AR092253A1 - Inhibidores de serina/treonina cinasa - Google Patents

Inhibidores de serina/treonina cinasa

Info

Publication number
AR092253A1
AR092253A1 ARP130103040A ARP130103040A AR092253A1 AR 092253 A1 AR092253 A1 AR 092253A1 AR P130103040 A ARP130103040 A AR P130103040A AR P130103040 A ARP130103040 A AR P130103040A AR 092253 A1 AR092253 A1 AR 092253A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
group
groups
Prior art date
Application number
ARP130103040A
Other languages
English (en)
Inventor
J Mohr Peter
Robarge Kirk
Schwarz Jacob
Zhou Aihe
Kintz Sam
F Blake James
Gazzard Lewis
Chen Huifen
Joseph Chicarelli Mark
Gaudino John
Original Assignee
Array Biopharma Inc
Genentech Inc
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 Array Biopharma Inc, Genentech Inc filed Critical Array Biopharma Inc
Publication of AR092253A1 publication Critical patent/AR092253A1/es

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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

Landscapes

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

Abstract

Se describen composiciones y métodos para tratar trastornos hiperproliferativos. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1) donde: X es CH o N; Z es (i) NH(CH₂)ₙCHR¹Ar donde n es 0 ó 1, o (ii) 1-alquil-4-aril-pirrolidin-3-ilamina o 4-aril-pirrolidin-3-ilamina donde alquilo es alquilo C₁₋₃ opcionalmente sustituido con un anillo fenilo y arilo es fenilo opcionalmente sustituido; R¹ es (a) hidrógeno, (b) alquilo C₁₋₆ opcionalmente sustituido con uno o más grupos hidroxilo o alcoxi C₁₋₆, (c) alquenilo C₁₋₆ opcionalmente sustituido con uno o más grupos hidroxilo o alcoxi C₁₋₆, (d) alquinilo C₁₋₆ con uno o más grupos hidroxilo o alcoxi C₁₋₆, (e) cicloalquilo C₃₋₆ opcionalmente sustituido con uno o más grupos que se seleccionan del grupo que consiste en hidroxilo, alcoxi C₁₋₆, alquilo C₁₋₆ y halógeno; (f) un heterociclo de 4 a 6 miembros con uno o dos heteroátomos que se seleccionan de N u O, donde el heterociclo está opcionalmente sustituido con uno o más grupos que se seleccionan del grupo que consiste en hidroxilo, alcoxi C₁₋₆, alquilo C₁₋₆ y halógeno, o (g) un heteroarilo de 5 a 6 miembros con uno o dos heteroátomos que se seleccionan de N u O, donde el heteroarilo está opcionalmente sustituido con uno o más grupos que se seleccionan del grupo que consiste en hidroxilo, alcoxi C₁₋₆, alquilo C₁₋₆ y halógeno; Ar es fenilo, piridinilo o indolilo opcionalmente sustituido con 1 a 3 grupos seleccionados independientemente de (a) alquilo C₁₋₆, (b) haloalquilo C₁₋₆, (c) alcoxi C₁₋₆, (d) cicloalquilo C₃₋₆, (e) halógeno, (f) haloalcoxi C₁₋₆, (g) alquiltio C₁₋₆, (f) ciano, (g) bencilo, (h) fenoxi donde dicho bencilo y fenoxi están opcionalmente sustituidos con halógeno, alquilo C₁₋₆ o alcoxi C₁₋₆, (i) 4-metilpiperazin-1-ilo, o (j) heteroarilo que se selecciona del grupo que consiste en piridinilo, pirazinilo, piridazinilo, pirimidinilo y pirazolilo donde dicho heteroarilo está opcionalmente sustituido con uno o más alquilo C₁₋₁₀; R² se selecciona del grupo que consiste en (a) alquilo C₁₋₁₀, (b) hidroxialquilo C₁₋₁₀ (c) haloalquilo C₁₋₆, (d) heterociclilo donde dicho heterociclo se selecciona del grupo que consiste en tetrahidropiranilo, tetrahidrofuranilo, oxetanilo, 2-oxa-biciclo[2.2.1]heptan-5-ilo, piperidinilo y pirrolidinilo y donde dicho heterociclilo está opcionalmente sustituido con 1 a 3 grupos que se seleccionan independientemente del grupo que consiste en alquilo C₁₋₆, haloalquilo C₁₋₆, aciloxi C₁₋₄-alquilo C₁₋₂, halógeno, hidroxilo, fenilo, hidroxialquilo C₁₋₃ u oxo, (e) heteroarilo donde dicho heteroarilo se selecciona del grupo que consiste en pirazolilo y piridinilo y donde dicho heteroarilo está opcionalmente sustituido con 1 a 3 grupos alquilo C₁₋₃, (f) cicloalquilo C₃₋₇ o cicloalquilo C₃₋₇-alquilo C₁₋₆ donde dicho cicloalquilo o cicloalquilo C₃₋₇-alquilo C₁₋₆ están opcionalmente sustituidos con hidroxilo o halo; o, un estereoisómero, tautómero o sal farmacéuticamente aceptable de estos.
ARP130103040A 2012-08-27 2013-08-27 Inhibidores de serina/treonina cinasa AR092253A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261693671P 2012-08-27 2012-08-27

Publications (1)

Publication Number Publication Date
AR092253A1 true AR092253A1 (es) 2015-04-08

Family

ID=49118823

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130103040A AR092253A1 (es) 2012-08-27 2013-08-27 Inhibidores de serina/treonina cinasa

Country Status (13)

Country Link
US (1) US9388171B2 (es)
EP (1) EP2888247B1 (es)
JP (1) JP6378182B2 (es)
KR (1) KR20150047597A (es)
CN (1) CN105143200B (es)
AR (1) AR092253A1 (es)
BR (1) BR112015004548A2 (es)
CA (1) CA2882750A1 (es)
HK (1) HK1210174A1 (es)
MX (1) MX369989B (es)
RU (1) RU2644947C2 (es)
TW (1) TW201408658A (es)
WO (1) WO2014036015A1 (es)

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Also Published As

Publication number Publication date
RU2644947C2 (ru) 2018-02-15
CN105143200B (zh) 2018-10-16
CA2882750A1 (en) 2014-03-06
US20140066453A1 (en) 2014-03-06
WO2014036015A1 (en) 2014-03-06
CN105143200A (zh) 2015-12-09
JP2015526519A (ja) 2015-09-10
HK1210174A1 (en) 2016-04-15
TW201408658A (zh) 2014-03-01
JP6378182B2 (ja) 2018-08-22
EP2888247B1 (en) 2020-03-25
RU2015110985A (ru) 2016-10-20
US9388171B2 (en) 2016-07-12
KR20150047597A (ko) 2015-05-04
EP2888247A1 (en) 2015-07-01
BR112015004548A2 (pt) 2017-08-08
MX2015002508A (es) 2015-10-12
MX369989B (es) 2019-11-27

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