公开(公告)号：US20050153905A1

公开(公告)日：2005-07-14

申请号：US10831522

申请日：2004-04-23

Applicant: Matthew Burger ,  Daniel Chu

Inventor： Matthew Burger ,  Daniel Chu

IPC: A61K31/7052 ,  A61P31/04 ,  C07H17/08

CPC classification number: C07H17/08

Abstract: Antimicrobial ketolide compounds are provided having the formula (A): as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds, methods of treating bacterial infections by the administration of such compounds, and processes for the preparation of the compounds.

Abstract translation: 提供具有式（A）的抗微生物酮内酯化合物：以及其药学上可接受的盐，酯或前药，包含这些化合物的药物组合物，通过施用这些化合物治疗细菌感染的方法，以及制备化合物的方法 。

公开(公告)号：US07163924B2

公开(公告)日：2007-01-16

申请号：US10831522

申请日：2004-04-23

Applicant: Matthew Burger ,  Daniel Chu

Inventor： Matthew Burger ,  Daniel Chu

IPC: A61K31/70 ,  C07H17/08

CPC classification number: C07H17/08

Abstract: Antimicrobial ketolide compounds are provided having the formula (A): as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds, methods of treating bacterial infections by the administration of such compounds, and processes for the preparation of the compounds.

Abstract translation: 提供具有式（A）的抗微生物酮内酯化合物：以及其药学上可接受的盐，酯或前药，包含这些化合物的药物组合物，通过施用这些化合物治疗细菌感染的方法，以及制备化合物的方法 。

公开(公告)号：US20050009764A1

公开(公告)日：2005-01-13

申请号：US10831749

申请日：2004-04-23

Applicant: Matthew Burger ,  Georgia Carroll ,  Daniel Chu ,  Xiaodong Lin ,  Jacob Plattner ,  Alice Rico

Inventor： Matthew Burger ,  Georgia Carroll ,  Daniel Chu ,  Xiaodong Lin ,  Jacob Plattner ,  Alice Rico

IPC: A61P31/04 ,  C07H17/08 ,  A61K31/7052

CPC classification number: C07H17/08

Abstract: Antimicrobial macrolide and ketolide compounds are provided having formulas XII: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract translation: 提供抗微生物大环内酯和酮内酯化合物，其具有式XII：及其药学上可接受的盐，酯或前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 和化合物的制备方法。

公开(公告)号：US06756359B2

公开(公告)日：2004-06-29

申请号：US10190431

申请日：2002-07-03

Applicant: Daniel Chu ,  Matthew Burger ,  Xiaodong Lin ,  Georgia Law Carroll ,  Jacob Plattner ,  Alice Rico

Inventor： Daniel Chu ,  Matthew Burger ,  Xiaodong Lin ,  Georgia Law Carroll ,  Jacob Plattner ,  Alice Rico

IPC: A61K3170

CPC classification number: C07H17/08

Abstract: Antimicrobial macrolide compounds are provided having formulas II: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract translation: 提供具有式II的抗微生物大环内酯类化合物及其药学上可接受的盐，酯或前药; 包含这些化合物的药物组合物; 通过施用这些化合物治疗细菌感染的方法; 和化合物的制备方法。

公开(公告)号：US08765945B2

公开(公告)日：2014-07-01

申请号：US13023140

申请日：2011-02-08

Applicant: Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Quan Jiang ,  Lei Lu

Inventor： Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Quan Jiang ,  Lei Lu

IPC: C07D237/36

CPC classification number: C07D405/06 ,  C07D249/08 ,  C07D401/04 ,  C07D403/06 ,  C07D471/06

Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.

