Patent AR-076036-A1 (AR)
Title: Derivados de pirazol (3,2-c) esteroides con actividad agonista del receptor de glucocorticoesteroides
Inventor: BLADH HAKAN
Filed: 2010-03-31
Abstract: Composiciones farmacéuticas que los contienen y su uso en terapia. Reivindicacion 1: Un compuesto caracterizado porque se elige entre el grupo que consiste en: metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2R)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-1-{[(2-hidroxietil)sulfanil]carbonil}-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (R)/(S) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (R)/(S) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-3-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (2S)-tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, (S)/(R) tetrahidrofuran-2-carboxilato de (1R,3aS,3bS,10aR,10bS,11S,12aS)-7-(4-fluorofenil)-11-hidroxi-1-{[(2-hidroxietil)sulfanil]ccarbonil}-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[cianometiloxi]carbonil}-10b-fluoro-7-(6-fluoropiridin-3-il)-11-hidroxi-10a,12a-dimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,10aS,10bR,11S,12aS)-1-{[cianometiloxi}carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, furan-2-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, furan-2-carboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-5,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, ciclopropanocarboxilato de (1R,3aS,3bS,5S,10aR,10bS,11S,12aS)-1-{[(fluorometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, propanoato de (1R,2R,3a5,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(fluorometil)sulfanil}carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, 1,3-oxazol-4-carboxilato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(4-fluorofenil)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, y metoxiacetato de (1R,2R,3aS,3bS,10aS,10bR,11S,12aS)-10b-fluoro-1-{[(cianometil)sulfanil]carbonil}-7-(6-fluoropiridin-3-il)-11-hidroxi-2,10a,12a-trimetil-1,2,3,3a,3b,4,5,7,10,10a,10b,11,12,12a-tetradecahidrociclopenta[5,6]nafto[1,2-f]indazol-1-ilo, o una de sus sales farmacéuticamente aceptables.