AR052419A1 - Derivados de bencimidazolil n-sustituidos,inhibidores del protooncogen c-kit - Google Patents

Derivados de bencimidazolil n-sustituidos,inhibidores del protooncogen c-kit

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Publication number
AR052419A1
AR052419A1 ARP050105014A ARP050105014A AR052419A1 AR 052419 A1 AR052419 A1 AR 052419A1 AR P050105014 A ARP050105014 A AR P050105014A AR P050105014 A ARP050105014 A AR P050105014A AR 052419 A1 AR052419 A1 AR 052419A1
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AR
Argentina
Prior art keywords
8alkyl
optionally substituted
independent
cyclyl
substituted
Prior art date
Application number
ARP050105014A
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English (en)
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Osi Pharm 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.)
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Publication date
Application filed by Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of AR052419A1 publication Critical patent/AR052419A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/12Heterocyclic 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
    • 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
    • C07D403/10Heterocyclic 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 aromatic 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • 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
    • C07D413/10Heterocyclic 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 aromatic rings
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/11Compounds covalently bound to a solid support
    • CCHEMISTRY; METALLURGY
    • C40COMBINATORIAL TECHNOLOGY
    • C40BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00Libraries per se, e.g. arrays, mixtures

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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones farmacéuticas que los contienen, usos como anticancerígenos y bancos combinatorios de benzimidazoles. Reivindicacion 1: Un compuesto represnetadop por la formula (1) o una sal o un N-oxido farmacéuticamente aceptable de la misma, en donde: R1 y R2 son independientemente C0-8 alquil sustituido opcionalmente con un sustituyente heterociclilo; C0-8 alquil sustituido opcionalmente con un halo independiente 1-6, -CONR11R12, -NR13CONR11R12, -NR13CO2R11, -S(O)0-2NR11R12, -NR11S(O)0- 2R12, CN, OH, o sustituyentes del arilo sustituido opcionalmente; -C0-8alquil-C3-8cicloalquil; -C0-8alquil-O-C0-8alquil-, -C0-8alquil- N(C0-8alquil)(C0-8alquil), -C0-8alquil-S(O)0-2-C0-8alquil-; o heterociclilo sustituido opcionalmente con ciclilo, C0-8alquil independiente 1-4, o sustituyentes del ciclilo sustituido; o R1 y R2, tomados juntos con el N al cual se encuentran unidos, forman un grupo heterocíclico, sustituido opcionalmente con grupos C0-8alquil, -C0-8alquil-O-C0-8alquil-, -C0- 8alquil-arilo independientes 1-4, o grupos -C0-8alquil-heteroarilo, siempre que el grupo heterocíclico que se forme no sea piperazina; R3 es un grupo arilo o hetarilo, sustituido opcionalmente con C0-8alquil, C0-8alquil-ciclil, halo, OH, -NR31S(O)0- 2R32, -(O)0-2NR31R32, -NR31COR32, -NR31CONR32R33, - CONR31R32, S(O)0-2R31, O-arilo, -O-hetarilo, NO2, CN, CF3, OCF3, OCHF2; independiente 1-4; R11, R12, R13, R31, R32, y R33 son cada uno independientemente C0-8alquil sustituido opcionalmente con un sustituyente heterociclilo, C0-8alquil sustituido opcionalmente con un sustituyente halo -CON(C0-8alquil)(C0-8alquil), -N(C0-8alquil)CON(C0-8alquil)(C0-8alquil), -N(C0-8alquil)CO2(C0-8alquil), S(O) 0-2N(C0-8alquil)(C0-8alquil), -NR11S(O)0-2(C0- 8alquil), CN, OH, independiente 1-6, o sustituyentes del arilo sustituido opcionalmente; -C0-8alquil-C3-8cicloalquil; -C0-8alquil-O-C0-8alquil-, -C0-8alquil-N(C0-8alquil)(C0-8alquil), -C0-8alquil-S(O)0-2-C0-8alquil-; o heterociclilo sustituido opcionalmente con ciclilo, C0-8alquil independiente 1-4, o sustituyentes del ciclilo sustituido; y siempre que R3 no sea un grupo tetrazolilo, 5-pirimidinilo, o 4-bifenilo.
ARP050105014A 2004-12-01 2005-11-30 Derivados de bencimidazolil n-sustituidos,inhibidores del protooncogen c-kit AR052419A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US63243204P 2004-12-01 2004-12-01

Publications (1)

Publication Number Publication Date
AR052419A1 true AR052419A1 (es) 2007-03-21

Family

ID=36128376

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050105014A AR052419A1 (es) 2004-12-01 2005-11-30 Derivados de bencimidazolil n-sustituidos,inhibidores del protooncogen c-kit

Country Status (12)

Country Link
US (1) US7419995B2 (es)
EP (1) EP1831206B1 (es)
JP (1) JP2008521903A (es)
KR (1) KR20070086865A (es)
CN (1) CN101193867A (es)
AR (1) AR052419A1 (es)
AT (1) ATE521604T1 (es)
AU (1) AU2005312028A1 (es)
BR (1) BRPI0518794A2 (es)
CA (1) CA2589770A1 (es)
TW (1) TW200633704A (es)
WO (1) WO2006060381A2 (es)

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Publication number Publication date
CN101193867A (zh) 2008-06-04
KR20070086865A (ko) 2007-08-27
US20060116402A1 (en) 2006-06-01
WO2006060381A2 (en) 2006-06-08
EP1831206A2 (en) 2007-09-12
WO2006060381A3 (en) 2006-12-28
TW200633704A (en) 2006-10-01
EP1831206B1 (en) 2011-08-24
CA2589770A1 (en) 2006-06-08
ATE521604T1 (de) 2011-09-15
US7419995B2 (en) 2008-09-02
JP2008521903A (ja) 2008-06-26
BRPI0518794A2 (pt) 2008-12-09
AU2005312028A1 (en) 2006-06-08

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