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1. 发明申请

WO2022020550A1 ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY 审中-公开
公开(公告)号：WO2022020550A1
公开(公告)日：2022-01-27
申请号：PCT/US2021/042702
申请日：2021-07-22
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , BOYCE, Christopher, W. , CUMMING, Jared, N. , DEMONG, Duane , GRAHAM, Thomas, H. , GUDIPATI, Subrahmanyam , HOOVER, Andrew, J. , HUANG, Xianhai , KUANG, Rongze , KIM, Jae-Hun , KELLY, Joseph, M. , LIM, Yeon-Hee , LO, Michael, Man-Chu , MORENO, Jesus , SU, Jing , WU, Heping , XIAO, Dong , YU, Younong , ZHU, Xiaohong
发明人： ALI, Amjad , BOYCE, Christopher, W. , CUMMING, Jared, N. , DEMONG, Duane , GRAHAM, Thomas, H. , GUDIPATI, Subrahmanyam , HOOVER, Andrew, J. , HUANG, Xianhai , KUANG, Rongze , KIM, Jae-Hun , KELLY, Joseph, M. , LIM, Yeon-Hee , LO, Michael, Man-Chu , MORENO, Jesus , SU, Jing , WU, Heping , XIAO, Dong , YU, Younong , ZHU, Xiaohong
IPC分类号： A61K31/519 , C07D487/04 , C07D487/08 , C07D513/04
摘要： The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

2. 发明申请

WO2018136678A1 SYSTEM AND METHOD FOR PRODUCING PULLING ROLL FOR MANUFACTURING SHEET 审中-公开
公开(公告)号：WO2018136678A1
公开(公告)日：2018-07-26
申请号：PCT/US2018/014320
申请日：2018-01-19
申请人： CORNING INCORPORATED , KIM, Jae-hun , KWON, Tae-hyung , LEE, Yong-jae , SHIN, Tae-bong , SIM, Youn-sub
发明人： KIM, Jae-hun , KWON, Tae-hyung , LEE, Yong-jae , SHIN, Tae-bong , SIM, Youn-sub
IPC分类号： F16C13/00 , G01G19/00
摘要： Provided are a method and system for producing a pulling roll for manufacturing a sheet. The method includes measuring a weight of each of a plurality of disks, classifying and stacking the plurality of disks into a plurality of disk groups divided into different first weight ranges, and selecting disks included in any one of the plurality of disk groups by a first gripper and mounting the disks on an adapter.

3. 发明申请

WO2016137131A3 SOFT CAPSULE COMPOSITION 审中-公开
标题翻译：软胶囊组合物
公开(公告)号：WO2016137131A3
公开(公告)日：2016-10-20
申请号：PCT/KR2016000999
申请日：2016-01-29
申请人： KIM JAE-HUN
发明人： KIM JAE-HUN
IPC分类号： A61K9/48 , A61K9/50 , A61K47/38
CPC分类号： A61K9/48 , A61K9/50 , A61K47/38
摘要： The present invention relates to a soft capsule composition comprising a film-forming agent in the form of a water-soluble cellulose ether, a gelling agent in the form of iota carrageenan, an auxiliary gelling agent in the form of an organic-based calcium salt, a plasticizer in the form of glycerol, a disintegration-promoting agent in the form of silicon dioxide and distilled water. According to the present invention, when a soft capsule is to be moulded, energy is reduced as the gelling temperature of a film solution is lowered, and it is possible to perform moulding work over a long time as a resilient wet film can be produced even if the film solution is stored over a long time. Consequently, the moulding workability of the soft capsule is improved. Also, according to the present invention, it is possible to provide a soft capsule having outstanding disintegrability despite also having outstanding resilience.
摘要翻译：本发明涉及一种软胶囊组合物，其包含水溶性纤维素醚形式的成膜剂，ι角叉菜胶形式的胶凝剂，有机基钙盐形式的辅助胶凝剂，甘油形式的增塑剂，二氧化硅和蒸馏水形式的崩解促进剂。根据本发明，当软胶囊被模塑时，由于膜溶液的凝胶化温度降低，所以能量降低，并且可以长时间进行成型加工，因为可以生产弹性湿膜甚至如果胶片溶液长时间存放。因此，软胶囊的成型加工性提高。此外，根据本发明，尽管也具有优异的弹性，但是可以提供具有优异的崩解性的软胶囊。

