专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

51. 发明申请

US20030113805A1 Intrinsically labelled solid support 审中-公开
标题翻译：本质标签固体支持
公开(公告)号：US20030113805A1
公开(公告)日：2003-06-19
申请号：US10339552
申请日：2003-01-09
申请人： Zeneca Limited, a London corporation
发明人： Brian Geoffrey Main , Richard Eden Shute
IPC分类号： G01N033/53 , G01N033/543
CPC分类号： C40B50/16 , C07B2200/11 , C40B20/04 , C40B30/00 , C40B40/04 , G01N33/58
摘要： A compound library comprises a plurality of different units each comprising a solid support with which is associated a single member of the compound library, each solid support has a defined chemical composition which acts as an intrinsic label capable of identifying the first choice in the synthesis of the associated member of the compound library.
摘要翻译：化合物文库包括多个不同的单元，每个单元包含固体支持物，与固体支持物相关联，化合物文库的单个成员与每个固体支持物相关联，每个固体支持物具有限定的化学组成，其作为能够鉴定合成中第一选择的内在标记化合物库的相关成员。

52. 发明授权

US06573387B1 Synthesis of &agr;,&bgr;-substituted amino amides, esters, and acids 有权
标题翻译： α，β-取代氨基酰胺，酯和酸的合成
公开(公告)号：US06573387B1
公开(公告)日：2003-06-03
申请号：US09381407
申请日：2000-01-31
申请人： K. Barry Sharpless , A. Erik Rubin
发明人： K. Barry Sharpless , A. Erik Rubin
IPC分类号： C07D20304
CPC分类号： C07D203/22 , C07C231/12 , C07C231/16 , C07C303/40 , C40B40/04 , C40B50/08 , C07C311/19
摘要： &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.
摘要翻译： α，β-不饱和酰胺和酯转化为α，β-取代的氨基酰胺，酯和酸。首先使用锇催化的氨基羟基化将α，β-不饱和酰胺或酯转化为α，β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯。然后将α，β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯环化脱水以产生α，β-N-磺酰基或α，β-N-氨基甲酰基氮丙啶酰胺或酯。然后将氮丙啶中间体环以区域选择性方式用各种亲核试剂进行亲核打开，得到$ g（α，β-取代的氨基酰胺或酯）。优选的亲核试剂包括硫，氧，碳和氮亲核试剂。

53. 发明授权

US06452050B1 Synthesis and use of &agr;-ketoamide derivatives and arrays 失效
标题翻译： α-酮酰胺衍生物和阵列的合成和应用
公开(公告)号：US06452050B1
公开(公告)日：2002-09-17
申请号：US09531737
申请日：2000-03-21
申请人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
发明人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
IPC分类号： C07C23307
CPC分类号： C40B40/04 , C07C275/40 , C07C335/20 , C07D333/60
摘要： The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
摘要翻译：本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000个α-酮酰胺衍生物，具有针对三个半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物通过本文所述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药剂。虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。

54. 发明授权

US06441172B1 Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof 失效
标题翻译：二酮二氮环化合物，二氮环化合物及其组合文库
公开(公告)号：US06441172B1
公开(公告)日：2002-08-27
申请号：US09310662
申请日：1999-05-12
申请人： Adel Nefzi , John M. Ostresh , Richard A. Houghten
发明人： Adel Nefzi , John M. Ostresh , Richard A. Houghten
IPC分类号： C07D24104
CPC分类号： C07D487/04 , C07D233/36 , C07D233/42 , C07D239/10 , C07D241/18 , C07D243/08 , C07D245/04 , C07D245/06 , C07D491/04 , C07D495/04 , C07D513/04 , C40B40/00 , C40B40/04 , C40B50/14
摘要： The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6-8 atoms in the ring is disclosed, as are libraries of such compounds. Methods of preparing and using the libraries of compounds as well as individual compounds of the libraries are also disclosed.
摘要翻译：在环中具有6-8个原子的单个二 - 和三 - 取代-1,4-二氮环化合物，它们相应的1,6-二酮-2,5-二氮杂环化合物和类似的1,4-二氮杂环公开了环中具有一个环羰基和6-8个原子的环化合物，以及这些化合物的文库。还公开了制备和使用化合物文库以及文库的单独化合物的方法。

