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1. 发明申请

WO2006093933A2 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型糖蛋白
公开(公告)号：WO2006093933A2
公开(公告)日：2006-09-08
申请号：PCT/US2006/007021
申请日：2006-02-27
申请人： CHIRON CORPORATION , NORTH CHINA PHARMACEUTICAL GROUP CORPORATION , CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
发明人： CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
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

WO2006094082A3 SEMI-SYNTHETIC DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开
公开(公告)号：WO2006094082A3
公开(公告)日：2006-09-08
申请号：PCT/US2006/007337
申请日：2006-02-27
申请人： CHIRON CORPORATION , NORTH CHINA PHARMACEUTICAL GROUP CORPORATION , CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
发明人： CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
IPC分类号： A61K38/04 , A61K38/14 , C07K7/50 , C07K7/54
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.

3. 发明申请

WO2003066587A3 PIPERIDINE OR PYRROLIDINE DERIVATIVES HAVING AN AMINOACYL SUBSTITUTED SIDE CHAIN AS MELANCORTIN-4 RECEPTOR AGONISTS 审中-公开
公开(公告)号：WO2003066587A3
公开(公告)日：2003-08-14
申请号：PCT/US2003/001079
申请日：2003-02-03
申请人： CHIRON CORPORATION , BOYCE, Rustum , CHU, Daniel , LENTINI, David
发明人： BOYCE, Rustum , CHU, Daniel , LENTINI, David
IPC分类号： A61K31/445
摘要： A variety of small, piperidine or pyrrolidine derivatives of formulae IA, IIIA, IVA and VA, wherein the substituents are defined as in the claims, capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases and may bet formulated into pharmaceutical formulations and compositions.

4. 发明申请

WO2005028493A1 ANTIMICROBIAL DERIVATIVES 审中-公开
标题翻译：抗微生物衍生物
公开(公告)号：WO2005028493A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/029836
申请日：2004-09-13
申请人： CHIRON CORPORATION , LIN, Xioadong , CHU, Daniel
发明人： LIN, Xioadong , CHU, Daniel
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Antimicrobial compounds are provided having the formula (Q): as well as tautomers, stereoisomers, 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：提供具有式（Q）的抗微生物化合物：以及互变异构体，立体异构体，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。

5. 发明申请

WO2006093947A2 SEMI-SYNTHETIC GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开
标题翻译：具有抗生素活性的半合成糖蛋白
公开(公告)号：WO2006093947A2
公开(公告)日：2006-09-08
申请号：PCT/US2006/007049
申请日：2006-02-27
申请人： CHIRON CORPORATION , CHU, Daniel , PREOBRAZHENSKAYA, Maria , PRINTSEVSKAYA, Svetlana , OLSUFYEVA, Eugenia
发明人： CHU, Daniel , PREOBRAZHENSKAYA, Maria , PRINTSEVSKAYA, Svetlana , OLSUFYEVA, Eugenia
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。

6. 发明申请

WO2004112793A1 GUANIDINO-SUBSTITUTED QUINAZOLINONE COMPOUNDS AS MC4-R AGONISTS 审中-公开
标题翻译：甘氨酸取代的喹唑啉酮化合物作为MC4-R AGONISTS
公开(公告)号：WO2004112793A1
公开(公告)日：2004-12-29
申请号：PCT/US2004/015959
申请日：2004-05-21
申请人： CHIRON CORPORATION , GLAXOSMITHKLINE , BOYCE, Rustum, S. , AURRECOECHEA, Natalia , CHU, Daniel , SMITH, Aaron , CONLEE, Christopher, R. , THOMPSON, Brian, D. , DE ARMAS KUNTZ, Judith , MUSSO, David, L. , BARVIAN, Kevin, K. , THOMSON, Stephen, A. , SWAIN, William, R. , DU, Kien, S. , CHAUDER, Brian, A. , SPEAKE, Jason, D. , BISHOP, Michael, J.
发明人： BOYCE, Rustum, S. , AURRECOECHEA, Natalia , CHU, Daniel , SMITH, Aaron , CONLEE, Christopher, R. , THOMPSON, Brian, D. , DE ARMAS KUNTZ, Judith , MUSSO, David, L. , BARVIAN, Kevin, K. , THOMSON, Stephen, A. , SWAIN, William, R. , DU, Kien, S. , CHAUDER, Brian, A. , SPEAKE, Jason, D. , BISHOP, Michael, J.
IPC分类号： A61K31/517
CPC分类号： C07D217/24 , C07D239/91 , C07D239/95 , C07D239/96 , C07D253/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： A variety of small molecule, guanidine-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases when administered to subjects. The compounds have the structure IA, IB, and IC where the values of the variables are defined herein.
摘要翻译：提供了能够作为MC4-R激动剂的各种小分子，含胍分子。当施用于受试者时，这些化合物可用于治疗MC4-R介导的疾病。这些化合物具有结构IA，IB和IC，其中变量的值在本文中定义。

