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1. 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

2. 发明专利

JP2011251978A Preparation and use of compound as protease inhibitor 有权
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：JP2011251978A
公开(公告)日：2011-12-15
申请号：JP2011153202
申请日：2011-07-11
申请人： Pharmacopeia Inc , Schering Corp , シェーリングコーポレイションSchering Corporation , フアーマコペイア・インコーポレイテツド
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： C07D209/44 , A61K31/4035 , A61K31/437 , A61K31/4439 , A61K31/519 , A61K45/00 , A61P9/00 , A61P9/12 , A61P13/12 , A61P25/28 , A61P31/10 , A61P31/18 , A61P33/06 , A61P35/00 , A61P43/00 , C07D401/10 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/44 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition that inhibits aspartyl protease, especially treats cardiovascular diseases, cognitive and neurodegenerative diseases.SOLUTION: This invention relates to the pharmaceutical composition represented by followings, or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof.
摘要翻译：要解决的问题：提供抑制天冬氨酰蛋白酶的药物组合物，特别是治疗心血管疾病，认知和神经退行性疾病。解决方案：本发明涉及由以下表示的药物组合物，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。版权所有（C）2012，JPO＆INPIT

3. 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

4. 发明专利

JP2009051860A New peptide as ns3-serine protease inhibitor of hepatitis c virus 审中-公开
标题翻译：新型肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
公开(公告)号：JP2009051860A
公开(公告)日：2009-03-12
申请号：JP2008275159
申请日：2008-10-27
申请人： Dendreon Corp , Schering Corp , シェーリングコーポレイションSchering Corporation , デンドレオンコーポレイション
发明人： SAKSENA ANIL K , GIRIJAVALLABHAN VIYYOOR MOOPIL , LOVEY RAYMOND G , JAO EDWIN E , BENNETT FRANK , MCCORMICK JINPING L , WANG HAIYAN , PIKE RUSSELL E , BOGEN STEPHANE L , CHAN TIN-YAU , LIU YI-TSUNG , ZHU ZHAONING , NJOROGE F GEORGE , ARASAPPAN ASHOK , PAREKH TEJAL N , GANGULY ASHIT K , CHEN KEVIN X , VENKATRAMAN SRIKANTH , VACCARO HENRY A , PINTO PATRICK A , SANTHANAM BAMA , WU WANLI , SISKA HENDRATA , HUANG YUHUA , SCOTT JEFFREY KEMP , ODILE ESTHER LEVY , LIM-WILBY MARGUERITA , TAMURA SUSAN Y
IPC分类号： A61K45/00 , C07K14/81 , A61K31/7052 , A61K31/7056 , A61K38/00 , A61K38/21 , A61K38/55 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07K5/02 , C07K5/062 , C07K5/065 , C07K5/08 , C07K5/087 , C07K7/02
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： PROBLEM TO BE SOLVED: To provide a novel hepatitis C virus (HCV) protease inhibitor, a pharmaceutical composition comprising at least one such inhibitor, a production method of the inhibitor and a method of using the inhibitor for treating hepatitis C and disorders associated therewith. SOLUTION: A new peptide compound is useful as an HCV NS3/NS4a serine protease inhibitor. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供一种新型丙型肝炎病毒（HCV）蛋白酶抑制剂，包含至少一种这样的抑制剂的药物组合物，抑制剂的制备方法和使用该抑制剂治疗丙型肝炎和病症的方法相关联。解决方案：新的肽化合物可用作HCV NS3 / NS4a丝氨酸蛋白酶抑制剂。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2010006817A Compound for curing inflammatory disorder 审中-公开
标题翻译：用于治疗炎症性疾病的化合物
公开(公告)号：JP2010006817A
公开(公告)日：2010-01-14
申请号：JP2009188147
申请日：2009-08-14
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
发明人： ZHU ZHAONING , MAZZOLA ROBERT JR , GUO ZHUYAN , LAVEY BRIAN J , SINNING LISA , KOZLOWSKI JOSEPH , MCKITTRICK BRIAN , SHIH NENG-YANG
IPC分类号： C07C259/08 , C07D249/06 , A61K31/165 , A61K31/167 , A61K31/194 , A61K31/215 , A61K31/216 , A61K31/225 , A61K31/275 , A61K31/277 , A61K31/353 , A61K31/36 , A61K31/4164 , A61K31/4192 , A61K31/428 , A61K31/435 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/02 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P31/18 , A61P33/06 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/06 , A61P37/08 , C07C61/39 , C07C62/34 , C07C69/757 , C07C233/63 , C07C235/40 , C07C255/54 , C07C279/08 , C07C311/21 , C07C311/29 , C07C317/22 , C07C323/19 , C07D213/30 , C07D213/40 , C07D213/53 , C07D213/73 , C07D213/74 , C07D215/14 , C07D215/18 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/54 , C07D233/58 , C07D233/64 , C07D249/04 , C07D271/06 , C07D277/24 , C07D277/44 , C07D277/64 , C07D295/14 , C07D295/18 , C07D311/58 , C07D311/74 , C07D317/64 , C07D401/04 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： PROBLEM TO BE SOLVED: To provide a hydroxamic acid or carboxylic acid-functional compound (which can inhibit production of a tumor necrosis factor alpha (TNF-α)), a pharmaceutical composition containing such a compound and a curing method using such a compound. SOLUTION: The compound provides a new kind of MMP and TNF-α conversion enzyme inhibitor, a pharmaceutical composition containing one or more kinds of the compound, a method for preparing a pharmaceutical formulation containing one or more kinds of such compounds and a method for curing, preventing or improving one or more symptoms of inflammation. The compound can be given in a nasal formula through local use of a proper nasal vehicle or a dermal pathway by using a dermal absorption patch known to those of skill in the art. For the administration in the form of a dermal delivery system, the dosage administration is, of course, continuous rather than intermittently over the whole administration regimen. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供异羟肟酸或羧酸官能化合物（其可以抑制肿瘤坏死因子α（TNF-α）的产生），含有这种化合物的药物组合物和使用这种化合物的固化方法一个化合物解决方案：该化合物提供了一种新型的MMP和TNF-α转化酶抑制剂，含有一种或多种化合物的药物组合物，制备含有一种或多种这类化合物的药物制剂的方法和治疗，预防或改善一种或多种炎症症状的方法。通过使用本领域技术人员已知的皮肤吸收贴剂，可以通过局部使用适当的鼻载体或真皮途径以鼻配方给药。对于以皮肤递送系统形式的给药，当然，在整个给药方案中，剂量施用是连续的而不是间歇的。版权所有（C）2010，JPO＆INPIT

