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1. 发明专利

AU2003275522A1 ROLLER-TYPE CAPACITIVE DIGITAL-DISPLAY CALIPER 未知
公开(公告)号：AU2003275522A1
公开(公告)日：2004-05-13
申请号：AU2003275522
申请日：2003-10-21
申请人： ZHAO ZHIQIANG , ZHAO BIAO
发明人： ZHAO ZHIQIANG , ZHAO BIAO
IPC分类号： G01B3/20 , G01B7/02

2. 发明申请

WO2021257353A1 PLASMA KALLIKREIN INHIBITORS 审中-公开
公开(公告)号：WO2021257353A1
公开(公告)日：2021-12-23
申请号：PCT/US2021/036706
申请日：2021-06-10
申请人： MERCK SHARP & DOHME CORP. , JABRI, Salman , OGAWA, Anthony, Ken , SINZ, Christopher, J. , HICKS, Jacqueline, D. , CHENG, Alan, C. , GAO, Ying-Duo , YANG, Song , BAO, Jianming , HAYES, Donna, A., A., W. , LANG, Simon, B. , TAOKA, Brandon, M. , TIAN, Maoqun , SHEARN-NANCE, Galen, Paul , KUANG, Rongze , LOMBARDO, Matthew, J. , WU, Zhicai , ZHAO, Zhiqiang
发明人： JABRI, Salman , OGAWA, Anthony, Ken , SINZ, Christopher, J. , HICKS, Jacqueline, D. , CHENG, Alan, C. , GAO, Ying-Duo , YANG, Song , BAO, Jianming , HAYES, Donna, A., A., W. , LANG, Simon, B. , TAOKA, Brandon, M. , TIAN, Maoqun , SHEARN-NANCE, Galen, Paul , KUANG, Rongze , LOMBARDO, Matthew, J. , WU, Zhicai , ZHAO, Zhiqiang
IPC分类号： A61K31/4155 , C07D401/14 , A61P7/02
摘要： 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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.

3. 发明申请

WO2009073777A1 GAMMA SECRETASE MODULATORS 审中-公开
公开(公告)号：WO2009073777A1
公开(公告)日：2009-06-11
申请号：PCT/US2008/085515
申请日：2008-12-04
申请人： SCHERING CORPORATION , HUANG, Xianhai , PALANI, Anandan , QIN, Jun , ASLANIAN, Robert, G. , ZHU, Zhaoning , GREENLEE, William, J. , JOSIEN, Hubert , ZHOU, Wei , ZHU, Xiaohong , BENNETT, Chad, E. , PISSARNITSKI, Dmitri , MANDAL, Mihirbaran , DHONDI, Pawan , MCCRACKEN, Troy , BARA, Thomas , ZHAO, Zhiqiang , BURNETT, Duane , CLADER, John
发明人： HUANG, Xianhai , PALANI, Anandan , QIN, Jun , ASLANIAN, Robert, G. , ZHU, Zhaoning , GREENLEE, William, J. , JOSIEN, Hubert , ZHOU, Wei , ZHU, Xiaohong , BENNETT, Chad, E. , PISSARNITSKI, Dmitri , MANDAL, Mihirbaran , DHONDI, Pawan , MCCRACKEN, Troy , BARA, Thomas , ZHAO, Zhiqiang , BURNETT, Duane , CLADER, John
IPC分类号： C07D403/10 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/4738 , A61P25/28
CPC分类号： C07D471/04 , C07D403/10 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R 2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).
摘要翻译：本发明提供了γ分泌酶调节剂的新化合物。该化合物具有式（I），其中R 2为式（II）的稠合双环。还公开了使用式（I）化合物调节γ分泌酶活性的方法和治疗阿尔茨海默氏病的方法。

