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1. 发明申请

WO2009020580A1 GAMMA SECRETASE MODULATORS 审中-公开
公开(公告)号：WO2009020580A1
公开(公告)日：2009-02-12
申请号：PCT/US2008/009369
申请日：2008-08-04
申请人： SCHERING CORPORATION , ZHU, Zhaoning , GREENLEE, William, J. , CALDWELL, John, P. , MAZZOLA, Robert, D. , MCKITTRICK, Brian , BENNETT, Chad, E. , HUANG, Xianhai , JOSIEN, Hubert, B. , BURNETT, Duane, A.
发明人： ZHU, Zhaoning , GREENLEE, William, J. , CALDWELL, John, P. , MAZZOLA, Robert, D. , MCKITTRICK, Brian , BENNETT, Chad, E. , HUANG, Xianhai , JOSIEN, Hubert, B. , BURNETT, Duane, A.
IPC分类号： C07D217/24 , C07D487/04 , C07D498/04
CPC分类号： C07D487/04 , C07D217/24 , C07D498/04
摘要： In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新的杂环化合物作为γ分泌酶的调节剂，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物制剂的方法，所述药物制剂包含一种或多种这样的化合物以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

2. 发明申请

WO2009045314A1 GAMMA SECRETASE MODULATORS 审中-公开
标题翻译： GAMMA秘密调节器
公开(公告)号：WO2009045314A1
公开(公告)日：2009-04-09
申请号：PCT/US2008/011112
申请日：2008-09-25
申请人： SCHERING CORPORATION , ZHU, Zhaoning , GREENLEE, William, J. , CALDWELL, John, P. , MAZZOLA, JR., Robert, D. , MCKITTRICK, Brian , BENNETT, Chad, E. , BURNETT, Duane, A.
发明人： ZHU, Zhaoning , GREENLEE, William, J. , CALDWELL, John, P. , MAZZOLA, JR., Robert, D. , MCKITTRICK, Brian , BENNETT, Chad, E. , BURNETT, Duane, A.
IPC分类号： C07D233/76 , C07D233/86 , C07D233/88 , C07D403/04 , A61K31/4178 , A61P25/28
CPC分类号： C07D233/86 , C07D233/76 , C07D233/88 , C07D403/04
摘要： In its many embodiments, the present invention provides a novel class of 5-membered, nitrogen-containing heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的5元含氮杂环化合物作为γ-分泌酶的调节剂，制备这种化合物的方法，含有一种或多种这类化合物的药物组合物，制备药物制剂的方法，包括一种或更多这样的化合物，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与中枢神经系统相关的一种或多种疾病的方法。

3. 发明申请

WO2012051036A1 QUINAZOLINONE-TYPE COMPOUNDS AS CRTH2 ANTAGONISTS 审中-公开
标题翻译：喹诺酮类化合物作为CRTH2拮抗剂
公开(公告)号：WO2012051036A1
公开(公告)日：2012-04-19
申请号：PCT/US2011/055054
申请日：2011-10-06
申请人： MERCK SHARP & DOHME CORP. , SCHERING CORPORATION , ASLANIAN, Robert, G. , BOYCE, Christopher, W. , MAZZOLA, Robert, D., Jr. , MCKITTRICK, Brian, A. , MCCORMICK, Kevin, D. , PALANI, Anandan , QIN, Jun , TANG, Haiqun , XIAO, Dong , YU, Younong , CALDWELL, John, P. , KELLEY, Elizabeth Helen , ZHANG, Hongjun , SILIPHAIVANH, Phieng , MACCOSS, Rachel, N. , METHOT, Joey, L. , GAUUAN, Jolicia Polivina , JIANG, Qin , LEYHANE, Andrew, J. , BIJU, Purakkattle Johny , DONG, Li , HUANG, Xianhai , SHAO, Ning , ZHOU, Wei , DHONDI, Pawan, K.
发明人： ASLANIAN, Robert, G. , BOYCE, Christopher, W. , MAZZOLA, Robert, D., Jr. , MCKITTRICK, Brian, A. , MCCORMICK, Kevin, D. , PALANI, Anandan , QIN, Jun , TANG, Haiqun , XIAO, Dong , YU, Younong , CALDWELL, John, P. , KELLEY, Elizabeth Helen , ZHANG, Hongjun , SILIPHAIVANH, Phieng , MACCOSS, Rachel, N. , METHOT, Joey, L. , GAUUAN, Jolicia Polivina , JIANG, Qin , LEYHANE, Andrew, J. , BIJU, Purakkattle Johny , DONG, Li , HUANG, Xianhai , SHAO, Ning , ZHOU, Wei , DHONDI, Pawan, K.
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04
CPC分类号： C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要： This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH 2 receptor.
摘要翻译：本申请提供式I化合物或其药学上可接受的盐，其中各个变量在本文中定义，以及制备这些化合物的方法，包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态受体。

