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21. 发明申请

WO2004011476A1 GLYCONJUGATES COMPRISING CARBOHYDRATE EPITOPES, METHODS FOR THEIRSYNTHESIS, AND THEIR USE FOR THE TREATMENT OR PROPHYLAXIS OF CANCER 审中-公开
标题翻译：包含碳水化合物抗体的糖衣，其治疗方法及其用于治疗或预防癌症的用途
公开(公告)号：WO2004011476A1
公开(公告)日：2004-02-05
申请号：PCT/US2003/022657
申请日：2003-07-18
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , COLTART, Don, M. , KEDING, Stacy, J. , BISWAS, Kaustav , LIVINGSTON, Philip, O. , RAGUPATHI, Govindaswami , ALLEN, Jennifer, R. , WILLIAMS, Lawrence
发明人： DANISHEFSKY, Samuel, J. , COLTART, Don, M. , KEDING, Stacy, J. , BISWAS, Kaustav , LIVINGSTON, Philip, O. , RAGUPATHI, Govindaswami , ALLEN, Jennifer, R. , WILLIAMS, Lawrence
IPC分类号： C07H15/10
CPC分类号： C07H15/04 , A61K31/715 , A61K38/00 , A61K39/0011 , A61K2039/55555 , A61K2039/55577 , A61K2039/55594 , A61K2039/6081 , A61K2039/627 , C07B2200/11 , C07H15/10 , C07H15/18 , C07K1/1077 , C07K5/06139 , C07K9/00 , C07K14/43509
摘要： The present invention provides novel glycosides and glycoconjugates, glycoamino acids, and methods for the synthesis thereof. In another aspect, the present invention provides novel clustered glycopeptides and methods for the synthesis thereof. In still another aspect, the present invention provides methods for the treatment of cancer, preferably for the prevention of recurrence of cancer, and methods for inducing antibodies in a subject, comprising administering to a subject in need, an effective amount of any of the inventive glycopeptides as disclosed herein, either in conjugated form or unconjugated and in combination with a suitable immunogenic carrier.
摘要翻译：本发明提供新的糖苷和糖缀合物，糖基氨基酸及其合成方法。另一方面，本发明提供了新颖的聚合糖肽及其合成方法。另一方面，本发明提供了治疗癌症的方法，优选用于预防癌症复发，以及用于在受试者中诱导抗体的方法，包括向有需要的受试者施用有效量的本发明的任何一种本文公开的糖肽，以缀合形式或未偶联的，并与合适的免疫原性载体组合。

22. 发明申请

WO2003022844A2 SYNTHESIS OF EPOTHILONES INTERMEDIATES THERETO AND ANALOGUES THEREOF 审中-公开
标题翻译：其中EPOTHILONS中间体的合成及其类似物
公开(公告)号：WO2003022844A2
公开(公告)日：2003-03-20
申请号：PCT/US2002/028425
申请日：2002-09-06
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BISWAS, Kaustav , CHAPELL, Mark , LIN, Hong , NJARDARSON, Jon, T. , LEE, Chulbom , RIVKIN, Alexey , CHOU, Ting-Chao
发明人： DANISHEFSKY, Samuel, J. , BISWAS, Kaustav , CHAPELL, Mark , LIN, Hong , NJARDARSON, Jon, T. , LEE, Chulbom , RIVKIN, Alexey , CHOU, Ting-Chao
IPC分类号： C07D419/06
CPC分类号： C07D413/06 , C07D417/06 , C07D493/04 , C07D493/08
摘要： The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula(I).
摘要翻译：本发明提供式（I）化合物：如本文中一般性地和类别和亚类所述。本发明另外提供包含式（I）化合物的药物组合物，并提供治疗癌症的方法，包括施用式（I）化合物。

23. 发明申请

WO1993020036A1 TOTAL SYNTHESIS OF TAXOL 审中-公开
标题翻译： TAXOL的总合成
公开(公告)号：WO1993020036A1
公开(公告)日：1993-10-14
申请号：PCT/US1993003031
申请日：1993-03-30
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BORNMANN, William, G. , QUENEAU, Yves , MAGEE, Thomas, V. , KROL, Walter, J.
IPC分类号： C07C49/603
CPC分类号： C07C403/08 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/46 , C07C403/14 , C07C403/16 , C07C403/20 , C07C2601/14 , C07C2601/16 , C07D305/14 , C07D317/72 , C07F7/1804
摘要： The present invention provides two basic routes for the total synthesis of taxol having structure (I). 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：本发明提供了具有结构（I）的紫杉醇的全合成的两条基本路线。本发明还提供了在上述方法中制备的中间体，用于合成这些中间体的方法以及与紫杉醇的类似物。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。

