ES2618520T3 - Pirrolocarboxamidas sustituidas con fluorometilo - Google Patents
Pirrolocarboxamidas sustituidas con fluorometilo Download PDFInfo
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- ES2618520T3 ES2618520T3 ES13756320T ES13756320T ES2618520T3 ES 2618520 T3 ES2618520 T3 ES 2618520T3 ES 13756320 T ES13756320 T ES 13756320T ES 13756320 T ES13756320 T ES 13756320T ES 2618520 T3 ES2618520 T3 ES 2618520T3
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
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- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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Abstract
Compuesto de fórmula general (I),**Fórmula** n representa 0, 1 o 2; m representa 0 o 1, con la condición de que n >= m; X se selecciona de entre el grupo consistente en O, S, NH o N-alquilo(C1-6); R1, R2 y R3 se seleccionan en cada caso, independientemente entre sí, de entre el grupo consistente en H; F; CI; Br; I; NO2; CN; alquilo(C1-6); CF3; CF2H; CFH2; CF2CI; CFCI2; C(>=O)-H; C(>=O)-alquilo(C1-6); C(>=O)-OH; C(>=O)-O-alquilo(C1-6); C(>=O)-N(H)(OH); C(>=O)-NH2; C(>=O)-N(H)-alquilo(C1-6); C(>=O)-N alquilo(C1-6)2; C(>=N-OH)-H; C(>=N-OH)-alquilo(C1-6); C(>=N-O-alquilo(C1-6))-H; C(>=N-O-alquilo(C1-6))- alquilo(C1-6); OH; OCF3; OCF2H; OCFH2; OCF2CI; OCFCI2; O-alquilo(C1-6); O-C(>=O)-alquilo(C1-6); OC(>= O)-O-alquilo(C1-6); O-(C>=O)-N(H)alquilo(C1-6); O-C(>=O)-N(alquilo(C1-6))2; O-S(>=O)2-alquilo(C1-6); OS(>= O)2-OH; O-S(>=O)2-O-alquilo(C1-6); O-S(>=O)2-NH2; O-S(>=O)2-N(H)(alquilo(C1-6)); O-S(>=O)2- N(alquilo(C1-6))2; NH2; N(H)(alquilo(C1-6)); N(alquilo(C1-6))2; N(H)-C(>=O)-alquilo(C1-6); N(H)-C(>=O)-O alquilo(C1-6); N(H)-C(>=O)-NH2; N(H)-C(>=O)-N(H)alquilo(C1-6); N(H)-C(>=O)-N(alquilo(C1-6))2; N(alquilo(C1- 6))-C(>=O)-alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-O-alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-NH2; N(alquilo(C1- 6))-C(>=O)-N(H)(alquilo(C1-6)); N(alquilo(C1-6))-C(>=O)-N(alquilo(C1-6))2; N(H)-S(>=O)2OH; N(H)-S(>=O)2- alquilo(C1-6); N(H)-S(>=O)2-O-alquilo(C1-6); N(H)-S(>=O)2-NH2; N(H)-S(>=O)2-N(H)(alquilo(C1-6)); N(H)- S(>=O)2N(alquilo(C1-6))2; N(alquilo(C1-6))-S(>=O)2-OH; N(alquilo(C1-6))-S(>=O)2-alquilo(C1-6); N(alquilo(C1- 6))-S(>=O)2-O-alquilo(C1-6); N(alquilo(C1-6))-S(>=O)2-NH2; N(alquilo(C1-6))-S(>=O)2-N(H)(alquilo(C1-6)); N(alquilo(C1-6))-S(>=O)2-N(alquilo(C1-6))2; SH; SCF3; SCF2H; SCFH2; SCF2CI; SCFCI2; S-alquilo(C1-6); S(>=O)-alquilo(C1-6); S(>=O)2-alquilo(C1-6); S(>=O)2-OH; S(>=O)2-O-alquilo(C1-6); S(>=O)2-NH2; S(>=O)2- N(H)alquilo(C1-6); o S(>=O)2-N(alquilo(C1-6))2, pudiendo el alquilo(C1-6) en cada caso ser lineal o ramificado; no sustituido o mono- o polisustituido; un residuo cicloalifático(C3-6) o heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono- o polisustituido; R4 representa CH2F; CHF2 o CF3; R5 representa H, alquilo(C1-6) lineal o ramificado, no sustituido o mono- o polisustituido, un