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1. 发明申请

WO2006065277A3 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：WO2006065277A3
公开(公告)日：2007-01-25
申请号：PCT/US2005020446
申请日：2005-06-09
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY , 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
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
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, 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，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拮抗剂组合来治疗认知或神经退行性疾病的方法。

2. 发明申请

WO2008103351A3 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：WO2008103351A3
公开(公告)日：2009-07-23
申请号：PCT/US2008002182
申请日：2008-02-20
申请人： SCHERING CORP , 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 , A61K31/513 , A61P25/28 , C07D239/22 , C07D401/06 , C07D401/10 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10
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.
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W是一个键，-C（= S） - ， - S（O） - ， - S（O） - ， - （= O） - ， - 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（= NR5） - ; U是一个键，-S（O） - ， - S（O）2 - ， - C（O） - ， - O - ， - O（OR）（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; 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。

3. 发明申请

WO2005016876A3 CYCLIC AMINE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT 审中-公开
标题翻译：具有苯甲酸替代物的循环胺BACE-1抑制剂
公开(公告)号：WO2005016876A3
公开(公告)日：2005-09-22
申请号：PCT/US2004025018
申请日：2004-08-04
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY , CUMMING JARED N , ISERLOH ULRICH , STAMFORD ANDREW , STRICKLAND COREY , VOIGT JOHANNES H , WU YUSHENG , HUANG YING , XIA YAN , CHACKALAMANNIL SAMUEL , GUO TAO , HOBBS DOUGLAS W , LE THUY X H , LOWRIE JEFFREY F , SAIONZ KURT W , BABU SURESH D
发明人： CUMMING JARED N , ISERLOH ULRICH , STAMFORD ANDREW , STRICKLAND COREY , VOIGT JOHANNES H , WU YUSHENG , HUANG YING , XIA YAN , CHACKALAMANNIL SAMUEL , GUO TAO , HOBBS DOUGLAS W , LE THUY X H , LOWRIE JEFFREY F , SAIONZ KURT W , BABU SURESH D
IPC分类号： A61K31/55 , A61K31/553 , A61K31/554 , A61K31/675 , C07D207/09 , C07D211/26 , C07D217/18 , C07D241/04 , C07D243/08 , C07D401/06 , C07D403/12 , C07D403/14 , C07D413/06 , C07F9/38 , A61K31/40 , A61K31/47 , A61K31/495 , A61K31/5355 , A61K33/42
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 R is-C(O)-N(R )(R ) 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 beta-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, and 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R是-C（O）-N（R 27）（R 28）），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，甾族抗炎剂和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。

4. 发明申请

WO2006138265A3 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS, PREPARATION AND USE THEREOF 审中-公开
标题翻译：杂环蛋白质蛋白酶抑制剂，其制备和使用
公开(公告)号：WO2006138265A3
公开(公告)日：2007-03-01
申请号：PCT/US2006022919
申请日：2006-06-12
申请人： SCHERING CORP , PHARMACOPEIA DRUG DISCOVERY , 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
IPC分类号： A61K31/519 , A61K31/4035 , A61P9/00 , A61P25/28 , A61P31/18 , A61P33/00 , 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, T, U, Y, Z, ring A 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）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，T，U，Y，Z，环A和R，R 1，R R 2，R 3，R 4，R 5，R 6，R 6，R 4， 7＆lt; 6＆gt;和＆lt; 7＆gt;和＆lt; 7＆gt;是如说明书中所定义的; 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。

5. 发明申请

WO2007146225A3 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：WO2007146225A3
公开(公告)日：2008-03-06
申请号：PCT/US2007013684
申请日：2007-06-07
申请人： SCHERING CORP , 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 , A61K31/513 , A61P25/28 , C07D401/04 , C07D401/10 , C07D403/04 , C07D405/04 , C07D409/14 , C07D411/04 , C07D417/04 , C07D417/10 , C07D495/20
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。

6. 发明申请

WO2006138264A3 ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：WO2006138264A3
公开(公告)日：2007-03-01
申请号：PCT/US2006022918
申请日：2006-06-12
申请人： SCHERING CORP , 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m 2拮抗剂组合治疗认知或神经变性疾病的方法。

