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31. 发明申请

WO2005061481A1 NOVEL MA CROCYCLES AND USES THEREOF 审中-公开
标题翻译：新加坡制造商及其用途
公开(公告)号：WO2005061481A1
公开(公告)日：2005-07-07
申请号：PCT/US2004/042887
申请日：2004-12-17
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , YANG, Zhi-Qiang , GENG, Xudong , CHOU, Ting-Chao , ROSEN, Neal
发明人： DANISHEFSKY, Samuel, J. , YANG, Zhi-Qiang , GENG, Xudong , CHOU, Ting-Chao , ROSEN, Neal
IPC分类号： C07D315/00
CPC分类号： C07D313/00
摘要： The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) (I) wherein R,,-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.
摘要翻译：本发明涉及其结构（及其药学上可接受的衍生物）（I）的化合物，其中R 1 -R 4，Z，X，AB，DE，GJ和KL如本文所定义，其合成和使用这些化合物作为治疗剂。

32. 发明申请

WO2004050711A3 GP120 SPECIFIC ANTIGENS, CONJUGATES THEREOF, METHODS FOR THEIR PREPARATION AND USES THEREOF 审中-公开
标题翻译： GP120特异性抗原，与其结合，其制备方法及其用途
公开(公告)号：WO2004050711A3
公开(公告)日：2005-01-27
申请号：PCT/US0338471
申请日：2003-12-03
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRBARAN
发明人： DANISHEFSKY SAMUEL J , DUDKIN VADIM , GENG XUDONG , MANDAL MIHIRBARAN
IPC分类号： A61K39/21 , C07K1/107 , C07K14/16 , C07K14/375 , C07K14/505
CPC分类号： C07K14/005 , A61K38/00 , A61K39/12 , A61K39/21 , A61K2039/55577 , A61K2039/6018 , A61K2039/6081 , A61K2039/627 , C07K1/1077 , C07K14/375 , C07K14/505 , C12N2740/16122 , C12N2740/16134
摘要： The present invention provides compounds having formula (I): wherein R , R , R , R , R , W , W and W are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods of use thereof in the treatment of HIV, methods for the prevention of HIV, and methods for inducing HIV-specific antibodies in a subject, comprising administering to a subject in need thereof, an effective amount of any of the inventive compounds as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier. In another aspect, the invention provides an antibody or antibody fragment which binds specifically to a gp 120 glycan or glycopeptide of the invention.
摘要翻译：本发明提供具有式（I）的化合物：其中R 1，R 2A，R 2B，R 3，R 4，W 1，W 2和W 3 >如本文定义; 并且另外提供其合成方法，其组合物及其用于治疗HIV的方法，用于预防HIV的方法以及在受试者中诱导HIV-特异性抗体的方法，包括向有需要的受试者施用，有效量的本文公开的任何本发明化合物，其以缀合形式或未缀合并与合适的免疫原性载体组合。另一方面，本发明提供了与本发明的gp120聚糖或糖肽特异性结合的抗体或抗体片段。

33. 发明申请

WO2003051303A3 THE TOTAL SYNTHESIS OF MERRILACTONE A 审中-公开
公开(公告)号：WO2003051303A3
公开(公告)日：2003-06-26
申请号：PCT/US2002/040003
申请日：2002-12-13
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , DANISHEFSKY, Samuel, J. , BIRMAN, Vladimir
发明人： DANISHEFSKY, Samuel, J. , BIRMAN, Vladimir
IPC分类号： C07D307/77
摘要： This invention provides a total synthesis of Merrillactone and Merrilactone analogues having the structure formula (I), wherein Z is 0 or >N-X, where X is H, straight or branched substituted or unsubstituted alkyl, alkenyl or alkynyl, or acyl, carbamoyl, cycloalkyl, aryl, heterocycloalkyl, heteroaryl, aralkyl, amino, alkyl amino, or dialkyl amino; and all the R’s groups are described in the specification.