4. 发明申请

WO2013039878A1 SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：含有SILYL的杂环化合物及其用于治疗病毒性疾病的方法
公开(公告)号：WO2013039878A1
公开(公告)日：2013-03-21
申请号：PCT/US2012/054603
申请日：2012-09-11
申请人： MERCK SHARP & DOHME CORP. , DWYER, Michael, P. , KEERTIKAR, Kartik, M. , ZENG, Qingbei , MAZZOLA, Robert, D., Jr. , CALDWELL, John, P. , TANG, Haiqun , NAIR, Anilkumar Gopinadhan , SHANKAR, Bandarpalle, B. , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A.
发明人： DWYER, Michael, P. , KEERTIKAR, Kartik, M. , ZENG, Qingbei , MAZZOLA, Robert, D., Jr. , CALDWELL, John, P. , TANG, Haiqun , NAIR, Anilkumar Gopinadhan , SHANKAR, Bandarpalle, B. , ROSENBLUM, Stuart, B. , KOZLOWSKI, Joseph, A.
IPC分类号： C07F7/10
CPC分类号： C07F7/0816 , A61K31/695 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/395
摘要： The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, D and R 2 are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新的含甲硅烷基的杂环化合物：（I）及其药学上可接受的盐，其中A，B，C，D和R2如本文所定义。本发明还涉及包含至少一种含甲硅烷基的杂环化合物的组合物，以及使用含有甲硅烷基的杂环化合物治疗或预防患者HCV感染的方法。

5. 发明申请

WO2018118829A1 HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2018118829A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/067163
申请日：2017-12-19
申请人： MERCK SHARP & DOHME CORP. , MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
IPC分类号： A61K31/4178 , C07D403/06 , C07D493/04
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

6. 发明申请

WO2018118827A1 HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2018118827A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/067160
申请日：2017-12-19
申请人： MERCK SHARP & DOHME CORP. , MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu
IPC分类号： A61K31/18 , C07C311/21 , C07D417/04 , A61K31/4439 , C07D317/68 , A61K31/36
摘要： The present invention is directed to compounds of Formula I, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

7. 发明申请

WO2018034917A1 COMPOUNDS USEFUL FOR ALTERING THE LEVELS OF BILE ACIDS FOR THE TREATMENT OF DIABETES AND CARDIOMETABOLIC DISEASE 审中-公开
标题翻译：可用于改变胆汁酸水平的化合物用于治疗糖尿病和心脏代谢病
公开(公告)号：WO2018034917A1
公开(公告)日：2018-02-22
申请号：PCT/US2017/046183
申请日：2017-08-10
申请人： MERCK SHARP & DOHME CORP. , CALDWELL, John, P. , CAPLEN, Mary Ann , CUMMING, Jared, N. , DYKSTRA, Kevin, D. , HRUZA, Alan , LANKIN, Claire , LI, Derun , LIU, Hong , MCCRACKEN, Amy , MCKITTRICK, Brian , RAO, Ashwin , TAGAT, Jayaram, R. , TANG, Haiqun , TAOKA, Brandon, M. , VERRAS, Andreas , WALSH, Shawn, P. , WU, Wen-Lian , ZHANG, Tianyuan
发明人： CALDWELL, John, P. , CAPLEN, Mary Ann , CUMMING, Jared, N. , DYKSTRA, Kevin, D. , HRUZA, Alan , LANKIN, Claire , LI, Derun , LIU, Hong , MCCRACKEN, Amy , MCKITTRICK, Brian , RAO, Ashwin , TAGAT, Jayaram, R. , TANG, Haiqun , TAOKA, Brandon, M. , VERRAS, Andreas , WALSH, Shawn, P. , WU, Wen-Lian , ZHANG, Tianyuan
IPC分类号： A61K31/445 , A61K31/47 , C07D215/16
摘要： Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
摘要翻译：本文描述了式I的化合物或其药学上可接受的盐。式I化合物作为Cyp8b1抑制剂，可用于预防，治疗或作为糖尿病和心血管疾病的治疗剂。

8. 发明申请

WO2014062553A1 TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：三环取代的三氮嗪二氧化物作为BACE抑制剂，组合物及其使用
公开(公告)号：WO2014062553A1
公开(公告)日：2014-04-24
申请号：PCT/US2013/064799
申请日：2013-10-14
申请人： MERCK SHARP & DOHME CORP. , GILBERT, Eric, J. , CUMMING, Jared, N. , STAMFORD, Andrew, W. , YU, Younong , SCOTT, Jack, D. , ISERLOH, Ulrich , WANG, Lingyan , CALDWELL, John, P.
发明人： GILBERT, Eric, J. , CUMMING, Jared, N. , STAMFORD, Andrew, W. , YU, Younong , SCOTT, Jack, D. , ISERLOH, Ulrich , WANG, Lingyan , CALDWELL, John, P.
IPC分类号： A61K31/54 , A01N43/00
CPC分类号： C07D417/14 , A61K31/549 , A61K45/06 , C07D417/10 , C07D495/04
摘要： In its many embodiments, the present invention provides provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as "ring B") of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
摘要翻译：在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）：（I）化合物及其互变异构体和立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中中环在本文中称为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括阿尔茨海默氏病。

