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PE20040832A1 - DERIVATIVES OF INDOLIL PIRAZINONE - Google Patents

DERIVATIVES OF INDOLIL PIRAZINONE

Info

Publication number
PE20040832A1
PE20040832A1 PE2003001136A PE2003001136A PE20040832A1 PE 20040832 A1 PE20040832 A1 PE 20040832A1 PE 2003001136 A PE2003001136 A PE 2003001136A PE 2003001136 A PE2003001136 A PE 2003001136A PE 20040832 A1 PE20040832 A1 PE 20040832A1
Authority
PE
Peru
Prior art keywords
atoms
quinoxalinone
indol
halo
alkyl
Prior art date
Application number
PE2003001136A
Other languages
Spanish (es)
Inventor
Gaetan H Ladouceur
Jacques Dumas
Cheng Bi
Brian Bear
Michael R Turner
Robert Sibley
Michael J Burke
James Cook
David R Britteli
Gang Chen
Original Assignee
Bayer Pharmaceuticals Corp
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 Bayer Pharmaceuticals Corp filed Critical Bayer Pharmaceuticals Corp
Publication of PE20040832A1 publication Critical patent/PE20040832A1/en

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE INDOLIL DE FORMULA I, SUS SALES O ESTERES FARMACEUTICAMENTE ACEPTABLES, EN DONDE Ar ES UN ANILLO AROMATICO DE 6 MIEMBROS CON 0, 1 o 2 ATOMOS DE N; R1 Y R2 SON, INDEPENDIENTEMENTE ENTRE SI, H, HALO, CF3, ENTRE OTROS; CON LA CONDICION DE QUE CUANDO Ar CONTIENE 1 o 2 ATOMOS DE N, R1 Y R2 DEBEN SER, CADA UNO, H; Y R1 Y R2 JUNTO CON LOS ATOMOS DE C ADYACENTES A LOS CUALES ESTAN UNIDOS FORMAN UN ANILLO SELECCIONADO DE BENZO, DIOXOLO E IMIDAZO, DONDE DICHO IMIDAZO ESTA OPCIONALMENTE SUSTITUIDO HASTA 2 VECES CON ALQUILO C1-C3; CON LA CONDICION DE QUE R1 Y R2 JUNTO CON LOS ATOMOS DE C ADYACENTES A LOS QUE ESTAN UNIDOS FORMAN UN ANILLO SOLO CUANDO Ar NO CONTIENE ATOMOS DE N; R3 ES H, ALQUILO C1-C4, H, NO2, NH2, ENTRE OTROS; R4 ES H, OH, HALO, CN, ENTRE OTROS; R5 ES H, HALO, CN, ALCOXI C1-C6 o ALQUILO C1-C6; R11 Y R12 SON, INDEPENDIENTEMENTE ENTRE SI, H, F, O Cl; CON LA CONDICION DE QUE CUANDO UNO DE R11 Y R12 ES F o Cl, EL OTRO DEBE SER H. SON COMPUESTOS PREFERIDOS: 3-(1H-INDOL-2-IL)-2(1H)-QUINOXALINONA; 3-(3-NITRO-1H-INDOL-2-IL)-2(1H)-QUINOXALINONA; 3-(3-AMINO-1H-INDOL-2-IL)-2(1H)-QUINOXALINONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN METODO. ESTOS COMPUESTOS SON UTILES PARA TRATAR TRASTORNOS HIPERPROLIFERATIVOSREFERS TO COMPOUNDS DERIVED FROM INDOLIL OF FORMULA I, ITS PHARMACEUTICALLY ACCEPTABLE SALTS OR ESTERS, WHERE Ar IS A 6-MEMBER AROMATIC RING WITH 0, 1, or 2 N ATOMS; R1 AND R2 ARE, INDEPENDENTLY BETWEEN IF, H, HALO, CF3, BETWEEN OTHERS; WITH THE CONDITION THAT WHEN Ar CONTAINS 1 or 2 ATOMS OF N, R1 AND R2 MUST EACH H; AND R1 AND R2 TOGETHER WITH THE ADJACENT C ATOMS TO WHICH THEY ARE UNITED FORM A SELECTED RING OF BENZO, DIOXOLO AND IMIDAZO, WHERE SAID IMIDAZO IS OPTIONALLY SUBSTITUTED UP TO 2 TIMES WITH C1-C3 ALKYL; WITH THE CONDITION THAT R1 AND R2 TOGETHER WITH THE ADJACENT C ATOMS TO WHICH THEY ARE UNITED, MAKE A RING ONLY WHEN Ar DOES NOT CONTAIN N ATOMS; R3 IS H, C1-C4 ALKYL, H, NO2, NH2, AMONG OTHERS; R4 IS H, OH, HALO, CN, AMONG OTHERS; R5 IS H, HALO, CN, C1-C6 ALCOXY or C1-C6 ALKYL; R11 AND R12 ARE, INDEPENDENTLY BETWEEN IF, H, F, OR Cl; WITH THE CONDITION THAT WHEN ONE OF R11 AND R12 IS F or Cl, THE OTHER MUST BE H. THE PREFERRED COMPOUNDS ARE: 3- (1H-INDOL-2-IL) -2 (1H) -QUINOXALINONE; 3- (3-NITRO-1H-INDOL-2-IL) -2 (1H) -QUINOXALINONE; 3- (3-AMINO-1H-INDOL-2-IL) -2 (1H) -QUINOXALINONE; AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A METHOD. THESE COMPOUNDS ARE USEFUL TO TREAT HYPERPROLIFERATIVE DISORDERS

