RU2012157646A - Комбинированная терапия для кожных нарушений - Google Patents
Комбинированная терапия для кожных нарушений Download PDFInfo
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- RU2012157646A RU2012157646A RU2012157646/15A RU2012157646A RU2012157646A RU 2012157646 A RU2012157646 A RU 2012157646A RU 2012157646/15 A RU2012157646/15 A RU 2012157646/15A RU 2012157646 A RU2012157646 A RU 2012157646A RU 2012157646 A RU2012157646 A RU 2012157646A
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- Prior art keywords
- bms
- alkyl
- alkenyl
- inhibitors
- acyl
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- 238000002648 combination therapy Methods 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims abstract 21
- -1 YM-92088 Chemical compound 0.000 claims abstract 11
- 239000003112 inhibitor Substances 0.000 claims abstract 10
- 125000004388 isoflavanoid group Chemical group 0.000 claims abstract 8
- 239000000051 antiandrogen Substances 0.000 claims abstract 6
- 239000003446 ligand Substances 0.000 claims abstract 6
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 claims abstract 6
- 229960002256 spironolactone Drugs 0.000 claims abstract 6
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims abstract 4
- 239000003242 anti bacterial agent Substances 0.000 claims abstract 4
- 229940088710 antibiotic agent Drugs 0.000 claims abstract 4
- 229960000997 bicalutamide Drugs 0.000 claims abstract 4
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims abstract 4
- 229960002074 flutamide Drugs 0.000 claims abstract 4
- 239000003394 isomerase inhibitor Substances 0.000 claims abstract 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 4
- 229910052794 bromium Inorganic materials 0.000 claims abstract 3
- 229910052801 chlorine Inorganic materials 0.000 claims abstract 3
- JWJOTENAMICLJG-QWBYCMEYSA-N dutasteride Chemical compound O=C([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)N[C@@H]4CC3)C)CC[C@@]21C)NC1=CC(C(F)(F)F)=CC=C1C(F)(F)F JWJOTENAMICLJG-QWBYCMEYSA-N 0.000 claims abstract 3
- 229960004199 dutasteride Drugs 0.000 claims abstract 3
- 229910052731 fluorine Inorganic materials 0.000 claims abstract 3
- 229910052740 iodine Inorganic materials 0.000 claims abstract 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims abstract 3
- 229920002554 vinyl polymer Polymers 0.000 claims abstract 3
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 claims abstract 2
- WQBIOEFDDDEARX-CHWSQXEVSA-N (4ar,10br)-8-chloro-4-methyl-1,2,4a,5,6,10b-hexahydrobenzo[f]quinolin-3-one Chemical compound C1CC2=CC(Cl)=CC=C2[C@@H]2[C@@H]1N(C)C(=O)CC2 WQBIOEFDDDEARX-CHWSQXEVSA-N 0.000 claims abstract 2
- IATHDHXYPWSJAL-UHFFFAOYSA-N 1,6,10-trihydroxy-2,8,10-trimethylanthracen-9-one Chemical compound C1=C(O)C=C2C(O)(C)C3=CC=C(C)C(O)=C3C(=O)C2=C1C IATHDHXYPWSJAL-UHFFFAOYSA-N 0.000 claims abstract 2
- GCBADRSMMMEBOC-UHFFFAOYSA-N 1,6,10-trihydroxy-2-(hydroxymethyl)-8,10-dimethylanthracen-9-one Chemical compound O=C1C2=C(O)C(CO)=CC=C2C(O)(C)C2=C1C(C)=CC(O)=C2 GCBADRSMMMEBOC-UHFFFAOYSA-N 0.000 claims abstract 2
- OUEODVPKPRQETQ-OCZCAGDBSA-N 2-chloro-4-[(1R,5S)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl]-3-methylbenzonitrile Chemical compound CC1=C(Cl)C(C#N)=CC=C1N1[C@@H]2CC[C@H]1CC(C)(O)C2 OUEODVPKPRQETQ-OCZCAGDBSA-N 0.000 claims abstract 2
