AR060633A1 - Derivados de furo[3, 2-d]pirimidina, furo[2, 3-d]pirimidina, tieno[3, 2-d]pirimidina y tieno[2, 3-d]pirimidina, metodos para su preparacion, composiciones farmaceuticas y obtencion de las mismas, el uso de estos derivados en la fabricacion de medicamentos, kits y productos para el tratamiento de enf - Google Patents

Derivados de furo[3, 2-d]pirimidina, furo[2, 3-d]pirimidina, tieno[3, 2-d]pirimidina y tieno[2, 3-d]pirimidina, metodos para su preparacion, composiciones farmaceuticas y obtencion de las mismas, el uso de estos derivados en la fabricacion de medicamentos, kits y productos para el tratamiento de enf

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Publication number
AR060633A1
AR060633A1 ARP070101761A ARP070101761A AR060633A1 AR 060633 A1 AR060633 A1 AR 060633A1 AR P070101761 A ARP070101761 A AR P070101761A AR P070101761 A ARP070101761 A AR P070101761A AR 060633 A1 AR060633 A1 AR 060633A1
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AR
Argentina
Prior art keywords
group
alq
unsubstituted
alkyl
substituted
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ARP070101761A
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English (en)
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Genentech Inc
Piramed Ltd
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Publication of AR060633A1 publication Critical patent/AR060633A1/es

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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • 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

