公开(公告)号：US20100216699A1

公开(公告)日：2010-08-26

申请号：US12697967

申请日：2010-02-01

申请人： Daniel Chu ,  Tao Ye

发明人： Daniel Chu ,  Tao Ye

IPC分类号： A61K38/14 ,  C07K9/00 ,  C07K7/64 ,  A61K38/12 ,  A61P31/04

CPC分类号： C07K9/008 ,  A61K38/00 ,  C07K7/06

摘要： Semi-synthetic glycopeptides having antibacterial activity are described. Also described are processes of preparing such semi-synthetic glycopeptides by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in mild acidic medium to give the amino acid-4 monosaccharide; protection of the amino groups in the molecule; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Also included are the process of conversion of the amide group in amino acid-3 on these scaffolds to various acylureas, acylamide, acylsulfonamide, acylsulfonylurea derivatives and aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction procedures. Further provided herein are pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, including bacterial infections.

摘要翻译： 描述了具有抗菌活性的半合成糖肽。 还描述了通过糖肽（化合物A，化合物B，化合物H或化合物C）的化学修饰或通过水解母体糖肽的氨基酸-4的二糖部分制备的单糖制备这种半合成糖肽的方法 温和酸性培养基，得到氨基酸-4单糖; 保护分子中的氨基; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 还包括在氨基酸-7上通过曼尼希反应方法将这些支架上的氨基酸3中的酰胺基团转化为各种酰基脲，酰基酰胺，酰基磺酰胺，酰基磺酰脲衍生物和氨基甲基化，其中氨基酸-7的取代基含有磺酰胺或酰基磺酰胺基团。 本文进一步提供含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病包括细菌感染的方法。

公开(公告)号：US20100105607A1

公开(公告)日：2010-04-29

申请号：US12603435

申请日：2009-10-21

申请人： Daniel Chu ,  Tao Ye ,  Bing Wang

发明人： Daniel Chu ,  Tao Ye ,  Bing Wang

IPC分类号： A61K38/08 ,  C07K9/00 ,  A61P31/04

CPC分类号： C07K9/006

摘要： Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these 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.

摘要翻译： 具体描述了具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽通过化学修饰糖肽（化合物A，化合物B，化合物H或化合物C）或通过水解二糖而制备的单糖 在酸性介质中母体糖肽的氨基酸-4部分得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 这些支架上氨基酸-3中的酰胺基转化为各种酰基酰胺，酰基磺酰胺，酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将这些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，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

公开(公告)号：US07632918B2

公开(公告)日：2009-12-15

申请号：US11361852

申请日：2006-02-24

申请人： Daniel Chu ,  Maria N. Preobrazhenskaya ,  Svetlana S. Printsevskaya ,  Eugenia N. Olsufyeva

发明人： Daniel Chu ,  Maria N. Preobrazhenskaya ,  Svetlana S. Printsevskaya ,  Eugenia N. Olsufyeva

IPC分类号： A61K38/14

CPC分类号： A61K38/14 ,  C07K9/008

摘要： 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.

摘要翻译： 具有抗菌活性的半合成糖肽基于依依霉素，A82846B，万古霉素，替考拉宁和A-40,926支架的修饰，特别是在具有某些酰基的这些支架上糖部分的酰化; 和/或将这些支架的大环上的酸部分转化为某些取代的酰胺; 或具有这些支架上的氨基取代的糖部分上的氨基取代基的烷基化修饰与某些烷基的组合或在该支架上的某些烷基上的氨基取代的糖部分上的氨基取代基的酰化修饰和转化 的该支架的大环上的酸部分与某些取代的酰胺。 还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

公开(公告)号：US20090197863A1

公开(公告)日：2009-08-06

申请号：US12355692

申请日：2009-01-16

申请人： Daniel Chu ,  Bing Wang

发明人： Daniel Chu ,  Bing Wang

IPC分类号： A61K31/422 ,  C07D263/54 ,  A61K31/423 ,  A61K31/496 ,  C07D413/02 ,  A61P35/00

CPC分类号： C07D263/57 ,  C07D413/04 ,  C07D413/10 ,  C07D455/02 ,  C07D487/04 ,  C07D487/08

摘要： A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

摘要翻译： 具有式（I）或式（II）所示结构的化合物：其中变量Y，R1，R2，R3和R4如本文所定义。 本文提供了聚（ADP-核糖）聚合酶活性的抑制剂。 本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗通过抑制PARP活性而改善的疾病，病症和病症的药物组合物。

