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公开(公告)号:US20100137361A1
公开(公告)日:2010-06-03
申请号:US12700417
申请日:2010-02-04
申请人: Axel BOUCHON , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmüller , Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
发明人: Axel BOUCHON , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmüller , Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
CPC分类号: C07D215/38
摘要: 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).
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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公开(公告)号:US07615557B2
公开(公告)日:2009-11-10
申请号:US10574122
申请日:2004-09-22
申请人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi , Hiroaki Yuasa , Jang Gupta , Fumihiko Hayashi
发明人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Yasuhiro Tsukimi , Hiroaki Yuasa , Jang Gupta , Fumihiko Hayashi
IPC分类号: A01N43/40 , A61K31/445 , A61K31/4965 , C07D295/00 , C07D241/04
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.
摘要翻译: 本发明涉及用作药物制剂活性成分的羟基 - 四氢 - 萘或脲衍生物式(I)及其盐,其中A表示式(II)或(III),其中#表示与 分子和Q1a,Q2a,Q3a和Q4a,E表示式(IV)或(V),其中#表示与分子的连接位置,Q1b,Q2b,Q3b,Q4b,Q5b,R1b,na,ma,Xa 和Ra。
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公开(公告)号:US07683076B2
公开(公告)日:2010-03-23
申请号:US10578413
申请日:2004-10-26
申请人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reiβmüller , Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
发明人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reiβmüller , Muneto Mogi , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
IPC分类号: C07D215/38 , A61K31/47
CPC分类号: C07D215/38
摘要: 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).
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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公开(公告)号:US20070167458A1
公开(公告)日:2007-07-19
申请号:US10574122
申请日:2004-09-22
申请人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Hiroaki Yuasa , Jang Gupta , Yasuhiro Tsukimi , Fumihiko Hayashi
发明人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Jean De Vry , Muneto Mogi , Klaus Urbahns , Takeshi Yura , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto , Hiroaki Yuasa , Jang Gupta , Yasuhiro Tsukimi , Fumihiko Hayashi
IPC分类号: A61K31/495 , C07D211/40 , C07D241/04
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.
摘要翻译: 本发明涉及用作药物制剂活性成分的羟基 - 四氢 - 萘或脲衍生物式(I)及其盐,其中A表示式(II)或(III),其中#表示与 分子和Q 1a,Q 2a,Q 3a和Q 4a定义,E表示式(IV )或(V)其中#表示与分子的连接位置和Q 1b,Q 2b,Q 3b,Q 4b α,α,α,α,α,α,α,α,α和R a a都被定义 。
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公开(公告)号:US20070213363A1
公开(公告)日:2007-09-13
申请号:US10578413
申请日:2004-10-26
申请人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Mogi Muneto , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
发明人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pernerstorfer , Elke Reissmuller , Mogi Muneto , Hiroshi Fujishima , Masaomi Tajimi , Noriyuki Yamamoto
IPC分类号: A61K31/47 , C07D215/02
CPC分类号: C07D215/38
摘要: This invention relates to tetrahydro-quinolinylurea derivatives and salts thereof which are useful as active ingredi- ents of pharmaceutical preparations. The tetrahydro-quinolinylurea derivative of the present invention has vanilloid receptor (VR I) C 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 pul- monary (or airways) disease (COPD).
摘要翻译: 本发明涉及四氢喹啉基脲衍生物及其盐,其可用作药物制剂的活性成分。 本发明的四氢 - 喹啉基脲衍生物具有香草素受体(VR I)C拮抗活性,可用于预防和治疗与VR1活性相关的疾病,特别是用于治疗泌尿系统疾病或病症,例如 作为逼尿肌过度活动(膀胱过度活动),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病(或气道)疾病(COPD)。
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公开(公告)号:US20080045546A1
公开(公告)日:2008-02-21
申请号:US10575027
申请日:2004-10-02
申请人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pemerstorfer , Elke Reissmuller , Muneto Mogi , Takeshi Yura , Hiroshi Fujishima , Masanori Seki , Yuji Koriyama , Kayo Yasoshima , Keiko Misawa , Masaomi Tajimi , Noriyuki Yammoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta
发明人: Axel Bouchon , Nicole Diedrichs , Achim Hermann , Klemens Lustig , Heinrich Meier , Josef Pemerstorfer , Elke Reissmuller , Muneto Mogi , Takeshi Yura , Hiroshi Fujishima , Masanori Seki , Yuji Koriyama , Kayo Yasoshima , Keiko Misawa , Masaomi Tajimi , Noriyuki Yammoto , Klaus Urbahns , Fumihiko Hayashi , Yasuhiro Tsukimi , Jang Gupta
IPC分类号: A61K31/519 , A61K31/44 , C07D211/68 , C07D213/06
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 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).
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活性相关的疾病,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,中风和炎性疾病如哮喘和慢性阻塞性肺(或气道)疾病(COPD)。
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公开(公告)号:US08173841B2
公开(公告)日:2012-05-08
申请号:US13052482
申请日:2011-03-21
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 , 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 an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have 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, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative 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四氢萘衍生物及其盐。 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,膀胱过度活动症,急迫性尿失禁,慢性疼痛,神经性疼痛 ,手术后疼痛,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。
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公开(公告)号:US08088826B2
公开(公告)日:2012-01-03
申请号:US12103396
申请日:2008-04-15
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: 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 an active ingredient of pharmaceutical preparations. The tethrahydro—Naphthalene derivatives of the present invention have 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, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative 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,膀胱过度活动症,敦促性尿失禁,慢性疼痛,神经性疼痛 ,手术后疼痛,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。
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公开(公告)号:US20080275047A1
公开(公告)日:2008-11-06
申请号:US12103396
申请日:2008-04-15
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: A61K31/5375 , A61K31/17 , A61P13/00 , A61K31/167
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 an active ingredient of pharmaceutical preparations. The tethrahydro-naphthalene derivatives of the present invention have 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, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative 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四氢萘衍生物及其盐。 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活性有关的疾病,特别是用于治疗尿失禁,膀胱过度活动症,敦促性尿失禁,慢性疼痛,神经性疼痛 ,手术后疼痛,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。
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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。
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