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11. 发明专利

JP2007145875A Adenosine a2a receptor antagonist 审中-公开
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：JP2007145875A
公开(公告)日：2007-06-14
申请号：JP2007069618
申请日：2007-03-16
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： NEUSTADT BERNARD R , LINDO NEIL A , GREENLEE WILLIAM J , TULSHIAN DEEN , SILVERMAN LISA S , XIA YAN , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL
IPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00
CPC分类号： C07D487/14
摘要： PROBLEM TO BE SOLVED: To provide a process for preparing 5-amino-2-(substituted) pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine. SOLUTION: The preferable aspect of this process is the dehydrorearrangement of an intermediate of formula IX for preparing 5-amino-2-(substituted) pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine of formula II. The preferable embodiment of the process uses 2-furoic hydrazide or 2-thienoyl hydrazide and thereby prepares a compound of formula II whose R is 2-furyl or 2-thienyl. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：提供制备5-氨基-2-（取代的）吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c]嘧啶的方法。解决方案：该方法的优选方面是用于制备5-氨基-2-（取代的）吡唑并[4,3-e] -1,2,4-三唑并 - [1 ，5-c]嘧啶。该方法的优选实施方案使用2-糠酰肼或2-噻吩酰肼，从而制备其R为2-呋喃基或2-噻吩基的式II化合物。版权所有（C）2007，JPO＆INPIT

12. 发明专利

JP2006219497A Adenosine a2a receptor antagonist 有权
标题翻译：腺苷A2A受体拮抗剂
公开(公告)号：JP2006219497A
公开(公告)日：2006-08-24
申请号：JP2006128415
申请日：2006-05-02
申请人： Schering Plough Corp , シェーリングコーポレイションSchering Corporation
发明人： NEUSTADT BERNARD R , LINDO NEIL A , GREENLEE WILLIAM J , TULSHIAN DEEN , SILVERMAN LISA S , XIA YAN , BOYLE CRAIG D , CHACKALAMANNIL SAMUEL
IPC分类号： C07D487/14 , A61K31/505 , A61K31/519 , A61K31/5377 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D519/00
CPC分类号： C07D487/14
摘要： PROBLEM TO BE SOLVED: To provide a process for preparing 5-amino-2-(substituted) pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine. SOLUTION: The preferable aspect of this process is dehydrorearrangement of an intermediate of formula IX for obtaining 5-amino-2-(substituted) pyrazolo[4,3-e]-1,2,4-triazolo-[1,5-c]pyrimidine of formula II. The preferable embodiment of the process uses 2-furoic hydrazide or 2-thienoyl hydrazide and thereby prepares a compound of formula II whose R is 2-furyl or 2-thienyl. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供制备5-氨基-2-（取代的）吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c]嘧啶的方法。解决方案：该方法的优选方面是式IX中间体的脱氢分解，得到5-氨基-2-（取代的）吡唑并[4,3-e] -1,2,4-三唑并 - [1,3] 5-c]嘧啶。该方法的优选实施方案使用2-糠酰肼或2-噻吩酰肼，从而制备其R为2-呋喃基或2-噻吩基的式II化合物。版权所有（C）2006，JPO＆NCIPI

13. 发明申请

WO2005046688A3 METHODS OF USE OF THROMBIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：使用硫蛋白受体拮抗剂的方法
公开(公告)号：WO2005046688A3
公开(公告)日：2005-09-29
申请号：PCT/US2004037519
申请日：2004-11-09
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
发明人： CHACKALAMANNIL SAMUEL , CLASBY MARTIN C , GREENLEE WILLIAM J , WANG YUGUANG , XIA YAN , VELTRI ENRICO P , CHELLIAH MARIAPPAN V , WU WENXUE , GRAZIANO MICHAEL P , KOSOGLOU TEDDY , CHINTALA MADHU
IPC分类号： A61K31/343 , A61K31/4525 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D521/00 , A61P9/00 , A61P11/00 , A61P13/12 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： A61K31/4525 , A61K31/343 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/06 , C07D405/14 , C07D413/14 , C07D417/14
摘要： A method of treating a therapeutic condition comprising administering to a mammal in need of such treatment an effective amount of at least one compound of the formulas (I) and (II) or a pharmaceutically acceptable isomer, salt, solvate or co-crystal form thereof, wherein the substituents are as defined in the specification, wherein said therapeutic condition is a cardiovascular or circulatory disease or condition, an inflammatory disease or condition, a respiratory tract or disease or condition, cancer, acute renal failure, astrogliosis, a fibrotic disorder of the liver, kidney, lung or intestinal tract, Alzheimer's disease, diabetes, diabetic neuropathy, rheumatoid arthritis, neurodegenerative disease, neurotoxic disease, systemic lupus erythematosus, multiple sclerosis, osteoporosis, glaucoma, macular degeneration, psoriasis, radiation fibrosis, endothelial dysfunction, a wound or a spinal cord injury, or a symptom or result thereof. Combination therapy with other therapeutically effective agents is also disclosed.
摘要翻译：治疗治疗条件的方法包括向需要这种治疗的哺乳动物施用有效量的至少一种式（I）和（II）化合物或其药学上可接受的异构体，盐，溶剂合物或共晶体形式其中所述取代基如说明书中所定义，其中所述治疗条件是心血管或循环系统疾病或病症，炎性疾病或病症，呼吸道或疾病或病症，癌症，急性肾功能衰竭，星形胶质细胞增生症，纤维化疾病肝，肾，肺或肠道，阿尔茨海默病，糖尿病，糖尿病性神经病，类风湿性关节炎，神经变性疾病，神经毒性疾病，系统性红斑狼疮，多发性硬化症，骨质疏松症，青光眼，黄斑变性，牛皮癣，放射纤维化，内皮功能障碍伤口或脊髓损伤，或其症状或结果。还公开了与其它治疗有效药物的联合治疗。

