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
- -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
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 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
- 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 atom 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
- 239000000546 pharmaceutical excipient 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 (cg-RX-API-DMAC7.html) | 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 (82)
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| 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 |
| CN103370315A (zh) * | 2010-12-20 | 2013-10-23 | Irm责任有限公司 | 用于调控法尼醇x受体的组合物和方法 |
| 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 |
| EP2655369A1 (en) * | 2010-12-20 | 2013-10-30 | 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 |
| 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 |
| HRP20201953T1 (hr) | 2013-09-11 | 2021-04-30 | Institut National De La Santé Et De La Recherche Médicale (Inserm) | Postupci i farmaceutski pripravci za liječenje virusne infekcije hepatitisom b |
| DK3065738T3 (en) | 2013-11-05 | 2018-06-06 | 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 |
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