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1. 发明申请

WO2015048306A1 NOVEL AGENTS TARGETING CYP51 审中-公开
标题翻译：新药代表CYP51
公开(公告)号：WO2015048306A1
公开(公告)日：2015-04-02
申请号：PCT/US2014/057483
申请日：2014-09-25
申请人： THE SCRIPPS RESEARCH INSTITUTE , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , ROUSH, William R. , CHOI, Jun Yong , PODUST, Larissa
发明人： ROUSH, William R. , CHOI, Jun Yong , PODUST, Larissa
IPC分类号： A61K31/4409
CPC分类号： C07D401/12 , A61K47/6951
摘要： The invention provides inhibitors of a sterol C14-demethylase, a new series of 4- aminopyridyl-based lead inhibitors targeting Trypanosoma cruzi CYP51 (TcCYP51) developed using structure-based drug design as well as structure -property relationship (SPR) analyses. The screening hit starting point, LP 10 (K D 50 of 0.65 μΜ), has been optimized to give the potential leads that have low nanomolar binding affinity to TcCYP51 and significant activity against T. cruzi amastigotes cultured in human myoblasts. Many of the optimized compounds have improved microsome stability, and most are selective against the T. cruzi CYP51 relative to human CYPs 1A2, 2D6 and 3A4 (
摘要翻译：本发明提供了使用基于结构的药物设计以及结构 - 性状关系（SPR）分析开发的甾体C14-去甲基化酶的抑制剂，其是针对使用基于结构的药物设计开发的锥虫CYP51（TcCYP51）的新系列的基于4-氨基吡啶基的铅抑制剂。筛选起始点LP 10（KD <42nM; EC 50为0.65μ＆Mgr）已经被优化，以产生对TcCYP51具有低纳摩尔结合亲和力的潜在引物和对人成肌细胞中培养的克氏锥虫无性状物的显着活性。许多优化的化合物具有改善的微粒体稳定性，并且大多数针对相对于人CYP1A2,2D6和3A4的克氏锥虫CYP51（对于1μM的抑制为<50％）是选择性的。提出了改善抑制剂对人代谢CYP酶的微粒体稳定性和选择性的理论依据。此外，本发明的几种化合物与T.brucei CYP51（TbCYP51）直系同源物的结合模式已经通过X射线结构分析进行了表征。已经显示口服活性化合物及其环糊精复合物对抗恰加亚感染的小鼠有效。

2. 发明申请

WO2008148074A2 INHIBITORS OF MTOR AND METHODS OF TREATMENT USING SAME 审中-公开
标题翻译： MTOR的抑制剂和使用它的治疗方法
公开(公告)号：WO2008148074A2
公开(公告)日：2008-12-04
申请号：PCT/US2008064809
申请日：2008-05-24
申请人： UNIV NEW YORK STATE RES FOUND , LIN RICHARD , DRUECKHAMMER DALE , CHOI JUN YONG , BALLOU LISA
发明人： LIN RICHARD , DRUECKHAMMER DALE , CHOI JUN YONG , BALLOU LISA
IPC分类号： A61K31/5377 , C07D487/04
CPC分类号： C07D471/04
摘要： The present invention provides novel compounds that inhibit mTOR activity. Compositions, including pharmaceutical compositions, comprising compounds of the present invention are also provided. The present invention also provides methods of treatment comprising administering compositions of the present invention to a subject in need thereof.
摘要翻译：本发明提供抑制mTOR活性的新型化合物。还提供了包含本发明化合物的组合物，包括药物组合物。本发明还提供了治疗方法，其包括将本发明的组合物施用于有需要的受试者。

