EA201691330A1 - Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы - Google Patents
Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазыInfo
- Publication number
- EA201691330A1 EA201691330A1 EA201691330A EA201691330A EA201691330A1 EA 201691330 A1 EA201691330 A1 EA 201691330A1 EA 201691330 A EA201691330 A EA 201691330A EA 201691330 A EA201691330 A EA 201691330A EA 201691330 A1 EA201691330 A1 EA 201691330A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- haa
- xaa
- diseases
- infections
- elastase
- Prior art date
Links
Classifications
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- 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
-
- 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
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/55—Protease inhibitors
-
- 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
- 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
- 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
- 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
- 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
- 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
- A61P37/02—Immunomodulators
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/81—Protease inhibitors
- C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
- C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Genetics & Genomics (AREA)
- Gastroenterology & Hepatology (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Otolaryngology (AREA)
- Pain & Pain Management (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (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 определенных типов, 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.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2013/078073 WO2015096873A1 (en) | 2013-12-27 | 2013-12-27 | Beta-hairpin peptidomimetics as selective elastase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA201691330A1 true EA201691330A1 (ru) | 2016-10-31 |
Family
ID=49911533
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201691330A EA201691330A1 (ru) | 2013-12-27 | 2013-12-27 | Бета-шпилечные пептидомиметики в качестве селективных ингибиторов эластазы |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US10273267B2 (ru) |
| EP (1) | EP3087094B1 (ru) |
| JP (1) | JP6499183B2 (ru) |
| KR (1) | KR102214694B1 (ru) |
| CN (1) | CN106029689B (ru) |
| AU (1) | AU2013409200B2 (ru) |
| BR (1) | BR112016014916B1 (ru) |
| CA (1) | CA2933660C (ru) |
| DK (1) | DK3087094T3 (ru) |
| EA (1) | EA201691330A1 (ru) |
| ES (1) | ES2925747T3 (ru) |
| HR (1) | HRP20221046T1 (ru) |
| HU (1) | HUE059846T2 (ru) |
| IL (1) | IL246175B (ru) |
| LT (1) | LT3087094T (ru) |
| MX (1) | MX2016008318A (ru) |
| NZ (1) | NZ722025A (ru) |
| PL (1) | PL3087094T3 (ru) |
| PT (1) | PT3087094T (ru) |
| RS (1) | RS63543B1 (ru) |
| SG (1) | SG11201605122WA (ru) |
| SI (1) | SI3087094T1 (ru) |
| WO (1) | WO2015096873A1 (ru) |
| ZA (1) | ZA201604821B (ru) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5140686B2 (ja) | 2007-02-28 | 2013-02-06 | ポリファー リミテッド | テンプレート固定ペプチド模倣薬 |
| MX2016008468A (es) * | 2013-12-27 | 2016-09-26 | Polyphor Ag | Peptidomimeticos de horquilla beta como inhibidores de elastasa selectivos. |
| EP3370518B1 (en) | 2015-10-14 | 2023-08-23 | X-Therma, Inc. | Compositions and methods for reducing ice crystal formation |
| LT3463280T (lt) * | 2016-05-31 | 2022-09-26 | Spexis Ag | Beta plaukų segtuko struktūros peptido mimetikas, pasižymintis elastazės slopiklio aktyvumu ir jo aerozolinės vaisto formos |
| 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 |
