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1. 发明申请

WO2003014064A1 AMINE DERIVATIVES 审中-公开
标题翻译：作为VANILLOID受体1（VR1）拮抗剂的萘甲酰胺和萘磺酰胺衍生物
公开(公告)号：WO2003014064A1
公开(公告)日：2003-02-20
申请号：PCT/EP2002/008493
申请日：2002-07-31
申请人： BAYER AKTIENGESELLSCHAFT , YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutoma , KOKUBO, Toshio , URBAHNS, Klaus , LOWINGER, Timothy, B. , YOSHIDA, Nagahiro , FREITAG, Joachim , MEIER, Heinrich , WITTKA-NOPPER, Reilinde , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
发明人： YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutoma , KOKUBO, Toshio , URBAHNS, Klaus , LOWINGER, Timothy, B. , YOSHIDA, Nagahiro , FREITAG, Joachim , MEIER, Heinrich , WITTKA-NOPPER, Reilinde , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
IPC分类号： C07C235/38
CPC分类号： C07D215/38 , C07C235/38 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/51 , C07C323/42 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D209/88 , C07D235/10 , C07D239/69 , C07D261/14 , C07D261/16 , C07D263/10 , C07D285/06 , C07D295/135 , C07D307/88 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/54
摘要： An amine derivative, its tautomeric or stereoisomeric form, or a salt thereof which has vanilloid receptor 1 (VR1) antagonistic activity, is disclosed. The amine derivative 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 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：公开了具有香草素1（VR1）拮抗剂活性的式（I）的萘基乙酰胺和萘基乙酰胺衍生物，其中Y代表并且变量Q，X，R 6，R 7，R 8a，R 9， R 10和R 11'如权利要求中所定义。该化合物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，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，失禁和/或炎症。

2. 发明申请

WO2004069805A1 BIS(HETERO)ARYL CARBOXAMIDE DERIVATIVES FOR USE AS PGI2 ANTAGONISTS 审中-公开
标题翻译：用作PGI2拮抗剂的BIS（HETERO）ARYL CARBOXAMIDE DERIVATIVES
公开(公告)号：WO2004069805A1
公开(公告)日：2004-08-19
申请号：PCT/EP2004/000711
申请日：2004-01-28
申请人： BAYER HEALTHCARE AG , MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
发明人： MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
IPC分类号： C07D231/14
CPC分类号： C07D207/325 , C07D211/14 , C07D213/64 , C07D213/82 , C07D231/12 , C07D231/14 , C07D239/34 , C07D261/18 , C07D333/38
摘要： The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R 6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 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 relate to PGI2.
摘要翻译：本发明涉及式（I）的芳基或杂芳基酰氨基烷烃衍生物，其中R 6表示羧基或四唑基，其可用作药物制剂的活性成分。本发明的芳基或杂芳基酰氨基烷烃具有PGI 2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。这些疾病包括泌尿系统疾病或病症如下：膀胱出口阻塞，膀胱过度活动症，尿失禁，逼尿肌超反射，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，膀胱过敏反应，前列腺肥大（BPH），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合症，前列腺痛，膀胱炎或自发性膀胱过敏反应。本发明化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压;血友病和出血; 和炎症，因为这些疾病也与PGI2有关。

3. 发明申请

WO2003095420A1 HYDROXY TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES 审中-公开
标题翻译：羟基四氢萘基衍生物
公开(公告)号：WO2003095420A1
公开(公告)日：2003-11-20
申请号：PCT/EP2003/004395
申请日：2003-04-28
申请人： BAYER AKTIENGESELLSCHAFT , YURA, Takeshi , MOGI, Muneto , URBAHNS, Klaus , FUJISHIMA, Hiroshi , MASUDA, Tsutomu , MORIWAKI, Toshiya , YOSHIDA, Nagahiro , KOKUBO, Toshio , SHIROO, Masahiro , TAJIMI, Masaomi , TSUKIMI, Yasuhiro , YAMAMOTO, Noriyuki
发明人： YURA, Takeshi , MOGI, Muneto , URBAHNS, Klaus , FUJISHIMA, Hiroshi , MASUDA, Tsutomu , MORIWAKI, Toshiya , YOSHIDA, Nagahiro , KOKUBO, Toshio , SHIROO, Masahiro , TAJIMI, Masaomi , TSUKIMI, Yasuhiro , YAMAMOTO, Noriyuki
IPC分类号： 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。

