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15 条记录 (耗时 0.078 秒)

    Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof
    4.
    发明授权
    Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof 失效
    制备1,5-（阿基米诺）-1,5-二脱氧-D-葡萄糖苷及其衍生物的方法

    公开(公告)号：US5151519A

    公开(公告)日：1992-09-29

    申请号：US521282

    申请日：1990-05-07

    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 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives of the formula: ##STR1## 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-dimethoxypropane to yield 1,2:4,6-di-O-(1-methylethylidene)-.alpha.-L-sorbanose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; adsorbing the compound on an ion exchange resin and hydrogenating to produce compounds of the above formula.

    摘要翻译： 制备1,5-（烷基亚氨基）-1,5-二脱氧-D-葡萄糖醇的方法和下式的衍生物：其中R是氢，1至13个碳原子的烷基，和其中烷基是 2至6个碳原子的低级烷基，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， 步骤：用2,2-二甲氧基丙烷处理L-山梨糖，得到1,2：4,6-di-O-（1-甲基亚乙基）-α-L-山梨糖; 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; 连续用磺酰氯和胺处理，得到6-（取代的氨基）-6-脱氧-1,2-（1-甲基乙基）-α-L-呋喃核糖; 将化合物吸附在离子交换树脂上并进行氢化以制备上式的化合物。

    Process for the preparation of 6-(n-butylamino)-6-deoxy-1,2-O-(imeihylethylidine)-a-L-Sorbofuranose and derivatives thereof
    5.
    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。

    Process for preparing prostaglandins
    6.
    发明授权
    Process for preparing prostaglandins 失效
    制备前列腺素的方法

    公开(公告)号：US5075478A

    公开(公告)日：1991-12-24

    申请号：US642718

    申请日：1991-01-17

    申请人： James R. Behling ,  John R. Medich

    发明人： James R. Behling ,  John R. Medich

    IPC分类号： C07C405/00

    CPC分类号： C07C405/00

    摘要： A process for preparing prostaglandin derivatives by reacting a trans bis-tin ethylene with an organo metal compound then with a compound selected from an epoxide, aldehyde, or ketone, then, without isolation and in the same reaction vessel, reacting with an organo lithium compound, a cuprate complex and a cyclopentenone to produce a prostaglandin intermediate having an unprotected hydroxyl group on the omega side chain.

    摘要翻译： 然后通过使反式二锡乙烯与有机金属化合物与选自环氧化物，醛或酮的化合物反应制备前列腺素衍生物的方法，然后在不分离的情况下和在相同的反应容器中与有机锂化合物 ，铜酸盐络合物和环戊烯酮，以产生在ω侧链上具有未被保护的羟基的前列腺素中间体。

    Method of treating ankylosing spondylitis
    7.
    发明授权
    Method of treating ankylosing spondylitis 有权
    强直性脊柱炎的治疗方法

    公开(公告)号：US08926975B2

    公开(公告)日：2015-01-06

    申请号：US14306658

    申请日：2014-06-17

    申请人： Robert L. Wong ,  Hartmut Kupper ,  John R. Medich

    发明人： Robert L. Wong ,  Hartmut Kupper ,  John R. Medich

    IPC分类号： A61K39/395 ,  C07K16/24

    CPC分类号： C07K16/241 ,  A61K2039/505

    摘要： The invention provides methods, uses and compositions for the treatment of ankylosing spondylitis (AS). The invention describes methods and uses for treating ankylosing spondylitis, wherein a TNFα inhibitor, such as a human TNFα antibody, or antigen-binding portion thereof, is used to reduce signs and symptoms of ankylosing spondylitis in a subject. Also described are methods for determining the efficacy of a TNFα inhibitor for treatment of ankylosing spondylitis in a subject.

    摘要翻译： 本发明提供了治疗强直性脊柱炎（AS）的方法，用途和组合物。 本发明描述了用于治疗强直性脊柱炎的方法和用途，其中使用TNFα抑制剂如人TNFα抗体或其抗原结合部分来减少受试者的强直性脊柱炎的体征和症状。 还描述了确定受试者中TNFα抑制剂治疗强直性脊柱炎的功效的方法。