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1. 发明授权

US07015321B2 Synthesis of non-symmetrical sulfamides using burgess-type reagents 失效
标题翻译：使用勃氏型试剂合成非对称磺酰胺
公开(公告)号：US07015321B2
公开(公告)日：2006-03-21
申请号：US10685658
申请日：2003-10-14
申请人： Kyriacos C. Nicolaou , Deborah Longbottom , Scott A. Snyder , Xianhai Huang
发明人： Kyriacos C. Nicolaou , Deborah Longbottom , Scott A. Snyder , Xianhai Huang
IPC分类号： C07D273/02 , C07D273/08 , C07D285/36 , C07D285/16 , C07D285/06
CPC分类号： C07D285/10 , C07D277/04 , C07D285/16 , C07D285/36 , C07D295/26 , C07D417/06 , C07D513/04
摘要： A practical and high-yielding method for the efficient, one-step synthesis of diverse classes of N,N′-differentiated sulfamides employs a wide range of amino alcohols and simple amines using Burgess-type reagents. This methodology extends the application and availability of sulfamides within the fields of chemical biology, medicinal chemistry, asymmetric synthesis, and supramolecular chemistry.
摘要翻译：用于不同种类的N，N'-分化磺酰胺的有效的一步合成的实用和高产方法使用广泛的氨基醇和简单的胺，使用Burgess型试剂。该方法扩展了在化学生物学，药物化学，不对称合成和超分子化学领域中的磺酰胺的应用和可用性。

2. 发明授权

US07579366B2 Epothilone derivatives and their synthesis and use 失效
标题翻译：埃坡霉素衍生物及其合成和用途
公开(公告)号：US07579366B2
公开(公告)日：2009-08-25
申请号：US10386999
申请日：2003-03-11
申请人： Kyriacos C. Nicolaou , Nigel Paul King , Maurice Raymond Verschoyle Finlay , Yun He , Frank Roschangar , Dionisios Vourloumis , Hans Vallberg , Antony Bigot
发明人： Kyriacos C. Nicolaou , Nigel Paul King , Maurice Raymond Verschoyle Finlay , Yun He , Frank Roschangar , Dionisios Vourloumis , Hans Vallberg , Antony Bigot
IPC分类号： A61K31/44 , C07D277/04
CPC分类号： C07D313/00 , C07D417/06 , C07D493/04 , Y02P20/55
摘要： The invention relates to epothilone analog represented by the formula I wherein (i) R2 is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R2 is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R2 is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R2, “b” and “c” are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH2; —C≡CH; —CH2F; —CH2Cl; —CH2—OH; —CH2—O—(C1-C6-alkyl); and —CH2—S—(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of the formula I where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.
摘要翻译：本发明涉及由式I表示的埃坡霉素类似物，其中（i）R2不存在或氧; “a”可以是单键或双键; “b”可以是缺席或单一债券; 和“c”可以不存在或单键，条件是如果R2是氧，则“b”和“c”都是单键，“a”是单键; 如果R2不存在，则“b”和“c”不存在，“a”是双键; 如果“a”是双键，那么R2，“b”和“c”不存在; R3是选自氢的基团; 低级烷基 -CH-CH 2; -C≡CH; -CH2F; -CH2Cl; -CH 2 -OH; -CH 2 -O-（C 1 -C 6 - 烷基）; 和-CH 2 -S-（C 1 -C 6 - 烷基）; R 4和R 5独立地选自氢，甲基或保护基; R1如本说明书中所定义，或其中存在成盐基团的式I化合物的盐。本发明的另一方面涉及埃坡霉素E的合成。这些化合物尤其具有微管解聚抑制活性，对增殖性疾病有用。

3. 发明申请

US20080293747A1 Chemical Synthesis of a Highly Potent Epothilone 失效
标题翻译：化学合成高效埃坡霉素
公开(公告)号：US20080293747A1
公开(公告)日：2008-11-27
申请号：US12092038
申请日：2006-11-09
申请人： Kyriacos C. Nicolaou , Benjamin Pratt , Stellios Arseniyadis
发明人： Kyriacos C. Nicolaou , Benjamin Pratt , Stellios Arseniyadis
IPC分类号： A61K31/52 , C07D417/02 , C07D405/02 , C07D257/04 , A61K31/41 , A61K31/4164 , A61K31/415 , A61K31/4196 , A61K31/426 , C07D277/02 , C07D473/00
CPC分类号： C07D493/04 , C07D405/06 , C07D417/06 , C07D519/00
摘要： A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
摘要翻译：作为包含合成埃坡霉素的药物组合物，公开了一种高活性的合成埃坡霉素化合物，其活性超过了埃博霉素EpoA或EpoB的活性，当被测定为对癌细胞系的细胞毒性剂时。