3. 发明申请

WO2008084889A1 DNA CHIP FOR DETECTION OF STAPHYLOCOCCUS AUREUS 审中-公开
标题翻译：用于检测油菜的DNA芯片
公开(公告)号：WO2008084889A1
公开(公告)日：2008-07-17
申请号：PCT/KR2007/000125
申请日：2007-01-08
申请人： MEDIGENES CO., LTD , LEE, Sang-Yup , YOO, Seung Min , KEUM, Ki-Chang , YOO, Nae-Choon , YOO, Won-Min , KIM, June-Myung , CHOI, Jun Yong
发明人： LEE, Sang-Yup , YOO, Seung Min , KEUM, Ki-Chang , YOO, Nae-Choon , YOO, Won-Min , KIM, June-Myung , CHOI, Jun Yong
IPC分类号： C12Q1/68
CPC分类号： C12Q1/689 , C12Q1/6837
摘要： The present invention relates to nucleic acid probes specific to Staphylococcus aureus , which is useful for detecting and identifying S. aureus in a biological sample. More particularly, the present invention relates to a DNA chip for detecting and identifying S. aureus , on which nucleic acid probes derived from 23 S rRNA gene of S. aureus are immobilized. The application of the DNA chips according to the present invention allows time-saving and accurate diagnosis of bacterial infection compared with the conventional bacterial culture methods.
摘要翻译：本发明涉及对金黄色葡萄球菌特异性的核酸探针，其可用于检测和鉴定生物样品中的金黄色葡萄球菌。更具体地，本发明涉及用于检测和鉴定金黄色葡萄球菌的DNA芯片，其上固定有金黄色葡萄球菌23S rRNA基因的核酸探针。与常规细菌培养方法相比，根据本发明的DNA芯片的应用允许节省细菌感染的准确诊断。

4. 发明申请

WO2008084888A1 DNA CHIP FOR DETECTION OF ESCHERICHIA COLI 审中-公开
标题翻译：用于检测ESCHERICHIA COLI的DNA芯片
公开(公告)号：WO2008084888A1
公开(公告)日：2008-07-17
申请号：PCT/KR2007/000123
申请日：2007-01-08
申请人： MEDIGENES CO., LTD , LEE, Sang-Yup , YOO, Seung Min , SHIN, So Youn , KEUM, Ki-Chang , YOO, Nae-Choon , YOO, Won-Min , KIM, June-Myung , CHOI, Jun Yong
发明人： LEE, Sang-Yup , YOO, Seung Min , SHIN, So Youn , KEUM, Ki-Chang , YOO, Nae-Choon , YOO, Won-Min , KIM, June-Myung , CHOI, Jun Yong
IPC分类号： C12Q1/68
CPC分类号： C12Q1/689 , C12Q1/6837
摘要： The present invention relates to nucleic acid probes specific to E. coli, which is useful for detecting and identifying E. coli in a biological sample. More particularly, the present invention relates to a DNA chip for detecting and identifying E. coli, on which nucleic acid probes derived from 23 S rRNA gene of E. coli are immobilized. The application of the DNA chip according to the present invention allows time- saving and accurate diagnosis of bacterial infection compared with the conventional of bacterial culture methods. In addition, it is not affected by antibiotics addition in clinical practice, thus leading to more accurate diagnosis.
摘要翻译：本发明涉及对大肠杆菌特异性的核酸探针，其可用于检测和鉴定生物样品中的大肠杆菌。更具体地，本发明涉及用于检测和鉴定大肠杆菌的DNA芯片，其上固定有大肠杆菌23S rRNA基因的核酸探针。根据本发明的DNA芯片的应用与常规的细菌培养方法相比，可以节省细菌感染的准确诊断。此外，临床实践中不受抗生素添加的影响，从而导致更准确的诊断。

5. 发明申请

WO2018226837A1 SELECTIVE MATRIX METALLOPROTEINASE-13 INHIBITORS 审中-公开
公开(公告)号：WO2018226837A1
公开(公告)日：2018-12-13
申请号：PCT/US2018/036266
申请日：2018-06-06
申请人： FLORIDA ATLANTIC UNIVERSITY BOARD OF TRUSTEES , ROUSH, William R. , CHOI, Jun Yong , FUERST, Rita
发明人： ROUSH, William R. , CHOI, Jun Yong , FUERST, Rita , FIELDS, Gregg B.
IPC分类号： C07D405/12 , C07D239/70 , A61K31/517 , A61P29/00
CPC分类号： C07D239/70 , A61P29/00 , C07D405/12
摘要： We describe the use of comparative structural analysis and structure-guided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metalloproteinase 13 (MMP-13). We applied a three-step process, starting with a comparative analysis of the X-ray crystallographic structure of compound 5 in complex with MMP-13 with published structures of known MMP-13inhibitor complexes followed by molecular design and synthesis of potent, but non-selective zinc-chelating MMP inhibitors (e.g., 10a and 10b). After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-10a, and 10b were binding within the MMP-13 active site, the Zn2+ chelating unit was replaced with non-chelating polar residues that bridged over the Zn2+ binding site and reach into a solvent accessible area. After two rounds of structural optimization, these design approaches led to small molecule MMP-13 inhibitors 10d and (S)-17b which bind within the substrate-binding site of MMP-13 and surround the catalytically active Zn2+ ion without chelating to the metal. These compounds exhibit at least 500-fold selectivity versus other MMPs.