公开(公告)号：USRE39836E1

公开(公告)日：2007-09-11

申请号：US11182038

申请日：2005-07-13

申请人： Daniel Chu ,  Gary Ashley

发明人： Daniel Chu ,  Gary Ashley

IPC分类号： A61K31/70 ,  C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： Compounds of the formula wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl, unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); Re is H or a protecting group; L is methylene or carbonyl; T is —O—, —N(R)—, —N(OR)—, —N(NHCOR)—, —N(N═CHR)—, or —N(NHR)— wherein R is H or Ra as defined above, with the proviso that when L is methylene, T is —O—; one of Z and Y is H and the other is OH, protected OH, or amino, mono- or dialkylamino, protected amino, or an amino heterocycle or Z and Y together are ═O, ═NOH or a derivatized oxime; including any pharmaceutically acceptable salts thereof and any stereoisomeric forms and mixtures of stereoisomeric forms thereof, are antimicrobial agents.

摘要翻译： 下式的化合物其中R a a为H; 取代或未取代的烷基（1-10C）; 取代或未取代的烯基（2-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳基烷基（5-20​​℃）; 或OR被替换为H; R b是H或卤素; R c是H或保护基; R d是甲基，未取代的烷基（3-10C）; 取代的烷基（1-10C）; 取代或未取代的炔基（2-10C）; 取代或未取代的芳基（4-14C）; 取代或未取代的芳基烷基（5-20​​℃）; 取代或未取代的芳基烯基（5-20​​℃）; 取代或未取代的芳基炔基（5-20​​℃）; 取代或未取代的酰氨基芳基烷基（5-20​​℃）; 取代或未取代的酰氨基芳基烯基（5-20​​℃）; 或取代或未取代的酰氨基芳基炔基（5-20​​℃）; R e是H或保护基; L是亚甲基或羰基; T是-O - ， - N（R） - ， - N（OR） - ， - N（NHCOR） - ， - N（N-CHR） - 或-N（NHR） 如上所定义，条件是当L是亚甲基时，T是-O-; Z和Y之一是H，另一个是OH，保护的OH或氨基，单或二烷基氨基，保护的氨基或氨基杂环，或Z和Y一起是-O，-NOH或衍生化的肟; 包括其任何药学上可接受的盐和其立体异构体形式及其立体异构形式的混合物均为抗微生物剂。

公开(公告)号：US20070202018A1

公开(公告)日：2007-08-30

申请号：US11361411

申请日：2006-02-24

申请人： Daniel Chu ,  Paul Patt ,  Jeffry Ceremony

发明人： Daniel Chu ,  Paul Patt ,  Jeffry Ceremony

IPC分类号： B01L9/00

CPC分类号： G01N35/028 ,  B01L9/523 ,  B01L2200/025 ,  B01L2300/0829

摘要： A platform that supports a sample plate such as a microtiter plate, a multi-well plate of any size, or a glass slide with sample spots distributed over its surface, and presents the plate for assay detection by a movable scanning head that has a field depth on the millimeter scale is leveled or otherwise adjusted in a planar orientation by an apparatus that includes a rocker plate, position sensors, and motorized risers arranged on the apparatus to provide the rocker plate with tilting capability along either or both or two orthogonal axes.

摘要翻译： 支撑样品板的平台，例如微量滴定板，任何尺寸的多孔板或具有分布在其表面上的样品斑点的玻片，并且通过具有场的可移动扫描头呈现用于测定检测的板 通过包括设置在设备上的摇臂板，位置传感器和电动立管的装置，平面定位或以其它方式调整深度，以使摇杆具有沿着一个或两个或两个正交轴线的倾斜能力。

公开(公告)号：US20070119945A1

公开(公告)日：2007-05-31

申请号：US11291423

申请日：2005-11-30

申请人： Daniel Chu

发明人： Daniel Chu

IPC分类号： G06K7/10

CPC分类号： H02K41/0356

摘要： A moving coil actuator contains a magnet assembly that is movable to shift the range of motion of the coil. The magnet assembly moves between two or more positions along a path of travel that is parallel to the path of travel of the reciprocating motion of the coil. With this feature, the width of an area scanned by a scanning head affixed to the coil can be increased by multiples allowing a simple moving coil actuator to be used for any scanning width.