- 108090000117 3-alpha-(17-beta)-hydroxysteroid dehydrogenase (NAD(+)) Proteins 0.000 claims abstract 2
- CYCKLVAQENOQPG-UHFFFAOYSA-N 4-(4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C(C#N)C(C(F)(F)F)=C1 CYCKLVAQENOQPG-UHFFFAOYSA-N 0.000 claims abstract 2
- ARBYGDBJECGMGA-UHFFFAOYSA-N 4-[3-(4-hydroxybutyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile Chemical compound O=C1C(C)(C)N(CCCCO)C(=O)N1C1=CC=C(C#N)C(C(F)(F)F)=C1 ARBYGDBJECGMGA-UHFFFAOYSA-N 0.000 claims abstract 2
- FIDNKDVRTLFETI-UHFFFAOYSA-N 4-[3-(4-hydroxybutyl)-4,4-dimethyl-5-oxo-2-sulfanylideneimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile Chemical compound O=C1C(C)(C)N(CCCCO)C(=S)N1C1=CC=C(C#N)C(C(F)(F)F)=C1 FIDNKDVRTLFETI-UHFFFAOYSA-N 0.000 claims abstract 2
- ZVWXHSNUBLIKJH-UHFFFAOYSA-N 4-[3-(cyanomethyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile Chemical compound O=C1C(C)(C)N(CC#N)C(=O)N1C1=CC=C(C#N)C(C(F)(F)F)=C1 ZVWXHSNUBLIKJH-UHFFFAOYSA-N 0.000 claims abstract 2
- KALFKWQLCWAXJO-WCFLWFBJSA-N 4-[[(1r,7s,7as)-7-hydroxy-1-(trifluoromethyl)-5,6,7,7a-tetrahydro-1h-pyrrolo[1,2-c][1,3]oxazol-3-ylidene]amino]-2-chloro-3-methylbenzonitrile Chemical compound CC1=C(Cl)C(C#N)=CC=C1N=C1N2CC[C@H](O)[C@H]2[C@H](C(F)(F)F)O1 KALFKWQLCWAXJO-WCFLWFBJSA-N 0.000 claims abstract 2
- HWLLYFXDDGGHOE-BCSUUIJWSA-N 6-[(2r,5r)-2-methyl-5-[(1r)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1h-quinolin-2-one Chemical compound C[C@@H]1CC[C@H]([C@@H](O)C(F)(F)F)N1C1=CC=C(NC(=O)C=C2C(F)(F)F)C2=C1 HWLLYFXDDGGHOE-BCSUUIJWSA-N 0.000 claims abstract 2
- 108010062875 Hydroxysteroid Dehydrogenases Proteins 0.000 claims abstract 2
- 102000011145 Hydroxysteroid Dehydrogenases Human genes 0.000 claims abstract 2
- 102000004317 Lyases Human genes 0.000 claims abstract 2
- 108090000856 Lyases Proteins 0.000 claims abstract 2
- 102000023984 PPAR alpha Human genes 0.000 claims abstract 2
- 108010015181 PPAR delta Proteins 0.000 claims abstract 2
- 101150014691 PPARA gene Proteins 0.000 claims abstract 2
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims abstract 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims abstract 2
- 102000001854 Steroid 17-alpha-Hydroxylase Human genes 0.000 claims abstract 2
- 108010015330 Steroid 17-alpha-Hydroxylase Proteins 0.000 claims abstract 2
- JDLUQDYTLSPFGS-FZCLSBEQSA-N [(3s,3as,9as,9bs)-6-ethyl-3a-methyl-7-oxo-2,3,4,5,8,9,9a,9b-octahydro-1h-cyclopenta[a]naphthalen-3-yl] acetate Chemical compound C1C[C@]2(C)[C@@H](OC(C)=O)CC[C@H]2[C@@H]2CCC(=O)C(CC)=C21 JDLUQDYTLSPFGS-FZCLSBEQSA-N 0.000 claims abstract 2
- 229950008527 bexlosteride Drugs 0.000 claims abstract 2
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims abstract 2
- 229960000978 cyproterone acetate Drugs 0.000 claims abstract 2
- 239000003687 estradiol congener Substances 0.000 claims abstract 2
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 claims abstract 2
- 229960004039 finasteride Drugs 0.000 claims abstract 2
- YPQLFJODEKMJEF-UHFFFAOYSA-N hydroxyflutamide Chemical compound CC(C)(O)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 YPQLFJODEKMJEF-UHFFFAOYSA-N 0.000 claims abstract 2
