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11. 发明申请

US20050192345A1 Crystalline polymorphs of a CXC-chemokine receptor ligand 审中-公开
标题翻译： CXC-趋化因子受体配体的结晶多晶型物
公开(公告)号：US20050192345A1
公开(公告)日：2005-09-01
申请号：US11045772
申请日：2005-01-28
申请人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
发明人： Mengwei Hu , Younong Yu , Michael Dwyer , Arthur Taveras , Agnes Kim-Meade , Jianguo Yin , Xiaoyong Fu , Timothy McAllister , Shuyi Zhang , Kevin Klopfer
IPC分类号： A61K31/34 , A61K31/341 , C07D307/52
CPC分类号： C07D307/52
摘要： The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure: These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.
摘要翻译：本发明涉及具有以下化学结构的化合物A的一水合物的四种不同的结晶多晶型物：这四种多晶型物，在本文中称为形式I，II，III和IV，作为CXC-趋化因子受体配体是有活性的。本发明进一步涉及这些多晶形式的制剂，治疗方法和合成方法。

12. 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。

13. 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。

14. 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。

15. 发明授权

US07956189B2 Maleate, tosylate, fumarate and oxalate salts of 5-(1-(S)-amino-2-hydroxyethyl)-N-[(2,4-difluorophenyl)-methy]-2-[8-methoxy-2-(triflouromethy)-5-quinoline]-4-oxazolecarboxamide and preparation process therefore 失效
标题翻译： 5-（1-（S） - 氨基-2-羟乙基）-N - [（2,4-二氟苯基） - 甲基] -2- [8-甲氧基-2-（三氟甲基）三氟甲磺酸盐，马来酸盐，甲苯磺酸盐，富马酸盐和草酸盐）-5-喹啉] -4-氧杂二甲酰胺及其制备方法
公开(公告)号：US07956189B2
公开(公告)日：2011-06-07
申请号：US11891351
申请日：2007-08-10
申请人： Xiaoming Chen , Xiao Chen , Jianguo Yin , Xiaoyong Fu , David J. Blythin , Rongze Kuang , Ho-Jane Shue , Scott Trzaska , Chee-Wah Tang , Vincenzo Liotta , Zaher Shabani
发明人： Xiaoming Chen , Xiao Chen , Jianguo Yin , Xiaoyong Fu , David J. Blythin , Rongze Kuang , Ho-Jane Shue , Scott Trzaska , Chee-Wah Tang , Vincenzo Liotta , Zaher Shabani
IPC分类号： C07D215/38
CPC分类号： C07D413/04
摘要： Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.
摘要翻译：公开了化合物5-（1（S） - 氨基-2-羟乙基）-N - [（2,4-二氟苯基） - 甲基] -2- [8-甲氧基 - 由式I表示的2-（三氟甲基）-5-喹啉啉-4-氧杂二甲酰胺及其制备方法。

16. 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。

17. 发明申请

US20080108818A1 Maleate, tosylate, fumarate and oxalate salts of 5-(1-(S)-amino-2-hydroxyethyl)-N-[(2,4-difluorophenyl)-methy]-2-[8-methoxy-2-(triflouromethy)-5-quinoline]-4-oxazolecarboxamide and preparation process therefore 失效
标题翻译： 5-（1-（S） - 氨基-2-羟乙基）-N - [（2,4-二氟苯基） - 甲基] -2- [8-甲氧基-2-（三氟甲基）三氟甲磺酸盐，马来酸盐，甲苯磺酸盐，富马酸盐和草酸盐）-5-喹啉] -4-氧杂二甲酰胺及其制备方法
公开(公告)号：US20080108818A1
公开(公告)日：2008-05-08
申请号：US11891351
申请日：2007-08-10
申请人： Xiaoming Chen , Xiao Chen , Jianguo Yin , Xiaoyong Fu , David Blythin , Rongze Kuang , Ho-Jane Shue , Scott Trzaska , Chee-Wah Tang , Vincenzo Liotta , Zaher Shabani
发明人： Xiaoming Chen , Xiao Chen , Jianguo Yin , Xiaoyong Fu , David Blythin , Rongze Kuang , Ho-Jane Shue , Scott Trzaska , Chee-Wah Tang , Vincenzo Liotta , Zaher Shabani
IPC分类号： C07D413/02
CPC分类号： C07D413/04
摘要： Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.
摘要翻译：公开了化合物5-（1（S） - 氨基-2-羟乙基）-N - [（2,4-二氟苯基） - 甲基] -2- [8-甲氧基 - 由式I表示的2-（三氟甲基）-5-喹啉啉-4-氧杂二甲酰胺及其制备方法。

