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1. 发明申请

WO2004075858A3 FLAVONE ACETIC ACID ANALOGS AND METHODS OF USE THEREOF 审中-公开
标题翻译： FLAVONE ACE酸类似物及其使用方法
公开(公告)号：WO2004075858A3
公开(公告)日：2005-01-20
申请号：PCT/US2004005826
申请日：2004-02-24
申请人： UNIV NORTH CAROLINA , LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , BASTOW KENNETH F , KUO SHENG-CHU
发明人： LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , BASTOW KENNETH F , KUO SHENG-CHU
IPC分类号： C07D215/22 , C07D215/233 , A61K31/525 , A61K31/44 , A61K31/47 , C07D215/16 , C07D311/04 , C07D491/00
CPC分类号： C07D215/233
摘要： Compounds are described having a structure according to Formula (I) or Formula (II), wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alkyl, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, -OC(=O)R6, -O(C=O)OR6; and -O(C=O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.
摘要翻译：描述具有根据式（I）或式（II）的结构的化合物，其中：X选自O，NH和S; Y选自O和S; m为1〜3; n为1〜5; R 1和R 3各自独立地选自H，羟基，低级烷基，低级烷氧基，卤素，氨基，氨基烷基，硝基，杂芳基，-OC（= O）R 6，-O（C = O）OR 6; 和-O（C = O）N（R 6）2; R2是侧链如乙酸侧链，其中p为0至4，R5为羟基，烷氧基或氨基，R6为H或低级烷基或其药学上可接受的盐。该化合物可用于治疗癌症。

2. 发明申请

WO0226730A3 FLUORINATED QUINOLONES AS ANTIMITOTIC AND ANTITUMOR AGENTS 审中-公开
标题翻译：氟化喹诺酮作为抗肿瘤和抗肿瘤药物
公开(公告)号：WO0226730A3
公开(公告)日：2002-09-19
申请号：PCT/US0129916
申请日：2001-09-25
申请人： UNIV NORTH CAROLINA
发明人： LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , KUO SHENG-CHU
IPC分类号： A61K31/4709 , A61K31/4741 , A61P35/00 , A61P43/00 , C07D215/38 , C07D491/04 , C07D491/056 , C07D215/22 , C07D493/04
CPC分类号： C07D491/04 , C07D215/38
摘要： The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or cancer by the administration of such compounds, and methods of inhibiting cellular mitosis by the administration of such compounds.
摘要翻译：本发明提供在其苯基上氟化的氟化喹诺酮，以及含有其的药物制剂，通过施用这些化合物治疗肿瘤或癌症的方法，以及通过施用这些化合物抑制细胞有丝分裂的方法。

3. 发明专利

CA2423482A1 FLUORINATED QUINOLONES AS ANTIMITOTIC AND ANTITUMOR AGENTS 未知
公开(公告)号：CA2423482A1
公开(公告)日：2002-04-04
申请号：CA2423482
申请日：2001-09-25
申请人： UNIV NORTH CAROLINA
发明人： KUO SHENG-CHU , YANG ZHENG-YU , XIA YI , LEE KUO-HSIUNG
IPC分类号： A61K31/4709 , A61K31/4741 , A61P35/00 , A61P43/00 , C07D215/38 , C07D491/04 , C07D491/056 , C07D493/04 , C07D215/22
摘要： The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or cancer by the administration of such compounds, and methods of inhibiting cellular mitosis by the administration of such compounds.

4. 发明申请

WO2006113498A3 2-AMINO-QUINAZ0LIN-5-ONES AS HSP90 INHIBITORS USEFUL IN TREATING PROLIFERATION DISEASES 审中-公开
标题翻译： 2-AMINO-QUINAZ0LIN-5-ONES作为HSP90抑制剂用于治疗增殖性疾病
公开(公告)号：WO2006113498A3
公开(公告)日：2007-01-11
申请号：PCT/US2006014194
申请日：2006-04-14
申请人： CHIRON CORP , MACHAJEWSKI TIMOTHY D , GAO ZHENHAI , LEVINE BARRY H , ANTONIOS-MCCREA WILLIAM , BELLAMACINA CORNELIA R , COSTALES ABRAN , DOUGHAN BRANDON M , FONG SUSAN , HENDRICKSON THOMAS , LIN XIAODONG , MCBRIDE CHRISTOPHER , MCKENNA MAUREEN , RICO ALICE C , SHAFER CYNTHIA M , WANG X MICHAEL , ZHOU YASHEEN , XIA YI , MENDENHALL KRIS G
发明人： MACHAJEWSKI TIMOTHY D , GAO ZHENHAI , LEVINE BARRY H , ANTONIOS-MCCREA WILLIAM , BELLAMACINA CORNELIA R , COSTALES ABRAN , DOUGHAN BRANDON M , FONG SUSAN , HENDRICKSON THOMAS , LIN XIAODONG , MCBRIDE CHRISTOPHER , MCKENNA MAUREEN , RICO ALICE C , SHAFER CYNTHIA M , WANG X MICHAEL , ZHOU YASHEEN , XIA YI , MENDENHALL KRIS G
IPC分类号： C07D239/84 , A61K31/517 , A61P35/00 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/10 , C07D417/10 , C07D417/12
CPC分类号： C07D401/14 , C07D239/84 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D409/10 , C07D413/10 , C07D417/10 , C07D417/12 , C07D417/14
摘要： 2-Amino-quinazolin-5-one compounds, stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the 2-amino-quinazolin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cell proliferative diseases.
摘要翻译： 2-氨基 - 喹唑啉-5-酮化合物，立体异构体，互变异构体，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种2-氨基 - 喹唑啉-5-酮化合物的组合物，单独或与至少一种另外的治疗剂组合。单独使用2-氨基 - 喹唑啉-5-酮化合物或与至少一种其它治疗剂组合使用的方法用于预防或治疗细胞增殖性疾病。

