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1. 发明申请

WO2007053506A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2007053506A1
公开(公告)日：2007-05-10
申请号：PCT/US2006/042193
申请日：2006-10-30
申请人： SCHERING CORPORATION , ZHU, Zhaoning , STAMFORD, Andrew, W. , MCKITTRICK, Brian
发明人： ZHU, Zhaoning , STAMFORD, Andrew, W. , MCKITTRICK, Brian
IPC分类号： C07D411/04 , A61K31/553
CPC分类号： C07D413/04 , C07F9/65848
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein (W, 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）的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（W，R 1，R 2，R 3，R 4，R 5，R 6和R 7）如说明书中所定义; 和包含式（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拮抗剂组合来治疗认知或神经退行性疾病的方法。

2. 发明申请

WO2006138265A2 THE PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
标题翻译：化合物作为蛋白酶抑制剂的制备和使用
公开(公告)号：WO2006138265A2
公开(公告)日：2006-12-28
申请号：PCT/US2006/022919
申请日：2006-06-12
申请人： SCHERING CORPORATION , PHARMACOPEIA DRUG DISCOVERY, INC. , STAMFORD, Andrew , LI, Guoqing , GREENLEE, William, J. , ZHU, Zhaoning , MCKITTRICK, Brian , MAZZOLA, Robert , HUANG, Ying , GUO, Tao , LE, Thuy X. H. , QIAN, Gang , SHAO, Yuefei
发明人： STAMFORD, Andrew , LI, Guoqing , GREENLEE, William, J. , ZHU, Zhaoning , MCKITTRICK, Brian , MAZZOLA, Robert , HUANG, Ying , GUO, Tao , LE, Thuy X. H. , QIAN, Gang , SHAO, Yuefei
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(R 5 )-; T is a bond, -O-, -C(O)-; S, -N(R 5 )-, or -C(R 6’ R 7’ ); U is a bond or -C(R 6 )(R 7 )- 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, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 6 , R 7 and R 7’ 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）的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是结合或-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。

3. 发明申请

WO2006065277A2 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2006065277A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/020446
申请日：2005-06-09
申请人： SCHERING CORPORATION , PHARMACOPEIA DRUG DISCOVERY, INC. , ZHU, Zhaoning , MCKITTRICK, Brian , SUN, Zhong-Yue , YE, Yuanzan, C. , VOIGT, Johannes, H. , STRICKLAND, Corey , SMITH, Elizabeth, M. , STAMFORD, Andrew , GREENLEE, William, J. , MAZZOLA, Robert , CALDWELL, John , CUMMING, Jared , WANG, Lingyan , WU, Yusheng , ISERLOH, Ulrich , GUO, Tao , LE, Thuy, X., H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C. , MORRIS, Michelle, L. , GU, Huizhong , QIAN, Gang , TADESSE, Dawit
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, Robert , CALDWELL, John , CUMMING, Jared , WANG, Lingyan , WU, Yusheng , ISERLOH, Ulrich , GUO, Tao , LE, Thuy, X., H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C. , MORRIS, Michelle, L. , GU, Huizhong , QIAN, Gang , TADESSE, Dawit
IPC分类号： A61K31/4168 , A61K31/4178 , C07D233/46 , C07D233/88 , C07D239/22 , C07D271/06 , C07D273/00 , C07D401/10 , C07D403/06 , C07D403/12 , C07D407/10 , C07D409/04 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , A61P9/00 , A61P25/00
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) 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(R 6 )(R 7 )-, -N(R 5 )- or -C(=N(R 5 ))-; X is -O-, -N(R 5 )- or -C(R 6 )(R 7 )-; 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)(OR 15 )-, -C(=NR 5 )-, -(C(R 6 )(R 7 )) b - or -N(R 5 )-; 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(R 5 )-; provided that when X is -N(R 5 )- and W is -S(O)-, -S(O) 2 -, -O-, or -N(R 5 )-, then U is not a bond; and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 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 m 1 agonist or m 2 antagonist.
摘要翻译：公开了式（I）的立体异构体，互变异构体或其药学上可接受的盐或溶剂化物的化合物，其中W是键，-C（= S） - ， - S（O） - ， - S（O） -C（= O） - ， - O - ， - C（R 6） - ， - N（R - 或-C（= N（R 5）） - ; 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（= NR5） - ; U是一个键，-S（O） - ， - S（O）2 - ， - C（O） - ， - O - ，-P（O）（C（R 6）） - ， - （C（R 6）） - ， - C（= NR 5） > - 或-N（R 5） - ; 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） 2 - ， - O-或-N（R 5） - ; 条件是当X是-N（R 5） - 且W是-S（O） - ，-S（O）2 - ， - O-或 - N（R 5） - ，则U不是键; 和R 1，R 2，R 3，R 4，R 5， R 6，R 6和R 7如说明书中所定义; 和包含式（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m 1激动剂或m 2 N拮抗剂组合治疗认知或神经变性疾病的方法。

