RU2018133158A - Способы применения агонистов fxr - Google Patents
Способы применения агонистов fxr Download PDFInfo
- Publication number
- RU2018133158A RU2018133158A RU2018133158A RU2018133158A RU2018133158A RU 2018133158 A RU2018133158 A RU 2018133158A RU 2018133158 A RU2018133158 A RU 2018133158A RU 2018133158 A RU2018133158 A RU 2018133158A RU 2018133158 A RU2018133158 A RU 2018133158A
- Authority
- RU
- Russia
- Prior art keywords
- cholestasis
- dose
- use according
- liver
- pbc
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- 206010008635 Cholestasis Diseases 0.000 claims 7
- 230000007870 cholestasis Effects 0.000 claims 7
- 231100000359 cholestasis Toxicity 0.000 claims 7
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 6
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 210000004185 liver Anatomy 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 102100038495 Bile acid receptor Human genes 0.000 claims 2
- 229940126062 Compound A Drugs 0.000 claims 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 2
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 230000007882 cirrhosis Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 231100000839 Vanishing bile duct syndrome Toxicity 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 230000001587 cholestatic effect Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 229940011871 estrogen Drugs 0.000 claims 1
- 239000000262 estrogen Substances 0.000 claims 1
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 claims 1
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims 1
- 230000007872 intrahepatic cholestasis Effects 0.000 claims 1
- 230000007257 malfunction Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 235000016236 parenteral nutrition Nutrition 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000035935 pregnancy Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4748—Quinolines; Isoquinolines forming part of bridged ring systems
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Claims (11)
1. Применение химического соединения структурной формулы (I)
его стереоизомера, энантиомера, фармацевтически приемлемой соли или его аминокислотного конъюгата, для получения лекарственного средства для лечения или предотвращения патологического состояния, опосредованного фарнезоидным X-рецептором (FXR), например заболевания или нарушения работы печени, где это химическое соединение вводят в дозе в диапазоне от примерно 3 мкг до примерно 100 мкг.
2. Применение по п.1, где заболевание представляет собой холестатическое нарушение, например, холестаз (например, внутрипеченочный холестаз, холестаз, вызванный эстрогенами, холестаз, вызванный лекарственными средствами, холестаз при беременности, холестаз связанный с парентеральным питанием), первичный билиарный холангит (ПБХ), цирроз, первичный склерозирующий холангит (ПСХ), прогрессирующий семейный холестаз (ПСХ), синдром Алагиля, атрезию желчевыводящих путей, отторжение трансплантата печени при дуктопении, кистозный фиброз печени.
3. Применение по п.1, где заболевание представляет собой холестаз, ПБХ, цирроз или кистозный фиброз печени.
4. Применение по любому из предшествующих пунктов, где доза представляет собой суточную дозу.
5. Применение по любому из пп. 1-3, где доза представляет собой дозу, вводимую дважды в день.
6. Применение по любому из пп. 1-3, где доза представляет собой дозу, вводимую каждые два дня.
7. Применение по любому из предшествующих пунктов, где химическое соединение агонист FXR представляет собой Соединение A или его аминокислотный конъюгат.
8. Композиция фармацевтической стандартной лекарственной формы, содержащая примерно 10 мкг, примерно 30 мкг, примерно 60 мкг или примерно 90 мкг Соединения A, подходящая для перорального введения, до максимальной общей дозы примерно 100 мкг в день.