5. 发明申请

WO2005070930A3 TETRAHYDROCARBOLINE COMPOUNDS AS ANTICANCER AGENTS 审中-公开
标题翻译：四氯化碳化合物作为反应剂
公开(公告)号：WO2005070930A3
公开(公告)日：2006-01-19
申请号：PCT/US2005002270
申请日：2005-01-24
申请人： CHIRON CORP , WANG WEIBO , NI ZHI-JIE , BARSANTI PAUL , PECCHI SABINA , XIA YI , BRAMMEIER NATHAN , TREUTLE MEGAN , JAZAN ELISA , WAYMAN KELLY , DIBBLE DAVID , CHENG JIE-KAI
发明人： WANG WEIBO , NI ZHI-JIE , BARSANTI PAUL , PECCHI SABINA , XIA YI , BRAMMEIER NATHAN , TREUTLE MEGAN , JAZAN ELISA , WAYMAN KELLY , DIBBLE DAVID , CHENG JIE-KAI
IPC分类号： A61K31/4745 , C07D471/02 , C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： Tetrahydrocarboline compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the tetrahydrocarboline compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the tetrahydrocarboline compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.
摘要翻译：四氢咔啉化合物，其药学上可接受的盐和前药; 包括药学上可接受的载体和一种或多种四氢咔啉化合物的组合物，单独或与至少一种其它治疗剂组合。单独使用四氢咔啉化合物或与至少一种另外的治疗剂组合使用的方法可用于预防或治疗增殖性疾病。

6. 发明申请

WO2006049835A3 INDOLE AND BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：吲哚和苯并咪唑衍生物
公开(公告)号：WO2006049835A3
公开(公告)日：2007-11-22
申请号：PCT/US2005036803
申请日：2005-10-14
申请人： NOVARTIS VACCINES & DIAGNOSTIC , BOYCE RUSTUM S , XIA YI , GUO HONGYAN , MENDENHULL KRIS G , WALTER ANNETTE O , WANG WEIBO
发明人： BOYCE RUSTUM S , XIA YI , GUO HONGYAN , MENDENHULL KRIS G , WALTER ANNETTE O , WANG WEIBO
IPC分类号： C07D235/14 , C07D209/14 , C07D401/12 , C07D403/06 , C07D403/14
CPC分类号： C07D403/12 , C07D209/14 , C07D235/14 , C07D401/12 , C07D403/04 , C07D403/14
摘要： The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula (I).
摘要翻译：本发明涉及新的吲哚和苯并咪唑化合物及其药学上可接受的盐，酯或前药，新化合物的组合物和药学上可接受的载体，以及新化合物的用途。本发明的化合物具有以下通式（I）。

7. 发明申请

WO0220463A3 FXR MODULATORS 审中-公开
标题翻译： FXR调制器
公开(公告)号：WO0220463A3
公开(公告)日：2003-08-21
申请号：PCT/US0127239
申请日：2001-08-31
申请人： TULARIK INC , HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
发明人： HOUZE JONATHAN , MCKENDRY SHARON , GERGELY JOSHUA P , XIA YI , SHAN BEI , KAYSER FRANK
IPC分类号： A61P35/00 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07D209/48 , C07D241/44 , C07D279/02 , A61K31/16 , C07C311/17 , C07K14/705
CPC分类号： C07D209/48 , C07C233/75 , C07C237/22 , C07C311/19 , C07C311/29 , C07C2601/14 , C07D241/44 , C07D279/02
摘要： The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7 alpha -hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR gamma and PPAR alpha . Thus, compounds described herein are useful in treating other biological activities such as obesity, diabetes, lipid associated disorders, cancer, inflammatory disorders, disorders involving a disrupted or dysfunctional epidermal barrier, and various other metabolic disorders.
摘要翻译：本发明提供了可用于调节法呢酯X受体（FXR）的化合物，药物组合物和方法。由于FXR涉及负调控胆固醇7α-羟化酶（cyp7a）的表达水平，涉及胆固醇胆固醇氧化代谢的限速酶，本文所述的化合物可用于治疗与异常高相关的疾病或低胆固醇水平在某些方面，本文所述的FXR调节剂（例如拮抗剂）阻断某些胆酸（FXR的内源性配体）产生的cyp7a表达的负反馈下调。此外，由于FXR在一些细胞类型中与类视黄醇X受体（RXR）形成异源二聚体，因此细胞中FXR活性水平的调节对由RXR或其他RXR相互作用介导的各种生物过程具有广泛的影响蛋白质如PPARγ和PPARα。因此，本文所述的化合物可用于治疗其它生物活性，例如肥胖症，糖尿病，脂质相关疾病，癌症，炎性疾病，涉及破坏性或功能失调的表皮屏障的疾病以及各种其它代谢紊乱。

