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1. 发明公开

EP1685112A2 TETRAHYDRO-QUINOLINYLUREA DERIVATIVES 有权
标题翻译：四氢呋喃 - 喹啉类衍生物
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）。

2. 发明公开

EP1677786A1 5-SUBSTITUTED 2-(PHENYLMETHYL)THIO-4-PHENYL-4H-1,2,4-TRIAZOLE DERIVATIVES AND RELATED COMPOUNDS AS GABA-AGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE AND RELATED DISEASES 审中-公开
标题翻译： 5-取代的-2-（苯基甲基）硫基-4-苯基-4H-1,2,4-三唑衍生物和相关化合物作为GABA激动剂尿失禁和相关疾病治疗
公开(公告)号：EP1677786A1
公开(公告)日：2006-07-12
申请号：EP04790125.1
申请日：2004-10-05
申请人： Bayer HealthCare AG
发明人： BAUSER, Marcus , KRÜGER, Joachim , MEIER, Heinrich , VÖHRINGER, Verena , BEYREUTHER, Bettina , MOGI, Muneto , MARUMO, Makiko , TSUNO, Naoki , SHIMIZU, Haruka , FUJISHIMA, Hiroshi , YUASA, Hiroaki , HAYASHI, Mayumi , UMEDA, Masaomi , IWATA, Atsuko
IPC分类号： A61K31/4196 , C07D249/12 , C07D401/04 , A61P13/10
CPC分类号： C07D401/10 , C04B35/632 , C07D249/12 , C07D401/12 , C07D403/10
摘要： This invention relates to phenyltriazole derivatives of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations : (I) wherein R1 represents alkyl optionally substituted or 3-8 membered saturated or unsaturated ring optionally substituted, R2 represents -COR21, -(CH2)n-R21 or tert-butyl, X represents CR10R11, NR12, S, O, SO2, or SO wherein R10, R11 and R12 independently represent hydrogen or methyl. The other substituents are as defined in the claims. The phenyltriazole derivatives of the present invention have an excellent activity as GABAb agonist and are useful for the prophylaxis and treatment of diseases associated with GABAb activity, in particular for the treatment of overactive bladder, urinary incontinence such as urge urinary incontinence, benign prostatic hyperplasia (BPH), chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, or nerve injury.

3. 发明公开

EP1572632A1 TETRAHYDRO-NAPHTHALENE DERIVATIVES AS VANILLOID RECEPTOR ANTAGONISTS 有权
标题翻译：四氢叶酸衍生物
公开(公告)号：EP1572632A1
公开(公告)日：2005-09-14
申请号：EP03780088.5
申请日：2003-11-28
申请人： Bayer HealthCare AG
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 , URBAHNS, Klaus
IPC分类号： C07C275/32 , C07C275/40 , C07D295/12 , C07D207/26 , C07D211/62 , C07D211/22 , C07D211/46 , A61K31/17 , A61K31/395 , A61P13/00 , A61P29/00
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 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。

4. 发明公开

EP1461311A2 UREA DERIVATIVES AS VR1-ANTAGONISTS 审中-公开
标题翻译： HARNSTOFF-DERIVATE ALS VR1-ANTAGONISTEN
公开(公告)号：EP1461311A2
公开(公告)日：2004-09-29
申请号：EP02793004.9
申请日：2002-12-13
申请人： Bayer HealthCare AG
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 , C07C275/26 , C07C275/32 , C07D209/44 , C07D217/06 , C07D223/16 , A61K31/17
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 of the formula (I), its tautomeric or stereoisomeric form, or a salt thereof: (I) wherein Y is R1- R6 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.
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。

5. 发明授权

EP1278750B1 IMIDAZOPYRIMIDINE DERIVATIVES AND TRIAZOLOPYRIMIDINE DERIVATIVES 有权
标题翻译：咪唑并嘧啶衍生物及其衍生物三唑
公开(公告)号：EP1278750B1
公开(公告)日：2004-08-04
申请号：EP01936242.5
申请日：2001-04-17
申请人： Bayer HealthCare AG
发明人： YURA, Takeshi , CONCEPCION, Arnel B. , HAN, Gyoonhee , HIRAOKA, Makiko , KATSUMATA, Hiroko , KAWAMURA, Norihiro , KOKUBO, Toshio , KOMURA, Hiroshi , LI, Yingfu , LOWINGER, Timothy B. , MOGI, Muneto , YAMAMOTO, Noriyuki , YOSHIDA, Nagahiro , Wang. Ming,
IPC分类号： C07D487/04 , A61K31/505 , A61P37/08 , A61P11/06 , A61P35/00 , A61P7/02
CPC分类号： C07D487/04

