AR047543A1 - Pirazolopirimidinas como inhibidores de proteinquinasas. composiciones farmaceuticas - Google Patents

Pirazolopirimidinas como inhibidores de proteinquinasas. composiciones farmaceuticas

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Publication number
AR047543A1
AR047543A1 ARP050100483A ARP050100483A AR047543A1 AR 047543 A1 AR047543 A1 AR 047543A1 AR P050100483 A ARP050100483 A AR P050100483A AR P050100483 A ARP050100483 A AR P050100483A AR 047543 A1 AR047543 A1 AR 047543A1
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AR
Argentina
Prior art keywords
aryl
alkyl
heteroaryl
nr5r10
cycloalkyl
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ARP050100483A
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English (en)
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Schering Corp
Pharmacopeia Drug Discovery
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Application filed by Schering Corp, Pharmacopeia Drug Discovery filed Critical Schering Corp
Publication of AR047543A1 publication Critical patent/AR047543A1/es

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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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (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

Los compuestos pertenecen a la categoría de los derivados de pirazolopirimidinas utilizados como inhibidores de proteinquinasas ciclina dependientes. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto representado por la formula estructural (1), o una sal aceptable para uso farmacéutico o solvato de dicho compuesto, en el cual: R es H, alquilo, alquenilo, alquinilo, arilalquilo, arilalquenilo, cicloalquilo, cicloalquilalquilo, alquenilalquilo, alquinilalquilo, heterociclilo, heterociclilalquilo, heteroarilalquilo (incluyendo el N-oxido de dicho heteroarilo), -(CHR5)n-arilo-, -(CHR5)n-heteroarilo, o es un resto del grupo de formula (2) a (7), donde cada uno de dichos alquilo, alquenilo, alquinilo, arilo, cicloalquilo, heterociclilo y heteroarilo puede ser no sustituido o sustituido opcionalmente con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halogeno, alquilo, arilo, cicloalquilo, heterociclilalquilo, CF3, OCF3, CN, -OR5, -NR5R10, -C(R4R5)p-R9, -N(R5)Boc, -C(R4R5)pOR5, -C(O2)R5, -C(O)R5, -C(O)NR5R10, -SO3H, -SR10, -S(O2)R7, -S(O2)NR5R10, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R10; R2 se selecciona del grupo que consiste en R9, alquilo, alquenilo, alquinilo, CF3, heterociclilo, heterociclilalquilo, halogeno, haloalquilo, arilo, arilalquilo, heteroarilalquilo, alquinilalquilo, cicloalquilo, heteroarilo, alquilo sustituido con 1-6 grupos R9 que pueden ser iguales o diferentes y se seleccionan independientemente del listado de R9 que se muestra a continuacion, arilo sustituido con 1-3 grupos arilo o heteroarilo que pueden ser iguales o diferentes y se seleccionan independientemente de grupos fenilo, piridilo, tiofenilo, furanilo y tiazolo, arilo fusionado con un grupo arilo o heteroarilo, heteroarilo sustituido con 1-3 grupos arilo o heteroarilo que pueden ser iguales o diferentes y se seleccionan independientemente de grupos fenilo, piridilo, tiofenilo, furanilo y tiazolo, heteroarilo fusionado con un grupo arilo o heteroarilo, o es un resto de grupo de formula (8), donde uno o más de los arilo y/o uno o más de los heteroarilo en las definiciones mencionadas anteriormente para R2 puede ser no sustituido o sustituido opcionalmente con una o más restos que pueden ser iguales o diferentes seleccionándose cada resto independientemente del grupo que consiste en halogeno, -CN, -OR5, -SR5, -S(O2)R6, -S(O2)NR5R6, -NR5R6, -C(O)NR5R6, CF3, alquilo, arilo, y OCF3; R3 se selecciona del grupo que consiste en H, halogeno, -NR5R6, -OR6, -SR6, -C(O)N(R5R6), alquilo, alquinilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo, o es un resto de grupo de formula (9), donde cada uno de dichos alquilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo para R3 y las restos heterociclilo cuyas estructuras se muestran en forma inmediatamente anterior para R3 puede ser no sustituido o sustituido independientemente de manera opcional con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halogeno, alquilo, arilo, cicloalquilo, CF3, CN, -OCF3,-(CR4R5)pOR5, -OR5, -NR5R6, -(CR4R5)pNR5R6, -C(O2)R5, -C(O)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 salvedad de que ningun carbono adyacente al átomo de nitrogeno en un anillo heterociclilo posea un resto -OR5; R4 es H, halo o alquilo; R5 es H, alquilo, arilo o cicloalquilo; R6 se selecciona del grupo que consiste en H, alquilo, alquenilo, arilo, arilalquilo, arilalquenilo, cicloalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo, donde cada uno de dichos alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo puede ser no sustituido o sustituido opcionalmente con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halogeno, alquilo, arilo, cicloalquilo, heterociclilalquilo, CF3, OCF3, CN, -OR5, -NR5R10, -C(R4R5)p-R9, - N(R5)Boc, -(CR4R5)pOR5, -C(O2)R5, -C(O)R5, -C(O)NR5R10, -SO3H, -SR10, -S(O2)R7, -S(O2)NR5R10, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R10; R10 se selecciona del grupo que consiste en H, alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo, donde cada uno de dichos alquilo, arilo, arilalquilo, cicloalquilo, heterociclilo, heterociclilalquilo, heteroarilo y heteroarilalquilo puede ser no sustituido o sustituido opcionalmente con uno o más restos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halogeno, alquilo, arilo, cicloalquilo, heterociclilalquilo, CF3, OCF3, CN, -OR5, -NR4R5, -C(R4R5)p-R9, -N(R5)Boc, - (CR4R5)pOR5, -C(O2)R5, -C(O)NR4R5, -C(O)R5, -SO3H, -SR5, -S(O2)R7, -S(O2)NR4R5, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR4R5; u opcionalmente (i) R5 y R10 en el resto -NR5R10, o (ii) R5 y R6 en el resto -NR5R6, se pueden unir para formar un resto cicloalquilo o heterociclilo, siendo cada uno de dichos restos cicloalquilo o heterociclilo no sustituidos o sustituidos opcionalmente de manera independiente con uno o más grupos R9; R7 se selecciona del grupo que consiste en alquilo, cicloalquilo, arilo, arilalquenilo, heteroarilo, arilalquilo, heteroarilalquilo, heteroarilalquenilo y heterociclilo, donde cada uno de dichos alquilo, cicloalquilo, heteroarilalquilo, arilo, heteroarilo, y arilalquilo pueden ser no sustituido o sustituido independientemente de manera opcional con uno o más retos que pueden ser iguales o diferentes, seleccionándose cada resto independientemente del grupo que consiste en halogeno, alquilo, arilo, cicloalquilo, CF3, OCF3, CN, -OR5, -NR5R10, -CH2OR5, - C(O2)R5, -C(O)NR5R10, -C(O)R5, -SR10, -S(O2)R10, -S(O2)NR5R10, -N(R5)S(O2)R10, -N(R5)C(O)R10 y -N(R5)C(O)NR5R10; R8 se selecciona del grupo que consiste en R6, -OR6, -C(O)NR5R10, -S(O2)NR5R10, -C(O)R7, -C(=N-CN)-NH2, -C(=NH)-NHR5, heterociclilo, y - S(O2)R7; R9 se selecciona del grupo que consiste en halogeno, -CN, -NR5R10, -C(O2)R6, -C(O)NR5R10, -OR6, -SR6, -S(O2)R7, -S(O2)NR5R10, -N(R5)S(O2)R7, -N(R5)C(O)R7 y -N(R5)C(O)NR5R10; m es 0 a 4; n es 1 a 4; y p es 1 a 4, con la salvedad de que cuando R2 es fenilo, R3 no sea alquilo, alquinilo o halogeno, y que cuando R2 es arilo, R no sea la formula (3), con la salvedad adicional de que cuando R es arilalquilo, entonces cualquier sustituyente heteroarilo en el arilo de dicho arilalquilo contiene al menos tres heteroátomos.
ARP050100483A 2004-02-11 2005-02-10 Pirazolopirimidinas como inhibidores de proteinquinasas. composiciones farmaceuticas AR047543A1 (es)

