EA202092444A1 - Тризамещенные арильные и гетероарильные производные как модуляторы киназы pi3 и путей аутофагии - Google Patents

Тризамещенные арильные и гетероарильные производные как модуляторы киназы pi3 и путей аутофагии

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Publication number
EA202092444A1
EA202092444A1 EA202092444A EA202092444A EA202092444A1 EA 202092444 A1 EA202092444 A1 EA 202092444A1 EA 202092444 A EA202092444 A EA 202092444A EA 202092444 A EA202092444 A EA 202092444A EA 202092444 A1 EA202092444 A1 EA 202092444A1
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EA
Eurasian Patent Office
Prior art keywords
autophagy
modulators
kinase
paths
trisubstituted aryl
Prior art date
Application number
EA202092444A
Other languages
English (en)
Inventor
Эмили М. Стокинг
Вольфганг Дж. Вразидло
Original Assignee
Нейропор Терапиз, Инк.
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Application filed by Нейропор Терапиз, Инк. filed Critical Нейропор Терапиз, Инк.
Publication of EA202092444A1 publication Critical patent/EA202092444A1/ru

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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • 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
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    • 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
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    • C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
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    • 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
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  • Chemical & Material Sciences (AREA)
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  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Настоящее изобретение относится к тризамещенным арильным и гетероарильным соединениям, к фармацевтическим композициям, содержащим их, и к способам их применения, включая способы модулирования аутофагии или предупреждения, реверсирования, замедления или ингибирования пути PI3K-AKT-MTOR, а также к способам лечения заболеваний, связанных с регуляцией аутофагии или пути PI3K-AKT-MTOR.
EA202092444A 2018-04-10 2019-04-09 Тризамещенные арильные и гетероарильные производные как модуляторы киназы pi3 и путей аутофагии EA202092444A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862655741P 2018-04-10 2018-04-10
PCT/US2019/026634 WO2019199864A1 (en) 2018-04-10 2019-04-09 Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways

Publications (1)

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EA202092444A1 true EA202092444A1 (ru) 2021-01-26

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US (2) US11492348B2 (ru)
EP (1) EP3774783A1 (ru)
JP (1) JP7369139B2 (ru)
KR (1) KR20200143709A (ru)
CN (1) CN112189012B (ru)
AU (1) AU2019251360A1 (ru)
CA (1) CA3094714A1 (ru)
EA (1) EA202092444A1 (ru)
MX (1) MX2020010576A (ru)
SG (1) SG11202008832TA (ru)
WO (1) WO2019199864A1 (ru)

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BR112021022504A2 (pt) 2019-05-10 2022-04-12 Deciphera Pharmaceuticals Llc Inibidores de autofagia de fenilaminopirimidina amida e métodos de uso dos mesmos
LT3966206T (lt) * 2019-05-10 2023-11-10 Deciphera Pharmaceuticals, Llc Heteroarilaminopirimidino amido autofagijos inhibitoriai ir jų naudojimo būdai
JP2022536540A (ja) 2019-06-17 2022-08-17 デシフェラ・ファーマシューティカルズ，エルエルシー アミノピリミジンアミドオートファジー阻害剤およびその使用方法
CN113121499B (zh) * 2021-04-13 2022-05-31 海南锦瑞制药有限公司 奥美拉唑的合成方法及应用

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JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
AU2008345225A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
AU2009256574A1 (en) * 2008-06-13 2009-12-17 Novartis Ag 2,4'-bipyridinyl compounds as protein kinase D inhibitors useful for the treatment of IA heart failure and cancer
GB2465405A (en) * 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
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KR101940831B1 (ko) 2011-03-28 2019-01-21 메이 파마, 아이엔씨. (알파-치환된 아르알킬아미노 및 헤테로아릴알킬아미노)피리미딘일 및 1,3,5-트라이아진일 벤즈이미다졸, 이들을 함유하는 약학 조성물, 및 증식성 질병의 치료에 사용하기 위한 이들 화합물
CA2944697C (en) * 2014-04-22 2022-07-19 Universitaet Basel Manufacturing process for triazine, pyrimidine and pyridine derivatives
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MX2020010576A (es) 2021-03-02
AU2019251360A1 (en) 2020-10-08
WO2019199864A1 (en) 2019-10-17
US20230265086A1 (en) 2023-08-24
EP3774783A1 (en) 2021-02-17
SG11202008832TA (en) 2020-10-29
US20210163462A1 (en) 2021-06-03
CA3094714A1 (en) 2019-10-17
CN112189012A (zh) 2021-01-05
CN112189012B (zh) 2024-02-13
JP2021521178A (ja) 2021-08-26
KR20200143709A (ko) 2020-12-24
US11492348B2 (en) 2022-11-08
JP7369139B2 (ja) 2023-10-25

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