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Estra-1,3,5 (10), 16-tetraeno-3-carboxamides for the inhibition of dehydrogenated 17 beta-hydroxysteroid (AKR1C3)
专利权人:
Bayer Pharma Aktiengesellschaft
发明人:
BOTHE, Ulrich,BUSEMANN, Matthias,BARAK, Naomi,ROTGERI, Andrea,FISCHER, Oliver Martin,MARQUARDT, Tobias
申请号:
ES14704817
公开号:
ES2678993T3
申请日:
2014.02.18
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
Compounds of the general formula (I) ** (See formula) ** where X independently means carbon or nitrogen, where carbon can be substituted with R1, Y means carbon or nitrogen, where carbon can be substituted with R2, R1 and R2 each independently represent hydrogen, halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C4-alkynyl, C3-C6-cycloalkyl, C1-C6-alkoxy, C1-C6-haloalkyl, C1- C6-haloalkoxy, nitrile, nitro, -SO2CH3, - SO2CH2CH3, - (C>; = O) CH3, carboxyl, hydroxyl, -NH2, -CH2NH2, -CH2OH, -CH (OH) CH3, -C (CH3) 2OH, - (C>; = O) NH2, - (C>; = O) NHCH3, - (C>; = O) NHCH2CH3, - (C>; = O) N (CH3) 2, -SO2NH2, -SO2NHCH3 or -SO2N (CH3 ) 2, R3 means hydrogen or halogen, R4 means hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl or C3-C6-cycloalkyl-C1-C6-alkyl, which are optionally substituted with up to 6 halogen atoms and if necessary, mono-substituted or disubstituted with hydroxyl, C1-C6-alkoxy, C1-C6-haloalkoxy, R5 means hydrogen, C1-C6-alkyl or C 3-C6-cycloalkyl, where C1-C6-alkyl and C3-C6-cycloalkyl are, where appropriate, substituted with up to 6 halogen atoms and are, if necessary, mono-substituted or disubstituted with hydroxyl, hydroxy-C1-C6-alkyl, C1- C6-alkyl, C1-C6-alkoxy, hydroxy-C2-C6-alkoxy, C1-C6-haloalkoxy, C3-C6-cycloalkyl, aryl, heteroaryl, 3-10 membered heterocycloalkyl, aryl-C1-C6-alkyl, heteroaryl -C1-C6-alkyl, - C (>; = O) R ', -C (>; = O) NH2, -C (>; = O) N (H) R', -C (>; = O) N (R ') R' ', -NH2, -NHR` -N (R') R``, -N (H) C (>; = O) R ', -N (R') C (>; = O) R ' , - N (H) C (>; = O) OR ', -N (R') C (>; = O) OR ', -NO2, -N (H) S (>; = O) R', -N ( R ') S (>; = O) R', -N (H) S (>; = O) 2R ', -N (R') S (>; = O) 2R ', -N>; = S (>; = O ) (R ') R' ', -S (>; = O) R', -S (>; = O) 2R ', -S (>; = O) 2NH2, -S (>; = O) 2NHR', -S (>; = O) 2N (R ') R' ', -S (>; = O) (>; = NR') R '', where aryl, heteroaryl, aryl-C1-C6-alkyl and heteroaryl-C1-C6- alkyl are, if necessary, monosubstituted or polysubstituted independently of each other with
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