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101. 发明公开

EP3253390A1 AMINOQUINAZOLINE COMPOUNDS AS A2A ANTAGONIST 有权转让
标题翻译：氨基喹唑啉化合物作为A2A拮抗剂
公开(公告)号：EP3253390A1
公开(公告)日：2017-12-13
申请号：EP16747041.8
申请日：2016-02-01
申请人： Merck Sharp & Dohme Corp.
发明人： ALI, Amjad , ZHOU, Gang , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , TING, Pauline C. , BIJU, Purakkattle , RUIZ, Manuel de Lera , DEGRADO, Sylvia J. , TUNG, Alexander L. , HENDERSON, Timothy J. , HONG, Liwu , KIM, Jae-Hun , KIM, David Won-Shik , LEE, Joe F. , WU, Jie , WU, Heping , XIAO, Yushi , YU, Tao , ZHU, Xiaohong , MCCORMICK, Kevin D. , TAGAT, Jayaram R. , XIAO, Dong , KHAN, Tanweer , CAO, Jianhua , BERLIN, Michael , ZHANG, Yonglian
IPC分类号： A61K31/517 , C07D239/84 , C07D403/12
CPC分类号： C07D239/84 , A61K31/517 , A61P25/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.

102. 发明公开

EP3220910A1 AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 有权转让
标题翻译：具有A2A拮抗剂性质的氨基嘧啶化合物
公开(公告)号：EP3220910A1
公开(公告)日：2017-09-27
申请号：EP15861650.8
申请日：2015-11-13
申请人： Merck Sharp & Dohme Corp.
发明人： KUANG, Rongze , TING, Pauline , ALI, Amjad , WU, Heping , BERLIN, Michael , STAMFORD, Andrew , WANG, Hongwu , ZHOU, Gang , KIM, David , DENG, Qiaolin , LIM, Yeon-Hee , YU, Younong
IPC分类号： A61K31/497 , C07D241/26 , 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 "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
摘要翻译：公开了式A和式A-1的化合物或其盐，以及包含这些化合物或其盐的药物制剂（药物组合物）其中“R1”，“RA-1”，“R2”，“R3”和“Het”如上文所定义，认为该化合物适用于选择性拮抗A2a受体，例如以高密度在基底神经节。据信这样的化合物和药物制剂可用于治疗或控制神经退行性疾病，例如帕金森病，或由于使用用于治疗或控制帕金森病的某些药物引起的运动障碍。

103. 发明授权

EP2861071B1 ALDOSTERONE SYNTHASE INHIBITORS 有权转让
标题翻译： ALDOSTERONSYNTHASEHEMMER
公开(公告)号：EP2861071B1
公开(公告)日：2017-03-15
申请号：EP13772609.7
申请日：2013-03-29
申请人： Merck Sharp & Dohme Corp. , Elexopharm GmbH
发明人： ALI, Amjad , BEY, Emmanuel , HARTMANN, Rolf , HU, Qungzhong , YIN, Lina
IPC分类号： A61K31/4745 , C07D471/04 , A61P9/00
CPC分类号： A61K31/4745 , A61K45/06 , C07D471/04

104. 发明公开

EP2701512A1 ALDOSTERONE SYNTHASE INHIBITORS 有权转让
标题翻译：醛固酮合成酶抑制剂
公开(公告)号：EP2701512A1
公开(公告)日：2014-03-05
申请号：EP12776492.6
申请日：2012-04-20
申请人： Merck Sharp & Dohme Corp. , Elexopharm GmbH
发明人： HOYT, Scott, B. , PETRILLI, Whitney Lane , LONDON, Clare , XIONG, Yusheng , TAYLOR, Jerry Andrew , ALI, Amjad , LO, Michael , HENDERSON, Timothy, J. , HU, Qingzhong , HARTMANN, Rolf , YIN, Lina , HEIM, Ralf , BEY; Emmanuel , SAXENA, Rohit , SAMANTA, Swapan Kumar , KULKARNI, Bheemashankar, A.
IPC分类号： A01N43/64 , A61K31/41
CPC分类号： C07D487/04 , A61K31/41 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
摘要翻译：本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中变量如本文所定义。本发明的化合物选择性地抑制醛固酮合成酶。本发明还提供了包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

105. 发明授权

EP2121665B1 NITRODERIVATIVES AS ANGIOTENSIN II RECEPTOR ANTAGONISTS 有权
标题翻译：硝基衍生物血管紧张素II受体的拮抗剂
公开(公告)号：EP2121665B1
公开(公告)日：2014-01-22
申请号：EP07862716.3
申请日：2007-12-11
申请人： Merck Sharp & Dohme Corp. , Nicox S.A.
发明人： SEBHAT, Iyassu, K. , LO, Michael Man-Chu , NARGUND, Ravi P. , ALI, Amjad , FRANKLIN, Chris , ALMIRANTE, Nicoletta , STORONI, Laura , STEFANINI, Silvia
IPC分类号： C07D403/10 , A61K31/41 , A61P9/12
CPC分类号： C07D403/10

106. 发明授权

EP2348859B1 PRODRUGS OF OXAZOLIDINONE CETP INHIBITORS 有权转让
标题翻译：恶唑烷酮CETP的药物前体抑制剂
公开(公告)号：EP2348859B1
公开(公告)日：2013-12-04
申请号：EP09818237.1
申请日：2009-09-21
申请人： Merck Sharp & Dohme Corp.
发明人： MILLS, Sander, G. , ALI, Amjad , SMITH, Cameron
IPC分类号： A01N43/76 , A61K31/42 , C07C219/22
CPC分类号： A61K31/42 , C07C219/22 , C07C219/28 , C07C229/36 , C07C329/06 , C07C2601/14 , C07F9/091 , C07F9/093 , C07F9/094

