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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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C07D271/07—1,2,4-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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/125—1,3,4-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
    • C07D285/135—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
Publication number Priority date Publication date Assignee Title
WO2013003467A2 (en) * 2011-06-27 2013-01-03 Massachusetts Eye And Ear Infirmary Methods for treating ocular inflammatory disorders
US9056867B2 (en) 2011-09-16 2015-06-16 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
JP6064062B2 (en) 2013-03-15 2017-01-18 ファイザー・インク Indazole compounds that activate AMPK
JP6426694B2 (en) 2013-03-15 2018-11-21 グローバル ブラッド セラピューティクス インコーポレイテッド Compounds for the modification of hemoglobin and their use
EA202092627A1 (en) 2013-11-18 2021-09-30 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
JP6195684B2 (en) 2014-06-03 2017-09-13 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ Pyrazole compounds and their use as T-type calcium channel blockers
PL3194374T3 (en) 2014-09-15 2019-01-31 Idorsia Pharmaceuticals Ltd Triazole compounds as t-type calcium channel blockers
US10604492B2 (en) 2015-12-24 2020-03-31 The Regents Of The Universtiy Of California CFTR regulators and methods of use thereof
IL299924B2 (en) * 2015-12-24 2025-01-01 Univ California Cftr regulators and methods of use thereof
JP6755778B2 (en) * 2016-11-11 2020-09-16 花王株式会社 PPARα activator
WO2018109152A1 (en) 2016-12-16 2018-06-21 Idorsia Pharmaceuticals Ltd Pharmaceutical combination comprising a t-type calcium channel blocker
WO2018141961A1 (en) 2017-02-06 2018-08-09 Idorsia Pharmaceuticals Ltd A novel process for the synthesis of 1-aryl-1-trifluoromethylcyclopropanes
US11839616B2 (en) 2017-08-24 2023-12-12 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
WO2021092264A1 (en) * 2019-11-05 2021-05-14 Dermira, Inc. MrgprX2 ANTAGONISTS AND USES THEREOF
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004103980A1 (en) * 2003-05-21 2004-12-02 Biovitrum Ab Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i
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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2524729A (en) 1945-03-12 1950-10-03 Monsanto Chemicals 2-amino-5-benzyl-1, 3, 4-thiadiazole and acid salts thereof
US2511371A (en) 1945-03-12 1950-06-13 Monsanto Chemicals Sulfa derivatives of 2-amino-5-alkenyl-1, 3, 4-thiadiazoles
US2420434A (en) 1945-03-12 1947-05-13 Monsanto Chemicals 2-amino-5-alkenyl-1, 3, 4 thiadiazoles and process for making the same
US3720685A (en) 1970-07-15 1973-03-13 Squibb & Sons Inc 3-amino-5-benzyl-1,2,4-oxadiazoles
US4054665A (en) 1974-11-29 1977-10-18 Sandoz, Inc. 2-Amino-5-(trifluoromethylphenylalkyl)-1,3,4 thiadiazoles used in the treatment of insomnia and anxiety
CH602685A5 (en) 1975-12-01 1978-07-31 Merck Patent Gmbh
DE2611965A1 (en) 1976-03-20 1977-09-29 Merck Patent Gmbh (1,3,4)-Thiadiazole-(5)-thiols prodn. - by solvolysis of corresp. S-(thio)acyl derivs. or their thione tautomers, useful as intermediates for pharmaceuticals
JP3258771B2 (en) 1992-11-16 2002-02-18 株式会社豊田製作所 Jig for measuring runout of brake rotor
WO2004004720A1 (en) 2002-07-03 2004-01-15 Astex Technology Limited 3-`(hetero) arylmethoxy ! pyridines and their analogues as p38 map kinase inhibitors
US7262020B2 (en) 2003-07-03 2007-08-28 The Regents Of The University Of California Methods for comparing relative flux rates of two or more biological molecules in vivo through a single protocol
WO2005002673A1 (en) 2003-07-03 2005-01-13 Astex Therapeutics Limited Raf kinase inhibitors
EP1902051A1 (en) 2005-06-09 2008-03-26 Merck Frosst Canada Ltd. Azacyclohexane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
WO2007010281A2 (en) 2005-07-21 2007-01-25 Betagenon Ab Use of thiazole derivatives and analogues in disorders caused by free fatty acids
US7754773B2 (en) 2005-10-06 2010-07-13 University Of Massachusetts Composition and synthesis of new reagents for inhibition of HIV replication
WO2008029266A1 (en) 2006-09-08 2008-03-13 Glenmark Pharmaceuticals S.A. Stearoyl coa desaturase inhibitors
US20080182851A1 (en) 2006-11-20 2008-07-31 Glenmark Pharmaceuticals S.A. Acetylene derivatives as stearoyl coa desaturase inhibitors
US20100120669A1 (en) 2007-02-28 2010-05-13 Anne Marie Jeanne Bouillot Thiadiazole derivatives, inhibitors of stearoyl-coa desaturase

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004103980A1 (en) * 2003-05-21 2004-12-02 Biovitrum Ab Inhibitors of 11-beta-hydroxy steroid dehydrogenase type i
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 2009, GOLDFARB, DAVID SCOTT: "Method using lifespan-altering compounds for altering the lifespan of eukaryotic organisms, and screening for such compounds", XP002593929, retrieved from STN Database accession no. 2009:846107 *

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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WO2010073011A2 (en) 2010-07-01

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