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US 8,022,250 B2Granted
1-phenylalkanecarboxylic acid derivatives for the treatment of neurodegenerative diseases
AssigneeChiesi Farmaceutici S.p.A.
InventorsLuca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
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Abstract
1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.
Claims6
A compound of formula (I):
- wherein:
- R and R1 are the same and are a linear or a branched C1-C4 alkyl;
- G is a —CONH2 or a —CONHSO2R′″ group wherein R′″ is a linear or a branched C1-C4 alkyl or a C3-C6 cycloalkyl;
- R2 is F;
- Ar is a group of formula
- wherein R3 represents one or more groups independently selected from:
- a halogen selected from the group consisting of F, Cl, Br, and I;
- —CF3;
- —C3-C8 cycloalkyl optionally substituted with one or more C1-C4 alkyl groups, oxo groups, or a combination thereof;
- CH═CH2;
- —CN;
- —CH2OH;
- methylendioxy or ethylendioxy;
- NO2
- phenyl optionally substituted with one or more of the following groups:
- halogen;
- —CF3;
- OCF3;
- —OH;
- a linear or a branched C1-C4 alkyl;
- a saturated heterocycle with at least 4 carbon atoms and at least 1 heteroatom;
- a C3-C8 cycloalkyl in turn optionally substituted with one or more of the following groups:
- a linear or a branched C1-C4 alkyl, —CF3 or —OH;
- —OR4 or —NHCOR4 wherein R4 is —CF3, a linear or a branched C2-C6 alkenyl or alkynyl;
- a benzyl;
- a phenyl optionally substituted with one or more of the following groups:
- halogen, —CF3, —OCF3, —OH, a linear or a branched C1-C4 alkyl;
- a saturated heterocycle with at least 4 carbon atoms and at least 1 heteroatom;
- a C3-C8 cycloalkyl in turn optionally substituted with one or more of the following groups:
- a linear or a branched C1-C4 alkyl, —CF3 or —OH;
- —SR5, —SO2R5 or —COR5 wherein R5 is a linear or a branched C1-C6 alkyl;
- or Ar is a substituted or unsubstituted heterocyclic ring selected from the group consisting of thiophene, benzothiophene, dibenzothiophene, thianthrene, pyrrole, pyrazole, furan, benzofuran, dibenzofuran, indole, isoindole, benzofurane, imidazole, benzoimidazole, oxazole, isoxazole, benzoxazole, thiazole, pyridine, pyrimidine, pyrazine, pyridazine, quinoline, isoquinoline, quinazoline, quinoxaline, cinnoline, pyrazole, pyran, benzopyran, pyrrolizine, phtalazine, 1,5-naphtiridine, 1,3-dioxole, and 1,3-benzodioxole, each of which may be substituted with one or more R3 groups;
- or a pharmaceutically acceptable salt or ester thereof.
30 more elements
A compound of formula (I):
- wherein:
- R and R1 are both methyl;
- G is a —CONH2 or a —CONHSO2R′″ group wherein R′″ is a linear or a branched C1-C4 alkyl or a C3-C6 cycloalkyl;
- R2 is F;
- and
- Ar is phenyl substituted with an optionally substituted phenyl group,
- or a pharmaceutically acceptable salt thereof.
4 more elements
2-methyl-2(2-fluoro-4′-cyclohexylbiphen-4-yl)propionic acid or a pharmaceutically acceptable salt or ester thereof.
Dependencies are inferred from the claim text.