发明名称 ARYLOXY AND ARYLTHIOPROPANOLAMINE DERIVATIVES USEFUL AS BETA 3-ADRENORECEPTOR AGONISTS AND ANTAGONISTS OF THE BETA 1 AND BETA 2-ADRENORECEPTORS AND PHARMACEUTICAL COMPOSITION THEREOF.
摘要 <p>A compound formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein R0 represents an aryl group optionally substituted with one, two or three substituents selected from the list consisting of: hydroxy, hydroxymethyl, nitro, amino, alkylamino, dialkylamino, alkylsulphonamido, arylsulphonamido, formamido, halogen, alkoxy and allyl; X represents O or S; R1 and R1a each independently represents hydrogen or an alkyl group; R2 represents OCH2CO2H, or an ester or amide thereof, or R2 represents a moiety of formula (b), wherein R4 represents hydrogen, alkyl, hydroxyalkyl, arylalkyl, aryloxyalkyl, aralkyloxyalkyl or cycloalkyl and R5 represents hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, aryloxyalkyloxy, arylalkoxyalkyloxy or cycloalkyloxy or R5 represents hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, aryloxyalkyl, arylalkyloxyalkyl or R5 together with OR4 represents O(CH2)nO, wherein n is 2, 3 or 4; and R3 represents hydrogen, halogen, alkyl or alkoxy or R3 together with R2 represents a moiety of formula (c) or an ester or amide thereof; providing that 4-[2-[2-hydroxy-3-(4-hydroxyphenoxy)propylamino]propyl]phenoxyacetic acid and salts and esters thereof and the compounds of examples 1 to 36 disclosed in EP0328251 are excluded from the scope of formula (I); a pharmaceutical composition containing such a compound, a process of preparing such a compound and the use of such a compound in medicine.</p>
申请公布号 MX9700765(A) 申请公布日期 1997.05.31
申请号 MX19970000765 申请日期 1995.07.27
申请人 SMITHKLINE BEECHAM PLC. 发明人 LEE JAMES BEELEY;MERVYN THOMPSON;DAVID KENNETH DEAN;NIKESH RASIKLAL KOTECHA;JOHN MICHAEL BERGE;ROBERT WILLIAM WARD
分类号 C07D317/58;A61K31/195;A61K31/215;A61K31/357;A61K31/36;A61K31/66;A61P1/00;A61P1/04;A61P3/00;A61P3/08;A61P9/10;A61P25/24;A61P25/26;A61P29/00;A61P43/00;C07C217/30;C07C217/34;C07C311/08;C07C311/21;C07C323/25;C07D317/46;C07F9/30;C07F9/32;C07F9/40;(IPC1-7):C07C217/60;C07C235/20;C07F09/38;A61K31/165;A61K31/19 主分类号 C07D317/58
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