PE20230235A1 - Compuestos para modular la actividad de fxr y usos de los mismos - Google Patents
Compuestos para modular la actividad de fxr y usos de los mismosInfo
- Publication number
- PE20230235A1 PE20230235A1 PE2022001004A PE2022001004A PE20230235A1 PE 20230235 A1 PE20230235 A1 PE 20230235A1 PE 2022001004 A PE2022001004 A PE 2022001004A PE 2022001004 A PE2022001004 A PE 2022001004A PE 20230235 A1 PE20230235 A1 PE 20230235A1
- Authority
- PE
- Peru
- Prior art keywords
- halogen
- compounds
- substituted
- compound
- independently selected
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
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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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and 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
- A61K31/435—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
- A61K31/33—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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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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
- A61K31/4965—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Referido a un compuesto de formula I, una sal farmaceuticamente aceptable, un ester o un estereoisomero del mismo; en donde R1, R2 y R3 se seleccionan independientemente de H, halogeno, alquilo C1-6 no sustituido o sustituido, entre otros; R0 se selecciona de alquilo C1-C6 no sustituido o sustituido con halogeno, cicloalquilo C3-C6 y alquilcicloalquilo C4-C7; X1 y X2 se seleccionan independientemente de H y halogeno; el resto -O-Z se une al anillo de naftaleno, en donde Z es un residuo que se selecciona de arilo de 5-10 miembros o heteroarilo de 5-10 miembros que tiene opcionalmente uno o mas heteroatomos que se seleccionan de N, O y S, entre otros. Estos compuestos modulan la actividad del receptor farnesoide X (FXR). Tambien se refiere a una composicion farmaceutica que comprende dicho compuesto, y su uso en el tratamiento de enfermedad del higado graso no alcoholico (NAFLD), esteatohepatitis no alcoholica, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2019/122595 WO2021108974A1 (en) | 2019-12-03 | 2019-12-03 | Compounds for modulating activity of fxr and uses thereof |
| PCT/CN2020/120369 WO2021109712A1 (en) | 2019-12-03 | 2020-10-12 | Compounds for modulating activity of fxr and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230235A1 true PE20230235A1 (es) | 2023-02-07 |
Family
ID=76111005
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022001004A PE20230235A1 (es) | 2019-12-03 | 2020-10-12 | Compuestos para modular la actividad de fxr y usos de los mismos |
| PE2022001013A PE20230182A1 (es) | 2019-12-03 | 2020-10-12 | Uso y composicion farmaceutica de derivados de fenilisoxazolil metilen-naftaleno-eter |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022001013A PE20230182A1 (es) | 2019-12-03 | 2020-10-12 | Uso y composicion farmaceutica de derivados de fenilisoxazolil metilen-naftaleno-eter |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US20220388997A1 (es) |
| EP (2) | EP4073071A4 (es) |
| JP (2) | JP7430263B2 (es) |
| KR (2) | KR20220101697A (es) |
| CN (2) | CN112891348B (es) |
| AU (2) | AU2020395393B2 (es) |
| BR (2) | BR112022010638A2 (es) |
| CA (2) | CA3163779A1 (es) |
| CO (2) | CO2022008719A2 (es) |
| IL (2) | IL293507A (es) |
| MX (2) | MX2022006742A (es) |
| PE (2) | PE20230235A1 (es) |
| WO (3) | WO2021108974A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021108974A1 (en) * | 2019-12-03 | 2021-06-10 | Gannex Pharma Co., Ltd | Compounds for modulating activity of fxr and uses thereof |
| TW202315608A (zh) * | 2021-07-06 | 2023-04-16 | 中國大陸商甘萊製藥有限公司 | 用於治療肝臟疾病的聯合治療 |
| TW202317110A (zh) * | 2021-07-06 | 2023-05-01 | 中國大陸商甘萊製藥有限公司 | 用於治療肝臟疾病的聯合治療 |
| WO2023035181A1 (en) * | 2021-09-09 | 2023-03-16 | Gannex Pharma Co., Ltd. | A pharmaceutical composition of fxr agonist and its preparation method |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009005998A1 (en) * | 2007-07-02 | 2009-01-08 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| HUE052856T2 (hu) * | 2013-09-11 | 2021-05-28 | Inst Nat Sante Rech Med | Eljárások és gyógyászati készítmények Hepatitis B vírus fertõzés kezelésére |
| US10369123B2 (en) * | 2014-08-14 | 2019-08-06 | Deutsches Zentrum Für Neurodegenerative Erkrankungen E.V. (Dzne) | Perk activator for the treatment of neurodegenerative diseases |
| US10080741B2 (en) * | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189663A1 (en) * | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2018190643A1 (en) * | 2017-04-12 | 2018-10-18 | Il Dong Pharmaceutical Co., Ltd. | An isoxazole derivatives as nuclear receptor agonists and used thereof |
| WO2019160813A1 (en) * | 2018-02-14 | 2019-08-22 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2021108974A1 (en) * | 2019-12-03 | 2021-06-10 | Gannex Pharma Co., Ltd | Compounds for modulating activity of fxr and uses thereof |
-
2019
- 2019-12-03 WO PCT/CN2019/122595 patent/WO2021108974A1/en active Application Filing
-
2020
- 2020-10-12 MX MX2022006742A patent/MX2022006742A/es unknown
- 2020-10-12 PE PE2022001004A patent/PE20230235A1/es unknown
- 2020-10-12 AU AU2020395393A patent/AU2020395393B2/en active Active
- 2020-10-12 US US17/756,789 patent/US20220388997A1/en active Pending
- 2020-10-12 IL IL293507A patent/IL293507A/en unknown
- 2020-10-12 IL IL293497A patent/IL293497A/en unknown
- 2020-10-12 MX MX2022006653A patent/MX2022006653A/es unknown
- 2020-10-12 JP JP2022533383A patent/JP7430263B2/ja active Active
- 2020-10-12 AU AU2020397245A patent/AU2020397245B2/en active Active
- 2020-10-12 EP EP20896203.5A patent/EP4073071A4/en active Pending
- 2020-10-12 US US17/781,730 patent/US20230165843A1/en active Pending
- 2020-10-12 CA CA3163779A patent/CA3163779A1/en active Pending
- 2020-10-12 KR KR1020227020581A patent/KR20220101697A/ko active Search and Examination
- 2020-10-12 CA CA3159899A patent/CA3159899A1/en active Pending
- 2020-10-12 WO PCT/CN2020/120369 patent/WO2021109712A1/en unknown
- 2020-10-12 CN CN202011083652.8A patent/CN112891348B/zh active Active
- 2020-10-12 KR KR1020227022709A patent/KR20220112278A/ko active Search and Examination
- 2020-10-12 BR BR112022010638A patent/BR112022010638A2/pt unknown
- 2020-10-12 JP JP2022533371A patent/JP2023505205A/ja active Pending
- 2020-10-12 EP EP20895007.1A patent/EP4073070A4/en active Pending
- 2020-10-12 WO PCT/CN2020/120370 patent/WO2021109713A1/en unknown
- 2020-10-12 PE PE2022001013A patent/PE20230182A1/es unknown
- 2020-10-12 BR BR112022010798A patent/BR112022010798A2/pt unknown
- 2020-10-12 CN CN202011084166.8A patent/CN112898289B/zh active Active
-
2022
- 2022-06-22 CO CONC2022/0008719A patent/CO2022008719A2/es unknown
- 2022-06-22 CO CONC2022/0008701A patent/CO2022008701A2/es unknown
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