4. 发明申请

WO2005058311A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2005058311A1
公开(公告)日：2005-06-30
申请号：PCT/US2004/041700
申请日：2004-12-13
申请人： SCHERING CORPORATION , PHARMACOPEIA DRUG DISCOVERY, INC. , ZHU, Zhaoning , MCKITTRICK, Brian , SUN, Zhong-Yue , YE, Yuanzan, C. , VOIGT, Johannes, H. , STRICKLAND, Corey , SMITH, Elizabeth, M. , STAMFORD, Andrew , GREENLEE, William, J. , WU, Yusheng , ISERLOH, Ulrich , MAZZOLA, Robert , CALDWELL, John , CUMMING, Jared , WANG, Lingyan , GUO, Tao , LE, Thuy, X. H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C.
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. , WU, Yusheng , ISERLOH, Ulrich , MAZZOLA, Robert , CALDWELL, John , CUMMING, Jared , WANG, Lingyan , GUO, Tao , LE, Thuy, X. H. , SAIONZ, Kurt, W. , BABU, Suresh, D. , HUNTER, Rachael, C.
IPC分类号： A61K31/4168
CPC分类号： C07D233/88 , C07D235/02 , C07D239/22 , C07D271/07 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof. 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）的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。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拮抗剂组合治疗认知或神经退行性疾病的方法。

5. 发明申请

WO2008103351A2 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2008103351A2
公开(公告)日：2008-08-28
申请号：PCT/US2008/002182
申请日：2008-02-20
申请人： SCHERING CORPORATION , PHARMACOPEIA, INC. , 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
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(R 6 )(R 7 )-, -N(R 5 )- or -C(=N(R 5 ))-; X is -O-, -N(R 5 )- or -C(R 6 )(R 7 )-; provided that when X is -O-, U is not -O-, -S(O)-, -S(O) 2 -, -C(=O)- or -C(=NR 5 )-; U is a bond, -S(O)-, -S(O) 2 -, -C(O)-, -O-, -P(O)(OR 15 )-, -C(=NR 5 )-, -(C(R 6 )(R 7 )) b - or -N(R 5 )-; wherein b is 1 or 2; provided that when W is -S(O)-, -S(O) 2 -, -O-, or -N(R 5 )-, U is not -S(O)-, -S(O) 2 -, -O-, or -N(R 5 )-; provided that when X is -N(R 5 )- and W is -S(O)-, -S(O) 2 -, -O-, or -N(R 5 )-, then U is not a bond; and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 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 m 1 agonist or m 2 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为键，-C（= S） - ， - S（O） - ， - S（O） -C（= O） - ， - O - ， - （R 6） - （R 7） - ， - N（ R 5） - 或-C（= N（R 5）） - ; 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 - ，-P（O）（C（R 6）） - ， - （C（R 6）） - ， - C（= NR 5） > - 或-N（R 5） - ; 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）2 - ， - O-或-N（R 5））。条件是当X是-N（R 5） - 且W是-S（O） - ，-S（O）2 - ， - O-或 - N（R 5） - ，则U不是键; 和R 1，R 2，R 3，R 4，R 5， R 6，R 6和R 7如说明书中所定义; 和包含式（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m 1激动剂或m 2 H 2拮抗剂组合治疗认知或神经变性疾病的方法。}

6. 发明申请

WO2006138230A3 THE PREPARATION AND USE OF PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2006138230A3
公开(公告)日：2006-12-28
申请号：PCT/US2006/022849
申请日：2006-06-12
申请人： SCHERING CORPORATION , MCKITTRICK, Brian , ZHU, Zhaoning , STAMFORD, Andrew
发明人： MCKITTRICK, Brian , ZHU, Zhaoning , STAMFORD, Andrew
IPC分类号： C07D205/06 , C07D487/04 , A61K31/397 , A61P31/18 , A61P25/28
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein, X is -C(R 3 R 4 )-; Y is -N(R 5 )-; Z is -C(=N-R 5 ’)-; and R 1 , R 2 , R 3 , and R 4 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.

7. 发明申请

WO2007146225A2 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：异源ASPARTYL蛋白酶抑制剂
公开(公告)号：WO2007146225A2
公开(公告)日：2007-12-21
申请号：PCT/US2007/013684
申请日：2007-06-07
申请人： SCHERING CORPORATION , WU, Yusheng , ISERLOH, Ulrich , CUMMING, Jared , LIU, Xiaoxiang , MAZZOLA, Robert, D. , SUN, Zhong-Yue , HUANG, Ying , STAMFORD, Andrew , MCKITTRICK, Brian , ZHU, Zhaoning
发明人： WU, Yusheng , ISERLOH, Ulrich , CUMMING, Jared , LIU, Xiaoxiang , MAZZOLA, Robert, D. , SUN, Zhong-Yue , HUANG, Ying , STAMFORD, Andrew , MCKITTRICK, Brian , ZHU, Zhaoning
IPC分类号： C07D239/20 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D409/14 , C07D411/04 , C07D417/14 , C07D495/20 , A61K31/513 , A61P25/28
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, R 1 , R 2 , R 6 , R 7 , R 30 and R 31 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）的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， SUP> 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。

