AR097862A1 - Inhibidores de tirosina quinasa de bruton - Google Patents

Inhibidores de tirosina quinasa de bruton

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Publication number
AR097862A1
AR097862A1 ARP140103633A ARP140103633A AR097862A1 AR 097862 A1 AR097862 A1 AR 097862A1 AR P140103633 A ARP140103633 A AR P140103633A AR P140103633 A ARP140103633 A AR P140103633A AR 097862 A1 AR097862 A1 AR 097862A1
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Argentina
Prior art keywords
substituted
unsubstituted
alkyl
heteroalkyl
pharmaceutically acceptable
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ARP140103633A
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English (en)
Inventor
Chen Wei
Wang Longcheng
J Jia Zhaozhong
J Loury David
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Pharmacyclics Inc
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Application filed by Pharmacyclics Inc filed Critical Pharmacyclics Inc
Publication of AR097862A1 publication Critical patent/AR097862A1/es

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    • 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
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    • 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
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    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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    • A61K9/0031—Rectum, anus
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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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    • A61K9/0012—Galenical forms characterised by the site of application
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    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
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    • A—HUMAN NECESSITIES
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • 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
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Dermatology (AREA)
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  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuestos que forman enlaces covalentes con la tirosina quinasa de Bruton (Btk). También se describen inhibidores irreversibles de Btk, inhibidores reversibles de Btk y composiciones farmacéuticas que incluyen los compuestos. Además se describen métodos para utilizar los inhibidores Btk, solos o en combinación con otros agentes terapéuticos, para el tratamiento de enfermedades o condiciones autoinmunes, enfermedades o condiciones heteroinmunes, cáncer, incluido el linfoma, y enfermedades o condiciones infamatorias. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque tiene la estructura de fórmula (1), donde: L¹ es -N(R²)C(O)- o -C(O)N(R²)-; R¹ es C₆₋₁₂ arilo o C₃₋₁₂ heteroarilo, donde C₆₋₁₂ arilo y C₃₋₁₂ heteroarilo están opcionalmente sustituidos con al menos un R³; R² es H o C₁₋₄ alquilo; R³ es halógeno, -CF₃, -CN, -NO₂, -OR⁶, -N(R⁶)(R⁷), C₁₋₆ alquilo sustituido o no sustituido, C₃₋₆ cicloalquilo sustituido o no sustituido, o C₁₋₆ heteroalquilo sustituido o no sustituido; R⁴ es H, C₁₋₆ alquilo sustituido o no sustituido, C₁₋₆ heteroalquilo sustituido o no sustituido, C₃₋₈ cicloalquilo sustituido o no sustituido, o C₂₋₉ heterocicloalquilo sustituido o no sustituido; R⁵ es C₃₋₈ cicloalquilo sustituido o no sustituido, o C₂₋₉ heterocicloalquilo sustituido o no sustituido; o R⁴ y R⁵ junto con el átomo de nitrógeno al cual están unidos forman un C₂₋₉ heterocicloalquilo; R⁶ es H, C₁₋₆ alquilo sustituido o no sustituido, o C₁₋₆ heteroalquilo sustituido o no sustituido; R⁷ es H, C₁₋₆ alquilo sustituido o no sustituido, C₁₋₆ heteroalquilo sustituido o no sustituido; R¹⁰ es halógeno, C₁₋₆ alquilo sustituido o no sustituido, o C₁₋₆ alcoxi sustituido o no sustituido; m es 1 ó 2; n es 0 ó 1; y p es 0, 1, ó 2; o una sal farmacéuticamente aceptable, solvato farmacéuticamente aceptable, o prodroga farmacéuticamente aceptable del mismo.
ARP140103633A 2013-09-30 2014-09-30 Inhibidores de tirosina quinasa de bruton AR097862A1 (es)

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US201361884888P 2013-09-30 2013-09-30

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AR097862A1 true AR097862A1 (es) 2016-04-20

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ARP140103633A AR097862A1 (es) 2013-09-30 2014-09-30 Inhibidores de tirosina quinasa de bruton

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US (2) US9624224B2 (es)
EP (1) EP3052486A1 (es)
JP (1) JP2016531941A (es)
KR (1) KR20160062103A (es)
CN (1) CN105764896A (es)
AR (1) AR097862A1 (es)
AU (1) AU2014324532A1 (es)
BR (1) BR112016006978A2 (es)
CA (1) CA2925124A1 (es)
CR (1) CR20160203A (es)
DO (1) DOP2016000071A (es)
EA (1) EA201690618A1 (es)
IL (1) IL244492A0 (es)
MA (1) MA38961A1 (es)
PE (1) PE20160560A1 (es)
PH (1) PH12016500575A1 (es)
SG (1) SG11201602421VA (es)
TN (1) TN2016000094A1 (es)
TW (1) TW201546061A (es)
WO (1) WO2015048689A1 (es)

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