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1. 发明申请

US20070021328A1 Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity 失效
标题翻译：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
申请人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Wang
发明人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Wang
IPC分类号： C07K9/00 , A61K38/14
CPC分类号： C07K9/008
摘要： 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.
摘要翻译：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。

2. 发明申请

US20070185015A1 Semi-synthetic desmethyl-vancomycin-based glycopeptides with antibiotic activity 审中-公开
标题翻译：具有抗菌活性的半合成脱甲基万古霉素基糖肽
公开(公告)号：US20070185015A1
公开(公告)日：2007-08-09
申请号：US11361682
申请日：2006-02-24
申请人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Wang
发明人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Wang
IPC分类号： A61K38/14 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, 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. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. 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.
摘要翻译：具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰，特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。此外，本发明的化合物包括去甲基 - 万古霉素支架，大环上的酸部分转化为某些取代的酰胺，氨基取代的糖部分上的氨基取代基被某些烷基烷基化。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。

3. 发明授权

US07368422B2 Semi-synthetic rearranged vancomycin/desmethyl-vancomycin-based glycopeptides with antibiotic activity 失效
标题翻译：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：US07368422B2
公开(公告)日：2008-05-06
申请号：US11361311
申请日：2006-02-24
申请人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
发明人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
IPC分类号： A61K38/02 , A61K38/12 , A61K31/70 , C07K7/64 , C07K9/00 , C07K5/12
CPC分类号： C07K9/008
摘要： 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.
摘要翻译：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。

4. 发明申请

US20080214444A1 SEMI-SYNTHETIC REARRANGED VANCOMYCIN/DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开
标题翻译：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
申请人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
发明人： Yaohui Lei , Yu Bai , Daniel Chu , Zhi-Jie Ni , John Jian-Xin Wang
IPC分类号： A61K38/14 , C07K9/00
CPC分类号： C07K9/008
摘要： 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.
摘要翻译：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。

5. 发明申请

US20090131304A1 Semi-Synthetic Desmethyl-Vancomycin-Based Glycopeptides With Antibiotic Activity 审中-公开
标题翻译：具有抗生素活性的半合成去甲基 - 万古霉素基糖肽
公开(公告)号：US20090131304A1
公开(公告)日：2009-05-21
申请号：US12268364
申请日：2008-11-10
申请人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Jian-Xin Wang
发明人： Daniel Chu , Yaohui Lei , Yu Bai , Zhi-Jie Ni , John Jian-Xin Wang
IPC分类号： A61K38/12 , C07K9/00
CPC分类号： C07K9/008 , A61K38/00
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, 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. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. 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.
摘要翻译：具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰，特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。此外，本发明的化合物包括去甲基 - 万古霉素支架，大环上的酸部分转化为某些取代的酰胺，氨基取代的糖部分上的氨基取代基被某些烷基烷基化。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。

6. 发明授权

US06638927B2 Guanidinobenzamides 失效
标题翻译：胍基苯甲酰胺
公开(公告)号：US06638927B2
公开(公告)日：2003-10-28
申请号：US09945384
申请日：2001-08-31
申请人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
发明人： Paul A. Renhowe , Daniel Chu , Rustum S. Boyce , Zhi-Jie Ni , David Duhl , Effie Tozzo , Kirk Johnson , David C. Myles
IPC分类号： C07D29520
CPC分类号： C07D233/64 , C07B2200/07 , C07B2200/09 , C07C279/18 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07C2601/18 , C07C2602/10 , C07C2602/42 , C07C2603/74 , C07D209/16 , C07D215/12 , C07D241/08 , C07D241/42 , C07D295/215 , C07D307/24 , C07D309/14 , C07D333/20 , C07D487/04 , C07D487/08
摘要： Compounds of formula IA and IB are new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type II diabetes, and may be provided as pharmaceutical formulations in conjunction with a pharmaceutically acceptable carrier.
摘要翻译：式IA和IB的化合物是新的，其中变量R 1至R 10具有本文所述的值。这些化合物可用于治疗诸如肥胖症和II型糖尿病的疾病，并且可以作为药物制剂与药学上可接受的载体一起提供。

7. 发明授权

US08765945B2 Processes of synthesizing dihydropyridophthalazinone derivatives 有权
标题翻译：合成二氢吡啶并酞嗪酮衍生物的方法
公开(公告)号：US08765945B2
公开(公告)日：2014-07-01
申请号：US13023140
申请日：2011-02-08
申请人： Bing Wang , Daniel Chu , Yongbo Liu , Quan Jiang , Lei Lu
发明人： Bing Wang , Daniel Chu , Yongbo Liu , Quan Jiang , Lei Lu
IPC分类号： C07D237/36
CPC分类号： C07D405/06 , C07D249/08 , C07D401/04 , C07D403/06 , C07D471/06
摘要： 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.
摘要翻译：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。

8. 发明授权

US08735392B2 Crystalline (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 有权
标题翻译：结晶（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 [4,3,2-de]酞嗪-3（7H） - 酮甲苯磺酸盐
公开(公告)号：US08735392B2
公开(公告)日：2014-05-27
申请号：US13277607
申请日：2011-10-20
申请人： Bing Wang , Daniel Chu , Yongbo Liu , Shichun Peng
发明人： Bing Wang , Daniel Chu , Yongbo Liu , Shichun Peng
IPC分类号： A01N43/58 , A61K31/495
CPC分类号： C07D471/06
摘要： 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.
摘要翻译：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。

9. 发明申请

US20120314092A1 CELL COUNTING SYSTEMS AND METHODS 有权
标题翻译：细胞计数系统和方法
公开(公告)号：US20120314092A1
公开(公告)日：2012-12-13
申请号：US13483771
申请日：2012-05-30
申请人： Daniel Chu , Eli A. Hefner , Yann Jouvenot
发明人： Daniel Chu , Eli A. Hefner , Yann Jouvenot
IPC分类号： H04N5/225 , B01L3/00
CPC分类号： G01N15/1463 , G01N2015/1006
摘要： 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.
摘要翻译：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。

10. 发明申请

US20110217323A1 IMIDAZOQUINOLINE COMPOUNDS 审中-公开
标题翻译：咪唑啉化合物
公开(公告)号：US20110217323A1
公开(公告)日：2011-09-08
申请号：US13108937
申请日：2011-05-16
申请人： Nicholas VALIANTE , Feng Xu , Xiaodong Lin , Daniel Chu , Xiaojing Michael Wang
发明人： Nicholas VALIANTE , Feng Xu , Xiaodong Lin , Daniel Chu , Xiaojing Michael Wang
IPC分类号： A61K39/00 , C07D471/04 , A61P37/02 , A61P37/04 , A61P35/00
CPC分类号： C07D471/14 , C07D471/04 , Y02P20/55
摘要： 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).
摘要翻译：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。

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