7. 发明申请

WO2005111031A3 NEUROPEPTIDE RECEPTOR MODULATORS 审中-公开
标题翻译：神经肽受体调节剂
公开(公告)号：WO2005111031A3
公开(公告)日：2005-12-22
申请号：PCT/US2005014518
申请日：2005-04-28
申请人： SCHERING CORP , 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： A61K31/428 , A61K31/541 , C07D417/00 , C07D417/12 , C07D487/04 , C07D513/04
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制备这些化合物的方法。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症，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，化学式在此以摘要形式出现在本文中应该没有改变。其中R 1为杂芳基，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的化合物或所述前药的任何药学上可接受的盐，溶剂化物，异构体或外消旋混合物; R15存在或不存在并且如果存在则为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，环亚烷基，亚杂环烷基或杂环烷基，其中所述芳基，杂芳基，环烷基，亚环烷基，亚杂环烷基和杂环烷基部分可以被取代或未被取代; 并且B，L，X和R 18如本文所定义。

8. 发明申请

WO2006138266A3 THE PREPARATION AND USE OF COMPOUNDS AS ASPARTYL PROTEASE INHIBITORS 审中-公开
标题翻译：化合物作为ASPARTYL蛋白酶抑制剂的制备和使用
公开(公告)号：WO2006138266A3
公开(公告)日：2007-03-08
申请号：PCT/US2006022920
申请日：2006-06-12
申请人： SCHERING CORP , MCKITTRICK BRIAN , ZHU ZHAONING , STAMFORD ANDREW , SMITH ELIZABETH M
发明人： MCKITTRICK BRIAN , ZHU ZHAONING , STAMFORD ANDREW , SMITH ELIZABETH M
IPC分类号： C07D251/10 , A61K31/53 , A61P9/00
CPC分类号： C07D251/72 , C07D239/70 , C07F9/6584
摘要： Disclosed are compounds of the formula I (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A is a bond, -C(O)-, or -C(R 3' )(R 4' )-; X is -N(R 1 )- or -C(R 6 )(R 7 )-; Y is -S(O) 2 -, -C(=O)-, -PO(OR 9 ) or -C(R 6' R 7' )-; is a single or double bond and R, R 1 , R 2 , R 3 , R 4 , R 3' , R 4' , R 5 , R 6 , R 6' , R 7 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 antagonist.
摘要翻译：公开了式I的化合物（化学式应该在此插入，如其以纸的形式出现）（I）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A为键，-C（O ） - 或-C（R 3'）（R 4'） - ; X是-N（R 1） - 或-C（R 6）（R 7） - ; Y是-S（O）2 - ， - C（= O） - ， - PO（OR 9）或-C（R 6' SUP> - [R ^{7' ） - ; 是单键或双键，R 1，R 2，R 2，R 3，R 4，R 4， R 4，R 4，R 5，R 6，R 6，S 6， >，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。}

9. 发明申请

WO2006138230A2 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：WO2006138230A2
公开(公告)日：2006-12-28
申请号：PCT/US2006022849
申请日：2006-06-12
申请人： SCHERING CORP , MCKITTRICK BRIAN , ZHU ZHAONING , STAMFORD ANDREW
发明人： MCKITTRICK BRIAN , ZHU ZHAONING , STAMFORD ANDREW
IPC分类号： C07D205/06
CPC分类号： C07D487/04 , C07D205/06
摘要： ABSTRACT 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.
摘要翻译：摘要公开了式（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X是-C（R 3）4， - ; Y是-N（R 5） - ; Z是-C（= N-R 5） - ; 和R 1，R 2，R 3和R 4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。

10. 发明申请

WO2009005646A3 SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS 审中-公开
标题翻译：取代的PIPERAZINES作为CB1拮抗剂
公开(公告)号：WO2009005646A3
公开(公告)日：2009-03-19
申请号：PCT/US2008007868
申请日：2008-06-25
申请人： SCHERING CORP , GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
发明人： GILBERT ERIC J , MILLER MICHAEL W , SCOTT JACK D , DEMONG DUANE EUGENE , STAMFORD ANDREW , GREENLEE WILLIAM J , CELLY CHANDER SHEKHER
IPC分类号： C07D241/04 , A61K31/496 , A61K31/506 , A61P3/00 , A61P9/10 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D241/04 , C07D401/06 , C07D401/14 , C07D403/12 , C07D403/14
摘要： Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
摘要翻译：式（I）化合物或其药学上可接受的盐，溶剂合物或酯可用于治疗由CB1受体介导的疾病或病症，例如代谢综合征和肥胖症，神经炎症性疾病，认知障碍和精神病，成瘾（例如戒烟），胃肠道疾病和心血管疾病。

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