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61. 发明授权

US06936714B2 Compounds of the saframycin-ecteinascidin series, uses, and synthesis thereof 失效
标题翻译：安全霉素类抗坏血病素系列化合物，用途及其合成
公开(公告)号：US06936714B2
公开(公告)日：2005-08-30
申请号：US10728580
申请日：2003-12-05
申请人： Samuel J. Danishefsky , Bishan Zhou
发明人： Samuel J. Danishefsky , Bishan Zhou
IPC分类号： A61K31/4995 , A61P35/00 , C07C271/22 , C07D217/24 , C07D471/18 , C07D491/04 , C07D491/056 , C07D491/22 , C07D471/14
CPC分类号： C07D491/04 , C07D217/24
摘要： Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.
摘要翻译：公开了具有以下通式及其用途和合成的具有细胞毒性的安全霉素 - 白in素类化合物的化合物：其中R 1和R 4均为H，C < 或C 1至C 4烷基，或酰基; 其中R 2是醚，酯，酰胺或邻苯二甲酰亚胺基团; 其中R 3为-O，OH，醚基，酰基如OC（O）Me，OC（O）Bn和OC（O）Et）或硫醚基; 其中R 5是H，卤素，OH，醚基，酰基或酰胺基; 其中R 6为-O，OH，OCH 3，CN或酰氧基; 其中R 7为-O，OH，卤素，醚基或酰基; 其中R 8和R 9独立地为H，CH 3，OCH 3，OC 2， CH 3，CF 3，卤素如Br和F，或R 8和R 9，作为亚甲二氧基或其它五元或六元环连接在一起; 其中R 10和R 11独立地是CH 3，OCH 3，OC 2， 5 H 3，SCH 3，或SC 2 H 5; 其中R 12是H，C 1至C 4烷基或酰基; 并且其中标记为*的手性中心具有R或S构型。

62. 发明授权

US06645935B2 Synthesis of glycoconjugates of the lewis Y epitope and uses thereof 有权
标题翻译：路易斯Y表位糖缀合物的合成及其用途
公开(公告)号：US06645935B2
公开(公告)日：2003-11-11
申请号：US09977185
申请日：2001-10-12
申请人： Samuel J. Danishefsky , Victor Behar , Kenneth O. Lloyd
发明人： Samuel J. Danishefsky , Victor Behar , Kenneth O. Lloyd
IPC分类号： A61K3816
CPC分类号： C07H15/10 , A61K38/00 , A61K39/0011 , C07H3/06 , C07H15/18 , C07H17/02 , C07K1/04 , C07K9/005 , C07K16/3015 , C07K16/44
摘要： The present invention provides a method of synthesizing an allyl pentasaccharide having the structure: as well as related oligosaccharide ceramides and other glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefor, and in a method for preventing recurrence of epithelial cancer.
摘要翻译：本发明提供一种合成具有以下结构的烯丙基五糖的方法：以及作为用于在其辅助治疗中诱导上皮癌细胞抗体的疫苗的相关寡糖神经酰胺和其它糖缀合物，以及用于预防上皮癌复发的方法。

63. 发明授权

US06303120B1 Synthesis of glycoconjugates of the lewis y epitope and uses thereof 失效
标题翻译：路易威因表位的糖缀合物的合成及其用途
公开(公告)号：US06303120B1
公开(公告)日：2001-10-16
申请号：US08506251
申请日：1995-07-24
申请人： Samuel J. Danishefsky , Victor Behar , Kenneth O. Lloyd
发明人： Samuel J. Danishefsky , Victor Behar , Kenneth O. Lloyd
IPC分类号： A61K39395
CPC分类号： C07H15/10 , A61K38/00 , A61K39/0011 , C07H3/06 , C07H15/18 , C07H17/02 , C07K1/04 , C07K9/005 , C07K16/3015 , C07K16/44
摘要： The present invention provides a method of synthesizing an allyl pentasaccharide having the structure: as well as related oligosaccharide ceramides and other glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefor, and in a method for preventing recurrence of epithelial cancer.
摘要翻译：本发明提供一种合成具有以下结构的烯丙基五糖的方法：以及作为用于在其辅助治疗中诱导上皮癌细胞抗体的疫苗的相关寡糖神经酰胺和其它糖缀合物，以及用于预防上皮癌复发的方法。

64. 发明授权

US6090789A Synthesis of the breast tumor-associated antigen defined by monoclonal antibody MBr1 and uses thereof 失效
标题翻译：由单克隆抗体MBr1定义的乳腺肿瘤相关抗原的合成及其用途
公开(公告)号：US6090789A
公开(公告)日：2000-07-18
申请号：US977215
申请日：1997-11-24
申请人： Samuel J. Danishefsky , Mark T. Bilodeau , Shuang Hua Hu , Tae Kyo Park , John T. Randolph , In Jong Kim , Philip O. Livingston
发明人： Samuel J. Danishefsky , Mark T. Bilodeau , Shuang Hua Hu , Tae Kyo Park , John T. Randolph , In Jong Kim , Philip O. Livingston
IPC分类号： C07H11/00 , A61K31/70 , A61K31/7028 , A61K31/7042 , A61K31/7048 , A61K38/00 , A61K39/00 , A61K39/39 , A61P35/00 , A61P37/04 , C07H3/06 , C07H15/10 , C07H15/18 , C07H17/02 , C07H17/04 , C07K1/04 , C07K9/00 , C07K16/30 , C07K16/44 , C07H5/06 , C07H15/04 , G01N33/00
CPC分类号： C07H15/10 , A61K39/0011 , C07H15/18 , C07H17/02 , C07H3/06 , C07K1/04 , C07K16/3015 , C07K16/44 , C07K9/005 , A61K38/00
摘要： The present invention provides a process for synthesizing a compound having the structure: ##STR1## wherein R is H, as well as related oligosaccharides useful as a vaccine for inducing antibodies to human breast cancer cells in an adjuvant therapy therefor.
摘要翻译：本发明提供一种合成具有以下结构的化合物的方法：其中R为H，以及可用作用于在其辅助治疗中诱导人乳腺癌细胞抗体的疫苗的相关寡糖。

65. 发明授权

US5597931A Total synthesis of taxol and analogues thereof 失效
标题翻译：紫杉醇及其类似物的总合成
公开(公告)号：US5597931A
公开(公告)日：1997-01-28
申请号：US436809
申请日：1995-05-05
申请人： Samuel J. Danishefsky , John Masters , Wendy Young , J. Thomas Link , Richard Isaacs , Lawrence B. Snyder
发明人： Samuel J. Danishefsky , John Masters , Wendy Young , J. Thomas Link , Richard Isaacs , Lawrence B. Snyder
IPC分类号： C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/46 , C07D305/14 , C07D317/72 , C07D493/08 , C07D493/18 , C07F7/18 , C07D317/70
CPC分类号： C07D493/08 , C07C255/31 , C07C255/46 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07D305/14 , C07D317/72 , C07F7/1852 , C07F7/1856 , C07C2101/14 , C07C2101/16
摘要： The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.
摘要翻译：本发明提供了具有以下结构的紫杉醇的总合成的三种基本途径：本发明还提供了上述方法中制备的中间体，合成这些中间体的方法以及紫杉醇和北美多酚的类似物。

66. 发明授权

US5527924A Total synthesis of taxol 失效
公开(公告)号：US5527924A
公开(公告)日：1996-06-18
申请号：US350251
申请日：1994-12-05
申请人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol
发明人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol
IPC分类号： A61K31/335 , C07C13/28 , C07C45/29 , C07C45/59 , C07C49/603 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/45 , C07C255/46 , C07D305/14 , C07D317/72 , C07D339/08 , C07D493/04 , C07F7/18 , C07D317/12
CPC分类号： C07C403/08 , C07C255/31 , C07C255/46 , C07C403/14 , C07C403/16 , C07C403/20 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07D305/14 , C07D317/72 , C07F7/1852 , C07F7/1856 , C07C2101/14 , C07C2101/16
摘要： The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.

