JP2010533722A5 - - Google Patents
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- Publication number
- JP2010533722A5 JP2010533722A5 JP2010517082A JP2010517082A JP2010533722A5 JP 2010533722 A5 JP2010533722 A5 JP 2010533722A5 JP 2010517082 A JP2010517082 A JP 2010517082A JP 2010517082 A JP2010517082 A JP 2010517082A JP 2010533722 A5 JP2010533722 A5 JP 2010533722A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- ylmethoxy
- isoxazol
- dichloro
- cyclopropyl
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 5
- 239000011780 sodium chloride Substances 0.000 claims 5
- -1 benzoisothiazolyl Chemical group 0.000 claims 3
- BHHQDQJNIROKNF-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]azepan-1-yl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1N1CCC(OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)CCC1 BHHQDQJNIROKNF-UHFFFAOYSA-N 0.000 claims 2
- FMYIBSTZKZVLRS-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]cyclohexyl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1C1CCC(OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)CC1 FMYIBSTZKZVLRS-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004787 chlorofluoromethoxy group Chemical group ClC(O*)F 0.000 claims 2
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- BMHSHVMYWHJZHM-UHFFFAOYSA-N 4-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-methylbenzoic acid Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2Cl)Cl)C=1COC(CC1)CCN1C1=CC=C(C(O)=O)C(C)=C1 BMHSHVMYWHJZHM-UHFFFAOYSA-N 0.000 claims 1
- OLWQNBCXCFTKAN-UHFFFAOYSA-N 4-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-phenylbenzoic acid Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2Cl)Cl)C=1COC(CC1)CCN1C(C=1)=CC=C(C(O)=O)C=1C1=CC=CC=C1 OLWQNBCXCFTKAN-UHFFFAOYSA-N 0.000 claims 1
- TUXQDUMYSZHKDF-UHFFFAOYSA-N 4-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-3-methylbenzoic acid Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2Cl)Cl)C=1COC(CC1)CCN1C1=CC=C(C(O)=O)C=C1C TUXQDUMYSZHKDF-UHFFFAOYSA-N 0.000 claims 1
- SARVSQBHGLWJDC-UHFFFAOYSA-N 4-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]benzoic acid Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2Cl)Cl)C=1COC(CC1)CCN1C1=CC=C(C(O)=O)C=C1 SARVSQBHGLWJDC-UHFFFAOYSA-N 0.000 claims 1
- LTQORJNFRTWNQZ-UHFFFAOYSA-N 4-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]naphthalene-1-carboxylic acid Chemical compound C1CN(C=2C3=CC=CC=C3C(C(O)=O)=CC=2)CCC1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl LTQORJNFRTWNQZ-UHFFFAOYSA-N 0.000 claims 1
- KMAPTVZHJWJUDZ-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-methylbenzoic acid Chemical compound C1=C(C(O)=O)C(C)=CC(N2CCC(CC2)OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)=C1 KMAPTVZHJWJUDZ-UHFFFAOYSA-N 0.000 claims 1
- FXODJZPFWQPPDM-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-phenylbenzoic acid Chemical compound OC(=O)C1=CC=C(N2CCC(CC2)OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)C=C1C1=CC=CC=C1 FXODJZPFWQPPDM-UHFFFAOYSA-N 0.000 claims 1
- ZPNMRIMLACQTND-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-3-methylbenzoic acid Chemical compound CC1=CC(C(O)=O)=CC=C1N1CCC(OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)CC1 ZPNMRIMLACQTND-UHFFFAOYSA-N 0.000 claims 1
- JDPVTPAYEUGANP-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]benzoic acid Chemical compound C1=CC(C(=O)O)=CC=C1N1CCC(OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2Cl)Cl)CC1 JDPVTPAYEUGANP-UHFFFAOYSA-N 0.000 claims 1
- YLOIALRDPVKHBC-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-methylbenzoic acid Chemical compound C1=C(C(O)=O)C(C)=CC(N2CCC(CC2)OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2)OC(F)(F)F)=C1 YLOIALRDPVKHBC-UHFFFAOYSA-N 0.000 claims 1
