公开(公告)号：EP1515941A1

公开(公告)日：2005-03-23

申请号：EP03735507.0

申请日：2003-05-30

申请人： Bayer HealthCare AG

发明人： SHIMAZAKI, Makoto ,  SAKURAI, Osamu ,  MURATA, Toshiki ,  URBAHNS, Klaus ,  YAMAMOTO, Noriyuki ,  YOSHIKAWA, Satoru ,  UMEDA, Masaomi ,  TAJIMI, Masaomi ,  MASUDA, Tsutomu ,  SHINTANI, Takuya ,  SHIMIZU, Haruka

IPC分类号： C07C235/34 ,  C07D209/20 ,  C07D213/55 ,  C07D333/24 ,  A61K31/197 ,  A61K31/405 ,  A61P13/00

CPC分类号： C07C235/66

摘要： 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), 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 disease is also 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2-萘酰胺。 本发明的2-萘酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性有关的疾病。 这些疾病包括泌尿系统疾病或病症如下：膀胱出口梗阻，膀胱过度活动症，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（BPH ），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受体拮抗剂治疗也可以缓解疾病。

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。

公开(公告)号：EP1515942A1

公开(公告)日：2005-03-23

申请号：EP03735608.6

申请日：2003-06-12

申请人： Bayer HealthCare AG

发明人： SHIMAZAKI, Makoto ,  SAKURAI, Osamu ,  HIRAI, Kanako ,  URBAHNS, Klaus ,  YAMAMOTO, Noriyuki ,  YOSHIKAWA, Satoru ,  UMEDA, Masaomi ,  TAJIMI, Masaomi

IPC分类号： C07C235/34 ,  A61K31/197 ,  A61P13/00

CPC分类号： C07C235/34

摘要： The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides 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 are alleviated by treatment with an IP receptor antagonist.