8. 发明申请

WO2005111031A2 NEUROPEPTIDE RECEPTOR MODULATORS 审中-公开
标题翻译：神经元受体调节剂
公开(公告)号：WO2005111031A2
公开(公告)日：2005-11-24
申请号：PCT/US2005/014518
申请日：2005-04-28
申请人： SCHERING CORPORATION , ZHU, Zhaoning , SUN, Zhong-Yue , YE, Yuanzan , MULLINS, Deborra, E. , MCKITTRICK, Brian , STAMFORD, Andrew , GREENLEE, William, J.
发明人： ZHU, Zhaoning , SUN, Zhong-Yue , YE, Yuanzan , MULLINS, Deborra, E. , MCKITTRICK, Brian , STAMFORD, Andrew , GREENLEE, William, J.
IPC分类号： C07D417/00
CPC分类号： C07D487/04 , C07D417/12 , C07D513/04
摘要： The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. The compounds are represented by the structural Formula 1, Chemical formula should be inderted here as it appears on the abstract in paper form. a prodrug thereof, or any pharmaceutically acceptable salt, solvate, isomer or racemic mixture of the compound or said prodrug wherein R1 is heteroaryl, N-arylaminocarbonyl, N-heteroarylaminocarbonyl, benzimidazolyl or benzothiazolyl; R15 is present or not and if present is H, aryl, alkyl, arylalky or heteroarylalkyl; A is aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene or heterocycloalkyl wherein said aryl, heteroaryl, cycloalkyl, cycloalkylidene, heterocycloalkylidene and heterocycloalkyl moieties may be substituted or unsubstituted; and B, L, X and R18 are defined herein.
摘要翻译：本发明公开了作为NPY Y1的新受体拮抗剂的化合物以及这些化合物的制备方法。在另一个实施方案中，本发明公开了包含这种NPY Y1受体拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。这些化合物由结构式1表示，化学式应该在这里被废弃，因为它以纸张的形式出现在抽象上。其前体药物，或化合物或所述前药的任何药学上可接受的盐，溶剂合物，异构体或外消旋混合物，其中R 1是杂芳基，N-芳基氨基羰基，N-杂芳基氨基羰基，苯并咪唑基或苯并噻唑基; 存在或不存在，如果存在，则为H，芳基，烷基，芳基烷基或杂芳基烷基; A是芳基，杂芳基，环烷基，环烷叉基，杂环亚烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，杂环亚烷基和杂环烷基部分可以是取代或未取代的; 并且B，L，X和R 18在本文中定义。

9. 发明申请

WO2006138264A2 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2006138264A2
公开(公告)日：2006-12-28
申请号：PCT/US2006/022918
申请日：2006-06-12
申请人： SCHERING CORPORATION , ZHU, Zhaoning , MCKITTRICK, Brian , STAMFORD, Andrew , GREENLEE, William, J. , LIU, Xiaoxiang , MANDAL, Mihirbaran , VOIGT, Johannes, H. , STRICKLAND, Corey
发明人： ZHU, Zhaoning , MCKITTRICK, Brian , STAMFORD, Andrew , GREENLEE, William, J. , LIU, Xiaoxiang , MANDAL, Mihirbaran , VOIGT, Johannes, H. , STRICKLAND, Corey
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R 1 , R 2 , R 3 , R 4 , R 6 , R 7 and R 7a 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 m 2 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j，k，U，W，R，R 1，R 2， R 3，R 4，R 4，R 6，R 7和R 7， / SUP>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退行性疾病的方法。

10. 发明申请

WO2006138217A1 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2006138217A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/022828
申请日：2006-06-12
申请人： SCHERING CORPORATION , PHARMACOPEIA DRUG DISCOVERY, INC. , ZHU, Zhaoning , MCKITTRICK, Brian , STAMFORD, Andrew, W. , LE, Thuy, X.H. , GUO, Tao
发明人： ZHU, Zhaoning , MCKITTRICK, Brian , STAMFORD, Andrew, W. , LE, Thuy, X.H. , GUO, Tao
IPC分类号： C07D239/70 , C07D491/10 , C07D495/10 , C07D471/10 , C07D487/10
CPC分类号： C07D471/10 , C07D239/70 , C07D487/10 , C07D491/10 , C07D495/10
摘要： Disclosed are compounds of the formula I here or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R 1 , R 2 , R 6a and R 7 , 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. 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 m 1 agonist or m 2 antagonist.
摘要翻译：公开了本文式I的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U，W，A，R，R 1，R 2， R 6a，R 7和R 7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。还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m 1激动剂或m 2 N拮抗剂组合治疗认知或神经变性疾病的方法。

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