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AR037330A1 - Derivado de quinazolina, composicion farmaceutica, su uso en la fabricacion de un medicamento y proceso para preparar dicho derivado de quinazolina - Google Patents

Derivado de quinazolina, composicion farmaceutica, su uso en la fabricacion de un medicamento y proceso para preparar dicho derivado de quinazolina

Info

Publication number
AR037330A1
AR037330A1 ARP020104181A ARP020104181A AR037330A1 AR 037330 A1 AR037330 A1 AR 037330A1 AR P020104181 A ARP020104181 A AR P020104181A AR P020104181 A ARP020104181 A AR P020104181A AR 037330 A1 AR037330 A1 AR 037330A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
group
carbamoyl
heterocyclyl
Prior art date
Application number
ARP020104181A
Other languages
English (en)
Inventor
Laurent Hennequin
Jason Kettle
Martin Pass
Robert Bradbury
Original Assignee
Astrazeneca Ab
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
Priority claimed from GBGB0126433.2A external-priority patent/GB0126433D0/en
Priority claimed from GB0129059A external-priority patent/GB0129059D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR037330A1 publication Critical patent/AR037330A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen 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
    • C07D403/12Heterocyclic 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
    • 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
    • C07D405/14Heterocyclic 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
    • 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
    • C07D413/14Heterocyclic 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un derivado de quinazolina que responde a la fórmula (1), donde: R1 es hidrógeno o alquilo (C1-6); Z es un enlace directo o se selecciona entre O, S y N(R2), donde R2 es hidrógeno o alquilo (C1-6); Q1 es cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), cicloalquelino (C3-7), cicloalquenil (C3-7)-alquilo (C1-6), heterociclilo o heterociclil-alquilo (C1-6), y donde los átomos de carbono adyacentes en cualquier cadena alquileno (C2-6) dentro del grupo Q1-Z- se separan opcionalmente por la inserción en la cadena de un grupo seleccionado entre O, S, SO, SO2, N(R3), CO, CH(OR3), CON(R3), N(R3)CO, SO2N(R3), N(R3)SO2, CH=CH y CsC donde R3 es hidrógeno o alquilo (C1-6), y donde cualquier grupo CH2 o CH3 dentro del grupo Q1-Z- opcionalmente lleva en cada uno de los dichos grupos CH2 o CH3 uno o más sustituyentes halógeno o alquilo (C1-6) o un sustituyente seleccionado entre hidroxi, ciano, amino, carboxi, carbamoilo, alcoxi (C1-6), alquiltio (C1-6), alquilsulfinilo (C1-6), alquilsulfonilo (C1-6), alquilamino (C1-6), di-[alquil (C1-6)]amino, alcoxicarbonilo (C1-6), N-alquilcarbamoilo (C1-6), N,N-di-[alquil (C1-6)]carbamoilo, alcanoilo (C2-6), alcanoiloxi (C2-6), alcanoilamino (C2-6), N-alquil (C1-6)-alcanoilamino (C2-6), N-alquilsulfamoilo (C1-6), N,N-di-[alquil (C1-6)]sulfamoilo, alcansulfonilamino (C1-6) y N-alquil (C1-6)-alcansulfonilamino (C1-6), y donde cualquier grupo heterociclilo, cicloalquilo (C3-7) o cicloalquelino (C3-7) dentro del grupo Q1-Z- opcionalmente lleva 1, 2 ó 3 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halógeno, trifluorometilo, ciano, nitro, hidroxi, amino, carboxi, carbamoilo, formilo, alquilo (C1-6), alquenilo (C2-8), alquinilo (C2-8), alcoxi (C1-6), alqueniloxi (C2-6), alquiniloxi (C2-6), alquiltio (C1-6), alquilsulfinilo (C1-6), alquilsulfonilo (C1-6), alquilamino (C1-6), di-[alquil (C1-6)]amino, alcoxicarbonilo (C1-6), N-alquilcarbamoilo (C1-6), N,N-di-[alquil (C1-6)]carbamoilo, alcanoilo (C2-6), alcanoiloxi (C2-6), amino-alcanoilo (C2-6), N-alquilamino (C1-6)-alcanoilo (C2-6), N,N-di-[alquil (C1-6)]amino-alcanoilo (C2-6), alcanoilamino (C2-6), N-alquil (C1-6)-alcanoilamino (C2-6), N-alquilsulfamoilo (C1-6), N,N-di-[alquil (C1-6)]sulfamoilo, alcansulfonilamino (C1-6), N-alquil (C1-6)-alcansulfonilamino (C1-6), de un grupo de la fórmula: -X1-R4, donde X1 es un enlace, directo o se selecciona entre O y N(R5), donde R5 es hidrógeno o alquilo (C1-6), y R4 es halógeno-alquilo (C1-6), hidroxi-alquilo (C1-6), alcoxi (C1-6)-alquilo (C1-6), ciano-alquilo (C1-6), carboxi-alquilo (C1-6), amino-alquilo (C1-6), alquilamino (C1-6)-alquilo (C1-6), di-[alquil (C1-6)]amino-alquilo (C1-6), carbamoil-alquilo (C1-6), N-alquilcarbonil (C1-6)-alquilo (C1-6), N,N-di-[alquil (C1-6)]carbamoil-alquilo (C1-6), alcanoil (C2-6)-alquilo (C1-6) o alcoxicarbonil (C1-6)-alquilo (C1-6), y un grupo de la fórmula: -X5-Q6 donde X5 es un enlace directo o se selecciona entre O, CO, y N(R10), donde R10 es hidrógeno o alquilo (C1-6), y Q6 es heterociclilo, heterociclil-alquilo (C1-6), cicloalquilo (C3-7), cicloalquil (C3-7)-alquilo (C1-6), cicloalquenilo (C3-7) o cicloalquenil (C3-7)-alquilo (C1-6), y en donde cualquier grupo heterociclilo, cicloalquilo (C3-7) o cicloalquenilo (C3-7) en Q6 opcionalmente lleva 1 ó 2 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halógeno, hidroxi, ciano, formilo, alquilo (C1-6), alquenilo (C2-6), alquinilo (C2-6), alcoxi (C1-6), amino, alquilamino (C1-6), di[alquil (C1-6)]amino, alcanoilo (C2-6), alcoxicarbonilo (C1-6), alquilsulfinilo (C1-6), carbamoilo, N-(C1-6)alquilcarbamoilo, N,N-di-[alquil (C1-6)]carbamoilo, halógeno-alquilo (C1-6), hidroxi-alquilo (C1-6), alcoxi (C1-6)-alquilo (C1-6), ciano-alquilo (C1-6), carboxi-alquilo (C1-6), amino-alquilo (C1-6), alquilamino (C1-6)-alquilo (C1-6), di-[alquil (C1-6)]amino-alquilo (C1-6), carbamoil-alquilo (C1-6), N-alquilcarbamoil (C1-6)-alquilo (C1-6) y N,N-di-[alquil (C1-6)]carbamoil-alquilo (C1-6), y donde cualquier grupo heterociclilo dentro del grupo Q1-Z- opcionalmente lleva 1 ó 2 sustituyentes oxo o tioxo; y Q2 se selecciona entre el grupo de fórmulas (2), donde G1, G2, G3, G4 y G5 son cada uno, independientemente, seleccionado entre hidrógeno, halógeno, trifluorometilo, ciano, nitro, hidroxi, amino, carboxi, carbamoilo, alquilo (C1-6), alquenilo (C2-8), alquinilo (C2-8), alcoxi (C1-6), alqueniloxi (C2-6), alquiniloxi (C2-6), alquilamino (C1-6) y di-[alquil (C1-6)]amino, G6 y G7 son cada uno, independientemente, seleccionado entre hidrógeno y halógeno, X2 es un enlace directo o se selecciona entre O, S, SO, SO2, N(R6), CH(OR6), CON(R6), N(R6)CO, SO2N(R6), N(R6)SO2, OC(R6)2, C(R6)2O, SC(R6)2, C(R6)2S, CO, C(R6)2N(R6) y N(R6)C(R6)2 donde cada R6 es, independientemente, hidrógeno o alquilo (C1-6), y Q3 es arilo, o heteroarilo, o X2 es CO y Q3 es un grupo heterociclilo con contenido de nitrógeno unido a X2 por un átomo de nitrógeno, X3 es un enlace directo o se selecciona entre SO2, CO, SO2N(R) y C(R7)2, donde cada R7 es, independientemente, hidrógeno o alquilo (C1-6), y Q4 es arilo o heteroarilo, y cualquier grupo arilo, heteroarilo o heterociclilo en el grupo -X2-Q3 y -X3-Q4 opcionalmente lleva 1, 2 ó 3 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halógeno, trifluorometilo, ciano, nitro, hidroxi, amino, carboxi, formilo, carbamoilo, sulfamoilo, mercapto, alquilo (C1-6), alquenilo (C2-8), alquinilo (C2-8), alcoxi (C1-6), alqueniloxi (C2-6), alquiniloxi (C2-6), alquiltio (C1-6), alquilsulfinilo (C1-6), alquilsulfonilo (C1-6), alquilamino (C1-6), di-[alquil (C1-6)]amino, alcoxicarbonilo (C1-6), N-alquilcarbamoilo (C1-6), N,N-di-[alquil(C1-6)]carbamoilo, alcanoilo (C2-6), alcanoiloxi (C2-6), alcanoilamino (C2-6), N-alquil (C1-6)-alcanoilamino (C2-6), N-alquilsulfamoilo (C1-6), N,N-di-[alquil(C1-6)]sulfamoilo, alcansulfonilamino (C1-6) y N-alquil (C1-6)-alcansulfonilamino (C1-6), o es un grupo de la fórmula X4-R8 donde X4 es un enlace directo o se selecciona entre O y N(R9), donde R9 es hidrógeno o alquilo (C1-6), y R8 es halógeno-alquilo (C1-6), hidroxi-alquilo (C1-6), alcoxi-alquilo (C1-6), ciano-alquilo (C1-6), carboxi-alquilo (C1-6), amino-alquilo (C1-6), alquilamino (C1-6)-alquilo (C1-6), di-[alquil (C1-6)]amino-alquilo (C1-6), carbamoilo-alquilo (C1-6), N-alquilcarbamoil (C1-6)-alquilo (C1-6), N,N-di-[alquil (C1-6)]carbamoil-alquilo (C1-6), alcanoil (C2-6)-alquilo (C1-6) o alcoxicarbonil (C1-6)-alquilo (C1-6), o es un grupo de la fórmula -Q5 donde Q5 se selecciona entre arilo, heteroarilo o heterociclilo que es opcionalmente sustituido por 1 ó 2 sustituyentes seleccionados entre halógeno, hidroxi, alquilo (C1-6), alcoxi (C1-6), amino, alquilamino (C1-6) y di-[alquil(C1-6)]amino, y donde cualquier grupo CH2 o CH3 dentro de un sustituyente en cualquier grupo arilo, heteroarilo o heterociclilo en el grupo -X2-Q3 y -X3-Q4 opcionalmente lleva en cada uno de dichos grupos CH2 o CH3 uno o más sustituyentes halógeno o alquilo (C1-6), y cualquier grupo heterociclilo representado por Q3 o Q4 opcionalmente lleva 1 ó 2 sustituyentes oxo o tioxo, o una sal aceptable para uso farmacéutico del mismo. Los procesos para su preparación, composiciones farmacéuticas que los contienen y su uso en la fabricación de un medicamento para usar en la prevención o tratamiento de tumores que son sensibles a la inhibición de miembros de la familia erbB de tirosina quinasas de receptor, también se describen.
ARP020104181A 2001-11-03 2002-11-01 Derivado de quinazolina, composicion farmaceutica, su uso en la fabricacion de un medicamento y proceso para preparar dicho derivado de quinazolina AR037330A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0126433.2A GB0126433D0 (en) 2001-11-03 2001-11-03 Compounds
GB0129059A GB0129059D0 (en) 2001-12-05 2001-12-05 Compounds

