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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.
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公开(公告)号:US07309704B2
公开(公告)日:2007-12-18
申请号:US11210291
申请日:2005-08-24
申请人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号: C07D239/24 , C07D403/04 , C07D403/12 , C07D403/14 , A61K31/506 , A61P3/04
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.
摘要翻译: 本发明涉及由结构式I表示的化合物或其药学上可接受的盐,其可用于治疗代谢和进食障碍如肥胖症和食欲过盛,以及用于治疗糖尿病和相关疾病。
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公开(公告)号:US20050038100A1
公开(公告)日:2005-02-17
申请号:US10933016
申请日:2004-09-01
申请人: William Greenlee , Ying Huang , Joseph Kelly , Stuart McCombie , Andrew Stamford , Yusheng Wu
发明人: William Greenlee , Ying Huang , Joseph Kelly , Stuart McCombie , Andrew Stamford , Yusheng Wu
IPC分类号: C07C275/30 , C07C311/07 , C07D211/58 , C07D211/96 , C07D401/04 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04 , A61K31/40 , A61K31/17 , C07D207/46
CPC分类号: C07D401/04 , C07C275/30 , C07C311/07 , C07C2601/14 , C07D211/58 , C07D211/96 , C07D401/06 , C07D409/12 , C07D409/14 , C07D417/04
摘要: A novel class of compounds such as antagonists of the neuropeptide Y Y5 receptor, methods of making such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration of one or more diseases associated with the neuropeptide Y Y5 receptor are disclosed.
摘要翻译: 一类新颖的化合物,例如神经肽Y Y5受体的拮抗剂,制备此类化合物的方法,含有一种或多种这类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,预防或改善方法 公开了与神经肽Y Y5受体相关的一种或多种疾病。
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公开(公告)号:US06982267B2
公开(公告)日:2006-01-03
申请号:US10026651
申请日:2001-12-18
申请人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号: C07D241/26 , C07D409/04 , A61K31/4965 , A61K31/497 , A61K3/04
CPC分类号: C07D401/12 , A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , A61K2300/00
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.
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公开(公告)号:US06946476B2
公开(公告)日:2005-09-20
申请号:US10177345
申请日:2002-06-20
申请人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
发明人: Andrew Stamford , Youhao Dong , Stuart W. McCombie , Yusheng Wu
IPC分类号: A61K31/4523 , A61K31/4535 , A61K31/4545 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D417/14 , C07D213/02 , A61K31/4418 , A61K31/4436 , A61P3/04 , C07D409/04
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.
摘要翻译: 本发明涉及由结构式I表示的化合物或其药学上可接受的盐,其可用于治疗代谢和进食障碍如肥胖症和食欲过盛,以及用于治疗糖尿病和相关疾病。
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公开(公告)号:US08778980B2
公开(公告)日:2014-07-15
申请号:US13551315
申请日:2012-07-17
申请人: Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人: Zhaoning Zhu , Brian A McKittrick , Zhong-Yue Sun , Yuanzan C Ye , Johannes H Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号: A01N43/82 , A61K31/41 , C07D271/06
CPC分类号: C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method 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:US08623867B2
公开(公告)日:2014-01-07
申请号:US13610162
申请日:2012-09-11
申请人: Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voight , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey H. Lowrie , Kurt W. Saionz , Suresh D. Babu
发明人: Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voight , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey H. Lowrie , Kurt W. Saionz , Suresh D. Babu
IPC分类号: A61K31/445 , A61K31/4458 , A61K31/454 , A61K31/4545 , A61K31/5377 , C07D295/027 , C07D401/06 , C07D401/12 , C07D413/12
CPC分类号: C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables 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 pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
摘要翻译: 公开了下式的化合物或其药学上可接受的盐或溶剂化物,其中R1是R是-C(O)-N(R27)(R28),或其余的变量如说明书中所定义。 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药物组合物和方法,其包含式I化合物与除式I以外的β-分泌酶抑制剂,HMG-CoA还原酶抑制剂,γ-分泌酶抑制剂, 甾族抗炎剂,N-甲基-D-天冬氨酸受体拮抗剂,胆碱酯酶抑制剂或抗淀粉样蛋白抗体。
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公开(公告)号:US08168641B2
公开(公告)日:2012-05-01
申请号:US11759336
申请日:2007-06-07
申请人: Yusheng Wu , Ulrich Iserloh , Jared N. Cumming , Xiaoxiang Liu , Robert D. Mazzola , Zhong-Yue Sun , Ying Huang , Andrew Stamford , Brian McKittrick , Zhaoning Zhu
发明人: Yusheng Wu , Ulrich Iserloh , Jared N. Cumming , Xiaoxiang Liu , Robert D. Mazzola , Zhong-Yue Sun , Ying Huang , Andrew Stamford , Brian McKittrick , Zhaoning Zhu
IPC分类号: C07D239/20 , C07D239/22 , A61K31/497 , A61K31/513 , A61K31/506 , A61P9/00 , A61P25/28 , A61P31/18 , C07D495/20 , A61K31/527
CPC分类号: C07D239/20 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D409/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D495/20
摘要: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. 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合物,U,W,X,R 1,R 2,R 6,R 7,R 30和R 31如上文在说明书中所述。 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,认知和神经变性疾病的方法。 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:US20110218194A1
公开(公告)日:2011-09-08
申请号:US13108454
申请日:2011-05-16
申请人: Zhaoning Zhu , Brian A. Mckittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachel C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人: Zhaoning Zhu , Brian A. Mckittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voight , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X. H. Le , Kurt W. Saionz , Suresh D. Babu , Rachel C. Hunter , Michelle L. Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号: A61K31/5395 , C07D273/04 , C07D413/10 , A61P9/00 , A61P33/02 , A61P31/10 , A61P25/28 , A61P25/00
CPC分类号: C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method 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:US20090306047A1
公开(公告)日:2009-12-10
申请号:US12480391
申请日:2009-06-08
申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter
发明人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew Stamford , William J. Greenlee , Robert Mazzola , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter
IPC分类号: A61K31/4178 , C07D403/10 , C07D233/88 , C07D401/14 , A61K31/4168 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/435 , A61K31/4353 , A61K31/55 , A61P25/28
CPC分类号: C07D233/88 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D233/46 , C07D233/70 , C07D235/02 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D295/15 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , Y02A50/411
摘要: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method 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 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W是键,-C(-S) - , - S(O) - , - S(O) -C( - ) - , - O - , - C(R6)(R7) - , - N(R5) - 或-C(-N(R5) X是-O - , - N(R 5) - 或-C(R 6)(R 7) - ; 条件是当X是-O-时,U不是-O-,-S(O) - , - S(O)2 - , - C(-O) - 或-C(-NR 5) - ; U是一个键,-S(O) - , - S(O)2 - , - C(O) - , - O - , - (O)(OR 15) - , - (C(R6)(R7))b-或-N(R5) - ; 其中b为1或2; 条件是当W是-S(O) - , - S(O)2 - , - O-或-N(R 5) - 时,U不是-S(O) - , - S(O) -O-或-N(R 5) - ; 条件是当X为-N(R5) - 且W为-S(O) - , - S(O)2 - , - O-或-N(R5) - 时,则U不为键; 并且R1,R2,R3,R4,R5,R6和R7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,认知和神经变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拮抗剂组合来治疗认知或神经变性疾病的方法。
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