[EN] PROCESS FOR PREPARATION OF NOVEL 42-0-(HETEROALKOXYALKYL) RAPAMYCIN COMPOUNDS WITH ANTI-PROLIFERATIVE PROPERTIES"<br/>[FR] PROCÉDÉ DE PRÉPARATION DE NOUVEAUX COMPOSÉS DE 42-O-(HÉTÉROALCOXYALKYL)RAPAMYCINE AYANT DES PROPRIÉTÉS ANTIPROLIFÉRATIVES
申请人:MERIL LIFE SCIENCES PVT LTD
公开号:WO2012017449A1
公开(公告)日:2012-02-09
The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol,Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2- methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2- dimethyl-6-phenyl 2H-Pyran-3-ol.
本发明公开了一种新型的42-0-(杂代烷氧基烷基) 霉素化合物,其化学式为(1),以及其制备方法。这些化合物在治疗高增殖性血管疾病,如再狭窄和动脉粥样硬化方面具有用途。其中,R代表选自四氢呋喃-3-醇、氧杂环戊烷-3-醇、四氢吡喃-3-醇、四氢-4-甲基呋喃-3-醇、四氢-2,5,5-三甲基呋喃-3-醇、四氢-2,5-二乙基-2-甲基呋喃-3-醇、四氢-6-甲氧基-2-甲基-2H-吡喃-3-醇和四氢-2,2-二甲基-6-苯基-2H-吡喃-3-醇的3、4和5元杂代3-羟基烷氧基烷基化合物。