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11. 发明申请

WO2008039420A3 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
公开(公告)号：WO2008039420A3
公开(公告)日：2008-04-03
申请号：PCT/US2007/020608
申请日：2007-09-24
申请人： MERCK & CO., INC. , BLIZZARD, Timothy, A. , CHEN, Helen, Y. , WU, Jane, Yang , KIM, Seongkon , HA, Sookhee , MORTKO, Christopher, J. , VARIANKAVAL, Narayan , CHIU, Anna
发明人： BLIZZARD, Timothy, A. , CHEN, Helen, Y. , WU, Jane, Yang , KIM, Seongkon , HA, Sookhee , MORTKO, Christopher, J. , VARIANKAVAL, Narayan , CHIU, Anna
IPC分类号： C07D487/04 , A61K31/407 , A61P31/04
摘要： A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.

12. 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。

13. 发明申请

WO2004091488A3 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2004091488A3
公开(公告)日：2005-04-07
申请号：PCT/US2004010853
申请日：2004-04-09
申请人： MERCK & CO INC , DININNO FRANK P , CHEN HELEN Y , TAN QIANG
发明人： DININNO FRANK P , CHEN HELEN Y , TAN QIANG
IPC分类号： A61K20060101 , A61K31/40 , A61K31/445 , C07D405/10
CPC分类号： C07D405/10 , C07D311/60
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, 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, and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其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相关的各种病症，包括：骨丢失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤病，热特别是乳腺，子宫和前列腺中的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，男子乳腺发育症，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

14. 发明申请

WO1997044453A1 NOVEL INHIBITORS OF VASCULAR ENDOTHELIAL GROWTH FACTOR ACTIVITY, THEIR USES AND PROCESSES FOR THEIR PRODUCTION 审中-公开
标题翻译：血管内皮生长因子活性的新型抑制剂，其生产用途及其制备方法
公开(公告)号：WO1997044453A1
公开(公告)日：1997-11-27
申请号：PCT/US1997007694
申请日：1997-05-06
申请人： GENENTECH, INC. , DAVIS-SMYTH, Terri, Lynn , CHEN, Helen, Hsifei , PRESTA, Leonard , FERRARA, Napoleone
发明人： GENENTECH, INC.
IPC分类号： C12N15/12
CPC分类号： C07K14/71 , A61K38/00 , C07K16/2863 , C07K2319/00 , C07K2319/30 , C07K2319/31
摘要： The present invention is directed to novel chimeric VEGF receptor proteins comprising amino acid sequences derived from the vascular endothelial growth factor (VEGF) receptors flt-1 and KDR, including the murine homologue to the human KDR receptor FLK-1, wherein said chimeric VEGF receptor proteins bind to VEGF and antagonize the endothelial cell proliferative and angiogenic activity thereof. The present invention is also directed to nucleic acids and expression vectors encoding these chimeric VEGF receptor proteins, host cells harboring such expression vectors, pharmaceutically acceptable compositions comprising such proteins, methods of preparing such proteins and to methods utilizing such proteins for the treatment of conditions associated with undesired vascularization.
摘要翻译：本发明涉及包含衍生自血管内皮生长因子（VEGF）受体flt-1和KDR的氨基酸序列的新型嵌合VEGF受体蛋白，包括人KDR受体FLK-1的鼠同源物，其中所述嵌合VEGF受体蛋白质结合VEGF并拮抗其内皮细胞增殖和血管生成活性。本发明还涉及编码这些嵌合VEGF受体蛋白质的核酸和表达载体，含有这种表达载体的宿主细胞，包含这种蛋白质的药学上可接受的组合物，制备这种蛋白质的方法以及利用这些蛋白质治疗相关病症的方法具有不希望的血管形成。

