C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/08 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/06 (2006.01) C07K 5/083 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2196334
Compounds of the invention inhibit urokinase plasminogen activator or uPAR, represented by general formula (I), where R10 is -CH(R9)XCH(R1)(R11) or a capping group, where X is NR12, CR12R15, O, S, SR12, or SR12R15; R1, R9, R11, R12, R15 are each H, lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, substituted with 0-3 halo, OH, NH2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO2; R16 is -CH(R5)C(=O)NH2, H, lower alkyl, cycloalkyl, or lower alkenyl; R2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl; R3 and R5 are each independently H or lower alkyl; R4 is -CH2C(=O)NR13R14, where R13 is H, lower alkyl, phenyl or benzyl, and R14 is H, aryl, or aralkyl, where R6 and R7 are each independently H, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl, and n and m are each independently an integer from 1 to 3; and pharmaceutically acceptable acid addition salts thereof.
La présente invention concerne des composés inhibiteurs de l'activateur du plasminogène de l'urokinase ou PARu, ces composés étant représentés par la formule générale (I). Dans cette formule générale, R¿10? est -CH(R¿9?)XCH(R¿1?)(R¿11?) ou un groupe coiffe, X étant NR¿12?, CR¿12?R¿15?, O, S, SR¿12?, ou SR¿12?R¿15?. R¿1?, R¿9?, R¿11?, R¿12?, R¿15? sont chacun H, alkyle inférieur, alcényle inférieur, alkynyle inférieur, aryle, aralkyle, arylalcényle, arylalcynyle, arylcycloalkyle, à substitution 0-3 halo, OH, NH¿2?, alkyle inférieur, haloalkyle inférieur, alcoxy inférieur, alkylamino inférieur, alkylthio inférieur, CN ou NO¿2?; R¿16? est -CH(R¿5?)C(=O)NH¿2?, H, alkyle inférieur, cycloalkyle ou alcényle inférieur; R2 est aryle ou aralkyle, sans ou avec substitution 1-3 halo, OH, NH¿2?, CN, NO¿2?, alkyle inférieur, haloalkyle inférieur, alcoxy inférieur, alkylamino inférieur, alkylthio inférieur ou cycloalkyle. R¿3? et R¿5? sont chacun indépendamment H ou alkyle inférieur, R¿4? est -CH¿2?C(=O)NR¿13?R¿14?, R¿13? étant H alkyle inférieur, phényle ou benzyle, et R¿14? étant H, aryle ou aralkyle, R¿6? et R¿7? étant chacun indépendamment H, OH, NH¿2?, CN, NO¿2?, alkyle inférieur, haloalkyle inférieur, alcoxy inférieur, alkylamino inférieur, alkylthio inférieur ou cycloalkyle. En outre, n et m valent chacun indépendamment un entier compris entre 1 et 3. L'invention concerne également des sels d'addition d'acides pharmaceutiquement acceptables, issus de ces composés.
Martin Eric J.
Rosenberg Steven
Spear Kerry L.
Borden Ladner Gervais Llp
Chiron Corporation
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