公开(公告)号：US5637589A

公开(公告)日：1997-06-10

申请号：US392558

申请日：1995-02-21

申请人： Kuo-Hsiung Lee ,  Yoshiki Kashiwada ,  Li Huang ,  Thomas T. Lee ,  Mark Cosentino ,  Jim Snider ,  Mark Manax ,  Lan Xie

发明人： Kuo-Hsiung Lee ,  Yoshiki Kashiwada ,  Li Huang ,  Thomas T. Lee ,  Mark Cosentino ,  Jim Snider ,  Mark Manax ,  Lan Xie

IPC分类号： C07D491/04 ,  C07D491/052 ,  C07D493/04 ,  A61K31/435

CPC分类号： C07D491/04 ,  C07D493/04

摘要： Compounds, including compositions and methods of making and using these compounds for treating retroviral infections, are provided according to formula (G-1): ##STR1## wherein M is O or NH; Z is O, NH or S; R.sup.240, and R.sup.250 are each H, C.sub.1-10 alkyl, C.sub.1-10 aryl, alkyl, amide, or CH.sub.2 COOR.sup.260, where R.sup.260 is C.sub.1-10 alkyl or acyl; R.sup.200, R.sup.210, R.sup.220 and R.sup.230 are each H, halogen, hydroxyl, NH.sub.2, NH-alkyl, N-(alkyl).sub.2, O-alkyl, O-acyl, COCF.sub.3, OCF.sub.3 or CH.sub.2 COO NH-alkyl; or R.sup.200 and R.sup.210 form C.sub.5 -C.sub.10 cyclo or heterocyclo optionally substituted with one or more of halogen, hydroxyl, NH.sub.2, NH-alkyl, N-(alkyl).sup.2, O-acyl, O-alkyl, CO, CF.sub.3, OCF.sub.3 or CH.sub.2 COONH-alkyl; wherein C3 and C4 can be bound by a single or double bond; configurations at 3' or 4' can be (R) or (S); and R.sup.240 and R.sup.250 are either cis-.beta. or cis.alpha., or trans-3'-.alpha. or trans-3'-.beta. oriented.Stereoselectivity can be enhanced by preparing these compounds by catalytic asymmetric dihyroxylation.

摘要翻译： 根据式（G-1）：其中M为O或NH的化合物，包括制备和使用这些化合物用于治疗逆转录病毒感染的组合物和方法：其中M为O或NH; Z是O，NH或S; R240和R250各自为H，C1-10烷基，C1-10芳基，烷基，酰胺或CH2COOR260，其中R260为C1-10烷基或酰基; R200，R210，R220和R230各自为H，卤素，羟基，NH2，NH-烷基，N-（烷基）2，O-烷基，O-酰基，COCF3，OCF3或CH2COO NH-烷基; 或R200和R210形成任选被一个或多个卤素，羟基，NH 2，NH-烷基，N-（烷基）2，O-酰基，O-烷基，CO，CF 3，OCF 3或CH 2 仲烷基; 其中C3和C4可以被单键或双键结合; 3'或4'的构型可以是（R）或（S）; R240和R250是顺式-β或顺式α或反式-3'-α或反式-3'-β取向的。 通过催化不对称二羟基化制备这些化合物可以提高立体选择性。