4. 发明申请

WO2009008980A2 TETRAHYDROPYRANOCHROMENE GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：四氢吡喃嗡烯γ-巯基化酶抑制剂
公开(公告)号：WO2009008980A2
公开(公告)日：2009-01-15
申请号：PCT/US2008008192
申请日：2008-07-01
申请人： SCHERING CORP , WU WEN-LIAN , BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI A , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL
发明人： WU WEN-LIAN , BARA THOMAS A , BURNETT DUANE A , CLADER JOHN W , DOMALSKI MARTIN S , JIN YAN , JOSIEN HUBERT B , LI HONGMEI , LIANG XIAN , PISSARNITSKI DMITRI A , SASIKUMAR THAVALAKULAMGARA K , WONG JESSE K , XU RUO , ZHAO ZHIQIANG , MCNAMARA PAUL
IPC分类号： C07D311/78 , A61K31/35 , A61K31/352 , A61P25/28 , C07D407/12 , C07D493/04
CPC分类号： C07D493/04 , C07D311/78 , C07D407/12
摘要： Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)-O-C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)-O-C(O)-heteroaryl and a basic tertiary amine.
摘要翻译：公开了下式的新型γ分泌酶抑制剂。还公开了抑制γ-分泌酶的方法，治疗神经退行性疾病的方法以及治疗阿尔茨海默氏病的方法。还公开了使用醛（或酮）和被两个吸电子基团取代的烷基的混合物在一个反应步骤中制备烯烃的方法，并使该混合物与以下物质反应：（a）磺酰卤（例如磺酰氯）（b）磺酰基酸酐和碱性胺，或（c）芳基-C（O） - 卤化物和碱性叔胺，或（d）芳基-C（O） - OC（O） - 芳基和碱性叔胺，或（e）杂芳基-C（O） - 卤化物和碱性叔胺，或（f）杂芳基-C（O）-OC（O） - 杂芳基和一种碱性叔胺。

5. 发明申请

WO2006004880A3 SUBSTITUTED N-ARYLSULFONYLHETEROCYCLIC AMINES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：作为GAMMA-分泌酶抑制剂的取代的N-芳基磺酰氧基化胺
公开(公告)号：WO2006004880A3
公开(公告)日：2007-03-08
申请号：PCT/US2005023187
申请日：2005-06-28
申请人： SCHERING CORP , JOSIEN HUBERT B , CLADER JOHN W , BARA THOMAS A , XU RUO , LI HONGMEI , PISSARNITSKI DMITRI , ZHAO ZHIQIANG
发明人： JOSIEN HUBERT B , CLADER JOHN W , BARA THOMAS A , XU RUO , LI HONGMEI , PISSARNITSKI DMITRI , ZHAO ZHIQIANG
IPC分类号： C07D265/30 , A61K31/5377 , A61P25/28 , C07D413/12 , C07D451/02 , C07D487/08
CPC分类号： C07D265/30 , C07D413/12 , C07D451/02 , C07D487/08
摘要： This invention discloses novel gamma secretase inhibitors of the formula I: wherein: L is -O- , -N(R 6 )-, -S-, -S(O)-, or -S(O 2 )-; R 1 is selected from the group consisting of aryl and heteroaryl; R 2 is selected from the group consisting of alkyl, -C(O)-Y, -X-C(O)-Y, -alkylene-X-C(O)-Y, -alkylene-C(O)-Y, -alkylene-cycloalkylene-X-C(O)-Y, -alkylene-cycloalkylene-C(O)-Y, -cycloalkylene-alkylene-X-C(O)-Y, -cycloalkylene-alkylene-C(O)-Y, -cycloalkylene-X-C(O)-Y, -cycloalkylene-C(O)-Y, -alkylene-cycloalkylene-alkylene-X-C(O)-Y, -alkylene-cycloalkylene-alkylene-C(O)-Y, aryl, and heteroaryl; R 3 is selected from the group consisting of aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, and alkoxyalkyl; each R 4 and R 5 is independently selected from the group consisting of H and alkyl; and Y is selected from the group consisting of -NR 8 R 9 , -N(R 6 )-(CH 2 ) b -NR 8 R 9 , aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, and arylheterocycloalkyl; or Y is selected from the group consisting of Formula II and Formula III: One or more compounds of formula I, or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
摘要翻译：本发明公开了式I的新型γ分泌酶抑制剂：其中：L是-O-，-N（R 6） - ， - S - ， - S（O） - 或-S（ 0 _{2 ） - ; R 1选自芳基和杂芳基; R 2选自烷基，-C（O）-Y，-XC（O）-Y， - 亚烷基-XC（O）-Y， - 亚烷基-C（O ）-Y-亚烷基 - 亚环烷基-OC（O）-Y-亚烷基 - 亚环烷基-C（O）-Y-亚烷基 - 亚烷基-OC（O）-Y-亚烷基 - 亚烷基-C（O） Y（ - ）亚环烷基-C（O）-Y-亚烷基-C（O）-Y-亚烷基 - 亚环烷基亚烷基-XC（O）-Y-亚烷基 - 亚环烷基 - 亚烷基-C（O）-Y，芳基和杂芳基; R 3选自芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基和烷氧基烷基; 每个R 4和R 5独立地选自H和烷基; 并且Y选自-NR 8 R 9，-N（R 6） - （CH 2）芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基和芳基杂环烷基 ; 或Y选自式II和式III的化合物：一种或多种式I化合物或包含该化合物的制剂可用于，例如，治疗阿尔茨海默病。}

