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1. 发明申请

WO2019125879A2 CONJUGATE BASED SYSTEMS FOR CONTROLLED INSULIN DELIVERY 审中-公开
公开(公告)号：WO2019125879A2
公开(公告)日：2019-06-27
申请号：PCT/US2018/065321
申请日：2018-12-13
申请人： MERCK SHARP & DOHME CORP. , SMARTCELLS, INC. , YAN, Lin , HUO, Pei , KEKEC, Ahmet , ZHU, Yuping , PISSARNITSKI, Dmitri , FENG, Danqing, D. , MOYES, Chris , ZHAO, Zhiqiang , HUNTER, David, N. , LIN, Songnian , LANCASTER, Thomas, M. , CHEN, Benjamin
发明人： YAN, Lin , HUO, Pei , KEKEC, Ahmet , ZHU, Yuping , PISSARNITSKI, Dmitri , FENG, Danqing, D. , MOYES, Chris , ZHAO, Zhiqiang , HUNTER, David, N. , LIN, Songnian , LANCASTER, Thomas, M. , CHEN, Benjamin
IPC分类号： A61K47/64
摘要： The present disclosure provides conjugates which comprise an insulin molecule conjugated via a conjugate framework to one or more separate ligands that include a first saccharide, and wherein the conjugate framework also comprises a fatty chain (e.g., a C8-30 fatty chain). In certain embodiments, a conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic (PK) and/or pharmacodynamic (PD) property of the conjugate is sensitive to serum concentration of a second saccharide. In certain embodiments, a conjugate is also characterized by having a protracted PK profile. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.

2. 发明申请

WO2016081670A3 INSULIN RECEPTOR PARTIAL AGONISTS 审中-公开
公开(公告)号：WO2016081670A3
公开(公告)日：2016-05-26
申请号：PCT/US2015/061445
申请日：2015-11-19
申请人： MERCK SHARP & DOHME CORP. , LIN, Songnian , YAN, Lin , HUO, Pei , PISSARNITSKI, Dmitri , FENG, Danqing , NARGUND, Ravi , ZHU, Yuping , KEKEC, Ahmet , MADSEN-DUGGAN, Christina, B. , SHI, Zhi-Cai , WU, Zhicai , MU, Yingjun
发明人： LIN, Songnian , YAN, Lin , HUO, Pei , PISSARNITSKI, Dmitri , FENG, Danqing , NARGUND, Ravi , ZHU, Yuping , KEKEC, Ahmet , MADSEN-DUGGAN, Christina, B. , SHI, Zhi-Cai , WU, Zhicai , MU, Yingjun
IPC分类号： C07K14/62 , A61K38/28 , A61K47/48
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

3. 发明申请

WO2011146371A1 DIAZENIUMDIOLATE CYCLOHEXYL DERIVATIVES 审中-公开
标题翻译：二氮杂环丁烷衍生物
公开(公告)号：WO2011146371A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/036607
申请日：2011-05-16
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , YAN, Lin , HUO, Pei , NARGUND, Ravi
发明人： ALI, Amjad , YAN, Lin , HUO, Pei , NARGUND, Ravi
IPC分类号： A01N33/26 , A61K31/13 , A61K31/15
CPC分类号： C07C291/02 , C07B59/001 , C07C2601/14
摘要： A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R 3 is hydrogen, deuterium, -OH, -OC 1-6 alkyl, or halogen; R 8 is hydrogen, deuterium, or C 1-6 alkyl; R 11 and R 12 are independently hydrogen, -C 1-6 alkyl, -OH, -OC 1-6 alkyl, or halogen; R 13 and R 14 are independently -C 1-6 alkyl, -(CH 2 ) 1-2 OH, or -OC 1-6 alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or -C 1-6 alkyl; R 15 is (CR 1 R 2 ) n C(O)OR 16 , wherein n is 0, 1 or 2, -C(O)NHCH(R 17 )OR 16 , or -C(O)NHCH(R 17 )C(O)NHCH(R 18 )C(O)OR 16 ; R 16 is hydrogen, C 1-6 alkyl, or (CH 2 ) 1-2 N+R 19 R 20 R 21 ; R 1 , R 2 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , R 17 , R 18 , R 19 , R 20 , and R 21 are independently hydrogen or -C 1-6 alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.
摘要翻译：具有结构（I）的化合物或其药学上可接受的盐，其中R 3是氢，氘，-OH，-OC 1-6烷基或卤素; R8是氢，氘或C1-6烷基; R 11和R 12独立地是氢，-C 1-6烷基，-OH，-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基， - （CH 2）1-2 OH或-OC 1-6烷基，或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环原子和0或1个氧原子，其中所述环是未取代的或被卤素或-C 1-6烷基单取代，二取代或三取代; R15是（CR1R2）nC（O）OR16，其中n是0,1或2，-C（O）NHCH（R17）OR16或-C（O）NHCH（R17）C（O）NHCH（R18）（O）OR 16; R16是氢，C1-6烷基或（CH2）1-2N + R19R20R21; R 1，R 2，R 4，R 5，R 6，R 7，R 9，R 10，R 17，R 18，R 19，R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。

