ES2374165T3 - Agonistas del receptor x farnesoide. - Google Patents
Agonistas del receptor x farnesoide. Download PDFInfo
- Publication number
- ES2374165T3 ES2374165T3 ES06840218T ES06840218T ES2374165T3 ES 2374165 T3 ES2374165 T3 ES 2374165T3 ES 06840218 T ES06840218 T ES 06840218T ES 06840218 T ES06840218 T ES 06840218T ES 2374165 T3 ES2374165 T3 ES 2374165T3
- Authority
- ES
- Spain
- Prior art keywords
- methyl
- compound
- formula
- dichlorophenyl
- oxy
- 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.)
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- 239000000556 agonist Substances 0.000 title description 10
- 150000001875 compounds Chemical class 0.000 claims description 312
- 238000011282 treatment Methods 0.000 claims description 95
- 239000000203 mixture Substances 0.000 claims description 71
- 125000000217 alkyl group Chemical group 0.000 claims description 56
- 102100038495 Bile acid receptor Human genes 0.000 claims description 54
- 239000003814 drug Substances 0.000 claims description 33
- 206010016654 Fibrosis Diseases 0.000 claims description 32
- 230000004761 fibrosis Effects 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 31
- -1 {[3- (2,6-dichlorophenyl) -5- (1-methylethyl) -4-isoxazolyl] methyl} oxy Chemical group 0.000 claims description 26
- 125000003342 alkenyl group Chemical group 0.000 claims description 24
- 238000002360 preparation method Methods 0.000 claims description 24
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 23
- 239000002253 acid Substances 0.000 claims description 21
- 239000012453 solvate Substances 0.000 claims description 18
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 17
- 210000000056 organ Anatomy 0.000 claims description 17
- 206010008635 Cholestasis Diseases 0.000 claims description 16
- 125000001188 haloalkyl group Chemical group 0.000 claims description 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 230000001404 mediated effect Effects 0.000 claims description 14
- 101100347612 Arabidopsis thaliana VIII-B gene Proteins 0.000 claims description 12
- 125000001424 substituent group Chemical group 0.000 claims description 12
- TUOXXRMLFZBSTB-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl TUOXXRMLFZBSTB-UHFFFAOYSA-N 0.000 claims description 11
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 229910052739 hydrogen Inorganic materials 0.000 claims description 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 8
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical class OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 claims description 8
- 239000003937 drug carrier Substances 0.000 claims description 7
- 239000003085 diluting agent Substances 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 238000002560 therapeutic procedure Methods 0.000 claims description 6
- DVZSPFZSZKKWIK-UHFFFAOYSA-N 6-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C(O)=O)C(Cl)=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl DVZSPFZSZKKWIK-UHFFFAOYSA-N 0.000 claims description 5
- ZHXAPIVBWDJTLN-UHFFFAOYSA-N 6-[4-[[3-[(2,6-dichlorophenyl)methyl]-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1CC1=C(Cl)C=CC=C1Cl ZHXAPIVBWDJTLN-UHFFFAOYSA-N 0.000 claims description 5
- GSTNOFVRIRGPDE-UHFFFAOYSA-N 7-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-2-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=C(C=CC3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl GSTNOFVRIRGPDE-UHFFFAOYSA-N 0.000 claims description 5
- YEOXFVQGKAJALY-UHFFFAOYSA-N 7-[4-[[3-[2-(2,6-dichlorophenyl)ethyl]-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C(C(O)=O)=CC=CC3=CC=2)C=CC=1OCC1=C(C(C)C)ON=C1CCC1=C(Cl)C=CC=C1Cl YEOXFVQGKAJALY-UHFFFAOYSA-N 0.000 claims description 5
- MXNUTDJISLUBCR-UHFFFAOYSA-N 7-[4-[[3-[2-(2,6-dichlorophenyl)ethyl]-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-2-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=C(C=CC3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1CCC1=C(Cl)C=CC=C1Cl MXNUTDJISLUBCR-UHFFFAOYSA-N 0.000 claims description 5
