公开(公告)号：EP1685112A2

公开(公告)日：2006-08-02

申请号：EP04790836.3

申请日：2004-10-26

申请人： Bayer HealthCare AG

发明人： BOUCHON, Axel ,  DIEDRICHS, Nicole ,  HERMANN, Achim ,  LUSTIG, Klemens ,  MEIER, Heinrich ,  PERNERSTORFER, Josef ,  REISSMÜLLER, Elke ,  MOGI, Muneto ,  FUJISHIMA, Hiroshi ,  TAJIMI, Masaomi, 1-8-17, Sakuragaoka, Seika-cho ,  YAMAMOTO, Noriyuki

IPC分类号： C07D215/00

CPC分类号： C07D215/38

摘要： This invention relates to tetrahydro quinolinylurea derivatives (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-quinolinylurea ueri votive (J.) of the present invention has vanilloid receptor (VRl) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VRl 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), beniyn proscatic 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四氢喹啉基脲衍生物（Ⅰ）及其盐。 本发明的四氢喹啉基尿酸还原剂（J.）具有类香草素受体（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科疾病或病症， 如逼尿肌过度活动（膀胱活动过度），尿失禁，神经原性逼尿肌过度活动（逼尿肌反射过度），特发性逼尿肌过度活动（逼尿肌不稳定），beniyn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，中风和炎症如哮喘和慢性阻塞性肺（气道）疾病（COPD）。

公开(公告)号：EP1678123A1

公开(公告)日：2006-07-12

申请号：EP04765763.0

申请日：2004-10-02

申请人： Bayer HealthCare AG

发明人： BOUCHON, Axel ,  DIEDRICHS, Nicole ,  HERMANN, Achim ,  LUSTIG, Klemens ,  MEIER, Heinrich ,  PERNERSTORFER, Josef ,  REISSMÜLLER, Elke ,  MOGI, Muneto ,  YURA, Takeshi ,  FUJISHIMA, Hiroshi ,  SEKI, Masanori ,  KORIYAMA, Yuji ,  YASOSHIMA, Kayo ,  MISAWA, Keiko ,  TAJIMI, Masaomi ,  YAMAMOTO, Noriyuki ,  URBAHNS, Klaus ,  HAYASHI, Fumihiko ,  TSUKIMI, Yasuhiro ,  GUPTA, Jang

IPC分类号： C07C275/32 ,  C07C275/38 ,  C07C275/30 ,  C07D317/66 ,  C07D261/14 ,  C07D213/40 ,  C07D213/89 ,  C07D285/06 ,  C07D209/18 ,  C07C235/56 ,  C07C233/56 ,  C07C233/75 ,  C07C237/04 ,  C07C235/16

CPC分类号： C07C275/32 ,  A61K31/167 ,  A61K31/17 ,  A61K31/357 ,  A61K31/42 ,  A61K31/433 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/455 ,  A61K31/4706 ,  A61K31/472 ,  A61K31/517 ,  A61K47/54 ,  C07C233/29 ,  C07C233/75 ,  C07C235/24 ,  C07C235/38 ,  C07C235/56 ,  C07C235/64 ,  C07C237/04 ,  C07C275/30 ,  C07C275/38 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/18 ,  C07D213/40 ,  C07D213/56 ,  C07D213/89 ,  C07D215/46 ,  C07D217/22 ,  C07D239/94 ,  C07D261/14 ,  C07D285/06 ,  C07D317/66

摘要： This invention relates to tetrahydro-naphthalene and urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene and urea derivatives of the present invention have 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). BHC 03 2 001-Foreign-Countries - 66 - BHC 03 2 001-Foreign-Countries - 65 -

摘要翻译： 本发明涉及四氢萘和脲衍生物及其盐，其可用作药物制剂的活性成分。 本发明的四氢萘和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病症，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，中风和炎症性疾病如哮喘和慢性阻塞性肺部（或气道）疾病（COPD）。

公开(公告)号：EP1670761A1

公开(公告)日：2006-06-21

申请号：EP04765478.5

申请日：2004-09-22

申请人： Bayer HealthCare AG

发明人： BOUCHON, Axel ,  DIEDRICHS, Nicole ,  HERMANN, Achim ,  LUSTIG, Klemens ,  MEIER, Heinrich ,  PERNERSTORFER, Josef ,  REISSMÜLLER, Elke ,  DE VRY, Jean ,  MOGI, Muneto ,  URBAHNS, Klaus ,  YURA, Takeshi ,  FUJISHIMA, Hiroshi ,  TAJIMI, Masaomi ,  YAMAMOTO, Noriyuki ,  YUASA, Hiroaki ,  GUPTA, Jang ,  TSUKIMI, Yasuhiro ,  HAYASHI, Fumihiko

IPC分类号： C07D211/62 ,  C07D401/04 ,  C07D295/215 ,  A61K31/445 ,  A61K31/506 ,  A61K31/495 ,  A61K31/496 ,  A61P13/00 ,  A61P29/00

CPC分类号： C07D295/215 ,  C07D211/62 ,  C07D401/04

摘要： This invention relates to a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q1a, Q2a, Q3a and Q4a are defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q1b, Q2b, Q3b, Q4b, Q5b, R1b, na, ma, Xa and Ra are defined.