55. 发明申请

US20020064799A1 Proteomic analysis 审中-公开
公开(公告)号：US20020064799A1
公开(公告)日：2002-05-30
申请号：US09836145
申请日：2001-04-16
申请人： The Scripps Research Institute of an Assignment
发明人： Benjamin F. Cravatt , Erik Sorensen , Matthew P. Patricelli , Martha Lovato , Gregory Adam
IPC分类号： G01N033/53 , C07C317/10 , C07D213/44 , C07D207/04
CPC分类号： C40B30/04 , C12Q1/26 , C12Q1/32 , C12Q1/37 , C40B40/04 , G01N33/535 , G01N33/557 , G01N33/6842 , G01N33/6845 , G01N2500/20 , G16B20/00 , Y10T436/16 , Y10T436/18
摘要： The present invention provides methods for analyzing proteomes, as cells or lysates. The analysis is based on the use of probes that have specificity to the active form of proteins, particularly enzymes and receptors. The probes can be identified in different ways. In accordance with the present invention, a method is provided for generating and screening compound libraries that are used for the identification of lead molecules, and for the parallel identification of their biological targets. By appending specific functionalities and/or groups to one or more binding moieties, the reactive functionalities gain binding affinity and specificity for particular proteins and classes of proteins. Such libraries of candidate compounds, referred to herein as activity-based probes, or ABPs, are used to screen for one or more desired biological activities or target proteins.

56. 发明授权

US06380429B1 Preparation of sulfonyl imine compounds 失效
标题翻译：磺酰亚胺化合物的制备
公开(公告)号：US06380429B1
公开(公告)日：2002-04-30
申请号：US09663737
申请日：2000-09-15
申请人： Eric Maurice Smith
发明人： Eric Maurice Smith
IPC分类号： G07C30340
CPC分类号： C40B40/04 , C07C249/02 , C07C303/40 , C07C303/44 , C07D307/52 , C07D311/70 , C07D333/22 , C40B40/00 , C40B50/14 , C07C311/03 , C07C311/09 , C07C311/16 , C07C311/29 , C07C311/51
摘要： Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.
摘要翻译：公开了使用二氧化铬（IV）作为氧化剂将磺酰胺氧化为磺酰亚胺的方法。

57. 发明申请

US20020028943A1 Multibinding inhibitors of microsomal triglyceride transferase protein 审中-公开
标题翻译：微粒体甘油三酯转移酶蛋白的多相关抑制剂
公开(公告)号：US20020028943A1
公开(公告)日：2002-03-07
申请号：US09760827
申请日：2001-01-17
发明人： John H. Griffin
IPC分类号： G01N033/53 , C07D211/56 , C07D211/92
CPC分类号： C40B30/04 , A61K31/00 , A61K47/54 , A61K47/55 , A61K47/552 , A61K47/60 , C07C233/36 , C07C233/78 , C07C237/24 , C07C271/20 , C07C321/04 , C07C323/12 , C07C335/08 , C07C335/32 , C07C2603/18 , C07D207/333 , C07D211/58 , C07D215/56 , C07D233/90 , C07D235/30 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/34 , C07D475/04 , C07D475/08 , C07D487/04 , C07D487/06 , C07D493/04 , C07D493/06 , C07H19/20 , C12Q1/26 , C12Q1/44 , C12Q1/48 , C12Q1/533 , C40B40/04 , G01N33/573 , G01N33/6842 , G01N33/6845 , G01N33/92 , G01N2500/00 , G01N2500/04 , G01N2800/044 , Y02A50/401 , Y02A50/57 , Y10S530/807
摘要： Disclosed are multibinding compounds which inhibit microsomal triglyceride transferase protein (MTP), a protein which mediates the transfer of lipids during the assembly of lipoproteins and related biomolecules. The multibinding compounds contain from 2 to 10 ligands covalently attached to one or more linkers. The multibinding compounds of this invention are useful for lowering serum lipid, cholesterol and/or triglyceride levels, and for preventing and treating disorders associated with hyperlipemia, hyperlipidemia, hyperlipoproteinemia, hypercholestrolemia, hypertriglyceridemia and the like, such atherosclerosis.
摘要翻译：公开了抑制微粒体甘油三酯转移酶蛋白（MTP）的多结合化合物，其是介导脂蛋白和相关生物分子组装期间脂质转移的蛋白质。多相结合的化合物含有共价连接到一个或多个连接体的2至10个配体。本发明的多重联结化合物可用于降低血清脂质，胆固醇和/或甘油三酯水平，以及用于预防和治疗与高脂血症，高脂血症，高脂蛋白血症，高胆固醇血症，高甘油三酯血症等相关的疾病，如动脉粥样硬化。

