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    Heterocyclo-substituted imidazoles for the treatment of inflammation
    1.
    发明申请
    Heterocyclo-substituted imidazoles for the treatment of inflammation 审中-公开
    杂环取代的咪唑用于治疗炎症

    公开(公告)号：US20050096368A1

    公开(公告)日：2005-05-05

    申请号：US10653399

    申请日：2003-09-02

    申请人： Ish Khanna ,  Richard Weier ,  Paul Collins ,  Yi Yu ,  Xiangdong Xu ,  Richard Partis ,  Francis Koszyk ,  Renee Huff

    发明人： Ish Khanna ,  Richard Weier ,  Paul Collins ,  Yi Yu ,  Xiangdong Xu ,  Richard Partis ,  Francis Koszyk ,  Renee Huff

    IPC分类号： A61K31/4178 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5377 ,  C07D233/32 ,  C07D233/54 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/02 ,  C07D419/04

    CPC分类号： C07D233/64 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D419/04

    摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy. aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R13 and R14 are independently selected from aryl and heterocyclo, wherein R13 and R14 are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R13 and R14 is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了一类咪唑基化合物用于治疗炎症。 特别感兴趣的化合物由式（V）定义，其中R 3是选自氢，烷基，卤代烷基，芳烷基，杂环烷基，杂芳烷基，酰基，氰基，烷氧基，烷硫基，烷硫基烷基，烷基磺酰基 环烷基硫基，环烷硫基烷基，环烷基磺酰基，环烷基磺酰基烷基，卤代烷基磺酰基，芳基磺酰基，卤素，羟基烷基，烷氧基烷基，烷基羰基，芳基羰基，芳烷基羰基，杂环羰基，氰基烷基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-烷基-N-芳基氨基烷基，羧基烷基，烷氧基羰基烷基， 卤代烷基羰基，羧基，氨基羰基，烷基氨基羰基，烷基氨基羰基烷基，杂芳基烷氧基烷基，杂芳氧基烷基，杂芳硫基烷基，芳烷氧基，芳烷硫基，杂芳烷氧基，杂芳烷硫基，杂芳基烷硫基烷基，杂芳氧基，杂芳硫基，芳硫基烷基，芳氧基烷基，芳硫基，芳氧基。 芳烷硫基烷基，芳烷氧基烷基，芳基和杂芳基; 其中R 4是选自氢，烷基和卤素的基团; 并且其中R 13和R 14独立地选自芳基和杂环，其中R 13和R 14是 任选地在可取代的位置被一个或多个独立地选自烷基磺酰基，氨基磺酰基，卤素，烷硫基，烷基，氰基，羧基，烷氧基羰基，卤代烷基，羟基，烷氧基，羟基烷基，烷氧基烷基，卤代烷氧基，氨基，烷基氨基，芳基氨基和硝基的基团取代。 只要R 13和R 14中的至少一个为被烷基磺酰基或氨基磺酰基取代的芳基; 或其药学上可接受的盐。

    Process for the preparation of 6-(n-butylamino)-6-deoxy-1,2-O-(imeihylethylidine)-a-L-Sorbofuranose and derivatives thereof
    9.
    发明授权
    Process for the preparation of 6-(n-butylamino)-6-deoxy-1,2-O-(imeihylethylidine)-a-L-Sorbofuranose and derivatives thereof 失效
    6-（正丁基氨基）-6-脱氧-1,2-（1-甲基乙基）-a-L-呋喃核糖及其衍生物的制备方法

    公开(公告)号：US5281724A

    公开(公告)日：1994-01-25

    申请号：US720335

    申请日：1991-06-25

    申请人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    发明人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    IPC分类号： C07D211/46 ,  C07D307/20 ,  C07D493/10

    CPC分类号： C07D493/10 ,  C07D211/46 ,  C07D307/20

    摘要： A process for the preparation of 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and 6-(n-substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and derivatives of the formula: ##STR1## wherein R' is benzyl or R, wherein R is hydrogen, alkyl of 1 to 13 carbon atoms, and aralkyl wherein alkyl is a lower alkyl of 2 to 6 carbon atoms and aryl is phenyl, unsubstituted or substituted with lower alkyl of 1 to 6 carbon atoms, halo, lower alkoxy of 1 to 4 carbon atoms or thio lower alkyl of 1 to 4 carbon atoms by the steps of: treating L-sorbose with 2,2-dimethoxy propane to yield 1,2:4,6-di-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; and consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy- 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose.

    摘要翻译： 制备1,2-O-（1-甲基乙基）-α-L-呋喃核糖和6-（正 - 取代氨基）-6-脱氧-1,2-（1-甲基乙基） - α -L-呋喃核糖和下式的衍生物：其中R'是苄基或R，其中R是氢，1至13个碳原子的烷基和芳烷基，其中烷基是2至6个碳原子的低级烷基和芳基 是未取代的或被1至6个碳原子的低级烷基取代的苯基，卤素，1至4个碳原子的低级烷氧基或1至4个碳原子的硫代低级烷基，其步骤为：用2,2-双 得到1,2：4,6-二-O-（1-甲基乙基）-α-L-呋喃核糖; 在溶剂中用硫酸处理该化合物以产生1,2-O-（1-甲基乙基）-α-L-呋喃核糖; 并用磺酰氯和胺连续处理，得到6-（取代的氨基）-6-脱氧-1,2-（1-甲基乙基）-α-L-呋喃核糖。