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13 条记录 (耗时 0.014 秒)

    Novel prodrugs of N-H bond-containing compounds and methods of making thereof
    6.
    发明申请
    Novel prodrugs of N-H bond-containing compounds and methods of making thereof 审中-公开
    含有N-H键的化合物的新型前体药物及其制备方法

    公开(公告)号：US20030119814A1

    公开(公告)日：2003-06-26

    申请号：US10272330

    申请日：2002-10-16

    申请人： The University of Kansas

    发明人： Victor R. Guarino ,  Veranja Karunaratne ,  Valentino J. Stella

    IPC分类号： A61K031/55 ,  C07C381/00 ,  A61K031/4015 ,  A61K031/445

    CPC分类号： C07D209/48 ,  C07C313/12 ,  C07C313/20 ,  C07C313/28 ,  C07C2601/16 ,  C07D223/20 ,  C07D223/26 ,  C07D261/20 ,  C07D263/20 ,  C07D305/14

    摘要： The present invention relates to novel prodrugs of pharmaceutical compounds containing one or more NnullH bonds. More specifically, the present embodiment of the invention relates to prodrugs wherein sulfur-containing promoieties are attached to pharmaceutical compounds which contain one or more NnullH bonds to produce prodrugs containing at least one NnullS bond. These NnullS bond-containing prodrugs could have optimized stability, solubility, cell membrane permeability, pharmacokinetic properties and other pharmaceutical properties over the pharmaceutical compounds from which they are formed, depending upon the nature of the promoiety. Reversion of the prodrug to the parent pharmaceutical compound occurs by the reaction of the prodrugs with thiol molecules such as cysteine, glutathione or any other thiol containing molecule. Further, the present invention relates to methods of making NnullS bond-containing prodrugs of pharmaceutical compounds containing one or more NnullH bonds whereby sulfur-containing promoieties are attached to the parent compounds to create at least one NnullS bond.

    摘要翻译： 本发明涉及含有一个或多个N-H键的药物化合物的新型前体药物。 更具体地说，本发明的本实施方案涉及前药，其中含硫衍生物与含有一个或多个N-H键的药物化合物连接以产生含有至少一个N-S键的前药。 这些含有N-S键的前药可以相对于形成它们的药物化合物具有优化的稳定性，溶解性，细胞膜通透性，药代动力学性质和其它药物性质，这取决于促进因素的性质。 通过前体药物与巯基分子如半胱氨酸，谷胱甘肽或任何其它含硫醇分子的反应，将前药转化为母体药物化合物。 此外，本发明涉及制备含有一个或多个N-H键的药物化合物的含N-S键的前体药物的方法，其中含硫衍生物与母体化合物连接以产生至少一个N-S键。

    Certain 2,4-pentadienamide pestacides
    8.
    发明授权
    Certain 2,4-pentadienamide pestacides 失效
    某些2,4-戊二烯酰胺类杀虫剂

    公开(公告)号：US5326755A

    公开(公告)日：1994-07-05

    申请号：US923970

    申请日：1992-09-10

    申请人： Robert J. Blade ,  George S. Cockerill

    发明人： Robert J. Blade ,  George S. Cockerill

    IPC分类号： A01N37/18 ,  A01N37/28 ,  A01N43/40 ,  A01N49/00 ,  A01N55/10 ,  A01P7/02 ,  A01P7/04 ,  C07C233/09 ,  C07C233/13 ,  C07C233/22 ,  C07C233/91 ,  C07C313/28 ,  C07D213/71 ,  C07F7/10 ,  A01N55/00 ,  C07C233/12 ,  C07C222/47

    CPC分类号： A01N49/00 ,  C07C233/91 ,  C07C313/28 ,  C07D213/71 ,  C07C2101/02

    摘要： The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-5 alkylcarbonyl or aryl or CO.sub.2 R.sup.9 where R.sup.9 is an C.sub.1-4 alkyl or aryl, and a is 1 or 2;(B) --CR.sup.15 R.sup.16 X.sup.3 R.sup.17 where R.sup.15 and R.sup.16 are hydrogen or C.sub.1-4 alkyl, X.sup.3 is oxygen or sulphur and R.sup.17 is C.sub.1-4 alkyl, C.sub.1-5 alkylcarbonyl or aralkylcarbonyl R.sup.17,R.sup.15 X.sup.3, their preparation, pesticidal compositions containing them and their use against pests.

    摘要翻译： PCT No.PCT / GB91 / 00539 Sec。 371日期：1992年9月10日 102（e）日期1992年9月10日PCT 1991年4月8日PCT PCT。 WO91 / 16301 PCT出版物 1991年10月31日。本申请公开了式I的杀虫活性化合物：QQ1CR1 = CR2CR3 = CR4C（= X1）NR5R6或其盐，其中Q为单环芳环，或Q为二卤代乙烯基或基团 R7-C = C-，其中R7是C1-4烷基，三C1-4烷基甲硅烷基，卤素或氢; Q1是任选被一个或多个选自C 1-3烷基，卤素，C 1-3卤代烷基，炔基或氰基的基团取代的1,2-环丙基环; R 1，R 2，R 3和R 4相同或不同，至少一个为氢，其余独立地选自氢，卤素，C 1-4烷基或C 1-4卤代烷基; X1是氧或硫; R 5为任选取代的C 1-8烃基，卤素，氰基，三氟甲基，三氟甲硫基或C 1-6烷氧基; 并且R 6选自：（A）-Y = X 2 - （R 8）a，其中X 2为O或S，Y为碳，R 8为氢，C 1-4烷基，C 1-4烷氧基，C 1-5烷基羰基或芳基或 CO 2 R 9，其中R 9为C 1-4烷基或芳基，a为1或2; （B）-CR15R16X3R17其中R15和R16为氢或C1-4烷基，X3为氧或硫，R17为C1-4烷基，C1-5烷基羰基或芳烷基羰基R17，R15X3，其制备方法，含有它们的杀虫组合物及其用途 反对有害生物