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1. 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

4. 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**

5. 发明专利

AU2013202193A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 未知
公开(公告)号：AU2013202193A1
公开(公告)日：2013-05-02
申请号：AU2013202193
申请日：2013-03-28
申请人： MERCK SHARP & DOHME , 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 , 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 , 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
摘要： Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof. Also disclosed is the 5 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, cathespin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (1) 10 in combination with a chlolinesterase inhibitor or a muscarinic antagonist. 30770551 (GHMatters) P60878.AU.1

6. 发明专利

AU2013201438A1 HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS 未知
公开(公告)号：AU2013201438A1
公开(公告)日：2013-03-28
申请号：AU2013201438
申请日：2013-03-07
申请人： MERCK SHARP & DOHME , 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 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
摘要： NeR2 X N Rl R4(I) 5 Disclosed are compounds of the formula (1) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(0) 2-, -C(=O)-, -0-, -C(R6)(R')-, -N(R5) or -C(=N(R5))-; 10 X is -0-, -N(R5 )- or -C(R 6 )(R7)-; provided that when X is -0-, U is not -0-, -S(O)-, -S(0) 2-, -C(=0)- or -C(=NR5)-; U is a bond, -S(0)-, -S(0)2-, -C(0)-, -0-, -P(0)(OR15 )-, -C(=NR 5)-, -(C(R6)(R7))b- or -N(R5)-; wherein b is 1 or 2; provided that when W is -S(0)-, -S(0) 2-, -0-, or -N(R5)-, U is not -S(0)-, -S(0) 2-, -0-, or -N(R5)-; provided that 15 when X is -N(R5)- and W is -S(0)-, -S(0)2-, -0-, or -N(R5)-, then U is not a bond; and R1, R2, R3, R4, R , R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula (1). 20 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 25 using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist. 41216141 (GHM~ar) P8809.AU 1

8. 发明专利

AU2008219071B2 Heterocyclic aspartyl protease inhibitors 未知
公开(公告)号：AU2008219071B2
公开(公告)日：2013-03-28
申请号：AU2008219071
申请日：2008-02-20
申请人： MERCK SHARP & DOHME , PHARMACOPEIA LLC
发明人： BABU SURESH D , YE YUANZAN C , PAN JIANPING , SHAO YUEFEI , ZHU ZHAONING , LI GUOQING , WANG LINGYAN , VOIGT JOHANNES H , MCKITTRICK BRIAN , SMITH ELIZABETH M , MORRIS MICHELLE L , HUNTER RACHAEL C , MAZZOLA JR ROBERT D , HUANG YING , GREENLEE WILLIAM J , WU YUSHENG , STAMFORD ANDREW , SAIONZ KURT W , MISIASZEK JEFFREY A , ISERLOH ULRICH , QIAN GANG , STRICKLAND COREY , LAI GAIFA , LIU XIAOXIANG , DUO JINGQI , GUO TAO , GU HUIZHONG , CUMMING JARED N , TADESSE DAWIT , SUN ZHONG-YUE , QU CHUANXING , CALDWELL JOHN , LE THUY X H
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
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)

9. 发明专利

AU2012200273A8 Heterocyclic aspartyl protease inhibitors 未知
公开(公告)号：AU2012200273A8
公开(公告)日：2012-02-16
申请号：AU2012200273
申请日：2012-01-17
申请人： MERCK SHARP & DOHME , 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 , 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 , 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
摘要： Disclosed are compounds of the formula (1) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof. Also disclosed is the 5 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, cathespin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula (1) 10 in combination with a chlolinesterase inhibitor or a muscarinic antagonist. 3077055 1 (GHMatters) P60878.AU.1

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