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21. 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

22. 发明申请

WO2014172188A2 4-PYRIDONE DERIVATIVE COMPOUNDS AND USES THEREOF AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译： 4-吡啶酮衍生化合物及其作为HIV整合酶抑制剂的用途
公开(公告)号：WO2014172188A2
公开(公告)日：2014-10-23
申请号：PCT/US2014033720
申请日：2014-04-11
申请人： MERCK SHARP & DOHME , GRAHAM THOMAS H , WAI JOHN S , STAMFORD ANDREW , LIU WENSHENG
发明人： GRAHAM THOMAS H , WAI JOHN S , STAMFORD ANDREW , LIU WENSHENG
IPC分类号： A61K31/55 , C07D487/04
CPC分类号： C07D491/147 , A61K31/4985 , A61K31/55 , A61K45/06 , C07D471/04 , C07D471/14 , C07D491/14 , C07D491/20 , A61K2300/00
摘要： The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R1, R2, and R3 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridone Compound, and methods of using the 4-Pyridone Compounds for treating or preventing HIV infection in a subject or the clinical manifestations thereof.
摘要翻译：本发明涉及式（I）的4-吡啶酮化合物; 和其药学上可接受的盐和前药，其中A，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种4-吡啶酮化合物的组合物，以及使用4-吡啶酮化合物治疗或预防受试者的HIV感染或其临床表现的方法。

23. 发明申请

WO2012142093A3 2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译： 2'-氰基取代的核苷衍生物及其用于治疗病毒性疾病的方法
公开(公告)号：WO2012142093A3
公开(公告)日：2013-02-07
申请号：PCT/US2012033028
申请日：2012-04-11
申请人： MERCK SHARP & DOHME , GIRIJAVALLABHAN VINAY , NJOROGE F GEORGE , BOGEN STEPHANE , KEREKES ANGELA , BENNETT FRANK , HUANG YING , NAIR LATHA , PISSARNITSKI DMITRI , VERMA VISHAL , DANG QUN , DAVIES IAN , OLSEN DAVID B , STAMFORD ANDREW , VACCA JOSEPH P
发明人： GIRIJAVALLABHAN VINAY , NJOROGE F GEORGE , BOGEN STEPHANE , KEREKES ANGELA , BENNETT FRANK , HUANG YING , NAIR LATHA , PISSARNITSKI DMITRI , VERMA VISHAL , DANG QUN , DAVIES IAN , OLSEN DAVID B , STAMFORD ANDREW , VACCA JOSEPH P
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00
CPC分类号： C07H19/16 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/11 , C07H19/20 , C07H19/207 , C07H19/213
摘要： The present invention relates to 2'-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3are as defined herein. The present invention also relates to compositions comprising at least one 2'-Cyano Substituted Nucleoside Derivative, and methods of using the 2'-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-氰基取代的核苷衍生物及其药学上可接受的盐，其中B，X，R 1，R 2和R 3如本文所定义。本发明还涉及包含至少一种2'-氰基取代的核苷衍生物的组合物，以及使用2'-氰基取代的核苷衍生物治疗或预防患者HCV感染的方法。

24. 发明申请

WO2014014794A3 MINERALOCORTICOID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：矿物胆碱受体拮抗剂
公开(公告)号：WO2014014794A3
公开(公告)日：2015-07-16
申请号：PCT/US2013050427
申请日：2013-07-15
申请人： MERCK SHARP & DOHME , CERNAK TIMOTHY A , DYKSTRA KEVIN D , SHEN DONG-MING , LIU KUN , STAMFORD ANDREW , TAN JOHN QIANG
发明人： CERNAK TIMOTHY A , DYKSTRA KEVIN D , SHEN DONG-MING , LIU KUN , STAMFORD ANDREW , TAN JOHN QIANG
IPC分类号： A61K31/404 , A61K31/416 , C07D209/10 , C07D231/56 , C07D403/06
CPC分类号： A61K31/416 , A61K45/06 , C07D231/56 , A61K2300/00
摘要： The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosteronemediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula (I), to their potential use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
摘要翻译：本发明涉及式（I）化合物及其药学上可接受的盐，其可用于治疗醛固酮增多症。本发明还涉及该化合物的具体非对映异构体和对映异构体，制备式（I）化合物的方法，以及其用于治疗和预防上述疾病和用于制备用于该目的的药物和药物组合物其包含式（I）的化合物。

