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公开(公告)号:US20070191332A1
公开(公告)日:2007-08-16
申请号:US11502116
申请日:2006-08-10
申请人: Zhaoning Zhu , Robert Mazzola , Wensheng Yu , Joseph Kozlowski
发明人: Zhaoning Zhu , Robert Mazzola , Wensheng Yu , Joseph Kozlowski
IPC分类号: A61K31/4709 , A61K31/4178 , A61K31/4025 , A61K31/405 , C07D403/02
CPC分类号: C07D401/12
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, wherein n, M, V, T, W, X, U, R1 and R2 are as disclosed in the present specification, and which compounds are useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂合物或异构体,其中n,M,V,T,W,X,U,R 1和R 2, SUP> 2如本说明书中所公开的,哪些化合物可用于治疗由MMPs,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US20060252778A1
公开(公告)日:2006-11-09
申请号:US11142601
申请日:2005-06-01
申请人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert Mazzola , Tin-Yau Chan , Henry Vaccaro , Brian McKittrick , Joseph Kozlowski , Brian Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline Ting , Kristin Rosner , Gerald Shipps , M. Siddiqui , David Belanger , Chaoyang Dai , Dansu Li , Vinay Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人: Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert Mazzola , Tin-Yau Chan , Henry Vaccaro , Brian McKittrick , Joseph Kozlowski , Brian Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline Ting , Kristin Rosner , Gerald Shipps , M. Siddiqui , David Belanger , Chaoyang Dai , Dansu Li , Vinay Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号: C07D471/02 , C07D498/02 , A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/43 , A61K31/4245
CPC分类号: C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂化物或异构体,其可用于治疗由MMP,ADAM,TACE,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US07034057B2
公开(公告)日:2006-04-25
申请号:US10716890
申请日:2003-11-19
申请人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号: A61K31/165 , A61K31/18 , A61K31/21 , A61K31/27
CPC分类号: C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
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公开(公告)号:US06838466B2
公开(公告)日:2005-01-04
申请号:US10323511
申请日:2002-12-19
申请人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号: C07D249/06 , A61K31/165 , A61K31/167 , A61K31/194 , A61K31/216 , A61K31/277 , A61K31/36 , A61K31/4164 , A61K31/4192 , A61K31/428 , A61K31/435 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/02 , A61P3/10 , A61P9/00 , A61P11/00 , A61P11/02 , A61P13/12 , A61P17/06 , A61P19/00 , A61P19/02 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/18 , A61P33/06 , A61P35/04 , A61P37/06 , A61P37/08 , C07C61/39 , C07C62/34 , C07C69/757 , C07C233/63 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/21 , C07C311/29 , C07C317/22 , C07C323/19 , C07D213/30 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/14 , C07D215/18 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/54 , C07D233/58 , C07D271/06 , C07D277/24 , C07D277/44 , C07D277/64 , C07D295/18 , C07D311/58 , C07D317/64 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号: C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
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公开(公告)号:US20060063843A1
公开(公告)日:2006-03-23
申请号:US11255130
申请日:2005-10-20
申请人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号: A61K31/66 , A61K31/165
CPC分类号: C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)的化合物:
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公开(公告)号:US07598242B2
公开(公告)日:2009-10-06
申请号:US11255130
申请日:2005-10-20
申请人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人: Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号: A61K31/535 , A61K31/497 , C07D401/12 , C07D413/04 , C07D295/02 , C07D217/06 , C07C255/03 , C07C69/76
CPC分类号: C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂化物或异构体,其可用于治疗由MMP,TNF-α或其组合介导的疾病或病症。
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公开(公告)号:US20080200445A1
公开(公告)日:2008-08-21
申请号:US11710582
申请日:2007-02-23
申请人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
发明人: Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao
IPC分类号: A61K31/506 , A61K31/4178 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/541 , A61P31/00 , C07D233/02 , C07D271/00 , C07D413/14 , C07D409/14 , C07D409/04 , C07D403/06 , C07D401/14 , C07D401/12 , C07D401/10 , C07D401/06 , C07D239/04 , A61P9/00 , A61P25/00 , A61K31/5377 , A61K31/4545 , A61K31/4709 , A61K31/498
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 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 1. 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: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: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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