residuo cicloalifático(C3-6) o heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono- o polisustituido; OH; O-alquilo(C1-6); NH2; N(H)-alquilo(C1-6); N(alquilo(C1-6))2 o SO2(alquilo(C1-6)), pudiendo el alquilo(C1-6) en cada caso ser lineal o ramificado; no sustituido o mono- o polisustituido; R6, R7 y R8 se seleccionan en cada caso, independientemente entre sí, entre el grupo consistente en H; F; CI; Br; I; NO2; CN; alquilo(C1-6); CF3; CF2H; CFH2; CF2CI; CFCI2; C(>=O)-H; C(>=O)-alquilo(C1-6); C(>=O)- OH; C(>=O)-O-alquilo(C1-6); C(>=O)-N(H)(OH); C(>=O)-NH2; C(>=O)-N(H)(alquilo(C1-6)); C(>=O)-N(alquilo(C1- 6))2; C(>=N-OH)-H; C(>=N-OH)-alquilo(C1-6); C(>=N-O-alquilo(C1-6))-H; C(>=N-O-alquilo(C1-6))-alquilo(C1-6); OH; OCF3; OCF2H; OCFH2; OCF2CI; OCFCI2; O-alquilo(C1-6); O-C(>=O)-alquilo(C1-6); O-C(>=O)-Oalquilo( C1-6); O-(C>=O)-N(H)(alquilo(C1-6)); O-C(>=O)-N(alquilo(C1-6))2; O-S(>=O)2-alquilo(C1-6); O-S(>=O)2- OH; O-S(>=O)2-O-alquilo(C1-6); O-S(>=O)2-NH2; O-S(>=O)2-N(H)(alquilo(C1-6)); O-S(>=O)2-N(alquilo(C1-6))2; NH2; N(H) (alquilo(C1-6)); N(alquilo(C1-6))2; N(H)-C(>=O)-alquilo(C1-6); N(H)-C(>=O)-O-alquilo(C1-6); N(H)- C(>=O)-NH2; N(H)-C(>=O)-N(H)(alquilo(C1-6)); N(H)-C(>=O)-N(alquilo(C1-6))2; N(alquilo(C1-6))-C(>=O)- alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-O-alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-NH2; N(alquilo(C1-6))-C(>=O)- N(H)(alquilo(C1-6)); N(alquilo(C1-6))-C(>=O)-N(alquilo(C1-6))2; N(H)-S(>=O)2OH; N(H)-S(>=O)2-alquilo(C1-6); N(H)-S(>=O)2-O-alquilo(C1-6); N(H)-S(>=O)2-NH2; N(H)-S(>=O)2-N(H)(alquilo(C1-6)); N(H)- S(>=O)2N(alquilo(C1-6))2; N(alquilo(C1-6))-S(>=O)2-OH; N(alquilo(C1-6))-S(>=O)2-alquilo(C1-6); N(alquilo(C1- 6))-S(>=O)2-O-alquilo(C1-6); N(alquilo(C1-6))-S(>=O)2-NH2; N(alquilo(C1-6))-S(>=O)2-N(H)(alquilo(C1-6)); N(alquilo(C1-6))-S(>=O)2-N(alquilo(C1-6))2; SH; SCF3; SCF2H; SCFH2; SCF2CI; SCFCI2; S-alquilo(C1-6); S(>=O)-alquilo(C1-6); S(>=O)2-alquilo(C1-6); S(>=O)2-OH; S(>=O)2-O-alquilo(C1-6); S(>=O)2-NH2; S(>=O)2- N(H)(alquilo(C1-6)); o S(>=O)2-N(alquilo(C1-6))2, pudiendo el alquilo(C1-6) en cada caso ser lineal o ramificado, no sustituido o mono- o polisustituido; un residuo cicloalifático(C3-6) o heterocicloalifático de 3 a 7 miembros, en cada caso no sustituido o mono- o polisustituido; R9 representa H, un residuo alifático(C1-10) lineal o ramificado, no sustituido o mono- o polisustituido; un residuo cicloalifático(C3-10) o heterocicloalifático de 3 a 10 miembros, en cada caso no sustituido o monoo polisustituido y en cada caso opcionalmente unido a través de un grupo alifático(C1-8) lineal o ramificado, que a su vez puede no estar sustituido o estar mono- o polisustituido; R10 representa H, un residuo alifático(C1-10) lineal o ramificado, no sustituido o mono- o polisustituido; un residuo cicloalifático(C3-10), heterocicloalifático de 3 a 10 miembros o un residuo heteroarilo, en cada caso no sustituido