- ITMGGFXMTLJIBH-UHFFFAOYSA-N 4-[4-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-2-phenylbenzoic acid Chemical compound OC(=O)C1=CC=C(N2CCC(CC2)OCC=2C(=NOC=2C2CC2)C=2C(=CC=CC=2)OC(F)(F)F)C=C1C1=CC=CC=C1 ITMGGFXMTLJIBH-UHFFFAOYSA-N 0.000 claims 1
- UVERNCKJGPCBJN-UHFFFAOYSA-N 4-[4-[[5-propan-2-yl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]benzoic acid Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2)OC(F)(F)F)C=1COC(CC1)CCN1C1=CC=C(C(O)=O)C=C1 UVERNCKJGPCBJN-UHFFFAOYSA-N 0.000 claims 1
- QYHGTOWHHXVPJY-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-benzothiophene-3-carboxylic acid Chemical compound C1CN(C=2C=C3SC=C(C3=CC=2)C(O)=O)CCC1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl QYHGTOWHHXVPJY-UHFFFAOYSA-N 0.000 claims 1
- QEPDFQBZEHAKMC-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-methylindole-3-carboxylic acid Chemical compound C1CN(C=2C=C3N(C)C=C(C3=CC=2)C(O)=O)CCC1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl QEPDFQBZEHAKMC-UHFFFAOYSA-N 0.000 claims 1
- QVSRRDPHMZENOC-UHFFFAOYSA-N 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]azepan-1-yl]-1-benzothiophene-3-carboxylic acid Chemical compound C=1C=C2C(C(=O)O)=CSC2=CC=1N(CC1)CCCC1OCC1=C(C2CC2)ON=C1C1=C(Cl)C=CC=C1Cl QVSRRDPHMZENOC-UHFFFAOYSA-N 0.000 claims 1
- VXDXGDBJVDCGPS-UHFFFAOYSA-N 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]azepan-1-yl]-1-methylindole-3-carboxylic acid Chemical compound C1=C2N(C)C=C(C(O)=O)C2=CC=C1N(CC1)CCCC1OCC1=C(C2CC2)ON=C1C1=C(Cl)C=CC=C1Cl VXDXGDBJVDCGPS-UHFFFAOYSA-N 0.000 claims 1
- GAPDATOJAODWBF-UHFFFAOYSA-N 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-benzothiophene-3-carboxylic acid Chemical compound C=1C=C2C(C(=O)O)=CSC2=CC=1N(CC1)CCC1OCC1=C(C2CC2)ON=C1C1=C(Cl)C=CC=C1Cl GAPDATOJAODWBF-UHFFFAOYSA-N 0.000 claims 1
- RPVDFHPBGBMWID-UHFFFAOYSA-N 6-[4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-methylindole-3-carboxylic acid Chemical compound C1=C2N(C)C=C(C(O)=O)C2=CC=C1N(CC1)CCC1OCC1=C(C2CC2)ON=C1C1=C(Cl)C=CC=C1Cl RPVDFHPBGBMWID-UHFFFAOYSA-N 0.000 claims 1
- GWXYJEDUVAMRFV-UHFFFAOYSA-N 6-[4-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]piperidin-1-yl]-1-methylindole-3-carboxylic acid Chemical compound C1=C2N(C)C=C(C(O)=O)C2=CC=C1N(CC1)CCC1OCC1=C(C2CC2)ON=C1C1=CC=CC=C1OC(F)(F)F GWXYJEDUVAMRFV-UHFFFAOYSA-N 0.000 claims 1
- GMKJZUNUHWUPRV-IRJFHVNHSA-N Cn1cc(C(O)=O)c2ccc(cc12)[C@H]1CC[C@@H](CC1)OCc1c(onc1-c1ccccc1OC(F)(F)F)C1CC1 Chemical compound Cn1cc(C(O)=O)c2ccc(cc12)[C@H]1CC[C@@H](CC1)OCc1c(onc1-c1ccccc1OC(F)(F)F)C1CC1 GMKJZUNUHWUPRV-IRJFHVNHSA-N 0.000 claims 1
- KLKSMSZZLBFWCT-IRJFHVNHSA-N OC(=O)c1ccc(cc1)[C@H]1CC[C@@H](CC1)OCc1c(onc1-c1ccccc1OC(F)(F)F)C1CC1 Chemical compound OC(=O)c1ccc(cc1)[C@H]1CC[C@@H](CC1)OCc1c(onc1-c1ccccc1OC(F)(F)F)C1CC1 KLKSMSZZLBFWCT-IRJFHVNHSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atoms Chemical class [H]* 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 0 CCC(CC*(C)[Al]C(O)=O)OCc1c(*C)[o]nc1-c1c(*)cccc1I Chemical compound CCC(CC*(C)[Al]C(O)=O)OCc1c(*C)[o]nc1-c1c(*)cccc1I 0.000 description 1
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 true JP2010533722A5 (US20070167479A1-20070719-C00034.png) | 2011-08-11 |
| JP5373788B2 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 (72)
| 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 |
| JP2014500318A (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 |
| WO2012087521A1 (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 |
| 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 |
| AU2014320463B2 (en) | 2013-09-11 | 2018-08-02 | Centre National De La Recherche Scientifique (Cnrs) | Methods and pharmaceutical compositions for the treatment of hepatitis B virus infection |