Applications Claiming Priority (1)

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US10/776,988 US7119200B2 (en) 2002-09-04 2004-02-11 Pyrazolopyrimidines as cyclin dependent kinase inhibitors

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AR047543A1 true AR047543A1 (es) 2006-01-25

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US (2) US7119200B2 (es)
EP (1) EP1720882B1 (es)
JP (2) JP4845743B2 (es)
KR (1) KR101196498B1 (es)
CN (1) CN1946725B (es)
AR (1) AR047543A1 (es)
AT (1) ATE494287T1 (es)
AU (1) AU2005212409C1 (es)
BR (1) BRPI0507644B8 (es)
CA (1) CA2555345C (es)
CY (1) CY1112400T1 (es)
DE (1) DE602005025733D1 (es)
DK (1) DK1720882T3 (es)
ES (1) ES2359410T3 (es)
HK (1) HK1090926A1 (es)
HR (1) HRP20110245T1 (es)
IL (1) IL177283A (es)
MY (1) MY149044A (es)
NO (1) NO337520B1 (es)
NZ (1) NZ590480A (es)
PE (1) PE20050774A1 (es)
PL (1) PL1720882T3 (es)
RU (1) RU2414472C9 (es)
SI (1) SI1720882T1 (es)
TW (1) TWI393566B (es)
WO (1) WO2005077954A2 (es)
ZA (1) ZA200606573B (es)

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