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公开(公告)号：WO2011146324A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036367
申请日：2011-05-13
Applicant: MERCK SHARP & DOHME CORP. , DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , FINKE, Paul, E. , ZANG, Yi , PLOTKIN, Michael, A. , ROMERO, F. Anthony , MONINGKA, Remond , HUSSAIN, Zahid
Inventor： DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , FINKE, Paul, E. , ZANG, Yi , PLOTKIN, Michael, A. , ROMERO, F. Anthony , MONINGKA, Remond , HUSSAIN, Zahid
CPC classification number: C07D498/10 , C07D519/00
Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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2.发明申请DERIVATIVES OF FLUORENE, ANTHRACENE, XANTHENE, DIBENZOSUBERONE AND ACRIDINE AND USES THEREOF 审中-公开荧光素，蒽醌，呫吨酮，二苯唑酮和吖啶的衍生物及其用途
公开(公告)号：WO2008140792A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/006015
申请日：2008-05-09
Applicant: AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Gene , CHELLAPPAN, Sheela , PADIA, Janak
Inventor： CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Gene , CHELLAPPAN, Sheela , PADIA, Janak
IPC: A61K31/185 , A61K31/135
CPC classification number: A61K31/395 , A61K31/18 , A61K31/409 , A61K31/435 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07C311/20 , C07C2601/14 , C07D211/96 , C07D295/26
Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
Abstract translation: 化学试剂，如芴，蒽，呫吨，二苯并uber酮和吖啶的二磺酰胺衍生物，以及类似的杂环结构（包括其盐），其作为抗癌剂和抗肿瘤剂，特别是当这些试剂调节Wnt的活性时 并且用于降低存在于细胞中的β-连环蛋白水平，例如癌细胞，或其中调节细胞系统（包括癌细胞）中基因表达水平的那些，以及其制备方法 试剂，以及含有这些试剂的活性成分的药物组合物和使用它们作为治疗剂的方法。
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公开(公告)号：WO2013165854A1
公开(公告)日：2013-11-07
申请号：PCT/US2013/038498
申请日：2013-04-26
Applicant: MERCK SHARP & DOHME CORP. , ACTON, John, J., III , YE, Feng , VACHAL, Petr , SHA, Deyou , DROPINSKI, James, F. , CHU, Lin , ONDEYKA, Debra , KIM, Alexander, J. , COLANDREA, Vincent, J. , ZANG, Yi , ZHANG, Fengqi , DONG, Guizhen
Inventor： ACTON, John, J., III , YE, Feng , VACHAL, Petr , SHA, Deyou , DROPINSKI, James, F. , CHU, Lin , ONDEYKA, Debra , KIM, Alexander, J. , COLANDREA, Vincent, J. , ZANG, Yi , ZHANG, Fengqi , DONG, Guizhen
IPC: A61K31/443
CPC classification number: C07D417/14 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/14
Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. Further, the pharmaceutical compositions of the present invention can include a pharmaceutically acceptable carrier and optionally other therapeutic ingredients.
Abstract translation: 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高人类患者的HDL-胆固醇和降低LDL-胆固醇，并用于治疗或预防动脉粥样硬化。 此外，本发明的药物组合物可以包括药学上可接受的载体和任选的其它治疗成分。
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公开(公告)号：WO2015047973A1
公开(公告)日：2015-04-02
申请号：PCT/US2014/056873
申请日：2014-09-23
Applicant: MERCK SHARP & DOHME CORP. , MERTZ, Eric , EDMONDSON, Scott, D. , SHAO, Ning , NEELAMKAVIL, Santhosh , POKER, Corey , HUSSAIN, Zahid , GUO, Zhuyan , KEVIN, Nancy Jo , ZANG, Yi , HE, Jiafang
Inventor： MERTZ, Eric , EDMONDSON, Scott, D. , SHAO, Ning , NEELAMKAVIL, Santhosh , POKER, Corey , HUSSAIN, Zahid , GUO, Zhuyan , KEVIN, Nancy Jo , ZANG, Yi , HE, Jiafang
IPC: C07K14/745
CPC classification number: C07D401/14 , A01N1/0226 , C07D211/60 , C07D401/06 , C07D401/10 , C12N9/6443 , C12Y304/21027
Abstract: The present invention provides a compound of Formula (I): and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract translation: 本发明提供式（I）的化合物：和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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公开(公告)号：WO2012024183A1
公开(公告)日：2012-02-23
申请号：PCT/US2011/047590
申请日：2011-08-12
Applicant: MERCK SHARP & DOHME CORP. , DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , ZWICKER, Aaron , SHERER, Edward, C. , PLOTKIN, Michael A. , MONINGKA, Remond , HUSSIAN, Zahid , WOOD, Harold B. , UJJAINWALLA, Feroze , ROMERO, Anthony , FINKE, Paul , ZANG, Yi , LIU, Weiguo
Inventor： DUFFY, Joseph, L. , BAO, Jianming , ONDEYKA, Debra, L. , TYAGARAJAN, Sriram , SHAO, Patrick , YE, Feng , KATIPALLY, Revathi , ZWICKER, Aaron , SHERER, Edward, C. , PLOTKIN, Michael A. , MONINGKA, Remond , HUSSIAN, Zahid , WOOD, Harold B. , UJJAINWALLA, Feroze , ROMERO, Anthony , FINKE, Paul , ZANG, Yi , LIU, Weiguo
CPC classification number: C07D498/10 , C07D519/00
Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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Patent Agency Ranking
公开(公告)号：WO2019070492A1
公开(公告)日：2019-04-11
申请号：PCT/US2018/053039
申请日：2018-09-27
Applicant: MERCK SHARP & DOHME CORP. , BIFTU, Tesfaye , HUANG, Xianhai , LIU, Weiguo , PAN, Weidong , PARK, Min , PASTERNAK, Alexander , SUN, Wanying , TANG, Haifeng , ZANG, Yi
Inventor： BIFTU, Tesfaye , HUANG, Xianhai , LIU, Weiguo , PAN, Weidong , PARK, Min , PASTERNAK, Alexander , SUN, Wanying , TANG, Haifeng , ZANG, Yi
IPC: A61K31/427 , A61K31/433 , A61K31/4439
Abstract: The present invention relates to monobactam compounds of Formula (I) and pharmaceutically acceptable salts thereof. The present invention also relates to compositions which comprise a monobactam compound of the invention or a pharmaceutically acceptable salt thereof, 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.