6. 发明授权

EP1687262B1 BICYCLIC AMIDE, CARBAMATE OR UREA DERIVATIVES AS VANILLOID RECEPTOR MODULATORS 有权
标题翻译：双酚A胺，卡巴胺 - 硬脂酸盐
公开(公告)号：EP1687262B1
公开(公告)日：2008-11-19
申请号：EP04790835.5
申请日：2004-10-26
申请人： Bayer HealthCare AG
发明人： MOGI, Muneto , FUJISHIMA, Hiroshi , TAJIMI, Masaomi , YAMAMOTO, Noriyuki , URBAHNS, Klaus , HAYASHI, Fumihiko , TSUKIMI, Yasuhiro , GUPTA, Jang , YUASA, Hiroaki
IPC分类号： C07C275/32 , C07C235/38 , A61K31/16 , A61K31/17
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，氨基甲酸酯或脲衍生物具有香草素受体（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，神经源性逼尿肌反应性（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）。

7. 发明授权

EP1594836B1 HYDROXY-TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES 有权
标题翻译： HYDROXYTETRAHYDRONAPHTHALENYLHARNSTOFFDERIVATE
公开(公告)号：EP1594836B1
公开(公告)日：2007-09-19
申请号：EP04708355.5
申请日：2004-02-05
申请人： Bayer HealthCare AG
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 , C07D295/08 , A61K31/17 , A61K31/44 , A61P13/00 , A61P25/00
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.

8. 发明公开

EP1740557A1 UREA DERIVATIVES AS ANTAGONISTS OF THE VANILLOID RECEPTOR (VR1) 审中-公开
标题翻译：脲衍生物AS香草素拮抗剂（VR1）
公开(公告)号：EP1740557A1
公开(公告)日：2007-01-10
申请号：EP05716548.2
申请日：2005-04-07
申请人： Bayer HealthCare AG
发明人： FUJISHIMA, Hiroshi , MOGI, Muneto , YUASA, Hiroaki , TAIJIMI, Masaomi , YAMAMOTO, Noriyuki , HAYASHI, Fumihiko , TSUKIMI, Yasuhiro , GUPTA, Jang
IPC分类号： C07D265/36 , C07D215/227 , A61K31/538 , A61P13/02
CPC分类号： C07D265/36 , C07D215/227
摘要： This invention relates to urea derivatives according to general formula I and salts thereof which are useful as active ingredients of pharmaceutical preparations. The urea 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 urological disorder or disease, 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 respiratory diseases and inflammatory disorders such as asthma, chronic obstructive pulmonary (or airways) disease (COPD), common cold, cough, sneeze, bronchitis including acute and chronic bronchitis, bronchiolitis, rhinitis, allergic rhinitis, vasomotor rhinitis, mucositis, sinusitis, allergy, disorders associated with exogenous irritants such as tobacco smoke, smog, high levels of atmospheric SO2 and noxious gases in the workplace, and airways hyperreactivity, milk product intolerance, Loffler's pneumonia, emphysema, cystic fibrosis, bronchiectasis, pulmonary fibrosis, pneumoconiosis, collagen vascular disease, granulomatous disease, laryngitis, pharyngitis, pneumonia, pleuritis, persistent asthma and chronic asthmatic bronchitis. Formula I Wherein n represents 0, 1, 2, 3, or 4; X represents O, CH2, S, or N(R10), Wherein R10 respresents hydrogen or C1-6 alkyl

9. 发明公开

EP1414788A1 NAPHTHYLUREA AND NAPHTHYLACETAMIDE DERIVATIVES AS VANILLOID RECEPTOR 1 (VR1) ANTAGONISTS 审中-公开
标题翻译：萘磺酰胺衍生物 - 硫酸盐 - 硫酸盐 - 抗坏血酸盐（VR1）
公开(公告)号：EP1414788A1
公开(公告)日：2004-05-06
申请号：EP02758413.5
申请日：2002-07-31
申请人： Bayer HealthCare AG
发明人： YURA, Takeshi , MOGI, Muneto , IKEGAMI, Yuka , MASUDA, Tsutomu , KOKUBO, Toshio , URBAHNS, Klaus , LOWINGER, Timothy, B. , YOSHIDA, Nagahiro , FREITAG, Joachim , MEIER, Heinrich , NOPPER, Reilinde , MARUMO, Makiko , SHIROO, Masahiro , TAJIMI, Masaomi , TAKESHITA, Keisuke , MORIWAKI, Toshiya , TSUKIMI, Yasuhiro
IPC分类号： C07C235/38 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/38 , C07C275/40 , C07C275/42 , C07C311/08 , C07C311/47 , C07C323/44 , C07D209/88
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, R6, R7, R8, R8a, R9, R10 and R11 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）拮抗活性的胺衍生物，其互变异构体或立体异构形式或其盐。胺衍生物作为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，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。

10. 发明授权

EP1506167B1 HYDROXY TETRAHYDRO-NAPHTHALENYLUREA DERIVATIVES 有权转让
标题翻译：羟基四氢NAPHTALENYLHARNSTOFF衍
公开(公告)号：EP1506167B1
公开(公告)日：2007-08-29
申请号：EP03722554.7
申请日：2003-04-28
申请人： Bayer HealthCare AG
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 , C07C275/42 , C07C275/40 , A61K31/17 , A61P13/00 , A61P29/00
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.

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