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71. 发明授权

US07910590B2 Cyclic amine bace-1 inhibitors having a heterocyclic substituent 有权
标题翻译：具有杂环取代基的环胺类bace-1抑制剂
公开(公告)号：US07910590B2
公开(公告)日：2011-03-22
申请号：US12490884
申请日：2009-06-24
申请人： Ying Huang , Guoqing Li , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Jianping Pan
发明人： Ying Huang , Guoqing Li , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Jianping Pan
IPC分类号： A61K31/496 , A61K31/506
CPC分类号： C04B35/632 , C07D207/277 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R 14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐或溶剂合物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24）（R 25）或-SR 35; R41是烷基，环烷基，-SO2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH3; 其余变量如本说明书中所定义。还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂疾病

72. 发明申请

US20110065634A1 GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE 有权
标题翻译： GLUCAGON受体拮抗剂，组合物及其使用方法
公开(公告)号：US20110065634A1
公开(公告)日：2011-03-17
申请号：US12992771
申请日：2009-05-13
申请人： William J. Greenlee , Andrew Stamford , Michael W. Miller , Duane Eugene DeMong
发明人： William J. Greenlee , Andrew Stamford , Michael W. Miller , Duane Eugene DeMong
IPC分类号： A61K38/28 , C07D231/18 , A61K31/415 , C07D231/22 , C07D231/38 , C07D401/12 , A61K31/41 , C07D231/12 , A61K38/22 , A61K31/7004 , A61P3/00
CPC分类号： C07D231/22 , C07D231/38
摘要： The present invention relates to compounds of general formula (I), wherein ring A, ring B, R1, R2, R3, Z, and L1 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
摘要翻译：本发明涉及通式（I）的化合物，其中环A，环B，R 1，R 2，R 3，Z和L 1彼此独立地并且如本文所定义，包含该化合物的组合物和方法使用该化合物作为胰高血糖素受体拮抗剂并用于治疗或预防2型糖尿病及与此有关的病症。

73. 发明申请

US20090105208A1 Substituted Piperazines as CB1 Antagonists 失效
标题翻译：取代的Piperazines作为CB1拮抗剂
公开(公告)号：US20090105208A1
公开(公告)日：2009-04-23
申请号：US12146039
申请日：2008-06-25
申请人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Duane Eugene DeMong , Andrew Stamford , William J. Greenlee , Chander Shekher Celly
发明人： Eric J. Gilbert , Michael W. Miller , Jack D. Scott , Duane Eugene DeMong , Andrew Stamford , William J. Greenlee , Chander Shekher Celly
IPC分类号： A61K31/397 , C07D405/12 , A61K31/496 , A61P25/18 , C07D401/04 , A61P25/16 , A61P9/10 , C07D241/04 , A61K31/495 , A61P25/28 , C07D401/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
摘要： Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如吸烟停止），胃肠道疾病和心血管疾病。

74. 发明授权

US07268141B2 Xanthine phosphodiesterase V inhibitors 失效
标题翻译：黄嘌呤磷酸二酯酶V抑制剂
公开(公告)号：US07268141B2
公开(公告)日：2007-09-11
申请号：US10777849
申请日：2004-02-12
申请人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
IPC分类号： C07D473/08 , C07D473/06 , C07D473/04 , A61K31/522 , A61P15/10
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:
摘要翻译：具有式（I）的黄嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其特别用于治疗男性（勃起）和女性性功能障碍等生理障碍：例如，本发明的代表性化合物是：

75. 发明申请

US20070203183A1 Diaryl piperidines as CB1 modulators 审中-公开
标题翻译：二芳基哌啶作为CB1调节剂
公开(公告)号：US20070203183A1
公开(公告)日：2007-08-30
申请号：US11652227
申请日：2007-01-11
申请人： Jack Scott , Jay Weinstein , Michael Miller , Andrew Stamford , Eric Gilbert , Yan Xia , William Greenlee , Sarah Li
发明人： Jack Scott , Jay Weinstein , Michael Miller , Andrew Stamford , Eric Gilbert , Yan Xia , William Greenlee , Sarah Li
IPC分类号： A61K31/454 , C07D211/54 , A61K31/445 , C07D401/02
CPC分类号： C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/58 , C07D211/60 , C07D211/76 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D471/10
摘要： A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome (e.g., obesity, waist circumference, lipid profile, and insulin sensitivity), neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂化物或酯可用于治疗疾病，病症或病症如代谢综合征（例如，肥胖，腰围，脂质分布和胰岛素敏感性），神经炎症性疾病，认知障碍，精神病，成瘾行为，胃肠道疾病和心血管疾病。

