DIAZACYCLOALKANEDIONE DERIVATIVES

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, bi...

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Main Authors WELZENBACH, KARL, ALBERT, RAINER, DAWSON KING, JANET, EHRHARDT, CLAUS, WATTANASIN, SOMPONG, WEITZ SCHMIDT, GABRIELE
Format Patent
LanguageEnglish
French
Published 11.04.2002
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary: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, R1 et R3 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, R2 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.
Bibliography:Application Number: WO2001EP11342