AR041346A1 - Derivados de imidazol[1,2-a]pirazinas como inhibidores de quinasas dependientes de ciclinas - Google Patents

Derivados de imidazol[1,2-a]pirazinas como inhibidores de quinasas dependientes de ciclinas

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Publication number
AR041346A1
AR041346A1 ARP030103440A ARP030103440A AR041346A1 AR 041346 A1 AR041346 A1 AR 041346A1 AR P030103440 A ARP030103440 A AR P030103440A AR P030103440 A ARP030103440 A AR P030103440A AR 041346 A1 AR041346 A1 AR 041346A1
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Argentina
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nr5r6
alkyl
heteroaryl
aryl
group
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ARP030103440A
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Schering Corp
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    • 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
    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

En sus muchas realizaciones, la presente proporciona compuestos de imidazo [1,2-a]pirazina como inhibidores de quinasas dependientes de ciclina, métodos de preparación de dichos compuestos, composiciones farmacéuticas que contienen uno o más dedichos compuestos, métodos de preparación de formulaciones farmacéuticas que comprenden uno o más de dichos compuestos, y métodos de tratamiento, prevención, inhibición o mejoría de una o más enfermedades asociadas con las CDK, utilizando dichoscompuestos o composiciones farmacéuticas. Reivindicación 1: Un compuesto representado por la fórmula estructural (1) en donde R se selecciona entre el grupo que consiste en alquilo, CF3, heteroarilo, heteroarilalquilo, cicloalquilo,cicloalquilalquilo, heterociclilo, heterociclilalquilo, arilalquilo, -C(O)R7, o como se muestra en los restos de fórmula (2), en donde cada uno de dichos alquilo, heteroarilo, arilalquilo, cicloalquilo, heterociclilo y las porciones heterociclilocuyas estructuras se muestran inmediatamente antes para R pueden estar no sustituidos o en forma opcional, independientemente sustituidos con una o más porciones iguales o diferentes, en donde cada porción se selecciona en forma independiente entreel grupo que consiste en halógeno, alquilo, cicloalquilo, CF3, CN, -OCF3, -OR6, -C(O)R7, NR5R6,-C(O2)R6, -C(O)NR5R6, -(CHR5)nOR6, -SR6, -S(O2)R7, -S(O2)NR5R6, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R6; R1 es H, halógeno o alquilo; R2 seselecciona entre el grupo que comprende H, halógeno, -CN, cicloalquilo, heterociclilo, alquinilo y -CF3; R3 se selecciona entre el grupo que consiste en arilo (excepto fenilo), heteroarilo (excepto furilo), heterociclilo, -(CHR5)n-heteroarilo, -S(O2)R6, -C(O)R6, -S(O2)NR5R6, -C(O)OR6, -C(O)NR5R6,o como se muestra en los restos de fórmula (3), en donde cada uno de dichos arilo, heteroarilo y heterociclilo pueden estar no sustituidos o en forma opcional sustituidos con una o más porcionesiguales o diferentes, en donde cada porción se selecciona en forma independiente entre el grupo que consiste en halógeno, alquilo, arilo, cicloalquilo, CF3, CN, OCF3, -OR5, -NR5R6, -C(O2)R5, -C(O)NR5R6, -SR6, -S(O2)R6, -S(O2)NR5R6, -N(R5)S(O2)R7, -N(R5)C(O)R7, y -N(R5)C(O)NR5R6; con la condición de que cuando R3 es -(CHR5)n-heteroarilo, R2 adicionalmente puede ser alquilo; R5 es H o alquilo; R6 se selecciona entre el grupo que consiste en H, alquilo, arilo, heteroarilo, arilalquilo, yheteroarilalquilo, en donde cada uno de dichos alquilo, heteroarilalquilo, arilo, heteroarilo y arilalquilo pueden estar no sustituidos o en forma opcional, sustituidos con una o más porciones iguales o diferentes, en donde cada porción seselecciona en forma independiente entre el grupo que consiste en halógeno, alquilo, arilo, cicloalquilo, CF3, OCF3, CN, -OR5, -NR5R6,-CH2OR5, -C(O2)R5, -C(O)NR5R6, -SR6, -S(O2)R7, -S(O2)NR5R6, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R6; R7 seselecciona entre el grupo que consiste en alquilo, arilo, heteroarilo, arilalquilo y heteroarilalquilo, en donde cada uno de dichos alquilo, heteroarilalquilo, arilo, heteroarilo y arilalquilo pueden estar no sustituidos o en forma opcional,sustituidos con una o más porciones iguales o diferentes, en donde cada porción se selecciona en forma independiente entre el grupo que consiste en halógeno, alquilo, arilo, cicloalquilo, -CF3, -OCF3, -CN, -OR5, -NR5R6, -CH2OR5, -C(O2)R5, -C(O)NR5R6, -SR6, -S(O2)R7, -S(O2)NR5R6, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R6; R8 se selecciona entre el grupo que consiste en R6, -C(O)NR5R6, -S(O2)NR5R6, -C(O)R7, -C(O2)R6, -S(O2)R7 y -(CH2)-arilo; m es 0 a 4; y n es 1 a 4.
ARP030103440A 2002-09-23 2003-09-22 Derivados de imidazol[1,2-a]pirazinas como inhibidores de quinasas dependientes de ciclinas AR041346A1 (es)

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US41290602P 2002-09-23 2002-09-23

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US (2) US7186740B2 (es)
EP (1) EP1542693A1 (es)
JP (1) JP2006503838A (es)
KR (1) KR20060010709A (es)
CN (1) CN1694706A (es)
AR (1) AR041346A1 (es)
AU (1) AU2003275031B2 (es)
CA (1) CA2499874A1 (es)
MX (1) MXPA05003119A (es)
NZ (1) NZ538686A (es)
TW (1) TW200412967A (es)
WO (1) WO2004026310A1 (es)
ZA (1) ZA200502380B (es)

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ZA200502380B (en) 2005-09-27
CN1694706A (zh) 2005-11-09
CA2499874A1 (en) 2004-04-01
US20070155751A1 (en) 2007-07-05
KR20060010709A (ko) 2006-02-02
EP1542693A1 (en) 2005-06-22
US7186740B2 (en) 2007-03-06
WO2004026310A8 (en) 2005-06-30
WO2004026310A1 (en) 2004-04-01
JP2006503838A (ja) 2006-02-02
US20040072835A1 (en) 2004-04-15
TW200412967A (en) 2004-08-01
MXPA05003119A (es) 2005-06-22
AU2003275031B2 (en) 2006-08-17
AU2003275031A1 (en) 2004-04-08
NZ538686A (en) 2008-01-31

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