4. 发明申请

WO2015026686A1 3'-PYRIDYL SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES 审中-公开
标题翻译： 3'-吡啶基取代的6,6-二氟双环衍生物衍生物
公开(公告)号：WO2015026686A1
公开(公告)日：2015-02-26
申请号：PCT/US2014/051404
申请日：2014-08-18
申请人： MERCK SHARP & DOHME CORP. , DROPINSKI, James Francis , MALETIC, Milana , KIM, Jae-Hun , SHA, Deyou
发明人： DROPINSKI, James Francis , MALETIC, Milana , KIM, Jae-Hun , SHA, Deyou
IPC分类号： A61K31/44 , C07D405/06
CPC分类号： A61K31/60 , A61K31/343 , A61K31/4365 , A61K31/444 , A61K45/06 , C07D405/14 , C07D409/04 , C07D409/14 , A61K2300/00
摘要： The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is halo; -CN; alkyi; cycloalkyi; alkoxy; phenyl, which is optionally substituted one or twice independently by alkyi, halo, or -CN; or a thiophene ring, which is optionally substituted once or twice independently by alkyi. The compounds of the invention are effective inhibitors of the PAR-I receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
摘要翻译：本发明涉及下式的双环贺姆酸衍生物或其药学上可接受的盐，其中：R1为卤素; -CN; 烷基; 环烷基; 烷氧基; 苯基，其任选被烷基，卤素或-CN独立地取代一次或两次; 或噻吩环，其任选被烷基独立地取代一次或两次。本发明的化合物是PAR-1受体的有效抑制剂。本发明化合物可用于治疗或预防疾病状态如ASC，二次预防心肌梗塞或中风或PAD。

5. 发明申请

WO2014101373A1 HETEROBICYCLO-SUBSTITUTED-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS FOR TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDER 审中-公开
标题翻译： [1,2,4]三唑并[1,5-C]喹唑啉-5-胺化合物用于治疗中枢神经系统疾病
公开(公告)号：WO2014101373A1
公开(公告)日：2014-07-03
申请号：PCT/CN2013/076853
申请日：2013-06-06
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping
发明人： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , HUANG, Xianhai , HENDERSON, Timothy J. , KIM, Jae-Hun , BOYCE, Christopher , TING, Pauline , ZHENG, Junying , METZGER, Edward , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping
IPC分类号： C07D519/00 , A61K31/519 , A61P25/16
CPC分类号： C07D519/00 , C07D487/04
摘要： Disclosed are compounds of heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine herein, which have specific binding on an A 2A -receptor and are useful for quantifying in vivo receptor-site occupancy of various compounds which have an affinity for binding to an A 2A -receptor.
摘要翻译：公开了本文中具有与A2A受体的特异性结合的异二环取代的[1,2,4]三唑并[1,5-c]喹唑啉-5-胺的化合物，并且可用于定量体内受体位点占有率具有与A2A受体结合的亲和力的各种化合物。