34. 发明申请

WO1997018215A1 ANALOGUES OF N-ACETYLARDEEMIN, METHOD OF PREPARATION AND USES THEREOF 审中-公开
标题翻译： N-乙酰胺的类似物，其制备方法及其用途
公开(公告)号：WO1997018215A1
公开(公告)日：1997-05-22
申请号：PCT/US1996019086
申请日：1996-11-15
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF , DANISHEFSKY, Samuel , DEPEW, Kristopher , MARSDEN, Stephen, P. , BORNMANN, William , WOO, Jonathan, C., G. , CHOU, Ting-Chao , SCHKERYANTZ, Jeffrey , ZATORSKI, Andrej
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF
IPC分类号： C07D487/22
CPC分类号： C07D487/22
摘要： The present invention provides a compound having structure (I) wherein R1, R6 and R7 are independently hydrogen, OH, NH2, SH, halogen, C1-C9 linear or branched chain alkyl, alkylmercapto, alkylamino, dialkylamino, alkoxy, phenyl, etc; wherein R0 and R2 are independently hydrogen, OH, linear or branched chain alkyl, -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH=CHR4, wherein R3 and R4 are independently hydrogen, halogen, C1-C9 linear or branched chain alkyl, phenyl, etc; wherein R5 is hydrogen, C1-C9 linear or branched chain alkyl, phenyl, etc; an wherein R8 is hydrogen, C1-C9 linear or branched chain acyl, benzoyl, etc; with the proviso that (a) when R2 is -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH=CHR4, then R0 is hydrogen; (b) when R0 is -CR3R3-CH(O)CH2, -CR3R3-CH2CH3, -CR3R3-CH2CH2OH, -CR3R3-CH(OH)R4 or -CR3R3-CH=CHR4, then R2 is OH; and (c) when (i) R0 or R2 is -CR3R3-CH=CHR4, (ii) R3 and R5 are CH3 and (iii) R4 is hydrogen, then R1, R6 and R7 are not all hydrogen. Also provided are related compounds and compositions, and methods of inhibiting the growth of multidrug resistant cells by means of MDR reversal, collateral sensitivity and quantitative synergism.
摘要翻译：本发明提供具有结构（I）的化合物，其中R 1，R 6和R 7独立地是氢，OH，NH 2，SH，卤素，C 1 -C 9直链或支链烷基，烷基巯基，烷基氨基，二烷基氨基，烷氧基，苯基等; 其中R 0和R 2独立地是氢，OH，直链或支链烷基，-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4 其中R3和R4独立地是氢，卤素，C1-C9直链或支链烷基，苯基等; 其中R5是氢，C1-C9直链或支链烷基，苯基等; 其中R8是氢，C1-C9直链或支链酰基，苯甲酰基等; 条件是（a）当R 2为-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4时，则R 0为氢; （b）当R 0是-CR 3 R 3 -CH（O）CH 2，-CR 3 R 3 -CH 2 CH 3，-CR 3 R 3 -CH 2 CH 2 OH，-CR 3 R 3 -CH（OH）R 4或-CR 3 R 3 -CH = CHR 4时，则R2是OH; 和（c）当（i）R 0或R 2为-CR 3 R 3 -CH = CHR 4时，（ⅱ）R 3和R 5为CH 3，（ⅲ）R 4为氢，则R 1，R 6和R 7不全为氢。还提供了相关的化合物和组合物，以及通过MDR逆转，附着敏感性和定量协同作用抑制多药耐药细胞生长的方法。

35. 发明申请

WO2012139074A3 MIGRASTATINS AND USES THEREOF 审中-公开
标题翻译： MIGRASTATINS及其用途
公开(公告)号：WO2012139074A3
公开(公告)日：2012-12-13
申请号：PCT/US2012032642
申请日：2012-04-06
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , MASSAGUE JOAN , CORTES MANUEL VALIENTE , OSKARSSON THORDUR , MOORE MALCOLM , LAMONTE NICOLAS , OUERFELLI OUATHEK , YANG GUANGLI
发明人： DANISHEFSKY SAMUEL J , MASSAGUE JOAN , CORTES MANUEL VALIENTE , OSKARSSON THORDUR , MOORE MALCOLM , LAMONTE NICOLAS , OUERFELLI OUATHEK , YANG GUANGLI
IPC分类号： A01N43/02 , A61K31/335
CPC分类号： C07D313/00 , A61K31/335
摘要： The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
摘要翻译：本发明提供了化合物，其药学上可接受的组合物及其使用方法。

36. 发明申请

WO2012139074A2 MIGRASTATINS AND USES THEREOF 审中-公开
标题翻译：偏移及其用途
公开(公告)号：WO2012139074A2
公开(公告)日：2012-10-11
申请号：PCT/US2012/032642
申请日：2012-04-06
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , MASSAGUE, Joan , CORTES, Manuel, Valiente , OSKARSSON, Thordur , MOORE, Malcolm , LAMONTE, Nicolas , OUERFELLI, Ouathek , YANG, Guangli
发明人： DANISHEFSKY, Samuel, J. , MASSAGUE, Joan , CORTES, Manuel, Valiente , OSKARSSON, Thordur , MOORE, Malcolm , LAMONTE, Nicolas , OUERFELLI, Ouathek , YANG, Guangli
IPC分类号： A61K31/335
CPC分类号： C07D313/00 , A61K31/335
摘要： The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
摘要翻译：本发明提供化合物，其药学上可接受的组合物及其使用方法。

