EA032007B1 - Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2 - Google Patents

Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2 Download PDF

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Publication number
EA032007B1
EA032007B1 EA201590881A EA201590881A EA032007B1 EA 032007 B1 EA032007 B1 EA 032007B1 EA 201590881 A EA201590881 A EA 201590881A EA 201590881 A EA201590881 A EA 201590881A EA 032007 B1 EA032007 B1 EA 032007B1
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EA
Eurasian Patent Office
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
subject
pyruvate kinase
Prior art date
Application number
EA201590881A
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English (en)
Russian (ru)
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EA201590881A1 (ru
Inventor
Джанета Поповичи-Мюллер
Джеффри О. Сондерз
Роберт Захлер
Джованни Чианкетта
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Аджиос Фармасьютикалз, Инк.
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Application filed by Аджиос Фармасьютикалз, Инк. filed Critical Аджиос Фармасьютикалз, Инк.
Publication of EA201590881A1 publication Critical patent/EA201590881A1/ru
Publication of EA032007B1 publication Critical patent/EA032007B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201590881A 2012-11-08 2013-11-08 Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2 EA032007B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261724266P 2012-11-08 2012-11-08
PCT/US2013/069193 WO2014074848A1 (en) 2012-11-08 2013-11-08 Therapeutic compounds and compositions and their use as pkm2 modulators

Publications (2)

Publication Number Publication Date
EA201590881A1 EA201590881A1 (ru) 2015-08-31
EA032007B1 true EA032007B1 (ru) 2019-03-29

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EA201590881A EA032007B1 (ru) 2012-11-08 2013-11-08 Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2

Country Status (12)

Country Link
US (1) US9458132B2 (enExample)
EP (1) EP2917207A1 (enExample)
JP (1) JP6362610B2 (enExample)
KR (1) KR20150080619A (enExample)
CN (1) CN104822672B (enExample)
AU (1) AU2013342203B2 (enExample)
CA (1) CA2890664A1 (enExample)
EA (1) EA032007B1 (enExample)
HK (1) HK1213888A1 (enExample)
MX (1) MX2015005841A (enExample)
NZ (1) NZ707778A (enExample)
WO (1) WO2014074848A1 (enExample)

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WO2014062838A2 (en) 2012-10-16 2014-04-24 Tolero Pharmaceuticals, Inc. Pkm2 modulators and methods for their use
HK1217092A1 (zh) 2013-02-15 2016-12-23 Kala Pharmaceuticals, Inc. 治疗性化合物及其用途
US9688688B2 (en) 2013-02-20 2017-06-27 Kala Pharmaceuticals, Inc. Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof
BR112015020139A2 (pt) 2013-02-20 2017-07-18 Kala Pharmaceuticals Inc compostos terapêuticos e usos dos mesmos
KR20160099084A (ko) 2013-11-01 2016-08-19 칼라 파마슈티컬스, 인크. 치료 화합물의 결정질 형태 및 그의 용도
US9890173B2 (en) 2013-11-01 2018-02-13 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CN104817490B (zh) * 2015-05-13 2017-10-13 北京大学 氨基二硫代甲酸酯类化合物及其制备方法与应用
WO2017095751A1 (en) 2015-12-02 2017-06-08 Partikula Llc Compositions and methods for modulating cancer cell metabolism
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (NR1H4)
EP3509423A4 (en) 2016-09-08 2020-05-13 Kala Pharmaceuticals, Inc. CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF
CA3036065A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
CA3036336A1 (en) 2016-09-08 2018-03-15 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
PT3448859T (pt) 2017-03-20 2019-10-25 Forma Therapeutics Inc Composições de pirrolopirrole como ativadores de piruvato quinase (pkr).
SG11202001262QA (en) 2017-08-15 2020-03-30 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in treating blood disorders
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
KR102725082B1 (ko) 2019-02-19 2024-11-04 길리애드 사이언시즈, 인코포레이티드 Fxr 효능제의 고체 형태
WO2020198077A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
WO2022170200A1 (en) 2021-02-08 2022-08-11 Global Blood Therapeutics, Inc. 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Citations (1)

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WO2012083246A1 (en) * 2010-12-17 2012-06-21 Agios Pharmaceuticals, Inc. Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators

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US6214879B1 (en) 1998-03-24 2001-04-10 Virginia Commonwealth University Allosteric inhibitors of pyruvate kinase
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JP5632379B2 (ja) * 2008-10-09 2014-11-26 アメリカ合衆国 ヒトピルビン酸キナーゼ活性化剤
JP6067226B2 (ja) 2009-03-13 2017-01-25 アジオス ファーマシューティカルズ, インコーポレイテッド 細胞増殖関連疾患のための方法および組成物
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MATTHEW B. BOXER, JIAN-KANG JIANG, MATTHEW G. VANDER HEIDEN, MIN SHEN, AMANDA P. SKOUMBOURDIS, NOEL SOUTHALL, HENRIKE VEITH, WILLI: "Evaluation of Substituted N , N ′-Diarylsulfonamides as Activators of the Tumor Cell Specific M2 Isoform of Pyruvate Kinase", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 53, no. 3, 11 February 2010 (2010-02-11), pages 1048 - 1055, XP055003691, ISSN: 00222623, DOI: 10.1021/jm901577g *

Also Published As

Publication number Publication date
WO2014074848A1 (en) 2014-05-15
US20150307473A1 (en) 2015-10-29
JP6362610B2 (ja) 2018-07-25
AU2013342203B2 (en) 2017-11-23
EP2917207A1 (en) 2015-09-16
KR20150080619A (ko) 2015-07-09
CN104822672A (zh) 2015-08-05
MX2015005841A (es) 2016-01-08
NZ707778A (en) 2019-03-29
US9458132B2 (en) 2016-10-04
CA2890664A1 (en) 2014-05-15
HK1213888A1 (zh) 2016-07-15
AU2013342203A1 (en) 2015-05-21
JP2016501189A (ja) 2016-01-18
CN104822672B (zh) 2018-08-28
EA201590881A1 (ru) 2015-08-31

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU