JP2024532129A - Ｐｃｓｋ９活性に関連する状態を治療するための化合物 - Google Patents

Ｐｃｓｋ９活性に関連する状態を治療するための化合物 Download PDF

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JP2024532129A
JP2024532129A JP2024509031A JP2024509031A JP2024532129A JP 2024532129 A JP2024532129 A JP 2024532129A JP 2024509031 A JP2024509031 A JP 2024509031A JP 2024509031 A JP2024509031 A JP 2024509031A JP 2024532129 A JP2024532129 A JP 2024532129A
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compound
formula
subject
pharmaceutical composition
amount
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JP2024532129A5 (https=
Inventor
ジョーンズ，ダグラス・ジー
バンカ，プージャ
ジョウ，ゼシュン
クラパラ，アーティス
ツァイ，フー－ロン
コン，ジョンロク
ヴァルソローナ，リチャード・ジェイ
デスモンド，リチャード
マリグレス，ピーター・イー
マロータ，メラニー
アレイン，キャンディス
オコー，グレイス・エー
ディヌンツィオ，ジェームズ・シー
ノフシンガー，レベッカ
リ，リ
スミス，ダニエル・ジェー
マジョール，マジッド
ケプリンガー，ケネス・アラン
ション，ユシェン
ウェフリング，ピーター・ダブリュー
ヒギンズ，ジョン・ディー
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メルク・シャープ・アンド・ドーム・エルエルシー
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Publication of JP2024532129A publication Critical patent/JP2024532129A/ja
Publication of JP2024532129A5 publication Critical patent/JP2024532129A5/ja
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4891—Coated capsules; Multilayered drug free capsule shells
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024509031A 2021-08-19 2022-08-18 Ｐｃｓｋ９活性に関連する状態を治療するための化合物 Pending JP2024532129A (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US202163234973P 2021-08-19 2021-08-19
US63/234,973 2021-08-19
US202163251972P 2021-10-04 2021-10-04
US63/251,972 2021-10-04
US202163263095P 2021-10-27 2021-10-27
US63/263,095 2021-10-27
US202263311622P 2022-02-18 2022-02-18
US63/311,622 2022-02-18
US202263371685P 2022-08-17 2022-08-17
US63/371,685 2022-08-17
PCT/US2022/040747 WO2023023245A1 (en) 2021-08-19 2022-08-18 Compounds for treating conditions related to pcsk9 activity

Publications (2)

Publication Number Publication Date
JP2024532129A true JP2024532129A (ja) 2024-09-05
JP2024532129A5 JP2024532129A5 (https=) 2025-12-25

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JP2024509031A Pending JP2024532129A (ja) 2021-08-19 2022-08-18 Ｐｃｓｋ９活性に関連する状態を治療するための化合物

Country Status (9)

Country Link
US (1) US20240238367A1 (https=)
EP (1) EP4387645A1 (https=)
JP (1) JP2024532129A (https=)
KR (1) KR20240050369A (https=)
AU (1) AU2022330007A1 (https=)
CA (1) CA3228604A1 (https=)
IL (1) IL310851A (https=)
MX (1) MX2024002146A (https=)
WO (1) WO2023023245A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025042927A2 (en) * 2023-08-24 2025-02-27 Merck Sharp & Dohme Llc Sustained-release formulations for poorly permeable cyclic peptides

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20190389909A1 (en) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

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US5104869A (en) 1989-10-11 1992-04-14 American Cyanamid Company Renin inhibitors
US5114937A (en) 1989-11-28 1992-05-19 Warner-Lambert Company Renin inhibiting nonpeptides
US5095119A (en) 1990-03-08 1992-03-10 American Home Products Corporation Renin inhibitors
US6054587A (en) 1997-03-07 2000-04-25 Metabasis Therapeutics, Inc. Indole and azaindole inhibitors of fructose-1,6-bisphosphatase
US6284748B1 (en) 1997-03-07 2001-09-04 Metabasis Therapeutics, Inc. Purine inhibitors of fructose 1,6-bisphosphatase
DE69819311T2 (de) 1997-03-07 2004-07-29 Metabasis Therapeutics Inc., San Diego Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase
KR100818845B1 (ko) 1998-09-09 2008-04-01 메타베이시스 테라퓨틱스, 인크. 신규한 프럭토스 1,6-비스포스파타제의 헤테로방향족 억제제
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
EP1357908A4 (en) 2001-01-30 2009-07-15 Merck & Co Inc "ACYLSULFAMIDES FOR THE TREATMENT OF FATIBILITY, DIABETES AND LIPID DISORDERS"
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
CN100457730C (zh) 2002-08-29 2009-02-04 默克公司 具有抗糖尿病活性的吲哚化合物
EP1546142A4 (en) 2002-08-29 2007-10-17 Merck & Co Inc INDOLES HAVING ANTIDIABETIC EFFECT
AU2004207444B2 (en) 2003-01-17 2008-07-31 Merck & Co., Inc. N-cyclohexylaminocarbonyl benzenesulfonamide derivatives
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US20190389909A1 (en) * 2018-06-21 2019-12-26 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

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Publication number Publication date
MX2024002146A (es) 2024-03-08
AU2022330007A1 (en) 2024-02-15
CA3228604A1 (en) 2023-02-23
IL310851A (en) 2024-04-01
KR20240050369A (ko) 2024-04-18
EP4387645A1 (en) 2024-06-26
US20240238367A1 (en) 2024-07-18
WO2023023245A1 (en) 2023-02-23

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