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1. 发明申请

US20110124867A1 Process and intermediates for the Synthesis of heterocyclic Substituted Piperazines with CXCR3 Antagonist Activity 审中-公开
标题翻译：用CXCR3拮抗剂活性合成杂环取代的哌嗪的方法和中间体
公开(公告)号：US20110124867A1
公开(公告)日：2011-05-26
申请号：US12809101
申请日：2008-12-16
申请人： Frank Xing Chen , Timothy D. Cutarelli , Xiayong Fu , Xian Liang , Timothy L. McAllister , Robert K. Orr , Jianguo Yin , Kelvin H. Yong , Man Zhu
发明人： Frank Xing Chen , Timothy D. Cutarelli , Xiayong Fu , Xian Liang , Timothy L. McAllister , Robert K. Orr , Jianguo Yin , Kelvin H. Yong , Man Zhu
IPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D241/04 , C07D211/44
CPC分类号： C07D413/14 , C07D211/44 , C07D239/42 , C07D295/205
摘要： The present invention relates to novel processes for the preparation of the compound of the Formula A45: or a physiologically acceptable salt, solvate or prodrug thereof, which has utility, for example, as a pharmaceutically active compound with CXCR3 antagonist activity, and to novel intermediates useful in the synthesis thereof.
摘要翻译：本发明涉及制备式A45化合物或其生理上可接受的盐，溶剂合物或前体药物的新方法，其可用于例如具有CXCR3拮抗剂活性的药物活性化合物和新中间体可用于其合成。

2. 发明授权

US07985860B2 Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives 失效
标题翻译：用于合成2-（喹啉-5-基）-4,5二取代 - 唑衍生物的方法和中间体
公开(公告)号：US07985860B2
公开(公告)日：2011-07-26
申请号：US11891348
申请日：2007-08-10
申请人： Timothy D. Cutarelli , Xiaoyong Fu , Timothy L. McAllister , Michael R. Reeder , Jianguo Yin , Kelvin H. Yong , Shuyi Zhang
发明人： Timothy D. Cutarelli , Xiaoyong Fu , Timothy L. McAllister , Michael R. Reeder , Jianguo Yin , Kelvin H. Yong , Shuyi Zhang
IPC分类号： C07D215/38
CPC分类号： C07D413/04 , C07C271/22 , C07D413/14
摘要： This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.
摘要翻译：本申请公开了一种合成2-（喹啉-5-基）-4,5-二取代 - 唑衍生物的新方法，其可用作药物制剂中的PDE IV抑制剂化合物。

3. 发明申请

US20100324295A1 PROCESS FOR THE PRODUCTION OF SUBSTITUTED 5-QUINOLYL-OXAZOLES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：生产取代的5-喹啉酮和其药学上可接受的盐的方法
公开(公告)号：US20100324295A1
公开(公告)日：2010-12-23
申请号：US12668192
申请日：2008-07-03
申请人： Timothy D. Cutarelli , Dimitar L. Filipov , Christopher Stanley Pridgen , Michael R. Reeder , Kelvin H. Yong , Dimitrios N. Zarkadas
发明人： Timothy D. Cutarelli , Dimitar L. Filipov , Christopher Stanley Pridgen , Michael R. Reeder , Kelvin H. Yong , Dimitrios N. Zarkadas
IPC分类号： C07D413/14 , C07D413/02
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention relates a process for the preparation of a compound of the formula: wherein R1, R2, R6, R9 and R10 are as described herein. The compounds are inhibitors of phosphodiesterase 4 (PDE4).
摘要翻译：本发明涉及制备下式化合物的方法：其中R 1，R 2，R 6，R 9和R 10如本文所述。这些化合物是磷酸二酯酶4（PDE4）的抑制剂。

4. 发明申请

US20100137597A1 SYNTHESIS Of DIETHYLPHOSPHONATE 有权
标题翻译：二乙基磷酸酯的合成
公开(公告)号：US20100137597A1
公开(公告)日：2010-06-03
申请号：US12701174
申请日：2010-02-05
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07F9/40
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

5. 发明授权

US08329905B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
标题翻译： {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成
公开(公告)号：US08329905B2
公开(公告)日：2012-12-11
申请号：US12701174
申请日：2010-02-05
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Thiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Thiruvettipuram K. Thiruvengadam
IPC分类号： C07F9/40
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

6. 发明授权

US07687631B2 Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
标题翻译： {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成
公开(公告)号：US07687631B2
公开(公告)日：2010-03-30
申请号：US11824245
申请日：2007-06-29
申请人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
发明人： Kelvin H. Yong , Ilia A. Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram K. Thiruvengadam
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07F9/58
摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.
摘要翻译：本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。本文教导的化学实例可以通过以下方案来举例说明：其中R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。

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