o mono- o polisustituido y en cada caso opcionalmente unido a través de un grupo alquileno(C1-8) lineal o ramificado, que a su vez puede no estar sustituido o estar mono- o polisustituido; o R9 y R10 junto con el átomo de nitrógeno que los une, forma un residuo heterocicloalifático de 3 a 10 miembros, que puede no estar sustituido o estar mono- o polisustituido; opcionalmente en forma de un estereoisómero simple o una mezcla de esteroisómeros; donde en relación con los términos "alquilo", "alquilo(C1-4)","alquilo(C1-6)", "residuo alifático", "grupo alifático", "residuo cicloalifático" y "residuo heterocicloalifático", el termino "mono- o polisustituido" se refiere, con respecto a los correspondientes grupos o residuos, a la sustitución simple o múltiple, por ejemplo disustitución, trisustitución, tetrasustitución o pentasustitución, de uno o más átomos de hidrógeno, en cada independientementre, por al menos un sustituyente seleccionado de entre el grupo consistente en F; Cl; Br; I; NO2; CN; >=O; >=NH; >=N(OH); >=N(O-alquilo(C1-6)); CF3; CF2H; CFH2; CF2Cl; CFCl2; alquilo(C1- 6); alquileno(C1-8)-OH; C(>=O)-H; C(>=O)-alquilo(C1-6); C(>=O)-OH; C(>=O)-O-alquilo(C1-6); C(>=O)-N(H)(OH); C(>=O)-NH2; C(>=O)-N(H)(alquilo(C1-6)); C(>=O)-N(alquilo(C1-6))2; C(>=N-OH)-H; C(>=NOH)-alquilo(C1-6); C(>=NO-alquilo(C1-6))-H; C(>=N-O-alquilo(C1-6))-alquilo(C1-6); OH; OCF3; OCF2H; OCFH2; OCF2Cl; OCFCl2; O-alquilo(C1-6); O-(alquileno(C1-8))-OH; O-(alquileno(C1-8))-O-alquilo(C1-8); O-C(>=O)-alquilo(C1- 6); O-C(>=O)-O-alquilo(C1-6); O-(C>=O)-N(H)(alquilo(C1-6)); O-C(>=O)-N(alquilo(C1-6))2; O-S(>=O)2-alquilo(C1- 6); O-S(>=O)2-OH; O-S(>=O)2-O-alquilo(C1-6); O-S(>=O)2-NH2; O-S(>=O)2-N(H)(alquilo(C1-6)); O-S(>=O)2- N(alquilo(C1-6))2; NH2; N(H)(alquilo(C1-6)); N(alquilo(C1-6))2; N(H)-C(>=O)-alquilo(C1-6); N(H)-C(>=O)-Oalquilo( C1-6); N(H)-C(>=O)-NH2; N(H)-C(>=O)-N(H) (alquilo(C1-6)); N(H)-C(>=O)-N(alquilo(C1-6))2; N(alquilo(C1-6))-C(>=O)-alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-O-alquilo(C1-6); N(alquilo(C1-6))-C(>=O)-NH2; N(alquilo(C1-6))-C(>=O)-N(H)(alquilo(C1-6)); N(alquilo(C1-6))-C(>=O)-N(alquilo(C1-6))2; N(H)-S(>=O)2-OH; N(H)-S(>=O)2-alquilo(C1-6); N(H)-S(>=O)2-O-alquilo(C1-6); N(H)-S(>=O)2-NH2; N(H)-S(>=O)2-N(H)(alquilo(C1- 6)); N(H)-S(>=O)2-N(alquilo(C1-6))2; N(alquilo(C1-6))-S(>=O)2-OH; N(alquilo(C1-6))-S(>=O)2-alquilo(C1-6); N(alquilo(C1-6))-S(>=O)2-O-alquilo(C1-6); N(alquilo(C1-6))-S(>=O)2-NH2; N(alquilo(C1-6))-S(>=O)2- N(H)(alquilo(C1-6)); N(alquilo(C1-6))-S(>=O)2-N(alquilo(C1-6))2; SH; SCF3; SCF2H; SCFH2; SCF2Cl; SCFCl2; S-alquilo(C1-6); S(>=O)-alquilo(C1-6); S(>=O)2-alquilo(C1-6); S(>=O)2-OH; S(>=O)2-O-alquilo(C1-6); S(>=O)2- NH2; S(>=O)2-N(H)(alquilo(C1-6)); S(>=O)2-N(alquilo(C1-6))2; un residuo cicloalifático o heterocicloalifático de 3 a 7 miembros, en forma de compuesto libre y/o de sal fisiológicamente aceptable y/o de solvato fisiológicamente aceptable del mismo.
