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1. 发明申请

WO2005005396A1 PROCESS OF MAKING DI-ARYL UREA COMPOUNDS 审中-公开
标题翻译：制备二氨基脲化合物的方法
公开(公告)号：WO2005005396A1
公开(公告)日：2005-01-20
申请号：PCT/US2004/018694
申请日：2004-06-11
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC. , HADDAD, Nizar , WEI, Xudong , SENANAYAKE, Chris, Hugh , XU, Jinghua , YEE, Nathan
发明人： HADDAD, Nizar , WEI, Xudong , SENANAYAKE, Chris, Hugh , XU, Jinghua , YEE, Nathan
IPC分类号： C07D239/46
CPC分类号： C07D239/47 , C07C275/34 , C07D239/545
摘要： Disclosed is a process of making compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and Ra of formula (I) are defined herein. The product compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation. Also disclosed are intermediates useful in making such compounds.
摘要翻译：公开了制备其中本文定义式（I）的R 1，R 2，R 3，R 4和R a的式（I）的化合物的方法。产物化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及炎症的疾病和病理状况。还公开了可用于制备这些化合物的中间体。

2. 发明申请

WO2009137432A1 A METHOD FOR PREPARING MACROCYCLES 审中-公开
标题翻译：一种制备大环化合物的方法
公开(公告)号：WO2009137432A1
公开(公告)日：2009-11-12
申请号：PCT/US2009/042773
申请日：2009-05-05
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , SHU, Chutian , SENANAYAKE, Chris, Hugh , TAN, Zhulin , YEE, Nathan , ZENG, Xingzhong
发明人： SHU, Chutian , SENANAYAKE, Chris, Hugh , TAN, Zhulin , YEE, Nathan , ZENG, Xingzhong
IPC分类号： C07K1/00 , C07K5/12 , C07C6/06
CPC分类号： C07K5/0804 , C07K1/107
摘要： The present invention is directed to a method for the preparation of macrocyclic compounds of formula (I), comprising the step of cyclizing a diene of formula (II), in the presence of a catalyst, wherein R 1 -R 6 , A, W and V are as defined herein. The present invention is also directed to intermediate compounds of formula (II).
摘要翻译：本发明涉及一种制备式（I）的大环化合物的方法，包括在催化剂存在下使式（II）二烯环化的步骤，其中R 1 -R 6，A，W和V 如本文所定义。本发明还涉及式（II）的中间体化合物。

3. 发明申请

WO2003006431A1 A NOVEL SYNTHESIS FOR HETEROARYLAMINE COMPOUNDS 审中-公开
标题翻译：一种新型合成化合物
公开(公告)号：WO2003006431A1
公开(公告)日：2003-01-23
申请号：PCT/US2001/021671
申请日：2001-07-11
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
发明人： YEE, Nathan , KAPADIA, Suresh, R. , SONG, Jinhua, J.
IPC分类号： C07D213/38
CPC分类号： C07D213/40 , C07D213/36 , C07D213/38 , C07D213/50 , C07D213/53 , C07D213/55 , C07D213/80 , C07D405/04
摘要： Disclosed is a novel method of producing heteroaryl amines of formula (I), wherein X, Y and Z are described herein, the heteroarylamines are useful in the production of heteroaryl ureas which are key component in pharmaceutically active compounds possessing a heteroaryl urea group.
摘要翻译：公开了一种制备式（I）的杂芳基胺的新方法，其中X，Y和Z在本文中描述，杂芳基胺可用于制备作为具有杂芳基脲基团的药物活性化合物的关键组分的杂芳基脲。

4. 发明公开

EP1414800A1 A NOVEL SYNTHESIS FOR HETEROARYLAMINE COMPOUNDS 有权
标题翻译：新合成为杂芳基化合物
公开(公告)号：EP1414800A1
公开(公告)日：2004-05-06
申请号：EP01952573.2
申请日：2001-07-11
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS INC.
发明人： YEE, Nathan , KAPADIA, Suresh, R. , SONG, Jinhua, J.
IPC分类号： C07D213/38
CPC分类号： C07D213/40 , C07D213/36 , C07D213/38 , C07D213/50 , C07D213/53 , C07D213/55 , C07D213/80 , C07D405/04
摘要： Disclosed is a novel method of producing heteroaryl amines of formula (I), wherein X, Y and Z are described herein, the heteroarylamines are useful in the production of heteroaryl ureas which are key component in pharmaceutically active compounds possessing a heteroaryl urea group.

