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AR111281A1 - Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1 - Google Patents

Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1

Info

Publication number
AR111281A1
AR111281A1 ARP180100604A ARP180100604A AR111281A1 AR 111281 A1 AR111281 A1 AR 111281A1 AR P180100604 A ARP180100604 A AR P180100604A AR P180100604 A ARP180100604 A AR P180100604A AR 111281 A1 AR111281 A1 AR 111281A1
Authority
AR
Argentina
Prior art keywords
alkyldiyl
heteroaryl
aryl
nr8so2
cycloalkyl
Prior art date
Application number
ARP180100604A
Other languages
English (en)
Original Assignee
Genentech Inc
Univ California
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=63522807&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR111281(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Genentech Inc, Univ California filed Critical Genentech Inc
Publication of AR111281A1 publication Critical patent/AR111281A1/es

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Classifications

    • 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
    • C07D401/14—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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pyridine Compounds (AREA)

Abstract

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.
ARP180100604A 2017-03-17 2018-03-15 Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1 AR111281A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2017077059 2017-03-17

Publications (1)

Publication Number Publication Date
AR111281A1 true AR111281A1 (es) 2019-06-26

Family

ID=63522807

Family Applications (1)

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ARP180100604A AR111281A1 (es) 2017-03-17 2018-03-15 Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1

Country Status (17)

Country Link
US (1) US10968203B2 (es)
EP (1) EP3596063A4 (es)
JP (1) JP6925435B2 (es)
KR (1) KR20190141145A (es)
CN (1) CN111247136A (es)
AR (1) AR111281A1 (es)
AU (1) AU2018233402A1 (es)
BR (1) BR112019019193A2 (es)
CA (1) CA3056833A1 (es)
CL (1) CL2019002671A1 (es)
CO (1) CO2019010078A2 (es)
CR (1) CR20190433A (es)
IL (1) IL269302A (es)
PE (1) PE20191557A1 (es)
SG (1) SG11201908517XA (es)
TW (1) TW201838981A (es)
WO (1) WO2018166528A1 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12156523B2 (en) 2017-03-17 2024-12-03 Mmag Co., Ltd. Plant disease control agent
US10392367B2 (en) 2017-06-01 2019-08-27 Quentis Therapeutics, Inc. IRE1 small molecule inhibitors
EP3630748B1 (en) 2017-06-01 2023-04-19 Cornell University Ire1 small molecule inhibitors
WO2020047518A1 (en) * 2018-08-30 2020-03-05 The Regents Of The University Of California Ire1 kinase inhibitors and uses thereof
TWI831829B (zh) 2018-09-12 2024-02-11 美商建南德克公司 苯氧基-吡啶基-嘧啶化合物及使用方法
CN112689528B (zh) * 2018-09-12 2024-05-14 基因泰克公司 嘧啶基-杂芳氧基-萘基化合物和使用方法
JP7546299B2 (ja) * 2018-12-03 2024-09-06 コーネル・ユニバーシティー Ｉｒｅ１小分子阻害物質
WO2020117634A1 (en) * 2018-12-03 2020-06-11 Cornell University Ire1 small molecule inhibitors
CN113508115A (zh) 2019-01-03 2021-10-15 基因泰克公司 吡啶并嘧啶酮和蝶啶酮化合物作为需要酶i(ire i α)的内切核糖核酸酶肌醇的抑制剂用于治疗癌症疾病
US12479818B2 (en) 2019-05-15 2025-11-25 Cornell University Treatment of fibrosis with IRE1 small molecule inhibitors
EP4192462A4 (en) * 2020-08-07 2024-09-04 Optikira LLC PYRAZOLOPYRIDINE COMPOUNDS AND METHODS OF INHIBITING IRE1 USING THEM
WO2022104148A1 (en) * 2020-11-13 2022-05-19 The Regents Of The University Of California Ire1alpha inhibitors and uses thereof
US11884649B2 (en) 2020-11-13 2024-01-30 The Regents Of The University Of California IRE1α inhibitors and uses thereof
CN114907350B (zh) * 2021-02-10 2023-12-29 上海凌达生物医药有限公司 一类含氮稠环类化合物、制备方法和用途
CN116693357B (zh) * 2023-06-07 2026-01-27 西安工程大学 一种β-三氟甲基不饱和酰胺及其合成方法

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* Cited by examiner, † Cited by third party
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WO2005113494A2 (en) * 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
US7868177B2 (en) 2006-02-24 2011-01-11 Amgen Inc. Multi-cyclic compounds and method of use
JP6144873B2 (ja) 2008-09-15 2017-06-07 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Ｉｒｅ１、ｓｒｃ、及びａｂｌ活性を調節するための方法及び組成物
ES2638317T3 (es) 2013-04-04 2017-10-19 Janssen Pharmaceutica Nv Nuevos derivados de N-(2,3-dihidro-1H-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina y N-(2,3-dihidro-1H-indol-5-il)-4-quinazolinamina como inhibidores de PERK

Also Published As

Publication number Publication date
CR20190433A (es) 2019-11-20
SG11201908517XA (en) 2019-10-30
CA3056833A1 (en) 2018-09-20
JP6925435B2 (ja) 2021-08-25
CN111247136A (zh) 2020-06-05
TW201838981A (zh) 2018-11-01
AU2018233402A1 (en) 2019-10-10
IL269302A (en) 2019-11-28
BR112019019193A2 (pt) 2020-04-22
JP2020514377A (ja) 2020-05-21
KR20190141145A (ko) 2019-12-23
CL2019002671A1 (es) 2019-12-06
US10968203B2 (en) 2021-04-06
CO2019010078A2 (es) 2020-01-17
EP3596063A4 (en) 2020-12-30
EP3596063A1 (en) 2020-01-22
US20180265497A1 (en) 2018-09-20
PE20191557A1 (es) 2019-10-24
WO2018166528A1 (en) 2018-09-20

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