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    Pyrazolo-pyridinone derivatives and methods of use
    44.
    发明授权
    Pyrazolo-pyridinone derivatives and methods of use 有权
    吡唑并吡啶酮衍生物及其用途

    公开(公告)号：US08080546B2

    公开(公告)日：2011-12-20

    申请号：US12288950

    申请日：2008-10-24

    Applicant: Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

    Inventor： Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

    IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of inflammatory diseases including rheumatoid arthritis, psoriasis and other disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

    Abstract translation: 本发明包括一类新的可用于预防和治疗促炎细胞因子介导的疾病，特别是p38活性介导的炎症和相关病症的化合物。 所述化合物具有通式I，其中A1，A2，A3，A4，A5，R1，R2和R3如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗炎性疾病（包括类风湿性关节炎，牛皮癣和其它病症）的用途，以及可用于制备式I化合物的中间体和方法 。

    Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof
    46.
    发明授权
    Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof 失效
    吡唑并吡啶酮和吡唑并吡嗪酮化合物作为P38调节剂及其使用方法

    公开(公告)号：US08022085B2

    公开(公告)日：2011-09-20

    申请号：US12150158

    申请日：2008-04-24

    Applicant: Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu

    Inventor： Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu

    IPC: C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D491/02 ,  C07D498/02 ,  A01N43/42 ,  A61K31/44

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

    Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 该化合物具有通式I，其中A1，A2，B，R1，R2，R4，R5，R6和Z如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体 和可用于制备式I化合物的方法。

    Vanilloid receptor ligands and their use in treatments
    47.
    发明授权
    Vanilloid receptor ligands and their use in treatments 失效
    香草素受体配体及其在治疗中的应用

    公开(公告)号：US07582761B2

    公开(公告)日：2009-09-01

    申请号：US10688246

    申请日：2003-10-16

    Applicant: Chenera Balan ,  Yunxin Bo ,  Celia Dominguez ,  Christopher H. Fotsch ,  Vijay K. Gore ,  Vu Van Ma ,  Mark H. Norman ,  Vassil I. Ognyanov ,  Yi-xin Qian ,  Xianghong Wang ,  Ning Xi ,  Shimin Xu

    Inventor： Chenera Balan ,  Yunxin Bo ,  Celia Dominguez ,  Christopher H. Fotsch ,  Vijay K. Gore ,  Vu Van Ma ,  Mark H. Norman ,  Vassil I. Ognyanov ,  Yi-xin Qian ,  Xianghong Wang ,  Ning Xi ,  Shimin Xu

    IPC: C07D401/04 ,  C07D401/06 ,  C07D403/04

    CPC classification number: C07D401/04 ,  C07D235/30 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

    Abstract: Therapeutic benzimidazoles having the general structure: and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

    Abstract translation: 具有一般结构的治疗性苯并咪唑和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管综合征，紧张性头痛，一般炎症，关节炎 ，风湿性疾病，骨关节炎，炎症性肠病，炎症性眼病，炎性或不稳定性膀胱疾病，牛皮癣，皮肤炎症成分炎症，慢性炎性病症，炎症性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛和相关的痛觉过敏和异常性疼痛，糖尿病性神经病变 疼痛，咳嗽，交感神经保持疼痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风， 胃肠疾病，胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

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