6. 发明申请

WO2011155661A1 LINEAR EFFUSION CELL, METHOD OF MANUFACTURING THE SAME AND EVAPORATOR USING THE SAME 审中-公开
标题翻译：线性效应细胞，其制造方法和使用其的蒸发器
公开(公告)号：WO2011155661A1
公开(公告)日：2011-12-15
申请号：PCT/KR2010/005031
申请日：2010-07-30
申请人： KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY , WOO, Deok Ha , KIM, Sun Ho , LEE, Seok , BYUN, Young Tae , JHON, Young Min , KIM, Jae Hun , PARK, Min Chul , KIM, Shin Geun , JUNG, Yong Woo
发明人： WOO, Deok Ha , KIM, Sun Ho , LEE, Seok , BYUN, Young Tae , JHON, Young Min , KIM, Jae Hun , PARK, Min Chul , KIM, Shin Geun , JUNG, Yong Woo
IPC分类号： C23C14/24 , C23C14/04
CPC分类号： C23C14/243 , C23C14/12 , C23C14/14 , C23C14/26
摘要： Disclosed herein is a linear effusion cell, which is used in a vacuum deposition system, including: a crucible made of pyrolytic boron nitride (PBN), having an open upper portion and containing a raw material; a first heat generating unit formed on an outer surface of the crucible and having a pattern suitable for heating; an array of orifices formed through the lateral sides of the crucible and the first heat generating unit.
摘要翻译：本文公开了一种在真空沉积系统中使用的线性渗流池，包括：由热解氮化硼（PBN）制成的坩埚，其具有敞开的上部并且包含原料; 形成在坩埚的外表面上并具有适于加热的图案的第一发热单元; 通过坩埚和第一发热单元的侧面形成的孔阵列。

7. 发明申请

WO2010059602A3 INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE 审中-公开
标题翻译：二乙酰胆碱酯酶抑制剂
公开(公告)号：WO2010059602A3
公开(公告)日：2010-07-15
申请号：PCT/US2009064738
申请日：2009-11-17
申请人： SCHERING CORP , TING PAULINE C , ASLANIAN ROBERT G , CAPLEN MARY ANN , CAO JIANHUA , CHAN TIN-YAU , KIM DAVID WON-SHIK , KIM HYUNJIN , KIM JAE-HUN , KUANG RONGZE , LEE JOE F , SCHWERDT JOHN H , WU HEPING , ZORN NICOLAS
发明人： TING PAULINE C , ASLANIAN ROBERT G , CAPLEN MARY ANN , CAO JIANHUA , CHAN TIN-YAU , KIM DAVID WON-SHIK , KIM HYUNJIN , KIM JAE-HUN , KUANG RONGZE , LEE JOE F , SCHWERDT JOHN H , WU HEPING , ZORN NICOLAS
IPC分类号： A61P3/00 , A61K31/422 , A61K31/427 , A61P9/00 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04
CPC分类号： C07D413/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04
摘要： The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase ("DGAT") inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).
摘要翻译：本发明涉及作为二酰基甘油酰基转移酶（“DGAT”）抑制剂的新型杂环化合物，包含杂环化合物的药物组合物以及该化合物用于治疗或预防心血管疾病，代谢障碍，肥胖或肥胖相关障碍的用途，糖尿病，血脂异常，糖尿病并发症，葡萄糖耐量降低或空腹血糖受损。本发明的说明性化合物如下所示：式（I）。

8. 发明申请

WO2018118829A1 HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS 审中-公开
公开(公告)号：WO2018118829A1
公开(公告)日：2018-06-28
申请号：PCT/US2017/067163
申请日：2017-12-19
申请人： MERCK SHARP & DOHME CORP. , MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
发明人： MCKITTRICK, Brian , CALDWELL, John, P. , MCCAULEY, John, A. , VACCARO, Henry , CHAN, Tin-Yau , KIM, Hyunjin , SMITH, Elizabeth , HONG, Liwu , KHAN, Tanweer , YING, Shihong , WANG, Hongwu , WILLIAMS, Peter, D. , KIM, Jae-Hun , NOLT, M. Brad , CAPLEN, Mary Ann
IPC分类号： A61K31/4178 , C07D403/06 , C07D493/04
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

