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AR105459A1 - Derivados de pirrolo[2,1-f][1,2,4]triazina útiles para tratar trastornos relacionados con kit y pdfgr - Google Patents

Derivados de pirrolo[2,1-f][1,2,4]triazina útiles para tratar trastornos relacionados con kit y pdfgr

Info

Publication number
AR105459A1
AR105459A1 ARP160102250A ARP160102250A AR105459A1 AR 105459 A1 AR105459 A1 AR 105459A1 AR P160102250 A ARP160102250 A AR P160102250A AR P160102250 A ARP160102250 A AR P160102250A AR 105459 A1 AR105459 A1 AR 105459A1
Authority
AR
Argentina
Prior art keywords
monocyclic
cycloalkyl
alkyl
bicyclic
heterocyclyl
Prior art date
Application number
ARP160102250A
Other languages
English (en)
Inventor
Zhang Yulian
J Wilson Kevin
L Hodous Brian
Original Assignee
Blueprint Medicines Corp
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 Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of AR105459A1 publication Critical patent/AR105459A1/es

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Classifications

    • 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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Child & Adolescent Psychology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

En la presente se describen compuestos y composiciones útiles para tratar trastornos relacionados con KIT y PDGFR. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de este, donde: W se selecciona de hidrógeno y un compuesto de fórmula (2), donde el Anillo A se selecciona de arilo monocíclico o bicíclico, heteroarilo, cicloalquilo y heterociclilo monocíclico o bicíclico; Z se selecciona de alquilo C₁₋₆, cicloalquilo, arilo monocíclico o bicíclico, aralquilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, y heterociclilalquilo monocíclico o bicíclico; donde cada alquilo C₁₋₆, cicloalquilo, arilo monocíclico o bicíclico, aralquilo monocíclico o bicíclico, heteroarilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, heterociclilalquilo monocíclico o bicíclico se sustituye independientemente con 0 - 5 apariciones de RC; L se selecciona de -N(R¹)-C(O)-, -N(R¹)C(O)N(R¹)-, -N(R¹)C(O)N(R¹)-(alquileno C₁₋₆)-, N(R¹)-(alquileno C₁₋₆)-, -N(R¹)-C(O)-(alquileno C₁₋₆)-, -N(R¹)-S(O)₂, y -N(R¹)-S(O)₂-(alquileno C₁₋₆)-; donde cada alquileno está sustituido independientemente con 0 - 5 apariciones de R²; cada RA se selecciona independientemente de alquilo C₁₋₆, alcoxi C₁₋₆, halo, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, heteroalquilo C₁₋₆, -N(R¹)(R¹), ciano y -OR¹; cada RB se selecciona independientemente de hidrógeno, alquilo C₁₋₆, cicloalquilo C₁₋₆, hidroxilo, halo, alcoxi C₁₋₆, haloalquilo C₁₋₆, -N(R¹)(R¹) y ciano; cada RC se selecciona independientemente de alquilo C₁₋₆, alquinilo C₁₋₆, halo, heteroalquilo C₁₋₆, haloalquilo C₁₋₆, haloalcoxi C₁₋₆, hidroxialquilo C₁₋₆, cicloalquilo, arilo monocíclico o bicíclico, ariloxi monocíclico o bicíclico, aralquilo monocíclico o bicíclico, heterociclilo monocíclico o bicíclico, heterociclilalquilo monocíclico o bicíclico, nitro, ciano, -C(O)R¹, -OC(O)R¹, -C(O)OR¹, -SR¹, -S(O)₂R¹, -S(O)₂-N(R¹)(R¹), -(alquileno C₁₋₆)-S(O)₂-N(R¹)(R¹), -N(R¹)(R¹), -C(O)-N(R¹)(R¹), -N(R¹)(R¹)-C(O)R¹, -(alquileno C₁₋₆)-N(R¹)-C(O)R¹, -NR¹S(O)₂R¹, -P(O)(R¹)(R¹) y -OR¹; donde cada heteroalquilo, haloalquilo, haloalcoxi, alquilo, alquinilo, cicloalquilo, arilo, ariloxi, aralquilo, heterociclilo, heterociclilalquilo se sustituye independientemente con 0 - 5 apariciones de Rᵃ; o 2 RC junto con el o los átomos de carbono a los que están unidos forman un anillo cicloalquilo o heterociclilo sustituido con 0 - 5 apariciones de Rᵃ; cada RD se selecciona independientemente de halo, alquilo C₁₋₆, cicloalquilo C₁₋₆, hidroxilo, halo, alcoxi C₁₋₆, haloalquilo C₁₋₆, -N(R²)(R²) y ciano; cada R¹ se selecciona independientemente de hidrógeno, hidroxilo, halo, tiol, alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, tioalquilo C₁₋₆, -NRR, cicloalquilo, cicloalquilalquilo, heterociclilo y heterociclilalquilo, donde cada uno de alquilo C₁₋₆, cicloalquilo y heterociclilo se sustituye independientemente con 0 - 5 apariciones de Rᵇ; o 2 R¹ junto con el o los átomos a los que están unidos forman un anillo cicloalquilo o heterociclilo; cada R² se selecciona independientemente de hidroxilo, alquilo C₁₋₆, alcoxilo C₁₋₆, -NRR; o 2 R² junto con el o los átomos a los que están unidos forman un anillo cicloalquilo o heterociclilo; cada Rᵃ y Rᵇ se selecciona independientemente de hidrógeno, halo, ciano, hidroxilo, alcoxilo C₁₋₆, -C(O)R, C(O)OR, alquilo C₁₋₆, haloalquilo C₁₋₆, heteroalquilo C₁₋₆, hidroxialquilo C₁₋₆, -NRR y cicloalquilo, donde cicloalquilo se sustituye con 0 - 5 apariciones de R; cada R se selecciona independientemente de hidrógeno, alquilo C₁₋₆, alcoxilo C₁₋₆, heteroalquilo C₁₋₆, halo, hidroxilo, haloalquilo C₁₋₆, hidroxialquilo C₁₋₆, cicloalquilo y ciano; o 2 R junto con el o los átomos a los que están unidos forman un anillo cicloalquilo o heterociclilo; cada R es hidrógeno, alquilo C₁₋₆, -C(O)-alquilo C₁₋₆, -C(O)-NRR o -C(S)-NRR; y cada q y r es independientemente 0, 1, 2, 3 ó 4.
ARP160102250A 2015-07-24 2016-07-22 Derivados de pirrolo[2,1-f][1,2,4]triazina útiles para tratar trastornos relacionados con kit y pdfgr AR105459A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562196445P 2015-07-24 2015-07-24

