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AR041347A1 - 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

Info

Publication number
AR041347A1
AR041347A1 ARP030103441A ARP030103441A AR041347A1 AR 041347 A1 AR041347 A1 AR 041347A1 AR P030103441 A ARP030103441 A AR P030103441A AR P030103441 A ARP030103441 A AR P030103441A AR 041347 A1 AR041347 A1 AR 041347A1
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AR
Argentina
Prior art keywords
nr5r6
aryl
alkyl
group
heteroaryl
Prior art date
Application number
ARP030103441A
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English (en)
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Schering Corp
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Publication of AR041347A1 publication Critical patent/AR041347A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (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 H, halógeno, arilo, heteroarilo, cicloalquilo, arilalquilo, heterociclilo,heterociclilalquilo, alquenilo, alquinilo, -C(O)R7,o como se muestra en los restos de fórmula (2), en donde cada uno de dichos arilo, heteroarilo, cicloalquilo, arilalquilo, alquenilo, heterociclilo y las porciones heterociclilo cuyas estructuras semuestran 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 entre el grupo que consisteen 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 se selecciona entre el grupo quecomprende halógeno, R9, alquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, heterociclilo, alquenilo, alquinilo, cicloalquilo, -CF3; -C(O)R7, alquilo sustituido con 1-6 grupos R9 iguales o diferentes, en donde cada R9 se selecciona en formaindependiente, como se muestra en los restos de fórmula (2) en donde cada uno de los dichos arilo, heteroarilo, arilalquilo y heterociclilo pueden estar no sustituidos o en forma opcional, independientemente 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, cicloalquilo, -CF3, -CN, -OCF3, -OR6, -C(O)R7, -NR5R6, -C(O2)R6, -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; R3 se selecciona entre el grupo que consiste en H, arilo, heteroarilo, heterociclilo, -(CHR5)n-arilo, -(CHR5)n-heteroarilo, -(CHR5)n-OR6, -S(O2)R6, -C(O)R6, -S(O2)NR5R6, -C(O)OR6, -C(O)NR5R6,cicloalquilo, -CH(arilo)2, -(CH2)m-NR8, -(CHR5)nCH(arilo)2,o como se muestra en los restos de fórmula (3), en donde cada uno de dichos arilo, heteroarilo y heterociclilo pueden estar sustituidos, o en forma opcional, sustituidos con una o másporciones iguales o diferentes, en donde cada porción se selecciona de manera 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; R5 es H o alquilo; R6 se selecciona entre el grupo que consiste en H, 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; R7 se selecciona entre el grupo que consiste en 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; R8 seselecciona 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; R9 se selecciona entre el grupo que comprende halógeno, -CN, -NR5R6, -C(O2)R6, -C(O)NR5R6, -OR6, -C(O)R7, -SR6, -S(O2)R7, -S(O2)NR5R6,-N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R6; m es 0 a 4; n es 1 a 4; y p es 0 a 3.
ARP030103441A 2002-09-23 2003-09-22 Derivados de imidazol[1,2-a]pirazinas como inhibidores de quinasas dependientes de ciclinas AR041347A1 (es)

Applications Claiming Priority (1)

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US41299702P 2002-09-23 2002-09-23

Publications (1)

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AR041347A1 true AR041347A1 (es) 2005-05-11

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Country Status (19)

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US (2) US6919341B2 (es)
EP (1) EP1543008B1 (es)
JP (1) JP4799864B2 (es)
KR (1) KR20050057520A (es)
CN (1) CN1694886A (es)
AR (1) AR041347A1 (es)
AT (1) ATE377600T1 (es)
AU (1) AU2003272476B2 (es)
CA (1) CA2499756C (es)
DE (1) DE60317353T2 (es)
ES (1) ES2293015T3 (es)
HK (1) HK1072056A1 (es)
MX (1) MXPA05003120A (es)
MY (1) MY134589A (es)
NZ (2) NZ563374A (es)
PE (1) PE20050081A1 (es)
TW (1) TW200413378A (es)
WO (1) WO2004026877A1 (es)
ZA (1) ZA200502375B (es)

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