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    2-naphthamide derivatives
    4.
    发明申请
    2-naphthamide derivatives 审中-公开
    2-萘甲酰胺衍生物

    公开(公告)号：US20060166989A1

    公开(公告)日：2006-07-27

    申请号：US10517677

    申请日：2003-05-30

    Applicant: Makoto Shimazaki ,  Osamu Sakurai ,  Toshiki Murata ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Satoru Yoshikawa ,  Masaomi Umeda ,  Masaomi Tajimi ,  Tsutomu Masuda ,  Takuya Shintani ,  Haruka Shimizu

    Inventor： Makoto Shimazaki ,  Osamu Sakurai ,  Toshiki Murata ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Satoru Yoshikawa ,  Masaomi Umeda ,  Masaomi Tajimi ,  Tsutomu Masuda ,  Takuya Shintani ,  Haruka Shimizu

    IPC: A61K31/537 ,  A61K31/44 ,  A61K31/195 ,  C07D213/55 ,  C07D265/30 ,  C07C237/40

    CPC classification number: C07C235/66

    Abstract: The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), pro-statitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.

    Abstract translation: 本发明涉及可用作药物制剂活性成分的2-萘甲酰胺。 本发明的2-萘甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。 这些疾病包括尿路疾病或病症如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺肥大 ），pro-statitis，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺增生症，膀胱炎或自发性膀胱过敏反应。 本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压 血友病和出血; 和炎症，因为该疾病也通过用IP受体拮抗剂治疗而缓解。

    Tetrahydro-quinolinylurea derivatives
    7.
    发明授权
    Tetrahydro-quinolinylurea derivatives 失效
    四氢 - 喹啉基脲衍生物

    公开(公告)号：US07683076B2

    公开(公告)日：2010-03-23

    申请号：US10578413

    申请日：2004-10-26

    Applicant: Axel Bouchon ,  Nicole Diedrichs ,  Achim Hermann ,  Klemens Lustig ,  Heinrich Meier ,  Josef Pernerstorfer ,  Elke Reiβmüller ,  Muneto Mogi ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto

    Inventor： Axel Bouchon ,  Nicole Diedrichs ,  Achim Hermann ,  Klemens Lustig ,  Heinrich Meier ,  Josef Pernerstorfer ,  Elke Reiβmüller ,  Muneto Mogi ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto

    IPC: C07D215/38 ,  A61K31/47

    CPC classification number: C07D215/38

    Abstract: This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

    Abstract translation: 本发明涉及可用作药物制剂活性成分的四氢 - 喹啉基脲衍生物及其盐。 本发明的四氢 - 喹啉基脲衍生物具有香草素受体（VR1）拮抗活性，可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗泌尿系统疾病或障碍，例如逼尿肌过度活动 膀胱过度活动），尿失禁，神经源性逼尿肌过度活动（逼尿肌hyperflexia），特发性逼尿肌过度活动（逼尿肌不稳定），良性前列腺增生和下尿路症状; 慢性疼痛，神经性疼痛，术后疼痛，类风湿性关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风和炎性疾病如哮喘和慢性阻塞性肺（或气道）疾病（COPD）。

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