14. 发明申请

WO2005035504A3 5-H -BENZO [D] NAPHTH [2, 1-B] AZEPINE DERIVATIVE AS SELECTIVE D1/D5 RECEPTOR ANTAGONISTS FOR THE TREATMENT OF OBESITY AND CNS DISORDERS 审中-公开
标题翻译： 5-H-BENZO [D] NAPHTH [2,1-B] AZEPINE衍生物作为选择性D1 / D5受体拮抗剂治疗肥胖和CNS疾病
公开(公告)号：WO2005035504A3
公开(公告)日：2005-06-30
申请号：PCT/US2004015760
申请日：2004-05-20
申请人： SCHERING CORP , BURNETT DUANE A , GREENLEE WILLIAM J , MCKITTRICK BRIAN , SU JING , ZHU ZHAONING , SASIKUMAR THAVALAKULAMGARA K , MAZZOLA ROBERT , QIANG LI , YE YUANZAN
发明人： BURNETT DUANE A , GREENLEE WILLIAM J , MCKITTRICK BRIAN , SU JING , ZHU ZHAONING , SASIKUMAR THAVALAKULAMGARA K , MAZZOLA ROBERT , QIANG LI , YE YUANZAN
IPC分类号： C07D223/14 , C07D401/12 , C07D403/10 , C07D407/12
CPC分类号： C07D223/14
摘要： The present invention provides compounds of formula (I), which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明提供式（I）化合物，其为D1 / D5受体的新型拮抗剂以及制备这些化合物的方法。在另一个实施方案中，本发明提供了包含这种D1 / D5受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

15. 发明申请

WO2010147969A3 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2010147969A3
公开(公告)日：2011-06-09
申请号：PCT/US2010038649
申请日：2010-06-15
申请人： SCHERING CORP , ZHU ZHAONING , HUANG XIANHAI , PALANI ANANDAN , GREENLEE WILLIAM J , ASLANIAN ROBERT G
发明人： ZHU ZHAONING , HUANG XIANHAI , PALANI ANANDAN , GREENLEE WILLIAM J , ASLANIAN ROBERT G
IPC分类号： C07D471/04 , A61K31/551 , A61K31/553 , A61K31/554 , A61P25/28 , C07D498/04 , C07D513/04
CPC分类号： C07D498/04 , C07D471/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
摘要翻译：本发明提供了作为γ分泌酶调节剂的新型化合物。化合物具有式（I）：还公开了使用式（I）的化合物调节γ-分泌酶活性的方法和治疗阿尔茨海默氏病的方法。

16. 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。

17. 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。

18. 发明申请

WO2008153793A3 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2008153793A3
公开(公告)日：2009-03-19
申请号：PCT/US2008006734
申请日：2008-05-28
申请人： SCHERING CORP , ZHU ZHAONING , GREENLEE WILLIAM J , HUANG XIANHAI , MCKITTRICK BRIAN A , CLADER JOHN W , MCBRIAR MARK D , PALANI ANANDAN
发明人： ZHU ZHAONING , GREENLEE WILLIAM J , HUANG XIANHAI , MCKITTRICK BRIAN A , CLADER JOHN W , MCBRIAR MARK D , PALANI ANANDAN
IPC分类号： C07D403/10 , A61K31/4166 , A61K31/517 , A61K31/519 , A61K31/5365 , A61P25/28 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D498/04 , C07D403/10 , C07D471/04 , C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing 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, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的下式杂环化合物：作为γ-分泌酶的调节剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种这样的化合物的药物制剂的方法化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

19. 发明申请

WO2007084450A3 CANNIBINOID RECEPTOR MODULATORS 审中-公开
标题翻译： CANNIBINOID接收器调制器
公开(公告)号：WO2007084450A3
公开(公告)日：2007-11-08
申请号：PCT/US2007001024
申请日：2007-01-16
申请人： SCHERING CORP , CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
发明人： CHACKALAMANNIL SAMUEL , CHELLIAH MARIAPPAN V , CLASBY MARTIN C , EAGEN KEITH A , SCOTT JACK D , WANG YUGUANG , XIA YAN , GREENLEE WILLIAM J
IPC分类号： C07D209/44 , C07C233/05 , C07C233/59 , C07D209/46 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
CPC分类号： C07D209/46 , C07C233/31 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/90 , C07D209/44 , C07D209/52 , C07D211/58 , C07D307/83 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/10
摘要： A compound having the general structure of Formula (I): Chemical formula should be inserted here as it appears on the abstract in paper form. or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
摘要翻译：具有式（I）通式结构的化合物：化学式应插入此处，如出现在摘要中的纸张形式。或其药学上可接受的盐，溶剂化物或酯可用于治疗诸如肥胖症，代谢紊乱，成瘾，中枢神经系统疾病，心血管疾病，呼吸系统疾病和胃肠疾病的疾病，病症或病症。

20. 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。

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