8-AZAPROSTAGLANDIN DERIVATIVES AND MEDICAL USE THEREOF
    1.
    发明申请
    8-AZAPROSTAGLANDIN DERIVATIVES AND MEDICAL USE THEREOF 审中-公开
    8-AZAPROSTAGLANDIN衍生物及其医疗用途

    公开(公告)号:US20080033033A1

    公开(公告)日:2008-02-07

    申请号:US11749531

    申请日:2007-05-16

    CPC分类号: C07D417/12 C07D417/14

    摘要: 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.

    摘要翻译: 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。

    Pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising EP4 agonist as the active ingredient
    3.
    发明授权
    Pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising EP4 agonist as the active ingredient 失效
    用于治疗与包含EP4激动剂作为活性成分的骨量减少相关的疾病的药物组合物

    公开(公告)号:US07608637B2

    公开(公告)日:2009-10-27

    申请号:US10484500

    申请日:2002-07-22

    IPC分类号: A61K31/40 A01N43/36

    摘要: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).

    摘要翻译: 用于预防和/或治疗与包含EP4激动剂作为活性成分的骨量减少相关的疾病的局部施用的药物组合物。 包含具有前列腺素骨架的化合物作为代表的EP4激动剂具有促进骨形成的作用,因此可用于预防和/或治疗与骨质量减少有关的疾病(骨疾病如原发性骨质疏松症,继发性骨质疏松症 骨质疏松症,癌症的骨转移,高钙血症,佩吉特氏病,骨丢失和骨坏死,术后成骨,骨移植的替代疗法)。

    8-azaprostaglandin derivatives and medical use thereof
    6.
    发明授权
    8-azaprostaglandin derivatives and medical use thereof 失效
    8-氮杂普罗兰前列腺素衍生物及其医疗用途

    公开(公告)号:US07256211B1

    公开(公告)日:2007-08-14

    申请号:US10542724

    申请日:2004-01-20

    CPC分类号: C07D417/12 C07D417/14

    摘要: 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.

    摘要翻译: 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。

    BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
    7.
    发明申请
    BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES 有权
    双相化合物及其用途用于医疗用途

    公开(公告)号:US20130310438A1

    公开(公告)日:2013-11-21

    申请号:US13982052

    申请日:2012-01-26

    IPC分类号: C07D335/04

    CPC分类号: C07D335/04 C07F7/1804

    摘要: Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc.Since a compound represented by the formula (I): (wherein definition of each group is as described in the specification), or a salt thereof, a solvate thereof, or a prodrug thereof has strong intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.

    摘要翻译: 本发明提供一种具有强烈的眼内降低作用,对眼睛无刺激性,幽默蛋白质上升等副作用的化合物。由式(I)表示的化合物:(其中,各组的定义如 说明书)或其盐,其溶剂合物或其前药具有强烈的眼内压降低活性,并且对眼睛没有副作用,例如眼刺激性(充血,角膜混浊等),房水蛋白 上升等,安全性高,可以作为预防和/或治疗青光眼等的优异剂。

    Bilirubin Excretion Enhancer
    10.
    发明申请
    Bilirubin Excretion Enhancer 审中-公开
    胆红素排泄增强剂

    公开(公告)号:US20140187744A1

    公开(公告)日:2014-07-03

    申请号:US14237694

    申请日:2012-08-09

    IPC分类号: C07K14/765

    摘要: The purpose of the present invention is to establish a novel therapy method for hyperbilirubinemia and therefore, to provide a bilirubin excretion enhancer. The present invention provides a bilirubin excretion enhancer comprising, as an active ingredient, a serum albumin domain II-like protein comprising a serum albumin subdomain IIA. In one embodiment, the serum albumin subdomain IIA has an amino acid sequence of SEQ ID NO: 1. In one embodiment, the serum albumin domain II-like protein is a serum albumin domain II. In one embodiment, the serum albumin domain II comprises the amino add sequence of SEQ ID NO: 4.

    摘要翻译: 本发明的目的是建立一种新的高胆红素血症治疗方法,从而提供一种胆红素排泄增强剂。 本发明提供一种胆红素排泄增强剂,其包含作为活性成分的血清白蛋白结构域II样蛋白,其包含血清白蛋白亚结构域IIA。 在一个实施方案中,血清白蛋白亚结构域IIA具有SEQ ID NO:1的氨基酸序列。在一个实施方案中,血清白蛋白结构域II样蛋白是血清白蛋白结构域II。 在一个实施方案中,血清白蛋白结构域II包含SEQ ID NO:4的氨基酸序列。