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filingDate 2014-03-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2015-11-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-095764-A1
titleOfInvention DERIVATIVES OF BIARIL-PROPIONIC ACID AND ITS USE AS PHARMACEUTICAL PRODUCTS
abstract They are cathepsin A protease inhibitors, and are useful for the treatment of diseases such as atherosclerosis, heart failure, kidney diseases, liver diseases or inflammatory diseases, for example, it also refers to procedures for the preparation of the compounds of the formula (1), its use and the pharmaceutical compositions that contain them. Claim 1: A compound of the formula (1), in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any proportion, or one of its physiologically acceptable salts, or a physiologically acceptable solvate of any of them, wherein the meanings they are: X is S or O; D is N or -C (R3) =; R is H, C₁₋₆ alkyl, C₃₋₈ cycloalkyl; R¹ is H, C₁₋₆ alkyl, C₃₋₈ cycloalkyl, C₁₋₆ alkylene-C₃₋₈ cycloalkyl; wherein alkyl is optionally substituted with one or more F atoms; R³ is H, methyl or ethyl; R² is hydrogen or C₁₋₆ alkyl; E¹ is N or -C (R⁴) =; E² is N or -C (R⁵) =; E³ is N or -C (R⁶) =; E⁴ is N or -C (R⁷) =; where none or one of E¹, E², E³ or E⁴ is N; R⁴ is H or O-C₁₋₆ alkyl; R⁵ is H, F, Cl, CF₃, C₁₋₆ alkyl, C₁₋₆ cycloalkyl; R⁶ is H or -O-CH₂-phenyl; R⁷ is H; G¹ is N or -C (R⁸) =; G² is N or -C (R⁹) =; G³ is N or -C (R¹⁰) =; G⁴ is N or -C (R¹¹) =; wherein none or one of G¹, G², G³ or G⁴ is N; or G³ and G⁴ are -C (R¹⁰) = and -C (R¹¹) =, where R¹⁰ and R¹¹ form a saturated carbocycle or heterocycle of 4 to 7 members with one or two oxygen atoms; which is optionally monosubstituted or disubstituted with C₁₋₃ alkyl; R⁸ is H, F, Cl, C₁₋₆ alkyl, O-C₁₋₆ alkyl, CF₃ or OCF₃; R⁹ is H, F, Cl, OH, O-C₁₋₆ alkyl, CH₂OH, CO-NH₂, C₁₋₆ alkyl, O-C₁₋₆ alkyl, CF₃ or OCF₃; R¹⁰ is H, F, Cl, OH, C₁₋₆ alkyl, CH₂OH, CO-O-C₁₋₆ alkyl, SO₂-C₁₋₆ alkyl, CN, O-C₁₋₆ alkyl, CF₃, CH₂-CN, (C (CH₃) ₂) -CN, C₁₋₆-OH alkyl, -O-C₁₋₆-OH alkyl, -O-CH₂-CO-C₁₋₆ alkyl or OCF₃; R¹¹ is H, F, Cl, OH, O-C₁₋₆ alkyl, CH₂OH, CO-C₁₋₆-methyl, CO-N (R²⁰R²¹), CO-O-C₁₋₆ alkyl, CN, C₁₋₆ alkyl, O-C₁₋₆ or OCF₃ alkyl; wherein R²⁰ and R²¹ are independently of each other, H or C₁₋₃ alkyl or together with the nitrogen to which a saturated ring of 5 or 6 members is attached.
priorityDate 2013-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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