AU2013342203B2 - Therapeutic compounds and compositions and their use as PKM2 modulators - Google Patents

Therapeutic compounds and compositions and their use as PKM2 modulators Download PDF

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Publication number
AU2013342203B2
AU2013342203B2 AU2013342203A AU2013342203A AU2013342203B2 AU 2013342203 B2 AU2013342203 B2 AU 2013342203B2 AU 2013342203 A AU2013342203 A AU 2013342203A AU 2013342203 A AU2013342203 A AU 2013342203A AU 2013342203 B2 AU2013342203 B2 AU 2013342203B2
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AU
Australia
Prior art keywords
compound
pharmaceutically acceptable
acceptable salt
subject
alkyl
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AU2013342203A
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AU2013342203A1 (en
Inventor
Giovanni Cianchetta
Janeta Popovici-Muller
Jeffrey O. Saunders
Robert Zahler
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Agios Pharmaceuticals Inc
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Agios Pharmaceuticals Inc
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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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2013342203A 2012-11-08 2013-11-08 Therapeutic compounds and compositions and their use as PKM2 modulators Ceased AU2013342203B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Publications (2)

Publication Number Publication Date
AU2013342203A1 AU2013342203A1 (en) 2015-05-21
AU2013342203B2 true AU2013342203B2 (en) 2017-11-23

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Family Applications (1)

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AU2013342203A Ceased AU2013342203B2 (en) 2012-11-08 2013-11-08 Therapeutic compounds and compositions and their use as PKM2 modulators

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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Publication number Priority date Publication date Assignee Title
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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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
BR0013694A (pt) 1999-09-04 2002-05-21 Astrazeneca Ab Composto, processo para a preparação de um composto, composição farmacêutica, e, uso de um composto
EP1797076A1 (en) 2004-09-24 2007-06-20 AstraZeneca AB Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
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
EP2417123A2 (en) 2009-04-06 2012-02-15 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
CA2759547A1 (en) 2009-04-22 2010-10-28 Janssen Pharmaceutica Nv Azetidinyl diamides as monoacylglycerol lipase inhibitors
CR20170071A (es) * 2009-06-29 2017-03-28 Agios Pharmaceuticals Inc Compuestos terapeuticos y composiciones
EP2448581B1 (en) * 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
CA2797694A1 (en) * 2010-04-29 2011-11-03 The United States Of America, As Represented By The Secretary, Departmen T Of Health And Human Services Activators of human pyruvate kinase
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
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
US9388164B2 (en) * 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
ME03074B (me) * 2011-05-03 2019-01-20 Agios Pharmaceuticals Inc Akтivatori piruvat kinaze za upotrebu u terapiji

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
WO2014074848A1 (en) 2014-05-15
US20150307473A1 (en) 2015-10-29
JP6362610B2 (ja) 2018-07-25
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
EA032007B1 (ru) 2019-03-29
EA201590881A1 (ru) 2015-08-31

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