Publications (1)

Publication Number Publication Date
AR037330A1 true AR037330A1 (es) 2004-11-03

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Application Number Title Priority Date Filing Date
ARP020104181A AR037330A1 (es) 2001-11-03 2002-11-01 Derivado de quinazolina, composicion farmaceutica, su uso en la fabricacion de un medicamento y proceso para preparar dicho derivado de quinazolina

Country Status (22)

Country Link
US (2) US20050043336A1 (es)
EP (1) EP1444210B1 (es)
JP (1) JP2005515176A (es)
KR (1) KR20050042055A (es)
CN (1) CN100343238C (es)
AR (1) AR037330A1 (es)
AT (1) ATE423104T1 (es)
BR (1) BR0213842A (es)
CA (1) CA2465068A1 (es)
CO (1) CO5580774A2 (es)
DE (1) DE60231230D1 (es)
ES (1) ES2320980T3 (es)
HU (1) HUP0401646A2 (es)
IL (1) IL161619A0 (es)
IS (1) IS7240A (es)
MX (1) MXPA04004219A (es)
NO (1) NO20042279L (es)
NZ (1) NZ532524A (es)
PL (1) PL369938A1 (es)
RU (1) RU2004116911A (es)
TW (1) TW200301702A (es)
WO (1) WO2003040108A1 (es)

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