Publications (1)

Publication Number Publication Date
AR105459A1 true AR105459A1 (es) 2017-10-04

Family

ID=56555836

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Country Status (17)

Country Link
US (2) US10000496B2 (es)
EP (1) EP3325481B1 (es)
JP (1) JP2018521076A (es)
KR (1) KR20180048635A (es)
CN (1) CN108026102A (es)
AR (1) AR105459A1 (es)
AU (1) AU2016297754A1 (es)
BR (1) BR112018001190A2 (es)
CA (1) CA2994819A1 (es)
HK (1) HK1255103A1 (es)
IL (1) IL256978A (es)
MX (1) MX2018001032A (es)
PH (1) PH12018500177A1 (es)
RU (1) RU2018106483A (es)
TW (1) TW201704237A (es)
WO (1) WO2017019442A1 (es)
ZA (1) ZA201801019B (es)

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SG11201602937UA (en) 2013-10-17 2016-05-30 Blueprint Medicines Corp Compositions useful for treating disorders related to kit
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
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US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
AU2016297754A1 (en) 2015-07-24 2018-02-15 Blueprint Medicines Corporation Compounds useful for treating disorders related to KIT and PDGFR
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
RS65069B1 (sr) 2015-11-02 2024-02-29 Blueprint Medicines Corp Inhibitori ret-a
TWI733713B (zh) 2015-11-19 2021-07-21 美商纜圖藥品公司 用於治療神經促進性酪氨酸受體激酶相關之異常的化合物與組成物
US10183928B2 (en) 2016-03-17 2019-01-22 Blueprint Medicines Corporation Inhibitors of RET
SG11201808907PA (en) 2016-04-15 2018-11-29 Blueprint Medicines Corp Inhibitors of activin receptor-like kinase

Also Published As

Publication number Publication date
ZA201801019B (en) 2019-04-24
BR112018001190A2 (pt) 2018-09-11
WO2017019442A1 (en) 2017-02-02
CN108026102A (zh) 2018-05-11
IL256978A (en) 2018-03-29
HK1255103A1 (zh) 2019-08-02
US20170022206A1 (en) 2017-01-26
JP2018521076A (ja) 2018-08-02
PH12018500177A1 (en) 2018-07-30
AU2016297754A1 (en) 2018-02-15
EP3325481B1 (en) 2019-06-12
KR20180048635A (ko) 2018-05-10
TW201704237A (zh) 2017-02-01
EP3325481A1 (en) 2018-05-30
US10000496B2 (en) 2018-06-19
US20190119280A1 (en) 2019-04-25
MX2018001032A (es) 2018-11-09
RU2018106483A (ru) 2019-08-26
CA2994819A1 (en) 2017-02-02

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