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24 条记录 (耗时 0.059 秒)

    Inhibition of FGFR3 and treatment of multiple myeloma
    12.
    发明授权
    Inhibition of FGFR3 and treatment of multiple myeloma 失效
    抑制FGFR3和治疗多发性骨髓瘤

    公开(公告)号：US07825132B2

    公开(公告)日：2010-11-02

    申请号：US10983174

    申请日：2004-11-05

    申请人： Shaopei Cai ,  Joyce Chou ,  Eric Harwood ,  Carla C. Heise ,  Timothy D. Machajewski ,  David Ryckman ,  Xiao Shang ,  Marion Wiesmann ,  Shuguang Zhu

    发明人： Shaopei Cai ,  Joyce Chou ,  Eric Harwood ,  Carla C. Heise ,  Timothy D. Machajewski ,  David Ryckman ,  Xiao Shang ,  Marion Wiesmann ,  Shuguang Zhu

    IPC分类号： A61K31/47 ,  A01N43/40

    CPC分类号： A61K31/496

    摘要： Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.

    摘要翻译： 提供了抑制成纤维细胞生长因子受体3并治疗由成纤维细胞生长因子受体3介导的各种病症的方法，其包括向受试者施用结构I的化合物，其药学上可接受的盐，其互变异构体或其药学上可接受的盐 互变异构体 具有结构I的化合物具有以下结构，并且具有本文所述的变量。 这样的化合物可以用于制备用于抑制成纤维细胞生长因子受体3的药物，并且用于治疗由成纤维细胞生长因子受体3如多发性骨髓瘤介导的病症。

    Methods for synthesizing heterocyclic compounds
    13.
    发明授权
    Methods for synthesizing heterocyclic compounds 失效
    杂环化合物合成方法

    公开(公告)号：US08222413B2

    公开(公告)日：2012-07-17

    申请号：US11920078

    申请日：2006-05-17

    申请人： Gabriel Galvin ,  Eric Harwood ,  David Ryckman ,  Shuguang Zhu

    发明人： Gabriel Galvin ,  Eric Harwood ,  David Ryckman ,  Shuguang Zhu

    IPC分类号： C07D401/00 ,  C07D403/00

    CPC分类号： C07D295/135

    摘要： A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.

    摘要翻译： 合成杂环化合物的方法包括：在足以提供式VIH化合物的内部温度下使1-甲基哌嗪与5-氯-2-硝基苯胺反应。1-甲基哌嗪和5-氯-2-硝基苯胺在 溶剂，其含量基于溶剂量大于50体积％，和/或在大气压下在包含沸点大于100℃的有机溶剂组分的溶剂中反应。

    METHODS FOR SYNTHESIZING HETEROCYCLIC COMPOUNDS.
    14.
    发明申请
    METHODS FOR SYNTHESIZING HETEROCYCLIC COMPOUNDS. 失效
    合成杂环化合物的方法。

    公开(公告)号：US20110046376A1

    公开(公告)日：2011-02-24

    申请号：US11920078

    申请日：2006-05-17

    申请人： Gabriel Galvin ,  Eric Harwood ,  David Ryckman ,  Shuguang Zhu

    发明人： Gabriel Galvin ,  Eric Harwood ,  David Ryckman ,  Shuguang Zhu

    IPC分类号： C07D401/14 ,  C07D241/04 ,  C07D403/10

    CPC分类号： C07D295/135

    摘要： A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reacted in a solvent that comprises water in an amount greater than 50 percent by volume based on the amount of the solvent and/or are reacted in a solvent that comprises an organic solvent component that has a boiling point of greater than 100° C. at atmospheric pressure.

    摘要翻译： 合成杂环化合物的方法包括：在足以提供式VIH化合物的内部温度下使1-甲基哌嗪与5-氯-2-硝基苯胺反应。1-甲基哌嗪和5-氯-2-硝基苯胺在 溶剂，其含量基于溶剂量大于50体积％，和/或在大气压下在包含沸点大于100℃的有机溶剂组分的溶剂中反应。

    Hydroxythiol grignard reaction synthesis
    16.
    发明授权
    Hydroxythiol grignard reaction synthesis 失效
    羟基硫醇格氏反应合成