4. 发明申请

WO2004052846A1 TETRAHYDRO-NAPHTHALENE DERIVATIVES 审中-公开
标题翻译：四氢萘衍生物
公开(公告)号：WO2004052846A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/013453
申请日：2003-11-28
申请人： BAYER HEALTHCARE AG , TAJIMI, Masaomi , KOKUBO, Toshio , SHIROO, Masahiro , TSUKIMI, Yasuhiro , YURA, Takeshi , URBAHNS, Klaus , YAMAMOTO, Noriyuki , MOGI, Muneto , FUJISHIMA, Hiroshi , MASUDA, Tsutomu , YOSHIDA, Nagahiro , MORIWAKI, Toshiya
发明人： TAJIMI, Masaomi , KOKUBO, Toshio , SHIROO, Masahiro , TSUKIMI, Yasuhiro , YURA, Takeshi , URBAHNS, Klaus , YAMAMOTO, Noriyuki , MOGI, Muneto , FUJISHIMA, Hiroshi , MASUDA, Tsutomu , YOSHIDA, Nagahiro , MORIWAKI, Toshiya
IPC分类号： C07C275/32
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 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 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，急性尿失禁，慢性疼痛，神经性疼痛，手术后疼痛，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，炎症性疾病，哮喘和COPD。

5. 发明申请

WO2003055848A3 UREA DERIVATIVES AS VR1- ANTAGONISTS 审中-公开
公开(公告)号：WO2003055848A3
公开(公告)日：2003-07-10
申请号：PCT/EP2002/014216
申请日：2002-12-13
申请人： BAYER AKTIENGESELLSCHAFT , YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
发明人： YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
IPC分类号： C07C275/24
摘要： This invention relates to urea derivatives of the formula (I), its tautomeric or stereoisomeric form, or a salt thereof: (I) wherein Y is R 1 - R 6 and X have the same meanings given in the description, 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 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.

6. 发明申请

WO2003055484A1 UREA DERIVATIVES 审中-公开
标题翻译：尿素衍生物
公开(公告)号：WO2003055484A1
公开(公告)日：2003-07-10
申请号：PCT/EP2002/014215
申请日：2002-12-13
申请人： BAYER AKTIENGESELLSCHAFT , YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
发明人： YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
IPC分类号： A61K31/428
CPC分类号： C07D333/54 , A61K31/365 , A61K31/404 , A61K31/416 , A61K31/4184 , A61K31/4192 , A61K31/428 , C07D209/08 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/10 , C07D249/18 , C07D277/62 , C07D277/64 , C07D277/72 , C07D277/74 , C07D307/83
摘要： A medicament which contains a urea derivative or a salt thereof as an active ingredient is disclosed. The medicament 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：公开了含有脲衍生物或其盐作为活性成分的药物。该药物作为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。

7. 发明申请

WO2003022277A1 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗炎症和免疫疾病的CCR3拮抗剂的磺酰苯胺衍生物
公开(公告)号：WO2003022277A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009873
申请日：2002-09-04
申请人： BAYER AKTIENGESELLSCHAFT , LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
发明人： LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
IPC分类号： A61K31/445
CPC分类号： C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
摘要： The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
摘要翻译：本发明涉及可用作药物制剂活性成分的磺酰胺衍生物。本发明的磺酰胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，可用于预防和治疗与CCR3活性有关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎症 /免疫学障碍。

8. 发明申请

WO2004052845A8 TETRAHYDRO-NAPHTHALENE DERIVATIVES AS VANILLOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为VANILLOID受体拮抗剂的四氢萘衍生物
公开(公告)号：WO2004052845A8
公开(公告)日：2005-06-09
申请号：PCT/EP0313452
申请日：2003-11-28
申请人： BAYER HEALTHCARE AG , TAJIMI MASAOMI , KOKUBO TOSHIO , SHIROO MASAHIRO , TSUKIMI YASUHIRO , YURA TAKESHI , URBAHNS KLAUS , YAMAMOTO NORIYUKI , MOGI MUNETO , FUJISHIMA HIROSHI , MASUDA TSUTOMU , YOSHIDA NAGAHIRO , MORIWAKI TOSHIYA
发明人： TAJIMI MASAOMI , KOKUBO TOSHIO , SHIROO MASAHIRO , TSUKIMI YASUHIRO , YURA TAKESHI , URBAHNS KLAUS , YAMAMOTO NORIYUKI , MOGI MUNETO , FUJISHIMA HIROSHI , MASUDA TSUTOMU , YOSHIDA NAGAHIRO , MORIWAKI TOSHIYA
IPC分类号： A61K31/17 , A61K31/395 , A61P13/00 , A61P29/00 , C07C275/32 , C07C275/40 , C07D207/26 , C07D207/27 , C07D211/22 , C07D211/46 , C07D211/62 , C07D295/12 , C07D295/135
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 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 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，敦促性尿失禁，膀胱过度活动症，慢性疼痛，神经病变疼痛，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。

