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1. 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。

2. 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。

3. 发明申请

WO2004043926A1 PHENYL OR HETEROARYL AMINO ALKANE DERIVATIVES AS IP RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为IP受体拮抗剂的苯基或异辛烯氨基酸衍生物
公开(公告)号：WO2004043926A1
公开(公告)日：2004-05-27
申请号：PCT/EP2003/011976
申请日：2003-10-29
申请人： BAYER HEALTHCARE AG , MURATA, Toshiki , UMEDA, Masaomi , YOSHIKAWA, Satoru , URBAHNS, Klaus , GUPTA, Jang , SAKURAI, Osamu
发明人： MURATA, Toshiki , UMEDA, Masaomi , YOSHIKAWA, Satoru , URBAHNS, Klaus , GUPTA, Jang , SAKURAI, Osamu
IPC分类号： C07D213/64
CPC分类号： C07D213/64 , C07C229/36 , C07D213/74 , C07D231/38 , C07D239/42 , C07D241/20 , C07D261/14 , C07D277/42 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10
摘要： The present invention relates to a phenyl or heteroaryl amino alkane derivatives which are useful as an active ingredient of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic 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 is 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苯基或杂芳基氨基烷烃衍生物。本发明的苯基或杂芳基氨基烷烃具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。这些疾病包括泌尿系统疾病或紊乱，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，膀胱反应过度，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，因为这些疾病也通过用IP受体拮抗剂治疗而缓解。

4. 发明申请

WO2005039569A1 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）硫代-4-苯基-4H-1,2,4-三唑衍生物及相关化合物作为用于治疗尿失禁和相关疾病的GABA-AGONISTS
公开(公告)号：WO2005039569A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011101
申请日：2004-10-05
申请人： BAYER HEALTHCARE AG , 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
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
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 R 1 represents alkyl optionally substituted or 3-8 membered saturated or unsaturated ring optionally substituted, R 2 represents -COR 21 , -(CH 2 ) n -R 21 or tert-butyl, X represents CR 10 R 11 , NR 12 , S, O, SO 2 , or SO wherein R 10 , R 11 and R 12 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.
摘要翻译：本发明涉及式（I）的苯基三唑衍生物及其盐，其可用作药物制剂的活性成分：（I）其中R 1表示任选取代的烷基或任选取代的3-8元饱和或不饱和环， R 2表示-COR 21， - （CH 2）n R 21或叔丁基，X表示CR 10 R 11，NR 12，S，O，SO 2或SO，其中R R 10和R 12独立地表示氢或甲基。其它取代基如权利要求中所定义。本发明的苯基三唑衍生物作为GABAb激动剂具有优异的活性，并且可用于预防和治疗与GABAb活性相关的疾病，特别是用于治疗膀胱过度活动症，尿失禁例如急迫性尿失禁，良性前列腺增生（ BPH），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，痛觉或神经损伤。

5. 发明申请

WO2003106403A1 CARBOXAMIDES DERIVATIVES 审中-公开
标题翻译：碳氧化物衍生物
公开(公告)号：WO2003106403A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006168
申请日：2003-06-12
申请人： BAYER HEALTHCARE AG , SHIMAZAKI, Makoto , SAKURAI, Osamu , HIRAI, Kanako , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi
发明人： SHIMAZAKI, Makoto , SAKURAI, Osamu , HIRAI, Kanako , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi
IPC分类号： C07C235/34
CPC分类号： C07C235/34
摘要： The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic 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 are 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羧酰胺。本发明的甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗作用相关的疾病。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，膀胱反应过度，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，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏症。本发明的化合物还可用于治疗疼痛，包括但不限于炎症性疼痛，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，因为通过用IP受体拮抗剂治疗来减轻疾病。

6. 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）。

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