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AR085958A1 - 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer - Google Patents

8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer

Info

Publication number
AR085958A1
AR085958A1 ARP120101217A ARP120101217A AR085958A1 AR 085958 A1 AR085958 A1 AR 085958A1 AR P120101217 A ARP120101217 A AR P120101217A AR P120101217 A ARP120101217 A AR P120101217A AR 085958 A1 AR085958 A1 AR 085958A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
nr10c
heteroaryl
heterocycloalkyl
Prior art date
Application number
ARP120101217A
Other languages
English (en)
Inventor
David Campbell
Sergio G Duron
Original Assignee
Afraxis Inc
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 Afraxis Inc filed Critical Afraxis Inc
Publication of AR085958A1 publication Critical patent/AR085958A1/es

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    • C—CHEMISTRY; METALLURGY
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    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Psychiatry (AREA)
  • Physiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Dispersion Chemistry (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (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

Inhibidores de PAK y métodos para utilizar inhibidores de PAK para el tratamiento de trastornos del CNS tales como trastornos neuropsiquiátricos o neurofibromatosis. También se describen aquí métodos para utilizar los inhibidores de PAK en el tratamiento de cáncer.Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de la fórmula (1) o un N-óxido o una sal farmacéuticamente aceptable del mismo, donde: R7 es un resto de formula (2), donde el anillo T es un anillo arilo o heteroarilo; R3 es un cicloalquilo sustituido o no sustituido, un heteroarilo sustituido o no sustituido unido al anillo T a través de un átomo de carbono de R3, o un heterocicloalquilo sustituido o no sustituido unido al anillo T a través de un átomo de carbono de R3; Q es un alquilo sustituido o no sustituido, un heteroalquilo sustituido o no sustituido, un heterocicloalquilo sustituido o no sustituido, un cicloalquilo sustituido o no sustituido, un cicloalquilalquilo sustituido o no sustituido, un heterocicloalquilalquilo sustituido o no sustituido, un arilo sustituido o no sustituido, un arilalquilo sustituido o no sustituido, un heteroarilo sustituido o no sustituido, o un heteroarilalquilo sustituido o no sustituido; cada R4 es en forma independiente halógeno, -CN, -NO2, -OH, -OCF3, -OCH2F, -OCF2H, -CF3, -SR8, -NR10S(=O)2R9, -S(=O)2N(R10)2, -C(=O)R8, -OC(=O)R9, -CO2R10, -N(R10)2, -C(=O)N(R10)2, -NR10C(=O)R10, -NR10C(=O)OR10, -NR10C(O)N(R10)2, un alquilo sustituido o no sustituido, un alcoxi sustituido o no sustituido, un heteroalquilo sustituido o no sustituido, un cicloalquilo sustituido o no sustituido, o un heterocicloalquilo sustituido o no sustituido; R8 es H o R9; R9 es un alquilo sustituido o no sustituido, un cicloalquilo sustituido o no sustituido, un heterocicloalquilo sustituido o no sustituido, un arilo sustituido o no sustituido, o un heteroarilo sustituido o no sustituido; cada R10 es en forma independiente H, un alquilo sustituido o no sustituido, un cicloalquilo sustituido o no sustituido, un heterocicloalquilo sustituido o no sustituido, un arilo sustituido o no sustituido, o un heteroarilo sustituido o no sustituido; o dos R10, junto con los átomos a los que se encuentran unidos forman un heterociclo; el anillo B es arilo o heteroarilo; cada R5 es en forma independiente halógeno, -CN, -NO2, -OH, -SR8, -S(=O)R9, -S(=O)2R9, NR10S(=O)2R9, -S(=O)2N(R10)2, -C(=O)R8, -OC(=O)R9, -CO2R10, -N(R10)2, -C(=O)N(R10)2, -NR10C(=O)R10, -NR10C(=O)OR10, -NR10C(=O)N(R10)2, -OR10, un alquilo sustituido o no sustituido, un alcoxi sustituido o no sustituido, un heteroalquilo sustituido o no sustituido, un cicloalquilo sustituido o no sustituido, o un heterocicloalquilo sustituido o no sustituido; r es entre 0 y 8; y s es entre 0 y 4.
ARP120101217A 2011-04-08 2012-04-09 8-etil-6-(aril)pirido[2,3-d]pirimidin-7(8h)-onas para el tratamiento de trastornos del cns y cancer AR085958A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161473683P 2011-04-08 2011-04-08

Publications (1)

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AR085958A1 true AR085958A1 (es) 2013-11-06

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Country Status (15)

Country Link
US (1) US20140163026A1 (es)
EP (1) EP2694504A4 (es)
JP (1) JP2014513079A (es)
KR (1) KR20140040715A (es)
CN (1) CN103596951A (es)
AR (1) AR085958A1 (es)
AU (1) AU2012313399A1 (es)
BR (1) BR112013025798A2 (es)
CA (1) CA2832309A1 (es)
IL (1) IL228681A0 (es)
MX (1) MX2013011518A (es)
RU (1) RU2013149800A (es)
TW (1) TW201300385A (es)
WO (1) WO2013043232A2 (es)
ZA (1) ZA201307296B (es)

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EP2694504A4 (en) 2014-08-27
AU2012313399A1 (en) 2013-05-09
ZA201307296B (en) 2014-12-23
RU2013149800A (ru) 2015-05-20
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CA2832309A1 (en) 2013-03-28
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JP2014513079A (ja) 2014-05-29
IL228681A0 (en) 2013-12-31
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