EA201691328A1 - Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы - Google Patents

Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы

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Publication number
EA201691328A1
EA201691328A1 EA201691328A EA201691328A EA201691328A1 EA 201691328 A1 EA201691328 A1 EA 201691328A1 EA 201691328 A EA201691328 A EA 201691328A EA 201691328 A EA201691328 A EA 201691328A EA 201691328 A1 EA201691328 A1 EA 201691328A1
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EA
Eurasian Patent Office
Prior art keywords
haa
xaa
diseases
infections
elastase
Prior art date
Application number
EA201691328A
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English (en)
Other versions
EA034910B1 (ru
Inventor
Фран Отто Гомберт
Даниэль Обрехт
Одиль Селье-Кесслер
Original Assignee
Полифор Аг
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Publication date
Application filed by Полифор Аг filed Critical Полифор Аг
Publication of EA201691328A1 publication Critical patent/EA201691328A1/ru
Publication of EA034910B1 publication Critical patent/EA034910B1/ru

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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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C07K1/061—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using protecting groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/10—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Analytical Chemistry (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)

Abstract

β-Шпилечные пептидомиметики общей формулы цикло(-Хаа-Хаа-Thr-Хаа-Ser-Хаа-Хаа-Хаа-Хаа-Хаа-Хаа-Хаа-Хаа-) и их фармацевтически приемлемые соли, причем Хаа, Хаа, Хаа, Хаа, Хаа, Хаа, Хаа, Хаа, Хаа, Хааи Хаапредставляют собой аминокислотные остатки, которые определены в описании изобретения и в формуле изобретения, имеют ингибирующие свойства в отношении эластазы, особенно в отношении человеческой нейтрофильной эластазы, и могут применяться для профилактики инфекций или заболеваний, связанных с такими инфекциями, у здоровых субъектов или для уменьшения инфекций у инфицированных пациентов. Соединения согласно настоящему изобретению могут также применяться, когда рак, или иммунологические заболевания, или легочные заболевания, или сердечно-сосудистые заболевания, или нейродегенеративные заболевания, или воспаление, или заболевания, связанные с воспалением, опосредованы или являются результатом эластазной активности. Эти пептидомиметики могут быть получены способом, который основан на смешанной стратегии твердофазного синтеза и синтеза в растворе.
EA201691328A 2013-12-27 2013-12-27 Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы EA034910B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2013/078072 WO2015096872A1 (en) 2013-12-27 2013-12-27 Beta-hairpin peptidomimetics as selective elastase inhibitors

Publications (2)

Publication Number Publication Date
EA201691328A1 true EA201691328A1 (ru) 2016-10-31
EA034910B1 EA034910B1 (ru) 2020-04-06

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EA201691328A EA034910B1 (ru) 2013-12-27 2013-12-27 Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы

Country Status (15)

Country Link
US (2) US10723765B2 (ru)
EP (1) EP3087087B1 (ru)
JP (1) JP6499182B2 (ru)
KR (1) KR102214693B1 (ru)
CN (1) CN105873939B (ru)
AU (1) AU2013409231B2 (ru)
BR (1) BR112016015018B1 (ru)
CA (1) CA2933656C (ru)
EA (1) EA034910B1 (ru)
ES (1) ES2957258T3 (ru)
IL (1) IL246108B (ru)
MX (1) MX2016008468A (ru)
NZ (1) NZ722030A (ru)
SG (1) SG11201605186QA (ru)
WO (1) WO2015096872A1 (ru)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA017583B1 (ru) 2007-02-28 2013-01-30 Полифор Лтд. Закрепленные на матрице пептидомиметики
ES2925747T3 (es) * 2013-12-27 2022-10-19 Spexis Ag Peptidomiméticos de horquilla beta como inhibidores selectivos de elastasa
WO2017207118A1 (en) * 2016-05-31 2017-12-07 Polyphor Ag Beta-hairpin peptidomimetic with elastase inhibitory activity and aerosol dosage forms thereof
US20220354833A1 (en) 2019-09-17 2022-11-10 Mereo Biopharma 4 Limited Alvelestat for use in the treatment of graft rejection, bronchiolitis obliterans syndrome and graft versus host disease
EP4252850A3 (en) 2020-04-16 2023-11-15 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
WO2023067103A1 (en) 2021-10-20 2023-04-27 Mereo Biopharma 4 Limited Neutrophil elastase inhibitors for use in the treatment of fibrosis

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5595756A (en) * 1993-12-22 1997-01-21 Inex Pharmaceuticals Corporation Liposomal compositions for enhanced retention of bioactive agents
GB9825854D0 (en) 1998-11-25 1999-01-20 Univ Bristol Peptide
CN1386759A (zh) * 2001-05-17 2002-12-25 上海博德基因开发有限公司 一种多肽——弹性蛋白酶抑制剂－43.12和编码这种多肽的多核苷酸
CN101157924A (zh) 2001-12-11 2008-04-09 人体基因组科学有限公司 嗜中性白细胞因子α
EP1856140B1 (en) * 2005-02-17 2013-12-25 Polyphor Ltd. Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity
CN102499925B (zh) * 2011-10-21 2015-11-11 上海中医药大学 一种中性粒细胞弹性蛋白酶抑制剂
ES2925747T3 (es) * 2013-12-27 2022-10-19 Spexis Ag Peptidomiméticos de horquilla beta como inhibidores selectivos de elastasa

Also Published As

Publication number Publication date
EP3087087B1 (en) 2021-07-21
US20200317735A1 (en) 2020-10-08
MX2016008468A (es) 2016-09-26
KR102214693B1 (ko) 2021-02-10
NZ722030A (en) 2019-06-28
JP6499182B2 (ja) 2019-04-10
JP2017504619A (ja) 2017-02-09
CA2933656C (en) 2021-04-20
CN105873939B (zh) 2021-08-27
SG11201605186QA (en) 2016-07-28
CN105873939A (zh) 2016-08-17
ES2957258T3 (es) 2024-01-16
AU2013409231A1 (en) 2016-07-21
US10723765B2 (en) 2020-07-28
EP3087087A1 (en) 2016-11-02
EA034910B1 (ru) 2020-04-06
KR20160102068A (ko) 2016-08-26
AU2013409231B2 (en) 2019-08-01
IL246108A0 (en) 2016-07-31
IL246108B (en) 2021-06-30
BR112016015018A2 (ru) 2017-08-08
WO2015096872A1 (en) 2015-07-02
US20160318976A1 (en) 2016-11-03
BR112016015018B1 (pt) 2022-10-04
CA2933656A1 (en) 2015-07-02

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