发明名称 1-ALKYL-, 1-ALKENYL- AND 1-ALKYNYLARYL-2-AMINO-1, 3-PROPANEDIOLS AND RELATED COMPOUNDS, A PROCESS AND INTERMEDIATES FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
摘要 The present invention relates to novel 1-alkyl-, 1-alkenyl- and 1-alkynylary l- 2-amino-1,3- propanediols, intermediates and processes for the preparation thereof. The compounds of the invention are of the formula I RCH(OR1)CH(NR2R3)R4 (I) wherein R is wherein R5 is CH3(CH2)mC=C. CH3(CH2)m,CH=CH, CH3(CH2)m,CH2CH2, wherein m is 3 to 15, n is 0 to 12, W and X are independently hydrogen, (C1- C8) alkyl, (C1-C8) alkoxy, halogen or trifluoromethyl, and Z is S. O, or C=O: and A is S or O: R1 is hydrogen or wherein R6 is hydrogen, (C1-C8) alkyl. (C1-C8) alkoxy. or :R2 is hy drogen (C1-C3) alkyl. R3 is hydrogen (C1-C3) alKyl or wherein R6 is as above: R4 is wherein R7 is hydrogen (C1-C8) alkyl. or CH2 OR8 wherein R8 is hydrogen or wherein R6 is as above: R1 and R8 taken together with the oxygen to which th ey are attached form a group of the formula wherein R9 and R10 are independently hydrogen or alkyl, where alkyl is a straight or branched chain hydrocarbon having no unsaturation and 1 to 10 carbon atoms, the optical isomers thereof, or the pharmaceutically acceptable salts thereof. The compounds of the invention exhibit antiinflammatory, memory dysfuncti on relieving, cell poliferation reducing, antibacterial and antifungal activity and can, therefore, be used as medicaments.
申请公布号 CA2038029(A1) 申请公布日期 1991.09.14
申请号 CA19912038029 申请日期 1991.03.12
申请人 HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED 发明人 TEGELER, JOHN J.;RAUCKMAN, BARBARA S.;HAMER, RUSSELL R.L.;FREED, BRIAN S.
分类号 A61K31/195;A61K31/115;A61K31/335;A61K31/34;A61K31/341;A61K31/38;A61K31/381;A61K31/40;A61K31/41;A61K31/42;A61K31/421;A61K31/425;A61K31/426;A61K31/44;A61K31/4418;A61P25/28;A61P29/00;A61P31/00;A61P31/04;A61P35/00;A61P43/00;C07C45/68;C07C47/542;C07C215/36;C07C219/22;C07C229/36;C07C231/12;C07C233/18;C07C233/47;C07D207/44;C07D213/36;C07D213/38;C07D213/40;C07D213/48;C07D213/54;C07D213/55;C07D213/61;C07D213/63;C07D213/80;C07D261/08;C07D263/32;C07D275/02;C07D277/20;C07D277/24;C07D277/28;C07D277/30;C07D307/56;C07D333/20;C07D333/22;C07D333/24;C07D333/26;C07D405/04;C07D409/04;(IPC1-7):C07D213/56;A61K31/00;C07C233/22 主分类号 A61K31/195
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