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1. 发明申请

US20170233382A1 PROCESSES FOR THE PREPARATION OF A BACE INHIBITOR 审中-公开
公开(公告)号：US20170233382A1
公开(公告)日：2017-08-17
申请号：US15503035
申请日：2015-08-10
申请人： Steven P. MILLER , Carmela MOLINARO , David THAISRIVONGS , Feng XU , Richard DESMOND , Hongming LI , Qinghao CHEN , Andrew STAMFORD , Zhiguo Jake SONG , Lushi TAN , Merck Sharp & Dohme Corp.
发明人： Steven P. Miller , Carmela Molinaro , David Thaisrivongs , Feng Xu , Richard Desmond , Hongming Li , Qinghao Chen , Andrew W. Stamford , Zhiguo Jake Song , Lushi Tan
IPC分类号： C07D417/12 , C07C313/06 , C07C311/33 , C07D213/81
CPC分类号： C07D417/12 , C07C303/40 , C07C311/33 , C07C311/35 , C07C313/06 , C07D213/81
摘要： This invention provides processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2. In addition, the invention provides certain synthetic intermediates which are useful, among other things, for the preparation of the Compound of Formula (I).

2. 发明申请

US20170166586A1 PROCESS FOR MAKING TETRACYCLIC HETEROCYCLE COMPOUNDS 审中-公开
公开(公告)号：US20170166586A1
公开(公告)日：2017-06-15
申请号：US15325392
申请日：2015-07-10
申请人： Hongming LI , Jingjun YIN , Kevin M. BELYK , Kevin R. CAMPOS , Qinghao CHEN , Alan M. HYDE , Tetsuji ITOH , Artis KLAPARS , Mathew Thomas TUDGE , Edward CLEATOR , Aaron M. DUMAS , Louis-Charles CAMPEAU , Yonggang CHEN , Ji QI , Wensong XIAO , MERCK SHARP & DOHME CORP. , MERCK SHARP & DOHME LIMITED , MSD R&D (CHINA) CO., LTD
发明人： Hongming Li , Jingjun Yin , Kevin M. Belyk , Kevin R. Campos , Qinghao Chen , Alan M. Hyde , Tetsuji Itoh , Artis Klapars , Matthew Thomas Tudge , Edward Cleator , Aaron M. Dumas , Louis-Charles Campeau , Yonggang Chen , Ji Qi , Wensong Xiao
IPC分类号： C07D498/04 , C07F9/6509 , C07D265/14 , C07D413/04 , C07C251/24 , C07D417/04
CPC分类号： C07D498/04 , C07C251/24 , C07D239/74 , C07D265/14 , C07D265/36 , C07D413/04 , C07D413/14 , C07D417/04 , C07F9/650994 , C07F17/02
摘要： The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2 and R3 are defined above herein. The present invention is also directed to compounds that are useful as synthetic intermediates in the process of the invention.

3. 发明授权

US09187488B2 Process for preparing chiral dipeptidyl peptidase-IV inhibitors 有权
标题翻译：制备手性二肽基肽酶-IV抑制剂的方法
公开(公告)号：US09187488B2
公开(公告)日：2015-11-17
申请号：US14119063
申请日：2012-06-25
申请人： Michael J. Zacuto , Robert F. Dunn , Aaron J. Moment , Jacob M. Janey , David Lieberman , Faye Sheen , Nadine Bremeyer , Jeremy Scott , Jeffrey T. Kuethe , Lushi Tan , Qinghao Chen
发明人： Michael J. Zacuto , Robert F. Dunn , Aaron J. Moment , Jacob M. Janey , David Lieberman , Faye Sheen , Nadine Bremeyer , Jeremy Scott , Jeffrey T. Kuethe , Lushi Tan , Qinghao Chen
IPC分类号： C07D487/04 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
摘要翻译：制备结构式I的吡唑并吡咯烷的方法：W是或P，其中在P中是胺保护基团。这些化合物可用于合成用于治疗2型糖尿病的二肽基肽酶-IV抑制剂。还提供了从该方法获得的有用的中间体。