15. 发明申请

WO1997036859A1 PARA-SUBSTITUTED PHENYLPROPANOIC ACID DERIVATIVES AS INTEGRIN ANTAGONISTS 审中-公开
标题翻译：作为整合拮抗剂的参考取代的苯丙酸衍生物
公开(公告)号：WO1997036859A1
公开(公告)日：1997-10-09
申请号：PCT/US1997004460
申请日：1997-03-26
申请人： G.D. SEARLE & CO. , CHEN, Barbara, B. , CHEN, Helen, Y. , GESICKI, Glen, J. , HAACK, Richard, A. , MALECHA, James, W. , PENNING, Thomas, D. , RICO, Joseph, G. , ROGERS, Thomas, E. , RUMINSKI, Peter, G. , RUSSELL, Mark, A. , YU, Stella, S.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C279/18
CPC分类号： C07D271/07 , A61K31/155 , C07C275/42 , C07C279/18 , C07C279/22 , C07C279/24 , C07C279/28 , C07C311/06 , C07C311/13 , C07C311/19 , C07C311/64 , C07C317/44 , C07C323/52 , C07D223/12 , C07D231/12 , C07D233/50 , C07D233/56 , C07D233/88 , C07D239/14 , C07D249/08 , C07D249/14 , C07D295/215
摘要： The present invention relates to a class of compounds represented by Formula (I) or a phramaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of Formula (I), and methods of selectively inhibiting or antagonizing the alpha v beta 3 integrin.
摘要翻译：本发明涉及一类由式（I）表示的化合物或其药学上可接受的盐，包含式（I）化合物的药物组合物，以及选择性抑制或拮抗αvβ3整联蛋白的方法。

16. 发明申请

WO2016022446A1 [5,6]-FUSED BICYCLIC ANTIDIABETIC COMPOUNDS 审中-公开
标题翻译： [5,6] - 双金属抗生素化合物
公开(公告)号：WO2016022446A1
公开(公告)日：2016-02-11
申请号：PCT/US2015/043352
申请日：2015-08-03
申请人： MERCK SHARP & DOHME CORP. , CHEN, Helen, Y. , DEMONG, Duane , FINKE, Paul, E. , PLUMMER, Christopher, W.
发明人： CHEN, Helen, Y. , DEMONG, Duane , FINKE, Paul, E. , PLUMMER, Christopher, W.
IPC分类号： A61K31/343 , A61K31/443 , C07D307/79
CPC分类号： C07D405/04 , A61K31/343 , A61K31/443 , A61K45/06 , C07D307/80 , C07D405/10 , 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.
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G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合或糖尿病性血脂异常，高脂血症，高胆固醇血症和高甘油三酯血症。

17. 发明申请

WO2013066714A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 审中-公开
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：WO2013066714A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/061884
申请日：2012-10-25
申请人： MERCK SHARP & DOHME CORP. , WALSH, Shawn, P. , PASTERNAK, Alexander , DEJESUS, Reynalda, K. , TANG, Haifeng , PIO, Barbara , SHAHRIPOUR, Aurash , BELYK, Kevin, M. , CHOBANIAN, Harry, R. , GUO, Yan , FRIE, Jessica, L. , SHI, Zhi-Cai , CHEN, Helen , BLIZZARD, Timothy, A. , CATO, Brian
发明人： WALSH, Shawn, P. , PASTERNAK, Alexander , DEJESUS, Reynalda, K. , TANG, Haifeng , PIO, Barbara , SHAHRIPOUR, Aurash , BELYK, Kevin, M. , CHOBANIAN, Harry, R. , GUO, Yan , FRIE, Jessica, L. , SHI, Zhi-Cai , CHEN, Helen , BLIZZARD, Timothy, A. , CATO, Brian
IPC分类号： A01N29/04
CPC分类号： C07D471/08 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D487/08 , C07D487/18 , C07D491/08 , C07D498/08
摘要： This invention relates to compounds of Formula I-VI having the following general structure: wherein R is a 6-8 membered saturated heterocyclic ring having 2 Nitrogen atoms connected with (CH 2)n1 - and (CH 2)n2 -, respectively, and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译：本发明涉及具有以下一般结构的式I-VI化合物：其中R是分别具有（CH2）n1和（CH2）n2-的2个氮原子的6-8元饱和杂环和药学上可接受的它们是肾外膜钾（ROMK）通道（Kir1.1）的抑制剂的盐。这些化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由于过量的盐和水分滞留引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

