TW202011965A - 嗜中性球彈性蛋白酶抑制劑在肝病中之用途 - Google Patents

嗜中性球彈性蛋白酶抑制劑在肝病中之用途 Download PDF

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Publication number
TW202011965A
TW202011965A TW108114343A TW108114343A TW202011965A TW 202011965 A TW202011965 A TW 202011965A TW 108114343 A TW108114343 A TW 108114343A TW 108114343 A TW108114343 A TW 108114343A TW 202011965 A TW202011965 A TW 202011965A
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Taiwan
Prior art keywords
compound
phenyl
solvates
day
liver disease
Prior art date
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TW108114343A
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English (en)
Chinese (zh)
Inventor
山吉夫 沙特亞爾
布萊恩 羅伯特斯
王學燕
史考特 薩維吉
顥寧 許
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韓商Ｐｈ製藥公司
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Publication of TW202011965A publication Critical patent/TW202011965A/zh

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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/26—Glucagons
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Zoology (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)
TW108114343A 2018-04-24 2019-04-24 嗜中性球彈性蛋白酶抑制劑在肝病中之用途 TW202011965A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862662074P 2018-04-24 2018-04-24
US62/662,074 2018-04-24

Publications (1)

Publication Number Publication Date
TW202011965A true TW202011965A (zh) 2020-04-01

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TW108114343A TW202011965A (zh) 2018-04-24 2019-04-24 嗜中性球彈性蛋白酶抑制劑在肝病中之用途

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Country Link
US (2) US10806735B2 (enExample)
EP (1) EP3784657A4 (enExample)
JP (1) JP2021522247A (enExample)
KR (1) KR20210002573A (enExample)
CN (1) CN113614070A (enExample)
AU (2) AU2019257632A1 (enExample)
CA (1) CA3101274A1 (enExample)
IL (1) IL278207A (enExample)
SG (1) SG11202010521VA (enExample)
TW (1) TW202011965A (enExample)
WO (1) WO2019209738A1 (enExample)

Families Citing this family (10)

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Publication number Priority date Publication date Assignee Title
CN121081472A (zh) 2018-12-13 2025-12-09 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
CA3154488A1 (en) 2019-08-23 2021-03-04 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
CA3154391A1 (en) 2019-09-12 2021-03-18 Terns Pharmaceuticals, Inc. Thyroid hormone receptor beta agonist compounds
US11478533B2 (en) 2020-04-27 2022-10-25 Novo Nordisk A/S Semaglutide for use in medicine
PE20231096A1 (es) 2020-08-25 2023-07-18 Lilly Co Eli Polimorfos de un inhibidor de ssao
EP4210705A4 (en) * 2020-09-11 2024-11-13 Terns Pharmaceuticals, Inc. SOLID DISPERSION FORMULATIONS OF A FXR AGONIST
CN114085173B (zh) * 2021-10-18 2024-04-16 嘉兴学院 一种2-硝基-4-甲砜基苯甲醛的制备方法
CN115976192A (zh) * 2022-12-02 2023-04-18 西安华壹健康医学检验实验室有限公司 一种用ne基因表达量检测评估脂肪肝的方法
CN117357508B (zh) * 2023-11-03 2024-05-17 中山大学孙逸仙纪念医院 西维来司他在制备治疗原发性胆汁性胆管炎的药物中的应用
CN119499379B (zh) * 2024-09-23 2025-09-05 广东医科大学 Elane基因作为心力衰竭靶点的制药用途和西维来司他的新用途

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Publication number Priority date Publication date Assignee Title
HRP20120457T1 (hr) * 2007-12-20 2012-06-30 Bayer Pharma Aktiengesellschaft 4-(4-cijano-2-tioaril)dihidropirimidinoni i njihova uporaba
US9475779B2 (en) * 2014-07-31 2016-10-25 Boehringer Ingelheim International Gmbh Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
AU2015314830B2 (en) * 2014-09-12 2021-01-07 Tobira Therapeutics, Inc. Cenicriviroc combination therapy for the treatment of fibrosis
WO2016050835A2 (en) 2014-10-02 2016-04-07 Ruprecht-Karls-Universität Heidelberg Selective inhibitors of neutrophil elastase for treating neuropathic pain and chronic pain states harbouring a neuropathic component
MX2017008844A (es) * 2015-01-09 2018-03-14 Gilead Apollo Llc Terapia de combinacion con inhibidor de acetil-coa carboxilasa (acc) para el tratamiento de enfermedad de higado graso no alcoholico.
CA2980071A1 (en) 2015-03-18 2016-09-22 Bayer Pharma Aktiengesellschaft Method for preparation of (4s)-4-[4-cyano-2-(methylsulfonyl)phenyl]-3,6-dimethyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2,3,4-tetrahydro pyrimidine-5-carbonitrile
CN107613986A (zh) * 2015-04-07 2018-01-19 英特塞普特医药品公司 用于组合疗法的药物组合物
WO2017081044A1 (en) 2015-11-13 2017-05-18 Bayer Pharma Aktiengesellschaft 4-(4-cyano-2-thioaryl)dihydropyrimidinones for treating chronic wounds
GB201608453D0 (en) 2016-05-13 2016-06-29 Univ Liverpool Muscle regeneration
KR102399254B1 (ko) * 2016-09-28 2022-05-17 아이거 바이오파마슈티컬스 인코포레이티드 비-알코올성 지방간염의 치료를 위한 방법 및 약제학적 조성물

Also Published As

Publication number Publication date
WO2019209738A1 (en) 2019-10-31
EP3784657A4 (en) 2022-02-09
US10806735B2 (en) 2020-10-20
JP2021522247A (ja) 2021-08-30
AU2019257632A1 (en) 2020-11-26
US20210069192A1 (en) 2021-03-11
IL278207A (en) 2020-11-30
KR20210002573A (ko) 2021-01-08
US20190321364A1 (en) 2019-10-24
SG11202010521VA (en) 2020-11-27
EP3784657A1 (en) 2021-03-03
AU2024227697A1 (en) 2024-11-21
CA3101274A1 (en) 2019-10-31
CN113614070A (zh) 2021-11-05

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