PE20090809A1 - Compuestos heterociclicos como agentes moduladores del receptor farnesoide x (fxr) - Google Patents
Compuestos heterociclicos como agentes moduladores del receptor farnesoide x (fxr)Info
- Publication number
- PE20090809A1 PE20090809A1 PE2008001168A PE2008001168A PE20090809A1 PE 20090809 A1 PE20090809 A1 PE 20090809A1 PE 2008001168 A PE2008001168 A PE 2008001168A PE 2008001168 A PE2008001168 A PE 2008001168A PE 20090809 A1 PE20090809 A1 PE 20090809A1
- Authority
- PE
- Peru
- Prior art keywords
- link
- fxr
- receptor
- farnesoid
- heterocyclic compounds
- Prior art date
Links
- 150000002391 heterocyclic compounds Chemical class 0.000 title abstract 2
- 102100038495 Bile acid receptor Human genes 0.000 title 2
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 title 2
- -1 ISOPROPYL Chemical group 0.000 abstract 3
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical group ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 239000000460 chlorine Substances 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 239000011737 fluorine Chemical group 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000032928 Dyslipidaemia Diseases 0.000 abstract 1
- WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical group F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical group [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P3/06—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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Indole Compounds (AREA)
Abstract
SE REFIERE A UN COMPUESTO HETEROCICLICO DE FORMULA I, LOS CUALES SON MODULADORES DEL RECEPTOR FXR, POR LO QUE SON UTILES PARA EL TRATAMIENTO DE DISLIPIDEMIAS Y ENFERMEDADES RELACIONADAS, TALES COMO HIPERLIPIDEMIA, HIPERTRIGLICEREMIA, COLESTASIS DE HIGADO, HDL BAJO EN PLASMA, LDL ALTO EN PLASMA, VLDL ALTO EN PLASMA, ATEROESCLEROSIS, TROMBOSIS, APOPLEJIA, HIPERTENSION, ENTRE OTROS. DONDE q ES 1 O 2, SIEMPRE QUE CUANDO X SEA C, q ES 1; U ES O, N o C; SIEMPRE QUE CUANDO U SEA O o N , R3a ESTA AUSENTE; Y SIEMPRE QUE CUANDO U SEA N o C, EL ENLACE UN ES UN ENLACE DOBLE; Y SIEMPRE QUE CUANDO W SEA C, EL ENLACE WN ES UN DOBLE ENLACE; W ES C o N; X ES C o N; R1 ES CLORO, FLUORO, O TRIFLUOROMETOXI; R2 ES H, CLORO, FLUORO, O TRIFLUOROMETOXI; R3a ES H, O ESTA AUSENTE; R3b ES TRIFLUOROMETILO, CICLOPROPILO O ISOPROPILO; Ar1 SE SELECCIONA DE 6-INDOLILO, 6-BENZOTIENILO, 4-NAFTILO, ENTRE OTROS Y R5 ES COOH; O UNA SAL, ENANTIOMERO, DIASTEREOMERO FARMACEUTICAMENTE ACEPTABLE O MEZCLA DE LOS MISMOS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94997407P | 2007-07-16 | 2007-07-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090809A1 true PE20090809A1 (es) | 2009-06-27 |
Family
ID=39855171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001168A PE20090809A1 (es) | 2007-07-16 | 2008-07-11 | Compuestos heterociclicos como agentes moduladores del receptor farnesoide x (fxr) |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8153624B2 (es) |
| EP (1) | EP2178851B1 (es) |
| JP (1) | JP5373788B2 (es) |
| KR (1) | KR101157334B1 (es) |
| CN (1) | CN101743232B (es) |
| AR (1) | AR067540A1 (es) |
| AT (1) | ATE539065T1 (es) |
| AU (1) | AU2008276236B2 (es) |
| BR (1) | BRPI0814571A2 (es) |
| CA (1) | CA2693406C (es) |
| CL (1) | CL2008002051A1 (es) |
| CO (1) | CO6270212A2 (es) |
| CY (1) | CY1112298T1 (es) |
| DK (1) | DK2178851T3 (es) |
| DO (1) | DOP2010000018A (es) |
| EA (1) | EA016475B1 (es) |
| EC (1) | ECSP109879A (es) |
| ES (1) | ES2376176T3 (es) |
| HR (1) | HRP20120048T1 (es) |
| IL (1) | IL202234A0 (es) |
| MA (1) | MA31683B1 (es) |
| MX (1) | MX2010000502A (es) |
| PE (1) | PE20090809A1 (es) |
| PL (1) | PL2178851T3 (es) |
| PT (1) | PT2178851E (es) |
| RS (1) | RS52216B (es) |
| SI (1) | SI2178851T1 (es) |
| SV (1) | SV2010003458A (es) |
| TN (1) | TN2010000028A1 (es) |
| TW (1) | TW200906823A (es) |
| WO (1) | WO2009012125A1 (es) |
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| US20130261108A1 (en) * | 2010-12-20 | 2013-10-03 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2013037482A1 (en) | 2011-09-15 | 2013-03-21 | Phenex Pharmaceuticals Ag | Farnesoid x receptor agonists for cancer treatment and prevention |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| CA2905242C (en) | 2013-03-15 | 2016-11-29 | Pfizer Inc. | Indole compounds that activate ampk |
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| LT3065738T (lt) * | 2013-11-05 | 2018-05-10 | Novartis Ag | Kompozicijos ir būdai, skirti x receptorių moduliavimui |
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| CN119013027A (zh) | 2021-11-11 | 2024-11-22 | 拓臻制药公司 | 用于治疗肝脏病症的SSAO抑制剂和THR-β激动剂的组合 |
| WO2023220404A1 (en) * | 2022-05-13 | 2023-11-16 | Terns Pharmaceuticals, Inc. | Treatment of non-alcoholic steatohepatitis |
| CN115850152B (zh) * | 2022-12-20 | 2025-10-31 | 河北鼎泰制药有限公司 | 一种杂质A-7-imp3的制备方法及其用途 |
| EP4568664A1 (en) | 2023-04-07 | 2025-06-18 | Terns Pharmaceuticals, Inc. | Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating a liver disorder or a cardiometabolic disease |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JPH07138258A (ja) | 1993-11-16 | 1995-05-30 | Taiho Yakuhin Kogyo Kk | チアゾリジンジオン誘導体又はその塩 |
| US6639078B1 (en) | 1998-12-23 | 2003-10-28 | Smithkline Beecham Corporation | Assays for ligands for nuclear receptors |
| US6967212B2 (en) * | 2001-05-30 | 2005-11-22 | Bristol-Myers Squibb Company | Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method |
| US7105556B2 (en) | 2001-05-30 | 2006-09-12 | Bristol-Myers Squibb Company | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method |
| DE60131967D1 (de) | 2001-08-13 | 2008-01-31 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| NZ537251A (en) | 2002-07-09 | 2007-02-23 | Bristol Myers Squibb Co | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| EP1562915A1 (en) | 2002-11-22 | 2005-08-17 | SmithKline Beecham Corporation | Farnesoid x receptor agonists |
| US7863302B2 (en) * | 2006-02-03 | 2011-01-04 | Eli Lilly And Company | Compounds and methods for modulating FX-receptors |
| BRPI0712262A2 (pt) * | 2006-05-24 | 2012-07-10 | Lilly Co Eli | agonistas de fxr |
| DE602007005256D1 (de) | 2006-05-24 | 2010-04-22 | Lilly Co Eli | Verbindungen und verfahren zur modulierung von fx-rezeptoren |
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