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EP12006120 | 2012-08-29 | ||
PCT/EP2013/002594 WO2014032801A1 (en) | 2012-08-29 | 2013-08-29 | Fluoromethyl-substituted pyrrole carboxamides |
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JP (1) | JP6114392B2 (es) |
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BR (1) | BR112015004306A2 (es) |
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DK (1) | DK2906534T3 (es) |
EA (1) | EA027640B1 (es) |
EC (1) | ECSP15007358A (es) |
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HU (1) | HUE032691T2 (es) |
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PL (1) | PL2906534T3 (es) |
PT (1) | PT2906534T (es) |
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AP2015008721A0 (en) | 2013-03-15 | 2015-09-30 | Global Blood Therapeutics Inc | Compounds and uses thereof for the modulation of hemoglobin |
EA201992707A1 (ru) | 2013-11-18 | 2020-06-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
AU2014365740A1 (en) | 2013-12-19 | 2016-05-26 | Grünenthal GmbH | Fluoromethyl-substituted pyrrole carboxamides iv |
JP2016540820A (ja) * | 2013-12-19 | 2016-12-28 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | CaV2.2カルシウムチャネルブロッカーとしてのフルオロメチル置換ピロールカルボキサミド |
ES2660760T3 (es) * | 2013-12-19 | 2018-03-26 | Grünenthal GmbH | Pirrolocarboxamidas fluorometil-sustituidas como bloqueantes del canal de Ca CaV2.2 |
TW201718557A (zh) * | 2015-10-08 | 2017-06-01 | 歌林達有限公司 | 經吡唑基取代之四氫吡喃基碸 |
TW201726128A (zh) * | 2015-10-08 | 2017-08-01 | 歌林達有限公司 | 經吡唑基取代之四氫哌喃基碸 |
WO2020140957A1 (en) * | 2019-01-04 | 2020-07-09 | Ascentage Pharma (Suzhou) Co., Ltd. | Method for preparing sulfonamides drugs |
CN113382990A (zh) * | 2019-01-11 | 2021-09-10 | 格吕伦塔尔有限公司 | 取代的吡咯烷酰胺iii |
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EP1466902A4 (en) * | 2001-12-28 | 2005-11-09 | Takeda Pharmaceutical | ANTAGONISTS OF THE ANDROGEN RECEPTOR |
US7498408B2 (en) * | 2002-09-23 | 2009-03-03 | E. I. Du Pont De Nemours And Company | Ryanodine receptor polypeptides |
DE10261130A1 (de) * | 2002-12-20 | 2004-07-01 | Grünenthal GmbH | Arzneimittel enthaltend substituierte 2,5-Diaminomethyl-1H-pyrrole |
DE102006027229A1 (de) * | 2006-06-09 | 2007-12-20 | Grünenthal GmbH | 1,3-Disubstituierte 4-Methyl-1H-pyrrol-2-carbonsäureamide und ihre Verwendung zur Herstellung von Arzneimitteln |
JP5815029B2 (ja) * | 2010-07-09 | 2015-11-17 | クオンベルゲンセ プハルマセウトイカルス リミテッド | カルシウムチャネル遮断薬としてのテトラゾール化合物 |
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