Abstract

Los compuestos de las Formulas 1a y 1b, y estereoisomeros, isomeros geométricos, tautomeros, solvatos, metabolitos y sales aceptables para uso farmacéutico de los mismos, son utiles para inhibir las lípido quinasas, que incluyen PI3K, y para el tratamiento de trastornos tales como cáncer mediado por lípido quinasas. Se revelan métodos para usar los compuestos de formula 1a y 1b para el diagnostico in vitro, in situ e in vitro, la prevencion o el tratamiento de tales trastornos en células de mamíferos o en afecciones patologicas asociadas, composiciones farmacéuticas que los contienen, preparacion de las mismas y su uso en la fabricacion de medicamentos, kits y productos para el tratamiento de enfermedades mediadas por PI3K. Reivindicacion 1: Un compuesto que es una pirimidina fusionada de formula (1a) o (1b): donde X es O o S; R1 es un grupo de formula (2) R2 es H, halo o alquilo C1-6; R4 es R5 forman, junto con el átomo de N al que están unidos, un grupo seleccionado de piperazina, piperidina, pirrolidina, oxazolidinona, diazepán y 2,5-diaza-biciclo[2,2,1]-heptano, grupo que está no sustituido o está sustituido con -[(alq)q-NR]r-S(O)2-(alq)q-Z o -C(O)-(alq)q-S(O)2Z, donde Z es R10 o -NR11R12, o con alquilo C1-6 no sustituido, hidroxil-alquilo C1-6, oxo (=O), -(alq)q-OR, -C(O)-C(R')2-N(R)2, -C(R)2-C(O)-N(R)2, -C(O)-(NR)q-(alq)q-OR, -C(O)-ciclilo, -C(O)R, -C(O)OR, -C(O)-Tet o -NR13R14; o uno de R4 y R5 es alquilo C1-6, -(alq)q-heterociclilo o - (alq)q-OR y el otro es un grupo piperazina, piperidina, pirrolidina, sulfonilpirano o -(alq)q-heterociclilo, donde dicha piperazina, piperidina, pirrolidina, sulfonilpirano o -heterociclilo está no sustituido o está sustituido con alquilo C1-6, - (alq)q-OR o -S(O)2R10; R es H o alquilo C1-6 que está no sustituido; cada R' es, independientemente, H o alquilo C1-6 que está no sustituido, o los dos grupos R' forman, junto con el átomo de C al que están unidos, un grupo ciclilo; R10 es H, ciclilo, alquilo C1-6 que está no sustituido o CF3; R11 y R12 se seleccionan cada uno en forma independiente de H, alquilo C1-6 que está no sustituido y -(alq)q-OR, o R11 y R12 juntos forman, con el átomo de N al que están unidos, un grupo heterocíclico saturado que contiene N de 5 o 6 miembros que contiene 0 o 1 heteroátomo adicional seleccionado de O, N y S; R13 y R14 se seleccionan cada uno en forma independiente de alquilo C1-6, -S(O)2R10 y -(alq)q-OR; Tet es un grupo tetrahidrofuranilo o tetrahidropiranilo, donde dicho grupo está no sustituido o está sustituido; -heterociclilo es un grupo heterociclílo saturado que contiene N de 5 o 6 miembros que contiene 0 o 1 heteroátomo adicional seleccionado de O, N y S; ciclilo es un grupo cicloalquilo C3-6; cada q es de modo independiente 0 o 1; R es 0 o 1; alq es alquileno C1-6; y R3 se selecciona de: (a) un grupo de la siguiente formula (3): donde B es un anillo fenilo que está no sustituido o está sustituido, y Z se selecciona de H, -OR, -SR, CH2OR, -CO2R, CF2OH, CH(CF3)OH, C(CF3)2OH, -(CH2)qOR, -(CH2)qNR2, -C(O)N(R)2, -NR2, -NRC(O)R, -S(O)mN(R)2, -OC(O)R, OC(O)N(R)2, -NRS(O)mR, -NRC(O)N(R)2, CN, halogeno y -NO2, donde cada R se selecciona de modo independiente de H, alquilo C1-6, cicloalquilo C3-10 y un grupo arilo o heteroarilo de 5 a 12 miembros, donde el grupo está sustituido o no sustituido, m es 1 o 2 y q es 0, 1 o 2; (b) un grupo heteroarilo que contiene 1, 2, 3 o 4 átomos de nitrogeno en el cilo y 0, 1 o 2 heteroátomos adicionales seleccionados de O y S, donde dicho grupo es monocíclico o bicíclico y que está no sustituido o sustituido; y (c) un grupo que comprende un anillo bencénico que está no sustituido o está sustituido y que está fusionado a un grupo heteroarilo como se definio antes; o una sal aceptable para uso farmacéutico del mismo; con las salvedades que: (i) cuando X en la formula (1a) es S, entonces R3 es diferente de un grupo indol o un 3-hidroxifenilo; (ii) cuando X en la formula (1b) es S, entonces R3 es diferente de un grupo indol; (iii) en la formula (1a) solamente, cuando X es S y R2 es H y R3 es indazol-4-ilo, entonces R4 y R5 no forman: (i) piperazina que está no sustituida o está sustituida con un grupo seleccionado de metilo, -S(O)2Me, -S(O)2 NMe2, -alq-OH, -alq-OMe, -S(O)2-alq-NMe2 y -S(O)2-alq-morfolino; o (ii) piperidina que está sustituida con un grupo seleccionado de -S(O)2 Me, -C(O)-NR-(alq)q-OR, -NMe-S(O)2-Me, metilo, piperidina y - NR13R14, donde uno de R13 y R14 es -(alq)q-OR.
ARP070101761A 2006-04-26 2007-04-24 Derivados de furo[3, 2-d]pirimidina, furo[2, 3-d]pirimidina, tieno[3, 2-d]pirimidina y tieno[2, 3-d]pirimidina, metodos para su preparacion, composiciones farmaceuticas y obtencion de las mismas, el uso de estos derivados en la fabricacion de medicamentos, kits y productos para el tratamiento de enf AR060633A1 (es)

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US (2) US8802670B2 (es)
EP (2) EP2402347A1 (es)
JP (1) JP5546240B2 (es)
KR (1) KR101422301B1 (es)
CN (1) CN101479274B (es)
AR (1) AR060633A1 (es)
AT (1) ATE532788T1 (es)
AU (1) AU2007243457B2 (es)
BR (1) BRPI0710943A2 (es)
CA (1) CA2650290C (es)
CL (1) CL2007001167A1 (es)
DK (1) DK2041139T3 (es)
ES (1) ES2377358T3 (es)
HK (1) HK1127356A1 (es)
IL (1) IL194762A (es)
MX (1) MX2008013584A (es)
NO (1) NO20084928L (es)
PL (1) PL2041139T3 (es)
PT (1) PT2041139E (es)
RU (1) RU2443706C2 (es)
TW (1) TWI498332B (es)
WO (1) WO2007127175A2 (es)
ZA (1) ZA200809546B (es)

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