SEMI-SYNTHETIC REARRANGED VANCOMYCIN/DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY
    42.
    发明申请
    SEMI-SYNTHETIC REARRANGED VANCOMYCIN/DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开
    具有抗生素活性的半合成重组型VANCOMYCIN / DESMETHYL-VANCOMYCIN型糖尿病

    公开(公告)号:US20080214444A1

    公开(公告)日:2008-09-04

    申请号:US12043076

    申请日:2008-03-05

    CPC classification number: C07K9/008

    Abstract: Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰,特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法,含有化合物的药物组合物,以及用于治疗和/或预防疾病,特别是细菌感染的化合物的使用方法。

    Masking to prevent overexposure and light spillage in microarray scanning
    45.
    发明申请
    Masking to prevent overexposure and light spillage in microarray scanning 审中-公开
    掩蔽以防止微阵列扫描过度暴露和轻度溢出

    公开(公告)号:US20070132831A1

    公开(公告)日:2007-06-14

    申请号:US11302695

    申请日:2005-12-13

    Applicant: Daniel Chu

    Inventor: Daniel Chu

    CPC classification number: G01N21/253 G01N2201/0446 G01N2201/1042

    Abstract: Scanning of a microarray is performed through a mask that exposes a plurality, but not all, of the sites of the microarray, and either the mask is movable relative to the microarray or the microarray is movable relative to the mask, or both. The mask is useful as a means of restricting the illumination of sites on the microarray to those that can be illuminated while the scan head is traveling at a steady, target velocity, blocking the passage of light between the scan head and the microarray at those points in the scan head trajectory where the scan head is either accelerating or decelerating. The mask is also useful for reducing background noise in the microarray image by preventing light spillage to sites adjacent to those being scanned.

    Abstract translation: 微阵列的扫描通过暴露微阵列的多个但不是全部的掩模进行,并且掩模相对于微阵列是可移动的,或者微阵列相对于掩模或两者都是可移动的。 该掩模可用作将扫描头以稳定的目标速度行进的情况下将微阵列上的部位的照明限制在可照亮的位置的手段,阻止在那些点处扫描头和微阵列之间的光通过 在扫描头轨迹中扫描头正在加速或减速。 该掩模也可用于通过防止光泄漏到与扫描的那些相邻的位置来减少微阵列图像中的背景噪声。

    Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity
    46.
    发明申请
    Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity 失效
    半合成重组万古霉素/脱甲基万古霉素类糖肽具有抗菌活性

    公开(公告)号:US20070021328A1

    公开(公告)日:2007-01-25

    申请号:US11361311

    申请日:2006-02-24

    CPC classification number: C07K9/008

    Abstract: Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰,特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法,含有化合物的药物组合物,以及用于治疗和/或预防疾病,特别是细菌感染的化合物的使用方法。

    Semi-synthetic glycopeptides with antibiotic activity

    公开(公告)号:US20060276623A1

    公开(公告)日:2006-12-07

    申请号:US11361852

    申请日:2006-02-24

    CPC classification number: A61K38/14 C07K9/008

    Abstract: Semi-synthetic glycopeptides having antibacterial activity are based on modifications of the eremomycin, A82846B, vancomycin, teicoplanin, and A-40,926 scaffolds, in particular, acylation of the sugar moieties on these scaffolds with certain acyl groups; and/or conversion of an acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides; or having a combination of an alkylation modification of the amino substituent on the amino-substituted sugar moiety on these scaffolds with certain alkyl groups or acylation modification of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain alkyl groups, and conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for the synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Novel guanidinyl derivatives
    49.
    发明申请
    Novel guanidinyl derivatives 审中-公开
    新型胍基衍生物

    公开(公告)号:US20050124597A1

    公开(公告)日:2005-06-09

    申请号:US10503401

    申请日:2003-02-03

    CPC classification number: C07K5/06165 A61K38/00 C07K5/06139

    Abstract: A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.

    Abstract translation: 提供了能够作为MC4-R激动剂的各种含有胍基的小分子。 化合物具有本文提供的各种结构。 该化合物可用于治疗MC4-R介导的疾病,并且可以配制成药物制剂和组合物。

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