9. 发明申请

WO2016126570A1 AMINOQUINAZOLINE COMPOUNDS AS A2A ANTAGONIST 审中-公开
标题翻译：氨基喹啉化合物作为A2A拮抗剂
公开(公告)号：WO2016126570A1
公开(公告)日：2016-08-11
申请号：PCT/US2016/015881
申请日：2016-02-01
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , ZHOU, Gang , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , TING, Pauline, C. , BIJU, Purakkattle , RUIZ, Manuel de Lera , DEGRADO, Sylvia, J. , TUNG, Alexander, L. , HENDERSON, Timothy, J. , HONG, Liwu , KIM, Jae-Hun , KIM, David Won-Shik , LEE, Joe, F. , WU, Jie , WU, Heping , XIAO, Yushi , YU, Tao , ZHU, Xiaohong , MCCORMICK, Kevin, D. , TAGAT, Jayaram, R. , XIAO, Dong , KHAN, Tanweer , CAO, Jianhua , BERLIN, Michael , ZHANG, Yonglian
发明人： ALI, Amjad , ZHOU, Gang , KUANG, Rongze , LIM, Yeon-Hee , LO, Michael Man-Chu , TING, Pauline, C. , BIJU, Purakkattle , RUIZ, Manuel de Lera , DEGRADO, Sylvia, J. , TUNG, Alexander, L. , HENDERSON, Timothy, J. , HONG, Liwu , KIM, Jae-Hun , KIM, David Won-Shik , LEE, Joe, F. , WU, Jie , WU, Heping , XIAO, Yushi , YU, Tao , ZHU, Xiaohong , MCCORMICK, Kevin, D. , TAGAT, Jayaram, R. , XIAO, Dong , KHAN, Tanweer , CAO, Jianhua , BERLIN, Michael , ZHANG, Yonglian
IPC分类号： A61K31/517 , C07D239/84 , C07D403/12
CPC分类号： C07D239/84 , A61K31/517 , A61P25/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to compounds of generic formula I: or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist.
摘要翻译：本发明涉及被认为可用作A2A受体拮抗剂的通式I化合物或其药学上可接受的盐。

10. 发明申请

WO2014101113A1 PIPERAZINE-SUBSTITUTED 7-METHOXY-[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 审中-公开
标题翻译：哌嗪取代的具有A2A拮抗剂性质的7-甲氧基 - [1,2,4]三唑[1,5-C]喹唑啉-5-胺化合物
公开(公告)号：WO2014101113A1
公开(公告)日：2014-07-03
申请号：PCT/CN2012/087851
申请日：2012-12-28
申请人： MERCK SHARP & DOHME CORP. , ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , BERLIN, Michael , TING, Pauline , ZHOU, Gang , YU, Tao , BOYCE, Christopher , KELLY, Joseph Michael , TAGAT, Jayaram R. , ZHENG, Junying , HUANG, Xianhai , ZHOU, Wei , KIM, Jae-Hun , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping , ANAND, Rajan
发明人： ALI, Amjad , LO, Michael Man-Chu , LIM, Yeon-Hee , STAMFORD, Andrew , KUANG, Rongze , TEMPEST, Paul , YU, Younong , BERLIN, Michael , TING, Pauline , ZHOU, Gang , YU, Tao , BOYCE, Christopher , KELLY, Joseph Michael , TAGAT, Jayaram R. , ZHENG, Junying , HUANG, Xianhai , ZHOU, Wei , KIM, Jae-Hun , ZORN, Nicolas , XIAO, Dong , GALLO, Gioconda V. , WON, Walter , WU, Heping , ANAND, Rajan
IPC分类号： C07D487/04 , A61K31/4196 , A61K31/517 , A61K31/519 , A61P25/28
CPC分类号： C07D487/04 , C07D487/08 , C07D487/18 , C07D513/04
摘要： Disclosed are compounds of Formula (A), as defined herein, which have binding activity for an A 2A -receptor and are believed to be useful for treatment or management of CNS diseases or conditions which can be treated or managed using compounds which have A 2A receptor antagonist activity.
摘要翻译：公开了本文定义的式（A）化合物，其具有对A2A受体的结合活性，并被认为可用于治疗或治疗CNS疾病或病症，其可以使用具有A2A受体拮抗剂的化合物治疗或治疗活动。

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