hr) 2007-06-15 2016-12-30 Msd K.K. Derivat bicikloanilina
GB0720038D0 (en) 2007-10-12 2007-11-21 Astex Therapeutics Ltd New compounds
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
US8216783B2 (en) * 2008-04-14 2012-07-10 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Over-expression and mutation of a tyrosine kinase receptor FGFR4 in tumors
EP2269993B1 (en) 2008-04-23 2013-02-27 Kyowa Hakko Kirin Co., Ltd. 2-aminoquinazoline derivative
AU2009248774B2 (en) 2008-05-23 2012-05-31 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
DK2361248T3 (en) 2008-06-27 2019-01-14 Celgene Car Llc Heteroberl compounds and uses thereof
MY156789A (en) 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
WO2010067888A1 (en) 2008-12-12 2010-06-17 Banyu Pharmaceutical Co.,Ltd. Dihydropyrimidopyrimidine derivatives
JP2012511502A (ja) 2008-12-12 2012-05-24 Ｍｓｄ株式会社 ジヒドロピリミドピリミジン誘導体
WO2010080712A2 (en) 2009-01-06 2010-07-15 Dana Farber Cancer Institute Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
RU2012114902A (ru) 2009-09-16 2013-10-27 Авила Терапьютикс, Инк. Конъюгаты и ингибиторы протеинкиназы
AR079257A1 (es) 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas
UA109888C2 (uk) * 2009-12-07 2015-10-26 ІЗОЛЬОВАНЕ АНТИТІЛО АБО ЙОГО ФРАГМЕНТ, ЩО ЗВ'ЯЗУЄТЬСЯ З β-КЛОТО, РЕЦЕПТОРАМИ FGF І ЇХНІМИ КОМПЛЕКСАМИ
WO2011075620A1 (en) 2009-12-18 2011-06-23 Novartis Ag Method for treating haematological cancers
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
US20120258967A1 (en) 2011-03-09 2012-10-11 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
MX342240B (es) 2011-04-07 2016-09-21 Genentech Inc Anticuerpos anti-fgfr4 y metodos de uso.
DK2710007T3 (da) 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
CN102887895B (zh) 2011-07-22 2016-08-24 山东轩竹医药科技有限公司 吡啶并嘧啶类mTOR抑制剂
BR112014010420A2 (pt) 2011-11-04 2017-04-25 Afraxis Holdings Inc inibidores de pak para o tratamento de distúrbios proliferativos celulares
MX372814B (es) 2012-06-07 2020-07-03 Deciphera Pharmaceuticals Llc Dihidronaftiridinas y compuestos relacionados útiles como inhibidores cinasas para el tratamiento de enfermedades proliferativas.
US8461179B1 (en) 2012-06-07 2013-06-11 Deciphera Pharmaceuticals, Llc Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
HUE055502T2 (hu) 2012-07-11 2021-11-29 Blueprint Medicines Corp Fibroblaszt növekedési faktor receptor gátlók
TWI629266B (zh) 2012-12-28 2018-07-11 藍印藥品公司 纖維母細胞生長因子受體之抑制劑
CN111793068A (zh) 2013-03-15 2020-10-20 西建卡尔有限责任公司 杂芳基化合物和其用途
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
KR102350704B1 (ko) 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
CA2917667A1 (en) 2013-07-09 2015-01-15 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
EP3027654B1 (en) 2013-07-30 2019-09-25 Blueprint Medicines Corporation Pik3c2g fusions
US10407509B2 (en) 2013-07-30 2019-09-10 Blueprint Medicines Corporation NTRK2 fusions
PL3057969T3 (pl) 2013-10-17 2018-11-30 Blueprint Medicines Corporation Kompozycje użyteczne do leczenia zaburzeń związanych z KIT
WO2015058129A1 (en) 2013-10-17 2015-04-23 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
KR101826015B1 (ko) 2013-10-18 2018-02-06 에자이 알앤드디 매니지먼트 가부시키가이샤 피리미딘 fgfr4 억제제
CA2928042C (en) 2013-10-25 2022-05-10 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor

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