AR060632A1 - Compuestos inhibidores de fosfoinositida 3- quinasa y metodos de uso - Google Patents

Compuestos inhibidores de fosfoinositida 3- quinasa y metodos de uso

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Publication number
AR060632A1
AR060632A1 ARP070101760A ARP070101760A AR060632A1 AR 060632 A1 AR060632 A1 AR 060632A1 AR P070101760 A ARP070101760 A AR P070101760A AR P070101760 A ARP070101760 A AR P070101760A AR 060632 A1 AR060632 A1 AR 060632A1
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AR
Argentina
Prior art keywords
cr14r15
nr10r11
nr12c
heterocyclyl
heteroaryl
Prior art date
Application number
ARP070101760A
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English (en)
Original Assignee
Genentech Inc
Piramed Ltd
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38561741&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR060632(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc, Piramed Ltd filed Critical Genentech Inc
Publication of AR060632A1 publication Critical patent/AR060632A1/es

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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—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
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Los compuestos de formulas (1) y (2), incluyendo estereoisomeros, isomeros geométricos, tautomeros, solvatos, metabolitos y sales farmacéuticamente aceptables de los mismos, son utiles para inhibir lípido quinasas incluyendo PI3K, y para tratar trastornos tales como cáncer causados por lípido quinasas. Se dan a conocer métodos para usar compuestos de formula (1) y (2) para el diagnostico, la prevencion o el tratamiento in vitro, in situ, e in vivo de tales trastornos en células de mamíferos, o estados patologicos asociados. Reivindicacion 1: Un compuesto seleccionado entre la formula (1) y la formula (2) y estereoisomeros, isomeros geométricos, tautomeros, solvatos, metabolitos, y sales farmacéuticamente aceptables del mismo, donde: X es O o S; R1 se selecciona entre H, F, CI, Br, I, CN, -CR14R15-NR16R17, -CR14R15-NHR10, -(CR14R15)tNR10R11, -C(R14R15)nNR12C(=Y)R10, -CR14R15)nNR12S(O)2R10, -(CR14R15)mOR10, -(CR14R15)mS(O)2R10, -(CR14R15)nS(O)2NR10R11, - C(OR10)R11R14, -C(R14)=CR18R19, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -C(=Y)NR12OR10, C(=O)NR12S(O)2R10, -C(=O)NR12(CR14R15)mNR10R11, -NO2, -NHR12, -NR12C(=Y)R11,-NR12C(=Y)OR11, -NR12C(=Y)NR10R11, -NR12S(O)2NR10R11, -S(O)2R10, -S(O)2NR10R11, - SC(=Y)R10, -SC(=Y)OR10, alquilo C2-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, o heteroarilo C1-20; R2 se selecciona entre H, F, CI, Br, I, CN, CF3, -NO2, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, - (CR14R15)mNR10R11, -(CR14R15)nOR10, -(CR14R15)t-NR12C(=O)(CR14R15)NR10R11, -NR12C(=Y)R10, -NR12C(=Y)OR10, -NR12C(=Y)NR10R11, -NR12SO2R10, OR10, -OC(=Y)R10, -OC(=Y)0R10, -OC(=Y)NR10R11, -OS(O)2(OR10), -OP(=Y)(OR10)(OR11), -OP(OR10)(OR11), SR10, - S(O)R10, -S(O)2R10, -S(O)2NR10R11, -S(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, -SC(=Y)OR10, -SC(=Y)NR10R11, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, y heteroarilo C1-20; R3 es heterociclilo C4- 20 bicíclico fusionado o heteroarilo C1-20 bicíclico fusionado; R10, R11 y R12 son de manera independiente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20, o heteroarilo C1-20, o R10 y R11 junto con el nitrogeno al cual están ligados forman opcionalmente un anillo heterocíclico C3-20 saturado, parcialmente insaturado o totalmente insaturado que contiene opcionalmente uno o más átomos anulares adicionales seleccionados entre N, O o S, donde dicho anillo heterocíclico está opcionalmente sustituido con uno o más grupos seleccionados de manera independiente entre oxo, (CH2)mOR10, NR10R11, CF3, F, CI, Br, I, SO2R10, C(=O)R10, NR12C(=Y)R11, NR12S(O)2R11, C(=Y)NR10R11, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, heterociclilo C2-20, arilo C6-20 y heteroarilo C1-20; R14 y R15 se seleccionan de manera independiente entre H, alquilo C1-12, o -(CH2)n-arilo, o R14 y R15 junto con los átomos a los cuales están ligados forman un anillo carbocíclico C3-12 saturado o parcialmente insaturado, R16 y R17 son de manera independiente H, alquilo C1-12, alquenilo C2-8, alquinilo C2-8, carbociclilo C3-12, o arilo C6-20, R18 y R19 junto con el carbono al cual están ligados forman un anillo heterocíclico C3-20, donde dicho alquilo, alquenilo, alquinilo, carbociclilo, heterociclilo, arilo, heteroarilo, heterociclilo C4-20 bicíclico fusionado, y heteroarilo C1-20 bicíclico fusionado están opcionalmente sustituidos con uno o más grupos seleccionados de manera independiente entre F, CI, Br, I, CN, CF3, -NO2, oxo, R10, -C(=Y)R10, -C(=Y)OR10, -C(=Y)NR10R11, -(CR14R15)nNR10R11, -(CR14R15)nOR10, -NR10R11, -NR12C(=Y)R10, -NR12C(=Y)OR11, - NR12C(=Y)NR10R11, -NR12SO2R10, =NR12, OR10, -OC(=Y)R10, -OC(=Y)OR10, -OC(=Y)NR10R11, -OS(O)2(OR10), -OP(=Y)(OR10)(OR11), -OP(OR10)(OR11), SR10, -S(O)R10, -S(O)2R10, -S(O)2NR10R11, -S(O)(OR10), -S(O)2(OR10), -SC(=Y)R10, -SC(=Y)OR10, -SC(=Y)NR10R11, alquilo C1-12 opcionalmente sustituido, alquenilo C2-8 opcionalmente sustituido, alquinilo C2-8 opcionalmente sustituido, carbociclilo C3-12 opcionalmente sustituido, heterociclilo C2-20 opcionalmente sustituido, arilo C6-20 opcionalmente sustituido, heteroarilo C1-20 opcionalmente sustituido, -(CR14R15)t-NR12C(=O)(CR14R15)NR10R11, y (CR4R5)t-R10R11; Y es O, S, o NR12; m es 0, 1, 2, 3, 4, 5 o 6; n es 1, 2, 3, 4, 5, o 6; y t es 2, 3, 4, 5 o 6.
ARP070101760A 2006-04-26 2007-04-24 Compuestos inhibidores de fosfoinositida 3- quinasa y metodos de uso AR060632A1 (es)

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US (2) US7846929B2 (es)
EP (1) EP2046799B1 (es)
JP (1) JP5291616B2 (es)
KR (1) KR101402474B1 (es)
CN (1) CN101511840A (es)
AR (1) AR060632A1 (es)
AU (1) AU2007243466B2 (es)
BR (1) BRPI0710908A2 (es)
CA (1) CA2650295C (es)
CL (1) CL2007001166A1 (es)
IL (1) IL194761A0 (es)
MX (1) MX2008013583A (es)
NO (1) NO20084927L (es)
RU (1) RU2437888C2 (es)
TW (1) TW200801012A (es)
WO (1) WO2007127183A1 (es)
ZA (1) ZA200810023B (es)

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