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1. 发明申请

WO2015112465A1 ISOQUINOLINE DERIVATIVES AS MGAT2 INHIBITORS 审中-公开
标题翻译：异喹啉衍生物作为MGAT2抑制剂
公开(公告)号：WO2015112465A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/011939
申请日：2015-01-20
申请人： MERCK SHARP & DOHME CORP. , BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
发明人： BERGER, Richard , BLIZZARD, Timothy, A. , CAMPBELL, Brian, T. , CHEN, Helen, Y. , DEBENHAM, John, S. , DEWNANI, Sunita, V. , DUBOIS, Byron , GUDE, Candido , GUO, Zhiqiang , HARPER, Bart , HU, Zhiyong , LIN, Songnian , LIU, Ping , WANG, Ming , UJJAINWALLA, Feroze , XU, Jiayi , XU, Libo , ZHANG, Rui
IPC分类号： C07D471/04
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/14 , C07D471/04
摘要： The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
摘要翻译：式I化合物作为MGAT2抑制剂，可用于预防，治疗或作为高脂血症，糖尿病和肥胖症的补救剂。

2. 发明申请

WO2014058538A1 SUBSTITUTED PYRROLIDINE THROMBIN INHIBITORS 审中-公开
标题翻译：替代吡咯啉抑制剂
公开(公告)号：WO2014058538A1
公开(公告)日：2014-04-17
申请号：PCT/US2013/056076
申请日：2013-08-22
申请人： MERCK SHARP & DOHME CORP. , ALBANY MOLECULAR RESEARCH INC. , BLIZZARD, Timothy, A. , CHOBANIAN, Harry , GREENLEE, William , SINGH, Sanjay
发明人： BLIZZARD, Timothy, A. , CHOBANIAN, Harry , GREENLEE, William , SINGH, Sanjay
IPC分类号： C07D207/00
CPC分类号： C07D209/54 , C07D217/16 , C07F7/0816 , C07F7/1844
摘要： 4-Substituted pyrrolidine carboxamide compounds are useful in inhibiting thrombin and associated thrombus formation for treating or preventing venous thromboembolisms.
摘要翻译： 4-取代的吡咯烷羧酰胺化合物可用于抑制凝血酶和相关的血栓形成用于治疗或预防静脉血栓栓塞。

3. 发明申请

WO1997040048A1 CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴因抗菌化合物，含有这些化合物的组合物和处理方法
公开(公告)号：WO1997040048A1
公开(公告)日：1997-10-30
申请号：PCT/US1997006626
申请日：1997-04-21
申请人： MERCK & CO., INC. , WILKENING, Robert, R. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A.
发明人： MERCK & CO., INC.
IPC分类号： C07D477/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14 , Y02P20/55
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式（I）表示。还包括药物组合物和使用方法。

4. 发明申请

WO1996004282A1 CARBAPENEM COMPOUNDS, COMPOSITIONS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴辛化合物，组合物和治疗方法
公开(公告)号：WO1996004282A1
公开(公告)日：1996-02-15
申请号：PCT/US1995010029
申请日：1995-07-25
申请人： MERCK & CO., INC. , WADDELL, Sherman, T. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A. , WILDONGER, Kenneth, J. , WILKENING, Robert, R. , SZUMILOSKI, Sandra, P.
发明人： MERCK & CO., INC.
IPC分类号： C07D487/04
CPC分类号： C07D477/20 , Y02P20/55
摘要： Carbapenems of formula (I) are disclosed as MRSA active agents. R represents hydrogen or methyl; CO2M represents a carboxylic acid, a carboxylate anion with or without a pharmaceutically acceptable counterion, a pharmaceutically acceptable ester group or a carboxylic acid protected by a protecting group; P* represents hydrogen or a hydroxyl protecting group; Het represents a heterocyclic group which is uncharged or positively charged, containing no more than three positively charged atoms, and is selected from the group consisting of: (a) and (b) wherein represents the point of attachment to S; A represents O or S; and X, Y and Z independently represent CR, N or N R .
摘要翻译：公开了式（I）的碳青霉烯作为MRSA活性剂。 R 1表示氢或甲基; CO 2 M表示羧酸，具有或不具有药学上可接受的抗衡离子的羧酸根阴离子，药学上可接受的酯基或被保护基保护的羧酸; P *表示氢或羟基保护基; Het表示不带电荷或带正电荷的杂环基，其含有不多于三个带正电荷的原子，并且选自：（a）和（b）其中表示与S的连接点; A代表O或S; X，Y和Z独立地表示CR，N或N + R a。

