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AR045387A1 - Compuestos bencimidazolil n-sustituidos inhibidores de c-kit; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de un trastorno proliferativo - Google Patents

Compuestos bencimidazolil n-sustituidos inhibidores de c-kit; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de un trastorno proliferativo

Info

Publication number
AR045387A1
AR045387A1 ARP040103008A ARP040103008A AR045387A1 AR 045387 A1 AR045387 A1 AR 045387A1 AR P040103008 A ARP040103008 A AR P040103008A AR P040103008 A ARP040103008 A AR P040103008A AR 045387 A1 AR045387 A1 AR 045387A1
Authority
AR
Argentina
Prior art keywords
alkyl
cyclyl
co2h
heterocyclyl
substituents
Prior art date
Application number
ARP040103008A
Other languages
English (en)
Original Assignee
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.)
Filing date
Publication date
Application filed by Osi Pharm Inc filed Critical Osi Pharm Inc
Publication of AR045387A1 publication Critical patent/AR045387A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • 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
    • 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
    • C07D405/12—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
    • 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
    • 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)
  • Engineering & Computer Science (AREA)
  • Health & Medical Sciences (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Materials Engineering (AREA)
  • Structural Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Abstract

La presente se refiere al uso del compuesto de fórmula (1) en composiciones farmacéuticas y para la preparación de un medicamento a utilizar en el tratamiento de un trastorno proliferativo, tal como cáncer de mama, cabeza, cuello, gastrointestinal o leucemia. Reivindicación 1: Un compuesto representado por la fórmula (1), o su sal aceptable para uso farmacéutico, o su N-óxido, donde uno de R11, R12, R13 y R14 es -NR3COR31, -NR3CONR3R31, -NR3SO2R31, -CO2R3, -CO2H, -alquil (0-8)NR3R31 o -CONR3R31; los otros cada uno de forma independiente F, Cl, alquilo C0-3, alcoxi C0-8, o -N(alquil C0-8)(alquilo C0-8); X es un grupo ciclilo o heterociclilo, sustituido de forma optativa con 1-4 sustituyentes halógeno, -NR32R33, -NR32COR33, -NR32CO2R33, -NR32SO2R33, -OR32, -SR32, -SO2R32, -SO2NR32R33, -CO2R32, -CO2H, -CONR32R33, -alquilo C0-8, -alquenilo C2-8, -alquinilo C2-8, -CN, -CF3, -OCF3, -NO2, oxo, ciclilo o heterocíclico, Y está ausente o es uno de los grupos de fórmulas (2) donde el punto de unión a X puede ser tanto de izquierda o derecha como se muestra; Ra y Rb son cada uno de forma independiente alquilo C0-8 o cicloalquilo C3-8, o Ra y Rb tomados en conjunto con el C al cual están unidos forman un anillo de 3 a 10 miembros saturado o parcialmente insaturado conteniendo 0-4 N, O, S, SO o SO2 en los nodos del anillo, siempre que no haya átomos de N O o S ubicados en forma adyacente uno del otro en los nodos del anillo; Rc es alquilo C0-8; o Rc, tomado con tanto Ra como Rb, forma un anillo saturado o parcialmente insaturado de 3-7 miembros; m es 0,1 2, 3, 4 o 5; siempre que cuando m es 0 o 1, no debe haber átomos de N, O o S adyacentes uno del otro en el puente conector N-X-Y-Z; n es 1, 2, 3, 4 o 5, siempre que cuando n es 1, no debe haber átomos de N, O o S adyacentes uno del otro en el puente conector N-X-Y-Z; Z es un grupo ciclilo o heterociclilo, sustituido en forma optativa con 1-5 sustituyentes independientemente halógeno, -NR34R35, -NR34COR35, -NR34C(O)OR35, -NR34SO2R35, -OR34, -SR34, -SO2R34, -SO2NR34R35, -C(O)OR34, -CO2H, -CONR34R35, alquilo C0-8, alquenilo C2-8, alquinilo C2-8, -O-alquilo C0-8, -Salquilo C0-8, -SO2alquilo C0-8, -SO2N(alquil C0-8-)(alquiloC0-8), -C(O)Oalquilo C0-8, CN, CF3, NO2, oxo, sustituyentes ciclilo o heterociclilo; o cuando Y esté presente, Z también puede ser alquil C0-8-O-alquilo C0-8, alquil C0-8-O-C(O)-alquilo C0-8, o alquil C0-8-C(O)-O-alquilo C0-8; siempre que cuando Y es -OCH2-, Z debe estar sustituido con 1-5 sustituyentes NR34R35, -NR34COR35, -NR34C(O)OR35, -NR34SO2R35, -OR34, -SR34, -SO2R34, -SO2NR34R35, -CO2R34, -CO2H, -CONR34R35, alquilo C0-8, alquenilo C2-8, alquinilo C2-8, CF3, NO2, oxo, ciclilo o heterociclilo; siempre que cuando Y es NHCH2, Z debe estar sustituido con 1-5 sustituyentes halógeno, -NR34R35, -NR34COR35, -NR34C(O)OR35, -NR34SO2R35, -OR34, -SR34, -SO2R34, -SO2NR34R35, -CO2R34, -CO2H, -CONR34R35, alquilo C0-8, alquenilo C2-8, alquinilo C2-8, CF3, NO2, oxo, ciclilo o heterociclilo; siempre que cuando Y esté ausente, X y Z no pueden contener N, R3, R31, R32, R33, R34 y R35 son en forma independiente alquilo C0-8 sustituido con sustituyentes heterociclilo u OH; CF3, CHF2, -alquil C0-8-O-alquil C0-8, -alquil C0-8-N(alquil C0-8)(alquilo C0-8), -alquil C0-8-S(O)0-2-alquilo C0-8 o -alquil C0-8-S(O)2N(alquil C0-8)(alquilo C0-8).
ARP040103008A 2003-08-21 2004-08-20 Compuestos bencimidazolil n-sustituidos inhibidores de c-kit; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de un trastorno proliferativo AR045387A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US49680603P 2003-08-21 2003-08-21

Publications (1)

Publication Number Publication Date
AR045387A1 true AR045387A1 (es) 2005-10-26

Family

ID=34272519

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103008A AR045387A1 (es) 2003-08-21 2004-08-20 Compuestos bencimidazolil n-sustituidos inhibidores de c-kit; composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de un trastorno proliferativo

Country Status (18)

Country Link
US (1) US7521448B2 (es)
EP (1) EP1664021A1 (es)
JP (1) JP4769720B2 (es)
KR (1) KR20060121818A (es)
CN (1) CN1852905A (es)
AP (1) AP2006003549A0 (es)
AR (1) AR045387A1 (es)
AU (1) AU2004268949A1 (es)
BR (1) BRPI0413746A (es)
CA (1) CA2535896A1 (es)
IL (1) IL173614A0 (es)
IS (1) IS8319A (es)
MX (1) MXPA06002018A (es)
NO (1) NO20060664L (es)
RU (1) RU2006108803A (es)
TW (1) TW200524905A (es)
UA (1) UA82395C2 (es)
WO (1) WO2005021531A1 (es)

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RU2006108803A (ru) 2007-09-27
IL173614A0 (en) 2006-07-05
BRPI0413746A (pt) 2006-10-24
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AU2004268949A1 (en) 2005-03-10
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AP2006003549A0 (en) 2006-04-30
JP4769720B2 (ja) 2011-09-07
KR20060121818A (ko) 2006-11-29
UA82395C2 (en) 2008-04-10
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