EA201590661A1 - Азахиназолиновые ингибиторы атипичной протеинкиназы c - Google Patents

Азахиназолиновые ингибиторы атипичной протеинкиназы c

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Publication number
EA201590661A1
EA201590661A1 EA201590661A EA201590661A EA201590661A1 EA 201590661 A1 EA201590661 A1 EA 201590661A1 EA 201590661 A EA201590661 A EA 201590661A EA 201590661 A EA201590661 A EA 201590661A EA 201590661 A1 EA201590661 A1 EA 201590661A1
Authority
EA
Eurasian Patent Office
Prior art keywords
azachinasoline
proteinkinase
atypical
inhibitors
compound
Prior art date
Application number
EA201590661A
Other languages
English (en)
Other versions
EA030253B1 (ru
Inventor
Генри Дж. Бреслин
Брюс Д. Дорси
Бенджамин Дж. Дуган
Кэтрин М. Фаулер
Роберт Л. Хадкинз
Юджин Ф. Месарос
Натаниэль ДжТ Монк
Эмма Л. Моррис
Икеолува Оловойе
Грегори Р. Отт
Грегуар А. Пейв
Джонатан Р.А. Роффи
Кристелль Н. Соуди
Мин Тао
Крейг А. Зификсак
Эллисон Л. Зулли
Original Assignee
Игнайта, Инк.
Кэнсэр Ресерч Текнолоджи Лимитед
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
Application filed by Игнайта, Инк., Кэнсэр Ресерч Текнолоджи Лимитед filed Critical Игнайта, Инк.
Publication of EA201590661A1 publication Critical patent/EA201590661A1/ru
Publication of EA030253B1 publication Critical patent/EA030253B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Изобретение относится к соединению формулы (I)или его соли, где R, R, R, G и X такие, как определено в описании. Соединение формулы (I) и его соли обладают ингибиторной активностью в отношении aPKC и могут использоваться для лечения пролиферативных заболеваний.
EA201590661A 2012-09-28 2013-09-27 Азахиназолиновые ингибиторы атипичной протеинкиназы c EA030253B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261707340P 2012-09-28 2012-09-28
US201361781364P 2013-03-14 2013-03-14
PCT/US2013/062085 WO2014052699A1 (en) 2012-09-28 2013-09-27 Azaquinazoline inhibitors of atypical protein kinase c

Publications (2)

Publication Number Publication Date
EA201590661A1 true EA201590661A1 (ru) 2015-09-30
EA030253B1 EA030253B1 (ru) 2018-07-31

Family

ID=49326872

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201590661A EA030253B1 (ru) 2012-09-28 2013-09-27 Азахиназолиновые ингибиторы атипичной протеинкиназы c

Country Status (19)

Country Link
US (2) US9914730B2 (ru)
EP (1) EP2900666B1 (ru)
JP (1) JP6535430B2 (ru)
KR (1) KR102215272B1 (ru)
CN (1) CN105102456B (ru)
AU (1) AU2013323360B2 (ru)
BR (1) BR112015007061B1 (ru)
CA (1) CA2886495C (ru)
CL (1) CL2015000781A1 (ru)
EA (1) EA030253B1 (ru)
HK (2) HK1211928A1 (ru)
IL (1) IL237918B (ru)
MX (1) MX2015004016A (ru)
NZ (1) NZ706857A (ru)
PH (1) PH12015500689B1 (ru)
SG (1) SG11201502301YA (ru)
TW (1) TWI663165B (ru)
WO (1) WO2014052699A1 (ru)
ZA (1) ZA201502783B (ru)

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UA118610C2 (uk) 2014-09-12 2019-02-11 Бьорінгер Інгельхайм Інтернаціональ Гмбх Спіроциклічні інгібітори катепсину c
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CN112638899B (zh) * 2018-08-01 2023-09-05 上海轶诺药业有限公司 一类具有免疫调节功能的芳香化合物的制备和应用
CN111100063B (zh) * 2018-10-25 2022-05-17 南京药石科技股份有限公司 一种合成2-氟甲基取代的吡咯烷、哌啶以及哌嗪衍生物的制备方法
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CN114349711B (zh) * 2022-02-28 2023-08-15 四川依维欣医药科技有限公司 一种（R）-1-Boc-3-羟甲基哌嗪的合成方法

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Also Published As

Publication number Publication date
EP2900666B1 (en) 2020-11-04
WO2014052699A9 (en) 2015-07-16
NZ706857A (en) 2018-05-25
MX2015004016A (es) 2016-02-18
PH12015500689A1 (en) 2015-05-25
ZA201502783B (en) 2016-01-27
CN105102456B (zh) 2017-11-14
CA2886495C (en) 2023-09-19
KR20150086248A (ko) 2015-07-27
AU2013323360B2 (en) 2017-09-07
KR102215272B1 (ko) 2021-02-15
US9896446B2 (en) 2018-02-20
EA030253B1 (ru) 2018-07-31
HK1212336A1 (en) 2016-06-10
JP2015533822A (ja) 2015-11-26
JP6535430B2 (ja) 2019-06-26
IL237918A0 (en) 2015-05-31
IL237918B (en) 2021-05-31
WO2014052699A1 (en) 2014-04-03
EP2900666A1 (en) 2015-08-05
TW201427978A (zh) 2014-07-16
CL2015000781A1 (es) 2016-04-01
CA2886495A1 (en) 2014-04-03
BR112015007061A8 (pt) 2019-08-20
US9914730B2 (en) 2018-03-13
CN105102456A (zh) 2015-11-25
BR112015007061B1 (pt) 2022-10-04
SG11201502301YA (en) 2015-04-29
AU2013323360A1 (en) 2015-04-30
US20160102094A1 (en) 2016-04-14
TWI663165B (zh) 2019-06-21
HK1211928A1 (en) 2016-06-03
BR112015007061A2 (pt) 2017-07-04
US20140113882A1 (en) 2014-04-24
PH12015500689B1 (en) 2015-05-25

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