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NOVEDOSOS DERIVADOS DE FTALAZINONA-PIRROLOPIRIMIDINACARBOXAMIDA
专利权人:
TAKEDA GMBH
发明人:
STENGEL, THOMAS,MAIER, THOMAS,MANN, ALEXANDER,STADLWIESER, JOSEF,FLOCKERZI, DIETER,PAHL, ANDREAS,BENEDIKTUS, EWALD,HESSMANN, MANUELA,KANACHER, TOBIAS,HUSSONG, RAGNA,ZITT, CHRISTOF,HOLST, HANS CHRISTOF
申请号:
PE0028012013
公开号:
PE06482014A1
申请日:
2012.06.12
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to ftalazinona - pirrolopirimidinacarboxamidade derivative compounds of formula (1) wherein R1 is a compound of formula (a) or (b) where R2 and R4 are each (c1-c4) alkoxy optionally substituted with F R3 is alkoxy (c1-c4), cicloalcoxi (c3-c5) between other R5 is alkyl (c1-c4) R6 H Or alkyl (c1-c4) R7 R8 is H, alkyl (c1-c4) R9 is H or alkyl (c1-c4) R10 is H(C5, C7 cycloalkyl) alkyl (C1 - C6), among others, R17 is H or Methyl R18 is cycloalkyl (C3 - CH2 - C6) R19 is H, Hydroxy, alkoxy (c1-c4), among others R20 is H, alkoxy (c1-c4), among others M is 1 or 2.Preferred compounds are: 4 - [5 - (Cyclopropylmethoxy) - 1,3 - benzodioxol - 4-yl] - N - [(2R) - 3 - (3,5 - difluorofenilo) - 1 - (4 - [(4aS, 8aR) - 4 - (4 - 1 dimetoxifenilo) - oxo - 4a, 5,6,7,8,8a - hexahidroftalazin il - 2 (1H) - piperidin-1-yl] - oxopropan} - 1 - 2 - yl] - 5h pyrrolo [3,2-d] pyrimidine - 7 - carboxamide 4 - [2 - (Cyclopropylmethoxy) - 5 - Fluo Ro - 4 - metoxifenilo] - N - [(2S) - 1 - (4 - [(4aS, 8aR) - 4 - (4 - 1 dimetoxifenilo) - oxo - 4a, 5,6,7,8,Hexahidroftalazin 8A - - 2 (1H) - yl] piperidin-1-yl) - 3 - (3 - methylphenyl) - 1 - oxopropan IL - 2 -] - 6 - methyl - 5h pyrrolo [3,2-d] pyrimidine - 7 - carboxamide among others. It also relates to a Pharmaceutical composition. These compounds are inhibitors of phosphodiesterases Mixed type 4 and type 5 being useful in the treatment of Interstitial lung disease, pulmonary fibrosis, cystic fibrosisSE REFIERE A COMPUESTOS DERIVADOS DE FTALAZINONA-PIRROLOPIRIMIDINACARBOXAMIDADE FORMULA (1) DONDE R1 ES UN COMPUESTO DE FORMULA (a) O (b), EN DONDE R2 Y R4 SON CADA UNO ALCOXI(C1-C4) OPCIONALMENTE SUSTITUIDO CON F R3 ES ALCOXI(C1-C4), CICLOALCOXI(C3-C5), ENTRE OTROS R5 ES ALQUILO(C1-C4) R6 ES H O ALQUILO(C1-C4) R7 ES H R8 ES ALQUILO(C1-C4) R9 ES H O ALQUILO(C1-C4) R10 ES H, CICLOALQUILO(C5-C7), ALQUILO(C1-C6), ENTRE OTROS R17 ES H O METILO R18 ES CH2-CICLOALQUILO(C3-C6) R19 ES H, HIDROXILO, ALCOXI(C1-C4), ENTRE OTROS R20 ES H, ALCOXI(C1-C4), ENTRE O
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