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US 2010/0168129 A1Published application
Drugs with anticholestatic activity
OwnerMario Brufani, Luciano Cellai +3inventors
InventorsMario Brufani, Luciano Cellai, Barbara Bartolini, Ilaria Medici, Bianca Maria Lagrasta
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Abstract
New compounds belonging to the structural formula (I) are described. in which R1, R2, A, Y and X are specified in the description, useful in the treatment of cholestasis and substantially devoid of antibacterial activity. The synthesis process of said compounds, the pharmaceutical compositions containing them and their use in therapy are also described.
Claims14
1-15. (canceled)
A compound of formula (I)
- where
- R1 and R2 are chosen from —OH or —OCH3, otherwise R1 and R2 taken together form a —O—C(CH3)2—O— group,
- the ring A is chosen from:
- Y is chosen from H and —CO—CH3,
- X is chosen from CH2, O, S, NH, NR3, N—COR3,
- where R3 denotes:
- a) a linear or branched alkyl group having 1 to 9 carbon atoms,
- b) a (CH2)n—R4 chain, where n is 0 to 8 and R4 is chosen from OH, NH2, halogen, a cycloalkyl, aryl or heterocyclic group, with the proviso that when n is 1, R4 is not phenyl, or
- c) a (CH2)m—Z—(CH2)nCH3 chain, where m+n is 1 to 8, and Z denotes —O—, —S—, —NH—, —N(R5), where R5 is a linear or branched alkyl having 1 to 9 carbon atoms.
6 more elements
Method for the treatment of cholestasis and diseases related thereto comprising the administration of a compound of formula (I)
- where
- R1 and R2 are chosen from —OH or —OCH3, otherwise R1 and R2 taken together form a —O—C(CH3)2—O— group,
- the ring A is chosen from:
- Y is chosen from H and —CO—CH3,
- X is chosen from CH2, O, S, NH, NR3, N—COR3,
- where R3 denotes:
- a) a linear or branched alkyl group having 1 to 9 carbon atoms,
- b) a (CH2)n—R4 chain, where n is 0 to 8, and R4 is chosen from OH, NH2, halogen, a cycloalkyl, aryl or heterocyclic group,
- c) a (CH2)m—Z—(CH2)nCH3 chain, where m+n is 1 to 8, and Z denotes —O—, —S—, —NH—, —N(R5), where R5 is a linear or branched alkyl having 1 to 9 carbon atoms.
6 more elements
Dependencies are inferred from the claim text.