5. 发明申请

WO2015176640A1 ANTIDIABETIC TRICYCLIC COMPOUNDS 审中-公开
公开(公告)号：WO2015176640A1
公开(公告)日：2015-11-26
申请号：PCT/CN2015/079262
申请日：2015-05-19
申请人： MERCK SHARP & DOHME CORP. , BIFU, Tesfaye , BIJU, Purakkattle , BLIZZARD, Timothy A. , CHEN, Zhengxia , CLEMENTS, Matthew J. , CUI, Mingxiang , FRIE, Jessica L. , HAGMANN, William K. , HU, Bin , JOSIEN, Hubert , NAIR, Anilkumar G. , PLUMMER, Christopher W. , ZHU, Cheng
发明人： BIFU, Tesfaye , BIJU, Purakkattle , BLIZZARD, Timothy A. , CHEN, Zhengxia , CLEMENTS, Matthew J. , CUI, Mingxiang , FRIE, Jessica L. , HAGMANN, William K. , HU, Bin , JOSIEN, Hubert , NAIR, Anilkumar G. , PLUMMER, Christopher W. , ZHU, Cheng
IPC分类号： C07D221/16 , C07D401/12 , C07D405/12 , A61K31/438 , A61K31/415 , A61P3/10
CPC分类号： C07D221/16 , A61K31/192 , A61K31/366 , A61K31/397 , A61K31/435 , A61K31/438 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/4985 , A61K31/538 , A61K31/55 , A61K45/06 , C07C61/39 , C07C2602/08 , C07C2603/12 , C07D215/14 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/12 , A61K2300/00
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

6. 发明申请

WO2006031607A2 A METHOD OF TREATING CANCER 审中-公开
标题翻译：一种治疗癌症的方法
公开(公告)号：WO2006031607A2
公开(公告)日：2006-03-23
申请号：PCT/US2005032037
申请日：2005-09-09
申请人： MERCK & CO INC , MERCK SHARP & DOHME , BLIZZARD TIMOTHY A , BUSER-DOEPNER CAROLYN A , FRANTZ DOUGLAS E , HAMILTON KELLY , HOANG MYLE , LEE LING , MOYES CHRISTOPHER R , MURRY JERRY A , SOHEILI ARASH
发明人： BLIZZARD TIMOTHY A , BUSER-DOEPNER CAROLYN A , FRANTZ DOUGLAS E , HAMILTON KELLY , HOANG MYLE , LEE LING , MOYES CHRISTOPHER R , MURRY JERRY A , SOHEILI ARASH
IPC分类号： G01N33/574
CPC分类号： C12Q1/42 , G01N33/6893 , G01N2500/00
摘要： The present invention relates to a method of treating cellular proliferative diseases, in particular cancer, which comprises administering a modulator of the activity of the mitotic kinesin KSP, wherein the activity of the KSP modulator is dependent on the presence of microtubules. It is believed that the KSP modulators utilized in the instant method bind to the KSP protein in a previously unreported manner, since the compounds do not bind competitively with respect to either microtubules or ATP, the substrates of KSP. The modulators useful in the instant methods are furthermore not active against the non-microtubule stimulated activity of KSP. Cellular proliferative diseases that may be treated using the method disclosed herein are, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要翻译：本发明涉及一种治疗细胞增殖性疾病，特别是癌症的方法，其包括施用有丝分裂驱动蛋白KSP活性的调节剂，其中KSP调节剂的活性取决于微管的存在。相信本方法中使用的KSP调节剂以先前未报道的方式结合KSP蛋白质，因为化合物相对于微管或ATP（KSP的底物）竞争性结合。在本方法中有用的调节剂还不能抵抗KSP的非微管刺激活性。可以使用本文公开的方法治疗的细胞增殖性疾病是例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。

