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1. 发明申请

US20160297809A1 ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权
标题翻译：芳基链接的咪唑和三唑衍生物及其用于改善药物药代动力学的方法
公开(公告)号：US20160297809A1
公开(公告)日：2016-10-13
申请号：US15036274
申请日：2014-11-07
申请人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Chun Sing Li , Tingting Yu
IPC分类号： C07D417/14 , C07D417/12 , A61K31/496 , C07D487/04 , A61K31/4985 , A61K31/4439 , A61K31/427 , C07D401/12 , C07D405/14 , A61K31/4178 , C07D403/10 , A61K31/5377 , A61K31/4545 , C07D401/14 , A61K45/06 , A61K31/4725
CPC分类号： C07D417/14 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , A61K2300/00
摘要： The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
摘要翻译：本发明涉及芳基连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。

2. 发明授权

US10745377B2 Piperidine or piperazine linked imidazole and triazole derivatives and methods of use 有权
公开(公告)号：US10745377B2
公开(公告)日：2020-08-18
申请号：US15036268
申请日：2014-11-07
申请人： MERCK SHARP & DOHME CORP. , Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
IPC分类号： A61K31/4178 , A61K31/4439 , A61K31/4436 , A61K31/443 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/496 , C07D401/06 , C07D401/14 , C07D401/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D413/04 , C07D417/04 , A61K45/06 , A61K31/454 , C07D405/14 , C07D413/14 , C07D417/14 , C07D249/08 , C07D233/61 , A61P31/18 , C07D213/14 , C07D471/04 , A61K31/4545 , C07D471/10
摘要： The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.

3. 发明申请

US20160297792A1 PIPERIDINE OR PIPERAZINE LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 审中-公开
标题翻译：哌啶或哌嗪联结的咪唑和三唑衍生物及其用于改善药物药代动力学的方法
公开(公告)号：US20160297792A1
公开(公告)日：2016-10-13
申请号：US15036268
申请日：2014-11-07
申请人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
发明人： Craig A. Coburn , Milana M. Maletic , Yunfu Luo , Zhiqi Qi , Tingting Yu , Richard Soll
IPC分类号： C07D401/06 , C07D417/14 , C07D405/14 , C07D413/14 , A61K31/4545 , A61K45/06 , A61K31/4178 , C07D403/06 , A61K31/551 , C07D471/10 , A61K31/541 , A61K31/454 , C07D401/14
摘要： The present invention relates to piperidine or piperazine linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhibiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
摘要翻译：本发明涉及哌啶或哌嗪连接的咪唑和三唑衍生物，包含所述化合物单独或与其它药物组合的组合物，以及使用该化合物改善药物药代动力学的方法。本发明的化合物可用于抑制CYP3A4的人和兽医药物，并且用于改善由CYP3A4代谢的治疗化合物的药代动力学。

4. 发明申请

US20160108048A1 IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG 有权
标题翻译：咪唑衍生物及其用于改善药物药物动力学的方法
公开(公告)号：US20160108048A1
公开(公告)日：2016-04-21
申请号：US14895406
申请日：2014-06-02
申请人： Craig A. COBURN , Milana MALETIC , Yunfu LUO , Zhiqi QI , Chunsing LI , Tingting YU , Richard SOLL , MERCK SHARP & DOHME CORP.
发明人： Craig A. Coburn , Milana Maletic , Yunfu Luo , Zhiqi Qi , Chunsing Li , Tingting Yu , Richard Soll
IPC分类号： C07D487/04 , A61K31/4545 , C07D498/04 , A61K31/5383 , A61K31/4985 , A61K45/06 , A61K31/496 , A61K31/551 , C07D405/14 , C07D401/06 , C07D413/14 , C07D401/14 , A61K31/454
CPC分类号： C07D487/04 , A61K31/4375 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/513 , A61K31/5365 , A61K31/5383 , A61K31/55 , A61K31/551 , A61K45/06 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to Imidazole Derivatives of Formula (I), and pharmaceutically acceptable salts thereof, wherein A, B, Y, R1 and R2 are as defined herein. The present invention also relates to compositions comprising at least one Imidazole Derivative, and methods of using the Imidazole Derivatives for inhibiting CYP450 3A. Inhibition of CYP450 3A can be used to improve the pharmacokinetics of a drug that is metabolized by CYP450 3A4.
摘要翻译：本发明涉及式（I）的咪唑衍生物及其药学上可接受的盐，其中A，B，Y，R 1和R 2如本文所定义。本发明还涉及包含至少一种咪唑衍生物的组合物，以及使用咪唑衍生物抑制CYP450A 3A的方法。 CYP450 3A的抑制可用于改善由CYP450 3A4代谢的药物的药代动力学。

5. 发明申请

US20120194804A1 SEMICONDUCTOR LASER BASED INTRA-CAVITY OPTICAL MICRO-FLUIDIC BIOSENSOR 审中-公开
标题翻译：基于半导体激光器的光敏微流体生物传感器
公开(公告)号：US20120194804A1
公开(公告)日：2012-08-02
申请号：US13496886
申请日：2010-10-14
申请人： Jian-Jun He , Tingting Yu , Min Lou
发明人： Jian-Jun He , Tingting Yu , Min Lou
IPC分类号： G01N21/41
CPC分类号： G01N21/7746 , G01N21/05 , G01N21/45 , G01N2021/0346 , G01N2021/391 , G01N2021/399 , G01N2021/458
摘要： A semiconductor laser based intra-cavity optical micro-fluidic biosensor comprises a coupled-cavity semiconductor laser, a 2×2 coupler and a phase adjustment section on one input port of the coupler. The dominant mode of the coupled-cavity laser appears in one output port of the coupler, while the adjacent mode comes out from the other output port of the coupler. The resonant frequency interval of the sensing cavity is slightly larger or smaller than one half of that of the reference cavity. Part of the sensing cavity is the sensing section which is covered by an analyte. The refractive index change of the analyte will cause the lasing mode of the coupled cavity to switch to an adjacent mode, resulting in a π-phase change in the phase difference between the two output ports of the two resonance cavities. By applying the Vernier effect, the power ratio of the two output ports of the coupler will change and the refractive index change of the analyte can be derived. A detection limit of 10−8 RIU or smaller can be achieved.
摘要翻译：基于半导体激光的腔内光学微流体生物传感器包括耦合腔的一个输入端口上的耦合腔半导体激光器，2×2耦合器和相位调整部分。耦合腔激光器的主要模式出现在耦合器的一个输出端口中，而相邻模式从耦合器的另一个输出端口出来。感应腔的谐振频率间隔略大于或小于参考腔的谐振频率间隔的一半。感测腔的一部分是被分析物覆盖的感测部分。分析物的折射率变化将导致耦合空腔的激光模式切换到相邻模式，导致两个谐振腔的两个输出端口之间的相位差的相位变化。通过应用游标效应，耦合器的两个输出端口的功率比将改变，并且可以导出分析物的折射率变化。可以实现10-8 RIU以下的检测限。

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