5. 发明授权

EP1414800B1 A NOVEL SYNTHESIS FOR HETEROARYLAMINE COMPOUNDS 有权
标题翻译：一种新型的杂芳胺化合物合成方法
公开(公告)号：EP1414800B1
公开(公告)日：2004-12-29
申请号：EP01952573.2
申请日：2001-07-11
申请人： BOEHRINGER INGELHEIM PHARMACEUTICALS INC.
发明人： YEE, Nathan , KAPADIA, Suresh, R. , SONG, Jinhua, J.
IPC分类号： C07D213/38
CPC分类号： C07D213/40 , C07D213/36 , C07D213/38 , C07D213/50 , C07D213/53 , C07D213/55 , C07D213/80 , C07D405/04
摘要： Disclosed is a novel method of producing heteroaryl amines of formula (I), wherein X, Y and Z are described herein, the heteroarylamines are useful in the production of heteroaryl ureas which are key component in pharmaceutically active compounds possessing a heteroaryl urea group.
摘要翻译：公开了生产式（I）的杂芳基胺的新方法，其中X，Y和Z如本文所述，杂芳基胺可用于制备杂芳基脲，杂芳基脲是具有杂芳基脲基团的药物活性化合物中的关键组分。

6. 发明申请

WO2010141334A1 SYNTHESIS OF CERTAIN TRIFLUOROMETHYL KETONES 审中-公开
标题翻译：某些三氟乙烯酮的合成
公开(公告)号：WO2010141334A1
公开(公告)日：2010-12-09
申请号：PCT/US2010/036504
申请日：2010-05-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , FANDRICK, Daniel Robert , YEE, Nathan , SONG, Jinhua J. , REEVES, Jonathan Timothy
发明人： FANDRICK, Daniel Robert , YEE, Nathan , SONG, Jinhua J. , REEVES, Jonathan Timothy
IPC分类号： C07C49/233 , C07C45/44 , C07C51/38 , C07C57/58 , C07C51/15 , C07C65/32 , C07C231/02 , C07C235/84
CPC分类号： C07C51/38 , C07C45/54 , C07C51/373 , C07C231/02 , C07C49/233 , C07C65/32 , C07C63/68 , C07C57/58 , C07C235/84
摘要： A process for synthesis of a compound of Formula (X) wherein R 1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; and R 2 and R 3 are each independently C 1 -C 5 alkyl.
摘要翻译：一种合成式（X）化合物的方法，其中R 1是被1至3个取代基取代的芳基，其中R 1的每个取代基独立地是C 1 -C 5烷基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，卤素，羧基，氰基或三氟甲基，其中R 1的每个取代基任选地独立地被一至三个选自C 1 -C 3烷基，C 1 -C 3烷氧基，苯基和烷氧基苯基的取代基取代; 并且R 2和R 3各自独立地为C 1 -C 5烷基。

7. 发明申请

WO2006033851A1 RING-CLOSING METATHESIS PROCESS IN SUPERCRITICAL FLUID 审中-公开
标题翻译：超临界流体中的闭环分解过程
公开(公告)号：WO2006033851A1
公开(公告)日：2006-03-30
申请号：PCT/US2005/032100
申请日：2005-09-09
申请人： BOEHRINGER INGELHEIM INTERNATIONAL, GMBH , GALLOU, Fabrice , YEE, Nathan
发明人： GALLOU, Fabrice , YEE, Nathan
IPC分类号： C07K1/00 , A61K38/06 , A61P31/14
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0804 , Y02P20/544
摘要： Disclosed is a process for preparing a compound of formula I comprising cyclizing a diene compound of formula III in the presence of a ruthenium catalyst in a suitable organic solvent, wherein the process is performed in a gaseous fluid at supercritical or near-supercritial conditions. The compounds of formula I are active agents for the treatment of hepatitis C viral (HCV) infections or are intermediates useful for the preparation of anti-HCV agents.
摘要翻译：公开了一种制备式I化合物的方法，其包括在钌催化剂存在下在合适的有机溶剂中使式III的二烯化合物环化，其中该方法在超临界或接近超临界条件下在气态流体中进行。式I化合物是用于治疗丙型肝炎病毒（HCV）感染的活性剂，或是可用于制备抗HCV药物的中间体。

