KR20240050369A - Pcsk9 활성과 관련된 상태를 치료하기 위한 화합물 - Google Patents

Pcsk9 활성과 관련된 상태를 치료하기 위한 화합물 Download PDF

Info

Publication number
KR20240050369A
KR20240050369A KR1020247008443A KR20247008443A KR20240050369A KR 20240050369 A KR20240050369 A KR 20240050369A KR 1020247008443 A KR1020247008443 A KR 1020247008443A KR 20247008443 A KR20247008443 A KR 20247008443A KR 20240050369 A KR20240050369 A KR 20240050369A
Authority
KR
South Korea
Prior art keywords
compound
formula
subject
amount
ldl
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.)
Pending
Application number
KR1020247008443A
Other languages
English (en)
Korean (ko)
Inventor
더글라스 지. 존스
푸자 반카
제쉔 주
아티스 클라파라
푸롱 차이
종락 공
리차드 제이. 바르솔로나
리차드 데스몬드
피터 이. 말리그레스
멜라니 마로타
캔디스 알리니
그레이스 에이. 오코
제임스 씨. 디눈지오
레베카 노프싱어
리 리
다니엘 제이. 스미스
마지드 마주르
케네스 앨런 쾨플링거
유쉥 시옹
피터 더블유. 위플링
존 디. 히긴스
Original Assignee
머크 샤프 앤드 돔 엘엘씨
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 머크 샤프 앤드 돔 엘엘씨 filed Critical 머크 샤프 앤드 돔 엘엘씨
Publication of KR20240050369A publication Critical patent/KR20240050369A/ko
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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
    • 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

Landscapes

  • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dispersion Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020247008443A 2021-08-19 2022-08-18 Pcsk9 활성과 관련된 상태를 치료하기 위한 화합물 Pending KR20240050369A (ko)

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 (1)

Publication Number Publication Date
KR20240050369A true KR20240050369A (ko) 2024-04-18

Family

ID=83319263

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020247008443A Pending KR20240050369A (ko) 2021-08-19 2022-08-18 Pcsk9 활성과 관련된 상태를 치료하기 위한 화합물

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

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3841520A1 (de) 1988-12-09 1990-06-13 Hoechst Ag Enzymhemmende harnstoffderivate von dipeptiden, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung
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
DE69819311T2 (de) 1997-03-07 2004-07-29 Metabasis Therapeutics Inc., San Diego Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase
US6054587A (en) 1997-03-07 2000-04-25 Metabasis Therapeutics, Inc. Indole and azaindole inhibitors of fructose-1,6-bisphosphatase
AU6452098A (en) 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
ATE246197T1 (de) 1998-09-09 2003-08-15 Metabasis Therapeutics Inc Neue heteroaromatische fructose 1,6- bisphosphatase inhibitoren
WO2002008188A1 (en) 2000-07-25 2002-01-31 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
WO2002060388A2 (en) 2001-01-30 2002-08-08 Merck & Co., Inc. Acyl sulfamides for treatment of obesity, 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
WO2004019869A2 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
WO2004020408A1 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
JP2007504285A (ja) 2003-01-17 2007-03-01 メルク　エンド　カムパニー　インコーポレーテッド Ｎ−シクロヘキシルアミノカルボニルベンゼンスルホンアミド誘導体
AU2008267724A1 (en) 2007-06-28 2008-12-31 Merck Frosst Canada Ltd Substituted fused pyrimidines as antagonists of GPR105 activity
EP2174343A1 (en) 2007-06-28 2010-04-14 Semiconductor Energy Laboratory Co, Ltd. Manufacturing method of semiconductor device
WO2009042053A2 (en) 2007-09-21 2009-04-02 Merck & Co., Inc. Neuromedin u receptor agonists and uses thereof
IL279363B2 (en) * 2018-06-21 2025-12-01 Merck Sharp & Dohme Pcsk9 antagonist compounds
EP4021919A1 (en) * 2019-08-30 2022-07-06 Merck Sharp & Dohme Corp. Pcsk9 antagonist compounds

Also Published As

Publication number Publication date
WO2023023245A1 (en) 2023-02-23
IL310851A (en) 2024-04-01
MX2024002146A (es) 2024-03-08
AU2022330007A1 (en) 2024-02-15
CA3228604A1 (en) 2023-02-23
JP2024532129A (ja) 2024-09-05
EP4387645A1 (en) 2024-06-26
US20240238367A1 (en) 2024-07-18

Similar Documents

Publication Publication Date Title
JP7607615B2 (ja) Ｐｃｓｋ９アンタゴニスト化合物
CN102091330B (zh) 含有缬沙坦和nep抑制剂的药物组合物
RU2298418C2 (ru) Комбинация по меньшей мере двух соединений, выбранных из групп антагонистов at1-рецептора или ингибиторов асе (ангиотензинпревращающий фермент), или ингибиторов hmg-coa-редуктазы (бета-гидрокси-бета-метилглутарил-кофермент-а-редуктаза)
US11306125B2 (en) PCSK9 antagonists bicyclo-compounds
EP3525784B1 (en) Sparsentan for use in the treatment of alport syndrome
JP2007509982A5 (https=)
JP2004514703A (ja) 有機化合物の組合せ剤
JP2016512234A (ja) 薬学的複合製剤
JP2016537353A (ja) 脂肪酸ナイアシン複合体
EP3860594B1 (en) Biphenyl sulfonamide compounds for the treatment of type iv collagen diseases
US20240238367A1 (en) Compounds for treating conditions related to pcsk9 activity
CN118159281A (zh) 治疗pcsk9活性相关病况的化合物
CN101829069B (zh) 匹伐他汀钙双层渗透泵控释片及其制备方法
TWI222883B (en) Pharmaceutical mixture comprising a combination of a profen and other active compounds
US20070299054A1 (en) Oral pharmaceutical composition of a poorly water-soluble active agent
AU2007263016A1 (en) Oral pharmaceutical composition of a poorly water-soluble active substance
HK40059411B (en) Biphenyl sulfonamide compounds for the treatment of type iv collagen diseases
HK1143095A1 (en) Zibotentan composition containing mannitol and microcrystalline cellulose
MX2008016418A (es) Composicion farmaceutica oral de una sustancia activa escasamente soluble en agua.

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

P11 Amendment of application requested

Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-NAP-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000