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71. 发明申请

US20130096103A1 IMIDAZOQUINOLINE COMPOUNDS 审中-公开
标题翻译：咪唑啉化合物
公开(公告)号：US20130096103A1
公开(公告)日：2013-04-18
申请号：US13527537
申请日：2012-06-19
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： C07D471/14
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。

72. 发明申请

US20120252741A1 NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：新型半合成糖苷作为抗菌剂
公开(公告)号：US20120252741A1
公开(公告)日：2012-10-04
申请号：US13440692
申请日：2012-04-05
申请人： Daniel Chu , Tao Ye , Bing Wang
发明人： Daniel Chu , Tao Ye , Bing Wang
IPC分类号： A61K38/14 , A61P31/04 , C07K1/06 , C07K9/00
CPC分类号： C07K9/006
摘要： Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide 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 with certain acyl groups; conversion of the amide group in amino acid-3 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 to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.
摘要翻译：本文提供具有抗菌活性的半合成糖肽。本文所述的半合成糖肽通过在酸性介质中水解母体糖肽的氨基酸-4的二糖部分而使糖肽进行化学修饰来制备，得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 用某些酰基酰化氨基酸4氨基取代的糖部分上的氨基取代基; 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; 并将大环上的酸部分转化为某些取代的酰胺。本文还提供了包含半合成糖肽的药物组合物，以及使用半合成糖肽来治疗和/或预防疾病，特别是细菌感染的方法。

73. 发明申请

US20110196153A1 PROCESSES OF SYNTHESIZING DIHYDROPYRIDOPHTHALAZINONE DERIVATIVES 有权
标题翻译：合成二羟基二苯基酮衍生物的方法
公开(公告)号：US20110196153A1
公开(公告)日：2011-08-11
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： C07D471/04 , C07D405/06 , C07D249/08 , C07D403/06 , C07D401/04
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，其是有效的聚（ADP-核糖）聚合酶（PARP）抑制剂以及新的合成中间体化合物。

74. 发明申请

US20110190288A1 DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY 有权
标题翻译：用于治疗与PTEN缺乏相关的疾病的聚（ADP-RIBOSE）聚合酶（PARP）的二氢吲哚哒嗪酮抑制剂
公开(公告)号：US20110190288A1
公开(公告)日：2011-08-04
申请号：US13020619
申请日：2011-02-03
申请人： Daniel Chu , Bing Wang , Ying Feng , Yuqiao Shen , Leonard Edwin Post
发明人： Daniel Chu , Bing Wang , Ying Feng , Yuqiao Shen , Leonard Edwin Post
IPC分类号： A61K31/5025 , A61P35/00 , A61P43/00 , A61K31/5377
CPC分类号： A61K31/5377 , A61K31/5025 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D487/06
摘要： A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 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 associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
摘要翻译：具有式（I）和式（II）所示结构的化合物：其中取代基Y，Z，A，B，R 1，R 2，R 3，R 4和R 5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活性而改善的与PTEN缺乏相关的疾病，病症和病况的药物组合物。

75. 发明申请

US20110178065A1 NOVEL CYP17 INHIBITORS 审中-公开
标题翻译：新CYP17抑制剂
公开(公告)号：US20110178065A1
公开(公告)日：2011-07-21
申请号：US13005646
申请日：2011-01-13
申请人： Daniel Chu , Bing Wang , Tao Ye
发明人： Daniel Chu , Bing Wang , Tao Ye
IPC分类号： A61K31/55 , A61P35/00 , C12N9/99 , A61K31/366 , C07D335/04 , C07D405/08 , C07D487/04 , C07D333/50 , A61K31/365 , A61K31/443 , C07D401/08 , A61K31/497
CPC分类号： C07J73/003 , C07D211/76 , C07D233/60 , C07D241/12 , C07D249/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07J61/00 , C07J73/005 , C07J73/006 , C07J73/008
摘要： Provided herein are inhibitors of CYP17 enzyme. 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 androgen-dependent diseases, disorders and conditions.
摘要翻译：本文提供了CYP17酶的抑制剂。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雄激素依赖性疾病，病症和病症的药物组合物。

76. 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。

77. 发明授权

US07332476B2 Pyridyl substituted ketolide antibiotics 失效
标题翻译：吡啶基取代的酮内酯抗生素
公开(公告)号：US07332476B2
公开(公告)日：2008-02-19
申请号：US10831749
申请日：2004-04-23
申请人： Matthew T. Burger , Georgia Law Carroll , Daniel Chu , Xiaodong Lin , Jacob Plattner , Alice Rico
发明人： Matthew T. Burger , Georgia Law Carroll , Daniel Chu , Xiaodong Lin , Jacob Plattner , Alice Rico
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/08
摘要： 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.
摘要翻译：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。

78. 再颁专利

USRE39762E1 Polyketide synthase enzymes and recombinant DNA constructs therefor 有权
标题翻译：聚酮化合物合成酶及其重组DNA构建体
公开(公告)号：USRE39762E1
公开(公告)日：2007-08-07
申请号：US11299244
申请日：2005-12-09
申请人： Christopher Reeves , Daniel Chu , Chaitan Khosla , Daniel Santi , Kai Wu
发明人： Christopher Reeves , Daniel Chu , Chaitan Khosla , Daniel Santi , Kai Wu
IPC分类号： C07D515/00 , C07D498/00
CPC分类号： C07D498/18 , C07K2319/00 , C12N9/1029 , C12N9/1205 , C12N15/52 , C12P17/188 , C12P19/32
摘要： Polyketide compounds of the formula but not including FK-506, FK-520, 18-hydroxy-FK520 and 18-hydroxy-FK-506.
摘要翻译：具有式但不包括FK-506，FK-520,18-羟基-FK520和18-羟基-FK-506的聚酮化合物。

79. 发明申请

US20070132831A1 Masking to prevent overexposure and light spillage in microarray scanning 审中-公开
标题翻译：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
申请人： Daniel Chu
发明人： Daniel Chu
IPC分类号： B41J15/14
CPC分类号： G01N21/253 , G01N2201/0446 , G01N2201/1042
摘要： 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.
摘要翻译：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。

80. 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。

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