6. 发明申请

WO2005097768A3 NOVEL GAMMA SECRETASE INHIBITORS 审中-公开
标题翻译：新的GAMMA SECRETASE抑制剂
公开(公告)号：WO2005097768A3
公开(公告)日：2005-12-15
申请号：PCT/US2005011456
申请日：2005-04-04
申请人： SCHERING CORP , ASBEROM THEODROS , CLADER JOHN W , JOSIEN HUBERT B , PISSARNITSKI DMITRI A , ZHAO ZHIQIANG , MCBRIAR MARK D
发明人： ASBEROM THEODROS , CLADER JOHN W , JOSIEN HUBERT B , PISSARNITSKI DMITRI A , ZHAO ZHIQIANG , MCBRIAR MARK D
IPC分类号： A61K31/44 , C07D211/96 , C07D401/06 , C07D401/12 , C07D401/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , A61P25/28
CPC分类号： C07D451/04 , C07D211/96 , C07D401/06 , C07D401/12 , C07D413/06 , C07D413/14 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Gamma-secretase inhibitors of the formula: Chemical formula should be inserted here as it appears on the abstract in paper form. are useful in treating various neurodegenerative diseases, wherein, for example: R1 includes unsubstituted or substituted aryl or heteroaryl groups; R2 includes -C(O)-Y, alkylene-C(O)-Y, alkylene-cycloalkylene-C(O)-Y, cycloalkylene-alkylene-C(O)-Y, alkylene cycloalkylene-alkylene-C(O)-Y, cycloalkylene-C(O)-Y, -S(O)-Y, alkylene-S(O)-Y, alkylene-cycloalkylene-S(O)-Y, cycloalkylene-alkylene-S(O)-Y, alkylene cycloalkylene-alkylene-S(O)-Y, cycloalkylene-S(O)-Y, -S(O2)-Y, alkylene-S(O2)-Y, alkylene cycloalkylene S(O2)-Y, cycloalkylene alkylene S(O2)-Y, alkylene cycloalkylene-alkylene-S(O2)-Y, and cycloalkylene-S(O2)-Y, wherein Y is as defined herein, and each of said alkylene or cycloalkylene may be unsubstituted or substituted as provided herein; each R3 is independently includes H, alkyl, O alkyl, OH, N(R9)2, acyl, and aroyl; or the moiety (R3)2, together with the ring carbon atom to which it is shown attached in formula I, defines a carbonyl group, -C(O)-; each R3A and R3B independently includes H, or alkyl; R11 includes aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. One or more of the compounds of formula I, or pharmaceutically acceptable salts, solvates, and/or esters, or compositions comprised thereof, may be used to treat, e.g., Alzheimer's Disease.
摘要翻译：化学式的γ-分泌酶抑制剂应插入此处，因为它以摘要形式出现在纸上。可用于治疗各种神经变性疾病，其中例如：R 1包括未取代或取代的芳基或杂芳基; R2包括-C（O）-Y，亚烷基-C（O）-Y，亚烷基 - 亚环烷基-C（O）-Y，亚环烷基 - 亚烷基-C（O）-Y，亚烷基亚环烷基 - 亚烷基-C （O）-Y，亚烷基-S（O）-Y，亚烷基 - 亚环烷基-S（O）-Y，亚环烷基 - 亚烷基-S（O）-Y （O）-Y，亚环烷基-S（O）-Y，-S（O 2）-Y，亚烷基-S（O 2）-Y，亚烷基亚环烷基S（O 2）-Y，亚环烷基亚烷基 S（O 2）-Y，亚烷基亚环烷基 - 亚烷基-S（O 2）-Y和亚环烷基-S（O 2）-Y，其中Y如本文所定义，并且所述亚烷基或亚环烷基中的每一个可以未被取代或如所提供的被取代本文; 每个R3独立地包括H，烷基，O烷基，OH，N（R9）2，酰基和芳酰基; 或部分（R 3）2与式I所示的环碳原子一起定义为羰基-C（O） - ; 每个R 3A和R 3B独立地包括H或烷基; R11包括芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。一种或多种式I化合物或其药学上可接受的盐，溶剂化物和/或酯或包含其的组合物可用于治疗例如阿尔茨海默氏病。

