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US 7,396,851 B2Granted
Heterocyclic and benzoheterocyclic polyamides structurally related to the natural antibiotic distamycin A for the treatment of β-thalassaemia
AssigneesUniversita' Degli Studi Di Ferrara, Associazione Veneta Per La Lotta Alla Talassemia, Associazione Per La Lotta Alla Talassemia Di Ferrara
InventorsPier Giovanni Baraldi, Nicoletta Bianchi, Giordana Feriotto, Roberto Gambari, Carlo Mischiati, Romeo Romagnoli
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Abstract
The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a medicament for the therapeutic treatment of β-thalassaemia.
Claims14
A method of treating β-thalassemia, comprising:
- administering as a medicament, to a patient suffering from β-thalassemia, a structural analogue of distamycin selected from the group consisting of:
- compounds of formula (I):
- in which:
- n is an integer selected from 2, 3 and 4,
- R is 4-[(ZCH2CH2)2N]C6H4CONH, and
- Z is selected from the group consisting of F, Cl, Br and I;
- compounds of formula (II):
- in which:
- n is an integer selected from 0 (zero), 1 and 2,
- Z is selected from the group consisting of F, Cl, Br and I,
- A, B, C and D are each CH,
- X1, X2, X3 and X4 are each CH;
- compounds of formula (III):
- in which:
- n is an integer selected from 2, 3 and 4,
- T is selected from the group consisting of 4-[(ZCH2CH2)2N]C6H4CONH,(ZCH2CH2)2N, and
- CH2=CZCONH,
- Z is selected from the group consisting of Cl, Br, F and I,
- E is selected from the group consisting of O (oxygen), S and NR1,
- R1 is H or CH3, and
- G is CH or N;
- compounds of formula (IV):
- in which:
- n is an integer selected from 1, 2, 3 and 4;
- T is selected from the group consisting of 4-[(ZCH2CH2)2N]C6H4CONH, (ZCH2CH2)2N, and
- CH2=CZCONH;
- Z is selected from the group consisting of F, Cl, Br and I;
- A is selected from the group consisting of O (oxygen), S and NR1;
- R1 is linear or branched alkyl having from 1 to 4 carbon atoms;
- B is CH or N;
- compounds of formula (V):
- in which:
- R1 and R2 are selected independently of one another from the group consisting of hydrogen, linear or branched alkyl having from 1 to 4 carbon atoms, nitrile (CN) and hydroxyl (OH), or R1 and R2 form, in combination with one another, a linear alkyl chain —(CH2)m —in which m is 2 or 3;
- and their pharmaceutically acceptable salts.
31 more elements
Dependencies are inferred from the claim text.