25. 发明公开

EP2696681A4 2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 无效转让
标题翻译： 2'-取代的核苷及使用方法进行病毒疾病治疗
公开(公告)号：EP2696681A4
公开(公告)日：2014-10-01
申请号：EP12771566
申请日：2012-04-11
申请人： MERCK SHARP & DOHME
发明人： GIRJAVALLABHAN VINAY , NJOROGE F GEORGE , BOGEN STEPHANE , VERMA VISHAL , BENNETT FRANK , KEREKES ANGELA , ARASAPPAN ASHOK , PISSARNITSKI DIMITRI , DANG QUN , DAVIES IAN , OLSEN DAVID B , STAMFORD ANDREW , VACCA JOSEPH P
IPC分类号： C07H21/02 , A61K31/7042 , A61K31/7068 , A61K31/7072 , A61K45/06 , C07H19/06 , C07H19/10 , C07H19/11 , C07H19/12 , C07H19/16 , C07H19/20 , C07H19/207 , C07H19/213
CPC分类号： A61K31/7072 , A01N47/36 , A61K31/7042 , A61K31/7068 , A61K45/06 , C07H17/02 , C07H19/10 , C07H19/11 , C07H19/207 , C07H19/213 , A01N2300/00 , A01N43/54 , A01N43/56 , A01N43/653 , A01N43/76 , A01N43/82 , A01N43/84 , A01N43/90
摘要： The present invention relates to 2′-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Substituted Nucleoside Derivative, and methods of using the 2′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的2'-取代的核苷衍生物：及其药学上可接受的盐，worin A，B，X，R 1，R 2和R 3如所定义。因此，本发明涉及组合物，其包含至少一个2'-取代的核苷衍生物，以及使用该2'-取代的核苷衍生物用于治疗或在患者中预防HCV感染症的方法。

26. 发明公开

EP2504010A4 FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：稠合双环嘧啶衍生物及其使用方法
公开(公告)号：EP2504010A4
公开(公告)日：2013-04-17
申请号：EP10832046
申请日：2010-11-16
申请人： MERCK SHARP & DOHME
发明人： NEELAMKAVIL SANTHOSH FRANCIS , BISWAS DIPSHIKHA , CHACKALAMANNIL SAMUEL , NEUSTADT BERNARD R , STAMFORD ANDREW , LIU HONG
IPC分类号： A61K31/4965 , A61K31/519 , A61K45/06 , A61P3/04 , C07D471/04 , C07D487/04 , C07D498/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/4965 , A61K31/519 , A61K45/06 , C07D498/04 , C07D519/00 , A61K2300/00

