SG11202108744WA - Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders - Google Patents

Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders

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Publication number
SG11202108744WA
SG11202108744WA SG11202108744WA SG11202108744WA SG11202108744WA SG 11202108744W A SG11202108744W A SG 11202108744WA SG 11202108744W A SG11202108744W A SG 11202108744WA SG 11202108744W A SG11202108744W A SG 11202108744WA SG 11202108744W A SG11202108744W A SG 11202108744WA
Authority
SG
Singapore
Prior art keywords
derivatives
pkm2
thieno
pyrrole
obesity
Prior art date
Application number
SG11202108744WA
Inventor
Tao Liu
Zhihua Sui
Jingjing Ji
Original Assignee
Agios Pharmaceuticals Inc
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.)
Filing date
Publication date
Application filed by Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Publication of SG11202108744WA publication Critical patent/SG11202108744WA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • 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
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/12Heterocyclic 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 three hetero rings
    • C07D513/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
SG11202108744WA 2019-02-13 2020-02-12 Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders SG11202108744WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962805040P 2019-02-13 2019-02-13
PCT/US2020/017965 WO2020167976A1 (en) 2019-02-13 2020-02-12 Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders

Publications (1)

Publication Number Publication Date
SG11202108744WA true SG11202108744WA (en) 2021-09-29

Family

ID=69941460

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202108744WA SG11202108744WA (en) 2019-02-13 2020-02-12 Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders

Country Status (14)

Country Link
US (1) US20220127267A1 (en)
EP (1) EP3924056A1 (en)
JP (1) JP2022520090A (en)
KR (1) KR20210128435A (en)
CN (1) CN113646050A (en)
AU (1) AU2020221837A1 (en)
BR (1) BR112021015996A2 (en)
CA (1) CA3129829A1 (en)
CO (1) CO2021011919A2 (en)
IL (1) IL285445A (en)
MA (1) MA54948A (en)
MX (1) MX2021009743A (en)
SG (1) SG11202108744WA (en)
WO (1) WO2020167976A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3668513T3 (en) 2017-08-15 2022-01-10 Agios Pharmaceuticals Inc PYRUVAT CHINASE ACTIVITIES FOR USE IN THE TREATMENT OF BLOOD DISEASES
CA3183980A1 (en) * 2020-07-21 2022-01-27 The Regents Of The University Of Michigan Compositions and methods for activating pyruvate kinase
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
WO2023052783A1 (en) 2021-09-30 2023-04-06 Sitryx Therapeutics Limited Novel compounds
AR127584A1 (en) 2021-11-05 2024-02-07 Sitryx Therapeutics Ltd NOVEL COMPOUNDS
WO2023118875A1 (en) 2021-12-22 2023-06-29 Sitryx Therapeutics Limited Phthalazine derivatives as pyruvate kinase modulators
CN115487190A (en) * 2022-11-01 2022-12-20 复旦大学附属中山医院 Application of pyruvate kinase M2 activator in preparation of medicine for treating systemic lupus erythematosus

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
UA107667C2 (en) 2009-06-29 2015-02-10 Аджиос Фармасьютікалз, Інк. Medical compounds stimulating activity of pyruvate kinase m2, compositions on their basis and use in the treatment of cancer
WO2012151452A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
BR112013028422B8 (en) * 2011-05-03 2022-01-11 Agios Pharmaceuticals Inc Pyruvate kinase activators for use in therapy
ES2829374T3 (en) * 2011-05-03 2021-05-31 Agios Pharmaceuticals Inc Use of pyruvate kinase activators to increase the lifespan of red blood cells and treat anemia
WO2014018851A1 (en) 2012-07-26 2014-01-30 Joslin Diabetes Center, Inc. Predicting and treating diabetic complications
DK3668513T3 (en) * 2017-08-15 2022-01-10 Agios Pharmaceuticals Inc PYRUVAT CHINASE ACTIVITIES FOR USE IN THE TREATMENT OF BLOOD DISEASES

Also Published As

Publication number Publication date
CA3129829A1 (en) 2020-08-20
MX2021009743A (en) 2021-11-12
AU2020221837A1 (en) 2021-09-02
CO2021011919A2 (en) 2021-12-10
WO2020167976A1 (en) 2020-08-20
KR20210128435A (en) 2021-10-26
JP2022520090A (en) 2022-03-28
BR112021015996A2 (en) 2021-11-09
EP3924056A1 (en) 2021-12-22
CN113646050A (en) 2021-11-12
IL285445A (en) 2021-09-30
MA54948A (en) 2021-12-22
US20220127267A1 (en) 2022-04-28

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