    公开(公告)号：US06476248B1

    公开(公告)日：2002-11-05

    申请号：US09515544

    申请日：2000-02-29

    申请人： David Ryckman ,  Mingbao Zhang ,  Guohua Chen

    发明人： David Ryckman ,  Mingbao Zhang ,  Guohua Chen

    IPC分类号： C07C32128

    CPC分类号： C07C319/02 ,  C07F7/1892 ,  Y02P20/55 ,  C07C323/20

    摘要： A method for the preparation of hydroxythiol compounds by reacting a hydroxyl-protected halide compound having the structure: X—R—OPg with magnesium in a Grignard-suitable solvent to form a hydroxyl-protected magnesium halide compound, wherein R is selected from substituted or unsubstituted aliphatic radicals, substituted or unsubstituted cyclic aliphatic radicals, substituted or unsubstituted aromatic radicals, substituted or unsubstituted araliphatic radicals and substituted or unsubstituted heterocyclic radicals; Pg is a protecting group; and X is selected from the group consisting of F, Cl, Br and I; then reacting said hydroxyl-protected magnesium halide compound with sulfur in the Grignard-suitable solvent to form a hydroxyl-protected thiomagnesium halide compound; and hydrolyzing the protected hydroxyl group to form a hydroxythiomagnesium halide compound and converting the thiomagnesium halide to a thiol; wherein the protecting group is selected so that species formed by the de-protection of the protecting group are inert toward thiols, or the method further includes the step of removing the protecting group species formed by de-protection of the hydroxyl group from the reaction mixture before converting the thiomagnesium halide to a thiol.

    摘要翻译： 通过使具有以下结构的羟基保护的卤化物与镁在格氏合适的溶剂中反应以形成羟基保护的卤化镁化合物来制备羟基硫醇化合物的方法，其中R选自取代或未取代的脂族基，取代的 取代或未取代的芳族基团，取代或未取代的芳脂族基团和取代或未取代的杂环基团; Pg是保护组; X选自F，Cl，Br和I; 然后使所述羟基保护的卤化镁化合物与格氏合适的溶剂中的硫反应形成羟基保护的卤化卤化镁化合物; 水解保护的羟基以形成羟基卤化镁化合物并将卤化硫化镁转化为硫醇; 其中选择保护基，使得通过保护基去保护形成的物质对硫醇是惰性的，或者该方法还包括从反应混合物中除去由羟基脱保护形成的保护基物种的步骤 之前将硫化镁卤化物转化为硫醇。

    Aromatic hydroxythiol synthesis using diazonium salts
    17.
    发明授权
    Aromatic hydroxythiol synthesis using diazonium salts 失效
    使用重氮盐的芳香族羟基硫醇合成

    公开(公告)号：US06303822B1

    公开(公告)日：2001-10-16

    申请号：US09515355

    申请日：2000-02-29

    申请人： Mingbao Zhang ,  David Ryckman ,  Eric MacMillan

    发明人： Mingbao Zhang ,  David Ryckman ,  Eric MacMillan

    IPC分类号： C07C32122

    CPC分类号： C07C319/06 ,  C07C319/22 ,  C07C319/24 ,  C07C323/35 ,  C07C323/20

    摘要： A method for the preparation of aromatic hydroxythiols including oxidizing an aromatic aminothiol to form an aminodisulfide compound; forming a bis-diazonium salt of the aminodisulfide compound; and reacting the bis-diazonium salt with water to form an aromatic hydroxyldisulfide compound, which is then reduced to the hydroxythiol. New bis-diazonium aromatic disulfide compounds are also disclosed.

    摘要翻译： 一种制备芳族羟基硫醇的方法，包括使芳族氨基硫醇氧化形成氨基二硫化物; 形成氨基二硫化物的双重重氮盐; 并使双重重氮盐与水反应形成芳族羟基二硫化物，然后将其还原成羟基硫醇。 还公开了新的二重氮芳族二硫化物。

    Process for preparing spirocyclic lactams
    18.
    发明授权
    Process for preparing spirocyclic lactams 失效
    制备螺环内酰胺的方法

    公开(公告)号：US5734061A

    公开(公告)日：1998-03-31

    申请号：US656334

    申请日：1996-06-13

    申请人： David Ryckman

    发明人： David Ryckman

    IPC分类号： C07D209/96

    CPC分类号： C07D209/96

    摘要： The invention is directed to an improved process for the preparation of spirocyclic lactams which utilizes diiodides in the spiro alkylation of lactams N-substituted with a tertiary amine group. The resultant spirocyclic lactams are useful in the production of various substituted azaspiranes which are useful as immunomodulatory agents.

    摘要翻译： PCT No.PCT / US94 / 14083 Sec。 371日期：1996年6月13日 102（e）日期1996年6月13日PCT 1994年12月7日PCT PCT。 公开号WO95 / 16657 日期1995年6月22日本发明涉及一种制备螺环内酰胺的改进方法，其利用二碘化物在用叔胺基团N-取代的内酰胺的螺烷基化中。 所得的螺环内酰胺可用于制备可用作免疫调节剂的各种取代的氮杂环丙烷。