JP5373788B2 - Ｆｘｒを調節するための化合物および方法 - Google Patents
Ｆｘｒを調節するための化合物および方法 Download PDFInfo
- Publication number
- JP5373788B2 JP5373788B2 JP2010517082A JP2010517082A JP5373788B2 JP 5373788 B2 JP5373788 B2 JP 5373788B2 JP 2010517082 A JP2010517082 A JP 2010517082A JP 2010517082 A JP2010517082 A JP 2010517082A JP 5373788 B2 JP5373788 B2 JP 5373788B2
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- cyclopropyl
- dichloro
- isoxazol
- ylmethoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- TTZKGZNYBSTZIY-UHFFFAOYSA-N COC(c(ccc(N(CC1)CCC1OCc1c(C2CC2)[o]nc1-c(c(Cl)ccc1)c1Cl)c1)c1-c1ccccc1)=O Chemical compound COC(c(ccc(N(CC1)CCC1OCc1c(C2CC2)[o]nc1-c(c(Cl)ccc1)c1Cl)c1)c1-c1ccccc1)=O TTZKGZNYBSTZIY-UHFFFAOYSA-N 0.000 description 1
- AQEHMPVXJZYZBG-RVWIWJKTSA-N C[n]1c(cc([C@H](CC2)CC[C@H]2OCc2c(C3CC3)[o]nc2-c2ccccc2OC(F)(F)F)cc2)c2c(C(OC)=O)c1 Chemical compound C[n]1c(cc([C@H](CC2)CC[C@H]2OCc2c(C3CC3)[o]nc2-c2ccccc2OC(F)(F)F)cc2)c2c(C(OC)=O)c1 AQEHMPVXJZYZBG-RVWIWJKTSA-N 0.000 description 1
- RPVDFHPBGBMWID-UHFFFAOYSA-N C[n]1c(cc(cc2)N(CC3)CCC3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2c(C(O)=O)c1 Chemical compound C[n]1c(cc(cc2)N(CC3)CCC3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2c(C(O)=O)c1 RPVDFHPBGBMWID-UHFFFAOYSA-N 0.000 description 1
- ZZTCHVDDPLWIOK-UHFFFAOYSA-N C[n]1c(cc(cc2)N(CC3)CCC3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2c(C(OC)=O)c1 Chemical compound C[n]1c(cc(cc2)N(CC3)CCC3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2c(C(OC)=O)c1 ZZTCHVDDPLWIOK-UHFFFAOYSA-N 0.000 description 1
- 0 Cc1c(*2N[U](*)C(*)=C2COC(CC2)C**2[Al]*)c(*)ccc1 Chemical compound Cc1c(*2N[U](*)C(*)=C2COC(CC2)C**2[Al]*)c(*)ccc1 0.000 description 1
- NCDRLKCHBVXWEL-UXBLZVDNSA-N Cc1c(/C=N/O)c(C)ccc1 Chemical compound Cc1c(/C=N/O)c(C)ccc1 NCDRLKCHBVXWEL-UXBLZVDNSA-N 0.000 description 1
- WQOFPZFDXPHYLX-UHFFFAOYSA-N Clc1c(-c2n[o]c(C3CC3)c2COC2CCNCC2)c(Cl)ccc1 Chemical compound Clc1c(-c2n[o]c(C3CC3)c2COC2CCNCC2)c(Cl)ccc1 WQOFPZFDXPHYLX-UHFFFAOYSA-N 0.000 description 1
- UXILXOQHNDMMJM-UHFFFAOYSA-N N=C(c(cccc1)c1OC(F)(F)F)Cl Chemical compound N=C(c(cccc1)c1OC(F)(F)F)Cl UXILXOQHNDMMJM-UHFFFAOYSA-N 0.000 description 1
- LXWQVTNZUIURFE-XFFZJAGNSA-N O/N=C(/c(c(Cl)ccc1)c1Cl)\Cl Chemical compound O/N=C(/c(c(Cl)ccc1)c1Cl)\Cl LXWQVTNZUIURFE-XFFZJAGNSA-N 0.000 description 1
- FXODJZPFWQPPDM-UHFFFAOYSA-N OC(c(c(-c1ccccc1)c1)ccc1N(CC1)CCC1OCc1c(C2CC2)[o]nc1-c(c(Cl)ccc1)c1Cl)=O Chemical compound OC(c(c(-c1ccccc1)c1)ccc1N(CC1)CCC1OCc1c(C2CC2)[o]nc1-c(c(Cl)ccc1)c1Cl)=O FXODJZPFWQPPDM-UHFFFAOYSA-N 0.000 description 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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94997407P | 2007-07-16 | 2007-07-16 | |
| US60/949,974 | 2007-07-16 | ||
| PCT/US2008/069719 WO2009012125A1 (en) | 2007-07-16 | 2008-07-11 | Compounds and methods for modulating fxr |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010533722A JP2010533722A (ja) | 2010-10-28 |
| JP2010533722A5 JP2010533722A5 (esLanguage) | 2011-08-11 |
| JP5373788B2 true JP5373788B2 (ja) | 2013-12-18 |
Family
ID=39855171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010517082A Active JP5373788B2 (ja) | 2007-07-16 | 2008-07-11 | Ｆｘｒを調節するための化合物および方法 |
Country Status (31)
Families Citing this family (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2289883A1 (en) | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2012087520A1 (en) * | 2010-12-20 | 2012-06-28 | Irm Llc | Compositions and methods for modulating farnesoid x receptors |