8. 发明申请

WO2011008092A2 GRAM-POSITIVE BACTERIA SPECIFIC BINDING COMPOUNDS 审中-公开
标题翻译：格兰氏阳性细菌特异性结合化合物
公开(公告)号：WO2011008092A2
公开(公告)日：2011-01-20
申请号：PCT/NL2010050456
申请日：2010-07-15
申请人： AIMM THERAPEUTICS BV , GENENTECH INC , BEAUMONT TIM , KWAKKENBOS MARK JEROEN , BROWN ERIC J , MORISAKI JOHN HIROSHI , HAZENBOS WOUTER L W , MARIATHASAN SANJEEV , KAJIHARA KIMBERLY , XIA YI
发明人： BEAUMONT TIM , KWAKKENBOS MARK JEROEN , BROWN ERIC J , MORISAKI JOHN HIROSHI , HAZENBOS WOUTER L W , MARIATHASAN SANJEEV , KAJIHARA KIMBERLY , XIA YI
IPC分类号： C07K16/12
CPC分类号： C07K16/1271 , C07K16/1278 , C07K2317/21 , C07K2317/52 , C07K2317/56 , C07K2317/565 , C07K2317/567 , G01N33/5091 , G01N33/6854 , G01N33/6893 , G01N2469/10 , G01N2800/26
摘要： The present invention provides improved binding compounds capable of specifically binding Gram-positive bacteria. Binding compounds are provided that are fully human, enabling therapeutic applications in human individuals.
摘要翻译：本发明提供了能够特异性结合革兰氏阳性菌的改进的结合化合物。提供的完整人类结合化合物使得能够在人类个体中进行治疗应用。

9. 发明申请

WO2009111676A8 BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：含硼的小分子作为抗炎剂
公开(公告)号：WO2009111676A8
公开(公告)日：2010-09-30
申请号：PCT/US2009036250
申请日：2009-03-05
申请人： ANACOR PHARMACEUTICALS INC , AKAMA TSUTOMU , ZHANG YONG-KANG , DING CHARLES Z , PLATTNER JACOB J , MAPLES KIRK R , FREUND YVONNE , SANDERS VIRGINIA , XIA YI , BAKER STEPHEN J , NIEMANN JAMES A , LU XIAOSONG , SALES MARCELO , SHARMA RASHMI , SINGH RAJESHWAR , JACOBS ROBERT , CHEN DAITAO , ALLEY MICHAEL RICHARD KEVIN
发明人： AKAMA TSUTOMU , ZHANG YONG-KANG , DING CHARLES Z , PLATTNER JACOB J , MAPLES KIRK R , FREUND YVONNE , SANDERS VIRGINIA , XIA YI , BAKER STEPHEN J , NIEMANN JAMES A , LU XIAOSONG , SALES MARCELO , SHARMA RASHMI , SINGH RAJESHWAR , JACOBS ROBERT , CHEN DAITAO , ALLEY MICHAEL RICHARD KEVIN
IPC分类号： A61K31/69
CPC分类号： C07F5/025
摘要： Compounds and methods of treating anti-inflammatory conditions are disclosed.
摘要翻译：公开了治疗抗炎症的化合物和方法。

10. 发明申请

WO2009111676A3 BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：含有BORON的小分子作为抗炎剂
公开(公告)号：WO2009111676A3
公开(公告)日：2010-04-01
申请号：PCT/US2009036250
申请日：2009-03-05
申请人： ANACOR PHARMACEUTICALS INC , AKAMA TSUTOMU , ZHANG YONG-KANG , DING CHARLES Z , PLATTNER JACOB J , MAPLES KIRK R , FREUND YVONNE , SANDERS VIRGINIA , XIA YI , BAKER STEPHEN J , NIEMANN JAMES A , LU XIAOSONG , SALES MARCELO , SHARMA RASHMI , SINGH RAJESHWAR , JACOBS ROBERT , CHEN DAITAO , ALLEY MICHAEL RICHARD KEVIN
发明人： AKAMA TSUTOMU , ZHANG YONG-KANG , DING CHARLES Z , PLATTNER JACOB J , MAPLES KIRK R , FREUND YVONNE , SANDERS VIRGINIA , XIA YI , BAKER STEPHEN J , NIEMANN JAMES A , LU XIAOSONG , SALES MARCELO , SHARMA RASHMI , SINGH RAJESHWAR , JACOBS ROBERT , CHEN DAITAO , ALLEY MICHAEL RICHARD KEVIN
IPC分类号： A61K31/69
CPC分类号： C07F5/025
摘要： Compounds and methods of treating anti-inflammatory conditions are disclosed.
摘要翻译：公开了治疗抗炎症状的化合物和方法。

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