6. 发明专利

JP2009292832A New peptide as ns3-serine protease inhibitor of hepatitis c virus 审中-公开
标题翻译：新型肽作为丙型肝炎病毒的NS3-丝氨酸蛋白酶抑制剂
公开(公告)号：JP2009292832A
公开(公告)日：2009-12-17
申请号：JP2009183355
申请日：2009-08-06
申请人： Dendreon Corp , Schering Corp , シェーリングコーポレイションSchering Corporation , デンドレオンコーポレイション
发明人： SAKSENA ANIL K , GIRIJAVALLABHAN VIYYOOR MOOPIL , BOGEN STEPHANE L , LOVEY RAYMOND G , JAO EDWIN E , BENNETT FRANK , MCCORMICK JINPING L , WANG HAIYAN , PIKE RUSSELL E , LIU YI-TSUNG , CHAN TIN-YAU , ZHU ZHAONING , ARASAPPAN ASHOK , CHEN KEVIN X , VENKATRAMAN SRIKANTH , PAREKH TEJAL N , PINTO PATRICK A , SANTHANAM BAMA , NJOROGE F GEORGE , GANGULY ASHIT K , VACCARO HENRY A , SCOTT JEFFREY KEMP , ODILE ESTHER LEVY , LIM-WILBY MARGUERITA , TAMURA SUSAN Y
IPC分类号： C07K7/06 , C12N9/99 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K31/7052 , A61K38/00 , A61K38/05 , A61K38/21 , A61K38/55 , A61K45/00 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07C205/51 , C07C229/00 , C07D209/02 , C07K5/02 , C07K5/103 , C07K7/02 , C07K7/04
CPC分类号： C07K7/06 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K38/05 , C07C205/51 , C07K5/101 , C07K7/02 , A61K2300/00
摘要： PROBLEM TO BE SOLVED: To provide a new peptide compound having HCV protease inhibition activity and a method for producing the compound, in addition, a pharmaceutical composition containing the compound and a method for using them in treating diseases associated with HCV proteases. SOLUTION: A new class of HCV protease inhibitors, a pharmaceutical composition containing one or more kinds of the compounds, a method for producing the pharmaceutical composition containing one or more kinds of the compounds, a method for treating, preventing or improving one or more symptoms of hepatitis C, a method for controlling the interaction between HCV polypeptides and HCV proteases, a compound inhibiting HCV NS3/NS4a serine protease activity and a peptide compound including an amino acid sequence from P3 to P2' are disclosed. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供具有HCV蛋白酶抑制活性的新型肽化合物及其制备方法，此外，含有该化合物的药物组合物及其用于治疗与HCV蛋白酶相关疾病的方法。解决方案：新一类HCV蛋白酶抑制剂，含有一种或多种化合物的药物组合物，含有一种或多种化合物的药物组合物的制备方法，治疗，预防或改善一种或更多的丙型肝炎症状，控制HCV多肽和HCV蛋白酶之间相互作用的方法，抑制HCV NS3 / NS4a丝氨酸蛋白酶活性的化合物和包含P3至P2'氨基酸序列的肽化合物。版权所有（C）2010，JPO＆INPIT

