Inhibitors of TNFalpha, PDE4 and B-RAF, compositions thereof and methods of use therewith
    2.
    发明申请
    Inhibitors of TNFalpha, PDE4 and B-RAF, compositions thereof and methods of use therewith 审中-公开
    TNFalpha,PDE4和B-RAF的抑制剂,其组合物及其使用方法

    公开(公告)号:US20080004271A1

    公开(公告)日:2008-01-03

    申请号:US11654344

    申请日:2007-01-16

    CPC分类号: C07D495/04

    摘要: Provided herein are compounds having TNFα and/or PDE4 and/or B-RAF inhibitory activity, and compositions thereof. In particular, provided herein are compounds of the formula I: and pharmaceutically acceptable salts, solvates, hydrates, clathrates, stereoisomers, polymorphs and prodrugs thereof, wherein Ar, R1, R2, R3, R4, n and Z are as described herein. Further provided herein are methods for treating or preventing various diseases and disorders by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors. In particular, provided herein are methods for preventing or treating cancer, inflammatory disorders, cognition and memory disorders and autoimmune disorders, or one or more symptoms thereof by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors.

    摘要翻译: 本文提供具有TNFα和/或PDE4和/或B-RAF抑制活性的化合物及其组合物。 特别地,本文提供了式I的化合物及其药学上可接受的盐,溶剂合物,水合物,包合物,立体异构体,多晶型物和前药,其中Ar,R 1,R 2, R S,R 3,R 4,n和Z如本文所述。 本文还提供了通过向患者施用一种或多种TNFα和/或PDE4和/或B-RAF抑制剂来治疗或预防各种疾病和病症的方法。 特别地,本文提供了通过向患者施用一种或多种TNFα和/或PDE4和/或B-RAF抑制剂来预防或治疗癌症,炎症性疾病,认知和记忆障碍和自身免疫性疾病或其一种或多种症状的方法 。

    Isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones and derivatives thereof a JNK inhibitors and compositions and methods related thereto
    3.
    发明申请
    Isothiazoloanthrones, isoxazoloanthrones, isoindolanthrones and derivatives thereof a JNK inhibitors and compositions and methods related thereto 失效
    异噻唑烷酮,异恶唑酮,异吲哚酮及其衍生物,JNK抑制剂及其组合物和方法

    公开(公告)号:US20060004080A1

    公开(公告)日:2006-01-05

    申请号:US11159592

    申请日:2005-06-22

    IPC分类号: A61K31/403 C07D209/80

    CPC分类号: C07D275/04 C07D417/12

    摘要: Isaothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein Ro is —CH2—, —SO—, —O—, —SO2—, or —S—; compositions comprising the iazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isaothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.

    摘要翻译: 异噻唑鎓,异恶唑酮,异吲哚酮,及其衍生物及其药学上可接受的盐,其中R 1是-CH 2 - , - SO-,-O- ,-SO 2 - 或-S-; 包含重氮芳烃,异恶唑酮,异吲哚酮及其衍生物的组合物; 本文描述了通过给予异噻唑酮,异恶唑酮,异吲哚酮及其衍生物来抑制Jun N末端激酶(JNK)减轻的疾病的治疗或预防方法。

    Indazole compounds and methods of use thereof
    4.
    发明申请
    Indazole compounds and methods of use thereof 审中-公开
    吲唑化合物及其使用方法

    公开(公告)号:US20060004043A1

    公开(公告)日:2006-01-05

    申请号:US10993981

    申请日:2004-11-19

    摘要: This invention is directed to Indazole Compounds or pharmaceutically acceptable salts, solvates and hydrates thereof. The Indazole Compounds have utility in the treatment or prevention of a wide range of diseases and disorders that are responsive to the inhibition, modulation or regulation of kinases, such as inflammatory diseases, abnormal angiogenesis and diseases related thereto, cancer, atherosclerosis, a cardiovascular disease, a renal disease, an autoimmune condition, macular degeneration, disease-related wasting, an asbestos-related condition, pulmonary hypertension, diabetes, obesity, pain and others. Thus, methods of treating or preventing such diseases and disorders are also disclosed, as are pharmaceutical compositions comprising one or more of the Indazole Compounds. This invention is based, in part, upon the discovery of a novel class of 5-triazolyl substituted indazole molecules that have potent activity with respect to the modulation of protein kinases. Thus, the invention encompasses orally active molecules as well as parenterally active molecules which can be used at lower doses or serum concentrations for treating diseses or disorders associated with protein kinase signal transduction.

