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    • 5. 发明授权
    • Pyrazolo-pyridinone compounds and methods of use thereof
    • 吡唑并吡啶酮化合物及其使用方法
    • US07846944B2
    • 2010-12-07
    • US12151478
    • 2008-05-06
    • Liping PettusAndrew TaskerShimin XuRyan Wurz
    • Liping PettusAndrew TaskerShimin XuRyan Wurz
    • C07D487/04A01N43/42A61K31/44
    • C07D471/04
    • 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, A3, A4, B, R1, R2, R3, R4 and R5 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.
    • 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。 化合物具有通式I,其中A1,A2,A3,A4,B,R1,R2,R3,R4和R5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。
    • 6. 发明申请
    • Pyrazolo-pyridinone compounds and methods of use thereof
    • 吡唑并吡啶酮化合物及其使用方法
    • US20090012299A1
    • 2009-01-08
    • US12151478
    • 2008-05-06
    • Liping PettusAndrew TaskerShimin XuRyan Wurz
    • Liping PettusAndrew TaskerShimin XuRyan Wurz
    • C07D487/04
    • C07D471/04
    • 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, A3, A4, B, R1, R2, R3, R4 and R5 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.
    • 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。 化合物具有通式I,其中A1,A2,A3,A4,B,R1,R2,R3,R4和R5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。
    • 8. 发明申请
    • Vanilloid receptor ligands and their use in treatments
    • 香草素受体配体及其在治疗中的应用
    • US20050165028A1
    • 2005-07-28
    • US11040668
    • 2005-01-21
    • Mark NormanVassil OgnyanovLiping Pettus
    • Mark NormanVassil OgnyanovLiping Pettus
    • A61K31/381A61K31/428A61K31/4433A61K31/452A61K31/506C07D213/26C07D277/82C07D319/18C07D319/20C07D401/12C07D405/12C07D409/12
    • C07D401/12C07D213/26C07D277/82C07D319/18C07D405/12C07D409/12
    • N-Bicyclic amides and derivatives thereof 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.
    • N-双环酰胺及其衍生物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,咳嗽症状,交感神经保持疼痛,输血综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道内脏运动性紊乱,泌尿生殖道,胃肠道或血管区域,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风, 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。
    • 9. 发明申请
    • Vanilloid receptor ligands and their use in treatments
    • 香草素受体配体及其在治疗中的应用
    • US20060058308A1
    • 2006-03-16
    • US11226844
    • 2005-09-13
    • Mark NormanLiping PettusXianghong WangJiawang Zhu
    • Mark NormanLiping PettusXianghong WangJiawang Zhu
    • A61K31/506A61K31/505C07D239/42C07D403/02
    • C07D239/48C07D401/12C07D401/14C07D403/12C07D405/12C07D405/14C07D417/12C07D417/14
    • Substituted pyridines and pyrimidines 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.
    • 取代的吡啶类和嘧啶类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,炎症性或不稳定性膀胱病,牛皮癣,皮肤炎症成分炎症,慢性炎性病症,炎性疼痛及相关的痛觉过敏和异常性疼痛,神经性疼痛及相关的痛觉过敏和异常性疼痛,糖尿病性神经病疼痛,灼痛 ,同情维持疼痛,传入综合征,哮喘,上皮组织损伤或功能障碍,单纯疱疹,呼吸道内脏运动性紊乱,泌尿生殖道,胃肠道或血管区域,伤口,烧伤,过敏性皮肤反应,瘙痒,白癜风,一般胃肠道疾病 严重溃疡,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。