- 229960004125 ketoconazole Drugs 0.000 claims abstract 2
- OMXGOGXEWUCLFI-UHFFFAOYSA-N lgd-3303 Chemical compound N1C(=O)C=C(Cl)C2=C1C=CC1=C2C(C)=C(CC)N1CC(F)(F)F OMXGOGXEWUCLFI-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000002697 lyase inhibitor Substances 0.000 claims abstract 2
- XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 claims abstract 2
- 229960002653 nilutamide Drugs 0.000 claims abstract 2
- 229940127234 oral contraceptive Drugs 0.000 claims abstract 2
- 239000003539 oral contraceptive agent Substances 0.000 claims abstract 2
- 108091008725 peroxisome proliferator-activated receptors alpha Proteins 0.000 claims abstract 2
- 150000003146 progesterones Chemical class 0.000 claims abstract 2
- 125000006725 C1-C10 alkenyl group Chemical group 0.000 claims 15
- 125000002252 acyl group Chemical group 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- ADFCQWZHKCXPAJ-UHFFFAOYSA-N 3-(4-Hydroxyphenyl)chroman-7-ol Chemical compound C1=CC(O)=CC=C1C1CC2=CC=C(O)C=C2OC1 ADFCQWZHKCXPAJ-UHFFFAOYSA-N 0.000 claims 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 6
- ILJSQTXMGCGYMG-UHFFFAOYSA-N triacetic acid Chemical compound CC(=O)CC(=O)CC(O)=O ILJSQTXMGCGYMG-UHFFFAOYSA-N 0.000 claims 4
- 239000004098 Tetracycline Substances 0.000 claims 3
- 229960002180 tetracycline Drugs 0.000 claims 3
- 229930101283 tetracycline Natural products 0.000 claims 3
- 235000019364 tetracycline Nutrition 0.000 claims 3
- 150000003522 tetracyclines Chemical class 0.000 claims 3
- SGKRLCUYIXIAHR-AKNGSSGZSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O SGKRLCUYIXIAHR-AKNGSSGZSA-N 0.000 claims 2
- UHHHTIKWXBRCLT-VDBOFHIQSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide;ethanol;hydrate;dihydrochloride Chemical compound O.Cl.Cl.CCO.C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O.C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O UHHHTIKWXBRCLT-VDBOFHIQSA-N 0.000 claims 2
- FZKWRPSUNUOXKJ-CVHRZJFOSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide;hydrate Chemical compound O.C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O FZKWRPSUNUOXKJ-CVHRZJFOSA-N 0.000 claims 2
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 claims 2
- WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 claims 2
- 229910004013 NO 2 Inorganic materials 0.000 claims 2
- 229960003957 dexamethasone Drugs 0.000 claims 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 2
- 229960003722 doxycycline Drugs 0.000 claims 2
- 229960001172 doxycycline hyclate Drugs 0.000 claims 2
- 229960004434 doxycycline monohydrate Drugs 0.000 claims 2
- 229960000785 fluocinonide Drugs 0.000 claims 2
- 229940070710 valerate Drugs 0.000 claims 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims 2
- RDEIXVOBVLKYNT-VQBXQJRRSA-N (2r,3r,4r,5r)-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(1-aminoethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol;(2r,3r,4r,5r)-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]o Chemical compound OS(O)(=O)=O.O1C[C@@](O)(C)[C@H](NC)[C@@H](O)[C@H]1O[C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@H](CC[C@@H](CN)O2)N)[C@@H](N)C[C@H]1N.O1C[C@@](O)(C)[C@H](NC)[C@@H](O)[C@H]1O[C@@H]1[C@@H](O)[C@H](O[C@@H]2[C@@H](CC[C@H](O2)C(C)N)N)[C@@H](N)C[C@H]1N.O1[C@H](C(C)NC)CC[C@@H](N)[C@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](NC)[C@@](C)(O)CO2)O)[C@H](N)C[C@@H]1N RDEIXVOBVLKYNT-VQBXQJRRSA-N 0.000 claims 1
- FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 claims 1
- MINDHVHHQZYEEK-UHFFFAOYSA-N (E)-(2S,3R,4R,5S)-5-[(2S,3S,4S,5S)-2,3-epoxy-5-hydroxy-4-methylhexyl]tetrahydro-3,4-dihydroxy-(beta)-methyl-2H-pyran-2-crotonic acid ester with 9-hydroxynonanoic acid Natural products CC(O)C(C)C1OC1CC1C(O)C(O)C(CC(C)=CC(=O)OCCCCCCCCC(O)=O)OC1 MINDHVHHQZYEEK-UHFFFAOYSA-N 0.000 claims 1
- WHBHBVVOGNECLV-OBQKJFGGSA-N 11-deoxycortisol Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 WHBHBVVOGNECLV-OBQKJFGGSA-N 0.000 claims 1
- WFJIVOKAWHGMBH-UHFFFAOYSA-N 4-hexylbenzene-1,3-diol Chemical compound CCCCCCC1=CC=C(O)C=C1O WFJIVOKAWHGMBH-UHFFFAOYSA-N 0.000 claims 1
- ULBPQWIGZUGPHU-UHFFFAOYSA-N 6-[bis(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)quinolin-2(1h)-one Chemical compound N1C(=O)C=C(C(F)(F)F)C2=CC(N(CC(F)(F)F)CC(F)(F)F)=CC=C21 ULBPQWIGZUGPHU-UHFFFAOYSA-N 0.000 claims 1
- MYYIMZRZXIQBGI-HVIRSNARSA-N 6alpha-Fluoroprednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3C[C@H](F)C2=C1 MYYIMZRZXIQBGI-HVIRSNARSA-N 0.000 claims 1
- HCKFPALGXKOOBK-NRYMJLQJSA-N 7332-27-6 Chemical compound C1([C@]2(O[C@]3([C@@]4(C)C[C@H](O)[C@]5(F)[C@@]6(C)C=CC(=O)C=C6CC[C@H]5[C@@H]4C[C@H]3O2)C(=O)CO)C)=CC=CC=C1 HCKFPALGXKOOBK-NRYMJLQJSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 108010001478 Bacitracin Proteins 0.000 claims 1
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- VPGRYOFKCNULNK-ACXQXYJUSA-N Deoxycorticosterone acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)COC(=O)C)[C@@]1(C)CC2 VPGRYOFKCNULNK-ACXQXYJUSA-N 0.000 claims 1
- WYQPLTPSGFELIB-JTQPXKBDSA-N Difluprednate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2CC[C@@](C(=O)COC(C)=O)(OC(=O)CCC)[C@@]2(C)C[C@@H]1O WYQPLTPSGFELIB-JTQPXKBDSA-N 0.000 claims 1
- POPFMWWJOGLOIF-XWCQMRHXSA-N Flurandrenolide Chemical compound C1([C@@H](F)C2)=CC(=O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O POPFMWWJOGLOIF-XWCQMRHXSA-N 0.000 claims 1
- DLVOSEUFIRPIRM-KAQKJVHQSA-N Hydrocortisone cypionate Chemical compound O=C([C@@]1(O)CC[C@H]2[C@H]3[C@@H]([C@]4(CCC(=O)C=C4CC3)C)[C@@H](O)C[C@@]21C)COC(=O)CCC1CCCC1 DLVOSEUFIRPIRM-KAQKJVHQSA-N 0.000 claims 1
- GZENKSODFLBBHQ-ILSZZQPISA-N Medrysone Chemical compound C([C@@]12C)CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@H](C(C)=O)CC[C@H]21 GZENKSODFLBBHQ-ILSZZQPISA-N 0.000 claims 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 1
- 108010093965 Polymyxin B Proteins 0.000 claims 1
- UFUVLHLTWXBHGZ-MGZQPHGTSA-N [(2r,3r,4s,5r,6r)-6-[(1s,2s)-2-chloro-1-[[(2s,4r)-1-methyl-4-propylpyrrolidine-2-carbonyl]amino]propyl]-4,5-dihydroxy-2-methylsulfanyloxan-3-yl] dihydrogen phosphate Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](OP(O)(O)=O)[C@@H](SC)O1 UFUVLHLTWXBHGZ-MGZQPHGTSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 229950003408 amcinafide Drugs 0.000 claims 1
- 229960003071 bacitracin Drugs 0.000 claims 1
- 229930184125 bacitracin Natural products 0.000 claims 1
