公开(公告)号：US07612113B2

公开(公告)日：2009-11-03

申请号：US10513848

申请日：2003-04-28

申请人： Takeshi Yura ,  Muneto Mogi ,  Klaus Urbahns ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Toshiya Moriwaki ,  Nagahiro Yoshida ,  Toshio Kokubo ,  Masahiro Shiroo ,  Masaomi Tajimi ,  Yasuhiro Tsukimi ,  Noriyuki Yamamoto

发明人： Takeshi Yura ,  Muneto Mogi ,  Klaus Urbahns ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Toshiya Moriwaki ,  Nagahiro Yoshida ,  Toshio Kokubo ,  Masahiro Shiroo ,  Masaomi Tajimi ,  Yasuhiro Tsukimi ,  Noriyuki Yamamoto

IPC分类号： A61K31/17 ,  C07C275/30 ,  C07C275/32

CPC分类号： C07C275/42 ,  C07C275/32 ,  C07C275/40

摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence, inflammatory disorders such as asthma and COPD.

摘要翻译： 本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。 本发明的四氢萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急性尿失禁，膀胱过度活动症，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，失禁，炎症性疾病如哮喘和COPD。

公开(公告)号：US20090209514A1

公开(公告)日：2009-08-20

申请号：US12432600

申请日：2009-04-29

申请人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： A61K31/55 ,  A61K31/4453 ,  A61K31/5375 ,  A61P13/00

CPC分类号： C07C275/32 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D295/135

摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydronaphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

摘要翻译： 本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。 本发明的四氢萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，敦促尿失禁，膀胱过度活动症，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，炎症性疾病，哮喘和COPD。

公开(公告)号：US20060128704A1

公开(公告)日：2006-06-15

申请号：US10537482

申请日：2003-11-28

申请人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： A61K31/537 ,  A61K31/277 ,  A61K31/165 ,  A61K31/17

CPC分类号： C07D295/088 ,  C07C233/29 ,  C07C233/75 ,  C07C235/42 ,  C07C237/40 ,  C07C275/32 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C317/32 ,  C07C323/44 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D295/135

摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. They have the general formula (I) in which R1 represents hydrogen or C1-6 alkyl, and X represents —N(H)Y1, —N(H)—C1-6 alkylene Y1, biphenyl or C1-6 alkyl substituted by biphenyl, and the group Y1 is an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have 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 urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

摘要翻译： 本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。 它们具有其中R 1表示氢或C 1-6烷基的通式（I），X表示-N（H）Y 1， -O（H）-C 1-6亚烷基Y 1，被联苯取代的联苯基或C 1-6烷基，和 基团Y 1是任选取代的联苯。 本发明的四氢 - 萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，急迫性尿失禁，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，炎性疾病，哮喘和COPD。

公开(公告)号：US07423175B2

公开(公告)日：2008-09-09

申请号：US10545556

申请日：2004-02-05

申请人： Takeshi Yura ,  Muneto Mogi ,  Hiroshi Fujishima ,  Klaus Urbahns ,  Tsutomu Masuda ,  Yasuhiro Tsukimi ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Takeshi Yura ,  Muneto Mogi ,  Hiroshi Fujishima ,  Klaus Urbahns ,  Tsutomu Masuda ,  Yasuhiro Tsukimi ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： C07C275/32 ,  A61K31/17

CPC分类号： C07D295/096 ,  C07C275/32 ,  C07C2602/10

摘要： This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

摘要翻译： 本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。 本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性 疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

公开(公告)号：US20080058377A1

公开(公告)日：2008-03-06

申请号：US10578490

申请日：2004-10-26

申请人： Muneto Mogi ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Klaus Urbahns ,  Fumihiko Hayashi ,  Yasuhiro Tsukimi ,  Jang Gupta ,  Hiroaki Yuasa

发明人： Muneto Mogi ,  Hiroshi Fujishima ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Klaus Urbahns ,  Fumihiko Hayashi ,  Yasuhiro Tsukimi ,  Jang Gupta ,  Hiroaki Yuasa

IPC分类号： A61K31/445 ,  A61K31/16 ,  A61K31/17 ,  A61P29/00 ,  C07C275/28 ,  C07C233/00 ,  A61P13/00 ,  A61K31/195

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，氨基甲酸酯或尿素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，例如 逼尿肌过度活动症（膀胱过度活动症），尿失禁，神经源性逼尿肌过敏反应（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）。

公开(公告)号：US20060135505A1

公开(公告)日：2006-06-22

申请号：US10537217

申请日：2003-11-28

申请人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： A61K31/445 ,  A61K31/40 ,  A61K31/397 ,  A61K31/17

CPC分类号： C07C275/32 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D295/135

摘要： This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene 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 urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.

公开(公告)号：US07544716B2

公开(公告)日：2009-06-09

申请号：US10537217

申请日：2003-11-28

申请人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： A61K31/17

CPC分类号： C07C275/32 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D295/135

摘要： This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene 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 urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.