18. 发明申请

WO2004091488A2 ESTROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：雌激素受体调节剂
公开(公告)号：WO2004091488A2
公开(公告)日：2004-10-28
申请号：PCT/US2004/010853
申请日：2004-04-09
申请人： MERCK & CO., INC. , DININNO, Frank, P. , CHEN, Helen, Y. , TAN, Qiang
发明人： DININNO, Frank, P. , CHEN, Helen, Y. , TAN, Qiang
IPC分类号： A61K
CPC分类号： C07D405/10 , C07D311/60
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, 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, and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其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相关的各种病症，包括：骨丢失，骨折，骨质疏松症，软骨退化，子宫内膜异位症，子宫肌瘤病，热特别是乳腺，子宫和前列腺中的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，男子乳腺发育症，血管平滑肌细胞增殖，肥胖症，失禁和癌症。

19. 发明申请

WO1997036862A1 META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS 审中-公开
标题翻译：金属取代的苯乙烯衍生物及其作为ALPHAVBETA3 INTEGRIN ANTAGONISTS或INHIBITORS的用途
公开(公告)号：WO1997036862A1
公开(公告)日：1997-10-09
申请号：PCT/US1997004461
申请日：1997-03-26
申请人： G.D. SEARLE & CO. , CHANDRAKUMAR, Nizal , CHEN, Barbara, B. , CHEN, Helen , CLARE, Michael , GASIECKI, Alan, F. , HAACK, Richard, A. , MALECHA, James, W. , RUMINSKI, Peter, G. , RUSSELL, Mark, A.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C311/47
CPC分类号： C07C45/673 , C07C49/796 , C07C205/35 , C07C205/45 , C07C205/56 , C07C205/57 , C07C257/16 , C07C259/18 , C07C275/42 , C07C279/18 , C07C279/24 , C07C279/28 , C07C311/46 , C07C311/47 , C07C317/42 , C07C323/44 , C07C335/16 , C07C335/22 , C07C335/32 , C07D223/06 , C07D233/50 , C07D233/88 , C07D235/30 , C07D239/14 , C07D311/18 , C07D311/20 , C07D405/12
摘要： The present invention relates to a class of compounds represented by Formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the alpha v beta 3 integrin.
摘要翻译：本发明涉及一类由式（I）表示的化合物或其药学上可接受的盐，包含式（I）化合物的药物组合物，以及选择性抑制或拮抗αvβ3整联蛋白的方法。

20. 发明申请

WO2017106064A1 BIARYL MONOBACTAM COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF BACTERIAL INFECTIONS 审中-公开
标题翻译：二芳基单胞菌素化合物及其用于治疗细菌感染的方法
公开(公告)号：WO2017106064A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/066064
申请日：2016-12-12
申请人： MERCK SHARP & DOHME CORP. , TANG, Haifeng , LIU, Weiguo , DING, Fa-Xiang , SUN, Wanying , ZANG, Yi , PAN, Weidong , OGAWA, Anthony , BROCKUNIER, Linda , HUANG, Xianhai , WANG, Hongwu , MAL, Rudrajit , BIFTU, Tesfaye , PARK, Min , GUO, Yan , JIANG, Jinlong , CHEN, Helen , PLUMMER, Christopher, W.
发明人： TANG, Haifeng , LIU, Weiguo , DING, Fa-Xiang , SUN, Wanying , ZANG, Yi , PAN, Weidong , OGAWA, Anthony , BROCKUNIER, Linda , HUANG, Xianhai , WANG, Hongwu , MAL, Rudrajit , BIFTU, Tesfaye , PARK, Min , GUO, Yan , JIANG, Jinlong , CHEN, Helen , PLUMMER, Christopher, W.
IPC分类号： C07D205/08 , A61K31/397 , A61P31/04
CPC分类号： A61K31/397 , C07D417/14 , C07D471/04
摘要： The present invention relates to biaryl monobactam compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A 1 , Q, A 2 , M, W, R X and R z are as defined herein. The present invention also relates to compositions which comprise a biaryl monobactam compound of the invention or a pharmaceutically acceptable salt therof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of a second beta-lactam antibiotic.
摘要翻译：本发明涉及式I的联芳基单环内酰胺化合物及其药学上可接受的盐，其中X，Y，Z，A 1，Q，A 2 M，W，R X和R Z如本文所定义。本发明还涉及包含本发明的联芳单胞菌素化合物或其药学上可接受的盐和药学上可接受的载体的组合物。本发明还涉及治疗细菌感染的方法，其包括向患者单独或与治疗有效量的第二种β-内酰胺抗生素联合给药治疗有效量的本发明化合物。

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