24. 发明申请

WO1996034005A1 SYNTHESIS OF THE BREAST TUMOR-ASSOCIATED ANTIGEN DEFINED BY MONOCLONAL ANTIBODY MBR1 AND USES THEREOF 审中-公开
标题翻译：由单克隆抗体MBR1定义的与乳腺癌相关的抗原的合成及其用途
公开(公告)号：WO1996034005A1
公开(公告)日：1996-10-31
申请号：PCT/US1996006109
申请日：1996-04-26
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BILODEAU, Mark, T. , HU, Shuang, Hua , PARK, Tae, Kyo , RANDOLPH, John, T. , KIM, In, Jong , LIVINGSTON, Philip, O.
IPC分类号： C07H15/24
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 process for synthesizing a compound having structure (I), 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：本发明提供了用于合成具有结构（I）的化合物的方法，其中R是H，以及可用作用于在其辅助治疗中诱导人乳腺癌细胞的抗体的疫苗的相关寡糖。

25. 发明申请

WO1995025113A1 SYNTHETIC COMPOUNDS WHICH BIND TO H. PYLORI, AND USES THEREOF 审中-公开
标题翻译：合成化合物，其与H.PYLORI的结合，及其用途
公开(公告)号：WO1995025113A1
公开(公告)日：1995-09-21
申请号：PCT/US1995003273
申请日：1995-03-15
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , RANDOLPH, John, T.
IPC分类号： C07H05/02
CPC分类号： C07H15/10 , A61K39/0011 , C07H3/06 , C07H15/18 , C07H17/02 , C07K16/3015 , C07K16/44
摘要： The present invention provides a compound having structure (I), wherein A is selected from the group consisting of (i) an amino acid bearing an omega -amino group or an omega -(C=O)- group, (ii) an amino acid residue of a peptide, which residue bears an omega -amino group or an omega -(C=O)- group, and (iii) an amino acid residue of a protein, which residue bears an omega -amino group or an omega -(C=O)- group; wherein R1 is H, OH, NH2 or NHR4, where R4 is SO2Ph, a linear or branched chain alkyl or acyl group, or an aryl group; wherein M is a saccharide wherein n is an integer from 0 to 18, and where n is greater than 1, each M is independently the same or different; wherein p is either 0 or 1; wherein R2, R3, R5 and R6 are independently the same or different and are H or OH, with the proviso that geminal R2 and R3 are not both OH, and geminal R5 and R6 are not both OH; wherein X and Y are independently the same or different and are H2 or O; and wherein k is an integer greater than or equal to 1, with the proviso that when A is an amino acid bearing an omega -amino group or an omega -(C=O)- group, k is equal to 1.
摘要翻译：本发明提供具有结构（I）的化合物，其中A选自（i）具有ω-氨基或ω-（C = O） - 基团的氨基酸，（ii）氨基肽的酸残基，该残基具有ω-氨基或ω-（C = O） - 基团，和（iii）蛋白质的氨基酸残基，该残基具有ω-氨基或ω- （C = O） - 基团; 其中R 1是H，OH，NH 2或NHR 4，其中R 4是SO 2 Ph，直链或支链烷基或酰基或芳基; 其中M是糖，其中n是0至18的整数，并且其中n大于1，每个M独立地相同或不同; 其中p是0或1; 其中R 2，R 3，R 5和R 6独立地相同或不同，为H或OH，条件是偕R 2和R 3不同时为OH，偕R 5和R 6不同时为OH; 其中X和Y独立地相同或不同，为H 2或O; 并且其中k是大于或等于1的整数，条件是当A是具有ω-氨基或ω-（C = O） - 基团的氨基酸时，k等于1。

26. 发明申请

WO1995012567A1 TOTAL SYNTHESIS OF TAXOL AND ANALOGUES THEREOF 审中-公开
标题翻译： TAXOL及其类似物的总合成
公开(公告)号：WO1995012567A1
公开(公告)日：1995-05-11
申请号：PCT/US1994012661
申请日：1994-11-02
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BORNMANN, William, G. , QUENEAU, Yves , MAGEE, Thomas, V. , KROL, Walter, J. , MASTERS, John, J. , JUNG, David, K.
IPC分类号： C07C49/543
CPC分类号： C07D305/14 , C07C45/29 , C07C45/59 , C07C49/613 , C07C49/687 , C07C49/713 , C07C49/723 , C07C49/737 , C07C49/747 , C07C49/753 , C07C49/757 , C07C255/31 , C07C255/46 , C07C403/08 , C07C403/14 , C07C403/16 , C07C403/20 , C07C2601/14 , C07C2601/16 , C07D317/72 , C07F7/1804
摘要： The present invention provides three basic routes for the total synthesis of taxol having structure (I). 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：本发明提供了具有结构（I）的紫杉醇的总合成的三条基本路线。本发明还提供了在上述方法中制备的中间体，用于合成这些中间体的方法以及紫杉醇和诺泰莫酚的类似物。