4. 发明申请

WO2020247297A1 GLUCOSE-RESPONSIVE INSULIN CONJUGATES 审中-公开
公开(公告)号：WO2020247297A1
公开(公告)日：2020-12-10
申请号：PCT/US2020/035503
申请日：2020-06-01
申请人： MERCK SHARP & DOHME CORP. , FENG, Danqing , LIN, Songnian , PISSARNITSKI, Dmitri, A. , PIPIK, Brenda , YAN, Lin , ZHU, Yuping
发明人： FENG, Danqing , LIN, Songnian , PISSARNITSKI, Dmitri, A. , PIPIK, Brenda , YAN, Lin , ZHU, Yuping
IPC分类号： A61K38/28 , A61K47/54 , A61K47/61 , C07K14/62
摘要： Glucose-responsive insulin conjugates that contain one or more linear oligomer sugar cluster are provided. Such insulin conjugates that may 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.

5. 发明申请

WO2017205309A1 INSULIN RECEPTOR PARTIAL AGONISTS 审中-公开
标题翻译：胰岛素受体部分激动剂
公开(公告)号：WO2017205309A1
公开(公告)日：2017-11-30
申请号：PCT/US2017/033900
申请日：2017-05-23
申请人： MERCK SHARP & DOHME CORP. , LIN, Songnian , YAN, Lin , HUO, Pei , PISSARNITSKI, Dmitri , FENG, Danqing , NARGUND, Ravi , MADSEN-DUGGAN, Christina , ZHU, Yuping , KEKEC, Ahmet , WU, Zhicai
发明人： LIN, Songnian , YAN, Lin , HUO, Pei , PISSARNITSKI, Dmitri , FENG, Danqing , NARGUND, Ravi , MADSEN-DUGGAN, Christina , ZHU, Yuping , KEKEC, Ahmet , WU, Zhicai
IPC分类号： A61K38/00 , A61K38/28 , C07K14/62 , C07K19/00
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
摘要翻译：公开了用作胰岛素受体的部分激动剂的胰岛素二聚体和胰岛素类似物二聚体。

6. 发明申请

WO2017160669A1 INSULIN-INCRETIN CONJUGATES 审中-公开
标题翻译：胰岛素 - INCRETIN共轭物
公开(公告)号：WO2017160669A1
公开(公告)日：2017-09-21
申请号：PCT/US2017/021999
申请日：2017-03-13
申请人： MERCK SHARP & DOHME CORP. , PALANI, Anandan , HUANG, Chunhui , YANG, Zhiqiang , YAN, Lin , LIN, Songnian , HUO, Pei , DENG, Qiaolin , BIANCHI, Elisabetta , ORVIETO, Federica
发明人： PALANI, Anandan , HUANG, Chunhui , YANG, Zhiqiang , YAN, Lin , LIN, Songnian , HUO, Pei , DENG, Qiaolin , BIANCHI, Elisabetta , ORVIETO, Federica
IPC分类号： C07K14/605 , C07K14/62 , C07D249/04
摘要： Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.
摘要翻译：包含对胰高血糖素样1（GLP-1）受体，胰高血糖素（GCG）受体和/或胃抑制蛋白（GIP）受体缀合物具有激动剂活性的肽的胰岛素 - 肠降血糖素缀合物涉及对胰岛素受体具有激动剂活性的胰岛素分子，以及使用所述缀合物治疗代谢疾病，例如2型糖尿病。

