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    PHENYL OR HETEROARYL AMINO ALKANE DERIVATIVES AS IP RECEPTOR ANTAGONIST
    1.
    发明公开
    PHENYL OR HETEROARYL AMINO ALKANE DERIVATIVES AS IP RECEPTOR ANTAGONIST 审中-公开
    苯基或杂芳基氨基烷烃衍生物作为IP受体拮抗剂

    公开(公告)号：EP1575919A1

    公开(公告)日：2005-09-21

    申请号：EP03810952.6

    申请日：2003-10-29

    申请人： Bayer HealthCare AG

    发明人： MURATA, Toshiki ,  UMEDA, Masaomi ,  YOSHIKAWA, Satoru ,  URBAHNS, Klaus ,  GUPTA, Jang ,  SAKURAI, Osamu,11-15, Koaza-Hiroshiki

    IPC分类号： C07D213/64 ,  C07D213/74 ,  C07D213/38 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D277/42 ,  C07D401/12 ,  C07D401/10 ,  C07D403/12 ,  C07D403/10 ,  C07D401/04 ,  C07D401/14 ,  C07D405/10 ,  A61K31/415

    CPC分类号： C07D213/64 ,  C07C229/36 ,  C07D213/74 ,  C07D231/38 ,  C07D239/42 ,  C07D241/20 ,  C07D261/14 ,  C07D277/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10

    摘要： The present invention relates to a phenyl or heteroaryl amino alkane derivatives which are useful as an active ingredient of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic 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, benighn prostatic hypertrophy (BPH), prostatitis, 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 diseases also is alleviated by treatment with an IP receptor antagonist.

    摘要翻译： 本发明涉及可用作药物制剂活性成分的苯基或杂芳基氨基烷烃衍生物。 本发明的苯基或杂芳基氨基烷烃具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。 这些疾病包括泌尿系统疾病或病症如下：膀胱出口梗阻，膀胱过动症，尿失禁，逼尿肌反射亢进，逼尿肌不稳定，膀胱容量减少，排尿次数，急迫性尿失禁，压力性尿失禁，膀胱高反应性，前列腺肥大 ），前列腺炎，尿频，夜尿，尿急，骨盆过敏症，尿道炎，骨盆疼痛综合征，前列腺痛，膀胱炎或特发性膀胱过敏症。 本发明化合物还可用于治疗疼痛，包括但不限于炎症性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙齿疼痛，经前期疼痛，内脏疼痛，头痛等; 低血压; 血友病和出血; 和炎症，因为通过用IP受体拮抗剂治疗也能减轻疾病。

    BICYCLIC AMIDE, CARBAMATE OR UREA DERIVATIVES AS VANILLOID RECEPTOR MODULATORS
    2.
    发明授权
    BICYCLIC AMIDE, CARBAMATE OR UREA DERIVATIVES AS VANILLOID RECEPTOR MODULATORS 有权
    双酚A胺，卡巴胺 - 硬脂酸盐

    公开(公告)号：EP1687262B1

    公开(公告)日：2008-11-19

    申请号：EP04790835.5

    申请日：2004-10-26

    申请人： Bayer HealthCare AG

    发明人： MOGI, Muneto ,  FUJISHIMA, Hiroshi ,  TAJIMI, Masaomi ,  YAMAMOTO, Noriyuki ,  URBAHNS, Klaus ,  HAYASHI, Fumihiko ,  TSUKIMI, Yasuhiro ,  GUPTA, Jang ,  YUASA, Hiroaki

    IPC分类号： C07C275/32 ,  C07C235/38 ,  A61K31/16 ,  A61K31/17

    CPC分类号： C07D295/155 ,  C07C235/38 ,  C07C275/32 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10

    摘要： This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea 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 oeractivity (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).

    摘要翻译： 本发明涉及可用作药物制剂活性成分的双环酰胺，氨基甲酸酯或脲衍生物及其盐。 本发明的双环酰胺，氨基甲酸酯或脲衍生物具有香草素受体（VR1）拮抗活性，并且可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗泌尿系统疾病或病症，例如 逼尿肌过度活动症（膀胱过度活动症），尿失禁，神经源性逼尿肌反应性（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，中风和炎症性疾病如哮喘和慢性阻塞性肺部（或气道）疾病（COPD）。

    UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1)
    3.
    发明公开
    UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1) 审中-公开
    脲衍生物AS香草素拮抗剂（VR1）

    公开(公告)号：EP1740557A1

    公开(公告)日：2007-01-10

    申请号：EP05716548.2

    申请日：2005-04-07

    申请人： Bayer HealthCare AG

    发明人： FUJISHIMA, Hiroshi ,  MOGI, Muneto ,  YUASA, Hiroaki ,  TAIJIMI, Masaomi ,  YAMAMOTO, Noriyuki ,  HAYASHI, Fumihiko ,  TSUKIMI, Yasuhiro ,  GUPTA, Jang

    IPC分类号： C07D265/36 ,  C07D215/227 ,  A61K31/538 ,  A61P13/02

    CPC分类号： C07D265/36 ,  C07D215/227

    摘要： This invention relates to urea derivatives according to general formula I and salts thereof which are useful as active ingredients of pharmaceutical preparations. The urea derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological disorder or disease, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (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 respiratory diseases and inflammatory disorders such as asthma, chronic obstructive pulmonary (or airways) disease (COPD), common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis. Formula I Wherein n represents 0, 1, 2, 3, or 4; X represents O, CH2, S, or N(R10), Wherein R10 respresents hydrogen or C1-6 alkyl

    USE OF HYDROXY TETRAHYDRO-NAPHTHALENE DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES
    4.
    发明公开
    USE OF HYDROXY TETRAHYDRO-NAPHTHALENE DERIVATIVES FOR THE TREATMENT OF RESPIRATORY DISEASES 审中-公开
    HYDROXYTETRAHYDRONAPHTHALINDERIVATEN的呼吸系统疾病治疗中的应用

    公开(公告)号：EP1893189A2

    公开(公告)日：2008-03-05

    申请号：EP06707142.3

    申请日：2006-02-22

    申请人： Bayer HealthCare AG

    发明人： ALONSO-ALIJA, Cristina ,  GUPTA, Jang ,  HINZEN, Berthold

    IPC分类号： A61K31/17 ,  A61P11/00

    CPC分类号： A61K31/17

    摘要： This invention relates to new uses of hydroxy-tetrahydro-naphthalenylurea derivatives which are described in WO 03/095420 as an active ingredient of pharmaceutical preparations for the treatment of diseases associated with VR1 activity. The new uses of the present invention are the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of respiratory diseases or disorders such as the common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis.