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21. 发明授权

US4929641B1 Mercapto-acylamino acid antihypertensives 失效
标题翻译：巯基 - 酰氨基酸抗高血压药
公开(公告)号：US4929641B1
公开(公告)日：1994-08-30
申请号：US19243588
申请日：1988-05-11
申请人： SCHERING CORP
发明人： HASLANGER MARTIN F , NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： C07C323/59 , C07C327/32 , C07C317/00 , C07C321/00 , C07C323/00 , C07C325/00 , C07C335/00 , C07C381/00
CPC分类号： C07C323/59 , C07C327/32

22. 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。}

23. 发明申请

WO2008033464A3 AZETIDINONE DERIVATIVES FOR THE TREATMENT OF DISORDERS OF THE LIPID METABOLISM 审中-公开
标题翻译：用于治疗脂肪代谢紊乱的AZETIDINONE衍生物
公开(公告)号：WO2008033464A3
公开(公告)日：2008-05-15
申请号：PCT/US2007019930
申请日：2007-09-13
申请人： SCHERING CORP , ASLANIAN ROBERT G , BENNETT CHAD E , BURNETT DUANE A , CHAN TIN-YAU , KISELGOF EUGENIA Y , KNUTSON CHAD E , HARRIS JOEL M , MC KITTRICK BRIAN A , PALANI ANANDAN , SMITH ELIZABETH M , VACCARO HENRY M , XIAO DONG , KIM HYUNJIN M
发明人： ASLANIAN ROBERT G , BENNETT CHAD E , BURNETT DUANE A , CHAN TIN-YAU , KISELGOF EUGENIA Y , KNUTSON CHAD E , HARRIS JOEL M , MC KITTRICK BRIAN A , PALANI ANANDAN , SMITH ELIZABETH M , VACCARO HENRY M , XIAO DONG , KIM HYUNJIN M
IPC分类号： C07D471/10 , A61K31/438 , A61P3/00
CPC分类号： C07D471/10
摘要： The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
摘要翻译：本发明涉及氮杂环丁酮衍生物，包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的氮杂环丁酮衍生物。

24. 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。

25. 发明申请

WO0032578A8 BENZIMIDAZOLE COMPOUNDS THAT ARE VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯并咪唑化合物是维生素C受体拮抗剂
公开(公告)号：WO0032578A8
公开(公告)日：2002-02-07
申请号：PCT/US9926023
申请日：1999-11-29
申请人： SCHERING CORP
发明人： NEUSTADT BERNARD R , SMITH ELIZABETH M
IPC分类号： C07D235/16 , A61K31/4184 , A61P9/10 , A61P19/10 , A61P27/02 , A61P35/00 , A61P43/00 , C07D235/10 , C07D235/14 , C07D405/12
CPC分类号： C07D405/12 , C07D235/14
摘要： The present invention provides compounds having formula (I) wherein n, p, q and r are each independently selected from 0 or 1; a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms; Y and Y' each independently represents 1-4 optional substituents selected from alkyl, alkoxy, halo, -CF3, and -C(O)OH; R , R , R and R are H or specified substituents; R , R , R , R , R , R , R and R are independently selected from H or C1-C3 alkyl; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. Also provided are methods of using these compounds for treating vitronectin-mediated disorders, e.g., cancer, retinopathy, artherosclerosis, vascular restenosis, and osteoporosis.
摘要翻译：本发明提供具有式（I）的化合物，其中n，p，q和r各自独立地选自0或1; a，b，c和d各自独立地表示碳原子或氮原子，条件是a，b，c和d中不超过两个是氮原子; Y和Y'各自独立地表示1-4个选自烷基，烷氧基，卤素，-CF 3和-C（O）OH的任选取代基; R 1，R 2，R 3和R 4是H或特定的取代基; R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12独立地选自H或C 1 -C 3烷基; 或其不可生物酯，或其药学上可接受的盐。还提供了使用这些化合物治疗玻连蛋白介导的病症例如癌症，视网膜病变，动脉粥样硬化，血管再狭窄和骨质疏松症的方法。

26. 发明专利

JP2012097122A Heterocyclic aspartyl protease inhibitor 审中-公开
标题翻译：异宿氨酸蛋白酶抑制剂
公开(公告)号：JP2012097122A
公开(公告)日：2012-05-24
申请号：JP2012034364
申请日：2012-02-20
申请人： Pharmacopeia Drug Discovery Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコペイアドラッグディスカバリー, インコーポレイテッド
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： C07D233/88 , A61K31/4164 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/5377 , A61P9/12 , A61P13/12 , A61P25/28 , A61P31/10 , A61P31/18 , A61P33/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07D235/02 , C07D239/22 , C07D239/47 , C07D271/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
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： PROBLEM TO BE SOLVED: To provide: heterocyclic aspartyl protease inhibitors; pharmaceutical compositions comprising the compounds; and their using method in the treatment of cardiovascular diseases, cognitive and neurodegenerative diseases.SOLUTION: 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：待解决的问题：提供：杂环天冬氨酰蛋白酶抑制剂; 包含该化合物的药物组合物; 及其使用方法治疗心血管疾病，认知和神经退行性疾病。解决方案：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治疗认知或神经退行性疾病的方法。版权所有（C）2012，JPO＆INPIT