7. 发明申请

WO2011043914A1 DIURETICS 审中-公开
标题翻译：利尿剂
公开(公告)号：WO2011043914A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/049425
申请日：2010-09-20
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
发明人： ALI, Amjad , LO, Michael, Man-Chu , YAN, Lin
IPC分类号： A61K31/535
CPC分类号： C07D491/04
摘要： A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
摘要翻译：具有结构式（I）的化合物或其药学上可接受的盐，以及使用该化合物治疗高血压的方法。

8. 发明申请

WO2022055877A2 INSULIN RECEPTOR PARTIAL AGONISTS 审中-公开
公开(公告)号：WO2022055877A2
公开(公告)日：2022-03-17
申请号：PCT/US2021/049277
申请日：2021-09-07
申请人： MERCK SHARP & DOHME CORP. , PISSARNITSKI, Dmitri, A. , FENG, Danqing , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , NARGUND, Ravi , SHI, Zhicai , WU, Zhicai , YAN, Lin , ZHU, Yuping
发明人： PISSARNITSKI, Dmitri, A. , FENG, Danqing , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , NARGUND, Ravi , SHI, Zhicai , WU, Zhicai , YAN, Lin , ZHU, Yuping
IPC分类号： A61K38/28 , C07K14/62 , A61P3/10 , A61K47/60 , A61K38/00 , A61K47/55
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

9. 发明申请

WO2022046739A1 INSULIN RECEPTOR PARTIAL AGONISTS 审中-公开
公开(公告)号：WO2022046739A1
公开(公告)日：2022-03-03
申请号：PCT/US2021/047304
申请日：2021-08-24
申请人： MERCK SHARP & DOHME CORP. , MADSEN-DUGGAN, Christina, B. , FENG, Danqing , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , NARGUND, Ravi , MOYES, Christopher, R. , PISSARNITSKI, Dmitri, A. , SHI, Zhicai , WU, Zhicai , YAN, Lin , ZHU, Yuping
发明人： MADSEN-DUGGAN, Christina, B. , FENG, Danqing , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , NARGUND, Ravi , MOYES, Christopher, R. , PISSARNITSKI, Dmitri, A. , SHI, Zhicai , WU, Zhicai , YAN, Lin , ZHU, Yuping
IPC分类号： C07K14/62 , A61P3/10
摘要： Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

10. 发明申请

WO2018175272A1 GLUCOSE RESPONSIVE INSULIN COMPRISING A TRI-VALENT SUGAR CLUSTER FOR TREATMENT OF DIABETES 审中-公开
公开(公告)号：WO2018175272A1
公开(公告)日：2018-09-27
申请号：PCT/US2018/023052
申请日：2018-03-19
申请人： MERCK SHARP & DOHME CORP. , FENG, Danqing , HUNTER, David, N. , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , MOYES, Christopher, R. , NARGUND, Ravi , PIPIK, Brenda , PISSARNITSKI, Dmitri, A. , YAN, Lin , ZHAO, Zhiqiang , ZHU, Yuping
发明人： FENG, Danqing , HUNTER, David, N. , HUO, Pei , KEKEC, Ahmet , LIN, Songnian , MOYES, Christopher, R. , NARGUND, Ravi , PIPIK, Brenda , PISSARNITSKI, Dmitri, A. , YAN, Lin , ZHAO, Zhiqiang , ZHU, Yuping
IPC分类号： A61K38/28 , C07K14/62
摘要： An insulin conjugate comprising or consisting of a tri-valent sugar cluster is described. In particular aspects, the insulin conjugate displays 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.

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