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AR097024A1 - Derivados sustituidos de quinazolin-4-ona - Google Patents

Derivados sustituidos de quinazolin-4-ona

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Publication number
AR097024A1
AR097024A1 ARP140102728A ARP140102728A AR097024A1 AR 097024 A1 AR097024 A1 AR 097024A1 AR P140102728 A ARP140102728 A AR P140102728A AR P140102728 A ARP140102728 A AR P140102728A AR 097024 A1 AR097024 A1 AR 097024A1
Authority
AR
Argentina
Prior art keywords
substituted
fluorine
unsubstituted
methyl
independently selected
Prior art date
Application number
ARP140102728A
Other languages
English (en)
Inventor
Jacquier Sbastien
Lehmann Hansjoerg
Moebitz Henrik
Stojanovic Aleksandar
Soldermann Nicolas
Hurth Konstanze
Hintermann Samuel
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR097024A1 publication Critical patent/AR097024A1/es

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    • 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
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P19/00—Drugs for skeletal disorders
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
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    • A61P7/06—Antianaemics
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms

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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente se refiere a compuestos de quinazolin-4-ona. Tales compuestos son adecuados para el tratamiento de un trastorno o enfermedad mediada por la actividad de las quinasas PI3 clase I, con aplicación a una amplia gama de trastornos, en particular trastornos autoinmunes, enfermedades de vías respiratorias y etc.. Además se divulgan procesos de preparación y sus intermediarios. Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo en donde R¹ se selecciona a partir de fenilo, que es sustituido o no sustituido por 1, 2 ó 3 sustituyentes independientemente seleccionados a partir de metilo, etilo, difluorometilo, metoxilo, difluorometoxilo, ciclopropilo, cloro o flúor; piridilo, que es sustituido o no sustituido por 1, 2 ó 3 sustituyentes independientemente seleccionados a partir de metilo, etilo, difluorometilo, metoxilo, difluorometoxilo, ciclopropilo, cloro o flúor; 1-metilpirazol-5-ilo; 2-metiltiofen-5-ilo; cicloalquilo-C₃₋₆, que es sustituido o no sustituido en la posición 1 por metilo; tetrahidropiran-4-ilo; piperidin-1-ilo; morfolin-4-ilo; pirolidin-3-ilo, que es sustituido o no sustituido en la posición 1 por un sustituyente que se selecciona a partir de metoxicarbonilo, metilsulfonilo, metilo o metilcarbonilo; o dimetilamina; R² se selecciona a partir de heteroarilo-C₄₋₇, que contiene un átomo de nitrógeno y 0, 1, 2 ó 3 heteroátomos adicionales independientemente seleccionados a partir de N, O ó S, en donde heteroarilo-C₄₋₇ es sustituido o no sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de alquilo-C₁₋₄, fluoroalquilo-C₁₋₄, hidroxi-alquilo-C₁₋₄, hidroxi-fluoroalquilo-C₁₋₄, alcoxilo-C₁₋₄, fluoroalcoxilo-C₁₋₄, cicloalquilo-C₃₋₆, que es sustituido o no sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de metilo, o flúor, heterocicloalquilo-C₃₋₆, que es sustituido o no sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de metilo, o flúor, ciano, flúor amino, alquilamino-C₁₋₄, o dialquilamino-C₁₋₄; o alquinilo-C₂₋₆, que es sustituido o no sustituido por 1 - 2 sustituyentes independientemente seleccionados a partir de fluoroalquilo-C₁₋₄, cicloalquilo-C₃₋₆, que es sustituido o no sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de metilo, o flúor, heterocicloalquilo-C₃₋₆, que es sustituido o no sustituido por 1 - 3 sustituyentes independientemente seleccionados a partir de metilo, o flúor, alcoxilo-C₁₋₄, fluoroalcoxilo-C₁₋₄, hidroxilo, ciano, flúor amino, alquilamino-C₁₋₄, o dialquilamino-C₁₋₄; R⁵ y R⁶ son independientemente seleccionados a partir de hidrógeno, deuterio o flúor; -L-R³ se selecciona a partir del grupo de fórmulas (2), en donde R⁷ se selecciona a partir de metoxilo, difluorometoxilo, trifluorometoxilo, hidroxilo, flúor o metilsulfonilamina; y R³ se selecciona a partir del grupo de fórmulas (3), en donde R⁴ se selecciona a partir de hidrógeno o amino, R⁸ se selecciona a partir de hidrógeno, metilo, fluorometilo, difluorometilo, trideuterometilo o amino, y X se selecciona a partir de NH, NMe o S.
ARP140102728A 2013-07-24 2014-07-23 Derivados sustituidos de quinazolin-4-ona AR097024A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13177827 2013-07-24

Publications (1)

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AR097024A1 true AR097024A1 (es) 2016-02-10

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US (1) US9840498B2 (es)
EP (1) EP3024827B1 (es)
JP (1) JP6437544B2 (es)
KR (1) KR20160033697A (es)
CN (1) CN105452235B (es)
AR (1) AR097024A1 (es)
AU (1) AU2014295538B2 (es)
CA (1) CA2917433A1 (es)
EA (1) EA031430B1 (es)
ES (1) ES2803513T3 (es)
MX (1) MX368066B (es)
PL (1) PL3024827T3 (es)
PT (1) PT3024827T (es)
TW (1) TW201534598A (es)
UY (1) UY35675A (es)
WO (1) WO2015010641A1 (es)

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