WO2020104578A3 - Modulators of free fatty acid receptor 1 and their use for treatment of diseases - Google Patents

Modulators of free fatty acid receptor 1 and their use for treatment of diseases Download PDF

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Publication number
WO2020104578A3
WO2020104578A3 PCT/EP2019/082057 EP2019082057W WO2020104578A3 WO 2020104578 A3 WO2020104578 A3 WO 2020104578A3 EP 2019082057 W EP2019082057 W EP 2019082057W WO 2020104578 A3 WO2020104578 A3 WO 2020104578A3
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
fatty acid
free fatty
modulators
diseases
Prior art date
Application number
PCT/EP2019/082057
Other languages
French (fr)
Other versions
WO2020104578A2 (en
Inventor
Michael LÜCKMANN
Thomas Michael Frimurer
Thue W. Schwartz
Original Assignee
University Of Copenhagen
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 University Of Copenhagen filed Critical University Of Copenhagen
Publication of WO2020104578A2 publication Critical patent/WO2020104578A2/en
Publication of WO2020104578A3 publication Critical patent/WO2020104578A3/en

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Classifications

    • 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
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics

Abstract

The present invention relates to the discovery and development of ago-allosteric modulators on the free fatty acid receptor 1 and their use in therapy, particularly their use in the treatment of diabetes.
PCT/EP2019/082057 2018-11-21 2019-11-21 Modulators of free fatty acid receptor 1 and their use for treatment of diseases WO2020104578A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18207521.8 2018-11-21
EP18207521 2018-11-21

Publications (2)

Publication Number Publication Date
WO2020104578A2 WO2020104578A2 (en) 2020-05-28
WO2020104578A3 true WO2020104578A3 (en) 2020-07-23

Family

ID=64650102

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2019/082057 WO2020104578A2 (en) 2018-11-21 2019-11-21 Modulators of free fatty acid receptor 1 and their use for treatment of diseases

Country Status (1)

Country Link
WO (1) WO2020104578A2 (en)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2216330A1 (en) * 2007-10-24 2010-08-11 Astellas Pharma Inc. Oxadiazolidinedione compound
CN106928246A (en) * 2017-03-09 2017-07-07 北京宜生堂医药科技研究有限公司 A kind of compound and preparation method thereof and purposes
CN108033927A (en) * 2017-10-27 2018-05-15 北京宜生堂医药科技研究有限公司 A kind of compound and its preparation method and application
WO2018122775A1 (en) * 2016-12-29 2018-07-05 Minoryx Therapeutics S.L. Heteroaryl compounds and their use

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2216330A1 (en) * 2007-10-24 2010-08-11 Astellas Pharma Inc. Oxadiazolidinedione compound
WO2018122775A1 (en) * 2016-12-29 2018-07-05 Minoryx Therapeutics S.L. Heteroaryl compounds and their use
CN106928246A (en) * 2017-03-09 2017-07-07 北京宜生堂医药科技研究有限公司 A kind of compound and preparation method thereof and purposes
CN108033927A (en) * 2017-10-27 2018-05-15 北京宜生堂医药科技研究有限公司 A kind of compound and its preparation method and application

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
14 March 2019 (2019-03-14), pages 1 - 21, XP055665086, Retrieved from the Internet <URL:https://www.pnas.org/highwire/filestream/854687/field_highwire_adjunct_files/0/pnas.1811066116.sapp.pdf> [retrieved on 20200204] *
ELEAZU CHINEDUM ET AL: "Free fatty acid receptor 1 as a novel therapeutic target for type 2 diabetes mellitus-current status", CHEMICO-BIOLOGICAL INTERACTIONS, ELSEVIER SCIENCE IRLAND, IR, vol. 289, 25 April 2018 (2018-04-25), pages 32 - 39, XP085398603, ISSN: 0009-2797, DOI: 10.1016/J.CBI.2018.04.026 *
HAN CAO ET AL: "Synthesis, Characterization, and Biological Evaluations of 1,3,5-Triazine Derivatives of Metformin Cyclization with Berberine and Magnolol in the Presence of Sodium Methylate", MOLECULES ONLINE, vol. 22, no. 10, 1 October 2017 (2017-10-01), DE, pages 1752, XP055589736, ISSN: 1433-1373, DOI: 10.3390/molecules22101752 *
MICHAEL LÜCKMANN ET AL: "Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES, vol. 116, no. 14, 14 March 2019 (2019-03-14), US, pages 7123 - 7128, XP055665079, ISSN: 0027-8424, DOI: 10.1073/pnas.1811066116 *
PARK H ET AL: "Discovery and biological evaluation of novel @a-glucosidase inhibitors with in vivo antidiabetic effect", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 18, no. 13, 1 July 2008 (2008-07-01), pages 3711 - 3715, XP022716281, ISSN: 0960-894X, [retrieved on 20080520], DOI: 10.1016/J.BMCL.2008.05.056 *

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Publication number Publication date
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