    摘要翻译: 本发明涉及吲唑化合物或其药学上可接受的盐,溶剂化物和水合物。 吲唑化合物可用于治疗或预防对抑制,调节或调节激酶(例如炎性疾病,异常血管生成和与之相关的疾病,癌症,动脉粥样硬化,心血管疾病)的各种疾病和病症 肾脏疾病,自身免疫性疾病,黄斑变性,疾病相关性消耗,石棉相关病症,肺动脉高压,糖尿病,肥胖,疼痛等。 因此,还公开了治疗或预防这些疾病和病症的方法,以及包含一种或多种吲唑化合物的药物组合物。 本发明部分基于发现关于蛋白激酶调节具有强力活性的新一类5-三唑基取代的吲唑分子。 因此,本发明包括口服活性分子以及肠胃外活性分子,其可以以较低剂量或血清浓度使用,用于治疗与蛋白激酶信号转导相关的疾病或障碍。

    Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer
    5.
    发明申请
    Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer 审中-公开
    苯并吡喃酮化合物,其组合物,以及治疗或预防癌症的方法

    公开(公告)号:US20070123511A1

    公开(公告)日:2007-05-31

    申请号:US11473564

    申请日:2006-06-23

    IPC分类号: A61K31/55 C07D405/02

    CPC分类号: C07D311/18 C07D311/16

    摘要: This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound to a patient in need thereof. The Benzopyranone Compounds have the formula: including pharmaceutically acceptable salts thereof, wherein R1 and n are as defined herein.

    摘要翻译: 本发明涉及苯并吡喃酮化合物,包含苯并吡喃酮化合物的组合物以及用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法,包括向有需要的患者施用有效量的苯并吡喃酮化合物。 苯并吡喃酮化合物具有下式:包括其药学上可接受的盐,其中R 1和n如本文所定义。

    4-((4-(2-Azaperhydroepinylethoxy)phenyl)methyl)-3-2(2,4-dichlorophenyl)-7-hydroxychromen-2-one, pharmaceutically acceptable salts thereof and methods of use therewith
    7.
    发明申请
    4-((4-(2-Azaperhydroepinylethoxy)phenyl)methyl)-3-2(2,4-dichlorophenyl)-7-hydroxychromen-2-one, pharmaceutically acceptable salts thereof and methods of use therewith 审中-公开
    4 - ((4-(2-氮杂氢化乙氧基)苯基)甲基)-3-2(2,4-二氯苯基)-7-羟基色烯-2-酮,其药学上可接受的盐及其使用方法

    公开(公告)号:US20070191343A1

    公开(公告)日:2007-08-16

    申请号:US11523376

    申请日:2006-09-18

    IPC分类号: A61K31/55 C07D409/02

    CPC分类号: C07D311/18 C07D311/16

    摘要: This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or neoplastic cell comprising administering an effective amount of a Benzopyranone Compound to a patient in need thereof. The Benzopyranone Compounds have the formula: including pharmaceutically acceptable salts thereof, wherein R1 and n are as defined herein.

    摘要翻译: 本发明涉及苯并吡喃酮化合物,包含苯并吡喃酮化合物的组合物以及用于治疗或预防癌症或抑制癌细胞或肿瘤细胞生长的方法,包括向有需要的患者施用有效量的苯并吡喃酮化合物。 苯并吡喃酮化合物具有下式:包括其药学上可接受的盐,其中R 1和n如本文所定义。