C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/06 (2006.01) A61K 31/495 (2006.01) A61K 31/4965 (2006.01) A61K 31/551 (2006.01) C07D 241/08 (2006.01) C07D 243/08 (2006.01) C07D 401/12 (2006.01)
Patent
CA 2424282
Compounds of formula (I) wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di- lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.
Composés de formule (I) dans laquelle R représente carboxy, carboxy estérifié ou carboxy aminé, R¿1? et R¿3? représentent chacun indépendamment alkyle inférieur, (hydroxy, alkyle inférieur, amino, acylamino, mono- ou dialkylamino inférieur ou mercapto)-alkyle inférieur, alkyle inférieur-(thio, sulfinyle ou sulfonyle)-alkyle inférieur, cycloalkyle, aryle, biaryle, (cycloalkyle, aryle ou biaryle)-alkyle inférieur, ou (carboxy, carboxy estérifié ou carboxy aminé)-alkyle inférieur, R¿2? représente hydrogène, alkyle inférieur, cycloalkyle, aryle, biaryle, arylaminocarbonyle ou aryle-(oxy, thio ou amino), n vaut 1 ou 2, Y représente alkylène inférieur ou alcénylène inférieur. La présente invention concerne également des sels pharmaceutiquement acceptables desdits composés. Les composés et sels selon la présente invention sont utiles en tant qu'antagonistes de LFA-1.
Albert Rainer
Dawson King Janet
Ehrhardt Claus
Wattanasin Sompong
Weitz Schmidt Gabriele
Fetherstonhaugh & Co.
Novartis Ag
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