4. 发明申请

US20100228036A1 PROCESS FOR MAKING GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开
标题翻译：制备葡萄糖激素受体配体的方法
公开(公告)号：US20100228036A1
公开(公告)日：2010-09-09
申请号：US12739483
申请日：2008-10-20
申请人： Qinghao Chen , Shinji Fujimori , Jacob M. Janey , John Limanto , Rafik Naccache , Andrew F. Nolting , Zhigou J. Song , Neil Strotman , Lushi Tan , Mark Weisel
发明人： Qinghao Chen , Shinji Fujimori , Jacob M. Janey , John Limanto , Rafik Naccache , Andrew F. Nolting , Zhigou J. Song , Neil Strotman , Lushi Tan , Mark Weisel
IPC分类号： C07D231/54
CPC分类号： C07D231/54
摘要： The invention encompasses a process for making 2-[1-phenyl-5-hydroxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives, which are glucocorticoid receptor ligands, useful for the treatment of inflammatory and immunological diseases.
摘要翻译：本发明包括制备可用于治疗炎症和免疫学的糖皮质激素受体配体的2- [1-苯基-5-羟基-4α-甲基 - 六氢环戊二烯并[f]吲唑-5-基]乙基苯基衍生物的方法疾病

5. 发明授权

US08406375B2 Article inspection device and inspection method 有权
标题翻译：物品检验装置及检验方法
公开(公告)号：US08406375B2
公开(公告)日：2013-03-26
申请号：US13142712
申请日：2010-12-28
申请人： Yigang Yang , Tiezhu Li , Qinjiar Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
发明人： Yigang Yang , Tiezhu Li , Qinjiar Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
IPC分类号： G01N23/201
CPC分类号： G01V5/0016 , G01N23/046 , G01N23/05 , G01N2223/419 , G01V5/0025
摘要： The present invention discloses an article inspection device, comprising: an x-ray machine, a collimation unit, a transmission detector array and a scattering detector array. The scattering detector array comprising a plurality of same scattering detector modules arranged in a matrix of i-rows and j-columns. A transmission cross section of the article transmitted by the x-rays is divided into a plurality of same sub-regions arranged in a matrix of i-rows and j-columns. The plurality of scattering detector modules arranged in i-rows and j-columns correspond to the plurality of sub-regions arranged in i-rows and j-columns one by one for detecting pair production effect annihilation photons and Compton-effect scattering photons from the respective sub-regions. Obtaining atomic numbers of the respective sub-regions based on a ratio of the pair production effect annihilation photon count to the Compton-effect scattering photon count, so as to form a three-dimensional image of the article. In addition, the present invention further discloses an article inspection method.
摘要翻译：本发明公开了一种物品检查装置，包括：x射线机，准直单元，透射检测器阵列和散射检测器阵列。散射检测器阵列包括以i行和j列的矩阵排列的多个相同的散射检测器模块。通过X射线透射的物品的透射截面被划分成以i行和j列的矩阵排列的多个相同的子区域。布置在i行和j列中的多个散射检测器模块对应于一排一列地排列在i行和j列中的多个子区域，用于检测来自该对象的生成效应湮灭光子和康普顿效应散射光子各分区域。基于对生产效应湮灭光子计数与康普顿效应散射光子计数的比率，获得各个子区域的原子序数，以形成物品的三维图像。此外，本发明还公开了一种物品检查方法。

6. 发明申请

US20120002788A1 ARTICLE INSPECTION DEVICE AND INSPECTION METHOD 有权
标题翻译：文章检查设备和检查方法
公开(公告)号：US20120002788A1
公开(公告)日：2012-01-05
申请号：US13142511
申请日：2010-12-29
申请人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
发明人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
IPC分类号： G01N23/201
CPC分类号： G01V5/0025
摘要： The present invention discloses an article inspection device, comprising: a x-ray machine, a collimation unit, a transmission detector array and at least one scattering detector array. Each of the at least one scattering detector array comprising a plurality of same scattering detector modules arranged in a matrix of i-rows and j-columns. A transmission cross section of the article transmitted by the x-rays is divided into a plurality of same sub-regions arranged in a matrix of i-rows and j-columns. The plurality of scattering detector modules arranged in i-rows and i-columns correspond to the plurality of sub-regions arranged in i-rows and j-columns one by one for detecting pair production effect annihilation photons and Compton-effect scattering photons from the respective sub-regions. Obtaining atomic numbers of the respective sub-regions based on a ratio of the pair production effect annihilation photon count to the Compton-effect scattering photon count, so as to form a three-dimensional image of the article. In addition, the present invention further discloses an article inspection method.
摘要翻译：本发明公开了一种物品检查装置，包括：x射线机，准直单元，透射检测器阵列和至少一个散射检测器阵列。所述至少一个散射检测器阵列中的每一个包括以i行和j列的矩阵排列的多个相同的散射检测器模块。通过X射线透射的物品的透射截面被划分成以i行和j列的矩阵排列的多个相同的子区域。布置在i行和i列中的多个散射检测器模块对应于一排一列地排列在i行和j列中的多个子区域，用于检测来自该对象的生成效应湮灭光子和康普顿效应散射光子各分区域。基于对生产效应湮灭光子计数与康普顿效应散射光子计数的比率来获得各个子区域的原子序数，以形成物品的三维图像。此外，本发明还公开了一种物品检查方法。