37. 发明申请

WO2010025272A1 COMPOUNDS, COMPOSITIONS AND METHODS FOR REDUCING TOXICITY AND TREATING OR PREVENTING DISEASES 审中-公开
标题翻译：用于减少毒性和治疗或预防疾病的化合物，组合物和方法
公开(公告)号：WO2010025272A1
公开(公告)日：2010-03-04
申请号：PCT/US2009/055221
申请日：2009-08-27
申请人： THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK , SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , CHOU, Ting-Chao , LEI, Xiaoguang , YUN, Heedong , NG, Fay , HARTUNG, John , SAMES, Dalibor
发明人： DANISHEFSKY, Samuel, J. , CHOU, Ting-Chao , LEI, Xiaoguang , YUN, Heedong , NG, Fay , HARTUNG, John , SAMES, Dalibor
IPC分类号： A61K31/34
CPC分类号： C07C33/048 , A61K31/047 , A61K31/075 , A61K31/165 , A61K31/196 , A61K31/337 , A61K31/343 , A61K31/357 , A61K31/4192 , A61K31/427 , A61K31/661 , A61K31/675 , A61K31/7048 , A61K45/06 , C07B2200/07 , C07C33/05 , C07C33/14 , C07C33/30 , C07C43/315 , C07C49/24 , C07C2601/02 , C07C2601/14 , C07D249/04 , C07D317/16 , C07D317/18 , C07D317/20 , C07D317/22 , C07D317/24 , C07D317/26 , C07D317/28 , C07D317/30 , A61K2300/00
摘要： The present invention provides compounds of Formula (I), compositions comprising an effective amount of a Compound of Formula (I), optionally with chemotherapeutic drug, such as a tubulin-binding drug, and methods of their use for reducing the toxicity of cytotoxic agents, for example chemotherapy agents, treating or preventing cancer or a neurotrophic disorder, inducing a chemoprotective phase II enzyme, DNA, or protein synthesis, enhancing the immune system, treating inflammation, improving and enhancing general health or well-being, and methods for making Compounds of Formula (I).
摘要翻译：本发明提供式（I）化合物，包含有效量的式（I）化合物，任选地与化学治疗药物如微管蛋白结合药物组合的组合物，及其用于降低细胞毒性剂毒性的方法，例如化疗剂，治疗或预防癌症或神经营养障碍，诱导化学保护性II期酶，DNA或蛋白质合成，增强免疫系统，治疗炎症，改善和增强一般健康或健康，以及制备方法式（I）的化合物。

38. 发明申请

WO2007120614A3 HOMOGENEOUS ERYTHROPOIETIN AND OTHER PEPTIDES AND PROTEINS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION 审中-公开
标题翻译：均质红细胞生成素和其他肽和蛋白质，其制备方法和中间体
公开(公告)号：WO2007120614A3
公开(公告)日：2008-08-21
申请号：PCT/US2007008764
申请日：2007-04-11
申请人： SLOAN KETTERING INST CANCER , DANISHEFSKY SAMUEL J , WARREN J DAVID , CHEN JIEHAO , WU BIN , CHEN GONG , WAN QIAN , TAN ZHONGPING , KAN CINDY , YUAN YU , HUA ZIHAO , RANGANATHAN KRISHNAKUMAR , TRZUPEK JOHN D
发明人： DANISHEFSKY SAMUEL J , WARREN J DAVID , CHEN JIEHAO , WU BIN , CHEN GONG , WAN QIAN , TAN ZHONGPING , KAN CINDY , YUAN YU , HUA ZIHAO , RANGANATHAN KRISHNAKUMAR , TRZUPEK JOHN D
IPC分类号： C07K14/00 , A61K38/00 , A61K38/16
CPC分类号： C07K14/505 , C07K9/00 , C12P21/005
摘要： The present invention provides isolated homogeneous polyfunctionalized proteins (e.g., erythropoietin), isolated glycopeptides, and a method for preparing polyfunctionalized peptides and/or proteins via cysteine-free native chemical ligation. In certain embodiments, the invention provides an isolated homogeneous polyfunctionalized protein having the structure (I). In certain other embodiments, the invention provides an isolated glycopeptide having Formula (II). In certain other embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently substituted with a moiety having the structure (III) -LH. wherein A and L1 are as defined herein.
摘要翻译：本发明提供了分离的均相多官能化蛋白质（例如红细胞生成素），分离的糖肽，以及通过不含半胱氨酸的天然化学连接制备多官能化肽和/或蛋白质的方法。在某些实施方案中，本发明提供具有结构（I）的分离的均相多官能化蛋白质。在某些其它实施方案中，本发明提供了具有式（II）的分离的糖肽。在某些其他实施方案中，本发明的方法是制备多功能化肽的方法，其包含由四个或更多个氨基酸组成的肽主链，其中两个或多个不相邻氨基酸独立地被具有结构（III）的部分取代， -LH。其中A和L1如本文所定义。