- KNQWLANNMODPOI-UHFFFAOYSA-N 3-(2,6-dichlorophenyl)-5-propan-2-yl-4-[[4-[5-(2h-tetrazol-5-yl)naphthalen-2-yl]phenoxy]methyl]-1,2-oxazole Chemical compound CC(C)C=1ON=C(C=2C(=CC=CC=2Cl)Cl)C=1COC(C=C1)=CC=C1C(C=C1C=CC=2)=CC=C1C=2C1=NN=NN1 KNQWLANNMODPOI-UHFFFAOYSA-N 0.000 claims description 4
- NWFKPERKLYEWII-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carbonitrile Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C#N)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl NWFKPERKLYEWII-UHFFFAOYSA-N 0.000 claims description 4
- FMCUKPUIJFXDAZ-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxamide Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C(N)=O)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl FMCUKPUIJFXDAZ-UHFFFAOYSA-N 0.000 claims description 4
- ZGRHLDTXNJVJLX-UHFFFAOYSA-N 6-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-2-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=CC(=CC3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl ZGRHLDTXNJVJLX-UHFFFAOYSA-N 0.000 claims description 4
- KTLMJKKEKJASFK-UHFFFAOYSA-N 6-[4-[[3-[2-(2,6-dichlorophenyl)ethyl]-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C=CC=C(C3=CC=2)C(O)=O)C=CC=1OCC1=C(C(C)C)ON=C1CCC1=C(Cl)C=CC=C1Cl KTLMJKKEKJASFK-UHFFFAOYSA-N 0.000 claims description 4
- MPCDMRMAXXSILO-UHFFFAOYSA-N 6-[4-[[5-cyclobutyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C2C(C(=O)O)=CC=CC2=CC=1C(C=C1)=CC=C1OCC1=C(C2CCC2)ON=C1C1=C(Cl)C=CC=C1Cl MPCDMRMAXXSILO-UHFFFAOYSA-N 0.000 claims description 4
- KVNUJCGFGCPUOA-UHFFFAOYSA-N 7-[4-[[3-(2,6-dichlorophenyl)-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-1-carboxylic acid Chemical compound C=1C=C(C=2C=C3C(C(O)=O)=CC=CC3=CC=2)C=CC=1OCC1=C(C(C)C)ON=C1C1=C(Cl)C=CC=C1Cl KVNUJCGFGCPUOA-UHFFFAOYSA-N 0.000 claims description 4
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims description 4
- 125000004450 alkenylene group Chemical group 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 159000000000 sodium salts Chemical class 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 229910003827 NRaRb Inorganic materials 0.000 claims description 3
- 150000002825 nitriles Chemical class 0.000 claims description 3
- XDENVSFWQSKKLZ-UHFFFAOYSA-N 1,2,4-oxadiazolidine-3,5-dione Chemical class O=C1NOC(=O)N1 XDENVSFWQSKKLZ-UHFFFAOYSA-N 0.000 claims description 2
- FUOSTELFLYZQCW-UHFFFAOYSA-N 1,2-oxazol-3-one Chemical class OC=1C=CON=1 FUOSTELFLYZQCW-UHFFFAOYSA-N 0.000 claims description 2
- YSVFAMDLJASIGW-UHFFFAOYSA-N 5h-1,2,3,5-oxathiadiazole 2-oxide Chemical class O=S1NC=NO1 YSVFAMDLJASIGW-UHFFFAOYSA-N 0.000 claims description 2
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical compound C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 claims description 2
- NBYFMFAXGSZXDW-UHFFFAOYSA-N methyl 6-[4-[[3-[2-(2,6-dichlorophenyl)ethyl]-5-propan-2-yl-1,2-oxazol-4-yl]methoxy]phenyl]naphthalene-2-carboxylate Chemical compound C1=CC2=CC(C(=O)OC)=CC=C2C=C1C(C=C1)=CC=C1OCC(=C(ON=1)C(C)C)C=1CCC1=C(Cl)C=CC=C1Cl NBYFMFAXGSZXDW-UHFFFAOYSA-N 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims 8
- 238000000034 method Methods 0.000 abstract description 60
- 239000008194 pharmaceutical composition Chemical class 0.000 abstract description 25
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- 150000002545 isoxazoles Chemical class 0.000 abstract 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 183
- 239000000243 solution Substances 0.000 description 149
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical group CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 100
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 86
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 85
- 235000019439 ethyl acetate Nutrition 0.000 description 68
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 63
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 58
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 54