- CLKOFPXJLQSYAH-ABRJDSQDSA-N bacitracin A Chemical compound C1SC([C@@H](N)[C@@H](C)CC)=N[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]1C(=O)N[C@H](CCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2N=CNC=2)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC1 CLKOFPXJLQSYAH-ABRJDSQDSA-N 0.000 claims 1
- 229950000210 beclometasone dipropionate Drugs 0.000 claims 1
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- 229960000676 flunisolide Drugs 0.000 claims 1
- 229960001347 fluocinolone acetonide Drugs 0.000 claims 1
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 claims 1
- FAOZLTXFLGPHNG-KNAQIMQKSA-N fluorometholone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FAOZLTXFLGPHNG-KNAQIMQKSA-N 0.000 claims 1
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- PGBHMTALBVVCIT-VCIWKGPPSA-N framycetin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CN)O2)N)O[C@@H]1CO PGBHMTALBVVCIT-VCIWKGPPSA-N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 229960003258 hexylresorcinol Drugs 0.000 claims 1
- 229960003331 hydrocortisone cypionate Drugs 0.000 claims 1
- 229960000631 hydrocortisone valerate Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 229940124589 immunosuppressive drug Drugs 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 229960001810 meprednisone Drugs 0.000 claims 1
- PIDANAQULIKBQS-RNUIGHNZSA-N meprednisone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)CC2=O PIDANAQULIKBQS-RNUIGHNZSA-N 0.000 claims 1
- 229960000282 metronidazole Drugs 0.000 claims 1
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 claims 1
- 229960004023 minocycline Drugs 0.000 claims 1
- 229960003128 mupirocin Drugs 0.000 claims 1
- 229930187697 mupirocin Natural products 0.000 claims 1
- DDHVILIIHBIMQU-YJGQQKNPSA-L mupirocin calcium hydrate Chemical compound O.O.[Ca+2].C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC([O-])=O)OC1.C[C@H](O)[C@H](C)[C@@H]1O[C@H]1C[C@@H]1[C@@H](O)[C@@H](O)[C@H](C\C(C)=C\C(=O)OCCCCCCCCC([O-])=O)OC1 DDHVILIIHBIMQU-YJGQQKNPSA-L 0.000 claims 1
- 229940053050 neomycin sulfate Drugs 0.000 claims 1
- 229960001699 ofloxacin Drugs 0.000 claims 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 229920000024 polymyxin B Polymers 0.000 claims 1
- 229960005266 polymyxin b Drugs 0.000 claims 1
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 claims 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 claims 1
- DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 claims 1
- 239000002023 wood Substances 0.000 claims 1
- KEJORAMIZFOODM-PWSUYJOCSA-N 2-chloro-4-[(7r,7as)-7-hydroxy-1,3-dioxotetrahydro-1h-pyrrolo[1,2-c]imidazol-2(3h)-yl]-3-methylbenzonitrile Chemical compound CC1=C(Cl)C(C#N)=CC=C1N1C(=O)N2CC[C@@H](O)[C@H]2C1=O KEJORAMIZFOODM-PWSUYJOCSA-N 0.000 abstract 1
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Abstract
