Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents
    81.
    发明授权
    Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents 失效
    作为抗感染剂的N-肉豆蔻酰基转移酶的丝氨酰赖氨酰基肽和肽模拟抑制剂

    公开(公告)号:US06632921B1

    公开(公告)日:2003-10-14

    申请号:US09277573

    申请日:1999-03-26

    IPC分类号: C07K508

    摘要: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C. albicans with little effect on human NMT enzyme and thus would.be useful in treating C. albicans fungal infections in humans.

    摘要翻译: 描述了基于丝氨酰赖氨酰的肽和拟肽化合物作为N-肉豆蔻酰转移酶酶的抑制剂,以提供对真菌生物体 的真菌生物的选择性控制。 特别感兴趣的拟肽化合物是下式的化合物:其中R 1选自氨基烷基,对氨基烷基苯基烷基,咪唑基烷基苯基烷基,2-烷基咪唑基烷基苯基烷基,苯并咪唑基烷基苯基烷基和2-烷基苯并咪唑基烷基苯基烷基; 其中R 1选自氢,烷基,环烷基,亚烯基,炔基,卤代烷基,苄基,烷基苯基烷基,烷氧基苯基烷基,卤代苯基烷基,苯乙基,环烷基烷基,卤代环烷基烷基,烷基环烷基烷基, 其中Y选自羧酸,异羟肟酸,膦酸和四唑基; 或其药学上可接受的盐,酰胺或酯。 式的化合物是 C的物种特异性抑制剂。 白色念珠菌 对人NMT酶几乎没有影响,因此可用于治疗 C。 白色念珠菌 人类真菌感染。

    Methods of reducing the water permeability of subterranean formations
    82.
    发明授权
    Methods of reducing the water permeability of subterranean formations 有权
    降低地层地层渗透性的方法

    公开(公告)号:US06364016B1

    公开(公告)日:2002-04-02

    申请号:US09697060

    申请日:2000-10-26

    IPC分类号: E21B4322

    CPC分类号: C09K8/508

    摘要: Improved methods of treating water and hydrocarbons producing subterranean formations to reduce the water permeabilities of the formations without substantially reducing the hydrocarbons permeabilities thereof are provided. The methods basically comprise introducing into the formation a chemical which does not resist water flow and attaches to adsorption sites on surfaces within the porosity of the formation but slowly washes off the sites as another fluid flows through the treated formation. Thereafter, a water flow resisting polymer is introduced into the formation so that it flows deeply into the porosity of the formation before the previously introduced chemical washes off and attaches to the adsorption sites as the chemical washes off.

    摘要翻译: 提供了改进的处理水和生产地下地层的烃的方法,以减少地层的水渗透性,而基本上不降低烃的渗透性。 这些方法基本上包括向地层中引入不能抵抗水流的化学物质,并且附着在地层孔隙中的表面上的吸附位点,但随着另一种流体流过经处理的地层而缓慢地洗出位点。 此后,将水流阻聚性聚合物引入地层,使其在先前引入的化学物质洗掉之前深深地流入地层的孔隙中,并随着化学物质洗脱而附着在吸附位置。

    System and method for analyzing topological features on a surface
    83.
    发明授权
    System and method for analyzing topological features on a surface 失效
    用于分析表面拓扑特征的系统和方法

    公开(公告)号:US6137570A

    公开(公告)日:2000-10-24

    申请号:US107391

    申请日:1998-06-30

    摘要: Disclosed is a method and apparatus for using far field scattered and diffracted light to determine whether a collection of topological features on a surface (e.g., a semiconductor wafer) conforms to an expected condition or quality. This determination is made by comparing the far field diffraction pattern of a surface under consideration with a corresponding diffraction pattern (a "baseline"). If the baseline diffraction pattern and far field diffraction pattern varies by more than a prescribed amount or in characteristic ways, it is inferred that the surface features are defective. The method may be implemented as a die-to-die comparison of far field diffraction patterns of two dies on a semiconductor wafer. The portion of the far field scattered and diffracted light sensitive to a relevant condition or quality can also be reimaged to obtain an improved signal-to-noise ratio.

