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42 条记录 (耗时 0.035 秒)

    Polyamine derivatives as antineoplastic agents
    34.
    发明授权
    Polyamine derivatives as antineoplastic agents 失效
    多胺衍生物作为抗肿瘤药

    公开(公告)号：US5654484A

    公开(公告)日：1997-08-05

    申请号：US457247

    申请日：1995-06-01

    申请人： Nellikunja J. Prakash ,  David M. Stemerick ,  Michael L. Edwards

    发明人： Nellikunja J. Prakash ,  David M. Stemerick ,  Michael L. Edwards

    IPC分类号： C07C211/09 ,  C07C211/14 ,  C07C211/00

    CPC分类号： C07C211/14 ,  C07C211/09

    摘要： The present invention relates to a method for the treatment of patients suffering from certain neoplastic disease states which comprises administering a therapeutically effective amount of a compound of the formula: ##STR1## wherein m is an integer 6 to 9, Z is a saturated (C.sub.2 -C.sub.6) alkylene moiety, each R group independently is hydrogen, methyl, ethyl, or n-propyl except that both R groups cannot be hydrogen when Z is a straight chain; or a pharmaceutically acceptable acid addition salt thereof. Said treatment can optionally comprise conjunctive therapy with a polyamine oxidase inhibitor. The invention also relates to certain novel polyamine derivatives.

    摘要翻译： 本发明涉及治疗患有某些肿瘤疾病状态的患者的方法，其包括施用治疗有效量的下式化合物：其中m为整数6至9，Z为饱和（C2 -C 6）亚烷基部分，每个R基团独立地为氢，甲基，乙基或正丙基，除了当Z为直链时，两个R基团不能为氢; 或其药学上可接受的酸加成盐。 所述治疗可以任选地包括与多胺氧化酶抑制剂的联合治疗。 本发明还涉及某些新型多胺衍生物。

    Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents
    35.
    发明授权
    Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents 失效
    烷基-4-甲硅烷基 - 苯酚及其酯作为抗动脉粥样硬化剂

    公开(公告)号：US5608095A

    公开(公告)日：1997-03-04

    申请号：US637968

    申请日：1996-04-30

    申请人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt, Jr. ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    发明人： Roger A. Parker ,  Michael L. Edwards ,  Mark J. Vaal ,  James E. Matt, Jr. ,  Kim S. Chen ,  Mark T. Yates ,  Paul S. Wright ,  Steven J. Busch

    IPC分类号： A61K31/695 ,  A61P3/06 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00 ,  A61P43/00 ,  C07F7/08 ,  C07F7/10 ,  C07F7/12 ,  C07F7/18

    CPC分类号： C07F7/0818

    摘要： This invention relates to compounds of the formula ##STR1## wherein R.sub.1 and R.sub.6 are each independently C.sub.1 -C.sub.6 alkyl;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group;R.sub.5 and R.sub.7 are each independently a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, or --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; with the proviso that when R.sub.2 and at least one of R.sub.5 or R.sub.7 is C.sub.1 -C.sub.6 alkyl, and Ar is not substituted with trifluoromethyl or --NR.sub.8 R.sub.9, then R is --C(O)--(CH.sub.2).sub.m --Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as antioxidant chemical additives useful for preventing oxidative deterioration in organic materials.

    摘要翻译： 本发明涉及式（1）的化合物，其中R 1和R 6各自独立地为C 1 -C 6烷基; R2，R3和R4各自独立地为氢或C1-C6烷基; R是氢或-C（O） - （CH 2）m-Q其中Q是氢或-COOH，m是整数1,2,3或4; Z是硫基，氧基或亚甲基; A是C1-C4亚烷基; R 5和R 7各自独立地为C 1 -C 6烷基或 - （CH 2）n - （Ar），其中n为整数0,1,2或3; 并且Ar是未取代的或被一至三个选自羟基，甲氧基，乙氧基，卤素，三氟甲基，C 1 -C 6烷基或-NR 8 R 9的取代基取代的苯基或萘基，其中R 8和R 9各自独立地为氢或C1- C6烷基; 条件是当R 2和R 5或R 7中的至少一个是C 1 -C 6烷基，并且Ar不被三氟甲基或-NR 8 R 9取代时，则R是-C（O） - （CH 2）m -Q; 或其药学上可接受的盐; 可用于治疗动脉粥样硬化和慢性炎症性疾病; 用于抑制VCAM-1和/或ICAM-1的细胞因子诱导的表达; 用于抑制LDL脂质的过氧化; 用于降低血浆胆固醇; 以及用作防止有机材料氧化变质的抗氧化剂添加剂。