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WO2010073011A3 - Heterocyclic compounds and their use as ampk activators - Google Patents

Heterocyclic compounds and their use as ampk activators Download PDF

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Publication number
WO2010073011A3
WO2010073011A3 PCT/GB2009/002945 GB2009002945W WO2010073011A3 WO 2010073011 A3 WO2010073011 A3 WO 2010073011A3 GB 2009002945 W GB2009002945 W GB 2009002945W WO 2010073011 A3 WO2010073011 A3 WO 2010073011A3
Authority
WO
WIPO (PCT)
Prior art keywords
heterocyclic compounds
ampk activators
ampk
compounds
cardioprotection
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/GB2009/002945
Other languages
French (fr)
Other versions
WO2010073011A2 (en
Inventor
Jacob Westman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Betagenon AB
Original Assignee
Betagenon AB
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 Betagenon AB filed Critical Betagenon AB
Publication of WO2010073011A2 publication Critical patent/WO2010073011A2/en
Publication of WO2010073011A3 publication Critical patent/WO2010073011A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/071,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

There is provided a compound of formula (I), wherein the dotted lines, X, T, G, Y, A1 to A5 and D1 to D5 have meanings given in the description, which compounds are useful in the treatment of conditions or disorders ameliorated by the activation of AMPK, for example skin diseases, lung disease, obesity, dry-type age-related macular degeneration, cardioprotection or, preferably, hyperinsulinemia, diabetes, cancer, fibrosis, neurodegenerative diseases, sexual dysfunction, heart failure, inflammation and osteoporosis.
PCT/GB2009/002945 2008-12-23 2009-12-22 Compounds useful as medicaments Ceased WO2010073011A2 (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US19377408P 2008-12-23 2008-12-23
US61/193,774 2008-12-23
US20208409P 2009-01-27 2009-01-27
US61/202,084 2009-01-27
US20287909P 2009-04-15 2009-04-15
US61/202,879 2009-04-15
US24146309P 2009-09-11 2009-09-11
US61/241,463 2009-09-11

Publications (2)

Publication Number Publication Date
WO2010073011A2 WO2010073011A2 (en) 2010-07-01
WO2010073011A3 true WO2010073011A3 (en) 2010-09-23

Family

ID=42061073

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2009/002945 Ceased WO2010073011A2 (en) 2008-12-23 2009-12-22 Compounds useful as medicaments

Country Status (1)

Country Link
WO (1) WO2010073011A2 (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
CN108578682B (en) * 2018-07-13 2022-04-12 浙江省医学科学院 Application of exenatide in the preparation of medicine for treating pulmonary fibrosis

Families Citing this family (19)

* Cited by examiner, † Cited by third party
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WO2013003467A2 (en) 2011-06-27 2013-01-03 Massachusetts Eye And Ear Infirmary Methods for treating ocular inflammatory disorders
ES2882807T3 (en) 2011-09-16 2021-12-02 Novartis Ag N-substituted heterocyclyl carboxamides
CN103467417B (en) * 2012-06-07 2015-05-20 中国科学院上海药物研究所 Arctigenin carboxamide derivative, preparation method thereof, composition comprising arctigenin carboxamide derivative and uses thereof
US8877980B2 (en) * 2012-09-11 2014-11-04 Al-Urdonia Lemudaddat Al-Ajsam Co. Phenylboronic acid
BR112015021985B1 (en) 2013-03-15 2022-12-13 Global Blood Therapeutics, Inc PHARMACEUTICALLY ACCEPTABLE COMPOUNDS OR SALTS THEREOF, THEIR USES AND COMPOSITION
US9394285B2 (en) 2013-03-15 2016-07-19 Pfizer Inc. Indole and indazole compounds that activate AMPK
EA201992707A1 (en) 2013-11-18 2020-06-30 Глобал Блад Терапьютикс, Инк. COMPOUNDS AND THEIR APPLICATIONS FOR HEMOGLOBIN MODULATION
WO2015103480A1 (en) 2014-01-02 2015-07-09 Massachusetts Eye & Ear Infirmary Treating ocular neovascularization
HRP20181670T1 (en) 2014-06-03 2018-12-14 Idorsia Pharmaceuticals Ltd PIRAZOL COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CALCIUM BLOCKERS
ES2693052T3 (en) 2014-09-15 2018-12-07 Idorsia Pharmaceuticals Ltd Triazole compounds as blockers of the T-type calcium channels
DK3394040T3 (en) 2015-12-24 2022-03-28 Univ California CFTR REGULATORS AND PROCEDURES FOR USING IT
JP6894902B2 (en) * 2015-12-24 2021-06-30 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア CFTR regulator and how to use it
JP6755778B2 (en) * 2016-11-11 2020-09-16 花王株式会社 PPARα activator
US11213517B2 (en) 2016-12-16 2022-01-04 Idorsia Pharmaceuticals Ltd Pharmaceutical combination comprising a T-type calcium channel blocker
ES2971626T3 (en) 2017-02-06 2024-06-06 Idorsia Pharmaceuticals Ltd A novel process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes
CA3073718A1 (en) 2017-08-24 2019-02-28 The Regents Of The University Of California Ocular pharmaceutical compositions
WO2019070709A1 (en) * 2017-10-02 2019-04-11 The Regents Of The University Of California Compounds for treating or preventing flavivirus infections
CN114728919B (en) * 2019-11-05 2025-12-30 德米拉公司 MrgprX2 antagonists and their uses
CN119661470A (en) * 2024-12-02 2025-03-21 安徽医科大学 A thiadiazole urone compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition and use thereof

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WO2005085220A1 (en) * 2004-02-26 2005-09-15 Merck Patent Gmbh Use of thiadiazole urea derivatives
WO2007002461A1 (en) * 2005-06-23 2007-01-04 Dr. Reddy's Laboratories Ltd. 3,4-substituted thiazoles as ampk activators
US20090163545A1 (en) * 2007-12-21 2009-06-25 University Of Rochester Method For Altering The Lifespan Of Eukaryotic Organisms

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WO2007002461A1 (en) * 2005-06-23 2007-01-04 Dr. Reddy's Laboratories Ltd. 3,4-substituted thiazoles as ampk activators
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
CN108578682B (en) * 2018-07-13 2022-04-12 浙江省医学科学院 Application of exenatide in the preparation of medicine for treating pulmonary fibrosis

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