    摘要翻译: 公开了一种使用远场散射和衍射光来确定表面(例如,半导体晶片)上的拓扑特征的集合是否符合预期状态或质量的方法和装置。 通过将考虑的表面的远场衍射图与相应的衍射图案(“基线”)进行比较来进行该确定。 如果基线衍射图案和远场衍射图案变化超过规定量或以特征方式,则推断表面特征是有缺陷的。 该方法可以实现为半导体晶片上的两个管芯的远场衍射图案的管芯与管芯的比较。 对于相关条件或质量敏感的远场散射和衍射光的部分也可以被重新成像以获得改善的信噪比。

    Substituted isoxazoles for the treatment of inflammation
    89.
    发明授权
    Substituted isoxazoles for the treatment of inflammation 失效
    用于治疗炎症的取代的异恶唑

    公开(公告)号:US5633272A

    公开(公告)日:1997-05-27

    申请号:US473884

    申请日:1995-06-07

    摘要: A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.3 is optionally substituted at a substitutable position with one or more radicals independently selected from lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; and wherein R.sup.4 is selected from lower alkyl, hydroxyl and amino; or a pharmaceutically-acceptable salt thereof.

    摘要翻译: 描述了一类用于治疗炎症和炎症相关疾病的取代的异恶唑基化合物。 特别感兴趣的化合物由式II其中R1选自羟基,低级烷基,羧基,低级羧基烷基,低级氨基羰基烷基,低级烷氧基羰基烷基,低级芳烷基,低级烷氧基烷基,低级芳烷氧基烷基,低级烷硫基烷基,低级芳烷硫基烷基,低级 低级芳氧基烷基,低级芳基硫代烷基,低级卤代烷基,低级羟基烷基,环烷基,环烷基烷基和芳烷基; 其中R 3选自环烷基,环烯基,芳基和杂芳基; 其中R 3在可取代的位置任选被一个或多个独立地选自低级烷基亚磺酰基,低级烷基,氰基,羧基,低级烷氧基羰基,低级卤代烷基,羟基,低级羟烷基,低级卤代烷氧基,氨基,低级烷基氨基,低级芳基氨基,低级 氨基烷基,硝基,卤素,低级烷氧基,氨基磺酰基和低级烷硫基; 并且其中R 4选自低级烷基,羟基和氨基; 或其药学上可接受的盐。

    Molded suture retainer
    90.
    发明授权
    Molded suture retainer 失效
    模制缝合保持架

    公开(公告)号:US5359831A

    公开(公告)日:1994-11-01

    申请号:US79642

    申请日:1993-06-18

    摘要: A molded suture retainer is provided for retaining and storing sutures. Both absorbable and nonabsorbable sutures fabricated from natural or synthetic materials can be advantageously retained and stored therein. The retainer is characterized by a wide spiraling oval passageway with minimal convolutions covered by a cover sheet. The length of the passageway is preferably proportional to 1/3 to 1/2 the overall length of the suture to be retained therein. Recesses are provided for receiving package stabilizing agents and/or needle parks. Sutures packaged in accordance with the invention exhibit fewer kinks and bends than prior packaged sutures.

    摘要翻译: 提供模制缝合线保持器用于保持和存储缝合线。 由天然或合成材料制成的可吸收和不可吸收的缝合线可以有利地保留并存储在其中。 保持器的特征在于具有宽的螺旋形椭圆形通道,具有由盖板覆盖的最小卷积。 通道的长度优选与要保留在其中的缝合线的总长度的1/3至1/2成比例。 提供了用于接收包装稳定剂和/或针园的凹槽。 根据本发明包装的缝合线比现有的包装缝合线显示出较少的扭结和弯曲。