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    • 8. 发明授权
    • 8-azaprostaglandin derivatives and medical use thereof
    • 8-氮杂普罗兰前列腺素衍生物及其医疗用途
    • US07256211B1
    • 2007-08-14
    • US10542724
    • 2004-01-20
    • Tohru KambeToru MaruyamaKaoru KobayashiKousuke TaniYoshihiko NakaiToshihiko NagaseTakayuki MaruyamaKiyoto SakataHideyuki YoshidaShinsei FujimuraAkio NishiuraNobutaka Abe
    • Tohru KambeToru MaruyamaKaoru KobayashiKousuke TaniYoshihiko NakaiToshihiko NagaseTakayuki MaruyamaKiyoto SakataHideyuki YoshidaShinsei FujimuraAkio NishiuraNobutaka Abe
    • A61K31/40A61K31/426C07D207/12C07D207/36
    • C07D417/12C07D417/14
    • The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc. Furthermore, the compounds also have an action of accelerating bone formation, so it is expected to be useful for the prevention and/or treatment of diseases associated with loss in bone mass, for example, primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss, osteonecrosis, bone formation after bone operation, alternative treatment for bone grafting.
    • 该药物组合物包含本发明化合物,其具有式(I)表示的8-氮杂前列腺素骨架(其中所有符号具有与说明书相同的含义)其盐,其溶剂合物或环糊精包合物,或 其前药和它们作为活性成分具有EP 4激动作用,因此被认为可用于预防和/或治疗免疫疾病,哮喘,神经元细胞死亡,关节炎,肺衰竭,肺纤维化, 肺气肿,支气管炎,慢性阻塞性肺疾病,肝损伤,急性肝炎,肾炎,肾功能不全,高血压,心肌缺血,全身炎症反应综合征,败血症,血液综合征,巨噬细胞活化综合征,Still氏病,川崎病,烧伤,全身性肉芽肿病 ,溃疡性结肠炎,克罗恩病,透析中的高细胞因子血症,多器官功能衰竭,休克和青光眼等。 该化合物还具有加速骨形成的作用,因此预期可用于预防和/或治疗与骨质量损失相关的疾病,例如原发性骨质疏松症,继发性骨质疏松症,癌症的骨转移, 高钙血症,佩吉特氏病,骨丢失,骨坏死,骨手术后的骨形成,骨移植的替代治疗。
    • 10. 发明申请
    • 8-AZAPROSTAGLANDIN DERIVATIVES AND MEDICAL USE THEREOF
    • 8-AZAPROSTAGLANDIN衍生物及其医疗用途
    • US20080033033A1
    • 2008-02-07
    • US11749531
    • 2007-05-16
    • Tohru KambeToru MaruyamaKaoru KobayashiKousuke TaniYoshihiko NakaiToshihiko NagaseTakayuki MaruyamaKiyoto SakataHideyuki YoshidaShinsei FujimuraAkio NishiuraNobutaka Abe
    • Tohru KambeToru MaruyamaKaoru KobayashiKousuke TaniYoshihiko NakaiToshihiko NagaseTakayuki MaruyamaKiyoto SakataHideyuki YoshidaShinsei FujimuraAkio NishiuraNobutaka Abe
    • A61K31/41A61K31/4015C07D207/18C07D257/04
    • C07D417/12C07D417/14
    • The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification.) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc. Furthermore, the compounds also have an action of accelerating bone formation, so it is expected to be useful for the prevention and/or treatment of diseases associated with loss in bone mass, for example, primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss, osteonecrosis, bone formation after bone operation, alternative treatment for bone grafting.
    • 包含本发明化合物的盐,其盐,其溶剂合物或环糊精包合物,其具有由式(I)表示的8-氮杂前列腺素骨架(其中所有符号具有与说明书相同的含义) 或其前药,并且它们作为活性成分具有EP 4激动作用,因此被认为可用于预防和/或治疗免疫疾病,哮喘,神经元细胞死亡,关节炎,肺衰竭,肺纤维化 ,肺气肿,支气管炎,慢性阻塞性肺疾病,肝损伤,急性肝炎,肾炎,肾功能不全,高血压,心肌缺血,全身炎症反应综合征,败血症,血液综合征,巨噬细胞活化综合征,静脉炎,川崎病,烧伤,系统性 肉芽肿病,溃疡性结肠炎,克罗恩病,透析中的高细胞因子血症,多器官功能衰竭,休克和青光眼等。 此外,化合物还具有促进骨形成的作用,因此预期可用于预防和/或治疗与骨量丧失相关的疾病,例如原发性骨质疏松症,继发性骨质疏松症,癌症的骨转移, 高钙血症,佩吉特氏病,骨丢失,骨坏死,骨手术后的骨形成,骨移植的替代治疗。