| 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 |
| EP3034501A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Hydroxy containing FXR (NR1H4) modulating compounds |
| EP3034499A1 (en) * | 2014-12-17 | 2016-06-22 | Gilead Sciences, Inc. | Novel FXR (NR1H4) modulating compounds |
| MA40814A1 (fr) | 2015-02-06 | 2019-08-30 | Intercept Pharmaceuticals Inc | Compositions pharmaceutiques pour thérapie combinée |
| 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 |
| CN107427527B (zh) | 2015-03-31 | 2021-01-26 | 英安塔制药有限公司 | 作为fxr/tgr5激动剂的胆汁酸衍生物及其使用方法 |
| KR20170132879A (ko) | 2015-04-07 | 2017-12-04 | 인터셉트 파마슈티컬즈, 인크. | 조합 요법을 위한 약제학적 조성물 |
| 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 |
| KR20180124123A (ko) | 2016-03-28 | 2018-11-20 | 인터셉트 파마슈티컬즈, 인크. | Fxr 효능제 및 arb의 조합에 의해 얻어지는 의약 |
| US10080743B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| US10080741B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017189651A1 (en) * | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10138228B2 (en) | 2016-05-18 | 2018-11-27 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use therof |
| WO2017201150A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| WO2017201155A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF |
| ES2921432T3 (es) | 2016-06-13 | 2022-08-25 | Gilead Sciences Inc | Derivados de azetidina como moduladores de FXR (NR1H4) |
| CA2968836A1 (en) | 2016-06-13 | 2017-12-13 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| TW201808283A (zh) | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| CN116854681A (zh) * | 2016-08-23 | 2023-10-10 | 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 |
| WO2018039384A1 (en) | 2016-08-23 | 2018-03-01 | Ardelyx, Inc. | Isoxazolyl-carbonyloxy azabicyclo[3.2.1]octanyl compounds as fxr activators |
| CN109689050A (zh) * | 2016-09-14 | 2019-04-26 | 诺华股份有限公司 | Fxr激动剂的新方案 |
| BR112019006651A2 (pt) | 2016-10-04 | 2019-07-02 | Enanta Pharm Inc | análogos de isoxazol como agonistas de fxr e métodos de uso do mesmo |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
| 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 |
| CN108218852A (zh) * | 2016-12-15 | 2018-06-29 | 宁波百纳西药业有限公司 | 一种螺环化合物、其制备方法、组合物及用途 |
| ES2927019T3 (es) | 2017-03-28 | 2022-11-02 | Gilead Sciences Inc | Combinaciones terapéuticas para el tratamiento de enfermedades hepáticas |
| WO2018178260A1 (en) | 2017-03-30 | 2018-10-04 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses |
| NZ758117A (en) * | 2017-04-12 | 2022-01-28 | Il Dong Pharma | Isoxazole derivatives as nuclear receptor agonists and uses thereof |
| CN109265471B (zh) * | 2017-06-30 | 2021-06-04 | 轩竹生物科技有限公司 | Fxr受体激动剂 |
| CN109320509B (zh) * | 2017-07-31 | 2022-02-08 | 轩竹生物科技股份有限公司 | Fxr受体激动剂 |
| WO2019055808A1 (en) | 2017-09-14 | 2019-03-21 | Ardelyx, Inc. | HORMONE RECEPTOR MODULATORS FOR THE TREATMENT OF MUTAGENIC AND FIBROTIC METABOLIC CONDITIONS AND DISORDERS |
| BR112020008121A2 (pt) | 2017-11-01 | 2020-11-03 | Bristol-Myers Squibb Company | compostos espirocíclico de alqueno como moduladores de receptor farnesoide x |
| EA202091101A1 (ru) | 2017-11-01 | 2020-08-06 | Бристол-Маерс Сквибб Компани | Спироциклические соединения в качестве модуляторов фарнезоидного x-рецептора |
| SG11202003827YA (en) | 2017-11-01 | 2020-05-28 | Bristol Myers Squibb Co | Bridged bicyclic compounds as farnesoid x receptor modulators |
| EP3704107B1 (en) | 2017-11-01 | 2023-04-12 | Bristol-Myers Squibb Company | Multicyclic compounds as farnesoid x receptor modulators |
| ES2944657T3 (es) * | 2017-11-01 | 2023-06-23 | Bristol Myers Squibb Co | Compuestos de alqueno como moduladores del receptor farnesoide X |
