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76 条记录 (耗时 0.032 秒)

    Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
    1.
    发明授权
    Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof 失效
    单酰化桦木醇和二氢甜菜蛋白衍生物，其制备及其用途

    公开(公告)号：US07365221B2

    公开(公告)日：2008-04-29

    申请号：US10870555

    申请日：2004-06-18

    申请人： Graham P. Allaway ,  Carl T. Wild ,  Yoshiki Kashiwada ,  Kuo-Hsiung Lee

    发明人： Graham P. Allaway ,  Carl T. Wild ,  Yoshiki Kashiwada ,  Kuo-Hsiung Lee

    IPC分类号： C07C69/74

    CPC分类号： C07J53/00 ,  A61K31/56 ,  A61K45/06 ,  A61K2300/00

    摘要： Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

    摘要翻译： 已经发现根据本发明的桦木醇和二氢甜菜碱酰基衍生物具有有效的抗HIV活性。 本发明的化合物具有本文所述的式I或其药学上可接受的盐; 其中R 1是C 2 -C 20 - 取代或未取代的羧酰基或其酯; R 2是氢，卤素，羟基或-OR 3，R 3是C 2 -C 3 取代或未取代的羧酰基; 且R 4是氢或C（C 6 H 5）3 N 3。 其中虚线表示C20和C29之间任选的双键。

    Substituted 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs, compositions thereof, and methods for using thereof
    2.
    发明授权
    Substituted 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs, compositions thereof, and methods for using thereof 失效
    取代的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物，其组合物及其使用方法

    公开(公告)号：US06768007B2

    公开(公告)日：2004-07-27

    申请号：US10096107

    申请日：2002-03-13

    申请人： Kuo-Hsiung Lee ,  Lan Xie ,  Graham P. Allaway ,  Carl T. Wild

    发明人： Kuo-Hsiung Lee ,  Lan Xie ,  Graham P. Allaway ,  Carl T. Wild

    IPC分类号： C07D21302

    CPC分类号： C07D471/04 ,  C07D493/04 ,  C07D495/04 ,  C07F9/6561

    摘要： 3′,4′-di-O-camphanoyl-(+)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.

    摘要翻译： 已经发现根据本发明的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物具有抗HIV活性。 本发明的化合物具有下式：或其药学上可接受的盐，酯或前药，其中R 1，R 2，R 3，R 4，X和Z被置于 规格。 本发明还涉及包含一种或多种式I化合物的药物组合物，任选地还包含一种或多种抗病毒剂或免疫刺激剂。 此外，本发明涉及式I化合物用于抑制动物细胞或组织中的逆转录病毒感染，用于治疗患有逆转录病毒相关病理学的患者，用于预防HIV传播 感染艾滋病毒的孕妇到胎儿的感染，以及在性交期间预防艾滋病毒感染的传播。

    Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof
    3.
    发明申请
    Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof 失效
    单酰化桦木醇和二氢甜菜蛋白衍生物，其制备及其用途

    公开(公告)号：US20050020548A1

    公开(公告)日：2005-01-27

    申请号：US10870555

    申请日：2004-06-18

    申请人： Graham Allaway ,  Carl Wild ,  Yoshiki Kashiwada ,  Kuo-Hsiung Lee

    发明人： Graham Allaway ,  Carl Wild ,  Yoshiki Kashiwada ,  Kuo-Hsiung Lee

    IPC分类号： A61K31/56 ,  A61K39/00 ,  A61K45/06 ,  C07J53/00

    CPC分类号： C07J53/00 ,  A61K31/56 ,  A61K45/06 ,  A61K2300/00

    摘要： Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

    摘要翻译： 已经发现根据本发明的桦木醇和二氢甜菜碱酰基衍生物具有有效的抗HIV活性。 本发明的化合物具有本文所述的式I或其药学上可接受的盐; 其中R1是C2-C20取代或未取代的羧酰基或其酯; R2是氢，卤素，羟基或-OR3，R3是C2-C20取代或未取代的羧酰基; R4为氢或C（C6H5）3; 其中虚线表示C20和C29之间任选的双键。

    Suksdorfin, analogs, compositions thereof, and methods for making and using thereof
    7.
    发明授权
    Suksdorfin, analogs, compositions thereof, and methods for making and using thereof 失效
    苏科多芬类似物，其组合物，及其制备和使用方法

    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。