9. Композиция стандартной лекарственной формы по п.8 для применения в лечении первичного билиарного холангита (ПБХ).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662298113P | 2016-02-22 | 2016-02-22 | |
| US62/298,113 | 2016-02-22 | ||
| PCT/IB2017/050962 WO2017145040A1 (en) | 2016-02-22 | 2017-02-20 | Methods for using fxr agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2018133158A true RU2018133158A (ru) | 2020-03-24 |
| RU2018133158A3 RU2018133158A3 (ru) | 2020-06-08 |
| RU2737324C2 RU2737324C2 (ru) | 2020-11-27 |
Family
ID=58192341
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2018133158A RU2737324C2 (ru) | 2016-02-22 | 2017-02-20 | Способы применения агонистов fxr |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11110083B2 (ru) |
| EP (2) | EP3842043A1 (ru) |
| JP (1) | JP6941109B2 (ru) |
| KR (1) | KR20180115700A (ru) |
| CN (1) | CN108697703A (ru) |
| AU (1) | AU2017223154B2 (ru) |
| CA (1) | CA3014733A1 (ru) |
| DK (1) | DK3419624T3 (ru) |
| ES (1) | ES2862194T3 (ru) |
| HU (1) | HUE053743T2 (ru) |
| IL (1) | IL261036A (ru) |
| PL (1) | PL3419624T3 (ru) |
| PT (1) | PT3419624T (ru) |
| RU (1) | RU2737324C2 (ru) |
| SI (1) | SI3419624T1 (ru) |
| TW (1) | TW201733583A (ru) |
| WO (1) | WO2017145040A1 (ru) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113908158A (zh) | 2016-02-22 | 2022-01-11 | 诺华股份有限公司 | 使用fxr激动剂的方法 |
| RU2743075C2 (ru) | 2016-02-22 | 2021-02-15 | Новартис Аг | Способы применения агонистов fxr |
| JOP20190040A1 (ar) * | 2016-09-14 | 2019-03-10 | Novartis Ag | توليفة من ناهضات fxr |
| JP2019530696A (ja) * | 2016-10-05 | 2019-10-24 | ノバルティス アーゲー | 線維性、硬変性の疾患もしくは障害を治療または予防するためのｆｘｒアゴニストを含む組合せ組成物 |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| AR114930A1 (es) | 2017-09-12 | 2020-11-11 | Novartis Ag | Composición farmacéutica |
| JP2020533339A (ja) * | 2017-09-13 | 2020-11-19 | ノバルティス アーゲー | Ｆｘｒアゴニストを含む組合せ |
| KR102732405B1 (ko) | 2017-11-01 | 2024-11-20 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 알켄 스피로시클릭 화합물 |
| AR113820A1 (es) | 2017-11-01 | 2020-06-17 | Bristol Myers Squibb Co | Compuestos bicíclicos en puente como moduladores del receptor farnesoide x |
| CA3081424A1 (en) | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Spirocyclic compounds as farnesoid x receptor modulators |
| KR102732404B1 (ko) | 2017-11-01 | 2024-11-19 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 알켄 화합물 |
| WO2019089664A1 (en) | 2017-11-01 | 2019-05-09 | Bristol-Myers Squibb Company | Multicyclic compounds as farnesoid x receptor modulators |
| TW201936189A (zh) * | 2017-11-30 | 2019-09-16 | 瑞士商諾華公司 | 用於使用fxr激動劑之方法 |
| CN111263759B (zh) | 2017-12-22 | 2023-03-28 | 四川科伦博泰生物医药股份有限公司 | 异噁唑衍生物及其制备方法和用途 |
| WO2020061114A1 (en) * | 2018-09-18 | 2020-03-26 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| EP3924337A1 (en) | 2019-02-15 | 2021-12-22 | Bristol-Myers Squibb Company | Substituted bicyclic compounds as farnesoid x receptor modulators |
| SG11202108794RA (en) | 2019-02-15 | 2021-09-29 | Bristol Myers Squibb Co | Substituted amide compounds useful as farnesoid x receptor modulators |
| AR118050A1 (es) | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| KR102883856B1 (ko) | 2019-02-15 | 2025-11-10 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서 유용한 치환된 아미드 화합물 |
