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NOUVEAUX ACTIVATEURS DE LA GUANYLATE CYCLASE SOLUBLES À DOUBLE MODE D'ACTION, INHIBITEURS DE PHOSPHODIESTÉRASE ET LEURS UTILISATIONS
专利权人:
TOPADUR PHARMA AG
发明人:
KOCH, Guido,LONE, Esra,DI MAIO, Selena,NAEF, Reto,PETERKE, Jeanette,SPOERRI, Michael,TENOR, Hermann,MARTINI, Elia
申请号:
EPEP2019/082668
公开号:
WO2020/109354A1
申请日:
2019.11.27
申请国别(地区):
EP
年份:
2020
代理人:
摘要:
The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) and said compound of formula II each comprises at least one ONO2 or ONO moiety; R1 is C1-C3alkyl; R2 is H, C1-C6alkyl, C3-C6cycloalkyl, C1-C2alkoxy, C2-C4alkenyl; R3 is C1-C4alkyl optionally substituted with C1-C2alkoxy, C3-C4cycloalkyl, C2-C4alkenyl; R4 and R5 are each independently H or C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, COOH, C1-C3alkoxy, C3-C6cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homo-piperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with independently one or more R6; R6 is C1-C6alkyl optionally substituted with independently one or more halogen, OH, ONO, ONO2, C1-C3alkoxy, C1-C3haloalkoxy, COOR7, NR8R9, C=NR10; R7 is H, or C1-C4alkyl optionally substituted with F, OH, ONO, ONO2, NR8R9; R8 and R9 are independently H, or C1-C4alkyl optionally substituted with ONO, ONO2; R10 is C1-C4alkyl optionally substituted with F, ONO, ONO2; C3-C6cycloalkyl; pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.La présente invention concerne des composés de formule (I) ou de formule (II) ou un sel, un solvate ou un hydrate pharmaceutiquement acceptable de ceux-ci, ledit composé de formule (I) et ledit composé de formule II comprenant chacun au moins une fraction ONO2 ou ONO ; R1 représente alkyle en C1-C3 ; R2 représente H, alkyle en C1-C6, cycloalkyle en C3-C6, alcoxy en C1-C2, alcényle en C2-C4 ; R3 représente alkyle en C1-C4 éventuellement substitué par alcoxy en C1-C2, cycloalkyle en C3-C4, alcé
来源网站:
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