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AR080757A1 - Morfolinilquinazolinas, procesos de obtencion, intermediarios, usos y composiciones farmaceuticas. - Google Patents

Morfolinilquinazolinas, procesos de obtencion, intermediarios, usos y composiciones farmaceuticas.

Info

Publication number
AR080757A1
AR080757A1 ARP110100836A AR080757A1 AR 080757 A1 AR080757 A1 AR 080757A1 AR P110100836 A ARP110100836 A AR P110100836A AR 080757 A1 AR080757 A1 AR 080757A1
Authority
AR
Argentina
Prior art keywords
alk
nyy
het2
hal
compounds
Prior art date
Application number
Other languages
English (en)
Inventor
Werner Mederski
Thomas Fuchss
Frank Zenke
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR080757A1 publication Critical patent/AR080757A1/es

Links

Classifications

    • 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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/06—Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Landscapes

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

Abstract

Se refiere a compuestos de las formulas (1), (2) y (3). Los compuestos de la formula (1) se pueden usar para la inhibicion de las serina-treonina-proteína quinasas, así como para la sensibilizacion de células cancerosas a los agentes anticáncer y/o radiacion ionizante. También es objeto de la solicitud el uso de los compuestos de la formula (1) en la prevencion, la terapia o el control del curso de cáncer, tumores, metástasis o trastornos de la angiogénesis, en combinacion con radioterapia y/o un agente anticáncer. La solicitud también se refiere a un procedimiento para la preparacion de los compuestos de la formula (1) por reaccion de los compuestos de las formulas (2) y (3) y eventualmente conversion de una base o un ácido de los compuestos de la formula (1) en una de sus sales. Reivindicacion 1: Compuestos de la formula (1) en donde R1 es H, Hal, CN, A, OY, NYY o -NH-C(NYY)=NY, R2 es H, Cyc, Ar, Het1 o Het2, R3 es Y, OH u OA, R4 es H o Hal, Y es H, A o Alk-OA, W1, W2 es, de modo independiente entre sí, CHR3 o NH, W1-W2 también son juntos CH=CH, L es enlace simple, -CYR3-, -CO-, -CO-NY-, -NY-CO-, -NY-CO-NY-, -NY-SO2-, -C(=NR3)-, -C(=N-CN)-, -Alk-, -Alk-NY-, -Alk-CO-, -Alk-CO-NY-, -AIkO-, -Alk-OAIk-, -Alk-C(Y)(OY)-, -C(Y)(CN)-, -C(Y)(Het1)-, -C(R3)(Het1)-, -C(Y)(Het1)-NY-, -C(Y)(Het2)-, -C(Y)(OY)-, -C(Y)(OCOOY)-, -C(Y)(NYY)-, -C(Y)(NY-COY)-, -C(Y)(NY-CO-NYY)-, -C(Y)(Oalk-CN)-, -C(Y) (Oalk-Het2)-, -C(Y)(Oalk-NYY)-, -C(Y)(OAlk-CO-NYY)-, -C(Y)(OY)-Alk-, -C(Y)(OCO-NYY)-, -C(Y)(OCO-NY-Alk-COOY)- o -C(Y)(OY)-Het1-Alk-OCO-NY-, A es alquilo no ramificado o ramificado C1-10, en donde, de modo independiente entre sí, 1-7 átomos de H pueden estar reemplazados por Hal, Alk es alquileno C1-6, en donde, de modo independiente entre si, 1-4 átomos de H pueden estar reemplazados por Hal y/o CN, Cyc es alquilo cíclico C3-7, en donde, de modo independiente entre sí, 1-4 átomos de H pueden estar reemplazados por A, Hal y/u OY, Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Y, OY, Hal, CN, COOY, -Alk-OY, NYY, -NY-COY, SiY3, Cyc y/o fenilo, Het1 es heteroarilo mono- o bicíclico C2-9 y 1-4 átomos de N, O y/o S, que no está sustituido o que puede estar mono-, di- o trisustituido con Y, OY, Hal, CN, COOY, -Alk-OY, NYY, -NY-COY, -Alk-Het2, -Alk-OCO-Het 2, -Alk-OCO-NY-Het2, -NY-CO-Het2, -NY-CO-Alk-Het2, S1Y3, Cyc y/o fenilo, en donde queda excluido el piridilmetoxi cuando R1 es NYY, Het2 es un heterociclo saturado monocíclico C2-7 y 1-4 átomos de N, O y/o S, que puede no estar sustituido o que puede estar monosustituido con R3 y/o COY, Hal es F, CI, Br o I, y n es 1, 2, 3 o 4, y/o sus sales, tautomeros y/o estereoisomeros fisiologicamente inocuos, incluyendo sus mezclas en todas las proporciones.
ARP110100836 2010-03-16 2011-03-16 Morfolinilquinazolinas, procesos de obtencion, intermediarios, usos y composiciones farmaceuticas. AR080757A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102010011493 2010-03-16

Publications (1)

Publication Number Publication Date
AR080757A1 true AR080757A1 (es) 2012-05-09

Family

ID=43828057

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100836 AR080757A1 (es) 2010-03-16 2011-03-16 Morfolinilquinazolinas, procesos de obtencion, intermediarios, usos y composiciones farmaceuticas.

Country Status (16)

Country Link
US (1) US9126952B2 (es)
EP (1) EP2547664B1 (es)
JP (1) JP2013522249A (es)
KR (1) KR20130017086A (es)
CN (1) CN102803227B (es)
AR (1) AR080757A1 (es)
AU (1) AU2011229542A1 (es)
BR (1) BR112012022868A2 (es)
CA (1) CA2793299A1 (es)
EA (1) EA201201289A1 (es)
ES (1) ES2586227T3 (es)
IL (1) IL221901A (es)
MX (1) MX2012010557A (es)
SG (1) SG183855A1 (es)
WO (1) WO2011113512A1 (es)
ZA (1) ZA201207727B (es)

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RU2636589C2 (ru) * 2009-12-23 2017-11-24 ДЖАСКО ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Аминопиримидиновые ингибиторы киназ

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AU2011229542A1 (en) 2012-11-08
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EP2547664B1 (de) 2016-05-04
KR20130017086A (ko) 2013-02-19
CA2793299A1 (en) 2011-09-22
US9126952B2 (en) 2015-09-08
EA201201289A1 (ru) 2013-08-30
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IL221901A0 (en) 2012-12-02
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