CAS: 29767-20-2; (5R,5Ar,8Ar,9S)-9-(((2R,4Ar,6R,7R,8R,8As)-7,8-Dihydroxy-2-(Thiophen-2-yl)Hexahydropyrano[3,2-D][1,3]Dioxin-6-yl)Oxy)-5-(4-Hydroxy-3,5-Dimethoxyphenyl)-5,5A,8A,9-Tetrahydrofuro[3',4':6,7]Naphtho[2,3-D][1,3]Dioxol-6(8H)-One

上下游产品

9-[(4,6-O-(Thien-2-Ylmethylidene-β-D-Glucopyranosyl)Oxy)-5,8,9A,9-Tetrahydro-5-(4-(5-Nitrothien-2-yl)Methoxy)3,5-Dimethoxyphenyl]Furo[3',4':6,7]Naphtha[2,3-D]-1,3-Dioxol-6(5Ah)-One

9-[(4,6-O-(Thien-2-Ylmethylidene-β-D-Glucopyranosyl)Oxy)-5,8,9A,9-Tetrahydro-5-(4-(5-Nitrothien-2-yl)Methoxy)3,5-Dimethoxyphenyl]Furo[3',4':6,7]Naphtha[2,3-D]-1,3-Dioxol-6(5Ah)-One 反应生成替尼泊苷
参考文献: Bioreductively-Activated Prodrugs[fr] Promédicaments Activés Par Une Bioréduction
标题: Bioreductively-Activated Prodrugs[fr] Promédicaments Activés Par Une Bioréduction
摘要:化合物的化学式(1),或其药学上可接受的盐,其中:-Ar是一种带有至少一个硝基或偶氮基的取代杂环芳基基团,或者是苯醌,萘醌或融合的杂环喹啉;-R1是氢,可选取代的烷基,可选取代的烯基,可选取代的炔基,可选取代的环烷基,可选取代的杂环环烷基,可选取代的芳基或可选取代的杂环芳基;-R2是糖苷,Oh,可选取代的烷基,可选取代的烷氧基,C2-C8烯基,C1-C8羟基烷基,可选取代的芳基氨基,可选取代的芳基c1-C4烷基氨基或羟基烷基氨基;以及-R3和r4各自独立地是h或卤素.

专利信息

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人：HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

专利号:US-5633260-A
优先权日:1994-04-19
标 题 :11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof
发明人：HAUSHEER FREDERICK H; HARIDAS KOCHAT
权利人:BIONUMERIK PHARMACEUTICALS INC
摘要:The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.