CA3144869C - Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity - Google Patents

Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity Download PDF

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Publication number
CA3144869C
CA3144869C CA3144869A CA3144869A CA3144869C CA 3144869 C CA3144869 C CA 3144869C CA 3144869 A CA3144869 A CA 3144869A CA 3144869 A CA3144869 A CA 3144869A CA 3144869 C CA3144869 C CA 3144869C
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Prior art keywords
compound
diabetes
pharmaceutically acceptable
carboxylic acid
acceptable salt
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CA3144869A
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English (en)
French (fr)
Other versions
CA3144869A1 (en
Inventor
Samit Kumar Bhattacharya
Leanne Marie BUZON
Kevin James Filipski
David Andrew Griffith
Bethany Lyn KORMOS
Luis Angel MARTINEZ-ALSINA
Russell Alan MILLER
Matthew Richard Reese
Rachel Jane ROTH FLACH
Yuan Zhang
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Pfizer Inc
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Pfizer Inc
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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3144869A 2019-06-28 2020-06-26 Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity Active CA3144869C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962868057P 2019-06-28 2019-06-28
US62/868,057 2019-06-28
US202062960817P 2020-01-14 2020-01-14
US62/960,817 2020-01-14
US202063031719P 2020-05-29 2020-05-29
US63/031,719 2020-05-29
PCT/IB2020/056066 WO2020261205A1 (en) 2019-06-28 2020-06-26 Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity

Publications (2)

Publication Number Publication Date
CA3144869A1 CA3144869A1 (en) 2020-12-30
CA3144869C true CA3144869C (en) 2023-12-05

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CA3144869A Active CA3144869C (en) 2019-06-28 2020-06-26 Thieno[3,2-b]thiophene-2-carboxylic acid compounds having bckdk inhibiting activity

Country Status (8)

Country Link
US (2) US11542270B2 (https=)
EP (1) EP3990461A1 (https=)
JP (1) JP2022540000A (https=)
CA (1) CA3144869C (https=)
PY (1) PY2030111A (https=)
TW (1) TW202115086A (https=)
UY (1) UY38768A (https=)
WO (1) WO2020261205A1 (https=)

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CN114903994A (zh) * 2022-04-19 2022-08-16 上海交通大学医学院附属瑞金医院 Bckdk作为靶点在制备2型糖尿病药物中的应用
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Also Published As

Publication number Publication date
US11059833B2 (en) 2021-07-13
UY38768A (es) 2021-01-29
US20210087204A1 (en) 2021-03-25
PY2030111A (es) 2021-12-20
US11542270B2 (en) 2023-01-03
EP3990461A1 (en) 2022-05-04
WO2020261205A1 (en) 2020-12-30
TW202115086A (zh) 2021-04-16
CA3144869A1 (en) 2020-12-30
JP2022540000A (ja) 2022-09-14
US20210024536A1 (en) 2021-01-28

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