76. 发明申请

US20060040948A1 Macrocyclic beta-secretase inhibitors 有权
标题翻译：大环β-分泌酶抑制剂
公开(公告)号：US20060040948A1
公开(公告)日：2006-02-23
申请号：US11189346
申请日：2005-07-26
申请人： Andrew Stamford , Ying Huang , Guoqing Li , Corey Strickand , Johannes Voigt
发明人： Andrew Stamford , Ying Huang , Guoqing Li , Corey Strickand , Johannes Voigt
IPC分类号： A61K31/496 , C07D491/14
CPC分类号： C07D498/04 , C07D413/06
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of β-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐或溶剂化物，其中R 1，R 2，R 3，n和X 如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的方法，其包括向需要这种治疗的患者施用至少一种式I化合物和至少一种选自β-分泌酶抑制剂的化合物的组合，所述β-分泌酶抑制剂除式I，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，非甾体抗炎剂，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂和抗淀粉样蛋白抗体。

77. 发明申请

US20060030588A1 Heteroaryl urea neuropeptide Y Y5 receptor antagonists 有权
公开(公告)号：US20060030588A1
公开(公告)日：2006-02-09
申请号：US11210291
申请日：2005-08-24
申请人： Andrew Stamford , Youhao Dong , Stuart McCombie , Yusheng Wu
发明人： Andrew Stamford , Youhao Dong , Stuart McCombie , Yusheng Wu
IPC分类号： A61K31/4545 , C07D41/14
CPC分类号： C07D401/12 , C07D213/75 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.

78. 发明申请

US20050239795A1 Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
标题翻译：吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US20050239795A1
公开(公告)日：2005-10-27
申请号：US11108916
申请日：2005-04-19
申请人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford , Joel Harris
发明人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford , Joel Harris
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，呋喃基，噻吩基，吡啶基，吡啶基N-氧化物，恶唑基或吡咯基，或环烯基R 1， R 3，R 3，R 4和R 5是H，烷基或烷氧基烷基; 和Z是任选取代的芳基或杂芳基。还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

79. 发明申请

US20050171129A1 Polycyclic guanine derivative phosphodiesterase V inhibitors 审中-公开
标题翻译：多环鸟嘌呤衍生物磷酸二酯酶V抑制剂
公开(公告)号：US20050171129A1
公开(公告)日：2005-08-04
申请号：US11020625
申请日：2004-12-23
申请人： Theodros Asberom , John Clader , Yueqing Hu , Dmitri Pissarnitski , Andrew Stamford , Ruo Xu
发明人： Theodros Asberom , John Clader , Yueqing Hu , Dmitri Pissarnitski , Andrew Stamford , Ruo Xu
IPC分类号： A61K31/519 , A61K31/55 , A61K31/551 , A61K45/00 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/12 , A61P11/00 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/10 , A61P27/06 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/14 , C07D487/20
CPC分类号： C07D487/14
摘要： A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
摘要翻译：具有式（Ia）或（b）的化合物，其盐或溶剂化物，具有本文定义的变量，其可以选择性抑制磷酸二酯酶V并且可用于治疗性功能障碍和其它生理障碍，症状和疾病：

80. 发明申请

US20050075349A1 Xanthine phosphodiesterase V inhibitors 审中-公开
标题翻译：黄嘌呤磷酸二酯酶V抑制剂
公开(公告)号：US20050075349A1
公开(公告)日：2005-04-07
申请号：US10990083
申请日：2004-11-16
申请人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
发明人： Samuel Chackalamannil , Yuguang Wang , Craig Boyle , Andrew Stamford
IPC分类号： A61K31/522 , A61K45/00 , A61P1/00 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P13/00 , A61P13/12 , A61P15/00 , A61P27/06 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D473/02 , C07D473/04 , C07D473/06 , C07D473/08 , C07F7/18 , C07D473/14
CPC分类号： C07D473/04 , C07D473/06 , C07D473/08
摘要： A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative compound of the invention is:
摘要翻译：具有式（I）的黄嘌呤磷酸二酯酶V抑制剂，具有本文定义的变量，其特别用于治疗男性（勃起）和女性性功能障碍等生理障碍：例如，本发明的代表性化合物是：

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