8. 发明申请

WO2010141331A2 STEREOSELECTIVE SYNTHESIS OF CERTAIN TRIFLUOROMETHYL-SUBSTITUTED ALCOHOLS 审中-公开
标题翻译：某些三氟甲磺酸取代醇的立体选择性合成
公开(公告)号：WO2010141331A2
公开(公告)日：2010-12-09
申请号：PCT/US2010/036499
申请日：2010-05-28
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , FANDRICK, Daniel Robert , REEVES, Jonathan Timothy , SONG, Jinhua J. , TAN, Zhulin , QU, Bo , YEE, Nathan , RODRIGUEZ, Sonia
发明人： FANDRICK, Daniel Robert , REEVES, Jonathan Timothy , SONG, Jinhua J. , TAN, Zhulin , QU, Bo , YEE, Nathan , RODRIGUEZ, Sonia
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07B2200/07
摘要： A process for stereoselective synthesis of a compound of Formula (X): wherein: wherein: R 1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; R 2 and R 3 are each independently C 1 -C 5 alkyl; R 4 is C 1 -C 5 alkyl optionally independently substituted with one to three substituent groups, wherein each substituent group of R 4 is independently C 1 -C 3 alkyl, hydroxy, halogen, amino, or oxo; and R 5 is a heteroaryl group substituted with one to three substituent groups, wherein each substituent group of R 5 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, C 1 - C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or C 1 -C 5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone.
摘要翻译：一种用于立体选择性合成式（X）的化合物的方法：其中：其中：R1是被1至3个取代基取代的芳基，其中R1的每个取代基独立地是C1-C5烷基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，卤素，羧基，氰基或三氟甲基，其中R 1的每个取代基任选地独立地被一至三个选自C 1 -C 3烷基，C 1 -C 3烷氧基，苯基和烷氧基苯基的取代基取代; R2和R3各自独立地为C1-C5烷基; R4是任选独立地被1至3个取代基取代的C 1 -C 5烷基，其中R 4的每个取代基独立地是C 1 -C 3烷基，羟基，卤素，氨基或氧代; R5是被一至三个取代基取代的杂芳基，其中R5的每个取代基独立地是C 1 -C 5烷基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，烷基磺酰基氨基，氨基磺酰基，C 1 -C 5烷基氨基磺酰基，C 1 -C 5二烷基氨基磺酰基，卤素，羟基，羧基，氰基，三氟甲基，三氟甲氧基，三氟甲硫基或C 1 -C 5烷硫基，其中硫原子任选被氧化成亚砜或砜。

9. 发明申请

WO2008100954A2 POWER CONTROL WITH LINK IMBALANCE ON DOWNLINK AND UPLINK 审中-公开
标题翻译：在LINKLINK和UPLINK上连接不间断的电源控制
公开(公告)号：WO2008100954A2
公开(公告)日：2008-08-21
申请号：PCT/US2008/053749
申请日：2008-02-12
申请人： QUALCOMM Incorporated , MONTOJO, Juan , PATEL, Ketan N. , YEE, Nathan
发明人： MONTOJO, Juan , PATEL, Ketan N. , YEE, Nathan
IPC分类号： H04B7/005
CPC分类号： H04W52/06 , H04W52/08 , H04W52/10 , H04W52/143 , H04W52/146 , H04W52/262 , H04W52/325 , H04W52/40
摘要： Techniques for controlling transmit power are described. Due to link imbalance, a downlink (DL) serving cell may have the best downlink for a UE, and an uplink (UL) serving cell may have the best uplink for the UE. In one design of UL power control, the UE receives first and second UL TPC commands from the DL and UL serving cells, respectively, and adjusts its transmit power based on these UL TPC commands and in accordance with an OR-of-the-UPs rule. In one design of DL power control, the UE generates a DL TPC command based on received signal qualities of both the DL and UL serving cells. In another design, power control is performed independently for the DL and UL serving cells. The UE generates a separate DL TPC command for each cell, which adjusts its transmit power based on the DL TPC command for that cell.
摘要翻译：描述了用于控制发射功率的技术。由于链路不平衡，下行链路（DL）服务小区对于UE可以具有最佳下行链路，并且上行链路（UL）服务小区可以具有用于UE的最佳上行链路。在UL功率控制的一种设计中，UE分别从DL和UL服务小区接收第一和第二UL TPC命令，并且基于这些UL TPC命令并根据OR-of-UPs调整其发射功率规则。在DL功率控制的一种设计中，UE基于DL和UL服务小区的接收信号质量生成DL TPC命令。在另一种设计中，为DL和UL服务小区独立地执行功率控制。 UE为每个小区生成单独的DL TPC命令，根据该小区的DL TPC命令调整其发射功率。

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