公开(公告)号：US07759399B2

公开(公告)日：2010-07-20

申请号：US10957242

申请日：2004-09-27

申请人： Stanley Michael Roberts ,  Maria Gabriella Santoro ,  Vasudev Jadhav ,  Alan Michael Happe ,  Paul Evans ,  Nicolette Christa Ross ,  Timothy James Snape

发明人： Stanley Michael Roberts ,  Maria Gabriella Santoro ,  Vasudev Jadhav ,  Alan Michael Happe ,  Paul Evans ,  Nicolette Christa Ross ,  Timothy James Snape

IPC分类号： A01N31/00

CPC分类号： C07C323/22 ,  C07C323/59 ,  C07C2601/08 ,  C07C2601/10 ,  C07F7/1804

摘要： A compound comprising a cyclopentanone, cyclopentenone, cyclohexanone or cyclohexenone group, wherein a first ring carbon atom carries an —SR substituent, R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group that, optionally, includes at least one heteroatom in its carbon skeleton, the remaining available ring carbon atoms are optionally substituted, and said compound either: —(a) is more soluble in water at a temperature of 20-40° C.; (b) is less lipophilic; and/or, (c) has a greater therapeutic index; or; (d) is less soluble in water at a temperature of 20-40° C.; (e) is more lipophilic; and/or, (f) has a greater therapeutic index; than an equivalent cyclohex-2-en-1-one or cyclopent-2-en-1-one derivative in which a hydrogen atom replaces said —SR group.

摘要翻译： 包含环戊酮，环戊烯酮，环己酮或环己烯酮基团的化合物，其中第一环碳原子带有-SR取代基，R是取代或未取代的烷基，烯基，炔基，芳基，芳烷基，芳烯基或芳炔基， 在其碳骨架中包含至少一个杂原子，剩余的可用环碳原子任选被取代，并且所述化合物： - （a）在20-40℃的温度下更可溶于水; （b）亲脂性较差; 和/或（c）具有较大的治疗指数; 要么; （d）在20-40℃的温度下较少溶于水; （e）更亲脂; 和/或（f）具有较大的治疗指数; 比其中氢原子取代所述-SR基团的当量环己-2-烯-1-酮或环戊-2-烯-1-酮衍生物。