| 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 |
| JP2014500319A (ja) * | 2010-12-20 | 2014-01-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | ファルネソイドｘ受容体を調節するための組成物および方法 |
| 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 |
| JP6064062B2 (ja) | 2013-03-15 | 2017-01-18 | ファイザー・インク | Ａｍｐｋを活性化させるインダゾール化合物 |
| MX377523B (es) | 2013-09-11 | 2025-03-10 | Inst Nat Sante Rech Med | Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b. |
| SG11201603026PA (en) | 2013-11-05 | 2016-05-30 | Novartis Ag | Compositions and methods for modulating farnesoid x receptors |
| CN104045635A (zh) * | 2014-06-23 | 2014-09-17 | 华东理工大学 | 3,4,5-三取代异恶唑类化合物及其用途 |
| EP3006939A1 (en) | 2014-10-06 | 2016-04-13 | Gilead Sciences, Inc. | Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| EP3034499A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| EP3034501A1 (en) | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| ES2905872T3 (es) | 2015-02-06 | 2022-04-12 | Intercept Pharmaceuticals Inc | Composiciones farmacéuticas para terapia combinada |
| TWI698430B (zh) | 2015-02-13 | 2020-07-11 | 南北兄弟藥業投資有限公司 | 三環化合物及其在藥物中的應用 |
| RU2712099C2 (ru) | 2015-03-31 | 2020-01-24 | Энанта Фармасьютикалс, Инк. | Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения |
| CN107613986A (zh) | 2015-04-07 | 2018-01-19 | 英特塞普特医药品公司 | 用于组合疗法的药物组合物 |
| 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 |
| CN107021958A (zh) * | 2016-02-01 | 2017-08-08 | 山东轩竹医药科技有限公司 | Fxr受体激动剂 |
| MX2018011813A (es) | 2016-03-28 | 2019-01-24 | Intercept Pharmaceuticals Inc | Medicina obtenida mediante la combinacion de agonista fxr y arb. |
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| US10080742B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
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| CN116854681B (zh) * | 2016-08-23 | 2026-05-26 | 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 |
| JP6915050B2 (ja) * | 2016-09-14 | 2021-08-04 | ノバルティス アーゲー | Ｆｘｒアゴニストの新規のレジーム |
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| PE20252787A1 (es) | 2023-04-07 | 2025-12-22 | Terns Pharmaceuticals Inc | Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica |
Family Cites Families (10)
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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 |
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| US7105556B2 (en) | 2001-05-30 | 2006-09-12 | Bristol-Myers Squibb Company | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method |
| US6967212B2 (en) * | 2001-05-30 | 2005-11-22 | Bristol-Myers Squibb Company | Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method |
| DE60131967D1 (de) | 2001-08-13 | 2008-01-31 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| US6875782B2 (en) | 2002-07-09 | 2005-04-05 | Bristol-Myers Squibb Company | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| JP2006515838A (ja) * | 2002-11-22 | 2006-06-08 | スミスクライン ビーチャム コーポレーション | ファルネソイドｘ受容体アゴニスト |
| ES2452031T3 (es) | 2006-02-03 | 2014-03-31 | Eli Lilly & Company | Compuestos y procedimientos para modular receptores FX |
| DK2029547T3 (da) * | 2006-05-24 | 2010-07-26 | Lilly Co Eli | FXR-agonister |
| ES2340221T3 (es) | 2006-05-24 | 2010-05-31 | Eli Lilly And Company | Compuestos y procedimientos para modular fxr. |
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