CA3076889A1 - Compositions and methods of reducing serum cholesterol and pcsk9 - Google Patents

Compositions and methods of reducing serum cholesterol and pcsk9 Download PDF

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Publication number
CA3076889A1
CA3076889A1 CA3076889A CA3076889A CA3076889A1 CA 3076889 A1 CA3076889 A1 CA 3076889A1 CA 3076889 A CA3076889 A CA 3076889A CA 3076889 A CA3076889 A CA 3076889A CA 3076889 A1 CA3076889 A1 CA 3076889A1
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CA
Canada
Prior art keywords
inhibitor
cholesterol
gtoreq
akr1a1
ldl
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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.)
Pending
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CA3076889A
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English (en)
French (fr)
Inventor
Jonathan S. Stamler
Original Assignee
Case Western Reserve University
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Application filed by Case Western Reserve University filed Critical Case Western Reserve University
Publication of CA3076889A1 publication Critical patent/CA3076889A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4174—Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA3076889A 2017-09-25 2018-09-21 Compositions and methods of reducing serum cholesterol and pcsk9 Pending CA3076889A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762562784P 2017-09-25 2017-09-25
US62/562,784 2017-09-25
PCT/US2018/052214 WO2019060720A1 (en) 2017-09-25 2018-09-21 COMPOSITIONS AND METHODS FOR REDUCING SERUM CHOLESTEROL AND PCSK9

Publications (1)

Publication Number Publication Date
CA3076889A1 true CA3076889A1 (en) 2019-03-28

Family

ID=65810650

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3076889A Pending CA3076889A1 (en) 2017-09-25 2018-09-21 Compositions and methods of reducing serum cholesterol and pcsk9

Country Status (6)

Country Link
US (2) US11576900B2 (enExample)
EP (1) EP3688163A4 (enExample)
JP (2) JP7414712B2 (enExample)
CN (2) CN118512442A (enExample)
CA (1) CA3076889A1 (enExample)
WO (1) WO2019060720A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7414712B2 (ja) * 2017-09-25 2024-01-16 ケース ウエスタン リザーブ ユニバーシティ 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法
EP3852750A4 (en) * 2018-09-21 2022-05-11 Case Western Reserve University Aldoketo reductase inhibitors and uses thereof
CN113648427B (zh) * 2021-08-20 2023-07-28 山东大学 透明质酸-es2-af肽偶联物及其制备方法和应用
CN117427170A (zh) * 2023-11-15 2024-01-23 首都医科大学附属北京安贞医院 Krt18蛋白在制备降低胆固醇的药物中的用途

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JPS58140020A (ja) 1982-02-13 1983-08-19 Nippon Zoki Pharmaceut Co Ltd 脂質代謝改善剤
US4436745A (en) 1982-04-15 1984-03-13 Alcon Laboratories, Inc. Method of inhibiting aldose reductase activity
IL68314A0 (en) * 1982-04-15 1983-07-31 Alcon Lab Inc Method and composition for inhibiting aldose reductase activity and process for preparing spirofluorofluoren and spiro-difluorofluoren compounds
US5153211A (en) 1983-09-14 1992-10-06 Alcon Laboratories, Inc. Spiro-tricyclicaromatic succinimide derivatives as inhibitors of aldose reductase
US20020132845A1 (en) 2000-12-15 2002-09-19 Miller Guy Michael Compositions and methods for the prevention and treatment of tissue ischemia
WO2002098510A1 (en) * 2001-06-07 2002-12-12 Wyeth Combination of a ptpase inhibitor and an aldose reductase inhibitor
EP1431399A1 (en) 2002-12-20 2004-06-23 Clinigenetics Methods and composition for identifying therapeutic agents of atherosclerotic plaque lesions
JP4544503B2 (ja) 2003-04-15 2010-09-15 株式会社アミノアップ化学 雲南苦丁茶成分を含有する組成物
AU2004251690A1 (en) 2003-06-04 2005-01-06 Duke University Compositions and methods for modulating S-nitrosoglutathione reductase
JP2007015924A (ja) 2003-06-12 2007-01-25 Sanwa Kagaku Kenkyusho Co Ltd 抗癌剤耐性を克服する薬剤及びそのスクリーニング方法
US20100292178A1 (en) 2003-07-21 2010-11-18 Jeffrey Young Method of treating non-insulin dependent diabetes mellitus and related complications
US9308206B2 (en) 2004-08-23 2016-04-12 The Board Of Regents Of The University Of Texas System Compositions and methods for treating colon cancer
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FR2885904B1 (fr) 2005-05-19 2007-07-06 Aventis Pharma Sa Nouveaux derives du fluorene, compositions les contenant et utilisation
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EP1987829A4 (en) 2006-02-20 2009-07-29 Sanwa Kagaku Kenkyusho Co PROPHYLACTIC OR THERAPEUTIC AGENT FOR LESIONS DUE TO BRAIN ISCHEMIA OR LESIONS DUE TO BRAIN ISCHEMIA WITH REPERFUSION IN BRAIN VASCULAR ACCIDENTS
JP2010510248A (ja) 2006-11-21 2010-04-02 ビアメト ファーマシューティカルズ，インク． 金属結合部分をターゲティング部分と組み合わせて使用する金属酸化還元酵素阻害剤
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US20150335615A1 (en) * 2013-01-04 2015-11-26 Toshihisa Kawai Cholesterol-lowering compounds in combination with lipid metabolism-altering compounds of non-absorbable sugars, compounds that convert nh3 to nh4+, or hydrogen-generating compounds for the treatment of high cholesterol and inflammation
EP3179995B1 (en) 2014-08-12 2018-11-07 University of Pécs (Pécsi Tudományegyetem) Methods and materials for reducing ischemia-reperfusion injury
EP3226859B1 (en) * 2014-12-05 2025-03-26 Case Western Reserve University Akr1a1 inhibitors for use in lowering cholesterol and modulate s-nitrosylation
US10537557B2 (en) 2016-01-27 2020-01-21 Case Western Reserve University Methods of treating respiratory disorders
JP7414712B2 (ja) * 2017-09-25 2024-01-16 ケース ウエスタン リザーブ ユニバーシティ 血清コレステロールおよびｐｃｓｋ９を低減する組成物および方法
EP3852750A4 (en) * 2018-09-21 2022-05-11 Case Western Reserve University Aldoketo reductase inhibitors and uses thereof
WO2021061763A1 (en) * 2019-09-23 2021-04-01 Case Western Reserve University Aldoketo reductase inhibitors and uses thereof

Also Published As

Publication number Publication date
CN118512442A (zh) 2024-08-20
EP3688163A4 (en) 2022-12-14
WO2019060720A1 (en) 2019-03-28
JP2020535142A (ja) 2020-12-03
CN111356764A (zh) 2020-06-30
JP7414712B2 (ja) 2024-01-16
CN111356764B (zh) 2024-05-24
US11576900B2 (en) 2023-02-14
JP2024001162A (ja) 2024-01-09
US20230190710A1 (en) 2023-06-22
US20200268717A1 (en) 2020-08-27
EP3688163A1 (en) 2020-08-05

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