| IL297211A (en) | 2020-04-16 | 2022-12-01 | Mereo Biopharma 4 Ltd | Methods involving the neutrophil elastase inhibitor albalstat for the treatment of respiratory disease mediated by alpha-1 antitrypsin deficiency |
| CA3234399A1 (en) | 2021-10-20 | 2023-04-27 | Mereo Biopharma 4 Limited | Neutrophil elastase inhibitors for use in the treatment of fibrosis |
Family Cites Families (5)
| 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 |
| 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 |
| WO2006087001A1 (en) * | 2005-02-17 | 2006-08-24 | Polyphor Ltd. | Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity |
| MX2016008468A (es) * | 2013-12-27 | 2016-09-26 | Polyphor Ag | Peptidomimeticos de horquilla beta como inhibidores de elastasa selectivos. |
-
2013
- 2013-12-27 WO PCT/EP2013/078073 patent/WO2015096873A1/en active Application Filing
- 2013-12-27 BR BR112016014916-5A patent/BR112016014916B1/pt active IP Right Grant
- 2013-12-27 PL PL13815527.0T patent/PL3087094T3/pl unknown
- 2013-12-27 MX MX2016008318A patent/MX2016008318A/es unknown
- 2013-12-27 EP EP13815527.0A patent/EP3087094B1/en active Active
- 2013-12-27 PT PT138155270T patent/PT3087094T/pt unknown
- 2013-12-27 RS RS20220817A patent/RS63543B1/sr unknown
- 2013-12-27 JP JP2016543043A patent/JP6499183B2/ja active Active
- 2013-12-27 LT LTEPPCT/EP2013/078073T patent/LT3087094T/lt unknown
- 2013-12-27 CA CA2933660A patent/CA2933660C/en active Active
- 2013-12-27 AU AU2013409200A patent/AU2013409200B2/en active Active
- 2013-12-27 DK DK13815527.0T patent/DK3087094T3/da active
- 2013-12-27 EA EA201691330A patent/EA201691330A1/ru unknown
- 2013-12-27 US US15/107,575 patent/US10273267B2/en active Active
- 2013-12-27 SI SI201332006T patent/SI3087094T1/sl unknown
- 2013-12-27 ES ES13815527T patent/ES2925747T3/es active Active
- 2013-12-27 CN CN201380082026.9A patent/CN106029689B/zh active Active
- 2013-12-27 KR KR1020167020452A patent/KR102214694B1/ko active IP Right Grant
- 2013-12-27 NZ NZ722025A patent/NZ722025A/en unknown
- 2013-12-27 HR HRP20221046TT patent/HRP20221046T1/hr unknown
- 2013-12-27 SG SG11201605122WA patent/SG11201605122WA/en unknown
- 2013-12-27 HU HUE13815527A patent/HUE059846T2/hu unknown
-
2016
- 2016-06-13 IL IL246175A patent/IL246175B/en unknown
- 2016-07-13 ZA ZA2016/04821A patent/ZA201604821B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2017504620A (ja) | 2017-02-09 |
| PL3087094T3 (pl) | 2022-09-26 |
| SG11201605122WA (en) | 2016-07-28 |
| KR102214694B1 (ko) | 2021-02-10 |
| WO2015096873A1 (en) | 2015-07-02 |
| US10273267B2 (en) | 2019-04-30 |
| EP3087094B1 (en) | 2022-06-01 |
| AU2013409200A1 (en) | 2016-07-21 |
| NZ722025A (en) | 2019-06-28 |
| ES2925747T3 (es) | 2022-10-19 |
| BR112016014916B1 (pt) | 2022-10-04 |
| DK3087094T3 (da) | 2022-08-29 |
| EP3087094A1 (en) | 2016-11-02 |
| JP6499183B2 (ja) | 2019-04-10 |
| IL246175B (en) | 2022-04-01 |
| BR112016014916A2 (ru) | 2017-08-08 |
| HUE059846T2 (hu) | 2023-01-28 |
| CN106029689B (zh) | 2021-09-28 |
| CA2933660C (en) | 2023-05-09 |
| CA2933660A1 (en) | 2015-07-02 |
| MX2016008318A (es) | 2016-10-13 |
| US20160333053A1 (en) | 2016-11-17 |
| KR20160102313A (ko) | 2016-08-29 |
| HRP20221046T1 (hr) | 2023-01-20 |
| PT3087094T (pt) | 2022-09-05 |
| ZA201604821B (en) | 2017-09-27 |
| LT3087094T (lt) | 2022-09-26 |
| RS63543B1 (sr) | 2022-09-30 |
| IL246175A0 (en) | 2016-07-31 |
| SI3087094T1 (sl) | 2022-11-30 |
| AU2013409200B2 (en) | 2019-08-15 |
| CN106029689A (zh) | 2016-10-12 |
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