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1. 发明申请

WO2004072020A1 HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES 审中-公开
标题翻译：羟基四氢萘基萘衍生物
公开(公告)号：WO2004072020A1
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001055
申请日：2004-02-05
申请人： BAYER HEALTHCARE AG , YURA, Takeshi , MOGI, Muneto , FUJISHIMA, Hiroshi , URBAHNS, Klaus , MASUDA, Tsutomu , TSUKIMI, Yasuhiro , TAJIMI, Masaomi , YAMAMOTO, Noriyuki , YOSHIDA, Nagahiro , MORIWAKI, Toshiya
发明人： YURA, Takeshi , MOGI, Muneto , FUJISHIMA, Hiroshi , URBAHNS, Klaus , MASUDA, Tsutomu , TSUKIMI, Yasuhiro , TAJIMI, Masaomi , YAMAMOTO, Noriyuki , YOSHIDA, Nagahiro , MORIWAKI, Toshiya
IPC分类号： C07C275/32
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 VRl antagonist and are useful for the prophylaxis and treatment of diseases associated with VRl 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，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。

2. 发明申请

WO2004052845A1 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：WO2004052845A1
公开(公告)日：2004-06-24
申请号：PCT/EP2003/013452
申请日：2003-11-28
申请人： BAYER HEALTHCARE AG , URBAHNS, Klaus , TAJIMI, Masaomi , KOKUBO, Toshio , SHIROO, Masahiro , TSUKIMI, Yasuhiro , YURA, Takeshi , 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 , YAMAMOTO, Noriyuki , MOGI, Muneto , FUJISHIMA, Hiroshi , MASUDA, Tsutomu , YOSHIDA, Nagahiro , MORIWAKI, Toshiya
IPC分类号： C07C275/32
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。

3. 发明申请

WO0244153A8 4-6-DIPHENYL PYRIDINE DERIVATIVES AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译： 4-6-二苯基吡啶衍生物作为抗炎剂
公开(公告)号：WO0244153A8
公开(公告)日：2002-11-28
申请号：PCT/EP0113338
申请日：2001-11-19
申请人： BAYER AG , MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
发明人： MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
IPC分类号： A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5365 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D498/04 , A61K31/44
CPC分类号： C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12
摘要： 4-aryl pyrimidine compounds of general formula and salts thereof:wherein X is CH or N; R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R is hydrogen, halogen, etc.; R is hydrogen, hydroxy, halogen, amino, etc.; R is hydroxy, amino, carboxy, etc. or R and R together form a ring; R is hydrogen, carbamoyl, cyano, carboxy, C1-16 alkoxycarbonyl, etc. and R is amino or C1-16 alkanoylamino or R and R together form a ring. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and act as inhibitors of IKK- beta and thus inhibit nuclear factor kappa B(NF-KB).
摘要翻译：通式为4-芳基嘧啶化合物及其盐：其中X为CH或N; R 1是氢，卤素，C 1-6烷基，C 1-6烷氧基等; R 2是氢，卤素等; R 3是氢，羟基，卤素，氨基等; R 4是羟基，氨基，羧基等，或者R 3和R 4一起形成环; R 5是氢，氨基甲酰基，氰基，羧基，C 1-6烷氧基羰基等，R 6是氨基或C 1-6烷酰基氨基或R 5和R 6一起形成环。化合物（I）或其盐具有优异的抗炎活性，并且作为IKK-β的抑制剂，从而抑制核因子κB（NF-κB）。

4. 发明申请

WO2008032164A3 BENZIMIDAZOLONE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO2008032164A3
公开(公告)日：2009-05-28
申请号：PCT/IB2007002583
申请日：2007-09-03
申请人： PFIZER PROD INC , ANDO KAZUO , BUCHLER INGRID PRICE , HEDGE SHRIDHAR GAJANAN , KAWAI MAKOTO , MASUDA TSUTOMU , OMURA HIROFUMI
发明人： ANDO KAZUO , BUCHLER INGRID PRICE , HEDGE SHRIDHAR GAJANAN , KAWAI MAKOTO , MASUDA TSUTOMU , OMURA HIROFUMI
IPC分类号： C07D235/26 , A61K31/16
CPC分类号： C07D413/06 , A61K31/16 , C07D235/26 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要： This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein. These compounds are useful in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, spasticity, epilepsy, Tourette's syndrome, Parkinson's disease, neuroprotection, anxiety, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, cachexia, nausea, emesis, chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasodialation, hypertension, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及用于治疗哺乳动物受试者（包括人）中由CB1受体活性介导的病症的化合物和方法，其包括向需要这种治疗的哺乳动物施用治疗有效量的式（I）化合物或其药学上可接受的盐，其中：A，B，R 1，R 2和R 3各自如本文所述。这些化合物可用于治疗由CB2受体结合活性介导的病症，例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛，慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，痉挛性，癫痫，Tourette综合征，帕金森病，神经保护，焦虑，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，恶病质，恶心，呕吐，化疗诱发呕吐，类风湿关节炎，哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，胃食管反流病（GERD），便秘功能性胃肠道疾病，皮肤T细胞淋巴瘤，多发性硬化，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑中风，血管扩张，高血压，血管炎，心肌梗死，脑缺血，可逆性气道阻塞，成人呼吸道疾病综合征，慢性阻塞性肺疾病（COPD），隐源性纤维化肺泡炎和支气管炎。