PE2003001136A 2002-11-12 2003-11-11 DERIVATIVES OF INDOLIL PIRAZINONE PE20040832A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42549002P 2002-11-12 2002-11-12
US46091503P 2003-04-07 2003-04-07
US48420203P 2003-06-30 2003-06-30

Publications (1)

Publication Number Publication Date
PE20040832A1 true PE20040832A1 (en) 2005-01-27

Family

ID=32314888

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001136A PE20040832A1 (en) 2002-11-12 2003-11-11 DERIVATIVES OF INDOLIL PIRAZINONE

Country Status (17)

Country Link
EP (1) EP1565455A1 (en)
JP (1) JP2006509840A (en)
KR (1) KR20050072824A (en)
AR (1) AR043059A1 (en)
AU (1) AU2003290744A1 (en)
BR (1) BR0316169A (en)
CA (1) CA2505819A1 (en)
EC (1) ECSP055851A (en)
HR (1) HRP20050496A2 (en)
MA (1) MA27557A1 (en)
MX (1) MXPA05004779A (en)
NO (1) NO20052796L (en)
PE (1) PE20040832A1 (en)
PL (1) PL376867A1 (en)
TW (1) TW200418834A (en)
UY (1) UY28074A1 (en)
WO (1) WO2004043950A1 (en)

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GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
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GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
JO3512B1 (en) 2014-03-26 2020-07-05 Astex Therapeutics Ltd Quinoxaline derivatives useful as fgfr kinase modulators
CA2943682C (en) 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of fgfr and cmet inhibitors and their use for the treatmentof cancer
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Also Published As

Publication number Publication date
WO2004043950A1 (en) 2004-05-27
HRP20050496A2 (en) 2006-06-30
TW200418834A (en) 2004-10-01
PL376867A1 (en) 2006-01-09
NO20052796D0 (en) 2005-06-09
ECSP055851A (en) 2005-09-20
MA27557A1 (en) 2005-10-03
NO20052796L (en) 2005-06-09
AU2003290744A1 (en) 2004-06-03
JP2006509840A (en) 2006-03-23
EP1565455A1 (en) 2005-08-24
CA2505819A1 (en) 2004-05-27
AR043059A1 (en) 2005-07-13
MXPA05004779A (en) 2005-07-22
BR0316169A (en) 2005-09-27
KR20050072824A (en) 2005-07-12
UY28074A1 (en) 2004-05-31

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