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1. AR111281 - COMPUESTOS DE PIRIMIDINIL-PIRIDILOXI-NAFTIL Y MÉTODOS PARA TRATAR ENFERMEDADES Y TRASTORNOS RELACIONADOS CON IRE1

Office Argentina
Application Number P180100604
Application Date 15.03.2018
Publication Number 111281
Publication Date 26.06.2019
Publication Kind A1
IPC
C07D 401/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
14containing three or more hetero rings
C07D 417/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic 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 C07D415/196
14containing three or more hetero rings
C07D 405/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
C07D 413/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
CPC
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 401/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
14containing three or more hetero rings
C07D 405/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
Applicants GENENTECH, INC.
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Inventors
Priority Data PCT/CN2017/077059 17.03.2017 WO
Title
(ES) COMPUESTOS DE PIRIMIDINIL-PIRIDILOXI-NAFTIL Y MÉTODOS PARA TRATAR ENFERMEDADES Y TRASTORNOS RELACIONADOS CON IRE1
Abstract
(ES)
Se describen en la presente compuestos de pirimidinil-piridiloxi-naftil con actividad o función de modulación de la enzima requirente de inositol 1 (IRE1) o estereoisómeros, tautómeros o sales farmacéuticamente aceptables de estos, y con los sustituyentes y las características estructurales que se describen en la presente. También se describen composiciones farmacéuticas y medicamentos que incluyen los compuestos de fórmula (1), así como métodos para utilizar dichos moduladores de IRE1, solos o combinados con otros agentes terapéuticos, para tratar enfermedades o afecciones que están mediadas o que dependen de los receptores de estrógeno. Reivindicación 1: Un compuesto seleccionado de la fórmula (1), y estereoisómeros, tautómeros o sales farmacéuticamente aceptables de estos, en donde: R¹ se selecciona de cicloalquilo C₃₋₁₂, heterociclilo C₃₋₁₂, heteroarilo C₁₋₁₂, arilo C₆₋₂₀, -(alquildiilo C₁₋₆)-(cicloalquilo C₃₋₁₂) y -(alquildiilo (C₁₋₆)-(heterociclilo C₃₋₁₂); R² se selecciona de H, F, Cl, -CN, -OCH₃, -OCH₂CH₃ y alquilo C₁₋₆; R³ y R⁴ se seleccionan independientemente de H, -CN, cicloalquilo C₃₋₁₂, heterociclilo C₃₋₁₂, heteroarilo C₁₋₁₂, arilo C₆₋₂₀, -O-(heteroarilo C₁₋₁₂), -O-(alquildiilo C₁₋₆)-(arilo C₆₋₂₀), -NR⁸R⁹, -NR⁸C(O)R⁹, -NR⁸C(O)OR⁹, -NR⁸C(O)NHR⁹, -NR⁸SO₂-(alquilo C₁₋₆), -NR⁸SO₂-(alquenilo C₁₋₆), -NR⁸SO₂-(heteroarilo C₁₋₁₂), -NR⁸SO₂-(alquildiilo C₁₋₆)-(cicloalquilo C₃₋₁₂), -NR⁸SO₂-(alquildiilo C₁₋₆)-(heterociclilo C₃₋₁₂), -NR⁸SO₂-(alquildiilo C₁₋₆)-(heteroarilo C₁₋₁₂), -NR⁸SO₂-(alquildiilo C₁₋₆)-(arilo C₆₋₂₀), -NR⁸SO₂NR⁸R⁹ y -SO₂NR⁸R⁹; R⁵ y R⁷ se seleccionan independientemente de H, F, Cl, -CN, -CH₂OH, -C(O)NH₂, -OH, -OCH₃, -OCH₂CH₃ y alquilo C₁₋₆; R⁶ se selecciona independientemente de H, F, Cl, Br, I,-CN, -NO₂ y alquilo C₁₋₆; R⁸ se selecciona independientemente de H y alquilo C₁₋₆; R⁹ se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, cicloalquilo C₃₋₁₂, heterociclilo C₃₋₁₂, heteroarilo C₁₋₁₂, arilo C₆₋₂₀; -(alquildiilo C₁₋₆)-(cicloalquilo C₃₋₁₂), -(alquildiilo C₁₋₆)-(heterociclilo C₃₋₁₂), -(alquildiilo C₁₋₆)-(heteroarilo C₁₋₆), -(alquildiilo C₁₋₆)-(arilo C₆₋₂₀) y -(alquildiilo C₁₋₆)-O-(arilo C₆₋₂₀); y n es 0, 1, 2 ó 3; en donde cicloalquilo, heterociclilo, heteroarilo, arilo, alquilo, alquildiilo y alquenilo están opcional e independientemente sustituidos con uno o más grupos seleccionados de F, Cl, Br, I, -CN, -CH₃, -CH₂CH₃, -CH₂CH₂CH₃, -CH(CH₃)₂, -CH₂CH(CH₃)₂, -CH(CH₃)CH₂CH₃, -CH₂C(CH₃)₃, -CH₂OH, -CH₂OCH₃, -CH₂CH₂OH, -C(CH₃)₂OH, -CH(OH)CH(CH₃)₂, -C(CH₃)₂CH₂OH, -CH₂CH₂CH₂OH, -CH₂CH₂C(CH₃)₂OH, -CH₂CH₂OCH₃, -CH₂CH(CH₃)OCH₃, -CH₂CH₂CH₂OCH₃, -CH₂CH₂C(CH₃)₂OCH₃, -CH₂CH₂SO₂CH₃, -CH₂OP(O)(OH)₂, -CH₂F, -CHF₂, -CH₂NH₂, -CH₂NHSO₂CH₃, -CH₂NHCH₃, -CH₂N(CH₃)₂, -CF₃, -CH₂CF₃, -CH₂CHF₂, -CH₂CH₂CHF₂, -CH₂CH₂CF₃, -CH(CH₃)CN, -C(CH₃)₂CN, -CH₂CN, -CO₂H, -COCH₃, -CO₂CH₃, -CO₂C(CH₃)₃, -COCH(OH)CH₃, -CONH₂, -CONHCH₃, -CONHCH₂CH₃, -CONHCH(CH₃)₂, -CON(CH₃)₂, -C(CH₃)₂CONH₂, -NH₂, -NHCH₃, -N(CH₃)₂, -N(CH₃)CH₂CH₃, -NHCOCH₃, -N(CH₃)COCH₃, -NHS(O)₂CH₃, -N(CH₃)C(CH₃)₂CONH₂, -N(CH₃)CH₂CH₂S(O)₂CH₃, -NO₂, =O, -OH, -OCH₃, -OCH₂CH₃, -OCH₂CH₂OCH₃, -OCH₂CH₂OH, -OCH₂CH₂N(CH₃)₂, -OP(O)(OH)₂, -S(O)₂N(CH₃)₂, -SCH₃, -S(O)₂CH₃, -S(O)₃H, ciclopropilo, ciclopropilamida, ciclobutilo, oxetanilo, azetidinilo, 1-metilazetidin-3-il)oxi, N-metil-N-oxetan-3-ilamino, azetidin-1-ilmetilo, benciloxifenilo, pirrolidin-1-ilo, pirrolidin-1-il-metanona, fenilo, piperazin-1-ilo, piperidin-1-ilo, morfolinometilo, morfolino-metanona y morfolino.