RU2018136580A - Цитратная соль (s)-4-((s)-3-фтор-3-(2-(5,6,7,8-тетрагидро-1,8-нафтиридин-2-ил)этил)пирролидин-1-ил)-3-(3-(2-метоксиэтокси)фенил)бутановой кислоты - Google Patents
Цитратная соль (s)-4-((s)-3-фтор-3-(2-(5,6,7,8-тетрагидро-1,8-нафтиридин-2-ил)этил)пирролидин-1-ил)-3-(3-(2-метоксиэтокси)фенил)бутановой кислоты Download PDFInfo
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- RU2018136580A RU2018136580A RU2018136580A RU2018136580A RU2018136580A RU 2018136580 A RU2018136580 A RU 2018136580A RU 2018136580 A RU2018136580 A RU 2018136580A RU 2018136580 A RU2018136580 A RU 2018136580A RU 2018136580 A RU2018136580 A RU 2018136580A
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- Prior art keywords
- disease
- pharmaceutical composition
- condition
- compound
- methoxyethoxy
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Links
- 150000003839 salts Chemical class 0.000 title 1
- 201000010099 disease Diseases 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 230000003176 fibrotic effect Effects 0.000 claims 6
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 3
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- MKIJZIVRJUMEAD-AMGIVPHBSA-N COCCOC1=CC=CC(=C1)[C@@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O Chemical compound COCCOC1=CC=CC(=C1)[C@@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O MKIJZIVRJUMEAD-AMGIVPHBSA-N 0.000 claims 1
- 229940123038 Integrin antagonist Drugs 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 150000001860 citric acid derivatives Chemical class 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
Claims (14)
1. Соединение, которое представляет собой цитратную соль (S)-4-((S)-3-фтор-3-(2-(5,6,7,8-тетрагидро-1,8-нафтиридин-2-ил)этил)пирролидин-1-ил)-3-(3-(2-метоксиэтокси)фенил)бутановой кислоты (1:1).
2. Фармацевтическая композиция, содержащая соединение по п. 1 и фармацевтически приемлемый носитель, разбавитель или эксципиент.
3. Фармацевтическая композиция по п. 2 в форме, адаптированной для перорального введения.
4. Фармацевтическая композиция по п. 3, которая представляет собой капсулу.
5. Соединение по п. 1 или фармацевтическая композиция по любому из пп. 2-4 для применения в терапии.
6. Соединение по п. 1 или фармацевтическая композиция по любому из пп. 2-4 для применения в лечении заболевания или состояния, при котором показан антагонист рецептора ανβ6.
7. Соединение для применения по п. 6 или фармацевтическая композиция для применения по п. 6, где заболевание или состояние представляет собой фиброзное заболевание.
8. Соединение для применения по п. 7 или фармацевтическая композиция для применения по п. 7, где фиброзное заболевание представляет собой идиопатический фиброз легких.
9. Способ лечения у человека заболевания или состояния, при котором показан антагонист интегрина αvβ6, включающий введение человеку, нуждающемуся в этом, терапевтически эффективного количества соединения по п.1.
10. Способ по п. 9, в котором заболевание или состояние представляет собой фиброзное заболевание.
11. Способ по п. 10, в котором фиброзное заболевание представляет собой идиопатический фиброз легких.
12. Применение соединения по п. 1 в производстве лекарственного средства для лечения заболевания или состояния, при котором показан антагонист рецептора αvβ6.
13. Применение по п. 12, в котором заболевание или состояние представляет собой фиброзное заболевание.
14. Применение по п. 13, в котором фиброзное заболевание представляет собой идиопатический фиброз легких.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1604589.0 | 2016-03-18 | ||
| GBGB1604589.0A GB201604589D0 (en) | 2016-03-18 | 2016-03-18 | Chemical compound |
| PCT/EP2017/056204 WO2017158072A1 (en) | 2016-03-18 | 2017-03-16 | Citrate salt of the compound (s)-4-((s)-3-fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthydrin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl) butanoic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2018136580A true RU2018136580A (ru) | 2020-04-20 |
Family
ID=55968504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018136580A RU2018136580A (ru) | 2016-03-18 | 2017-03-16 | Цитратная соль (s)-4-((s)-3-фтор-3-(2-(5,6,7,8-тетрагидро-1,8-нафтиридин-2-ил)этил)пирролидин-1-ил)-3-(3-(2-метоксиэтокси)фенил)бутановой кислоты |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20200291017A1 (ru) |
| EP (1) | EP3430003A1 (ru) |
| JP (1) | JP2019508475A (ru) |
| KR (1) | KR20180127979A (ru) |
| CN (1) | CN108699036A (ru) |
| AU (1) | AU2017232285A1 (ru) |
| BR (1) | BR112018068877A2 (ru) |
| CA (1) | CA3017796A1 (ru) |
| GB (1) | GB201604589D0 (ru) |
| RU (1) | RU2018136580A (ru) |
| WO (1) | WO2017158072A1 (ru) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417011D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| MA47697A (fr) | 2017-02-28 | 2020-01-08 | Morphic Therapeutic Inc | Inhibiteurs de l'(alpha-v)(bêta-6) intégrine |
| EP3760202A1 (en) | 2017-02-28 | 2021-01-06 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| TW202035400A (zh) | 2018-08-29 | 2020-10-01 | 美商莫菲克醫療股份有限公司 | 抑制αvβ6整合素 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2001024797A1 (en) * | 1999-10-04 | 2001-04-12 | Merck & Co., Inc. | Integrin receptor antagonists |
| GB201305668D0 (en) * | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417002D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
-
2016
- 2016-03-18 GB GBGB1604589.0A patent/GB201604589D0/en not_active Ceased
-
2017
- 2017-03-16 CA CA3017796A patent/CA3017796A1/en not_active Abandoned
- 2017-03-16 EP EP17710941.0A patent/EP3430003A1/en not_active Withdrawn
- 2017-03-16 BR BR112018068877A patent/BR112018068877A2/pt not_active Application Discontinuation
- 2017-03-16 JP JP2018548927A patent/JP2019508475A/ja active Pending
- 2017-03-16 US US16/086,265 patent/US20200291017A1/en not_active Abandoned
- 2017-03-16 CN CN201780014325.7A patent/CN108699036A/zh active Pending
- 2017-03-16 WO PCT/EP2017/056204 patent/WO2017158072A1/en active Application Filing
- 2017-03-16 RU RU2018136580A patent/RU2018136580A/ru not_active Application Discontinuation
- 2017-03-16 KR KR1020187026510A patent/KR20180127979A/ko not_active Withdrawn
- 2017-03-16 AU AU2017232285A patent/AU2017232285A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN108699036A (zh) | 2018-10-23 |
| BR112018068877A2 (pt) | 2019-01-22 |
| AU2017232285A1 (en) | 2018-08-02 |
| KR20180127979A (ko) | 2018-11-30 |
| JP2019508475A (ja) | 2019-03-28 |
| US20200291017A1 (en) | 2020-09-17 |
| WO2017158072A1 (en) | 2017-09-21 |
| EP3430003A1 (en) | 2019-01-23 |
| CA3017796A1 (en) | 2017-09-21 |
| GB201604589D0 (en) | 2016-05-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA93 | Acknowledgement of application withdrawn (no request for examination) |
Effective date: 20200317 |