利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

425 条记录 (耗时 0.03 秒)

    Imidazole lipoxygenase inhibitors
    51.
    发明授权
    Imidazole lipoxygenase inhibitors 失效
    咪唑脂氧合酶抑制剂

    公开(公告)号：US6037355A

    公开(公告)日：2000-03-14

    申请号：US43256

    申请日：1998-06-29

    申请人： Takashi Mano ,  Rodney W. Stevens

    发明人： Takashi Mano ,  Rodney W. Stevens

    IPC分类号： C07D493/08 ,  A61K31/35 ,  A61K31/415 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D521/00 ,  A01N43/40 ,  A01N43/50 ,  C07D233/02 ,  C07D401/04

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The present invention provides a compound of formula (I): ##STR1## and a pharmaceutically acceptable salt thereof, wherein Ar is phenylene optionally substituted with halo, hydroxy, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 halo-substituted alkyl or C.sub.1 -C.sub.4 halo-substituted alkoxy, X is --A--X.sup.1 -- or --X.sup.2 --A--, where A is a direct bond or C.sub.1 -C.sub.4 alkylene, and X.sup.1 is oxy, thio, sulfinyl or sulfonyl; Ar is phenylene, pyridylene or thienylene optionally substituted with halo, hydroxy, cyano, nitro, amino, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 halo-substituted alkyl, C.sub.1 -C.sub.4 halo-substituted alkoxy, C.sub.1 -C.sub.4 alkylamino or di(C.sub.1 -C.sub.4)alkylamino; Y is CN or CONR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 are independently hydrogen or C.sub.1 -C.sub.4 alkyl; and R is hydrogen or C.sub.1 -C.sub.6 alkyl; W is C.sub.2 -C.sub.3 alkylene, one carbon atom of which may be replaced by an oxygen atom. Further the invention provides a pharmaceutical composition for treating an inflammatory disease, allergy or cardiovascular diseases or the like in a mammalian subject which comprises a compound of formula (I) and a pharmaceutically acceptable carrier.

    摘要翻译： PCT No.PCT / IB96 / 00744 Sec。 371日期1998年6月29日第 102（e）1998年6月29日PCT PCT 1996年7月24日PCT公布。 出版物WO97 / 11079 日期：1997年3月27日本发明提供式（I）化合物及其药学上可接受的盐，其中Ar为任选被卤素，羟基，氰基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4 烷硫基，C 1 -C 4卤素取代的烷基或C 1 -C 4卤素取代的烷氧基，X是-A-X 1或-X 2 -A-，其中A是直接键或C 1 -C 4亚烷基，X 1是氧基，硫代 ，亚磺酰基或磺酰基; Ar是任选被卤素，羟基，氰基，硝基，氨基，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4卤素取代的烷基，C 1 -C 4卤素取代的烷氧基取代的亚苯基，亚吡啶基或噻吩基 ，C 1 -C 4烷基氨基或二（C 1 -C 4）烷基氨基; Y是CN或CONR1R2，其中R1和R2独立地是氢或C1-C4烷基; 和R是氢或C 1 -C 6烷基; W是C 2 -C 3亚烷基，其一个碳原子可被氧原子代替。 此外，本发明提供了用于治疗哺乳动物受试者中的炎性疾病，过敏或心血管疾病等的药物组合物，其包含式（I）化合物和药学上可接受的载体。

    Nitrophenyl, 10-deacetylated substituted taxol derivatives as dual functional cytotoxic/radiosensitizers
    54.
    发明授权
    Nitrophenyl, 10-deacetylated substituted taxol derivatives as dual functional cytotoxic/radiosensitizers 失效
    硝基苯基，10-脱乙酰基取代紫杉醇衍生物作为双功能细胞毒/放射增敏剂

    公开(公告)号：US5780653A

    公开(公告)日：1998-07-14

    申请号：US485496

    申请日：1995-06-07

    申请人： Chunlin Tao ,  Neil P. Desai ,  Patrick Soon-Shiong ,  Paul A. Sandford

    发明人： Chunlin Tao ,  Neil P. Desai ,  Patrick Soon-Shiong ,  Paul A. Sandford

    IPC分类号： A61K41/00 ,  C07D233/91 ,  C07D305/14 ,  C07D305/00 ,  A61K51/04 ,  C07D233/02 ,  C07D413/00

    CPC分类号： C07D305/14 ,  A61K41/0038

    摘要： In accordance with the present invention, there are provided derivatives of chemotherapeutic agents (e.g., paclitaxel), which serve as bifunctional agents. Invention derivatives retain the antitumor activity of the parent compound, and, coupled with the electron affinic substituents thereon, produce compounds which show a strong capability for radiosensitizing tumor cells growing in vitro. It is expected that a single drug which combines the properties of a radiosensitizer with chemotherapeutic activity will offer significant advantages not only to patients, but also to radiotherapists seeking improved modes of treatment. The combination of antitumor properties with electron-affinic function produces novel radiosensitizers, a second generation of drugs which are more powerful to fight cancers. Bifunctional agents with the dual properties of tubulin assembly and electron affinity will make the compounds useful not only as radiosensitizers, but also as cytotoxins.

    摘要翻译： 根据本发明，提供了用作双功能试剂的化学治疗剂（例如紫杉醇）的衍生物。 本发明衍生物保留了母体化合物的抗肿瘤活性，并且与其上的电子亲和取代基一起产生显示出对体外生长的肿瘤细胞放射增敏的强大能力的化合物。 预期将放射增敏剂的性质与化疗活性相结合的单一药物将不仅对患者具有显着的优点，而且还将提供寻求改善治疗方式的放射治疗师的显着优点。 抗肿瘤性质与电子亲和功能的组合产生新型放射增敏剂，第二代更强大的抗癌药物。 具有微管蛋白装配和电子亲和力的双重特性的双功能试剂将使得该化合物不仅用作放射增敏剂，而且用作细胞毒素。

    Photographically useful compounds including at least one 1,3-sulfur-oxygen ring system
    55.
    发明授权
    Photographically useful compounds including at least one 1,3-sulfur-oxygen ring system 失效
    包含至少一个1,3-硫氧环体系的照相有用的化合物

    公开(公告)号：US5674986A

    公开(公告)日：1997-10-07

    申请号：US645258

    申请日：1996-05-13

    申请人： Peter Viski ,  David P. Waller

    发明人： Peter Viski ,  David P. Waller

    IPC分类号： B82B1/00 ,  G03C8/10 ,  G03C8/40 ,  C09B29/01 ,  C07D233/02 ,  C09B29/036 ,  C09B29/15 ,  C09B29/36

    CPC分类号： G03C8/10 ,  G03C8/4033

    摘要： There are described heat-developable photosensitive image-recording materials which include a compound having at least one cyclic 1,3-sulfur-oxygen moiety. The compound is stable in the photographic processing composition but capable of undergoing cleavage in the presence of an imagewise distribution of silver ions and/or soluble silver complex made available as a function of development to liberate a reagent in an imagewise distribution corresponding to that of the silver ion and/or the soluble silver complex. The reagent includes a photographically useful group such as a complete dye or dye intermediate.

    摘要翻译： 描述了包含具有至少一个环状1,3-硫 - 氧部分的化合物的热显影光敏图象记录材料。 该化合物在照相处理组合物中是稳定的，但是在存在作为显影功能的银离子和/或可溶性银络合物的成像分布的存在下能够进行裂解以释放相应于 银离子和/或可溶性银络合物。 试剂包括照相用的基团，例如完整的染料或染料中间体。