| US20220241376A1 (en) | 2019-07-18 | 2022-08-04 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| WO2021009331A1 (en) * | 2019-07-18 | 2021-01-21 | Enyo Pharma | Improved treatment using eyp001 |
| EP4041233A1 (en) * | 2019-09-30 | 2022-08-17 | Novartis AG | Treatment comprising the use of fxr agonists |
| ES3014367T3 (en) | 2020-01-15 | 2025-04-22 | Inst Nat Sante Rech Med | Use of fxr agonists for treating an infection by hepatitis d virus |
| EP4277622A1 (en) | 2021-01-14 | 2023-11-22 | ENYO Pharma | Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection |
| CN114903905B (zh) * | 2021-02-09 | 2024-04-02 | 中国人民解放军陆军军医大学第二附属医院 | 甘氨脱氧胆酸在制备治疗肝内胆汁淤积药物中的应用及其药物组合物 |
| CA3213217A1 (en) | 2021-04-28 | 2022-11-03 | Raphael Darteil | Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1562915A1 (en) | 2002-11-22 | 2005-08-17 | SmithKline Beecham Corporation | Farnesoid x receptor agonists |
| CU24152B1 (es) * | 2010-12-20 | 2016-02-29 | Irm Llc | 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr |
| CN113908158A (zh) | 2016-02-22 | 2022-01-11 | 诺华股份有限公司 | 使用fxr激动剂的方法 |
| RU2743075C2 (ru) | 2016-02-22 | 2021-02-15 | Новартис Аг | Способы применения агонистов fxr |
-
2017
- 2017-02-20 US US16/078,431 patent/US11110083B2/en not_active Expired - Fee Related
- 2017-02-20 EP EP21150907.0A patent/EP3842043A1/en not_active Withdrawn
- 2017-02-20 ES ES17708341T patent/ES2862194T3/es active Active
- 2017-02-20 CA CA3014733A patent/CA3014733A1/en not_active Abandoned
- 2017-02-20 EP EP17708341.7A patent/EP3419624B1/en active Active
- 2017-02-20 RU RU2018133158A patent/RU2737324C2/ru active
- 2017-02-20 PT PT177083417T patent/PT3419624T/pt unknown
- 2017-02-20 HU HUE17708341A patent/HUE053743T2/hu unknown
- 2017-02-20 CN CN201780012782.2A patent/CN108697703A/zh active Pending
- 2017-02-20 AU AU2017223154A patent/AU2017223154B2/en not_active Ceased
- 2017-02-20 KR KR1020187023975A patent/KR20180115700A/ko not_active Withdrawn
- 2017-02-20 JP JP2018544147A patent/JP6941109B2/ja not_active Expired - Fee Related
- 2017-02-20 SI SI201730697T patent/SI3419624T1/sl unknown
- 2017-02-20 DK DK17708341.7T patent/DK3419624T3/da active
- 2017-02-20 WO PCT/IB2017/050962 patent/WO2017145040A1/en not_active Ceased
- 2017-02-20 PL PL17708341T patent/PL3419624T3/pl unknown
- 2017-02-22 TW TW106105852A patent/TW201733583A/zh unknown
-
2018
- 2018-08-07 IL IL261036A patent/IL261036A/en unknown
-
2021
- 2021-07-23 US US17/383,634 patent/US20210386729A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| RU2018133158A3 (ru) | 2020-06-08 |
| CN108697703A (zh) | 2018-10-23 |
| AU2017223154A1 (en) | 2018-08-30 |
| HK1257649A1 (en) | 2019-10-25 |
| EP3419624A1 (en) | 2019-01-02 |
| RU2737324C2 (ru) | 2020-11-27 |
| US11110083B2 (en) | 2021-09-07 |
| JP6941109B2 (ja) | 2021-09-29 |
| PL3419624T3 (pl) | 2021-08-02 |
| HUE053743T2 (hu) | 2021-07-28 |
| US20190083481A1 (en) | 2019-03-21 |
| EP3419624B1 (en) | 2021-01-13 |
| IL261036A (en) | 2018-10-31 |
| CA3014733A1 (en) | 2017-08-31 |
| ES2862194T3 (es) | 2021-10-07 |
| KR20180115700A (ko) | 2018-10-23 |
| DK3419624T3 (da) | 2021-04-19 |
| SI3419624T1 (sl) | 2021-05-31 |
| WO2017145040A1 (en) | 2017-08-31 |
| US20210386729A1 (en) | 2021-12-16 |
| AU2017223154B2 (en) | 2019-08-15 |
| EP3842043A1 (en) | 2021-06-30 |
| JP2019511476A (ja) | 2019-04-25 |
| PT3419624T (pt) | 2021-04-07 |
| TW201733583A (zh) | 2017-10-01 |
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