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1. 发明申请

WO2012038850A1 PYRIDMIDONES FOR TREATMENT OF POTASSIUM CHANNEL RELATED DISEASES 审中-公开
标题翻译：用于治疗钾通道相关疾病的吡虫啉
公开(公告)号：WO2012038850A1
公开(公告)日：2012-03-29
申请号：PCT/IB2011/053917
申请日：2011-09-07
申请人： PFIZER INC. , SAKURADA, Isao , ZHANG, Lei
发明人： SAKURADA, Isao , ZHANG, Lei
IPC分类号： C07D471/04 , A61K31/519 , A61P25/00 , A61P29/00
CPC分类号： C07D471/04 , A61K31/519 , A61K45/06
摘要： The present invention relates to compounds of Formula I as described herein or a 1 pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogenital disorders, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
摘要翻译：本发明涉及本文所述的式I化合物或其药学上可接受的盐，包含式I化合物或其药学上可接受的盐的药物组合物和治疗或制备治疗疾病，其中包括双相情感障碍，抑郁障碍，焦虑障碍，认知障碍，疼痛障碍，泌尿生殖系统疾病和癫痫等中枢神经系统的疾病，病症或状况在本文中所讨论的其他疾病，病症或病症中作为单一治疗或与另一种活性药物成分。

2. 发明申请

WO2006090224A1 BENZISOXAZOLE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：WO2006090224A1
公开(公告)日：2006-08-31
申请号：PCT/IB2006/000313
申请日：2006-02-15
申请人： PFIZER JAPAN INC. , PFIZER INC. , NOGUCHI, Hirohide , SAKURADA, Isao , UCHIDA, Chikara , WAIZUMI, Nobuaki
发明人： NOGUCHI, Hirohide , SAKURADA, Isao , UCHIDA, Chikara , WAIZUMI, Nobuaki
IPC分类号： C07D413/12 , C07D413/14 , A61K31/454 , A61P9/00 , A61P25/00 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14
摘要： This invention relates to compounds of the formula (I): wherein A, B, R 1 , R 4 , m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT 4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）化合物：其中A，B，R 1，R 4，m和n各自如本文所述，或药学上可接受的其盐和含有这些化合物的组合物以及这些化合物在治疗5-HT 4受体活性介导的病症中的用途，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢10神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病如心力衰竭和心律失常，糖尿病和呼吸暂停综合征。

3. 发明申请

WO2005080317A2 THERAPEUTIC AMIDE DERIVATIVES 审中-公开
标题翻译：治疗酰胺衍生物
公开(公告)号：WO2005080317A2
公开(公告)日：2005-09-01
申请号：PCT/IB2005/000258
申请日：2005-02-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
发明人： KAWAI, Makoto , KAWAMURA, Mitsuhiro , SAKURADA, Isao , MORITA, Asato
IPC分类号： C07C235/00
CPC分类号： C07C235/48 , C07C2601/14 , C07D207/34 , C07D209/34 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/227 , C07D215/48 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/26 , C07D237/04 , C07D237/24 , C07D249/04 , C07D263/38 , C07D277/68 , C07D303/22 , C07D309/06 , C07D317/72 , C07D401/12 , C07D405/06 , C07D405/12
摘要： The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: A and B independently represent CH 2 or O, with the proviso that A and B are not simultaneously O; Cy represents one of the following Formula (II) optionally substituted by one to three groups selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, C 1-6 alkylamino and amino; R 1 and R 2 are independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl and C 3-8 cycloalkyl; n represents an integer from 0-4; X is hydrogen, hydroxy, halogen or C 1-6 alkoxy; Y is oxy, thio, a 1-4 membered alkylene, a 2-4 membered alkylene ether, 2-4 membered alkylene thioether or an oxyethyleneoxy group, optionally substituted by 1 to 4 groups independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy and C 1-6 haloalkyl; Z is CH or N; and p represents an integer from 0-5 when Z is CH or 0-4 when Z is N; when p represents 2 or more, two of R 2 s may be taken together with the carbon atoms to which they are attached to form a 5-8 membered cycloalkyl ring to processes for the preparation of, intermediates used in the preparation of, compositions containing such compounds and the uses of such compounds as antagonists of the NMDA NR2B receptor.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：A和B独立地表示CH 2或O，条件是A和B不同时为O; Cy表示任选被一至三个选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6烷基氨基和氨基的基团取代的下式（II）之一。 R 1和R 2独立地选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基和C 3-8环烷基; n表示0-4的整数; X是氢，羟基，卤素或C 1-6烷氧基; Y是氧基，硫代，1-4元亚烷基，2-4元亚烷基醚，2-4元亚烷基硫醚或氧化乙烯氧基，任选被1至4个独立地选自羟基，卤素，C 1-6烷基， C 1-6烷氧基和C 1-6卤代烷基; Z是CH或N; 当Z为CH时，p表示0-5的整数，Z为N时为0〜4的整数。当p表示2或更多时，R 2中的两个可以与它们所连接的碳原子一起形成5-8元环烷基环，以制备用于制备中间体的中间体，含有这些化合物的组合物以及这些化合物作为NMDA NR2B受体的拮抗剂的用途。

