AR053446A1 - Compuestos cis-2,4,5-triaril-imidazolinas y su uso como medicamento anti-cancer - Google Patents

Compuestos cis-2,4,5-triaril-imidazolinas y su uso como medicamento anti-cancer

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Publication number
AR053446A1
AR053446A1 ARP060100970A ARP060100970A AR053446A1 AR 053446 A1 AR053446 A1 AR 053446A1 AR P060100970 A ARP060100970 A AR P060100970A AR P060100970 A ARP060100970 A AR P060100970A AR 053446 A1 AR053446 A1 AR 053446A1
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AR
Argentina
Prior art keywords
chosen
group
lower alkyl
lower alkoxy
substituted
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ARP060100970A
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English (en)
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Hoffmann La Roche
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Publication of AR053446A1 publication Critical patent/AR053446A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/22Radicals substituted by oxygen atoms
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/24Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/20Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D233/26Radicals substituted by carbon atoms having three bonds to hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

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

Abstract

Estos compuestos inhiben la interaccion MDM2-p53 y que, como tales, los compuestos tendrán una actividad celular anti- hiperproliferativa. Composicion, uso y proceso. Reivindicacion 1: Un compuesto de formula (1), y las sales y ésteres farmacéuticamente aceptables del mismo; en la que X1 se elige entre el grupo formado por: alcoxi inferior; alcoxi inferior sustituido por trifluorometilo o fluor; X2 y X3 con independencia entre sí se eligen entre el grupo formado por: hidrogeno; halogeno; ciano; alquilo inferior; alcoxi inferior; piperidinilo; -NX4X5; -SO2NX4X5; -C(O) NX4X5; -C(O)X6; -SOX6, -SO2X6; -NC(O)-alcoxi inferior; -C:::C-X7; con la condicion de que X2 y X3 no sean ambos hidrogeno, alquilo inferior ni alcoxi inferior; con la condicion de que cuando X2 o X3 es hidrogeno, el otro no sea alquilo inferior, alcoxi inferior ni halogeno; X2 y X3 pueden tomarse juntos para formar un anillo elegido entre anillos insaturados de 5 a 7 eslabones, y anillos insaturados de 5 a 7 eslabones que contienen por lo menos un heteroátomo elegido entre S, N y O; X4 y X5 con independencia entre sí se eligen entre el grupo formado por: hidrogeno; alquilo inferior; cicloalquilo; alcoxi inferior; alquilo inferior sustituido por alcoxi inferior; -SO2-alquilo inferior; -C(O)-piperazinil-3-ona; X6 se elige entre el grupo formado por: alquilo inferior; morfolina; piperidina; pirrolidina; X7 se elige entre el grupo formado por: hidrogeno; alquilo inferior; trifluorometilo; Y1 e Y2 con independencia entre sí se eligen entre el grupo formado por: halogeno; acetileno; R se elige entre el grupo formado por: alcoxi inferior; piperidinilo sustituido por un heterociclo de cinco o seis eslabones; piperidinilo sustituido por hidroxi, - CH2OH o -C(O)NH2; piperazinilo sustituido por R1; [1,4] diazepanilo sustituido por R1; R1 puede ser uno o dos sustituyentes elegidos entre el grupo formado por: hidrogeno; oxo; alquilo inferior sustituido por R2; -C(O)R3; -SO2-alquilo inferior; -SO2- heterociclilo de cinco eslabones; R2 se elige entre el grupo formado por: -SO2-alquilo inferior; hidroxi; alcoxi inferior; trifluorometilo; -NH-SO2-alquilo inferior; -NH-C(O)-alquilo inferior; -C(O)-alquilo inferior; -ciano; -C(O)R4; R3 se elige entre el grupo formado por: heterociclilo; alquilo inferior; alquenilo inferior; alquilo inferior sustituido por alcoxi inferior o un heterociclilo de cinco o seis eslabones; alcoxi inferior; cicloalquilo; R4 se elige entre el grupo formado por: hidroxi; alcoxi inferior; morfolina; piperidina; pirrolidina; aziridina; 4-acetil-piperazinilo; -NR5R6; R5 y R6 con independencia entre sí se eligen entre el grupo formado por: hidrogeno; alquilo inferior; alquilo inferior sustituido por alcoxi inferior o ciano; alcoxi inferior; y cicloalquilo.
ARP060100970A 2005-03-16 2006-03-14 Compuestos cis-2,4,5-triaril-imidazolinas y su uso como medicamento anti-cancer AR053446A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US66251605P 2005-03-16 2005-03-16

Publications (1)

Publication Number Publication Date
AR053446A1 true AR053446A1 (es) 2007-05-09

Family

ID=36572145

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060100970A AR053446A1 (es) 2005-03-16 2006-03-14 Compuestos cis-2,4,5-triaril-imidazolinas y su uso como medicamento anti-cancer

Country Status (16)

Country Link
US (1) US7579368B2 (es)
EP (1) EP1861376A1 (es)
JP (1) JP4955646B2 (es)
KR (2) KR101139263B1 (es)
CN (1) CN101155784A (es)
AR (1) AR053446A1 (es)
AU (1) AU2006224765B2 (es)
BR (1) BRPI0607445A2 (es)
CA (1) CA2599476A1 (es)
IL (1) IL185381A0 (es)
MX (1) MX2007011151A (es)
NO (1) NO20074391L (es)
RU (1) RU2411238C2 (es)
TW (1) TWI314552B (es)
WO (1) WO2006097261A1 (es)
ZA (1) ZA200707653B (es)

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Also Published As

Publication number Publication date
BRPI0607445A2 (pt) 2009-09-01
TWI314552B (en) 2009-09-11
KR101139263B1 (ko) 2012-05-16
CN101155784A (zh) 2008-04-02
WO2006097261A1 (en) 2006-09-21
US20060211693A1 (en) 2006-09-21
CA2599476A1 (en) 2006-09-21
JP2008533073A (ja) 2008-08-21
KR20100031783A (ko) 2010-03-24
RU2411238C2 (ru) 2011-02-10
EP1861376A1 (en) 2007-12-05
AU2006224765B2 (en) 2012-02-09
KR20070107129A (ko) 2007-11-06
TW200700393A (en) 2007-01-01
AU2006224765A1 (en) 2006-09-21
ZA200707653B (en) 2013-02-27
NO20074391L (no) 2007-12-11
RU2007137987A (ru) 2009-04-27
MX2007011151A (es) 2007-10-17
US7579368B2 (en) 2009-08-25
JP4955646B2 (ja) 2012-06-20
IL185381A0 (en) 2008-02-09

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