7. 发明专利

JP2008201784A Aspartyl protease inhibitor 审中-公开
标题翻译： ASPARTYL PROTEASE抑制剂
公开(公告)号：JP2008201784A
公开(公告)日：2008-09-04
申请号：JP2008055596
申请日：2008-03-05
申请人： Schering Corp , シェーリングコーポレイションSchering Corporation
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： C07D239/70 , A61K31/517 , A61K31/519 , A61P19/04 , A61P21/04 , A61P25/28 , A61P31/18 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/04
CPC分类号： C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide an aspartyl protease inhibitor for treating cognitive diseases or neurodegenerative diseases. SOLUTION: The present invention provides a compound represented by the formula or a stereoisomer, tautomer or pharmaceutically acceptable salt or solvate thereof, wherein b is 1-5; c is 0-5; W is a bond, -C(=O)- or the like; R is 1-5C alkyl or the like; R 1 , R 2 , R 3 , R 5 and R 6 are each H, an alkyl, an arylalkyl or the like. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供用于治疗认知疾病或神经变性疾病的天冬氨酰蛋白酶抑制剂。解决方案：本发明提供由下式表示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b为1-5; c为0-5; W是键，-C（= O） - 等; R为1-5C烷基等; R 1 ，R 2 ，R 3 ，R 5 和R 6 每个H，烷基，芳基烷基等。版权所有（C）2008，JPO＆INPIT

8. 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

9. 发明专利

JP2007297410A Muscarinic antagonist 审中-公开
标题翻译：心理拮抗剂
公开(公告)号：JP2007297410A
公开(公告)日：2007-11-15
申请号：JP2007203608
申请日：2007-08-03
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： MCKITTRICK BRIAN A , GUO GUIHUA , ZHU ZHAONING , YE YUANZAN
IPC分类号： C07D211/34 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/4525 , A61K31/453 , A61K31/4545 , A61K31/46 , A61K45/00 , A61P25/00 , A61P25/28 , A61P43/00 , C07D211/58 , C07D401/12 , C07D405/04 , C07D451/04
CPC分类号： C07D451/04 , C07D211/34 , C07D405/04
摘要： PROBLEM TO BE SOLVED: To provide a muscarinic antagonist which is a piperidine derivative useful for treating cognitive disorders such as Alzheimer's disease.
SOLUTION: The compound is an amide derivative of a 1,4 di-substituted piperidine compound of formula (I) (wherein R
1 is an optionally substituted cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or heteroaryl; R
2 is H, an alkyl or an optionally substituted cycloalkyl, cycloalkylalkyl, heterocycloalkyl, bridged cycloalkyl or bridged heterocycloalkyl; R
3 is an alkyl or -CH
2 OH; R
4 is H or an alkyl; R
5 is 1-4 substituents each independently chosen from the group consisting of H, an alkyl, a halogen, -OH, an alkoxy, CF
3 , -CN, -CO
2 R
4 , -CONHR
4 , -SO
2 NHR
4 , -NHSO
2 R
4 and -NHC(O)R
4 ; and R
6 is 1-4 substituents each independently chosen from the group consisting of H, an alkyl, a halogen, -OH, an alkoxy, CF
3 , -NH
2 , an alkylamino, phenyl, an alkylenedioxy and an alkoxycarbonyl) or a pharmaceutically acceptable salt, ester or solvate thereof.
COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供毒蕈碱拮抗剂，其是用于治疗认知障碍如阿尔茨海默氏病的哌啶衍生物。解决方案：该化合物是式（I）的1,4-二取代的哌啶化合物的酰胺衍生物（其中R 1 SP 1是任选取代的环烷基，环烷基烷基，芳基，芳基烷基或杂芳基 R 2是H，烷基或任选取代的环烷基，环烷基烷基，杂环烷基，桥连环烷基或桥连杂环烷基; R 3是烷基或-CH 2 S 2 OH; R SP 4是H或烷基; R 6是独立地选自H，烷基，卤素的1-4个取代基，-OH，烷氧基，CF 3 SB，-CN，-CO 2 SBR，SPON 4，SPON 4，，-SO 2 SBR，NHSO 2，R 4，和-NHC（O）R SP 3， 4 ; R 6是独立地选自H，烷基，卤素，-OH，烷氧基，CF 3，苯基，烷基氨基，苯基，亚烷基二氧基和烷氧基羰基）或其药学上可接受的盐，酯或溶剂合物。版权所有（C）2008，JPO＆INPIT

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