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1. 发明专利

JP2013032389A Novel peptides as ns3-serine protease inhibitors of hepatitis c virus 有权
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：JP2013032389A
公开(公告)日：2013-02-14
申请号：JP2012243691
申请日：2012-11-05
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. , Dendreon Corp , 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 , A61K31/7056 , A61K38/00 , A61K38/21 , A61P31/14 , A61P43/00 , C07K5/02 , C07K5/08 , C07K5/087 , C07K7/02 , C12N9/99
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： PROBLEM TO BE SOLVED: To provide novel hepatitis C virus ("HCV") protease inhibitors, pharmaceutical compositions containing one or more such inhibitors, methods of preparing such inhibitors and methods of using such inhibitors to treat hepatitis C and related disorders.SOLUTION: This invention discloses novel peptide compounds as inhibitors of the HCV NS3/NS4a serine protease.
摘要翻译：要解决的问题：提供新型丙型肝炎病毒（“HCV”）蛋白酶抑制剂，含有一种或多种这样的抑制剂的药物组合物，制备这种抑制剂的方法和使用这种抑制剂治疗丙型肝炎和相关病症的方法。解决方案：本发明公开了作为HCV NS3 / NS4a丝氨酸蛋白酶抑制剂的新型肽化合物。版权所有（C）2013，JPO＆INPIT

2. 发明专利

AU2009210423B2 Novel peptides as NS3-serine protease inhibitors of hepatitis C virus 未知
公开(公告)号：AU2009210423B2
公开(公告)日：2012-11-15
申请号：AU2009210423
申请日：2009-08-21
申请人： DENDREON CORP , MERCK SHARP & DOHME
发明人： SAKSENA ANIL K , GIRIJAVALLABHN VIYYOOR M , LOVEY RAYMOND G , JAO EDWIN , 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 , GANGULY ASHIT K , CHEN KEVIN X , VENKATRAMAN SRIKANTH , VACCARO HENRY A , PINTO PATRICK A , SANTHANAM BAMA , KEMP SCOTT JEFFREY , LEVY ODILE ESTHER , LIM-WILBY MARGUERITA , TAMURA SUSAN Y , WU WANLI , HENDRATA SISKA , HUANG YUHUA , WONG JESSE K , NAIR LATHA G
IPC分类号： C07K7/02 , C12N9/99 , A61K31/70 , A61K38/00 , A61K38/21 , A61P1/16 , A61P31/14 , A61P43/00 , C07K5/02 , C07K5/023
摘要： Abstract The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising 5 such compounds as well as methods of using them to treat disorders associated with the HCV protease.

3. 发明专利

AU2001276988B2 Peptides as NS3-serine protease inhibitors of hepatitis C virus 未知
公开(公告)号：AU2001276988B2
公开(公告)日：2007-01-25
申请号：AU2001276988
申请日：2001-07-19
申请人： DENDREON CORP , MERCK SHARP & DOHME
发明人： PIKE RUSSELL E , GIRIJAVALLABHAN VIYYOOR MOOPIL , PINTO PATRICK A , LIU YI-TSUNG , TAMURA SUSAN Y , LOVEY RAYMOND G , SANTHANAM BAMA , CHAN TIN-YAU , SAKSENA ANIL K , CHEN KEVIN X , LEVY ODILE ESTHER , HENDRATA SISKA , VENKATRAMAN SRIKANTH , BOGEN STEPHANE L , ZHU ZHAONING , WANG HAIYAN , KEMP SCOTT JEFFREY , VACCARO HENRY A , PAREKH TEJAL N , HUANG YUHUA , GANGULY ASHIT K , JAO EDWIN E , ARASAPPAN ASHOK , LIM-WILBY MARGUERITA , WU WANLI , BENNETT FRANK , NJOROGE F GEORGE , CORMICK JINPING L MC
IPC分类号： A61K45/00 , A61K31/7056 , A61K38/00 , A61K38/08 , A61K38/21 , A61P31/14 , A61P43/00 , C07K5/02 , C07K5/08 , C07K5/087 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

5. 发明专利

SK288064B6 Peptide compounds, pharmaceutical compositions comprising them and their use 未知
公开(公告)号：SK288064B6
公开(公告)日：2013-04-03
申请号：SK752003
申请日：2001-07-19
申请人： MERCK SHARP & DOHME , DENDREON CORP
发明人： SAKSENA ANIL K , GIRIJAVALLABHAN VIYYOOR MOOPIL , LOVEY RAYMOND G , JAO EDWIN E , BENNETT FRANK , MC CORMICK JINPING L , WANG HAIYAN , PIKE RUSSELL E , BOGEN STEPHANE L , CHAN TIN-YAU , LIU YI-TSUNG , ZHU ZHAONING , NJOROGE GEORGE F , ARASAPPAN ASHOK , PAREKH TEJAL N , GANGULY ASHIT K , CHEN KEVIN X , VENKATRAMAN SRIKANTH , VACCARO HENRY A , PINTO PATRICK A , SANTHANAM BAMA , WU WANLI , HENDRATA SISKA , HUANG YUHUA , KEMP SCOTT JEFFREY , LEVY ODILE ESTHER , LIM-WILBY MARGUERITA , TAMURA SUSAN Y
IPC分类号： A61K45/00 , C07K5/02 , A61K31/7056 , A61K38/00 , A61K38/08 , A61K38/21 , A61P31/14 , A61P43/00 , C07K5/08 , C07K5/087 , C07K7/02
摘要： Described are peptide compounds of the general formula (I) wherein the meanings of substituents are mentioned in the claims, pharmaceutical compositions comprising such compounds as well as their use in treating disorders associated with HCV protease. The compounds have the HCV protease inhibitory activity.

