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公开(公告)号:US06887889B2
公开(公告)日:2005-05-03
申请号:US10120080
申请日:2002-04-10
申请人: Douglas W. Hobbs , Tao Guo , Rachael C. Hunter , Huizhong Gu , Suresh D. Babu , Yuefei Shao
发明人: Douglas W. Hobbs , Tao Guo , Rachael C. Hunter , Huizhong Gu , Suresh D. Babu , Yuefei Shao
IPC分类号: A61K31/438 , A61K31/4433 , A61K31/445 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K45/00 , A61P3/04 , A61P5/14 , A61P43/00 , C07D211/26 , C07D211/32 , C07D211/34 , C07D211/64 , C07D401/06 , C07D401/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D471/10 , C07D221/26
CPC分类号: C07D401/10 , C07D211/26 , C07D405/04 , C07D405/10 , C07D405/12 , C07D471/10
摘要: In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor. An illustrative inventive compound is shown below:
摘要翻译: 在一个实施方案中,本发明提供了一类新颖的化合物作为MCH受体的拮抗剂,制备此类化合物的方法,含有一种或多种化合物的药物组合物,制备包含一种或多种此类化合物的药物制剂的方法,以及 治疗,预防或改善或与MCH受体相关的一种或多种疾病。 示例性的本发明化合物如下所示:
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公开(公告)号:US20140206715A1
公开(公告)日:2014-07-24
申请号:US14226338
申请日:2014-03-26
申请人: Andrew W. Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.E. Le , Gang Qian , Yuefei Shao
发明人: Andrew W. Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.E. Le , Gang Qian , Yuefei Shao
IPC分类号: C07D471/04
CPC分类号: C07D471/04 , C07D209/44 , C07D487/04
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译: 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐或溶剂合物,其中Q是键或-N(R 5) - ; T是键,-O - , - C(O) - ; S,-N(R 5) - 或-C(R 6'R 7'); U是键或-C(R6)(R7)-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个,优选0至2个杂原子的3至9元环烷基,环烯基,杂环基,杂环烯基,芳基和杂芳基环,其独立地选自O,S, N和-N(R) - ,其中当环A是环烷基,环烯基,杂环基或杂环烯基时,环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。 并且R,R 1,R 2,R 3,R 4,R 5,R 6,R 6,R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经变性疾病的方法。
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公开(公告)号:US08722708B2
公开(公告)日:2014-05-13
申请号:US11451065
申请日:2006-06-12
申请人: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
发明人: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
IPC分类号: C07D487/04 , A61K31/519 , A61K31/4035 , A61K31/4406 , C07D487/14 , A61K31/437 , A61P25/28 , A61P9/00 , A61P31/14
CPC分类号: C07D471/04 , C07D209/44 , C07D487/04
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译: 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐或溶剂合物,其中Q是键或-N(R 5) - ; T是键,-O - , - C(O) - ; S,-N(R 5) - 或-C(R 6'R 7'); U是键或-C(R6)(R7)-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个,优选0至2个杂原子的3至9元环烷基,环烯基,杂环基,杂环烯基,芳基和杂芳基环,其独立地选自O,S, N和-N(R) - ,其中当环A是环烷基,环烯基,杂环基或杂环烯基时,环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。 并且R,R 1,R 2,R 3,R 4,R 5,R 6,R 6,R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经变性疾病的方法。
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公开(公告)号:US08691833B2
公开(公告)日:2014-04-08
申请号:US13415404
申请日:2012-03-08
申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey O. Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, Jr. , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X.E. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号: A01N43/54 , A61K31/505 , C07D239/02
CPC分类号: C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
摘要翻译: 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐或溶剂化物,其中式1中的每个变量如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经退行性疾病的方法,以及抑制人类免疫缺陷病毒,plasmepins,组织蛋白酶D和 原生动物酶。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。
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公开(公告)号:US20120231017A1
公开(公告)日:2012-09-13
申请号:US13415404
申请日:2012-03-08
申请人: ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人: ZHAONING ZHU , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey O. Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert D. Mozzola , John P. Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoiang Liu , Tao Guo , Thuy X. E. Le , Kurt W. Sainoz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey A. Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号: A61K39/395 , C07D239/70 , C07F5/02 , C07D403/10 , A61K31/513 , A61K31/506 , C07D409/04 , C07D409/14 , C07D401/04 , C07D405/14 , C07D417/14 , C07D417/04 , C07D413/14 , C07D413/10 , A61K31/5377 , A61P29/00 , A61P9/00 , A61P25/28 , A61P31/10 , A61P33/02 , C07D495/04 , A61P25/00 , A61P31/04 , C07D239/22
CPC分类号: C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
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公开(公告)号:US20080176868A1
公开(公告)日:2008-07-24
申请号:US11451065
申请日:2006-06-12
申请人: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.H. Le , Gang Qian , Yuefei Shao
发明人: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.H. Le , Gang Qian , Yuefei Shao
IPC分类号: A61K31/519 , C07D209/44 , A61K31/4035 , A61P25/00 , A61P25/28 , A61P31/18 , A61P9/00 , C07D487/04
CPC分类号: C07D471/04 , C07D209/44 , C07D487/04
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocylcyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl;and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译: 公开了式I化合物或其立体异构体,互变异构体或其药学上可接受的盐或溶剂化物,其中Q是一个键或-N(R 5) - ; T是键,-O - , - C(O) - ; S,-N(R 5) - 或-C(R 6',R 7'); U是键或-C(R 6)(R 7) - Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个,优选0至2个杂原子的3至9元环烷基,环烯基,杂环基,杂环烯基,芳基和杂芳基环,其独立地选自O,S, N和-N(R) - ,其中当环A是环烷基,环烯基,杂环基或杂环烯基时,环A是未取代的或被1至5个独立选择的R 1 O 1部分和/或氧代取代。 R 1,R 2,R 2,R 3,R 4,R 5, R 4,R 6,R 6,R 7和R 7'如说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法,特别是治疗心血管疾病,认知和神经变性疾病的方法。
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