- CSNNHWWHGAXBCP-UHFFFAOYSA-L Magnesium sulfate Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 description 52
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 51
- 101150027485 NR1H4 gene Proteins 0.000 description 50
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 49
- 239000007787 solid Substances 0.000 description 37
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 36
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 33
- 238000005481 NMR spectroscopy Methods 0.000 description 32
- 235000002639 sodium chloride Nutrition 0.000 description 31
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- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 23
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 22
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- WJKHJLXJJJATHN-UHFFFAOYSA-N triflic anhydride Chemical compound FC(F)(F)S(=O)(=O)OS(=O)(=O)C(F)(F)F WJKHJLXJJJATHN-UHFFFAOYSA-N 0.000 description 22
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- 125000005843 halogen group Chemical group 0.000 description 18
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Classifications
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
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- 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
- 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
Landscapes
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75159705P | 2005-12-19 | 2005-12-19 | |
| US751597P | 2005-12-19 | ||
| PCT/US2006/061966 WO2007076260A2 (en) | 2005-12-19 | 2006-12-13 | Farnesoid x receptor agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2374165T3 true ES2374165T3 (es) | 2012-02-14 |
Family
ID=38218762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES06840218T Active ES2374165T3 (es) | 2005-12-19 | 2006-12-13 | Agonistas del receptor x farnesoide. |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7705028B2 (enExample) |
| EP (1) | EP1962838B1 (enExample) |
| JP (1) | JP5081161B2 (enExample) |
| AT (1) | ATE526318T1 (enExample) |
| ES (1) | ES2374165T3 (enExample) |
| WO (1) | WO2007076260A2 (enExample) |
Families Citing this family (73)
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| JP5301286B2 (ja) * | 2006-02-03 | 2013-09-25 | イーライ リリー アンド カンパニー | Ｆｘ受容体を調節するための化合物及び方法 |
| CL2007003035A1 (es) * | 2006-10-24 | 2008-05-16 | Smithkline Beechman Corp | Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos, |
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| US7943619B2 (en) | 2007-12-04 | 2011-05-17 | Hoffmann-La Roche Inc. | Isoxazolo-pyridazine derivatives |
| CA2706990C (en) | 2007-12-04 | 2016-05-10 | F. Hoffmann-La Roche Ag | Isoxazolo-pyrazine derivatives |
| EP2367554A4 (en) * | 2008-11-26 | 2020-03-25 | Satiogen Pharmaceuticals, Inc. | Bile acid reflux inhibitor for the treatment of obesity and diabetes |
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| WO2010127976A1 (en) | 2009-05-05 | 2010-11-11 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives |
| AU2010244552A1 (en) | 2009-05-05 | 2011-09-29 | F. Hoffmann-La Roche Ag | Isoxazole-pyrazole derivatives |
| ES2467701T3 (es) | 2009-05-05 | 2014-06-12 | F. Hoffmann-La Roche Ag | Derivados de isoxazol-piridazina |
| AU2010244555A1 (en) | 2009-05-07 | 2011-11-03 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives as GABA modulators |
| EP2289883A1 (en) | 2009-08-19 | 2011-03-02 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| EP3593802A3 (en) | 2010-05-26 | 2020-03-25 | Satiogen Pharmaceuticals, Inc. | Bile acid recycling inhibitors and satiogens for treatment of diabetes, obesity, and inflammatory gastrointestinal conditions |
| 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 |
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| KR102051031B1 (ko) | 2011-10-28 | 2019-12-02 | 루메나 파마수티컬즈, 인코포레이티드 | 고담혈증 및 담즙 정체성 간 질환 치료용 담즙산 재순환 억제제 |