1. Применение пероральной композиции, содержащей одно или несколько антиандрогенных средств, один или несколько антибиотиков и изофлаваноид для облегчения состояния кожи у пациента, нуждающегося в этом.2. Пероральная композиция, содержащая одно или несколько антиандрогенных средств, один или несколько антибиотиков, изофлаваноид и фармацевтически приемлемые вспомогательные вещества или наполнители для облегчения состояния кожи.3. Композиция по п.2, в которой антиандрогенное средство содержит одно или несколько из пероральных противозачаточных средств, аналогов эстрогена, аналогов прогестерона, спиронолактона, инокотерон ацетата, ципротерон ацетата, флутамида, нилутамида, бикалутамида, кетоконазола, финастерида, дутастерида, бекслостерида, изонстерида, эпрестерида, туростерида, изофлаваноида, RU-58642, RU-56279, WS9761 A и B, RU-59063, RU-58841, бекслостерида, LG-2293, L-245976, LG-121071, LG-121091, LG-121104, LGD-2226, LGD-2941, YM-92088, YM-175735, LGD-1331, LGD-3303, BMS-357597, BMS-30 391197, S-40503, BMS-482404, EM-4283, EM-4977, BMS-564929, BMS-391197, BMS-434588, BMS-487745, BMS-501949, SA-766, YM-92088, YM-580, LG-123303, LG-123129, PMCol, YM-175735, BMS-591305, BMS-591309, BMS-665139, BMS-665539, CE 590, 116BG33, 154BG31, аркарина, ACP-105, флутамида, гидроксифлутамида, бикалутамида, нилутарнида, ингибиторов гидроксистероиддегидрогеназы, лигандов PPARa, лигандов PPARα, лигандов PPAR двойного действия, PN-2034, PPAR δ; ингибиторов 17-кеторедуктазы, ингибиторов 3β-DHΔ4,6-изомеразы, ингибиторов 3β-DHΔ4,5-изомеразы, ингибиторов 17,20 десмолазы, ингибиторов p450c17, ингибиторов p450ssc и ингибиторов 17,20-лиазы.4. Композиция по п.2, где изофлаваноид содержит,,где R-Rнезависимо представляют собой H, OH, C-Cалкил, C-Cалкенил, C-Cалкинил, винил, N, CN, Cl, Br, F, I, NO, C(O)O(C-Cалкил), C(O)O(C-Cалкил), C(O)O(C-Cалкинил), C(O)O(C-Cалкенил), O(Cацил), O(C-Cалкил), O(C-Cалкени�
Claims (12)
1. Применение пероральной композиции, содержащей одно или несколько антиандрогенных средств, один или несколько антибиотиков и изофлаваноид для облегчения состояния кожи у пациента, нуждающегося в этом.
2. Пероральная композиция, содержащая одно или несколько антиандрогенных средств, один или несколько антибиотиков, изофлаваноид и фармацевтически приемлемые вспомогательные вещества или наполнители для облегчения состояния кожи.
3. Композиция по п.2, в которой антиандрогенное средство содержит одно или несколько из пероральных противозачаточных средств, аналогов эстрогена, аналогов прогестерона, спиронолактона, инокотерон ацетата, ципротерон ацетата, флутамида, нилутамида, бикалутамида, кетоконазола, финастерида, дутастерида, бекслостерида, изонстерида, эпрестерида, туростерида, изофлаваноида, RU-58642, RU-56279, WS9761 A и B, RU-59063, RU-58841, бекслостерида, LG-2293, L-245976, LG-121071, LG-121091, LG-121104, LGD-2226, LGD-2941, YM-92088, YM-175735, LGD-1331, LGD-3303, BMS-357597, BMS-30 391197, S-40503, BMS-482404, EM-4283, EM-4977, BMS-564929, BMS-391197, BMS-434588, BMS-487745, BMS-501949, SA-766, YM-92088, YM-580, LG-123303, LG-123129, PMCol, YM-175735, BMS-591305, BMS-591309, BMS-665139, BMS-665539, CE 590, 116BG33, 154BG31, аркарина, ACP-105, флутамида, гидроксифлутамида, бикалутамида, нилутарнида, ингибиторов гидроксистероиддегидрогеназы, лигандов PPARa, лигандов PPARα, лигандов PPAR двойного действия, PN-2034, PPAR δ; ингибиторов 17-кеторедуктазы, ингибиторов 3β-DHΔ4,6-изомеразы, ингибиторов 3β-DHΔ4,5-изомеразы, ингибиторов 17,20 десмолазы, ингибиторов p450c17, ингибиторов p450ssc и ингибиторов 17,20-лиазы.