67. 发明授权

US5525731A Camptothecin analogues and methods of preparation thereof 失效
标题翻译：喜树碱类似物及其制备方法
公开(公告)号：US5525731A
公开(公告)日：1996-06-11
申请号：US328415
申请日：1994-10-25
申请人： Samuel J. Danishefsky , Lawrence B. Snyder
发明人： Samuel J. Danishefsky , Lawrence B. Snyder
IPC分类号： C07D491/14 , C07D491/147 , C07D491/22 , C07H17/00 , A61K31/435
CPC分类号： C07D491/14 , C07H17/00
摘要： Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, or CN; R.sup.0 and R.sup.1 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.2, R.sup.3 and R.sup.4 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl or aryl group, or an alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano or aminoalkoxy group, or CO.sub.2 R, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12 or OR.sup.13 ; R is H, an alkyl, aryl, alkylaryl or hydroxyalkyl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, an alkyl, aryl, alkylaryl or acyl group; R.sup.13 is glycosyl; and n is 0 or 1. Also provided are compositions comprising the analogues and methods of treating tumors as well as methods for preparing the analogues.
摘要翻译：具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2或CN; R 0和R 1独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基，羟烷基或芳基; R2，R3和R4独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基，羟基烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，直链或支链烷基芳基或芳基，或烷氧基，芳氧基，羟基烷基，C-缩醛，硝基，氰基或氨基烷氧基或CO2R，Cl，F，Br，I，SR10，NR11R12或OR13; R是H，烷基，芳基，烷基芳基或羟烷基; R 10，R 11和R 12独立地相同或不同，为H，烷基，芳基，烷基芳基或酰基; R13是糖基; 并且n为0或1.还提供了包含治疗肿瘤的类似物和方法的组合物以及制备类似物的方法。

68. 发明授权

US5416225A Total synthesis of taxol 失效
标题翻译：紫杉醇的总合成
公开(公告)号：US5416225A
公开(公告)日：1995-05-16
申请号：US860792
申请日：1992-03-30
申请人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol
发明人： Samuel J. Danishefsky , William G. Bornmann , Yves Queneau , Thomas V. Magee , Walter J. Krol
IPC分类号： A61K31/335 , C07C13/28 , C07C45/29 , C07C45/59 , C07C49/603 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/45 , C07C255/46 , C07D305/14 , C07D317/72 , C07D339/08 , C07D493/04 , C07F7/18
CPC分类号： C07C403/08 , C07C255/31 , C07C255/46 , C07C403/14 , C07C403/16 , C07C403/20 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07D305/14 , C07D317/72 , C07F7/1852 , C07F7/1856 , C07C2101/14 , C07C2101/16
摘要： The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.
摘要翻译：本发明提供了具有以下结构的紫杉醇的总合成的两条基本路线：本发明还提供了上述方法中制备的中间体，合成这些中间体的方法以及类似物的紫杉醇。紫杉醇的中间体和类似物都可能被证明是有价值的抗癌剂。

69. 发明授权

US09598466B2 Glycopeptide constructs and uses thereof 有权
公开(公告)号：US09598466B2
公开(公告)日：2017-03-21
申请号：US13003739
申请日：2009-07-13
申请人： Samuel J. Danishefsky , Jianglong Zhu , Dongjoo Lee , Philip Livingston , Govind Ragupathi
发明人： Samuel J. Danishefsky , Jianglong Zhu , Dongjoo Lee , Philip Livingston , Govind Ragupathi
IPC分类号： A61K38/00 , C07K9/00 , A61K39/00
CPC分类号： C07K9/001 , A61K38/00 , A61K39/0011 , A61K2039/6081 , A61K2039/6093 , C07K9/006
摘要： Glycopeptide conjugates, and methods of making and using such conjugates are disclosed. Certain glycopeptide conjugates comprise tumor associated carbohydrate antigens and peptide epitopes. Certain glycopeptide conjugates comprise cyclic peptide scaffolds that display carbohydrate antigens in a clustered fashion. The immunogenicity of select glycopeptide conjugates is demonstrated.

70. 发明授权

US09303009B2 Migrastatins and uses thereof 有权
标题翻译： Migrastatins及其用途
公开(公告)号：US09303009B2
公开(公告)日：2016-04-05
申请号：US14110115
申请日：2012-04-06
申请人： Samuel J. Danishefsky , Joan Massague , Manuel Valiente Cortes , Thordur Oskarsson , Malcom Moore , Nicolas Lecomte , Ouathek Ouerfelli , Guangli Yang
发明人： Samuel J. Danishefsky , Joan Massague , Manuel Valiente Cortes , Thordur Oskarsson , Malcom Moore , Nicolas Lecomte , Ouathek Ouerfelli , Guangli Yang
IPC分类号： C07D313/00 , 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。

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