PE20240118A1 - Compuestos y metodos para modular elfxr - Google Patents
Compuestos y metodos para modular elfxrInfo
- Publication number
- PE20240118A1 PE20240118A1 PE2023001991A PE2023001991A PE20240118A1 PE 20240118 A1 PE20240118 A1 PE 20240118A1 PE 2023001991 A PE2023001991 A PE 2023001991A PE 2023001991 A PE2023001991 A PE 2023001991A PE 20240118 A1 PE20240118 A1 PE 20240118A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- alkyl
- elfxr
- modulate
- methods
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 208000019423 liver disease Diseases 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 102000006419 Glucagon-Like Peptide Receptors Human genes 0.000 abstract 1
- 108010083749 Glucagon-Like Peptide Receptors Proteins 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005549 heteroarylene group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 abstract 1
Classifications
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D417/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
- C07D451/06—Oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Steroid Compounds (AREA)
- Liquid Crystal Substances (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Refiere a compuestos de formula (I) que pueden usarse como agonistas del receptor X farnesoide (FXR), en donde R1 y R2 son alquilo C1-C6 o alcoxi C1-C6, sustituidos opcionalmente por uno a tres halogenos; n es 1 o 2; m, p, q es 0-2; Ra y Rb son independientemente halogeno o alquilo C1-C6, los cuales forman un puente C4-C6 con los atomos de carbono; L es fenileno o heteroarileno de 5 o 6 miembros sustituidos opcionalmente por alquilo C1-C6 ,alcoxi C1-C6, halogeno y ciano; y X es heterociclilo o heteroarilo de 3 a 6 miembros que presentan 1-4 heteroatomos anulares seleccionados de N, O o S, y ambos estan sustituidos opcionalmente por halogeno, ciano y oxo. Asimismo, la presente reivindica una composicion farmaceutica a base de dichos compuestos y un excipiente parmaceuticamente aceptable, un metodo para tratar enfermedades hepaticas mediadas por el receptor de peptido similar al glucagon tipo 1 (GLP-1R) como la enfermedad de NASH, y el uso de los presentes compuestos en la fabricacion de un medicamento para el tratamiento de enfermedades hepaticas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063132363P | 2020-12-30 | 2020-12-30 | |
| PCT/US2021/073153 WO2022147448A1 (en) | 2020-12-30 | 2021-12-29 | Compounds and methods for modulating fxr |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240118A1 true PE20240118A1 (es) | 2024-01-22 |
Family
ID=82258672
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001991A PE20240118A1 (es) | 2020-12-30 | 2021-12-29 | Compuestos y metodos para modular elfxr |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20240116912A1 (es) |
| EP (1) | EP4271377A1 (es) |
| JP (1) | JP2024501700A (es) |
| KR (1) | KR20230142478A (es) |
| CN (1) | CN116887827A (es) |
| AU (1) | AU2021413366A1 (es) |
| CA (1) | CA3207069A1 (es) |
| CL (1) | CL2023001913A1 (es) |
| CO (1) | CO2023009817A2 (es) |
| IL (1) | IL304121A (es) |
| PE (1) | PE20240118A1 (es) |
| WO (1) | WO2022147448A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7450951B2 (ja) | 2022-02-17 | 2024-03-18 | カスケード ファーマシューティカルズ、インコーポレーテッド | 新型ｆｘｒ小分子作動剤の製造およびその使用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4360464A (en) * | 1969-11-28 | 1982-11-23 | Teikoku Hormone Mfg. Co. Ltd. | Process for production of 1-aryloxy-aminopropane derivatives |
| CN106946867B (zh) * | 2016-01-06 | 2019-11-12 | 广州市恒诺康医药科技有限公司 | Fxr受体调节剂及其制备方法和用途 |
| US10080742B2 (en) * | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CN110177783B (zh) * | 2016-08-23 | 2023-06-06 | 阿德利克斯股份有限公司 | 用于治疗代谢病状和病症的激素受体调节剂 |
| EP3957640A4 (en) * | 2019-04-19 | 2022-12-14 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences | FXR SMALL MOLECULE AGONIST AND METHOD OF MANUFACTURE THEREOF AND USE THEREOF |
-
2021
- 2021-12-29 CN CN202180094097.5A patent/CN116887827A/zh active Pending
- 2021-12-29 AU AU2021413366A patent/AU2021413366A1/en active Pending
- 2021-12-29 CA CA3207069A patent/CA3207069A1/en active Pending
- 2021-12-29 US US18/259,888 patent/US20240116912A1/en active Pending
- 2021-12-29 KR KR1020237025959A patent/KR20230142478A/ko unknown
- 2021-12-29 JP JP2023540117A patent/JP2024501700A/ja active Pending
- 2021-12-29 WO PCT/US2021/073153 patent/WO2022147448A1/en active Application Filing
- 2021-12-29 EP EP21916609.7A patent/EP4271377A1/en active Pending
- 2021-12-29 PE PE2023001991A patent/PE20240118A1/es unknown
-
2023
- 2023-06-28 CL CL2023001913A patent/CL2023001913A1/es unknown
- 2023-06-28 IL IL304121A patent/IL304121A/en unknown
- 2023-07-25 CO CONC2023/0009817A patent/CO2023009817A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3207069A1 (en) | 2022-07-07 |
| AU2021413366A1 (en) | 2023-08-17 |
| CN116887827A (zh) | 2023-10-13 |
| CL2023001913A1 (es) | 2024-02-09 |
| KR20230142478A (ko) | 2023-10-11 |
| EP4271377A1 (en) | 2023-11-08 |
| US20240116912A1 (en) | 2024-04-11 |
| CO2023009817A2 (es) | 2023-09-08 |
| WO2022147448A1 (en) | 2022-07-07 |
| IL304121A (en) | 2023-09-01 |
| JP2024501700A (ja) | 2024-01-15 |
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