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PE20030895A1 - Cis-imidazolinas - Google Patents

Cis-imidazolinas

Info

Publication number
PE20030895A1
PE20030895A1 PE2003000024A PE2003000024A PE20030895A1 PE 20030895 A1 PE20030895 A1 PE 20030895A1 PE 2003000024 A PE2003000024 A PE 2003000024A PE 2003000024 A PE2003000024 A PE 2003000024A PE 20030895 A1 PE20030895 A1 PE 20030895A1
Authority
PE
Peru
Prior art keywords
imidazolines
cis
formula
peptide
inhibit
Prior art date
Application number
PE2003000024A
Other languages
English (en)
Inventor
Norman Kong
Bihn Thanh Vu
Emily Aijun Liu
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20030895A1 publication Critical patent/PE20030895A1/es

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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/22—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/20—Heterocyclic 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
    • C07D233/26—Radicals substituted by carbon atoms having three bonds to hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

SE REFIERE A CIS-IMIDAZOLINAS DE FORMULA I DONDE R ES -C=OR1 DONDE R1 ES ALQUILO C1-C6, -C=CHCOOH, -NHCH2CH2R2, -N(CH2CH2OH)CH2CH2OH, ANILLOS DE 4 A 6 MIEMBROS SATURADOS Y ANILLOS DE 5 Y 6 MIEMBROS CON HETEROATOMOS; R5 ES H, ALQUILO C1-C6, -NH2, -N-, ALQUILO C1-C6, ENTRE OTROS; R2 ES -N(CH3)CH3, -NCH2CH2NH2, -NH2, MORFOLINILO Y PIPERAZINILO; X1, X2 Y X3 SON OH, ALQUILO C1-C2, ALCOXILO C1-C6, Cl, F, Br, ENTRE OTROS; R3 ES -F, OCH3, -N(CH3)CH3, -Cl, -Br, ANILLOS DE 5 Y 6 MIEMBROS, ENTRE OTROS; R4 ES UN ANILLO SATURADO DE 3 A 5 MIEMBROS; Y1 E Y2 SON -Cl, -Br, -NO2, -C=N, -C=CH. SON COMPUESTOS PREFERIDOS 1-[4,5-BIS-(4-CLORO-FENIL)-2-(2,4-DIMETOXI-FENIL)-4,5-DIHIDRO-IMIDAZOL-1-IL]-2-METIL-PROPAN-1-ONA, 1-[4,5-BIS-(4-CLORO-FENIL)-2-(2,4-DIMETOXI-FENIL)-4,5-DIHIDRO-IMIDAZOL-1-IL] ETANONA, 1-[4,5-BIS-(4-CLORO-FENIL)-2-(2,4-DIMETOXI-FENIL)-4,5-DIHIDRO-IMIDAZOL-1-IL]-2,2-DIMETIL-PROPAN-1-ONA, [4,5-BIS-(4-CLORO-FENIL)-2-(2,4-DIMETOXI-FENIL)-4,5-DIHIDRO-IMIDAZOL-1-IL]-CICLOPENTILO-METANONA, ENTRE OTROS. LOS COMPUESTOS CIS-IMIDAZOLINA SON PEQUENOS INHIBIDORES MOLECULARES DE LA INTERACCION MDM2-p53 Y SON UTILES PARA EL TRATAMIENTO DE TUMORES
PE2003000024A 2001-12-18 2003-01-06 Cis-imidazolinas PE20030895A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34171401P 2001-12-18 2001-12-18
US39087402P 2002-06-21 2002-06-21

Publications (1)

Publication Number Publication Date
PE20030895A1 true PE20030895A1 (es) 2003-10-25

Family

ID=26992625

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000024A PE20030895A1 (es) 2001-12-18 2003-01-06 Cis-imidazolinas

Country Status (19)

Country Link
US (1) US6734302B2 (es)
EP (1) EP1458380B1 (es)
JP (1) JP4477351B2 (es)
KR (2) KR20060096513A (es)
CN (1) CN100486969C (es)
AT (1) ATE389400T1 (es)
AU (1) AU2002366278B2 (es)
BR (1) BR0215157A (es)
CA (1) CA2469187C (es)
DE (1) DE60225719T2 (es)
ES (1) ES2301717T3 (es)
MX (1) MXPA04005906A (es)
PA (1) PA8561901A1 (es)
PE (1) PE20030895A1 (es)
PL (1) PL370823A1 (es)
RU (1) RU2305095C2 (es)
TW (1) TW200301112A (es)
UY (1) UY27585A1 (es)
WO (1) WO2003051359A1 (es)

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DE60225719D1 (de) 2008-04-30
EP1458380A1 (en) 2004-09-22
TW200301112A (en) 2003-07-01
EP1458380B1 (en) 2008-03-19
PL370823A1 (en) 2005-05-30
CA2469187A1 (en) 2003-06-26
RU2004122414A (ru) 2005-06-27
CA2469187C (en) 2012-07-17
PA8561901A1 (es) 2003-11-12
KR20040068277A (ko) 2004-07-30
CN100486969C (zh) 2009-05-13
JP2005511766A (ja) 2005-04-28
BR0215157A (pt) 2004-10-19
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US20030153580A1 (en) 2003-08-14
KR100650966B1 (ko) 2006-11-30
KR20060096513A (ko) 2006-09-11
AU2002366278A1 (en) 2003-06-30
RU2305095C2 (ru) 2007-08-27
ATE389400T1 (de) 2008-04-15
UY27585A1 (es) 2003-06-30
DE60225719T2 (de) 2009-04-23
CN1606439A (zh) 2005-04-13
AU2002366278B2 (en) 2007-07-19
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