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。

公开(公告)号：US07183440B2

公开(公告)日：2007-02-27

申请号：US11059086

申请日：2005-02-07

申请人： Stanley Michael Roberts ,  Maria Gabriella Santoro ,  Vasudev Jadhav ,  Alan Michael Happe ,  Jérôme Dauvergne

发明人： Stanley Michael Roberts ,  Maria Gabriella Santoro ,  Vasudev Jadhav ,  Alan Michael Happe ,  Jérôme Dauvergne

IPC分类号： C07C315/00 ,  C07C49/00 ,  A61K31/12 ,  A61K31/095

CPC分类号： C07C323/59 ,  C07C45/673 ,  C07C49/647 ,  C07C49/653 ,  C07C49/657 ,  C07C49/753 ,  C07C205/45 ,  C07C225/20 ,  C07C233/32 ,  C07C233/76 ,  C07C271/24 ,  C07C271/36 ,  C07C271/56 ,  C07C271/66 ,  C07C311/20 ,  C07C311/53 ,  C07C323/43 ,  C07C2601/08 ,  C07C2601/10

摘要： A compound of formula (I) or (II): wherein A is hydrogen or CR1R2; Y and Z are each, independently, hydrogen or a halogen; X is —NR4R5, or R7; R1 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–4 carbon atoms; when X is —NR4R5, R2 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 and contains 1–12 carbon atoms; when X is R7, R2 is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; R3 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 and contains 1–12 carbon atoms; R4 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms, —COOR8, or —COR8; R5 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–5 carbon atoms; R7 is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1–4 carbon atoms; and, R8 is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1–12 carbon atoms

摘要翻译： 式（I）或（II）的化合物：其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X是-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时，R 2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 基团，其任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子; 当X是R 7时，R 2是未取代的烷基，烯基或炔基，或取代或未取代的芳基，芳烷基芳烯基或芳炔基，其任选地包括在 其碳骨架中至少有一个杂原子，含有1-12个碳原子; R 3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，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; R 4是氢，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，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子， -COOR 8或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基，烯基或炔基; 并且R 8是含有1-12个碳原子的未取代或卤素取代的烷基，芳基或芳烷基