7. 发明申请

WO2016210215A1 3-TETRAZOLYL-BENZENE-1,2-DISULFONAMIDE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译：作为金属 - β-谷氨酰胺酶抑制剂的3-四氢 - 苯甲基-1,2-二磺酰胺衍生物
公开(公告)号：WO2016210215A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/039156
申请日：2016-06-24
申请人： MERCK SHARP & DOHME CORP. , BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack, D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , YANG, Dexi , YOUNG, Katherine , XIAO, Li , ZHANG, Zhibo , FU, Jianmin
发明人： BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack, D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , YANG, Dexi , YOUNG, Katherine , XIAO, Li , ZHANG, Zhibo , FU, Jianmin
IPC分类号： C07D403/12 , C07D413/14 , C07D401/10 , C07D403/10 , C07D403/14 , C07D407/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , A61K31/41 , A61K31/4184 , A61K31/428 , A61K31/4439 , A61P31/04
CPC分类号： C07D403/14 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/12 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to metallo-beta-lactamase inhibitor compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein Z, R A , X 1 , X 2 and R 1 are as defined herein. The present invention also relates to compositions which comprise a metallo-beta-lactamase inhibitor compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination with a beta-lactam antibiotic and/or a beta-lactamase inhibitor. The invention further relates to methods for treating a bacterial infection comprising administering to a patient a therapeutically effective amount of a compound of the invention, in combination with a therapeutically effective amount of one or more β-lactam antibiotics and optionally in combination with one or more beta-lactamase inhibitor compounds. The compounds of the invention are useful in the methods described herein for overcoming antibiotic resistance.
摘要翻译：本发明涉及式I的金属-β-内酰胺酶抑制剂化合物及其药学上可接受的盐，其中Z，RA，X 1，X 2和R 1如本文所定义。本发明还涉及包含本发明的金属-β-内酰胺酶抑制剂化合物或其药学上可接受的盐和可药用载体的组合物，任选地与β-内酰胺抗生素和/或β-内酰胺酶抑制剂组合。本发明还涉及用于治疗细菌感染的方法，其包括向患者施用治疗有效量的本发明化合物与治疗有效量的一种或多种β-内酰胺抗生素并任选与一种或多种组合 β-内酰胺酶抑制剂化合物。本发明的化合物可用于本文所述用于克服抗生素抗性的方法。

8. 发明申请

WO2016206101A1 METALLO-BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译： METALLO-BETA-LACTAMASE抑制剂
公开(公告)号：WO2016206101A1
公开(公告)日：2016-12-29
申请号：PCT/CN2015/082514
申请日：2015-06-26
申请人： MERCK SHARP & DOHME CORP. , BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , HUNTER, David , YANG, Dexi , ZHANG, Zhibo , FU, Jianmin , BAI, Yunfeng , ZHENG, Zhixiang , ZHANG, Xu , YOUNG, Katherine , XIAO, Li
发明人： BENNETT, Frank , JIANG, Jinlong , PASTERNAK, Alexander , DONG, Shuzhi , GU, Xin , SCOTT, Jack D. , TANG, Haiqun , ZHAO, Zhiqiang , HUANG, Yuhua , HUNTER, David , YANG, Dexi , ZHANG, Zhibo , FU, Jianmin , BAI, Yunfeng , ZHENG, Zhixiang , ZHANG, Xu , YOUNG, Katherine , XIAO, Li
IPC分类号： C07D257/04 , A61K31/41 , A61P31/04
CPC分类号： C07D403/14 , A61K31/416 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/498 , A61K31/5025 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K45/06 , A61P31/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D403/12 , C07D407/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
摘要翻译：本发明涉及金属β-内酰胺酶抑制剂的式I化合物，这种化合物的合成，以及这些化合物与β-内酰胺抗生素一起用于克服抗性的用途。

