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    • 1. 发明授权
    • (3R)-3-amino-4-carboxybutyraldehyde derivatives inhibiting the release of interleukin-1/beta
    • (3R)-3-氨基-4-羧基丁醛衍生物抑制白细胞介素-1 /β的释放
    • US06593300B1
    • 2003-07-15
    • US09423006
    • 2000-02-07
    • Sandor BajuszIren VeghelyiKlara NemethEva BarabasAttila JuhaszJozsef LangoEmilia LavichZsuzsanna MohaiImre MoravcsikZsuzsanna TaschlerGabor Toth
    • Sandor BajuszIren VeghelyiKlara NemethEva BarabasAttila JuhaszJozsef LangoEmilia LavichZsuzsanna MohaiImre MoravcsikZsuzsanna TaschlerGabor Toth
    • A61K3800
    • C07K7/02A61K38/00C07K5/0202
    • The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n=0, an &agr;-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an &agr;-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an &agr;-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosine and valine; and Q2-Q4 represent an acyl group selected from the following &agr;-hydroxyacids of R or S configuration: 2-cycloheptyl-2-hydroxy-acetic acid, 2-cyclohexyl-2-hydroxyacetic acid, 3-cyclohexyllactic acid, 3-phenyllactic acid, 2-hydroxy-3-methylbutyric acid, 2-hydroxy-3-methylvaleric acid, mandelic acid or lactic acid, and salts thereof formed with organic or inorganic bases, and pharmaceutical compositions containing the same. The compounds of general formula (I) of the invention are valuable inhibitors of the interleukin-1&bgr; converting enzyme.
    • 本发明涉及通式(I)的新的(3R)-3-氨基-4-羧基丁醛衍生物,其中X代表C1-4烷氧基羰基,任意取代的苯基 - (C 1-2烷氧基) - 羰基, 4烷基羰基或任选取代的苯基 - (C 1-3烷基) - 羰基,n表示1或0,Y表示在n = 1的情况下,通式Y4-Y3-Y2-Y1的四肽,三肽 通式Y3-Y2-Y1或通式Y2-Y1的二肽或通式Y1的氨基酸残基,或在n = 0的情况下,通式为Q4-Y3-Y2的α-羟基酰基三肽 -Y1,通式为Q3-Y2-Y1的α-羟酰基二肽或通式为Q2-Y1的α-羟基酰基 - 酰基残基; 其中Y 1 -Y 4表示选自以下L-或D-氨基酸的残基:丙氨酸,异亮氨酸,环己基 - 甘氨酸,苯丙氨酸,谷氨酰胺,组氨酸,异亮氨酸,亮氨酸,赖氨酸,甲硫氨酸,哌可酸,脯氨酸 ,酪氨酸和缬氨酸; 和Q 2 -Q 4表示选自以下R或S构型的α-羟基酸的酰基:2-环庚基-2-羟基 - 乙酸,2-环己基-2-羟基乙酸,3-环己基乳酸,3-苯基乳酸 ,2-羟基-3-甲基丁酸,2-羟基-3-甲基戊酸,扁桃酸或乳酸,以及与有机或无机碱形成的盐,以及含有它们的药物组合物。 本发明通式(I)的化合物是白细胞介素-1β转换酶的有价值的抑制剂。
    • 4. 发明授权
    • Systems and methods for reducing alteration of a specimen during analysis for charged particle based and other measurement systems
    • 用于减少基于带电粒子和其他测量系统的分析期间样品变化的系统和方法
    • US07394067B1
    • 2008-07-01
    • US11185915
    • 2005-07-20
    • David SoltzPaul WieczorekAaron ZuoGabor Toth
    • David SoltzPaul WieczorekAaron ZuoGabor Toth
    • G01B15/04
    • G03F1/84
    • Systems and methods for reducing alteration of a specimen during by charged particle based and other measurements systems are provided. One system configured to reduce alteration of a specimen during analysis includes a vacuum chamber in which the specimen is disposed during the analysis and an element disposed within the vacuum chamber. A surface of the element is cooled such that molecules in the vacuum chamber are adsorbed onto the surface and cannot cause alteration of a characteristic of the specimen during the analysis. One system configured to analyze a specimen includes an analysis subsystem configured to analyze the specimen while the specimen is disposed in a vacuum chamber and an element disposed within the vacuum chamber. A surface of the element is cooled such that molecules in the vacuum chamber are adsorbed onto the surface and cannot cause alteration of a characteristic of the specimen during the analysis.
    • 提供了通过基于带电粒子和其他测量系统来减少样品变化的系统和方法。 被配置为减少分析期间样品变化的一个系统包括:真空室,其中在分析过程中放置​​试样并设置在真空室内的元件。 元件的表面被冷却,使得真空室中的分子被吸附到表面上,并且在分析期间不能引起样品特性的改变。 被配置为分析样本的一个系统包括分析子系统,该分析子系统构造成在样本被布置在真空室中并且设置在真空室内的元件时分析样本。 元件的表面被冷却,使得真空室中的分子被吸附到表面上,并且在分析期间不能引起样品特性的改变。
    • 6. 发明申请
    • Centralized link-scope configuration of an internet protocol (IP) network
    • 互联网协议(IP)网络的集中链路范围配置
    • US20050135274A1
    • 2005-06-23
    • US10742731
    • 2003-12-19
    • Gergely MolnarGabor TothBalazs GeroAttila Nohl
    • Gergely MolnarGabor TothBalazs GeroAttila Nohl
    • H04L12/24H04L12/28
    • H04L41/0806
    • A method of configuring link-scope-type managed objects in IP-based networks from a centralized management node. An IP-based network includes at least one management station, a set of network nodes, and communication links between the network nodes and between the management station and the network nodes. Preferably, an Open Shortest Path First (OSPF) topology graph of the network is prepared, and a set of target links to be configured is identified. The target links are then classified into N disjoint subsets, T1-TN. The links in each subset are then configured in parallel, starting with subset T1 and sequentially handling each subset one-by-one. The target links may be classified by removing non-target links that are not to be configured from the OSPF topology graph, building a LinkGraph to determine the dependencies between the links remaining in the OSPF topology graph, and building a LinkTree from the LinkGraph to classify the target links into the subsets based upon the dependencies between the links.
    • 一种从集中管理节点在基于IP的网络中配置链路范围类型管理对象的方法。 基于IP的网络包括至少一个管理站,一组网络节点以及网络节点之间以及管理站和网络节点之间的通信链路。 优选地,准备网络的开放最短路径优先(OSPF)拓扑图,并且识别要配置的一组目标链路。 然后将目标链路分为N个不相交的子集,T 1,N 2,N 2,N 3。 然后每个子集中的链接被并行地配置,从子集T 1开始,并逐个地依次处理每个子集。 可以通过从OSPF拓扑图中去除不配置的非目标链路来分类目标链路,构建LinkGraph以确定OSPF拓扑图中剩余的链路之间的依赖关系,以及从LinkGraph构建LinkTree以对其进行分类 基于链接之间的依赖关系,目标链接到子集中。