ES2685568T3 - Inhibidores de la isoquinolinona o quinazolinona fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de la isoquinolinona o quinazolinona fosfatidilinositol 3-quinasa Download PDF

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Publication number
ES2685568T3
ES2685568T3 ES13818961T ES13818961T ES2685568T3 ES 2685568 T3 ES2685568 T3 ES 2685568T3 ES 13818961 T ES13818961 T ES 13818961T ES 13818961 T ES13818961 T ES 13818961T ES 2685568 T3 ES2685568 T3 ES 2685568T3
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haloalkyl
substituted
alkyl
unsubstituted
cyano
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Jerry Evarts
Leena Patel
Joshua Kaplan
Jennifer A. TREIBERG
Stephane Perreault
Gary Phillips
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Gilead Calistoga LLC
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Gilead Calistoga LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Abstract

Un compuesto que tiene la estructura de la Fórmula (J):**Fórmula** o una sal farmacéuticamente aceptable, o solvato del mismo, en donde: A es N o CH; n es 0, 1, 2, o 3; m es 0, 1, 2, o 3; cada R2 es independientemente halo, ciano, alquilo no sustituido o sustituido, haloalquilo no sustituido o sustituido, o alcoxi no sustituido o sustituido; y también (A) cada R1 es independientemente halo, ciano, alquilo no sustituido o sustituido, haloalquilo no sustituido o sustituido, alcoxi no sustituido o sustituido, hidroxi, cicloalquilo no sustituido o sustituido, SO2R1r, o C(O)NR1sR1t, en donde cada R1r, R1s y R1t es independientemente hidrógeno o alquilo no sustituido o sustituido; R3 es hidrógeno o alquilo no sustituido o sustituido; y R4 es ciano, CON(R4a)2, SO2-alquilo, halo, o haloalquilo, donde cada R4a es independientemente hidrógeno, o alquilo no sustituido o sustituido; o (B) cada R1 es independientemente halo, ciano, OR1x, C(>=O)OR1x, SO2R1x, o C(>=O)N(R1x)2, en donde R1x es independientemente hidrógeno, o alquilo no sustituido o sustituido; R3 es hidrógeno, alquilo no sustituido o sustituido, o haloalquilo no sustituido o sustituido; y R4 es ciano, CON(R4a)2, halo, o haloalquilo, donde cada R4a es independientemente hidrógeno, o alquilo no sustituido o sustituido; en donde para ambos compuestos de 1(A) y 1(B) "alquilo sustituido", "haloalquilo sustituido" y "alcoxi sustituido" se refiere a un grupo alquilo, haloalquilo o alcoxi, respectivamente, que tiene uno o más sustituyentes seleccionados del grupo que comprende hidroxilo, haloalquilo, alcoxi, cicloalquilo, heterocicloalquilo, arilo, heteroarilo, ciano, halo, carboxilo, y NR2, donde cada R es independientemente hidrógeno, alquilo, haloalquilo, alquilC(O)-, alquilOC(O)-, o H2NC(O)-; "cicloalquilo sustituido" se refiere a un grupo cicloalquilo que tiene uno o más sustituyentes seleccionados del grupo que comprende alquilo, haloalquilo, heterocicloalquilo, arilo, heteroarilo, alcoxi, ciano, halo, carboxilo, hidroxilo, y NR2, donde cada R es independientemente hidrógeno, alquilo, haloalquilo, alquilC(O)-, alquilOC(O)-, o H2NC(O)-; "heterocicloalquilo sustituido" se refiere a un grupo heterocicloalquilo que tiene uno o más sustituyentes seleccionados del grupo que comprende aalquilo, haloalquilo, cicloalquilo, arilo, heteroarilo, alcoxi, ciano, halo, carboxilo, hidroxilo, y NR2, donde cada R es independientemente hidrógeno, alquilo, haloalquilo, alquilC(O)-, alquilOC(O)-, o H2NC(O)-; "arilo sustituido" se refiere a un grupo arilo que tiene uno o más sustituyentes seleccionados del grupo que comprende halo, OR, NR2, C(O)NR'2, SO2NR'2, alquilo, haloalquilo, heterocicloalquilo, heteroarilo, alcoxi, amino, ciano, y carboxilo, donde cada R es independientemente hidrógeno, alquilo, haloalquilo, alquilC(O)-, alquilOC(O)-, o H2NC(O)- y cada R' es independientemente hidrógeno, alquilo, o haloalquilo; "heteroarilo sustituido" se refiere a un grupo heteroarilo que tiene uno o más sustituyentes seleccionados del grupo que comprende alquilo, haloalquilo, halo, NR2, OR, -C(O)OR, heterocicloalquilo, arilo, y ciano, donde cada R es independientemente hidrógeno, alquilo, haloalquilo, alquilC(O)-, alquilOC(O)-, o H2NC(O)-.
ES13818961T 2012-12-21 2013-12-20 Inhibidores de la isoquinolinona o quinazolinona fosfatidilinositol 3-quinasa Active ES2685568T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261745437P 2012-12-21 2012-12-21
PCT/US2013/077315 WO2014100767A1 (en) 2012-12-21 2013-12-20 Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors

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ES2685568T3 true ES2685568T3 (es) 2018-10-10

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US (2) US9029384B2 (es)
EP (1) EP2935246B1 (es)
JP (2) JP6207100B2 (es)
AR (1) AR094314A1 (es)
AU (1) AU2013364070B2 (es)
BR (1) BR112015014592A2 (es)
CA (1) CA2895785A1 (es)
ES (1) ES2685568T3 (es)
HK (1) HK1215024A1 (es)
NZ (1) NZ708870A (es)
PT (1) PT2935246T (es)
TW (1) TW201437203A (es)
UY (1) UY35243A (es)
WO (1) WO2014100767A1 (es)

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