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21. 发明申请

US20080108808A1 DIPEPTIDYL PEPTIDASE INHIBITORS 有权
标题翻译： DIPEPTIDYL PEPTIDASE抑制剂
公开(公告)号：US20080108808A1
公开(公告)日：2008-05-08
申请号：US11929673
申请日：2007-10-30
申请人： Jun Feng , Stephen Gwaltney , Jeffrey Stafford , Zhiyuan Zhang , Bruce Elder , Paul Isbester , Grant Palmer , Jonathon Salsbury , Luckner Ulysse
发明人： Jun Feng , Stephen Gwaltney , Jeffrey Stafford , Zhiyuan Zhang , Bruce Elder , Paul Isbester , Grant Palmer , Jonathon Salsbury , Luckner Ulysse
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04
CPC分类号： C07D403/04 , C07D239/545 , C07D401/04 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C═NR9; and each L, X, R1, R2, and R3 are as defined herein.
摘要翻译：提供化合物，药物，试剂盒和方法用于DPP-IV和其它S9蛋白酶，其包含包含以下的化合物：其中M为N或CR 4; Q 1和Q 2各自独立地选自CO，SO，SO 2和C-NR 9 并且每个L，X，R 1，R 2和R 3 3如本文所定义。

22. 发明授权

US07265222B2 Process of making di-aryl urea compounds 有权
标题翻译：制备二芳基脲化合物的方法
公开(公告)号：US07265222B2
公开(公告)日：2007-09-04
申请号：US10881589
申请日：2004-06-30
申请人： Nizar Haddad , Xudong Wei , Chris Hugh Senanayake , Jinghua Xu , Nathan Yee
发明人： Nizar Haddad , Xudong Wei , Chris Hugh Senanayake , Jinghua Xu , Nathan Yee
IPC分类号： C07D239/34
CPC分类号： C07D239/47 , C07C275/34 , C07D239/545
摘要： Disclosed is a process of making compounds of formula(I): wherein R1, R2, R3, R4 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：公开了制备式（I）化合物的方法：其中R 1，R 2，R 3，R 4，（I）的R a和R A在本文中定义。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。

23. 发明申请

US20070049757A1 Methods for the synthesis of substituted amino uracils 审中-公开
标题翻译：用于合成取代氨基尿嘧啶的方法
公开(公告)号：US20070049757A1
公开(公告)日：2007-03-01
申请号：US11510632
申请日：2006-08-28
申请人： Jayson Rieger , Robert Thompson
发明人： Jayson Rieger , Robert Thompson
IPC分类号： C07D239/46 , C07D403/02
CPC分类号： C07D239/545
摘要： The invention provides novel methods of preparing substituted amino uracil compounds that can be employed as useful intermediates in the synthesis of various xanthines. Highly regioselective unsymmetrical amino uracils can be obtained using these methods which is a particular advantage over other existing methods.
摘要翻译：本发明提供了制备取代氨基尿嘧啶化合物的新方法，其可用作合成各种黄嘌呤的有用中间体。使用这些方法可以获得高度区域选择性的不对称氨基尿嘧啶，这是相对于其它现有方法的特别优点。

24. 发明申请

US20060281921A1 A2B adenosine receptor antagonists 有权
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US20060281921A1
公开(公告)日：2006-12-14
申请号：US11508592
申请日：2006-08-22
申请人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
发明人： Elfatih Elzein , Rao Kalla , Tim Marquart , Jeff Zablocki , Xiaofen Li
IPC分类号： C07D403/02
CPC分类号： C07D473/06 , C07D239/545 , C07D403/12 , C07D473/00 , C07D473/08
摘要： Disclosed are processes for the synthesis of novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
摘要翻译：公开了用于合成可用于治疗各种疾病状态（包括哮喘和腹泻）的Aβ2A腺苷受体拮抗剂的新化合物的方法。

25. 发明申请

US20060106214A1 8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
标题翻译： 8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂
公开(公告)号：US20060106214A1
公开(公告)日：2006-05-18
申请号：US11329889
申请日：2006-01-11
申请人： Gurdip Bhalay , Stephen Collingwood , Robin Fairhurst , Sylvie Gomez , Reto Naef , David Sandham
发明人： Gurdip Bhalay , Stephen Collingwood , Robin Fairhurst , Sylvie Gomez , Reto Naef , David Sandham
IPC分类号： A61K31/522 , C07D473/04
CPC分类号： C07D239/545 , A61K31/522 , C07D473/04 , C07D473/06
摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsufonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclyl group.
摘要翻译：式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷基硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基烷基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