7. 发明申请

WO2005123757A1 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2005123757A1
公开(公告)日：2005-12-29
申请号：PCT/US2005/019870
申请日：2005-06-07
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , GUDE, Candido
发明人： BLIZZARD, Timothy, A. , GUDE, Candido
IPC分类号： C07J1/00
CPC分类号： C07J1/00
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget’s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, inflammation, inflammatory bowel disease, sexual dysfunction, hypertension, retinal degeneration and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及化合物及其衍生物，它们的合成，以及它们作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能有关的多种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨疾病，佩吉特氏病，牙周病，软骨退化，子宫内膜异位，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子女性型乳房，血管平滑肌细胞增殖，肥胖症，失禁，炎症，性功能障碍，高血压，视网膜变性和癌症，特别是乳房，子宫和前列腺。

8. 发明申请

WO1998010761A1 CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴因抗菌化合物，含有这些化合物的组合物和处理方法
公开(公告)号：WO1998010761A1
公开(公告)日：1998-03-19
申请号：PCT/US1997016786
申请日：1997-09-09
申请人： MERCK & CO., INC. , CAMA, Lovji, D. , WILKENING, Robert, R. , RATCLIFFE, Ronald, W. , BLIZZARD, Timothy, A.
发明人： MERCK & CO., INC.
IPC分类号： A61K31/425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula (I). Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式（I）表示。还包括药物组合物和使用方法。

9. 发明申请

WO1995025108A1 CARBAPENEM COMPOUNDS, COMPOSITIONS AND METHODS OF TREATMENT 审中-公开
标题翻译：卡巴辛化合物，组合物和治疗方法
公开(公告)号：WO1995025108A1
公开(公告)日：1995-09-21
申请号：PCT/US1995002702
申请日：1995-03-10
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , RATCLIFFE, Ronald, W. , WADDELL, Sherman, T. , SZUMILOSKI, Sandra, P. , WILKENING, Robert, R. , WILDONGER, Kenneth, J.
发明人： MERCK & CO., INC.
IPC分类号： C07D487/04
CPC分类号： C07D477/20
摘要： Carbapenems of formula (I) are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：公开了式（I）的碳青霉烯作为有用的抗菌剂。还公开了药物组合物和使用方法。

10. 发明申请

WO2017095759A1 C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译： C5-C6-碳环稠合的亚硝基二嗪二氧化物作为BACE抑制剂，组合物及其用途
公开(公告)号：WO2017095759A1
公开(公告)日：2017-06-08
申请号：PCT/US2016/063892
申请日：2016-11-29
申请人： MERCK SHARP & DOHME CORP. , SCOTT, Jack, D. , BLIZZARD, Timothy, A. , WALSH, Shawn, P. , CUMMING, Jared, N.
发明人： SCOTT, Jack, D. , BLIZZARD, Timothy, A. , WALSH, Shawn, P. , CUMMING, Jared, N.
IPC分类号： A61P25/28 , C07D471/04 , A61K31/541
CPC分类号： C07D471/04 , C07D285/20 , C07D417/12
摘要： In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1 , ring A, R A , m, -L 1 -, ring B, R B , n, q, ring C, R C , and p 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 for the possible treatment of 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C 5 -C 6 - 碳环稠合的亚氨噻嗪二氧化物化合物，包括式（I）化合物及其互变异构体，以及所述化合物和所述互变异构体的药学上可接受的盐，其中R 1，环A，R A，m，-L 1 - ，环B，R B，，n，q，环C，R c和p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有关的各种病症。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他活性剂组合）的药物组合物，以及它们的制备和使用方法，包括用于可能治疗阿尔茨海默氏病的方法。

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