27. 发明申请

WO2015034920A2 GRANULOCYTE MACROPHAGE COLONY-STIMULATING FACTOR COMPOSITIONS 审中-公开
公开(公告)号：WO2015034920A2
公开(公告)日：2015-03-12
申请号：PCT/US2014/053895
申请日：2014-09-03
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： DANISHEFSKY, Samuel, J. , ZHANG, Qiang , JOHNSTON, Eric
IPC分类号： A61K38/19
CPC分类号： C07K14/535 , A61K38/00 , A61K39/0011 , A61K39/39 , A61K2039/55522
摘要： The present invention provides a composition of homogeneously glycosylated GM-CSF or a homogeneously glycosylated fragment thereof, wherein each molecule of GM-CSF or fragment thereof has the same glycosylation pattern, and for a given glycosylation site each molecule of GM-CSF or fragment thereof has the same glycan. The present invention further provides methods of making and using such compositions.
摘要翻译：本发明提供了均匀糖基化的GM-CSF或其均匀糖基化的片段的组合物，其中GM-CSF或其片段的每个分子具有相同的糖基化模式，并且对于给定的糖基化位点，每个分子的GM-CSF或其片段具有相同的聚糖。本发明还提供制备和使用这些组合物的方法。

28. 发明申请

WO1999001124A1 SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO, ANALOGUES AND USES THEREOF 审中-公开
标题翻译：爱乐酮的合成，中间体，类似物及其用途
公开(公告)号：WO1999001124A1
公开(公告)日：1999-01-14
申请号：PCT/US1997022381
申请日：1997-12-03
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BALOG, Aaron , BERTINATO, Peter , SU, Dai-Shi , CHOU, Ting-Chau , MENG, Dong, Fang , KAMENECKA, Ted , SORENSEN, Erik, J.
IPC分类号： A61K31/34
CPC分类号： A61K31/704 , A61K31/335 , A61K31/337 , A61K31/425 , A61K31/475 , A61K31/70 , A61K45/06 , C07C69/007 , C07D277/24 , C07D313/00 , C07D417/06 , C07D417/14 , C07D493/04 , C07F7/1852 , C07F7/1856 , A61K2300/00
摘要： The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.
摘要翻译：本发明涉及用于制备埃博霉素A和B，脱氧埃坡霉素A和B及其类似物的会聚方法。它还涉及与埃博霉素A和B有关的类似物以及用于其制备的中间体。它还涉及基于所述埃博霉素的新型组合物以及治疗癌症和多药耐药性癌症的方法。

29. 发明申请

WO1994011376A1 CAMPTOTHECIN ANALOGUES AND METHODS OF PREPARATION THEREOF 审中-公开
标题翻译： CAMPTOTHECIN类似物及其制备方法
公开(公告)号：WO1994011376A1
公开(公告)日：1994-05-26
申请号：PCT/US1993006918
申请日：1993-07-23
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BORNMANN, William, G. , SHEN, Wang , COBURN, Craig, A.
IPC分类号： C07D491/14
CPC分类号： C07D491/14 , C07H17/00
摘要： Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of general structure (I), wherein E is H, CO2R, CONH2, CONHR, CONR2, acyl, or CN; X is H, OH, or OR; R , R , R and R are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R , R , R , R and R are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO2R, nitro, cyano, Cl, F, Br, I, SR , NR R , or OR ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R , R and R are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R is glycosyl; n is 0 or 1; with the proviso that when R is ethyl, and n is 0, E, R , R and R are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D and E fused together. Methods for preparing the analogues involve condensation of such intermediates with variably substituted protected alpha -aminobenzaldehydes.
摘要翻译：具有一般结构（I）的癌细胞具有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，酰基或CN; X是H，OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟基烷基或芳基; 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，烷基芳基，烷氧基，羟基烷基或氨基烷氧基氰基，Cl，F，Br，I，SR 10，NR 11 R 12或OR 13中的至少一个或多个。 R是H或直链或支链烷基，烷基芳基或羟基烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷芳基，羟基烷基或酰基或芳基; R 13是糖基; n为0或1; 条件是当R 1是乙基且n是0时，E，R 2，R 3和R 4不是全部H.导致喜树碱类似物的中间体化合物包括取代的三环化合物，其中由融合在一起的环C，D和E组成。制备类似物的方法涉及这种中间体与可变取代的被保护的α-氨基苯甲醛的缩合。

30. 发明申请

WO2013166053A2 HOMOGENOUS AND FULLY GLYCOSYLATED HUMAN ERYTHROPOIETIN 审中-公开
标题翻译：均质和全谷氨酰化人类红细胞生成素
公开(公告)号：WO2013166053A2
公开(公告)日：2013-11-07
申请号：PCT/US2013/038923
申请日：2013-04-30
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： DANISHEFSKY, Samuel, J. , WANG, Ping , DONG, Suwei , MOORE, Malcolm, Andrew Stephen , SHIEH, Jae-hung , BRAILSFORD, John, Andrew
IPC分类号： C07K14/505 , G01N33/74
CPC分类号： C07K14/505 , G01N33/746
摘要： The present invention provides homogenously glycosylated erythropoietin and the methods of preparing the same.
摘要翻译：本发明提供均匀的糖基化促红细胞生成素及其制备方法。

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