18. 发明申请

US20080004449A1 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：US20080004449A1
公开(公告)日：2008-01-03
申请号：US11824245
申请日：2007-06-29
申请人： Kelvin Yong , Ilia Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram Thiruvengadam
发明人： Kelvin Yong , Ilia Zavialov , Jianguo Yin , Xiaoyong Fu , Tiruvettipuram Thiruvengadam
IPC分类号： C07D405/02
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R 9选自具有1至10个碳原子的烷基，芳基杂芳基和芳基烷基，R 11是从烷基，芳基杂芳基和具有1-10个碳原子的芳基烷基和氢独立地选择，X 2是Cl，Br或I; X 3选自Cl和Br; 并且PdL n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。

19. 发明授权

US6022977A Dynamic resolution of isoxazoline thioesters to isoxazoline carboxylic acids 失效
标题翻译：异恶唑啉硫代酯向异恶唑啉羧酸的动态拆分
公开(公告)号：US6022977A
公开(公告)日：2000-02-08
申请号：US47555
申请日：1998-03-25
申请人： Lin-Hua Zhang , Luigi Anzalone , Jaan A. Pesti , Jianguo Yin
发明人： Lin-Hua Zhang , Luigi Anzalone , Jaan A. Pesti , Jianguo Yin
IPC分类号： A61P7/02 , A61P43/00 , C07D261/04 , C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C07D261/04 , C12P41/005
摘要： The present invention relates generally to a novel method for preparation of substituted isoxazolin-5-yl acetic acid in high optical purity from a stereoisomeric mixture of an esterified substituted isoxazolin-5-yl acetate. The products are useful in the synthesis of compounds for pharmaceuticals, especially the treatment of thrombolytic disorders, and agricultural products.
摘要翻译：本发明一般涉及由酯化的取代的异恶唑啉-5-基乙酸酯的立体异构体混合物制备高光学纯度的取代的异恶唑啉-5-基乙酸的新方法。该产品可用于药物化合物的合成，特别是治疗血栓溶解症和农产品。

20. 发明授权

US06297410B1 Process for the preparation of cyclopropylacetylene 有权
标题翻译：环丙基乙炔的制备方法
公开(公告)号：US06297410B1
公开(公告)日：2001-10-02
申请号：US09481812
申请日：2000-01-12
申请人： Joseph M. Fortunak , Zhe Wang , Jianguo Yin
发明人： Joseph M. Fortunak , Zhe Wang , Jianguo Yin
IPC分类号： C07C202
CPC分类号： C07C51/353 , C07C1/30 , C07C13/04 , C07C17/093 , C07C51/38 , C07C2601/02 , C07C2601/04 , C07C22/00 , C07C57/26
摘要： The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, cyclopropane carboxaldehyde is condensed with malonic acid to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E,Z)-1-halo-2-cyclopropylethylene; and (E,Z)-1-halo-2-cyclopropylethylene is dehydrohalogenated to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
摘要翻译：本发明一般涉及用于合成环己基乙炔的新方法，其是不对称合成（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1 苯并恶嗪-2-酮; 一种有用的人类免疫缺陷病毒（HIV）逆转录酶抑制剂。在此过程中，环丙烷甲醛与丙二酸缩合形成3-环丙基丙烯酸; 将3-环丙基丙烯酸卤化形成（E，Z）-1-卤代-2-环丙基乙烯; 和（E，Z）-1-卤代-2-环丙基乙烯脱卤化氢形成环丙基乙炔。这种改进提供了廉价的，容易获得的起始原料转化成环丙基乙炔的高转化率，高的总收率并且可以在工业规模上进行。

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