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    Cyclic antitumor compounds
    1.
    发明授权
    Cyclic antitumor compounds 失效
    循环抗体化合物

    公开(公告)号：US5223506A

    公开(公告)日：1993-06-29

    申请号：US710230

    申请日：1991-06-04

    申请人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    发明人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    IPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153

    CPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/14

    摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.3 is hydrogen or methoxy and R.sup.4 is hydrogen;iii) when R.sup.2 is hydroxy, methoxy or amino, R.sup.3 is hydrogen, hydroxy or methoxy, and R.sup.4 is hydrogen;iv) when R.sup.4 is hydroxy or amino, R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is hydroxy or amino; and.v) when R.sup.1 is fluoro, chloro, iodo or amino, R.sup.2 is hydrogen, hydroxy or methoxy, R.sup.3 is hydrogen, hydroxy or methoxy and R.sup.4 is hydrogenand the use of these compounds as topoisomerase inhibitors and antitumor agents.

    Cyclic antitumor compounds
    2.
    发明授权
    Cyclic antitumor compounds 失效
    环状抗肿瘤化合物

    公开(公告)号：US5318976A

    公开(公告)日：1994-06-07

    申请号：US931611

    申请日：1992-08-18

    申请人： Michael J. Luzzi ,  Jeffrey Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    发明人： Michael J. Luzzi ,  Jeffrey Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    IPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153 ,  A61K31/435 ,  C07D471/14

    CPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/14

    摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen;X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; andX.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen.

    摘要翻译： 本发明涉及式（I）的某些取代的四环稠合喹啉衍生物：其中：R 1是氢，羟基，氟，氯，溴，碘，甲氧基或氨基; R2是氢，羟基，甲氧基或氨基; R3是氢，羟基，甲氧基，甲氧基甲氧基，氨基，-OCONH2，[2（5H）-3,4-二氢-3-呋喃酮]，2-羟基乙氧基，2-氨基乙氧基，3-羟基丙氧基或3-氨基丙氧基; 或与R2或R4一起亚甲二氧基或亚乙二氧基取代; R4是氢，羟基或氨基; Z是-CH 2 - ， - O-或-NH-; 和a）X1是氢; X2是氢，羟基，氟，氯，溴，碘或甲氧基; X3为氢或羟基; 或b）X 2与X 3一起为亚甲二氧基或亚乙二氧基，并且X 1为氢或其药学上可接受的盐，条件是：i）R 1至R 4中的至少一个不是氢。

    Antitumor compounds
    3.
    发明授权
    Antitumor compounds 失效
    抗菌化合物

    公开(公告)号：US5126351A

    公开(公告)日：1992-06-30

    申请号：US645373

    申请日：1991-01-24

    申请人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson

    发明人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson

    IPC分类号： C07D491/04 ,  C07D491/056

    CPC分类号： C07D491/04

    摘要： The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.4 substituents are hydrogen,intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

    Process for the synthesis of cyclopentene derivatives of purines
    5.
    发明授权
    Process for the synthesis of cyclopentene derivatives of purines 失效
    合成环丙基衍生物的方法

    公开(公告)号：US5144034A

    公开(公告)日：1992-09-01

    申请号：US505969

    申请日：1990-04-06

    申请人： M. Ross Johnson ,  Michael R. Peel ,  Daniel D. Sternbach

    发明人： M. Ross Johnson ,  Michael R. Peel ,  Daniel D. Sternbach

    IPC分类号： C07D473/00 ,  C07F7/08

    CPC分类号： C07F7/0818 ,  C07D473/00

    摘要： This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-amino-1,9-dihydro-9[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purin-6-one, an antiviral agent.

    摘要翻译： 本发明涉及制备某些光学活性环戊烯衍生物的新方法和用于该方法的新型中间体。 特别地，本发明涉及羰基维生素的1'R-顺式异构体的合成，（1'R-顺式）-2-氨基-1,9-二氢-9- [4-（羟基甲基）-2-环戊烯-1-酮 - 基] -6H-嘌呤-6-酮，抗病毒剂。

    Treatment of HIV and other viral infections using combinatorial therapy
    6.
    发明授权
    Treatment of HIV and other viral infections using combinatorial therapy 失效
    使用组合疗法治疗艾滋病毒和其他病毒感染

    公开(公告)号：US06475491B1

    公开(公告)日：2002-11-05

    申请号：US08973952

    申请日：1998-05-29

    申请人： M. Ross Johnson ,  Dennis Michael Lambert

    发明人： M. Ross Johnson ,  Dennis Michael Lambert

    IPC分类号： A61K3921

    CPC分类号： C07K14/005 ,  A61K38/00 ,  A61K38/21 ,  C12N2740/16122 ,  C12N2740/16134 ,  A61K38/162 ,  A61K2300/00 ,  A61K38/19

    摘要： Novel antiviral combinations for the treatment or prevention of viral infections, in particular, HIV, are disclosed. This new antiviral therapy employs either DP-178 or DP-107, viral fusion inhibitors, in combination with at least one other antiviral therapeutic agent. The combinations of the invention are better than single therapies alone, and in certain cases are synergistic. The use of DP-178 or DP-107 is an ideal therapy to combine with another antiviral, given both the novel mechanism which this therapeutic blocks HIV transmission and the non-toxicity of the therapeutic.

    摘要翻译： 公开了用于治疗或预防病毒感染，特别是HIV的新型抗病毒组合。 这种新的抗病毒疗法使用DP-178或DP-107，病毒融合抑制剂，与至少一种其它抗病毒治疗剂组合。 本发明的组合优于单一疗法，在某些情况下是协同的。 给予DP-178或DP-107是一种理想的治疗方法，与另一种抗病毒药物结合，既有这种治疗性阻断HIV传播的新机制和治疗无毒性的新机制。