Abstract translation: 本文提供了合成二氢吡啶并二氮杂萘酮衍生物的方法，例如5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基） 9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3（7H） - 酮及其立体异构体，它们是有效的聚（ADP-核糖）聚合酶（PARP）抑制剂以及新的合成中间体化合物。

公开(公告)号：US08735392B2

公开(公告)日：2014-05-27

申请号：US13277607

申请日：2011-10-20

Applicant: Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Shichun Peng

Inventor： Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Shichun Peng

IPC: A01N43/58 ,  A61K31/495

CPC classification number: C07D471/06

Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.

Abstract translation: 本文提供的是（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H- - 吡啶并[4,3,2-de]酞嗪-3（7H） - 酮甲磺酸盐形式，包括晶型，及其制备方法。 包含（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢 - 还提供了使用（8S，9R）-5-氟-8-（4-氟苯基）-9（7H） - 酮的方法，使用2-吡啶并[4,3,2- - （1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3（7H） - 酮甲苯磺酸盐 治疗疾病或病症，如癌症。

公开(公告)号：US20120314092A1

公开(公告)日：2012-12-13

申请号：US13483771

申请日：2012-05-30

Applicant: Daniel Chu ,  Eli A. Hefner ,  Yann Jouvenot

Inventor： Daniel Chu ,  Eli A. Hefner ,  Yann Jouvenot

IPC: H04N5/225 ,  B01L3/00

CPC classification number: G01N15/1463 ,  G01N2015/1006

Abstract: An automated system captures multiple digital images of a sample, from different viewing areas of the sample. The images are analyzed and a test result may be reported based on the count of cells in all of the digital images. The system may be especially applicable to the testing of samples having low cell concentrations, as the variability between tests may be reduced as compared with a system that bases its test results on only a single image of the sample. The system may count the cells in a first digital image of the sample, and may capture or analyze one or more additional digital images only when it is recognized that additional measurements are needed to ensure adequate accuracy and repeatability of the test.

Abstract translation: 自动化系统从样品的不同观察区域捕获样品的多个数字图像。 分析图像，并且可以基于所有数字图像中的单元的计数来报告测试结果。 该系统可能特别适用于具有低细胞浓度的样品的测试，因为与将其测试结果仅基于样品的单个图​​像的系统相比，可以减少测试之间的可变性。 系统可以对样本的第一数字图像中的单元进行计数，并且可以仅在认识到需要额外的测量以确保测试的足够的精度和可重复性时才捕获或分析一个或多个附加的数字图像。

公开(公告)号：US20110217323A1

公开(公告)日：2011-09-08

申请号：US13108937

申请日：2011-05-16

Applicant: Nicholas VALIANTE ,  Feng Xu ,  Xiaodong Lin ,  Daniel Chu ,  Xiaojing Michael Wang

Inventor： Nicholas VALIANTE ,  Feng Xu ,  Xiaodong Lin ,  Daniel Chu ,  Xiaojing Michael Wang

IPC: A61K39/00 ,  C07D471/04 ,  A61P37/02 ,  A61P37/04 ,  A61P35/00

CPC classification number: C07D471/14 ,  C07D471/04 ,  Y02P20/55

Abstract: The invention provides novel compositions comprising imidazoquinoline compounds. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).

Abstract translation: 本发明提供包含咪唑并喹啉化合物的新型组合物。 还提供了以有效量施用组合物以增强受试者的免疫应答的方法。 进一步提供了组合物与（一种或多种）其它试剂组合施用的新组合物和方法。

公开(公告)号：US20100216699A1

公开(公告)日：2010-08-26

申请号：US12697967

申请日：2010-02-01

Applicant: Daniel Chu ,  Tao Ye

Inventor： Daniel Chu ,  Tao Ye

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

CPC classification number: C07K9/008 ,  A61K38/00 ,  C07K7/06

Abstract: 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.

Abstract translation: 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

Applicant: Daniel Chu ,  Tao Ye ,  Bing Wang

Inventor： Daniel Chu ,  Tao Ye ,  Bing Wang

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

CPC classification number: C07K9/006

Abstract: 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.

Abstract translation: 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。