4. Композиция по п.2, где изофлаваноид содержит
где R1-R9 независимо представляют собой H, OH, C1-C10 алкил, C1-C10 алкенил, C1-C10 алкинил, винил, N3, CN, Cl, Br, F, I, NO2, C(O)O(C1-C10 алкил), C(O)O(C1-C10 алкил), C(O)O(C1-C10 алкинил), C(O)O(C1-C10 алкенил), O(C1-18 ацил), O(C1-C10 алкил), O(C1-C10 алкенил), S(C1-C18 ацил), S(C1-C10 алкил), S(C1-C10 алкинил), S(C1-C10 алкенил), SO(C1-C18 ацил), SO(C1-C10 алкил), SO(C1-C10 алкинил), SO(C1-C10 алкенил), SO2(C1-C18 ацил), SO2(C1-C10 алкил), SO2(C1-C10 алкинил), SO2(C1-C10 алкенил), O3S(C1-C18 ацил), O3S(C1-C10 алкил), O3S(C1-C10 алкенил), NH2, NH(C1-C10 алкил), NH(C1-C10 алкенил), NH(C1-C10 алкинил), NH(C1-C18 ацил), N(C1-C10 алкил)2, N(C1-C18 ацил)2, где алкил, алкинил, алкенил и винил необязательно замещены N3, CN, одним-тремя галогенами (Cl, Br, F, I), NO2, С(O)О(C1-C10 алкил), С(O)O(C1-C10 алкил), С(O)О(C1-C10 алкинил), С(O)O(C1-C10 алкенил), O(C1-C18 ацил), О(C1-C10 алкил), О(C1-C10 алкенил), S(C1-C18 ацил), S(C1-C10 алкил), S(C1-C10 алкинил), S(C1-C10 алкенил), SO(C1-C18 ацил), SO(C1-C10 алкил), SO(C1-C10 алкинил), SO(C1-C10 алкенил), SO2(C1-C18 ацил), SO2(C1-C10 алкил), SO2(C1-C10 алкинил), SO2(C1-C10 алкенил), O3S(C1-C18 ацил), O3S(C1-C10 алкил), O3S(C1-C10 алкенил), NH2, NH(C1-C10 алкил), NH(C1-C10 алкенил), NH(C1-C10 алкинил), NH(C1-C18 ацил), N(C1-C10 алкил)2 и N(C1-C18 ацил)2.
5. Композиция по п.2, в которой антибиотик содержит один или несколько из мупироцина, неомицин сульфат бацитрацина, полимиксина B, 1-офлоксацина, клиндамицин фосфата, гентамицин сульфата, метронидазола, гексилрезорцинола, метилбензетония хлорида, фенола, соединений четвертичного аммония, масла чайного дерева, кортикостероидов, гидроксилтриамцинолон альфаметил дексаметазона, дексаметазонфосфата, беклометазон дипропионата, клобетазол валерата, десонида, дезоксиметазона, дезоксикортикостерон ацетата, дексаметазона, дихлоризона, дифлоразон диацетата, дифлукотолон валерата, флуадренолона, флукларолон ацетонида, флудрокортизона, флуметазон пивалата, флуоцинолон ацетонида, флуоцинонида, флукортин бутилового сложного эфира, флуокортолона, флупредниден (флупреднилиден) ацетата, флурандренолона, галцинонида, гидрокортизон ацетата, гидрокортизон бутирата, метилпреднизолона, триамцинолон ацетонида, кортизона, кортодоксона, флуцетонида, флудрокортизона, дифлуорозон диацетата, флурадреналон ацетонида, медризона, амциафела, амцинафида, бетаметазона, хлорпреднизона, хлорпреднизон ацетата, клокортелона, клесцинолона, дихлоризона, дифлупредната, флуклоронида, флунизолида, флуорометалона, флуперолона, флупреднизолона, гидрокортизон валерата, гидрокортизон циклопентилпропионата, гидрокортамата, мепреднизона, параметазона, преднизолона, преднизона, беклометазон дипропионата, бетаметазон дипропионата, триамцинолона, ингибиторов COX, ингибиторов LOX, ингибиторов p38 киназы, иммунодепрессивных средств, тетрациклина, миноциклина и доксициклина.
6. Пероральная композиция, содержащая спиронолактон, 4′,7-изофлавандиол и доксициклин для облегчения состояния кожи.
7. Композиция по п.2, содержащая спиронолактон, 4′,7-изофлавандиол и доксициклин моногидрат.
