JP6362610B2 - 治療用化合物及び組成物並びにpkm2調節剤としてのそれらの使用 - Google Patents

治療用化合物及び組成物並びにpkm2調節剤としてのそれらの使用 Download PDF

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JP6362610B2
JP6362610B2 JP2015541933A JP2015541933A JP6362610B2 JP 6362610 B2 JP6362610 B2 JP 6362610B2 JP 2015541933 A JP2015541933 A JP 2015541933A JP 2015541933 A JP2015541933 A JP 2015541933A JP 6362610 B2 JP6362610 B2 JP 6362610B2
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pharmaceutically acceptable
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JP2016501189A5 (enExample
JP2016501189A (ja
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ギオバンニ シアンチェッタ,
ギオバンニ シアンチェッタ,
ジャニータ ポポビシ−ムラー,
ジャニータ ポポビシ−ムラー,
ジェフリー オー. サウンダーズ,
ジェフリー オー. サウンダーズ,
ロバート ザーラー,
ロバート ザーラー,
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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
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
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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
    • C07D401/02Heterocyclic 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
JP2015541933A 2012-11-08 2013-11-08 治療用化合物及び組成物並びにpkm2調節剤としてのそれらの使用 Expired - Fee Related JP6362610B2 (ja)

Applications Claiming Priority (3)

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US201261724266P 2012-11-08 2012-11-08
US61/724,266 2012-11-08
PCT/US2013/069193 WO2014074848A1 (en) 2012-11-08 2013-11-08 Therapeutic compounds and compositions and their use as pkm2 modulators

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JP2016501189A JP2016501189A (ja) 2016-01-18
JP2016501189A5 JP2016501189A5 (enExample) 2016-12-22
JP6362610B2 true JP6362610B2 (ja) 2018-07-25

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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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DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
CA2900652C (en) 2013-02-15 2021-05-04 Kala Pharmaceuticals, Inc. Therapeutic compounds and uses thereof
CN107915751A (zh) 2013-02-20 2018-04-17 卡拉制药公司 治疗性化合物和其用途
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
WO2015066482A1 (en) 2013-11-01 2015-05-07 Kala Pharmaceuticals, Inc. Crystalline forms of therapeutic compounds and uses thereof
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
CA3252823A1 (en) 2016-06-13 2025-02-25 Gilead Sciences, Inc. Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds
AU2017324716B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
MX2019002629A (es) 2016-09-08 2019-10-07 Kala Pharmaceuticals Inc Formas cristalinas de compuestos terapéuticos y usos de los mismos.
AU2017324713B2 (en) 2016-09-08 2020-08-13 KALA BIO, Inc. Crystalline forms of therapeutic compounds and uses thereof
EP3680241A1 (en) * 2017-03-20 2020-07-15 Forma Therapeutics, Inc. Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
CN111032045B (zh) 2017-08-15 2023-08-15 安吉奥斯医药品有限公司 用于治疗血液病症的丙酮酸激酶激活剂
US20200237766A1 (en) 2017-10-13 2020-07-30 Tolero Pharmaceuticals, Inc. Pkm2 activators in combination with reactive oxygen species for treatment of cancer
WO2020061255A1 (en) * 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
US10675274B2 (en) 2018-09-19 2020-06-09 Forma Therapeutics, Inc. Activating pyruvate kinase R
US11524005B2 (en) 2019-02-19 2022-12-13 Gilead Sciences, Inc. Solid forms of FXR agonists
EP3941463A1 (en) 2019-03-22 2022-01-26 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
HUE072832T2 (hu) 2019-09-19 2025-12-28 Novo Nordisk Healthcare Ag Piruvát kináz R-t (PKR) aktiváló készítmények
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

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JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
US6214879B1 (en) 1998-03-24 2001-04-10 Virginia Commonwealth University Allosteric inhibitors of pyruvate kinase
WO2001017956A1 (en) 1999-09-04 2001-03-15 Astrazeneca Ab Substituted n-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity
WO2006033628A1 (en) 2004-09-24 2006-03-30 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US8841305B2 (en) * 2008-10-09 2014-09-23 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of the human pyruvate kinase M2 receptor
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
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EP2448581B1 (en) * 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
WO2011137089A1 (en) * 2010-04-29 2011-11-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
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CA2821975A1 (en) * 2010-12-17 2012-06-21 Shunqi Yan N-(4-(azetidine-1-carbonyl)phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase m2 pkm2 modulators
TWI549947B (zh) * 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
JP6272754B2 (ja) * 2011-05-03 2018-01-31 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 ピルビン酸キナーゼ活性化剤の使用方法
WO2012151448A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy

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CN104822672B (zh) 2018-08-28
EP2917207A1 (en) 2015-09-16
MX2015005841A (es) 2016-01-08
US9458132B2 (en) 2016-10-04
NZ707778A (en) 2019-03-29
AU2013342203B2 (en) 2017-11-23
HK1213888A1 (zh) 2016-07-15
EA201590881A1 (ru) 2015-08-31
CA2890664A1 (en) 2014-05-15
JP2016501189A (ja) 2016-01-18
US20150307473A1 (en) 2015-10-29
WO2014074848A1 (en) 2014-05-15
AU2013342203A1 (en) 2015-05-21
EA032007B1 (ru) 2019-03-29
CN104822672A (zh) 2015-08-05
KR20150080619A (ko) 2015-07-09

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