6. 发明申请

WO2008148074A3 INHIBITORS OF MTOR AND METHODS OF TREATMENT USING SAME 审中-公开
公开(公告)号：WO2008148074A3
公开(公告)日：2008-12-04
申请号：PCT/US2008/064809
申请日：2008-05-24
申请人： RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK , LIN, Richard , DRUECKHAMMER, Dale , CHOI, Jun Yong , BALLOU, Lisa
发明人： LIN, Richard , DRUECKHAMMER, Dale , CHOI, Jun Yong , BALLOU, Lisa
IPC分类号： A01N57/00
摘要： The present invention provides novel compounds that inhibit mTOR activity. Compositions, including pharmaceutical compositions, comprising compounds of the present invention are also provided. The present invention also provides methods of treatment comprising administering compositions of the present invention to a subject in need thereof.

7. 发明申请

WO2006025690A1 HERB COMPOSITION FOR ASTHMA MAINTENANCE THERAPY AND MANUFACTURING METHOD THEREOF 审中-公开
标题翻译：用于ASTHMA维持治疗的HERB组合物及其制造方法
公开(公告)号：WO2006025690A1
公开(公告)日：2006-03-09
申请号：PCT/KR2005/002873
申请日：2005-08-30
申请人： PURIMED CO., LTD. , JUNG, Sung-Ki , JUNG, Hee-Jae , HWANG, Woo-Suck , CHOI, Jun-Yong , BAE, Hyun-Su , KWACK, Kyu-Bum , KIM, Hong-Yeoul
发明人： JUNG, Sung-Ki , JUNG, Hee-Jae , HWANG, Woo-Suck , CHOI, Jun-Yong , BAE, Hyun-Su , KWACK, Kyu-Bum , KIM, Hong-Yeoul
IPC分类号： A61K35/78
CPC分类号： A61K36/752 , A61K36/346 , A61K36/40 , A61K36/428 , A61K36/484 , A61K36/539 , A61K36/65 , A61K36/718 , A61K36/736 , A61K36/79 , A61K36/804 , A61K36/884 , A61K36/8888 , A61K36/8945 , A61K36/896 , A61K36/8965 , A61K36/8966 , A61K2300/00
摘要： The present invention relates to a herb composition for asthma maintenance therapy based on Chungsangboha-tang, which is known to be effective in asthma, capable of reducing the long- term suffering of asthma patients and improving their quality of lives and a manufacturing method thereof. The herbal composition of the present invention is characterized by comprising 5-18 parts by weight of Rehmanniae radix vaporata, 4-14 parts by weight oÊDioscoreae radix, 4-14 parts by weight of Corni fructus, 2-9 parts by weight of Pachyma hoelen, 2-9 parts by weight of Moutan radicis cortex, 2-9 parts by weight ofAlismatis rhizoma, 2-7 parts by weight of Schizandrae fructus, 2-7 parts by weight of Aspargus cochinchinensis, 2-7 parts by weight of Liriopsis tuber, 2-7 parts by weight of Fritillariae bulbus, 2-7 parts by weight of Trichosantes kirilowii, 2-7 parts by weight of Prunus armeniacae linn, 2-7 parts by weight of Pinelliae rhizoma, 2-7 parts by weight oÊAurantii immaturus fructus, 2-7 parts by weight of Platycodi radix, 2-7 parts by weight of Scutellariae radix, 2-7 parts by weight of Coptidis rhizoma and 1-5 parts by weight of Glycyrrhizae radix.
摘要翻译：本发明涉及一种已知能有效哮喘的中山双浜哮喘维持治疗用草药组合物，其能够减轻哮喘患者的长期痛苦，提高其生活质量及其制造方法。本发明的草药组合物的特征在于包含5-18重量份的地黄，4-14重量份的石菖蒲，4-14重量份的康乃馨，2-9重量份的Pachyma hoelen ，2-9重量份的黄芪皮质，2-9重量份的紫草，2-7重量份的五味子，2-7重量份的天竺葵，2-7重量份的Liriopsis块茎，2-7重量份的贝母，2-7重量份的三叶草（Trichosantes kirilowii），2-7重量份的李属（Prunus armeniacae lin），2-7重量份的皮麻，2-7重量份的不饱和天竺葵果仁，2-7重量份扁柏，2-7重量份黄芩，2-7重量份黄连和1-5重量份甘草。

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