BICYCLIC COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
    11.
    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。

    8-AZAPROSTAGLANDIN DERIVATIVES AND MEDICAL USE THEREOF
    12.
    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。

    Bicyclic compound and use thereof for medical purposes
    14.
    发明授权
    Bicyclic compound and use thereof for medical purposes 有权
    双环化合物及其用于医疗用途

    公开(公告)号:US09150537B2

    公开(公告)日:2015-10-06

    申请号:US13982052

    申请日:2012-01-26

    IPC分类号: C07D335/04 C07F7/18

    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。

    8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient
    17.
    发明授权
    8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient 失效
    8-氮杂的前列腺素衍生物化合物和包含该化合物作为活性成分的试剂

    公开(公告)号:US07683094B2

    公开(公告)日:2010-03-23

    申请号:US12139260

    申请日:2008-06-13

    IPC分类号: A61K31/40 C07D207/00

    摘要: An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.

    摘要翻译: 由式(I)(其中所有符号具有与说明书中所述相同的含义)表示的8-氮杂前列腺素,其药学上可接受的盐或其环糊精包合物。 由于式(I)表示的化合物强烈地与PGE受体中的EP2亚型结合,因此可用于免疫疾病,过敏性疾病,神经元细胞死亡,痛经,早产,流产,秃发,视网膜神经病变等的预防和/或治疗 青光眼,勃起功能障碍,关节炎,肺损伤,肺纤维化,肺气肿,支气管炎,慢性阻塞性肺病,肝损伤,急性肝炎,肝硬化,休克,肾炎,肾衰竭,循环系统疾病,全身性炎症反应综合征,败血症, 血细胞增多综合征,巨噬细胞活化综合征,静止病,川崎病,烧伤,全身肉芽肿,溃疡性结肠炎,克罗恩病,透析中的高细胞因子血症,多器官功能衰竭或骨骼疾病等。

    8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient
    18.
    发明授权
    8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient 失效
    8-氮杂的前列腺素衍生物化合物和含有这些化合物作为活性成分的药物

    公开(公告)号:US07402605B2

    公开(公告)日:2008-07-22

    申请号:US10506536

    申请日:2003-03-04

    IPC分类号: A61K31/40 C07D207/00

    摘要: An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.

    摘要翻译: 由式(I)(其中所有符号具有与说明书中所述相同的含义)表示的8-氮杂前列腺素,其药学上可接受的盐或其环糊精包合物。 由于式(I)表示的化合物强烈地与PGE受体中的EP2亚型结合,因此可用于免疫疾病,过敏性疾病,神经元细胞死亡,痛经,早产,流产,秃发,视网膜神经病变等的预防和/或治疗 青光眼,勃起功能障碍,关节炎,肺损伤,肺纤维化,肺气肿,支气管炎,慢性阻塞性肺病,肝损伤,急性肝炎,肝硬化,休克,肾炎,肾衰竭,循环系统疾病,全身炎症反应综合征,败血症, 血细胞增多综合征,巨噬细胞活化综合征,静止病,川崎病,烧伤,全身肉芽肿,溃疡性结肠炎,克罗恩病,透析中的高细胞因子血症,多器官功能衰竭或骨骼疾病等。