7. 发明授权

US08588370B2 Article inspection device and inspection method 有权
标题翻译：物品检验装置及检验方法
公开(公告)号：US08588370B2
公开(公告)日：2013-11-19
申请号：US13142511
申请日：2010-12-29
申请人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
发明人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
IPC分类号： G01N23/201
CPC分类号： G01V5/0025
摘要： The present invention discloses an article inspection device, comprising: a x-ray machine, a collimation unit, a transmission detector array and at least one scattering detector array. Each of the at least one scattering detector array comprising a plurality of same scattering detector modules arranged in a matrix of i-rows and j-columns. A transmission cross section of the article transmitted by the x-rays is divided into a plurality of same sub-regions arranged in a matrix of i-rows and j-columns. The plurality of scattering detector modules arranged in i-rows and i-columns correspond to the plurality of sub-regions arranged in i-rows and j-columns one by one for detecting pair production effect annihilation photons and Compton-effect scattering photons from the respective sub-regions. Obtaining atomic numbers of the respective sub-regions based on a ratio of the pair production effect annihilation photon count to the Compton-effect scattering photon count, so as to form a three-dimensional image of the article. In addition, the present invention further discloses an article inspection method.
摘要翻译：本发明公开了一种物品检查装置，包括：x射线机，准直单元，透射检测器阵列和至少一个散射检测器阵列。所述至少一个散射检测器阵列中的每一个包括以i行和j列的矩阵排列的多个相同的散射检测器模块。通过X射线透射的物品的透射截面被划分成以i行和j列的矩阵排列的多个相同的子区域。布置在i行和i列中的多个散射检测器模块对应于一排一列地排列在i行和j列中的多个子区域，用于检测来自该对象的生成效应湮灭光子和康普顿效应散射光子各分区域。基于对生产效应湮灭光子计数与康普顿效应散射光子计数的比率来获得各个子区域的原子序数，以形成物品的三维图像。此外，本发明还公开了一种物品检查方法。

8. 发明申请

US20120207271A1 ARTICLE INSPECTION DEVICE AND INSPECTION METHOD 有权
标题翻译：文章检查设备和检查方法
公开(公告)号：US20120207271A1
公开(公告)日：2012-08-16
申请号：US13142712
申请日：2010-12-28
申请人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
发明人： Yigang Yang , Tiezhu Li , Qinjian Zhang , Yi Zhang , Yingkang Jin , Qinghao Chen , Yuanjing Li , Yinong Liu
IPC分类号： G01N23/06
CPC分类号： G01V5/0016 , G01N23/046 , G01N23/05 , G01N2223/419 , G01V5/0025
摘要： The present invention discloses an article inspection device, comprising: an x-ray machine, a collimation unit, a transmission detector array and a scattering detector array. The scattering detector array comprising a plurality of same scattering detector modules arranged in a matrix of i-rows and j-columns. A transmission cross section of the article transmitted by the x-rays is divided into a plurality of same sub-regions arranged in a matrix of i-rows and j-columns. The plurality of scattering detector modules arranged in i-rows and j-columns correspond to the plurality of sub-regions arranged in i-rows and j-columns one by one for detecting pair production effect annihilation photons and Compton-effect scattering photons from the respective sub-regions. Obtaining atomic numbers of the respective sub-regions based on a ratio of the pair production effect annihilation photon count to the Compton-effect scattering photon count, so as to form a three-dimensional image of the article. In addition, the present invention further discloses an article inspection method.
摘要翻译：本发明公开了一种物品检查装置，包括：x射线机，准直单元，透射检测器阵列和散射检测器阵列。该散射检测器阵列包括以i行和j列的矩阵排列的多个相同的散射检测器模块。通过X射线透射的物品的透射截面被划分成以i行和j列的矩阵排列的多个相同的子区域。布置在i行和j列中的多个散射检测器模块对应于一排一列地排列在i行和j列中的多个子区域，用于检测来自该对象的生成效应湮灭光子和康普顿效应散射光子各分区域。基于对生产效应湮灭光子计数与康普顿效应散射光子计数的比率来获得各个子区域的原子序数，以形成物品的三维图像。此外，本发明还公开了一种物品检查方法。

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