| US10689391B2 (en) | 2017-12-12 | 2020-06-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| US11667629B2 (en) | 2017-12-22 | 2023-06-06 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Isoxazole derivative, preparation method therefor, and use thereof |
| CN110128432B (zh) | 2018-02-02 | 2021-03-02 | 广东东阳光药业有限公司 | 含氮三环化合物及其在药物中的应用 |
| US10829486B2 (en) | 2018-02-14 | 2020-11-10 | Enanta Pharmacueticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CN110452235B (zh) * | 2018-05-08 | 2023-02-17 | 中国科学院上海药物研究所 | 一类含氟异噁唑类化合物及其制备方法、药物组合物和用途 |
| JP2022508402A (ja) * | 2018-08-30 | 2022-01-19 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | 肝障害の治療 |
| DK3911647T3 (da) | 2019-01-15 | 2024-02-26 | Gilead Sciences Inc | Isoxazol-forbindelse som FXR-agonist og farmaceutiske sammensætninger, der omfatter en sådan |
| AR118050A1 (es) | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| CN113439078B (zh) | 2019-02-19 | 2024-04-23 | 吉利德科学公司 | Fxr激动剂的固体形式 |
| WO2020231917A1 (en) * | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| JP2022536060A (ja) | 2019-05-30 | 2022-08-12 | インターセプト ファーマシューティカルズ， インコーポレイテッド | 胆汁鬱滞性肝疾患の処置で使用するためのｆｘｒアゴニストおよびフィブラートを含む医薬組成物 |
| MX2022000742A (es) | 2019-07-18 | 2022-02-14 | Enyo Pharma | Metodo para disminuir los efectos adversos del interferon. |
| CA3160445A1 (en) * | 2019-11-08 | 2021-05-14 | Terns Pharmaceuticals, Inc. | Treating liver disorders |
| EP4090327A1 (en) | 2020-01-15 | 2022-11-23 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Use of fxr agonists for treating an infection by hepatitis d virus |
| AU2021273487A1 (en) * | 2020-05-13 | 2023-01-05 | Terns Pharmaceuticals, Inc. | Combination treatment of liver disorders |
| MX2023002308A (es) | 2020-08-25 | 2023-07-11 | Lilly Co Eli | Polimorfos de un inhibidor de ssao. |
| JP2023541423A (ja) * | 2020-09-11 | 2023-10-02 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | Ｆｘｒアゴニストの固体分散体製剤 |
| IL302099A (en) * | 2020-10-15 | 2023-06-01 | Lilly Co Eli | FXR agonist polymorphs |
| CN117202905A (zh) | 2021-01-14 | 2023-12-08 | 埃尼奥制药公司 | Fxr激动剂和ifn用于治疗hbv感染的协同效果 |
| JP2024517181A (ja) | 2021-04-28 | 2024-04-19 | ウエヌイグレックオ・ファーマ | 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強 |
| AU2022387121A1 (en) | 2021-11-11 | 2024-06-20 | Terns Pharmaceuticals, Inc. | Combination of a ssao inhibitor and thr-beta agonist for use in the treatment of liver disorders |
| WO2023220404A1 (en) * | 2022-05-13 | 2023-11-16 | Terns Pharmaceuticals, Inc. | Treatment of non-alcoholic steatohepatitis |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP1140079B1 (en) | 1998-12-23 | 2009-06-03 | Glaxo Group Limited | 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 |
| ATE381542T1 (de) | 2001-08-13 | 2008-01-15 | Phenex Pharmaceuticals Ag | Nr1h4-kern-rezeptor-bindende verbindungen |
| AU2003248861B2 (en) | 2002-07-09 | 2009-01-22 | Bristol-Myers Squibb Company | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| WO2004048349A1 (en) * | 2002-11-22 | 2004-06-10 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| BRPI0707427A2 (pt) * | 2006-02-03 | 2011-05-03 | Lilly Co Eli | composto ou um sal farmaceuticamente aceitável do mesmo, método para tratar dislipidemia, aterosclerose, e diabetes e complicações da mesma, para elevar os nìveis plásmicos de hdl, e para diminuir triglicerìdeos plásmicos, composição farmacêutica, e, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo |
| TW200812982A (en) | 2006-05-24 | 2008-03-16 | Lilly Co Eli | Compounds and methods for modulating FXR |
| WO2007140183A1 (en) | 2006-05-24 | 2007-12-06 | Eli Lilly And Company | Fxr agonists |
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