9. 发明申请

WO2017106134A1 BENZIMIDAZOLES AND INDOLES AS TARO INHIBITORS 审中-公开
标题翻译：苯并咪唑和吲哚作为TARO抑制剂
公开(公告)号：WO2017106134A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/066277
申请日：2016-12-13
申请人： MERCK SHARP & DOHME CORP. , CALDWELL, John, P. , HO, Ginny Dai , HA, Sookhee, N. , KOSEOGLU, Sandra, J. , LABROLI, Marc, A. , LEE, Sang Ho , MADSEN-DUGGAN, Christina , MANDAL, Mihir , PAN, Jianping , PAN, Weidong , ROEMER, Terry , SU, Jing , TAN, Christopher Michael , TAN, Zheng , WANG, Hao , YANG, Christine , YANG, Shu-Wei
发明人： CALDWELL, John, P. , HO, Ginny Dai , HA, Sookhee, N. , KOSEOGLU, Sandra, J. , LABROLI, Marc, A. , LEE, Sang Ho , MADSEN-DUGGAN, Christina , MANDAL, Mihir , PAN, Jianping , PAN, Weidong , ROEMER, Terry , SU, Jing , TAN, Christopher Michael , TAN, Zheng , WANG, Hao , YANG, Christine , YANG, Shu-Wei
IPC分类号： A61P29/00 , C07D235/02 , C07D405/12
CPC分类号： C07D471/04 , C07D209/08 , C07D235/08 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/06 , C07D417/14
摘要： Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.
摘要翻译：结构式I的新型化合物及其药学上可接受的盐是TarO的抑制剂并且可用于预防，治疗和抑制由TarO介导的疾病，例如细菌感染，包括革兰氏阴性细菌感染和革兰氏阳性细菌感染例如MRSA和MRSE，单独或与β-内酰胺抗生素组合。

10. 发明申请

WO2003032996A1 IMIDAZO (4,3-E)-1,2,4-TRIAZOLO(1,5-C) PYRIMIDINES AS ADENOSINE A2A RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为腺苷A2A受体拮抗剂的咪唑（4,3-E）-1,2,4-三唑（1,5-C）嘧啶
公开(公告)号：WO2003032996A1
公开(公告)日：2003-04-24
申请号：PCT/US2002/032630
申请日：2002-10-11
申请人： SCHERING CORPORATION
发明人： TULSHIAN, Deen , SILVERMAN, Lisa, S. , MATASI, Julius, J. , KISELGOF, Eugenia, Y. , CALDWELL, John, P.
IPC分类号： A61K31/505
CPC分类号： C07D487/14 , A61K31/198 , A61K31/505 , A61K45/06 , Y02P20/582 , A61K2300/00
摘要： Compounds having the structural formula (I) or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl or heteroaryl, cycloalkenyl, -C(=CH2)CH3, -C°C-CH3, -CH=C(CH3)2, X is alkylene, -C(O)CH2- or -C(O)N(R2)CH2-;Y is -N(R2)CH2CH2N(R3)-, -OCH2CH2N(R2)-, -O-, -S-, -CH2S-, -(CH2)2-N(R2)-, or optionally substituted divalent heteroaryl, piperidinyl or piperazinyl; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl or R6-C(O)-; or when Y is formula (II) Z is also R6-SO2-, R7-N(R8)-C(O)-, R7-N(R8)-C(S)- or R6OC(O)-;or when Y is 4-piperidinyl, Z can be phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl, substituted pyrrolidinyl or substituted phenyl; R14 is H, halogen or optionally substituted alkyl; and Q, Q1, m, n, R2, R3, R4, R6, R7 and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，其中R是任选取代的苯基或杂芳基，环烯基，-C（= CH 2）CH 3，-C≡C-CH 3，-CH = C（CH 3） X是亚烷基，-C（O）CH2-或-C（O）N（R2）CH2-; Y是-N（R2）CH2CH2N（R3） - ，-OCH2CH2N（R2） - ， - O - ， - - ， - CH 2 S - ， - （CH 2）2 -N（R 2） - 或任选取代的二价杂芳基，哌啶基或哌嗪基; Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基或R6-C（O） - ; 或当Y为式（II）时，Z也为R6-SO2-，R7-N（R8）-C（O） - ，R7-N（R8）-C（S） - 或R6OC（O） Y是4-哌啶基，Z可以是苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基，取代的吡咯烷基或取代的苯基; R 14是H，卤素或任选取代的烷基; 并且Q，Q1，m，n，R2，R3，R4，R6，R7和R8如说明书中所定义，其用于治疗帕金森病，单独使用或与其他治疗帕金森病药物组合使用，和包含它们的药物组合物。

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