摘要翻译： 本发明涉及式（I）的四氢 - 萘衍生物，其中可变基团如说明书和权利要求中所定义，以及其可用作药物制剂活性成分的互变异构体和立体异构形式及其盐。 本发明的四氢 - 萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，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，炎症性疾病，哮喘和COPD。 公开并要求保护所述化合物，含有它们的药物组合物和使用它们的治疗方法。

公开(公告)号：US07381840B2

公开(公告)日：2008-06-03

申请号：US10537482

申请日：2003-11-28

申请人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Masaomi Tajimi ,  Toshio Kokubo ,  Masahiro Shiroo ,  Yasuhiro Tsukimi ,  Takeshi Yura ,  Klaus Urbahns ,  Noriyuki Yamamoto ,  Muneto Mogi ,  Hiroshi Fujishima ,  Tsutomu Masuda ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： C07C273/00

CPC分类号： C07D295/088 ,  C07C233/29 ,  C07C233/75 ,  C07C235/42 ,  C07C237/40 ,  C07C275/32 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C317/32 ,  C07C323/44 ,  C07C2602/10 ,  C07D207/27 ,  C07D211/22 ,  C07D211/46 ,  C07D211/62 ,  C07D295/135

摘要： This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. They have the general formula (I) in which R1 represents hydrogen or C1-6 alkyl, and X represents —N(H)Y1, —(H)—C1-6 alkyleneY1, biphenyl or C1-6 alkyl substituted by biphenyl, and the group Y1 is an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have 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 urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

摘要翻译： 本发明涉及四氢萘衍生物及其盐，其可用作药物制剂的活性成分。 它们具有其中R 1表示氢或C 1-6烷基的通式（I），X表示-N（H）Y 1， ， - （H）-C 1-6亚烷基，由联苯取代的联苯基或C 1-6烷基，以及基团 Y 1是任选取代的联苯。 本发明的四氢 - 萘衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁，膀胱过度活动症，急迫性尿失禁，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，炎性疾病，哮喘和COPD。

公开(公告)号：US20070027187A1

公开(公告)日：2007-02-01

申请号：US10545556

申请日：2004-02-05

申请人： Takeshi Yura ,  Muneto Mogi ,  Hiroshi Fujishima ,  Klaus Urbahns ,  Tsutomu Masuda ,  Yasuhiro Tsukimi ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Nagahiro Yoshida ,  Toshiya Moriwaki

发明人： Takeshi Yura ,  Muneto Mogi ,  Hiroshi Fujishima ,  Klaus Urbahns ,  Tsutomu Masuda ,  Yasuhiro Tsukimi ,  Masaomi Tajimi ,  Noriyuki Yamamoto ,  Nagahiro Yoshida ,  Toshiya Moriwaki

IPC分类号： A61K31/445 ,  A61K31/277 ,  A61K31/195 ,  A61K31/17

CPC分类号： C07D295/096 ,  C07C275/32 ,  C07C2602/10

摘要： This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

摘要翻译： 本发明涉及可用作药物制剂活性成分的羟基 - 四氢 - 萘基脲衍生物及其盐。 本发明的羟基 - 四氢 - 萘基脲衍生物作为VR1拮抗剂具有优异的活性，并且可用于预防和治疗与VR1活性有关的疾病，特别是用于治疗尿失禁，敦促性尿失禁，膀胱过度活动症，慢性 疼痛，神经性疼痛，术后疼痛，类风湿关节炎疼痛，神经痛，神经病，痛觉，神经损伤，局部缺血，神经变性，中风，炎性疾病，哮喘和COPD。

公开(公告)号：US20050154230A1

公开(公告)日：2005-07-14

申请号：US10499785

申请日：2002-12-13

申请人： Takeshi Yura ,  Muneto Mogi ,  Yuka Ikegami ,  Tsutomu Masuda ,  Toshio Kokubo ,  Klaus Urbahns ,  Nagahiro Yoshida ,  Makiko Marumo ,  Masahiro Shiroo ,  Masaomi Tajimi ,  Keisuke Takeshita ,  Toshiya Moriwaki ,  Yasuhiro Tsukimi

发明人： Takeshi Yura ,  Muneto Mogi ,  Yuka Ikegami ,  Tsutomu Masuda ,  Toshio Kokubo ,  Klaus Urbahns ,  Nagahiro Yoshida ,  Makiko Marumo ,  Masahiro Shiroo ,  Masaomi Tajimi ,  Keisuke Takeshita ,  Toshiya Moriwaki ,  Yasuhiro Tsukimi

IPC分类号： C07D295/12 ,  A61K31/167 ,  A61K31/17 ,  A61K31/216 ,  A61K31/277 ,  A61K31/341 ,  A61K31/36 ,  A61K31/381 ,  A61K31/403 ,  A61K31/416 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/472 ,  A61K31/496 ,  A61P9/10 ,  A61P13/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P29/00 ,  A61P29/02 ,  A61P43/00 ,  C07C275/10 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/32 ,  C07C275/34 ,  C07C275/36 ,  C07C275/38 ,  C07C275/40 ,  C07C275/42 ,  C07C323/33 ,  C07C323/43 ,  C07D209/88 ,  C07D213/40 ,  C07D213/75 ,  C07D215/38 ,  C07D217/06 ,  C07D231/56 ,  C07D295/135 ,  C07D307/52 ,  C07D317/06 ,  C07D317/58 ,  C07D317/66 ,  C07D333/20 ,  C07D333/36

CPC分类号： C07D333/36 ,  C07C275/24 ,  C07C275/28 ,  C07C275/30 ,  C07C275/32 ,  C07C275/40 ,  C07C275/42 ,  C07C323/43 ,  C07C2602/10 ,  C07C2603/18 ,  C07D209/88 ,  C07D213/40 ,  C07D213/75 ,  C07D217/06 ,  C07D231/56 ,  C07D295/135 ,  C07D307/52 ,  C07D317/06 ,  C07D317/58 ,  C07D333/20

摘要： This invention relates to urea derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The urea derivatives of the present invention has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

摘要翻译： 本发明涉及尿素衍生物及其盐，其可用作药物制剂的活性成分。 本发明的脲衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗与VR1活性相关的疾病，特别是用于治疗急性尿失禁，膀胱过度活动症，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，酸痛，神经损伤，局部缺血，神经变性，中风，失禁和/或炎症性疾病。