EA201890153A1 - Ингибиторы поглощения глюкозы - Google Patents

Ингибиторы поглощения глюкозы

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Publication number
EA201890153A1
EA201890153A1 EA201890153A EA201890153A EA201890153A1 EA 201890153 A1 EA201890153 A1 EA 201890153A1 EA 201890153 A EA201890153 A EA 201890153A EA 201890153 A EA201890153 A EA 201890153A EA 201890153 A1 EA201890153 A1 EA 201890153A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
absorption inhibitors
glucose absorption
uptake activity
transporters
Prior art date
Application number
EA201890153A
Other languages
English (en)
Inventor
Келлен Олшевски
Джи-Ин Ким
Маша Поюровски
Кевин Лю
Энтони Барсотти
Кой Моррис
Original Assignee
КАДМОН КОРПОРЕЙШН, ЭлЭлСи
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.)
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Publication date
Application filed by КАДМОН КОРПОРЕЙШН, ЭлЭлСи filed Critical КАДМОН КОРПОРЕЙШН, ЭлЭлСи
Publication of EA201890153A1 publication Critical patent/EA201890153A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

В данном документе предложены соединения, которые модулируют активность поглощения глюкозы и являются пригодными для лечения рака, аутоиммунных заболеваний, воспаления, инфекционных заболеваний и метаболических заболеваний. В некоторых вариантах реализации указанные соединения модулируют активность поглощения глюкозы посредством модулирования клеточных компонентов, включая, но не ограничиваясь ими, компоненты, связанные с гликолизом, и известные транспортеры/котранспортеры глюкозы, такие как GLUT1 и другие члены семейства GLUT/альтернативные транспортеры гексозы. В некоторых вариантах реализации изобретения соединения имеют структуру формулы Iгде переменные имеют значения, описанные в данном документе.
EA201890153A 2015-06-26 2016-06-24 Ингибиторы поглощения глюкозы EA201890153A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562185223P 2015-06-26 2015-06-26
PCT/US2016/039365 WO2016210330A1 (en) 2015-06-26 2016-06-24 Glucose uptake inhibitors

Publications (1)

Publication Number Publication Date
EA201890153A1 true EA201890153A1 (ru) 2018-06-29

Family

ID=57586425

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890153A EA201890153A1 (ru) 2015-06-26 2016-06-24 Ингибиторы поглощения глюкозы

Country Status (8)

Country Link
US (2) US10273248B2 (ru)
EP (1) EP3313825A4 (ru)
JP (1) JP2018518518A (ru)
CN (1) CN108349910A (ru)
CA (1) CA3028355A1 (ru)
EA (1) EA201890153A1 (ru)
HK (1) HK1254835A1 (ru)
WO (1) WO2016210330A1 (ru)

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JP7078960B2 (ja) * 2017-01-26 2022-06-01 エス． トサントリゾス，ヨウラ 置換二環式ピリミジン系化合物および組成物ならびにその使用
US11071735B2 (en) 2017-04-28 2021-07-27 Kadmon Corporation, Llc Treatment of inflammatory conditions and autoimmune diseases with glucose uptake inhibitors
CN109020957B (zh) * 2017-06-12 2023-01-13 南京天印健华医药科技有限公司 作为mnk抑制剂的杂环化合物
KR102469161B1 (ko) 2017-06-30 2022-11-23 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Ｒｈｏ-관련 단백질 키나아제 억제제, Ｒｈｏ-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
EP3421465B1 (en) 2017-06-30 2022-10-26 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
CN110582489B (zh) 2017-06-30 2023-10-27 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
CN109384782A (zh) * 2017-08-04 2019-02-26 厦门大学 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途
WO2019126739A1 (en) 2017-12-21 2019-06-27 Shepherd Therapeutics, Inc. Pyrvinium pamoate anti-cancer therapies
WO2019173500A1 (en) 2018-03-07 2019-09-12 Duquesne University Of The Holy Spirit PYRAZOLO[4,3-d]PYRIMIDINES AS ANTITUMOR AGENTS
WO2020005935A1 (en) * 2018-06-25 2020-01-02 Kadmon Corporation, Llc Glucose uptake inhibitors
EP4058027A4 (en) * 2019-11-13 2023-11-01 Metabomed Ltd GLUCOSE UPtake INHIBITORS AND THEIR USES
AU2020395397A1 (en) * 2019-12-02 2022-06-09 Shanghai Yingli Pharmaceutical Co., Ltd Oxygen-containing heterocyclic compound, preparation method and application thereof
WO2022012409A1 (zh) * 2020-07-14 2022-01-20 武汉朗来科技发展有限公司 一种rock抑制剂及其制备方法和用途
CN112479913A (zh) * 2020-11-19 2021-03-12 安徽修一制药有限公司 一种n,n-二乙基氯代乙酰胺的制备方法
CN112741828B (zh) * 2021-01-08 2022-04-26 武汉大学 药物联用物及其制备方法和用途
US20240109868A1 (en) * 2022-08-29 2024-04-04 Miracure Biotechnology Limited Ep300/cbp modulator, preparation method therefor and use thereof

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US8207178B2 (en) 2007-12-14 2012-06-26 Ardea Biosciences, Inc. Fused pyrimidines as reverse transcriptase inhibitors
CA2777762A1 (en) * 2009-10-12 2011-04-21 Myrexis, Inc. Amino - pyrimidine compounds as inhibitors of tbk1 and/or ikk epsilon
WO2012040499A2 (en) * 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
BR112013026521A2 (pt) * 2011-04-21 2016-12-27 Origenis Gmbh pirazolo[4,3-d]pirimidinas úteis como inibidores de cinase
CN102901456B (zh) 2012-09-12 2015-10-28 深圳深蓝精机有限公司 检测装置及检测圆轴的外径、跳动值、真圆度的方法
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WO2016210331A1 (en) * 2015-06-26 2016-12-29 Kadmon Corporation, Llc Treatment of infectious diseases with glucose uptake inhibitors

Also Published As

Publication number Publication date
HK1254835A1 (zh) 2019-07-26
CA3028355A1 (en) 2016-12-29
US20180298029A1 (en) 2018-10-18
EP3313825A1 (en) 2018-05-02
WO2016210330A1 (en) 2016-12-29
US10273248B2 (en) 2019-04-30
US20190315772A1 (en) 2019-10-17
US10988484B2 (en) 2021-04-27
CN108349910A (zh) 2018-07-31
EP3313825A4 (en) 2019-03-13
JP2018518518A (ja) 2018-07-12

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