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New thio-derivatives that carry lactams as potent HDAC inhibitors and their uses as medicines
专利权人:
SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
发明人:
GIANNINI, Giuseppe,CABRI, Walter,BATTISTUZZI, Gianfranco,VIGNOLA, Davide,FANTO', Nicola,PISANO, Claudio,VESCI, Loredana
申请号:
ES12761967
公开号:
ES2579321T3
申请日:
2012.09.17
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound having the general Formula (I) ** Formula ** in which, R1 is H, alkyl- (C1-C6) or aryl; or alternatively R1 and R4, each attached to two adjacent carbon atoms, if n is 2 or 3, are considered together to form a cyclopropane ring; R2 is phenyl optionally substituted with halogen, benzyloxy, (C1-C3) alkyl or CF3; cycloalkyl- (C3-C6); arylalkyl- (C1-C6) in which the aryl is optionally substituted with benzyloxy, alkyl- (C1-C3) or CF3; R3 is H, PO (OH) 2, or a group of Formula (II) - (CO) -R7 Formula II R7 is alkyl- (C1-C7), alkoxy- (C1-C6) or -CH (NH2) R8 ; R8 is H, or the side chain of a natural α-amino acid selected from the group consisting of glycine, alanine, phenylalanine, valine, leucine, isoleucine, aspartic acid, asparagine, glutamic acid, glutamine, serine, lysine, histidine, methionine, proline, cysteine, threonine, tryptophan, arginine and tyrosine; R4 and R5 are in each case independently H, halogen, alkyl- (C1-C6), or alternatively, when n is 2 or 3, an R4 and an R5, each attached to two adjacent carbon atoms, are considered together to form a cyclopropane ring; R6 is H or, alternatively, R2 and R6 are considered together to form a five to six membered heterocycle that may be optionally fused with an aryl moiety; -A-E- is - (CO) - (NR9) - or - (NR9) - (CO) -; R9 is H or alkyl- (C1-C3); m is an integer between 0 and 3; n is an integer between 0 and 3 with the proviso that when it is 2 or 3, each of R4 and R5 can adopt a different meaning in each case; the symbol means that the carbon atom carrying said symbol can adopt an R or S configuration; the symbol may be absent, but if present it means that the cycle may be partially unsaturated with the proviso that when the carbon atom carrying R4 is involved in a double bond, R5 is absent; their tautomers, their geometric isomers, their optically active forms such as enantiomers, diastereomers and their racemate forms, as well as the pharmaceutically acceptable salts thereof.Un compuesto que tiene la Fó
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