| US 7,531,692 B2 | ||
| Derivatives of 1-phenylalkanecarboxylic acids for the treatment of neurodegenerative diseases | ||
| Luca Raveglia, Parma (Italy); Ilaria Peretto, Parma (Italy); Stefano Radaelli, Parma (Italy); Bruno Pietro Imbimbo, Parma (Italy); Andrea Rizzi, Parma (Italy); and Gino Villetti, Parma (Italy) | ||
| Assigned to Chiesi Farmaceutici S.p.A., Parma (Italy) | ||
| Appl. No. 11/572,974 PCT Filed Jul. 26, 2005, PCT No. PCT/IB2005/002189 § 371(c)(1), (2), (4) Date Oct. 12, 2007, PCT Pub. No. WO2006/016219, PCT Pub. Date Feb. 16, 2006. |
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| Claims priority of application No. 04425604 (EP), filed on Aug. 03, 2004. | ||
| Prior Publication US 2008/0096968 A1, Apr. 24, 2008 | ||
| Int. Cl. C07C 233/05 (2006.01); A61K 31/16 (2006.01) | ||
| U.S. Cl. 564—155 [514/616] | 21 Claims |
1. A compound of formula (I):
 B is H or the side chain of an alpha-amino acid;
R and R1 are the same and are linear or branched C1-C4 alkyl;
or together with the carbon atom to which they are linked form a ring containing 3 to 6 carbon atoms;
R2 is H, CF3, OCF3 or a halogen selected from the group consisting of F, Cl, Br, and I; and
Ar is phenyl substituted with one or more groups R3, wherein R3 represents:
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 and/or oxo groups; CH═CH2; NO2; CH2OH; CN; methylenedioxy; ethylenedioxy; phenyl optionally substituted with one or more of the following groups: halogen selected
from the group consisting of F, Cl, Br, and I; CF3; OCF3; OH; linear or branched C1-C4 alkyl; a saturated heterocycle with at least 4 carbon atoms and at least 1 heteroatom; and C3-C8 cycloalkyl optionally substituted with one or more linear or branched C1-C4 alkyl groups, CF3 and/or OH; OR4 or NHCOR4 wherein R4 is CF3, linear or branched C2-C6 alkenyl or alkynyl; benzyl; phenyl optionally substituted with one or more of the following groups: halogen as previously
defined, CF3, OCF3, OH, linear or branched C1-C4 alkyl; a saturated heterocycle with at least 4 carbon atoms and at least 1 heteroatom; C3-C8 cycloalkyl optionally substituted with one or more linear or branched C1-C4 alkyl groups, CF3 and/or OH; and SR5, SO2R5 or COR5 wherein R5 is linear or branched C1-C6 alkyl; or
Ar is a heterocycle selected from the group consisting of pyrrole, pyrazole, furan, thiophene, indole, isoindole, benzofuran,
benzothiophene, imidazole, oxazole, isoxazole, thiazole, benzoimidazole, benzoxazole, benzothiazole, pyrimidine, pyrazine,
quinoline, isoquinoline, quinazoline, quinoxaline, dibenzofuran, dibenzothiophene, thianthrene, carbazole, pyridazine, cinnoline,
phthalazine, 1,5-naphthiridine, 1,3-dioxole, and 1,3-benzodioxole, said heterocycle being optionally substituted with one
or more groups R3 as defined above;
or a pharmaceutically acceptable salt or ester thereof.
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