| BR112014010223B8 (pt) | 2011-10-28 | 2021-02-23 | Lumena Pharmaceuticals Llc | uso de uma composição compreendendo inibidores de reciclagem de ácido de bílis e forma de dosagem pediátrica |
| KR20160003664A (ko) | 2013-03-15 | 2016-01-11 | 루메나 파마수티컬즈, 인코포레이티드 | 바렛 식도 및 위식도 역류 질환 치료용 담즙산 재순환 억제제 |
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| PL3043865T3 (pl) | 2013-09-11 | 2021-07-05 | Institut National De La Santé Et De La Recherche Médicale (Inserm) | SPOSOBY I KOMPOZYCjE FARMACEUTYCZNE W LECZENIU ZAKAŻENIA WIRUSEM ZAPALENIA WĄTROBY TYPU B |
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| EP3463373A4 (en) * | 2016-05-25 | 2020-04-22 | Akarna Therapeutics, Ltd. | COMBINATION THERAPIES WITH FARNESOID-X RECEPTOR (FRX) MODULATORS |
| US10772813B2 (en) | 2016-06-03 | 2020-09-15 | Colradel, LLC | Compositions and methods of administering a colchicine based topical composition for the prevention of radiation fibrosis |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| BR112018075734A2 (pt) | 2016-06-13 | 2019-04-02 | Gilead Sciences, Inc. | composto, composição farmacêutica, método para tratar um paciente com uma doença ou condição mediada pelo menos em parte por fxr, e, uso de um composto. |
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| US20210085662A1 (en) | 2017-03-30 | 2021-03-25 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses |
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| KR102905880B1 (ko) | 2019-02-15 | 2025-12-29 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 치환된 비시클릭 화합물 |
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| AU2020312735A1 (en) | 2019-07-18 | 2021-12-16 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| WO2021108974A1 (en) | 2019-12-03 | 2021-06-10 | Gannex Pharma Co., Ltd | Compounds for modulating activity of fxr and uses thereof |
| US20230060715A1 (en) | 2020-01-15 | 2023-03-02 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of fxr agonists for treating an infection by hepatitis d virus |
| US20240100125A1 (en) | 2021-01-14 | 2024-03-28 | Enyo Pharma | Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection |
| CN117320722A (zh) | 2021-04-28 | 2023-12-29 | 埃尼奥制药公司 | 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用 |
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| GB9706707D0 (en) | 1997-04-02 | 1997-05-21 | Glaxo Group Ltd | Chemical compounds |
| US6639076B1 (en) * | 1998-08-18 | 2003-10-28 | Eli Lilly And Company | Growth hormone secretagogues |
| ES2326850T3 (es) * | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| US20070010562A1 (en) | 2001-08-13 | 2007-01-11 | Ulrike Bauer | Nr1h4 nuclear receptor binding compounds |
| AU2002333655A1 (en) * | 2001-09-25 | 2003-04-07 | Smithkline Beecham Corporation | Bicyclic heterocycles as rxr ligands |
| AU2003219028A1 (en) | 2002-04-13 | 2003-10-27 | Lion Bioscience Ag | NON-PRIMATE FXRb AS A LANOSTEROL SENSING NUCLEAR HORMONE RECEPTOR AND RELATED USES |
| US7232828B2 (en) * | 2002-08-10 | 2007-06-19 | Bethesda Pharmaceuticals, Inc. | PPAR Ligands that do not cause fluid retention, edema or congestive heart failure |
| 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 |
| WO2007072751A1 (ja) | 2005-12-20 | 2007-06-28 | Sharp Kabushiki Kaisha | 送信機および送信方法 |
| JP5301286B2 (ja) * | 2006-02-03 | 2013-09-25 | イーライ リリー アンド カンパニー | Ｆｘ受容体を調節するための化合物及び方法 |
| WO2007109275A2 (en) | 2006-03-20 | 2007-09-27 | Bayer Healthcare Llc. | Paclitaxel combination |
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Also Published As
| Publication number | Publication date |
|---|---|
| WO2007076260A3 (en) | 2007-11-01 |
| US20100160398A1 (en) | 2010-06-24 |
| EP1962838A2 (en) | 2008-09-03 |
| JP5081161B2 (ja) | 2012-11-21 |
| EP1962838A4 (en) | 2009-11-18 |
| ATE526318T1 (de) | 2011-10-15 |
| WO2007076260A2 (en) | 2007-07-05 |
| US20080167356A1 (en) | 2008-07-10 |
| US8158665B2 (en) | 2012-04-17 |
| JP2009519965A (ja) | 2009-05-21 |
| EP1962838B1 (en) | 2011-09-28 |
| US7705028B2 (en) | 2010-04-27 |
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