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7.发明申请BIARYL MONOBACTAM COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF BACTERIAL INFECTIONS 审中-公开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
Applicant: 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.
Inventor： 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: C07D205/08 , A61K31/397 , A61P31/04
CPC classification number: A61K31/397 , C07D417/14 , C07D471/04
Abstract: 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.
Abstract translation: 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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公开(公告)号：WO2016168098A1
公开(公告)日：2016-10-20
申请号：PCT/US2016/026858
申请日：2016-04-11
Applicant: MERCK SHARP & DOHME CORP. , MERTZ, Eric , EDMONDSON, Scott, D. , SO, Sung-Sau , SUN, Wanying , LIU, Weiguo , NEELAMKAVIL, Santhosh, F. , GAO, Ying-Duo , HRUZA, Alan , ZANG, Yi , ALI, Amjad , MAL, Rudrajit , HE, Jiafang , KUANG, Rongze , WU, Heping , OGAWA, Anthony, K. , NOLTING, Andrew, F.
Inventor： MERTZ, Eric , EDMONDSON, Scott, D. , SO, Sung-Sau , SUN, Wanying , LIU, Weiguo , NEELAMKAVIL, Santhosh, F. , GAO, Ying-Duo , HRUZA, Alan , ZANG, Yi , ALI, Amjad , MAL, Rudrajit , HE, Jiafang , KUANG, Rongze , WU, Heping , OGAWA, Anthony, K. , NOLTING, Andrew, F.
IPC: C07D233/68 , A61K31/426 , A61K31/4178 , A61P9/00 , C07D241/00
CPC classification number: C07D401/14 , C07D409/14 , C07D413/14
Abstract: The present invention provides a compound of Formula (I); and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract translation: 本发明提供式（I）的化合物; 和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维化改变的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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9.发明申请DERIVATIVES OF MULTI-RING AROMATIC COMPOUNDS AND USES AS ANTI-TUMOR AGENTS 审中-公开多环芳烃化合物的衍生物和作为抗肿瘤剂的用途
公开(公告)号：WO2010082912A1
公开(公告)日：2010-07-22
申请号：PCT/US2009/000257
申请日：2009-01-15
Applicant: AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W. H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
Inventor： CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W. H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
CPC classification number: C07D219/08
Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
Abstract translation: 公开了作为抗癌剂和抗肿瘤剂的化学试剂，例如芴，蒽，呫吨，二苯并西泮和吖啶的二磺酰胺衍生物，以及类似的杂环结构，包括其盐，以及制备这些试剂的方法 ，以及含有活性成分的药剂和使用它们作为治疗剂的方法的药物组合物。
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公开(公告)号：WO2015054087A1
公开(公告)日：2015-04-16
申请号：PCT/US2014/059213
申请日：2014-10-06
Applicant: MERCK SHARP & DOHME CORP. , SHAO, Ning , EDMONDSON, Scott, D. , NEELAMKAVIL, Santhosh , GUO, Zhuyan , MERTZ, Eric , ZANG, Yi , HE, Jiafang
Inventor： SHAO, Ning , EDMONDSON, Scott, D. , NEELAMKAVIL, Santhosh , GUO, Zhuyan , MERTZ, Eric , ZANG, Yi , HE, Jiafang
IPC: A61K31/397 , A61K31/7088 , C07D413/14
CPC classification number: C07D401/14 , C07C269/06 , C07D401/04 , C07D401/10 , C07D413/14
Abstract: The present invention provides a compound of Formula (I) (structurally represented) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Abstract translation: 本发明提供式（I）的化合物（结构上表示）和包含一种或多种所述化合物的药物组合物，以及使用所述化合物治疗或预防血栓形成，栓塞，高凝状态或纤维变化的方法。 该化合物是选择性因子XIa抑制剂或因子XIa和血浆激肽释放酶的双重抑制剂。
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