26. 发明授权

US07015230B1 Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade 失效
公开(公告)号：US07015230B1
公开(公告)日：2006-03-21
申请号：US09717051
申请日：2000-11-20
申请人： Michael S. South , Darin E. Jones , Melvin L. Rueppel
发明人： Michael S. South , Darin E. Jones , Melvin L. Rueppel
IPC分类号： C07D239/54 , A61K31/505
CPC分类号： C07D417/12 , C07D239/545 , C07D253/075
摘要： The invention relates to substituted polycyclic aryl and heteroaryl uracil compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

27. 发明申请

US20050085639A1 Novel alkansulfonamides as endothelin antagonists 失效
标题翻译：新型烷磺酰胺作为内皮素拮抗剂
公开(公告)号：US20050085639A1
公开(公告)日：2005-04-21
申请号：US10500485
申请日：2002-12-10
申请人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli , Thomas Weller
发明人： Martin Bolli , Christoph Boss , Martine Clozel , Walter Fischli , Thomas Weller
IPC分类号： C07D239/47 , A61K31/506 , A61K31/5377 , A61P1/04 , A61P7/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/10 , A61P25/00 , A61P25/06 , A61P25/28 , A61P27/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P43/00 , C07D239/46 , C07D239/52 , C07D239/54 , C07D239/545 , C07D239/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D43/02
CPC分类号： C07D239/47 , C07D239/52 , C07D239/545 , C07D239/56 , C07D401/14 , C07D403/14
摘要： The invention relates to novel alkansulfonamides of structure (I), wherein R1 is a lowel alzyl group and the other variables are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention aslo concerns related aspects inluding processes for the preparation of the compounds, pharmaccutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists in the treatment and prevention of diseases associated to the endothelin system.
摘要翻译：本发明涉及结构（I）的新型烷磺酰胺，其中R 1是低级烷基，其它变量如说明书中所定义，并且它们作为制备药物组合物中的活性成分的用途。本发明涉及包括制备化合物的方法，含有一种或多种这些化合物的药物组合物，特别是其作为内皮素受体拮抗剂的用途的相关方面，用于治疗和预防与内皮素系统相关的疾病。

28. 发明申请

US20050042771A1 Capture compounds, collections thereof and methods for analyzing the proteome and complex compositions 审中-公开
标题翻译：捕获化合物，其收集物和分析蛋白质组合物和复合物组合物的方法
公开(公告)号：US20050042771A1
公开(公告)日：2005-02-24
申请号：US10760085
申请日：2004-01-16
申请人： Hubert Koster , Daniel Little , Suhaib Siddiqi , Matthew Grealish , Subramanian Marappan , Chester Hassman , Ping Yip
发明人： Hubert Koster , Daniel Little , Suhaib Siddiqi , Matthew Grealish , Subramanian Marappan , Chester Hassman , Ping Yip
IPC分类号： C07C69/76 , C07C69/96 , C07D207/40 , C07D207/404 , C07D207/46 , C07D209/48 , C07D211/60 , C07D211/78 , C07D213/79 , C07D215/48 , C07D239/54 , C07D239/545 , C07D241/44 , C07D261/12 , C07D271/06 , C07D271/07 , C07D303/14 , C07D303/16 , C07D317/36 , C07D401/12 , C07D405/10 , C07D405/12 , C07D495/04 , C07D498/18 , C07D519/00 , G01N33/68 , G01N33/543
CPC分类号： C07D495/04 , C07C69/76 , C07C69/96 , C07C2603/74 , C07D207/404 , C07D207/46 , C07D209/48 , C07D211/60 , C07D211/78 , C07D213/79 , C07D215/48 , C07D239/54 , C07D239/545 , C07D241/44 , C07D261/12 , C07D271/07 , C07D303/14 , C07D303/16 , C07D317/36 , C07D401/12 , C07D405/10 , C07D405/12 , C07D417/12 , C07D417/14 , C07D519/00 , G01N33/6803 , G01N33/6842 , G01N33/6845 , G01N33/6848
摘要： Capture compounds and collections thereof and methods using the compounds for the analysis of biomolecules are provided. In particular, collections, compounds and methods are provided for analyzing complex protein mixtures, such as the proteome. The compounds are multifunctional reagents that provide for the separation and isolation of complex protein mixtures. Automated systems for performing the methods also are provided.
摘要翻译：提供捕获化合物及其收集物和使用该化合物分析生物分子的方法。特别地，提供收集，化合物和方法用于分析复合蛋白质混合物，例如蛋白质组。这些化合物是提供复杂蛋白质混合物分离和分离的多功能试剂。还提供了用于执行方法的自动化系统。