4. 发明申请

WO2007125398A3 : SULFONAMIDE COMPOUNDS AS ANTAGONISTS OF THE N-TYPE CALCIUM CHANNEL 审中-公开
公开(公告)号：WO2007125398A3
公开(公告)日：2007-11-08
申请号：PCT/IB2007/001084
申请日：2007-04-17
申请人： PFIZER JAPAN INC. , PFIZER INC. , INOUE, Tadashi , NOGUCHI, Hirohide , SAKURADA, Isao , TATSUTA, Miyuki
发明人： INOUE, Tadashi , NOGUCHI, Hirohide , SAKURADA, Isao , TATSUTA, Miyuki
IPC分类号： C07D265/30 , C07D265/34 , C07D413/04 , C07D413/14 , A61K31/5377 , A61K31/538 , A61K31/4545 , A61P25/00
摘要： This invention provides the compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein Q is CH 2 or the like; Z 1 is CR a or the like; Z 2 is CR b or the like; R 1 and R 2 are each independently hydrogen or the like, R a , R b , R 3 , R 4 and R 5 are each independently hydrogen or the like and n is 1 or the like. These compounds are useful for the treatment of disease conditions caused by overactivation of N type calcium channel such as pain or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

5. 发明申请

WO2004089366A1 BICYCLIC COMPOUNDS AS NR2B RECEPTOR ANTAGONISTS 审中-公开
标题翻译：双环化合物作为NR2B受体拮抗剂
公开(公告)号：WO2004089366A1
公开(公告)日：2004-10-21
申请号：PCT/IB2004/001177
申请日：2004-04-01
申请人： PFIZER JAPAN, INC. , PFIZER INC. , ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
发明人： ANDO, Kazuo , KAWAI, Makoto , KAWAMURA, Mitsuhiro , MATSUMIZU, Miyako , MORITA, Asato , SAKURADA, Isao
IPC分类号： A61K31/4184
CPC分类号： C07D239/94 , C07D209/08 , C07D215/12 , C07D215/26 , C07D231/56 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/26 , C07D261/20 , C07D263/56 , C07D471/04
摘要： This invention provides a compound of the formula (I) wherein R 1 and R 2 independently represent a hydrogen atom or the like; X represents a covalent bond or the like: A represents a bicyclic, aromatic, saturated or partially unsaturated heterocyclic or carbocyclic group having from 8 to 12 ring atoms; or the like: B represents a phenyl group or a heteroaryl group having from 5 to 6 ring atoms or the like: These compounds are useful for the treatment of disease conditions caused by overactivation of NMDA NR2B receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物，其中R 1和R 2独立地表示氢原子等; X表示共价键或类似物：A表示具有8至12个环原子的双环，芳族，饱和或部分不饱和的杂环或碳环基团; B表示苯基或具有5〜6个环原子的杂芳基等：这些化合物可用于治疗NMDA NR2B受体过度活化引起的疾病状况，例如哺乳动物的疼痛等。本发明还提供了包含上述化合物的药物组合物。

6. 发明申请

WO2015160636A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2015160636A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/025229
申请日：2015-04-10
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
发明人： SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC分类号： C07D413/14 , C07D261/20 , C07D207/02
CPC分类号： C07D413/14 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/52 , A61K45/06 , C07D413/04 , C07D417/14 , C07D471/04 , C07D498/04 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：在其许多实施方案中，本发明提供了一类新的由式（I）表示的苯甲酰胺化合物或其药学上可接受的盐或溶剂合物，或包含一种或多种所述化合物或药学上可接受的盐或其溶剂化物，以及使用所述化合物或其药学上可接受的盐或溶剂合物治疗或预防血栓形成，栓塞，高凝血性或纤维变性的方法。

7. 发明申请

WO2015160634A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2015160634A1
公开(公告)日：2015-10-22
申请号：PCT/US2015/025219
申请日：2015-04-10
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
发明人： SAKURADA, Isao , HIRABAYASHI, Tomokazu , MAEDA, Yoshitaka , NAGASUE, Hiroshi , MIZUNO, Takashi , XU, Jiayi , ZHANG, Ting , SMITH, Cameron , PARKER, Dann
IPC分类号： C07D413/14 , C07D261/20 , C07D207/02
CPC分类号： A61K31/439 , A61K31/444 , A61K31/501 , A61K31/506 , A61K45/06 , C07D209/52 , C07D261/20 , C07D413/04 , C07D413/14 , C07D498/04 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
摘要翻译：在其许多实施方案中，本发明提供了由式（I）表示的新一类苯甲酰胺化合物或其药学上可接受的盐或溶剂化物，或包含一种或多种所述化合物或其药学上可接受的盐或溶剂化物的药物组合物，以及使用所述化合物或其药学上可接受的盐或溶剂合物用于治疗或预防血栓形成，栓塞，高凝状态或纤维变性。

8. 发明申请

WO2016094260A1 FACTOR IXA INHIBITORS 审中-公开
标题翻译：因子IXA抑制剂
公开(公告)号：WO2016094260A1
公开(公告)日：2016-06-16
申请号：PCT/US2015/064176
申请日：2015-12-07
申请人： MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD. , ZHANG, Ting , CHEN, Yi-Heng , GUO, Liangqin , HRUZA, Alan , JIAN, Tianying , LI, Bing , MENG, Dongfang , PARKER, Dann, L., Jr. , SHERER, Edward, C. , WOOD, Harold, B. , SAKURADA, Isao
发明人： ZHANG, Ting , CHEN, Yi-Heng , GUO, Liangqin , HRUZA, Alan , JIAN, Tianying , LI, Bing , MENG, Dongfang , PARKER, Dann, L., Jr. , SHERER, Edward, C. , WOOD, Harold, B. , SAKURADA, Isao
IPC分类号： A61K31/4184 , C07D235/04
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
摘要翻译：本发明提供式I化合物和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防不稳定型心绞痛，难治性心绞痛，心肌梗死，短暂性脑缺血发作，心房颤动，血栓性中风，栓塞的方法中风，深静脉血栓形成，弥散性血管内凝血，纤维蛋白眼睛积聚，以及再通血管的再闭塞或再狭窄。该化合物是选择性因子IXa抑制剂。

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