摘要翻译： 运动线圈致动器包括可移动以移动线圈的运动范围的磁体组件。 磁体组件沿着平行于线圈的往复运动的行进路径的行进路径在两个或更多个位置之间移动。 利用该特征，由固定到线圈上的扫描头扫描的区域的宽度可以增加多倍，从而允许使用简单的移动线圈致动器用于任何扫描宽度。

公开(公告)号：US20070104414A1

公开(公告)日：2007-05-10

申请号：US11488113

申请日：2006-07-18

申请人： Daniel Chu ,  Ying-Chih Chen ,  Shun-Tien Lee

发明人： Daniel Chu ,  Ying-Chih Chen ,  Shun-Tien Lee

IPC分类号： G02B6/12

CPC分类号： G02B6/02314 ,  G02B6/12002 ,  G02B6/12004 ,  G02B6/43

摘要： An optoelectric converting substrate includes a substrate, at least one honeycomb-shaped micro-structured optical waveguide embedded in the substrate and having two ends exposed through the substrate, a plurality of optoelectronic elements disposed on the substrate and coupled with the two ends of the honeycomb-shaped micro-structured optical waveguide, and a plurality of IC driving elements disposed on the substrate and electrically connected with the optoelectronic elements by conductive wires to drive the optoelectronic elements such that optical signals are transmitted through the honeycomb-shaped micro-structured optical waveguide. The optoelectric converting substrate can be easily fabricated at a low cost and effectively increases the displacement tolerance of the optoelectronic elements in substrate packaging.

摘要翻译： 光电转换基板包括基板，至少一个蜂窝状微结构光波导，其嵌入在该基板内并且具有通过该基板露出的两端;多个光电元件，设置在该基板上并与该蜂窝体的两端连接 形状的微结构光波导，以及多个IC驱动元件，其设置在基板上并通过导线与光电元件电连接，以驱动光电元件，使得光信号通过蜂窝状微结构光波导 。 可以以低成本容易地制造光电转换基板，并有效地增加基板封装中的光电元件的位移公差。

公开(公告)号：US07034033B2

公开(公告)日：2006-04-25

申请号：US10444495

申请日：2003-05-23

申请人： Rustum S. Boyce ,  Natalia Aurrecoechea ,  Daniel Chu ,  Aaron Smith ,  Bryan Chang

发明人： Rustum S. Boyce ,  Natalia Aurrecoechea ,  Daniel Chu ,  Aaron Smith ,  Bryan Chang

IPC分类号： C07D239/90 ,  A61K31/517 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D253/08 ,  C07D217/24 ,  C07D239/88 ,  C07D239/90 ,  C07D239/91 ,  C07D239/96 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D471/04

摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

公开(公告)号：US20060030573A1

公开(公告)日：2006-02-09

申请号：US11248040

申请日：2005-10-11

申请人： Rustum Boyce ,  Natalia Aurrecoechea ,  Daniel Chu ,  Aaron Smith ,  Bryan Chang

发明人： Rustum Boyce ,  Natalia Aurrecoechea ,  Daniel Chu ,  Aaron Smith ,  Bryan Chang

IPC分类号： A61K31/519 ,  A61K31/517 ,  C07D239/88 ,  C07D403/02 ,  C07D487/02

CPC分类号： C07D253/08 ,  C07D217/24 ,  C07D239/88 ,  C07D239/90 ,  C07D239/91 ,  C07D239/96 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D471/04

摘要： A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.

摘要翻译： 提供了能够作为MC4-R激动剂的各种低分子量含胍基分子。 该化合物可用于治疗MC4-R介导的疾病。 化合物具有结构IA，IB或IC，其中变量的值在本文中定义。