27. 发明专利

JP2008174570A Heterocyclic aspartyl protease inhibitor 审中-公开
标题翻译：异宿氨酸蛋白酶抑制剂
公开(公告)号：JP2008174570A
公开(公告)日：2008-07-31
申请号：JP2008079293
申请日：2008-03-25
申请人： Pharmacopeia Drug Discovery Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコペイアドラッグディスカバリー, インコーポレイテッド
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： C07D233/88 , A61K31/4164 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/5377 , A61P9/12 , A61P13/12 , A61P25/28 , A61P31/10 , A61P31/18 , A61P33/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07D235/02 , C07D239/22 , C07D239/47 , C07D271/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
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： PROBLEM TO BE SOLVED: To provide an aspartyl protease inhibitor. SOLUTION: Disclosed are compounds of the 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 in combination with a cholinesterase inhibitor or a muscarinic antagonist. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供天冬氨酰蛋白酶抑制剂。解决方案：公开了式（I）的化合物。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。还公开了使用该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。版权所有（C）2008，JPO＆INPIT

28. 发明专利

JP2011132261A Heterocyclic aspartyl protease inhibitor 有权
标题翻译：异宿氨酸蛋白酶抑制剂
公开(公告)号：JP2011132261A
公开(公告)日：2011-07-07
申请号：JP2011082314
申请日：2011-04-01
申请人： Pharmacopeia Drug Discovery Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , ファーマコペイアドラッグディスカバリー, インコーポレイテッド
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： C07D233/88 , A61K31/27 , A61K31/4168 , A61K31/4425 , A61K31/445 , A61K31/473 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P9/00 , A61P25/28 , A61P31/18 , A61P33/02 , A61P43/00 , C07D235/02 , C07D239/22 , C07D271/06 , C07D271/07 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
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： PROBLEM TO BE SOLVED: To provide heterocyclic aspartyl protease inhibitors, pharmaceutical compositions comprising the compounds, and the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases using the compounds.
SOLUTION: Compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof are disclosed. In addition, 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, plasmepin, cathepsin D and protozoal enzymes are disclosed. Furthermore, methods of treating cognitive or neurodegenerative diseases using the compounds of formula (I) in combination with a cholinesterase inhibitor or a muscarinic antagonist are disclosed.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供杂环天冬氨酰蛋白酶抑制剂，包含该化合物的药物组合物，以及使用该化合物治疗心血管疾病，认知和神经变性疾病的方法。解决方案：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。此外，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，plasmepin，组织蛋白酶D和原生动物酶的方法。此外，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变性疾病的方法。版权所有（C）2011，JPO＆INPIT

29. 发明专利

AU2005317204B2 Heterocyclic aspartyl protease inhibitors 未知
公开(公告)号：AU2005317204B2
公开(公告)日：2011-02-17
申请号：AU2005317204
申请日：2005-06-09
申请人： MERCK SHARP & DOHME , PHARMACOPEIA INC
发明人： VOIGT JOHANNES H , ISERLOH ULRICH , TADESSE DAWIT , STAMFORD ANDREW , GUO TAO , QIAN GANG , GREENLEE WILLIAM J , SMITH ELIZABETH M , LE THUY X H , GU HUIZHONG , WU YUSHENG , STRICKLAND COREY , HUNTER RACHAEL C , CALDWELL JOHN , ZHU ZHAONING , BABU SURESH D , YE YUANZAN C , CUMMING JARED , SAIONZ KURT W , WANG LINGYAN , SUN ZHONG-YUE , MORRIS MICHELLE L , MAZZOLA ROBERT , MCKITTRICK BRIAN
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.

30. 发明专利

CA2678958C HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 未知
公开(公告)号：CA2678958C
公开(公告)日：2014-10-14
申请号：CA2678958
申请日：2008-02-20
申请人： SCHERING CORP , PHARMACOPEIA LLC
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 D JR , 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： C07D409/04 , A61K31/4168 , A61K31/4439 , A61K31/4709 , A61K31/513 , A61K31/5395 , A61P25/28 , C07D233/88 , C07D239/22 , C07D273/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14 , C07D413/04 , C07D417/04
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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