8. Композиция по п.2, содержащая спиронолактон, 4′,7-изофлавандиол и доксициклин гиклат.
9. Композиция по п.2, содержащая спиронолактон, 4′,7-изофлавандиол и тетрациклин.
10. Композиция по п.2, причем композиция содержит 4′,7-изофлавандиол и доксициклин моногидрат.
11. Композиция по п.2, причем композиция содержит 4′,7-изофлавандиол и доксициклин гиклат.
12. Композиция по п.2, причем композиция содержит 4′,7-изофлавандиол и тетрациклин.
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| US9220788B2 (en) * | 2009-06-17 | 2015-12-29 | Nanopharmaceuticals Llc | Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations and uses thereof |
| US9498536B2 (en) | 2005-09-15 | 2016-11-22 | Nanopharmaceuticals Llc | Method and composition of thyroid hormone analogues and nanoformulations thereof for treating anti-inflammatory disorders |
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| EP2120913B1 (en) | 2006-12-22 | 2015-01-21 | NanoPharmaceuticals LLC | Nanoparticle and polymer formulations for thyroid hormone analogs, antagonists, and formulations and uses thereof |
| US20100159021A1 (en) * | 2008-12-23 | 2010-06-24 | Paul Davis | Small Molecule Ligands of the Integrin RGD Recognition Site and Methods of Use |
| US9180107B2 (en) * | 2009-03-31 | 2015-11-10 | Nanopharmaceuticals Llc | Combination treatment of cancer with cetuximab and tetrac |
| US8633178B2 (en) | 2011-11-23 | 2014-01-21 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
| US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
| US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
| US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
| US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
| US9198331B2 (en) | 2013-03-15 | 2015-11-24 | Switch, Ltd. | Data center facility design configuration |
| EP3145489A1 (en) | 2014-05-22 | 2017-03-29 | TherapeuticsMD, Inc. | Natural combination hormone replacement formulations and therapies |
| KR20170134514A (ko) | 2015-03-23 | 2017-12-06 | 바이오팜엑스 인코포레이티드 | 피부과 사용을 위한 약학 테트라사이클린 조성물 |
| US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
| CN105362351A (zh) * | 2015-12-16 | 2016-03-02 | 成都昊健生物科技有限责任公司 | 用于治疗皮肤瘙痒病症的药物组合物及其应用 |
| WO2017173044A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd Inc. | Steroid hormone compositions in medium chain oils |
| WO2017173071A1 (en) | 2016-04-01 | 2017-10-05 | Therapeuticsmd, Inc. | Steroid hormone pharmaceutical composition |
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| RU2639085C1 (ru) * | 2017-03-22 | 2017-12-19 | Общество С Ограниченной Ответственностью "Фармвет" | Средство для лечения кожных инфекций |
| RU2017138097A (ru) * | 2017-11-01 | 2019-05-07 | Анастасия Владимировна Серебрянская | Трансдермальный терапевтический препарат |
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| US4925833A (en) * | 1983-12-29 | 1990-05-15 | The Research Foundation Of State University Of New York | Use of tetracycline to enhance bone protein synthesis and/or treatment of osteoporosis |
| US5202449A (en) * | 1987-07-28 | 1993-04-13 | Nippon Kayaku Kabushiki Kaisha | Process for purifying 7-dimethylamino-6-demethyl-6-deoxytetracycline |
| CN104643057A (zh) * | 2002-07-24 | 2015-05-27 | 儿童医院医疗中心 | 含有对映体牛尿酚的组合物和产物及其用途 |
| US8668914B2 (en) | 2002-07-24 | 2014-03-11 | Brigham Young University | Use of equol for treating skin diseases |
| CA2564399A1 (en) * | 2004-04-28 | 2005-11-17 | Brigham Young University | Use of equol for treating skin diseases |
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| US20080188446A1 (en) * | 2007-02-02 | 2008-08-07 | Warner Chilcott Company Inc. | Tetracycline compositions for topical administration |
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| US20180153909A1 (en) | 2018-06-07 |
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| EP2575816A4 (en) | 2014-03-26 |
| RU2603479C2 (ru) | 2016-11-27 |
| CA2800838A1 (en) | 2011-12-01 |
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