9. 发明申请

WO03014064A8 NAPHTHYLUREA AND NAPHTHYLACETAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) ANTAGONISTS 审中-公开
标题翻译：作为VANILLOID受体1（VR1）拮抗剂的萘甲酰胺和萘磺酰胺衍生物
公开(公告)号：WO03014064A8
公开(公告)日：2003-11-27
申请号：PCT/EP0208493
申请日：2002-07-31
申请人： BAYER AG , YURA TAKESHI , MOGI MUNETO , IKEGAMI YUKA , MASUDA TSUTOMA , KOKUBO TOSHIO , URBAHNS KLAUS , LOWINGER TIMOTHY B , YOSHIDA NAGAHIRO , FREITAG JOACHIM , MEIER HEINRICH , WITTKA-NOPPER REILINDE , MARUMO MAKIKO , SHIROO MASAHIRO , TAJIMI MASAOMI , TAKESHITA KEISUKE , MORIWAKI TOSHIYA , TSUKIMI YASUHIRO
发明人： YURA TAKESHI , MOGI MUNETO , IKEGAMI YUKA , MASUDA TSUTOMA , KOKUBO TOSHIO , URBAHNS KLAUS , LOWINGER TIMOTHY B , YOSHIDA NAGAHIRO , FREITAG JOACHIM , MEIER HEINRICH , WITTKA-NOPPER REILINDE , MARUMO MAKIKO , SHIROO MASAHIRO , TAJIMI MASAOMI , TAKESHITA KEISUKE , MORIWAKI TOSHIYA , TSUKIMI YASUHIRO
IPC分类号： C07D295/12 , A61K31/17 , A61K31/18 , A61K31/192 , A61K31/24 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/403 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/433 , A61K31/47 , A61K31/505 , A61K31/5375 , A61P7/12 , A61P9/10 , A61P13/00 , A61P13/10 , A61P25/00 , A61P25/04 , A61P25/28 , A61P29/00 , A61P43/00 , C07C235/38 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/47 , C07C311/51 , C07C323/42 , C07C323/44 , C07D209/88 , C07D215/38 , C07D235/10 , C07D239/69 , C07D261/14 , C07D261/16 , C07D263/10 , C07D285/06 , C07D295/135 , C07D307/88 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/54
CPC分类号： C07D215/38 , C07C235/38 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/51 , C07C323/42 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D209/88 , C07D235/10 , C07D239/69 , C07D261/14 , C07D261/16 , C07D263/10 , C07D285/06 , C07D295/135 , C07D307/88 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/54
摘要： Naphthylurea and naphthylacetamide derivatives of formula (I) which have vanilloid receptor 1 (VR1) antagonistic activity are disclosed, formula (I) wherein Y represents formula (II) and formula (III) and the variables Q, X, R , R , R , R , R , R and R are as defined in the claims. The compounds are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of 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：公开了具有香草素受体1（VR1）拮抗活性的式（I）的萘基乙酰胺和萘基乙酰胺衍生物，式（I）其中Y表示式（II）和式（III），变量Q，X，R 6， R 7，R 8，R 8a，R 9，R 10和R 11如权利要求中所定义。该化合物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，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，痛觉神经痛，神经损伤，局部缺血，神经变性，中风，失禁和/或炎症性疾病。

10. 发明申请

WO2003055848A2 UREA DERIVATIVES 审中-公开
标题翻译：尿素衍生物作为VR1-拮抗剂
公开(公告)号：WO2003055848A2
公开(公告)日：2003-07-10
申请号：PCT/EP2002/014216
申请日：2002-12-13
申请人： BAYER AKTIENGESELLSCHAFT , YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
发明人： YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , YOSHIDA, Nagahiro , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
IPC分类号： C07C275/24
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：本发明涉及式（I）的脲衍生物，其互变异构体或立体异构形式或其盐：（I）其中Y为R 1 -R 6且X具有与本说明书中相同的含义，其可用作活性药物制剂成分。本发明的尿素衍生物作为VR1拮抗剂具有优异的活性，可用于预防和治疗急迫性尿失禁，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，失禁和/或炎症性疾病。

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