39. 发明申请

WO2007087220A3 THE TOTAL SYNTHESIS OF ECTEINASCIDIN 743 AND DERIVATIVES THEREOF 审中-公开
标题翻译： ECTEINASCIDIN 743及其衍生物的全合成
公开(公告)号：WO2007087220A3
公开(公告)日：2007-11-08
申请号：PCT/US2007001329
申请日：2007-01-19
申请人： UNIV COLUMBIA , DANISHEFSKY SAMUEL J , CHAN COLLIN
发明人： DANISHEFSKY SAMUEL J , CHAN COLLIN
IPC分类号： A61K33/24 , C07D491/14
CPC分类号： C07D471/18 , C07D317/54 , C07D491/056 , C07D491/22
摘要： This invention provides a method of synthesizing ecteinascidin 743 and derivatives. This invention also provides intermediate compounds and methods of treating tumors.
摘要翻译：本发明提供了一种合成ecteinascidin 743及其衍生物的方法。本发明还提供了治疗肿瘤的中间体化合物和方法。

40. 发明申请

WO2007120614A2 HOMOGENEOUS ERYTHROPOIETIN AND OTHER PEPTIDES AND PROTEINS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION 审中-公开
标题翻译：均质的红细胞生成素和其他肽和蛋白质，其制备方法和中间体
公开(公告)号：WO2007120614A2
公开(公告)日：2007-10-25
申请号：PCT/US2007/008764
申请日：2007-04-11
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , WARREN, J., David , CHEN, Jiehao , WU, Bin , CHEN, Gong , WAN, Qian , TAN, Zhongping , KAN, Cindy , YUAN, Yu , HUA, Zihao , RANGANATHAN, Krishnakumar , TRZUPEK, John, D.
发明人： DANISHEFSKY, Samuel, J. , WARREN, J., David , CHEN, Jiehao , WU, Bin , CHEN, Gong , WAN, Qian , TAN, Zhongping , KAN, Cindy , YUAN, Yu , HUA, Zihao , RANGANATHAN, Krishnakumar , TRZUPEK, John, D.
IPC分类号： C07K14/505
CPC分类号： C07K14/505 , C07K9/00 , C12P21/005
摘要： The present invention provides isolated homogeneous polyfunctionalized proteins (e.g., erythropoietin), isolated glycopeptides, and a method for preparing polyfunctionalized peptides and/or proteins via cysteine-free native chemical ligation. In certain embodiments, the invention provides an isolated homogeneous polyfunctionalized protein having the structure (I). In certain other embodiments, the invention provides an isolated glycopeptide having Formula (II). In certain other embodiments, the inventive method is a method for preparing a polyfunctionalized peptide comprising a peptidic backbone made up of four or more amino acids, wherein two or more non-adjacent amino acids are independently substituted with a moiety having the structure (III) -LH. wherein A and L1 are as defined herein.
摘要翻译：本发明提供了分离的均相多官能化蛋白（例如促红细胞生成素），分离的糖肽，以及通过不含半胱氨酸的天然化学连接制备多官能化肽和/或蛋白质的方法。在某些实施方案中，本发明提供具有结构（I）的分离的均相多官能化蛋白质。在某些其他实施方案中，本发明提供了具有式（II）的分离的糖肽。在某些其他实施方案中，本发明的方法是制备包含由四个或更多个氨基酸组成的肽主链的多官能化肽的方法，其中两个或更多个不相邻氨基酸独立地被具有结构（III）的部分取代， -LH。其中A和L1如本文所定义。

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