9. 发明申请

WO2015112441A1 METALLO-BETA-LACTAMASE INHIBITORS 审中-公开
标题翻译： METALLO-BETA-LACTAMASE抑制剂
公开(公告)号：WO2015112441A1
公开(公告)日：2015-07-30
申请号：PCT/US2015/011735
申请日：2015-01-16
申请人： MERCK SHARP & DOHME CORP. , MANDAL, Mihir , TANG, Haifeng , XIAO, Li , SU, Jing , LI, Guoqing , YANG, Shu-Wei , PAN, Weidong , TANG, Haiqun , DEJESUS, Reynalda , HICKS, Jacqueline , LOMBARDO, Matthew , CHU, Hong , HAGMANN, William , PASTERNAK, Alex , GU, Xin , JIANG, Jinlong , DONG, Shuzhi , DING, Fa-Xiang , LONDON, Clare , BISWAS, Dipshikha , YOUNG, Katherine , HUNTER, David, N. , ZHAO, Zhiqiang , YANG, Dexi
发明人： MANDAL, Mihir , TANG, Haifeng , XIAO, Li , SU, Jing , LI, Guoqing , YANG, Shu-Wei , PAN, Weidong , TANG, Haiqun , DEJESUS, Reynalda , HICKS, Jacqueline , LOMBARDO, Matthew , CHU, Hong , HAGMANN, William , PASTERNAK, Alex , GU, Xin , JIANG, Jinlong , DONG, Shuzhi , DING, Fa-Xiang , LONDON, Clare , BISWAS, Dipshikha , YOUNG, Katherine , HUNTER, David, N. , ZHAO, Zhiqiang , YANG, Dexi
IPC分类号： A61K31/41 , A61K31/4184 , C07D257/04
CPC分类号： C07D491/048 , A61K31/197 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D257/04 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D451/04 , C07D471/04 , C07D471/10 , C07D487/04 , Y02A50/473 , A61K2300/00
摘要： The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
摘要翻译：本发明涉及金属-β-内酰胺酶抑制剂的式（I）化合物，这些化合物的合成，以及这些化合物与β-内酰胺抗生素一起用于克服抗性的用途。

10. 发明申请

WO2015051052A3 GLUCOSE-RESPONSIVE INSULIN CONJUGATES 审中-公开
标题翻译：葡萄糖反应性胰岛素结合
公开(公告)号：WO2015051052A3
公开(公告)日：2015-07-02
申请号：PCT/US2014058714
申请日：2014-10-02
申请人： MERCK SHARP & DOHME , LIN SONGNIAN , YAN LIN , KEKEC AHMET , ZHU YUPING , HUNTER DAVID N , HUO PEI , FENG DANQING , NARGUND RAVI P , MOYES CHRISTOPHER R , ZHAO ZHIQIANG , PIPIK BRENDA , PISSARNITSKI DMITRI , DUFFY JOSEPH L , GUIDRY ERIN N
发明人： LIN SONGNIAN , YAN LIN , KEKEC AHMET , ZHU YUPING , HUNTER DAVID N , HUO PEI , FENG DANQING , NARGUND RAVI P , MOYES CHRISTOPHER R , ZHAO ZHIQIANG , PIPIK BRENDA , PISSARNITSKI DMITRI , DUFFY JOSEPH L , GUIDRY ERIN N
IPC分类号： A61K47/48 , A61P3/10
CPC分类号： A61K47/4823 , A61K38/28 , A61K47/48092 , A61K47/549 , A61K47/61 , C07K14/62
摘要： Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
摘要翻译：胰岛素缀合物包含共价连接到具有两个臂的至少一个双齿连接体的胰岛素分子，每个臂独立地连接到包含糖的配体，并且其中至少一个连接体的配体是岩藻糖。胰岛素缀合物显示药代动力学（PK）和/或药效学（PD）谱，其对糖类如葡萄糖或α-甲基甘露糖的全身浓度有反应，即使在不存在外源多价的情况下施用于有需要的受试者时糖结合分子如Con A.

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