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公开(公告)号：EP2097387A2
公开(公告)日：2009-09-09
申请号：EP08714220.4
申请日：2008-02-20
发明人： ZHU, Zhaoning , MCKITTRICK, Brian , SUN, Zhong-Yue , YE, Yuanzan, C. , VOIGT, Johannes, H. , STRICKLAND, Corey , SMITH, Elizabeth, M. , STAMFORD, Andrew , GREENLEE, William, J. , MAZZOLA, JR., Robert, D. , CALDWELL, John , CUMMING, Jared, N. , WANG, Lingyan , WU, Yusheng , ISERLOH, Ulrich , LIU, Xiaoxiang , HUANG, Ying , LI, Guoqing , PAN, Jianping , MISIASZEK, Jeffrey, A. , GUO, Tao , LE, Thuy X. H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C. , MORRIS, Michelle, L. , GU, Huizhong , QIAN, Gang , TADESSE, Dawit , LAI, Gaifa , DUO, Jingqi , QU, Chuanxing , SHAO, Yuefei
IPC分类号： C07D233/88 , C07D239/22 , C07D401/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/14 , C07D495/10 , C07D401/10 , C07D417/10 , A61K31/513 , A61P25/28
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 (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：EP1660447B1
公开(公告)日：2008-07-30
申请号：EP04780561.9
申请日：2004-08-04
发明人： CUMMING, Jared, N. , HUANG, Ying , LI, Guoqing , ISERLOH, Ulrich , STAMFORD, Andrew , STRICKLAND, Corey , VOIGT, Johannes, H. , WU, Yusheng , PAN, Jianping , GUO, Tao , HOBBS, Douglas, W. , LE, Thuy, X., H. , LOWRIE, Jeffrey, F.
IPC分类号： C07D207/26 , C07D413/12 , C07D401/12 , C07D403/12 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D405/06 , C07D409/06
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 (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)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, -S02(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.
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公开(公告)号：EP1660447A1
公开(公告)日：2006-05-31
申请号：EP04780561.9
申请日：2004-08-04
发明人： CUMMING, Jared, N. , HUANG, Ying , LI, Guoqing , ISERLOH, Ulrich , STAMFORD, Andrew , STRICKLAND, Corey , VOIGT, Johannes, H. , WU, Yusheng , PAN, Jianping , GUO, Tao , HOBBS, Douglas, W. , LE, Thuy, X., H. , LOWRIE, Jeffrey, F.
IPC分类号： C07D207/26 , C07D413/12 , C07D401/12 , C07D403/12 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14 , C07D405/06 , C07D409/06
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 (I)or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is formula (I) X is -0-, -C(R14)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, -S02(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.
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