58. 发明授权

US06265228B1 Process for preparing combinatorial amide alcohol libraries 失效
标题翻译：组合酰胺醇文库的制备方法
公开(公告)号：US06265228B1
公开(公告)日：2001-07-24
申请号：US09336634
申请日：1999-06-18
申请人： Roland Ellwood Dolle, III , Timothee Felix Herpin , Yvonne Class Shimshock , Cullen Lee Cavallaro
发明人： Roland Ellwood Dolle, III , Timothee Felix Herpin , Yvonne Class Shimshock , Cullen Lee Cavallaro
IPC分类号： G01N3353
CPC分类号： C40B40/04 , C07B2200/11 , C07C233/16 , C40B30/04 , C40B50/14
摘要： Combinatorial chemical libraries of the Formula [S]—C(O)—L′—Z containing dihyroxy amides and hydroxyphosphonate amides are disclosed, in which [S] represents a solid support and —L′—Z is a linker/ligand residue. In these libraries, Z is and Y is —P(O)(OR6)(OR7), —CH(OH)—COR8, —CH,CH═CH2—CH2CH(OH)CH2OH, —CH2CHO, —CH2CH2OH, —CH2CH2OC(O)NHR26, —CH2CH2NR27R28, or The combinatorial libraries are optionally encoded with tags. The use of these libraries in assays to discover biologically active compounds is also disclosed.
摘要翻译：公开了含有二羟基酰胺和羟基膦酸酯的式[S] -C（O）-L'-Z的组合化学文库，其中[S]表示固体载体，-L'-Z是连接体/配体残基。在这些文库中，Z是且Y是-P（O）（OR 6）（OR 7），-CH（OH）-COR 8，-CH，CH = CH 2 -CH 2 CH（OH）CH 2 OH，-CH 2 CHO，-CH 2 CH 2 OH，-CH 2 CH 2 OC O）NHR 26，-CH 2 CH 2 NR 27 R 28，或者组合文库可选地用标签编码。还公开了这些文库在测定中发现生物活性化合物的用途。

59. 发明授权

US06255120B1 Combinatorial library of substituted statine esters and amides via a novel acid-catalyzed rearrangement 失效
标题翻译：通过新的酸催化重排的取代的酯基酯和酰胺的组合文库
公开(公告)号：US06255120B1
公开(公告)日：2001-07-03
申请号：US09079932
申请日：1998-05-15
申请人： Roland Ellwood Dolle, III , Cullen Lee Cavallaro , Timothee Felix Herpin
发明人： Roland Ellwood Dolle, III , Cullen Lee Cavallaro , Timothee Felix Herpin
IPC分类号： G01N33543
CPC分类号： C40B40/04 , C07B2200/11 , C07C233/16 , C40B30/04 , C40B50/14
摘要： A combinatorial chemical library comprising a plurality of members of the Formula [S]—C(O)—L′-Z containing hydroxyamides is disclosed, in which [S] represents a solid support and L′-Z is a linker/compound residue. In this library, Z is and Y is —NR3R4 or —OR9. R3 and R4 are independently selected from the group consisting of H, alkyl, aralkyl, heteroarylalkyl, heterocycloalkyl, —CH(R5)CH(R6)OH, —CH(R5)C(O)NHR6 and —CH(R5)C(O)NHCH(R6)C(O)NHR7. R3 and R4 together are wherein X=O or NR8 and R9 is aryl, aralkyl or R7CH═CH(CH2){overscore (n)}. The combinatorial library can be optionally encoded with identifiers T′-L, which are covalently attached to the solid support. The methods of synthesizing such a library are described. The use of such library in assays to discover biologically active compounds is also disclosed.
摘要翻译：公开了包含式[S] -C（O）-L'-Z的羟基酰胺的多个成员的组合化学文库，其中[S]表示固体支持物，而L'-Z是接头/化合物残基。在该文库中，Z是且Y是-NR 3 R 4或-OR 9。 R3和R4独立地选自H，烷基，芳烷基，杂芳基烷基，杂环烷基，-CH（R5）CH（R6）OH，-CH（R5）C（O）NHR6和-CH（R5）C（ O）NHCH（R 6）C（O）NHR 7。 R3和R4一起在X = O或NR8中，R9是芳基，芳烷基或R7CH = CH（CH2）（过核（n）}）。组合库可以任选地用标识符T'-L进行编码，标识符T'-L共价连接到固体支持物上。描述了合成这种文库的方法。还公开了在测定中使用这种文库发现生物活性化合物。

60. 发明授权

US06221319B1 Plasma discharge reactors for the preparation of bioactive compounds 失效
标题翻译：用于制备生物活性化合物的等离子体放电反应器
公开(公告)号：US06221319B1
公开(公告)日：2001-04-24
申请号：US09339315
申请日：1999-06-23
申请人： Bruce M. Johnson , Walter C. Babcock , James B. West , Dwayne T. Friesen
发明人： Bruce M. Johnson , Walter C. Babcock , James B. West , Dwayne T. Friesen
IPC分类号： B01J1908
CPC分类号： C40B40/04 , B01J8/025 , B01J12/002 , B01J19/0046 , B01J19/088 , B01J2219/00135 , B01J2219/00286 , B01J2219/00599 , B01J2219/0072 , B01J2219/0809 , B01J2219/0886 , B01J2219/1942 , C07B61/00 , C40B50/08 , G01N2500/00 , Y10S422/907
摘要： Plasma discharge reactors of various designs are disclosed; the reactors are capable of synthesizing large numbers of bioactive compounds of great chemical diversity.
摘要翻译：公开了各种设计的等离子体放电反应器; 反应器能够合成大量化学多样性的生物活性化合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式