29. 发明授权

US06790885B2 Thermally stabilized polyvinyl chloride compositions 失效
标题翻译：热稳定的聚氯乙烯组合物
公开(公告)号：US06790885B2
公开(公告)日：2004-09-14
申请号：US09907173
申请日：2001-07-17
申请人： Gabriele Pietro Norcini , Guido Allieri , Angelo Roberto Casiraghi , Mauro Ferracini , Marco Visconti , Giuseppe Li Bassi
发明人： Gabriele Pietro Norcini , Guido Allieri , Angelo Roberto Casiraghi , Mauro Ferracini , Marco Visconti , Giuseppe Li Bassi
IPC分类号： C08K534
CPC分类号： C07D239/545 , C07D239/56 , C08K5/3462 , C08L27/06 , C08L79/04 , C08L27/04 , C08L2666/20
摘要： Disclosed are chlorine containing polymer compositions containing stabilizers which impart good thermal stability. PVC compositions and, in particular, flexible PVC compositions containing stabilizers which are oligomeric and/or polymeric aminouracyls exhibit high thermal stability as evidenced by improved resistance to yellowing and blistering upon extended exposure to high temperatures.
摘要翻译：公开了含有赋予良好热稳定性的稳定剂的含氯聚合物组合物。 PVC组合物，特别是含有作为低聚和/或聚合氨基酰基的稳定剂的柔性PVC组合物表现出高的热稳定性，这通过在长时间暴露于高温下的改善的黄变和起泡性能来证明。

30. 发明申请

US20030134859A1 PPAR-gamma modulator 审中-公开
标题翻译： PPAR-gamma调制器
公开(公告)号：US20030134859A1
公开(公告)日：2003-07-17
申请号：US10278387
申请日：2002-10-23
申请人： SANKYO COMPANY, LIMITED
发明人： Yoshiya Amemiya , Kenji Wakabayashi , Sachiko Takaishi , Chie Fukuda
IPC分类号： A61K031/506 , A61K031/501 , A61K031/497 , A61K031/4439 , A61K031/427 , A61K031/422 , A61K031/4035 , A61K031/404 , A61K031/4709 , A61K031/366
CPC分类号： C07D249/08 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C233/81 , C07C255/58 , C07C271/28 , C07C275/14 , C07C275/28 , C07C275/40 , C07C275/50 , C07C311/08 , C07C311/21 , C07C311/46 , C07C311/48 , C07C311/58 , C07C311/64 , C07C335/16 , C07C335/20 , C07C335/26 , C07C335/28 , C07C2603/72 , C07D207/325 , C07D213/40 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/38 , C07D215/40 , C07D217/22 , C07D231/12 , C07D231/14 , C07D231/40 , C07D231/42 , C07D231/56 , C07D233/56 , C07D235/30 , C07D237/20 , C07D239/42 , C07D239/47 , C07D239/545 , C07D241/20 , C07D241/26 , C07D243/38 , C07D261/16 , C07D263/50 , C07D263/58 , C07D277/40 , C07D277/46 , C07D277/50 , C07D277/66 , C07D277/82 , C07D285/135 , C07D285/14 , C07D295/135 , C07D295/185 , C07D295/192 , C07D295/205 , C07D295/215 , C07D295/26 , C07D295/32 , C07D311/24 , C07D333/38 , C07D333/68 , C07D417/04 , C07D471/04
摘要： A compound of the following formula or a pharmacologically acceptable salt thereof: 1 wherein A represents a phenyl group or the like, B represents an aryl group or the like, X represents an oxygen atom or the like, and n represents 0 or 1. The compound is a PPAR null modulator which is a therapeutic agent for retrograde osteoporosis in which excessive differentiation of adipocytes is inhibited and formation and differentiation of osteoblasts from stem cells is facilitated, and for diabetes mellitus without characteristics such as excessive adipogenesis, liver dysfunction, vascular disorders, heart diseases and the like.
摘要翻译：下式的化合物或其药理学上可接受的盐：其中A表示苯基等，B表示芳基等，X表示氧原子等，n表示0或1.化合物是一种PPARγ调节剂，其是逆行性骨质疏松症的治疗剂，其中脂肪细胞的过度分化被抑制，成骨细胞从干细胞的形成和分化促进，并且对于没有特征的糖尿病，例如脂肪形成过多，肝功能障碍，血管疾病，心脏病等。

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