AU2009303335B2 - Activators of human pyruvate kinase - Google Patents

Activators of human pyruvate kinase Download PDF

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Publication number
AU2009303335B2
AU2009303335B2 AU2009303335A AU2009303335A AU2009303335B2 AU 2009303335 B2 AU2009303335 B2 AU 2009303335B2 AU 2009303335 A AU2009303335 A AU 2009303335A AU 2009303335 A AU2009303335 A AU 2009303335A AU 2009303335 B2 AU2009303335 B2 AU 2009303335B2
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Australia
Prior art keywords
benzo
dihydro
dioxinyl
difluorophenyl
cio
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AU2009303335A
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AU2009303335A1 (en
Inventor
Douglas S. Auld
Matthew Boxer
James Inglese
Jian-kang JIANG
Amanda P. Skoumbourdis
Craig J. Thomas
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US Department of Health and Human Services
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Government of the United States of America
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Priority to AU2016216705A priority Critical patent/AU2016216705B2/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/22Heterocyclic 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 hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D319/00Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/101,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/141,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/161,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18Ethylenedioxybenzenes, not substituted on the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2009303335A 2008-10-09 2009-10-09 Activators of human pyruvate kinase Active AU2009303335B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2016216705A AU2016216705B2 (en) 2008-10-09 2016-08-19 Activators of human pyruvate kinase

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10409108P 2008-10-09 2008-10-09
US61/104,091 2008-10-09
PCT/US2009/060237 WO2010042867A2 (en) 2008-10-09 2009-10-09 Activators of human pyruvate kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2016216705A Division AU2016216705B2 (en) 2008-10-09 2016-08-19 Activators of human pyruvate kinase

Publications (2)

Publication Number Publication Date
AU2009303335A1 AU2009303335A1 (en) 2010-04-15
AU2009303335B2 true AU2009303335B2 (en) 2016-05-19

Family

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AU2009303335A Active AU2009303335B2 (en) 2008-10-09 2009-10-09 Activators of human pyruvate kinase
AU2016216705A Active AU2016216705B2 (en) 2008-10-09 2016-08-19 Activators of human pyruvate kinase

Family Applications After (1)

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AU2016216705A Active AU2016216705B2 (en) 2008-10-09 2016-08-19 Activators of human pyruvate kinase

Country Status (7)

Country Link
US (4) US8841305B2 (enExample)
EP (2) EP3173415B1 (enExample)
JP (2) JP5632379B2 (enExample)
AU (2) AU2009303335B2 (enExample)
CA (2) CA2740148C (enExample)
ES (1) ES2620634T3 (enExample)
WO (1) WO2010042867A2 (enExample)

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WO2008019139A2 (en) 2006-08-04 2008-02-14 Beth Israel Deaconess Medical Center Inhibitors of pyruvate kinase and methods of treating disease
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EP2417123A2 (en) 2009-04-06 2012-02-15 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
DK2427441T3 (en) 2009-05-04 2017-03-20 Agios Pharmaceuticals Inc PKM2 Activators for use in the treatment of cancer
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
CR20170071A (es) 2009-06-29 2017-03-28 Agios Pharmaceuticals Inc Compuestos terapeuticos y composiciones
JP5909482B2 (ja) 2010-03-31 2016-04-26 ザ スクリプス リサーチ インスティテュート 細胞の再プログラム
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
EP2632920A1 (en) 2010-10-27 2013-09-04 Dynamix Pharmaceuticals Ltd. Sulfonamides for the modulation of pkm2
EP2651898B1 (en) 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
WO2012088314A1 (en) * 2010-12-21 2012-06-28 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
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
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WO2012151440A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
EP3372230B1 (en) 2011-05-03 2020-08-12 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
WO2013005157A1 (en) * 2011-07-05 2013-01-10 Lupin Limited Sulfone derivatives and their use as pkm2 modulators for the treatment of cancer
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WO2014074848A1 (en) * 2012-11-08 2014-05-15 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions and their use as pkm2 modulators
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
CN104370936A (zh) * 2014-09-28 2015-02-25 苏州维泰生物技术有限公司 一种新型丙酮酸激酶m2激活剂及其合成方法
MA44392B1 (fr) 2015-06-11 2023-10-31 Agios Pharmaceuticals Inc Procédés d'utilisation d'activateurs de la pyruvate kinase
KR101713678B1 (ko) * 2015-08-24 2017-03-09 대우제약 주식회사 신규 화합물 4-Ethyl-7-(2-fluoro-benzylsulfanyl)-2-methyl-1-thia-3b, 5, 6-triaza-cyclopenta[a]indene 및 이를 포함하는 항암제용 약제학적 조성물
JP7332295B2 (ja) 2016-01-25 2023-08-23 スーパ-メタリクス,インコーポレイテッド. 四ホウ化タングステンの結合材組成物及びそれらの研磨方法
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
US12233063B2 (en) 2017-10-20 2025-02-25 The Regents Of The University Of Michigan Compositions and methods for treating eye disorders
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
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CN110483504B (zh) * 2019-08-02 2022-04-26 桂林理工大学 以DMF为甲酰化试剂构建2-(2-萘基)咪唑[1,2-a]吡啶-3-醛的新方法
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
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Publication number Publication date
US20150105395A1 (en) 2015-04-16
AU2009303335A1 (en) 2010-04-15
JP2015078188A (ja) 2015-04-23
JP5632379B2 (ja) 2014-11-26
WO2010042867A2 (en) 2010-04-15
US20160199370A1 (en) 2016-07-14
EP3173415A3 (en) 2017-08-23
JP5960770B2 (ja) 2016-08-02
US8937067B2 (en) 2015-01-20
JP2012505247A (ja) 2012-03-01
US9707230B2 (en) 2017-07-18
WO2010042867A3 (en) 2010-08-05
US20110195958A1 (en) 2011-08-11
EP2344453B1 (en) 2016-12-28
ES2620634T3 (es) 2017-06-29
US9290512B2 (en) 2016-03-22
AU2016216705B2 (en) 2018-04-26
US20120245141A1 (en) 2012-09-27
EP3173415B1 (en) 2019-06-05
CA3041868A1 (en) 2010-04-15
AU2016216705A1 (en) 2016-09-08
EP3173415A2 (en) 2017-05-31
US8841305B2 (en) 2014-09-23
CA2740148C (en) 2019-06-18
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CA3041868C (en) 2023-03-07

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