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    FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS
    5.
    发明申请
    FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS 审中-公开
    含有吡啶化合物的配方

    公开(公告)号：US20090325973A1

    公开(公告)日：2009-12-31

    申请号：US12298652

    申请日：2007-04-27

    申请人： D. Martin Watterson ,  Linda Van Eldik ,  Wenhui Hu

    发明人： D. Martin Watterson ,  Linda Van Eldik ,  Wenhui Hu

    IPC分类号： A61K31/501 ,  C07D403/04

    CPC分类号： A61K31/506 ,  A61K31/501 ,  C07D237/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

    摘要： The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfenyl, sulfinyl, sulfonyl, sulfonate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, ═O, ═S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications.

    摘要翻译： 本发明涉及化合物，组合物和制备和使用它们的方法。 特别地，本发明提供选择的式I的哒嗪化合物独立地是氢，羟基，烷基，烯基，炔基，亚烷基，亚烯基，烷氧基，烯氧基，环烷基，环烯基，环炔基，环烷氧基，芳基，芳氧基，芳基烷氧基，芳酰基， 杂环，酰基，酰氧基，氨基，亚氨基，叠氮基，硫醇，硫代烷基，硫代烷氧基，硫代芳基，硝基，氰基，卤素，硫酸根，亚磺酰基，亚磺酰基，磺酰基，磺酸酯，亚砜，甲硅烷基，甲硅烷氧基，甲硅烷基烷基，甲硅烷硫基， -S，膦酸酯，脲基，羧基，羰基，氨基甲酰基或甲酰胺; X是任选取代的嘧啶基或哒嗪基，异构体，药用盐或其衍生物。 本发明另外涉及包含该化合物的组合物，以及使用该化合物和组合物调节细胞途径，用于治疗或预防炎性疾病，用于研究，药物筛选和治疗应用的方法。

    SALTS OF PYRIDAZINE COMPOUNDS
    8.
    发明申请
    SALTS OF PYRIDAZINE COMPOUNDS 审中-公开
    吡啶化合物的盐

    公开(公告)号：US20100168120A1

    公开(公告)日：2010-07-01

    申请号：US12298624

    申请日：2007-04-27

    申请人： D.Martin Watterson ,  Linda Van Eldik ,  Wenhui Hu

    发明人： D.Martin Watterson ,  Linda Van Eldik ,  Wenhui Hu

    IPC分类号： A61K31/506 ,  C07D403/14 ,  A61P29/00

    CPC分类号： A61K31/506 ,  C07D403/12

    摘要： The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, ═S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.

    摘要翻译： 本发明涉及式I的哒嗪化合物的稳定且基本纯化的合成药学上可接受的酸加成盐，其中R 10是氢，羟基，烷基，烷氧基，烯基，炔基，亚烷基，芳基，杂芳基，磺酰基，亚磺酰基，亚硫酰基，氨基， 亚氨基，叠氮基，硫醇，硫代烷基，硫代烷氧基，硫代芳基，硝基，氰基，卤素，= O，S，羧基，羰基，氨基甲酰基，甲酰胺或膦酸酯，R 11是烷基，烷氧基，烯基，炔基，亚烷基，亚烯基， 烷氧基，芳基，芳氧基，芳基烷氧基，芳酰基，杂芳基，杂环，酰基，酰氧基，磺酰基，亚磺酰基，亚磺酰基，氨基，亚氨基，叠氮基，硫醇，硫代烷基，硫代烷氧基，硫代芳基，硝基，氰基，卤素，= 0， 膦酸酯，羧基，羰基，氨基甲酰基，羧酰胺或脲基。 本发明还涉及制剂，剂型和包含盐的组合物，以及使用盐，制剂，剂型和组合物的方法。

    Protein Kinase Targeted Therapeutics
    9.
    发明申请
    Protein Kinase Targeted Therapeutics 审中-公开
    蛋白激酶靶向治疗

    公开(公告)号：US20080051410A1

    公开(公告)日：2008-02-28

    申请号：US11833152

    申请日：2007-08-02

    申请人： D. Watterson ,  Linda Van Eldik

    发明人： D. Watterson ,  Linda Van Eldik

    IPC分类号： A61K31/50 ,  A61P43/00

    CPC分类号： A61K31/50 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated protein kinase (MAPK) pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or casein kinase (CK) pathways (e.g., CK1δ, and upstream and downstream protein kinases), and diseases and disorders related to MAPK pathways (e.g., p38 MAPK, JNK, ERK, and upstream and downstream protein kinases) and/or CK pathways (e.g., CK1δ, and upstream and downstream protein kinases).

    摘要翻译： 本发明涉及可用于治疗与蛋白激酶相关的疾病和病症的组合物和方法。 特别地，本发明涉及用于靶向与丝裂原活化蛋白激酶（MAPK）途径相关的蛋白激酶（例如p38MAPK，JNK，ERK以及上游和下游蛋白激酶）和/或酪蛋白激酶（CK）的组合物和方法 ）途径（例如CK1delta以及上游和下游蛋白激酶）以及与MAPK途径相关的疾病和病症（例如p38 MAPK，JNK，ERK以及上游和下游蛋白激酶）和/或CK途径（例如CK1delta， 和上游和下游蛋白激酶）。