7. 发明申请

WO2004096823A2 NOVEL KETOLIDE DERIVATIVES 审中-公开
标题翻译：新型硬脂酸衍生物
公开(公告)号：WO2004096823A2
公开(公告)日：2004-11-11
申请号：PCT/US2004/012778
申请日：2004-04-23
申请人： CHIRON CORPORATION , BURGER, Matthew , CHU, Daniel
发明人： BURGER, Matthew , CHU, Daniel
IPC分类号： C07H17/00
CPC分类号： C07H17/08
摘要： Antimierobial 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.
摘要翻译：提供了具有式（A）的抗微生物素酮内酯化合物，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。

8. 发明申请

WO2004096822A2 PYRIDYL SUBSTITUTED KETOLIDE ANTIBIOTICS 审中-公开
标题翻译：吡啶基取代的Ketolide抗生素
公开(公告)号：WO2004096822A2
公开(公告)日：2004-11-11
申请号：PCT/US2004/012645
申请日：2004-04-23
申请人： CHIRON CORPORATION , BURGER, Matthew , CARROLL, Georgia , CHU, Daniel , LIN, Xiaodong , PLATTNER, Jacob , RICO, Alice
发明人： BURGER, Matthew , CARROLL, Georgia , CHU, Daniel , LIN, Xiaodong , PLATTNER, Jacob , RICO, Alice
IPC分类号： C07H17/00
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：提供了具有式（XII）的抗微生物大环内酯和酮内酯化合物及其药学上可接受的盐，酯或前药; 包含此类化合物的药物组合物通过施用这些化合物来治疗细菌感染的方法; 和制备这些化合物的方法。

9. 发明申请

WO2003004509A3 C12 MODIFIED ERYTHROMYCIN MACROLIDES AND KETOLIDES HAVING ANTIBACTERIAL ACTIVITY 审中-公开
公开(公告)号：WO2003004509A3
公开(公告)日：2003-01-16
申请号：PCT/US2002/021209
申请日：2002-07-03
申请人： CHIRON CORPORATION , CHU, Daniel , BURGER, Matthew , LIN, Xiaodong , CARROLL, Georgia, Law , PLATTNER, Jacob , RICO, Alice
发明人： CHU, Daniel , BURGER, Matthew , LIN, Xiaodong , CARROLL, Georgia, Law , PLATTNER, Jacob , RICO, Alice
IPC分类号： C07H17/08
摘要： 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.

10. 发明申请

WO2006031878A2 IMIDAZOQUINOLINE COMPOUNDS 审中-公开
标题翻译：咪唑啉化合物
公开(公告)号：WO2006031878A2
公开(公告)日：2006-03-23
申请号：PCT/US2005/032721
申请日：2005-09-14
申请人： CHIRON CORPORATION , VALIANTE, Nicholas , XU, Feng , LIN, Xiaodong , CHU, Daniel , WANG, Xiaojing, Michael
发明人： VALIANTE, Nicholas , XU, Feng , LIN, Xiaodong , CHU, Daniel , WANG, Xiaojing, Michael
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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