27. 发明专利

ES2789756T3 Moduladores alostéricos de 6,7-dihidro-5H-pirrolo[3,4-b]piridin-5-ona del receptor de acetilcolina muscarínico M4 未知
公开(公告)号：ES2789756T3
公开(公告)日：2020-10-26
申请号：ES16826815
申请日：2016-12-21
申请人： MERCK SHARP & DOHME , MSD R&D CHINA CO LTD
发明人： BAO JIANMING , GAO XIAOLEI , KNOWLES SANDRA , LI CHUNSING , LO MICHAEL MAN-CHU , MAZZOLA ROBERT , ONDEYKA DEBRA , STAMFORD ANDREW , ZHANG FENGQI
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00 , C07D519/00 , C07F9/22
摘要： Un compuesto de fórmula I: **(Ver fórmula)** en donde: R1 se selecciona del grupo que consiste en: (1) hidrógeno; (2) -alquilo C1-6, que está sin sustituir o sustituido con sustituyentes seleccionados entre el grupo que consiste en: hidroxi, flúor, -CN, -O-alquilo C1-6, cicloalquilo C3-6, biciclo[1.1.1]pentano, tetrahidrofuranilo, fenilo, piridilo, oxazolilo, -NH2, -NH(-alquilo C1-6), -N(-alquilo C1-6)2 y -N(C=O)-alquilo C1-6, en donde el alquilo C1-6 o el cicloalquilo C3-6 está sin sustituir o sustituido con sustituyentes seleccionados entre el grupo que consiste en: flúor, ciano, CF3, alquilo C1-6 u -O-alquilo C1-6; (3) un anillo fenilo, heteroarilo o heterociclilo, en edonde el anillo fenilo, heteroarilo o heterociclilo está sustituido con uno o más R1a, R1b y R1c, donde R1a, R1b y R1c se seleccionan independientemente entre el grupo que consiste en: (a) hidrógeno, (b) hidroxi, (c) halógeno, (d) alquilo C1-6, que está sin sustituir o sustituido con sustituyentes seleccionados entre el grupo que consiste en: hidroxi, ciclopropilo, ciclobutilo, ciclopentilo, azetidinilo, flúor, -OCH3, -OCH2CH2OCH3, - (C=O)-alquilo C1-6, -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2 y -N(cicloalquilo C3-6), (e) -O-alquilo C1-6, que está sin sustituir o sustituido con sustituyentes seleccionados entre el grupo que consiste en: hidroxi, ciclopropilo, ciclobutilo, ciclopentilo, azetidinilo, flúor, -OCH3, -NH2, -NH(alquilo C1-6), - N(alquilo C1-6)2, -N(cicloalquilo C3-6) y -NH(C=O)(alquilo C1-6), (f) cicloalquilo C3-6, que está sin sustituir o sustituido con sustituyentes seleccionados entre el grupo que consiste en: alquilo C1-6, hidroxi, ciclopropilo, ciclobutilo, ciclopentilo, azetidinilo, flúor, -OCH3, -NH2, - NH(alquilo C1-6), -N(alquilo C1-6)2 y -N(cicloalquilo C3-6), (g) -NH2, (h) -NH(alquilo C1-6), (i) -NH(alquilo C2-6)-OH, (j) -N(alquilo C1-6)2, (k) -N(cicloalquilo C3-6), (l) -SO2-alquilo C-6, (m) -(C=O)H, (n) -(C=O)-alquilo C1-6, (o) -(C=O)O-alquilo C1-6 y (p) -CN; R2 y R3 se seleccionan independientemente entre el grupo que consiste en: (1) hidrógeno, (2) flúor, (3) hidroxi y (4) -CH3; ...

28. 发明专利

AU2015350315B2 Aminopyrazine compounds with A2A antagonist properties 未知
公开(公告)号：AU2015350315B2
公开(公告)日：2020-06-25
申请号：AU2015350315
申请日：2015-11-13
申请人： MERCK SHARP & DOHME
发明人： KUANG RONGZE , ALI AMJAD , TING PAULINE , WU HEPING , BERLIN MICHAEL , STAMFORD ANDREW , WANG HONGWU , ZHOU GANG , KIM DAVID , DENG QIAOLIN , LIM YEON-HEE , YU YOUNONG
IPC分类号： C07D241/26 , A61K31/497 , C07D413/04
摘要： Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R

30. 发明专利

AU2013370977B2 Heterobicyclo-substituted-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A antagonist properties 未知
公开(公告)号：AU2013370977B2
公开(公告)日：2017-12-14
申请号：AU2013370977
申请日：2013-12-20
申请人： MERCK SHARP & DOHME
发明人： ALI AMJAD , LO MICHAEL MAN-CHU , LIM YEON-HEE , STAMFORD ANDREW , KUANG RONGZE , TEMPEST PAUL , YU YOUNONG , HUANG XIANHAI , HENDERSON TIMOTHY J , KIM JAE-HUN , BOYCE CHRISTOPHER , TING PAULINE , ZHENG JUNYING , METZGER EDWARD , ZORN NICOLAS , XIAO DONG , GALLO GIOCONDA V , WON WALTER , WU HEPING , DENG QIAOLIN
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/519 , A61P25/16
摘要： Disclosed are compounds of Formula Gl (structurally represented): where "RG3" "Rd1" to "Rd4", "n", "m", "p", "W", "X", "Y", and "Z" are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

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