6. 发明专利

JP2013014628A 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：JP2013014628A
公开(公告)日：2013-01-24
申请号：JP2012232894
申请日：2012-10-22
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. , Pharmacopeia Llc , ファーマコピア, エルエルシー
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 , A61K31/121 , A61K31/13 , A61K31/192 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/404 , A61K31/4168 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/498 , A61K31/505 , A61K31/513 , A61K31/527 , A61K31/5377 , A61K31/5395 , A61K31/541 , A61K31/551 , A61K31/695 , A61K45/00 , A61P9/00 , A61P25/28 , A61P29/00 , A61P31/18 , A61P33/02 , A61P43/00 , C07D239/22 , C07D239/26 , C07D239/70 , C07D243/04 , C07D263/28 , C07D273/04 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/107 , C07D495/04 , C07D495/10 , C07F7/10
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： PROBLEM TO BE SOLVED: To provide heterocyclic aspartyl protease inhibitors, pharmaceutical compositions comprising the compounds, their use in the treatment of cardiovascular diseases, cognitive and neurodegenerative diseases, and their use as inhibitors of the Human Immunodeficiency Virus, plasmepsins, cathepsin D and protozoal enzymes.SOLUTION: 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 are methods 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：要解决的问题：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，其用于治疗心血管疾病，认知和神经退行性疾病及其作为人免疫缺陷病毒，血浆素，组织蛋白酶D抑制剂的用途和原生动物酶。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; 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m1激动剂或m2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）2013，JPO＆INPIT

7. 发明公开

EP2773202A4 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMASEKRETASEMODULATOREN
公开(公告)号：EP2773202A4
公开(公告)日：2015-06-17
申请号：EP12845486
申请日：2012-10-26
申请人： MERCK SHARP & DOHME
发明人： GREENLEE WILLIAM , PISSARNITSKI DMITRI , ZHAO ZHIQIANG , ZHU ZHAONING
IPC分类号： A01N43/00 , A61K31/42 , A61P25/28 , C07D413/10 , C07D413/14
CPC分类号： C07D413/10 , C07D413/14

10. 发明专利

ES2436795T3 Inhibidores heterocíclicos de aspartil proteasa, preparación y uso de los mismos 未知
公开(公告)号：ES2436795T3
公开(公告)日：2014-01-07
申请号：ES11157371
申请日：2006-06-12
申请人： PHARMACOPEIA LLC , MERCK SHARP & DOHME
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 , C07D471/04 , C07D487/04
摘要： Un compuesto para su uso en la inhibición de aspartil proteasa en un paciente, en el que el compuesto es un compuesto que tiene la fórmula estructural **Fórmula** o un estereoisómero, tautómero, o sal o solvato farmacéuticamente aceptable del mismo, en la que R1 está seleccionado independientemente del grupo que consiste en H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, heterocicloalquilo, heterocicloalquilalquilo, arilo, arilalquilo, heteroarilo, heteroarilalquilo, halo, -CN, -OR15, -C (O) R15, -C (O) OR15, -C (O) N (R15) (R16), - S (O)0-2R15, -S (O) N (R15) (R16), - S (O)1-2- N (R15) (R16), S (O)2N (R15) (R16), - C (>=NOR15) R16, -P (O) (OR15) (OR16), - N (R15) (R16), - N (R15) C (O) R16, -N (R15) S (O) R16, -N (R15) S (O)2R16, -N (R15) S (O)2N (R16) (R17), - N (R15) S (O) N (R16) (R17), - N (R15) C (O) N (R16) (R17), y- N (R15) C (O) OR16; R3 está seleccionado del grupo que consiste en H, alquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo, heterocicloalquilalquilo, arilcicloalquilalquilo, heteroarilcicloalquilalquilo, arilheterocicloalquilalquilo, heteroarilheterocicloalquilalquilo, cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, alquenilo, arilalquenilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, alquinilo, arilalquinilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo, heterocicloalquenilarilo, halo, -CH2- O- Si (R9) (R10) (R19), - SH, -CN, -OR9, -C (O) R8, -C (O) OR9, -C (O) N (R11) (R12), - SR19, -S (O) N (R11) (R12), - S (O)2N (R11) (R12), - N (R11) (R12), - N (R11) C (O) R8, -N (R11) S (O) R10, -N (R11) S (O)2R10, -N (R11) C (O) N (R12) (R13), - N (R11) C (O) OR9 y- C (>=NOH) R8; R4 está seleccionado del grupo que consiste en cicloalquilo, arilcicloalquilo, heteroarilcicloalquilo, heterocicloalquilo, arilheterocicloalquilo, heteroarilheterocicloalquilo, cicloalquenilo, arilcicloalquenilo, heteroarilcicloalquenilo, heterocicloalquenilo, arilheterocicloalquenilo, heteroarilheterocicloalquenilo, arilo, cicloalquilarilo, heterocicloalquilarilo, heterocicloalquenilarilo, heteroarilo, cicloalquilheteroarilo, heterocicloalquilheteroarilo, cicloalquenilarilo y heterocicloalquenilarilo; y opcionalmente, (i) R3 y R4, junto con el carbono al que están unidos, forman un anillo de cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilo, arilo o heteroarilo de 3 a 8 miembros que tiene de 0 a 3 heteroátomos seleccionados independientemente del grupo que consiste en O, N, S, y- N (R) -, que está opcionalmente sustituido con de 1 a 5 grupos R14 y/o oxo, cuando dicho anillo es un anillo de cicloalquilo, cicloalquenilo, heterociclilo, o heterociclenilo; o (ii) R3 y R4, junto con el carbono al que están unidos forman uno de los siguientes grupos multicíclicos: **Fórmula**

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