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US 6,887,892 B2Granted
Tricyclic derivatives of indole with antiangiogenic activity
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsGiuseppe Giannini, Mauro Marzi, Maria Ornella Tinti, Claudio Pisano
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Abstract
Compounds of formula useful for treating tumors, particularly mammary carcinoma and colon carcinoma.
Claims8
A compound having the formula (I):
- wherein:
- X=CH
- X1=N
- R and R1, which are the same or different, are selected from the group consisting of —H, OH, OR5 in which R5 may be C1-C4 alkyl or benzyl, when two groups OR5 are vicinal R5 is methylene;
- or R and R1 may be independently nitro;
- amino optionally mono- or di-substituted with C1-C4 alkyl;
- carboxy;
- or alkoxy (C1-C4) carbonyl;
- R and R1 taken together form an aliphatic or aromatic cyclic group having 5 or 6 atoms;
- R2 is selected from the group consisting of —H, phenyl, benzyl, linear or branched C1-C6 alkyl;
- n=is an integer ranging from 0 and 4;
- R3, which is the same as or different from R4, is —H, —OH, —OR6, wherein R6 is linear or branched C1-C4 alkyl, or when R3=R4=OR6 vicinal, R6 is isopropylidene
- R7=C1-C4 linear or branched alkyl optionally substituted with one or two groups OH, OR6, in case of 2 groups OR6 vicinal, R6 is isopropylidene;
- or R7 is formyl (CHO), oxime (CH═NOH), their isomers and their mixtures.
11 more elements
Dependencies are inferred from the claim text.