5. 发明申请

WO2008032164A2 BENZIMIDAZOLONE DERIVATIVES 审中-公开
标题翻译：苯并咪唑衍生物
公开(公告)号：WO2008032164A2
公开(公告)日：2008-03-20
申请号：PCT/IB2007/002583
申请日：2007-09-03
申请人： PFIZER PRODUCTS INC. , ANDO, Kazuo , BUCHLER, Ingrid, Price , HEDGE, Shridhar Gajanan , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
发明人： ANDO, Kazuo , BUCHLER, Ingrid, Price , HEDGE, Shridhar Gajanan , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
CPC分类号： C07D413/06 , A61K31/16 , C07D235/26 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D413/14 , C07D471/04
摘要： This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R 1 , R 2 and R 3 are each as described herein. These compounds are useful in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, spasticity, epilepsy, Tourette's syndrome, Parkinson's disease, neuroprotection, anxiety, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, cachexia, nausea, emesis, chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasodialation, hypertension, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis and bronchitis.
摘要翻译：本发明涉及用于治疗哺乳动物受试者（包括人）中由CB1受体活性介导的病症的化合物和方法，其包括向需要这种治疗的哺乳动物施用治疗有效量的式（I）化合物或其药学上可接受的盐，其中：A，B，R 1，R 2和R 3各自如本文所述。这些化合物可用于治疗由CB2受体结合活性介导的病症，例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛，慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，痉挛性，癫痫，Tourette综合征，帕金森病，神经保护，焦虑，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，恶病质，恶心，呕吐，化疗诱发呕吐，类风湿关节炎，哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，胃食管反流病（GERD），便秘功能性胃肠道疾病，皮肤T细胞淋巴瘤，多发性硬化，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病，青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑中风，血管扩张，高血压，血管炎，心肌梗死，脑缺血，可逆性气道阻塞，成人呼吸道疾病综合征，慢性阻塞性肺疾病（COPD），隐源性纤维化肺泡炎和支气管炎。

6. 发明申请

WO2006097808A1 BENZIMIDAZOLONE DERIVATIVES AS CB2 RECEPTOR LIGANDS 审中-公开
标题翻译：苯并咪唑衍生物作为CB2受体配体
公开(公告)号：WO2006097808A1
公开(公告)日：2006-09-21
申请号：PCT/IB2006/000521
申请日：2006-03-02
申请人： PFIZER JAPAN INC. , PFIZER INC. , ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
发明人： ANDO, Kazuo , KAWAI, Makoto , MASUDA, Tsutomu , OMURA, Hirofumi
IPC分类号： C07D235/26 , C07D401/06 , C07D403/12 , C07D413/12 , C07D417/12 , C07D405/06 , C07D471/04 , A61K31/4168 , A61P29/00
CPC分类号： C07D471/04 , C07D235/26 , C07D401/06 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R 1 , R 2 and R 3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：A，B，R 1，R 2和R 3， / SUP>各自如本文所述，并且含有这些化合物的组合物和这些化合物在治疗由CB2受体结合活性介导的病症（例如但不限于炎性疼痛，伤害性疼痛，神经性疼痛，纤维肌痛）慢性腰痛，内脏痛，急性脑缺血，疼痛，慢性疼痛，急性疼痛，疱疹后神经痛，神经病，神经痛，糖尿病性神经病，HIV相关神经病，神经损伤，类风湿性关节炎疼痛，骨关节炎疼痛，背痛，癌症疼痛，牙痛，纤维肌痛，神经炎，坐骨神经痛，炎症，神经变性疾病，咳嗽，支气管收缩，肠易激综合征（IBS），炎性肠病（IBD），结肠炎，脑血管缺血，呕吐如癌症化疗诱发呕吐，类风湿关节炎哮喘，克罗恩病，溃疡性结肠炎，哮喘，皮炎，季节性过敏性鼻炎，胃食管反流病（GERD），便秘，腹泻，功能性胃肠道疾病，皮肤T细胞淋巴瘤，多发性硬化症，骨关节炎，牛皮癣，系统性红斑狼疮，糖尿病青光眼，骨质疏松症，肾小球性肾炎，肾缺血，肾炎，肝炎，脑卒中，血管炎，心肌梗塞，脑缺血，可逆性气道梗阻，成人呼吸道疾病综合征，慢性阻塞性肺病（COPD），隐源性纤维化性肺泡炎或支气管炎。

7. 发明申请

WO2003106402A1 2-NAPHTAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2003106402A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/005705
申请日：2003-05-30
申请人： BAYER AKTIENGESELLSCHAFT , SHIMAZAKI, Makoto , SAKURAI, Osamu , MURATA, Toshiki , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi , MASUDA, Tsutomu , SHINTANI, Takuya , SHIMIZU, Haruka
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
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-萘甲酰胺。本发明的2-萘甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。这些疾病包括尿路疾病或病症如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，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，膀胱高反应性，良性前列腺肥大），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。本发明的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，因为该疾病也通过用IP受体拮抗剂治疗而缓解。

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

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。

10. 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。

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