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WO2020175957A1 - Composés dérivés d'amide de pirazole et leur utilisation - Google Patents

Composés dérivés d'amide de pirazole et leur utilisation Download PDF

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Publication number
WO2020175957A1
WO2020175957A1 PCT/KR2020/002897 KR2020002897W WO2020175957A1 WO 2020175957 A1 WO2020175957 A1 WO 2020175957A1 KR 2020002897 W KR2020002897 W KR 2020002897W WO 2020175957 A1 WO2020175957 A1 WO 2020175957A1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutically acceptable
acceptable salt
amide derivative
optical isomer
derivative compound
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/KR2020/002897
Other languages
English (en)
Korean (ko)
Inventor
양민규
김좌진
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.)
Mother"s Pharmaceutical Co ltd
Original Assignee
Mother"s Pharmaceutical Co ltd
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 Mother"s Pharmaceutical Co ltd filed Critical Mother"s Pharmaceutical Co ltd
Publication of WO2020175957A1 publication Critical patent/WO2020175957A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Definitions

  • the present invention relates to a pyrazole amide derivative compound and its use.
  • [16] and 11 2 are each independently or 0-04 alkyl.
  • a pharmaceutically acceptable salt refers to a salt commonly used in the pharmaceutical industry, for example, an inorganic ion salt made of calcium, potassium, sodium and magnesium; hydrochloric acid, nitric acid, phosphoric acid, Inorganic acid salts prepared from bromic acid, iodic acid, perchloric acid and sulfuric acid; acetic acid, trifluoroacetic acid, citric acid, maleic acid, 2020/175957 1»(:1 ⁇ 1 ⁇ 2020/002897 Succinic acid, oxalic acid, benzoic acid, tartaric acid, fumaric acid, manderic acid, propionic acid, lactic acid, glycolic acid, gluconic acid, galacturonic acid, glutamic acid, glutaric acid, glucu Organic acid salts made of Ronic acid, aspartic acid, ascorbic acid, carboxylic acid, vanillic acid, hydroiodic acid, etc.; methanesulfonic acid, ethanes
  • the present invention provides a use of a pyrazole amide derivative compound represented by the following formula (1), an optical isomer thereof, or a pharmaceutically acceptable salt thereof.
  • the pharmaceutical composition of the present invention may contain one or more active ingredients that exhibit the same or similar drug efficacy.
  • Silver TBS-T buffer (40 mM Tris-HCl pH 7.4, 25 mM NaCl, 0.1% Tween-20) was added with 5% non-fat dry milk or 5% bovine serum albumin to inhibit non-specific binding with antibodies. The reaction was carried out on a shaker for 1 hour. After that, the blocking solution was reacted with an antibody for 2 hours at room temperature, and washed 5 times with TBS-T buffer for 5 minutes each, followed by HRP-conjugated reaction with the primary antibody. The secondary antibody was added to the blocking solution and reacted for 2 hours under the same conditions as the primary antibody. After washing 5 times with TBS-T buffer for 5 minutes each, the film was sensitized using an ECL system in a dark room to observe the expression pattern of each protein.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne un composé dérivé possédant une structure d'amide de pirazole, un énantiomère de celui-ci ou un sel pharmaceutiquement acceptable de celui-ci. Selon la présente invention, le composé dérivé d'amide de pyrazole, l'énantiomère de celui-ci et le sel pharmaceutiquement acceptable de celui-ci, en inhibant la mitsugumine 53 (MG53), peuvent augmenter la sécrétion d'insuline, et même lorsqu'ils sont pris sur une longue période, peuvent abaisser les taux de glycémie très efficacement sans induire d'hypoglycémie, tout en ayant une fonction de protection sur les cellules bêta pancréatiques, et en même temps, résoudre de façon spectaculaire le problème de prise de poids et de résistance à l'insuline.
PCT/KR2020/002897 2019-02-28 2020-02-28 Composés dérivés d'amide de pirazole et leur utilisation Ceased WO2020175957A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2019-0023970 2019-02-28
KR20190023970 2019-02-28

Publications (1)

Publication Number Publication Date
WO2020175957A1 true WO2020175957A1 (fr) 2020-09-03

Family

ID=72239640

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2020/002897 Ceased WO2020175957A1 (fr) 2019-02-28 2020-02-28 Composés dérivés d'amide de pirazole et leur utilisation

Country Status (2)

Country Link
KR (1) KR102396602B1 (fr)
WO (1) WO2020175957A1 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008008286A2 (fr) * 2006-07-12 2008-01-17 Merck & Co., Inc. Pyrazoles substitués servant d'antagonistes des récepteurs de la ghréline
WO2008149379A2 (fr) * 2007-06-06 2008-12-11 Torrent Pharmaceuticals Ltd. Nouveaux composés
US20100190979A1 (en) * 2005-11-28 2010-07-29 David Robert Bolin Diacylglycerol acyltransferase inhibitors
KR20140029517A (ko) * 2011-06-09 2014-03-10 에프. 호프만-라 로슈 아게 피라졸 유도체
WO2016027253A1 (fr) * 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Amides hétérocycliques utilisés comme inhibiteurs de la rip1 kinase en tant que médicaments

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100190979A1 (en) * 2005-11-28 2010-07-29 David Robert Bolin Diacylglycerol acyltransferase inhibitors
WO2008008286A2 (fr) * 2006-07-12 2008-01-17 Merck & Co., Inc. Pyrazoles substitués servant d'antagonistes des récepteurs de la ghréline
WO2008149379A2 (fr) * 2007-06-06 2008-12-11 Torrent Pharmaceuticals Ltd. Nouveaux composés
KR20140029517A (ko) * 2011-06-09 2014-03-10 에프. 호프만-라 로슈 아게 피라졸 유도체
WO2016027253A1 (fr) * 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Amides hétérocycliques utilisés comme inhibiteurs de la rip1 kinase en tant que médicaments

Also Published As

Publication number Publication date
KR20200105443A (ko) 2020-09-07
KR102396602B1 (ko) 2022-05-11

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