107. 发明公开

EP2632255A1 DIAZENIUMDIOLATE HETEROCYCLIC DERIVATIVES 有权转让
标题翻译：杂环衍生物二醇二氮烯
公开(公告)号：EP2632255A1
公开(公告)日：2013-09-04
申请号：EP11836944.6
申请日：2011-10-25
申请人： Merck Sharp & Dohme Corp.
发明人： ALI, Amjad , LO, Michael Man-Chu , BAKER, Robert, K. , GUO, Zhiqiang , WHITEHEAD, Brent , HENDERSON, Timothy, J. , METZGER, Edward , YAN, Lin , SHAH, Shrenik, K. , DELLUREFICIO, James , WANG, Jun
IPC分类号： A01N33/26 , A61K31/655
CPC分类号： C07D211/44 , A61K31/655 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/273 , C07D307/20 , C07D309/12 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04
摘要： A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.

108. 发明公开

EP2533644A1 DIAZENIUMDIOLATE CYCLOPENTYL DERIVATIVES 有权转让
标题翻译：二醇二氮烯衍生物环戊
公开(公告)号：EP2533644A1
公开(公告)日：2012-12-19
申请号：EP11742769.0
申请日：2011-02-10
申请人： Merck Sharp & Dohme Corp.
发明人： ALI, Amjad , LO, Michael Man-Chu , METZGER, Edward , YAN, Lin
IPC分类号： A01N51/00
CPC分类号： C07C291/00 , C07C291/08 , C07C2601/08 , C07D249/04
摘要： A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R
1 is hydrogen, -OH, -O-C
1 -
6 alkyl, =O, or halogen;R
2 is hydrogen, C(O)OR
8 , C
6 H
5 C(O)OR
8 , (CH
2 )
1-2 OH, CR
9 R
10 OH, C(O)O(CH
2 )
0-2 aryl, C(O)NR
9 R
10 , C(O)SO
2 NR
9 R
10 , C
6 H
5 OR
9 , W-C(O)OR
8 , W-OR
9 , Y, or P(O)(OR
9 )(ORlO); R
3 is hydrogen or -C
1-6 alkyl; R
4 is hydrogen, -OH or -C(O)OR
9 ; R
5 is hydrogen or deuterium; R
6 and R
7 are independently-C
1-6 alkyl, fluoro-substituted -C
1-6 alkyl, deutero-substituted -C
1-6 alkyl or -(CH
2 )
1-2 R
11 , wherein any carbon atom of the fluoro-substituted -C
1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted -C
1-6 alkyl is mono- or di-substituted with fluoro; R
8 , in each instance in which it occurs, is independently hydrogen, -C
1-6 alkyl, or -(CH
2 )
2 N
+ (CH
3 )
3 ; R
9 and R
10 , in each instance in which they occur, are independently -C
1-6 alkyl; R
11 is -OH, -O-C
1-6 alkyl, -0CD3, -OC(O)OC
1-6 alkyl, -NH
2 , -C
6 H
5 , -N
3 , or W; W is an unsubslituted 5- or 6-raembered heteroaryl ring having 1, 2, or 3 nitrogen atoms, or a substituted 5- or 6-membered heteroaryl ring having 1, 2, or 3 nitrogen atoms that is mono- or di-substituted at any carbon atom with R
6 or R
7 ; Y is a 5- or 6-membered heterocyclic ring having 1, 2, 3 or 4 heteroatoms which are N, O or S or stereoisomers thereof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using the compounds for treating hypertension.

109. 发明授权

EP1973546B1 CHOLESTERYL ESTER TRANSFER PROTEIN INHIBITORS 有权
标题翻译： CHOLESTERYLESTERTRANSFERPROTEINHEMMER
公开(公告)号：EP1973546B1
公开(公告)日：2012-06-13
申请号：EP06849198.4
申请日：2006-12-29
申请人： Merck Sharp & Dohme Corp.
发明人： ALI, Amjad , SINCLAIR, Peter, J. , TAYLOR, Gayle, E.
IPC分类号： C07D293/10 , C07D413/06
CPC分类号： C07D265/10 , C07D413/06
摘要： Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), A1 is a cyclic group, and B is a cyclic group which is attached to the heterocyclic ring directly or through a methylene group.

110. 发明授权

EP1954287B1 CETP INHIBITORS 有权
标题翻译： CETP抑制剂
公开(公告)号：EP1954287B1
公开(公告)日：2011-11-16
申请号：EP06826999.2
申请日：2006-10-30
申请人： Merck Sharp & Dohme Corp.
发明人： ALI, Amjad , HUNT, Julianne, A. , KALLASHI, Florida , KOWALCHICK, Jennifer, E. , KIM, Dooseop , SMITH, Cameron, J. , SINCLAIR, Peter, J. , SWEIS, Ramzi, F. , TAYLOR, Gayle, E. , THOMPSON, Christopher, F. , CHEN, Liya , QURAISHI, Nazia
IPC分类号： A61K31/41
CPC分类号： C07D263/57 , C07D235/18 , C07D239/74 , C07D277/64 , C07D277/66 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/10 , C07D498/04
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I

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