4. 发明授权

US07173137B2 Epothilone analogs 失效
标题翻译：埃博霉素类似物
公开(公告)号：US07173137B2
公开(公告)日：2007-02-06
申请号：US10732698
申请日：2003-12-09
申请人： Kyriacos C. Nicolaou , Yun He , Sacha Ninkovic , Joaquin Pastor , Frank Roschangar , Francisco Sarabia , Hans Vallberg , Dionisios Vourloumis , Nicolas Winssinger , Zhen Yang , Nigel Paul King , Maurice Raymond Verschoyle Finlay
发明人： Kyriacos C. Nicolaou , Yun He , Sacha Ninkovic , Joaquin Pastor , Frank Roschangar , Francisco Sarabia , Hans Vallberg , Dionisios Vourloumis , Nicolas Winssinger , Zhen Yang , Nigel Paul King , Maurice Raymond Verschoyle Finlay
IPC分类号： C07D417/06 , C07D417/14 , A61K31/427
CPC分类号： C07D417/06 , C07D313/00 , C07D493/04
摘要： Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.
摘要翻译：埃博霉素A，埃坡霉素B，埃坡霉素类似物和埃坡霉素类似物文库合成。埃博霉素A和B是已知的抗癌剂，其通过微管蛋白装配的诱导和稳定来预防有丝分裂来获得它们的抗癌活性。埃坡霉素的类似物是新颖的。与埃坡霉素A或埃坡霉素B相比，几种类似物被证明具有优异的细胞毒性活性，如通过增强诱导微管聚合和稳定化的能力所证实的。

5. 发明授权

US5504206A Formation of esperamicin precursors 失效
标题翻译：形成埃斯霉素前体
公开(公告)号：US5504206A
公开(公告)日：1996-04-02
申请号：US312106
申请日：1994-09-26
申请人： Kyriacos C. Nicolaou , David A. Clark
发明人： Kyriacos C. Nicolaou , David A. Clark
IPC分类号： C07D498/10 , C07D265/12
CPC分类号： C07D498/10
摘要： Intermediates useful in preparing the aglycon or core structure of esperamicin are disclosed, as are methods of making and using the same.
摘要翻译：公开了用于制备埃曲霉素的糖苷配基或核心结构的中间体，以及制备和使用它们的方法。

6. 发明授权

US5384412A Saccharide intermediates in the formation of the calicheamicin and esperamicin oligosaccharides 失效
标题翻译：糖中间体形成加利车霉素和埃斯波霉素寡糖
公开(公告)号：US5384412A
公开(公告)日：1995-01-24
申请号：US972246
申请日：1992-11-05
申请人： Kyriacos C. Nicolaou , Robert D. Groneberg , Erwin P. Schreiner , Wilhelm Stahl
发明人： Kyriacos C. Nicolaou , Robert D. Groneberg , Erwin P. Schreiner , Wilhelm Stahl
IPC分类号： C07D263/24 , C07D309/30 , C07D491/04 , C07D493/04 , C07D521/00 , C07F7/18 , C07D233/00 , C07D315/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D263/24 , C07D309/30 , C07D491/04 , C07D493/04 , C07F7/1856
摘要： Intermediates useful in preparing the calicheamicin and esperamicin oligosaccharides, and particularly the sulfur- and O-substituted hydroxylamine-containing B ring of both oligosaccharides, are disclosed as are methods of making and using the same, including the preparation of chimeric antibiotics using the same.
摘要翻译：用于制备加利车霉素和埃斯波霉素寡糖的中间体，特别是两种寡糖的含硫和O-取代的含羟胺的B环都是公开的制备和使用它们的方法，包括使用其制备嵌合抗生素。

7. 发明授权

US5274141A Designed quinone- and hydroquinone-containing cyclic enediyneols and enediyneones having DNA cleaving and cytotoxic properties 失效
标题翻译：设计含有醌和氢醌的环烯雌醇和具有DNA切割和细胞毒性的烯二酮
公开(公告)号：US5274141A
公开(公告)日：1993-12-28
申请号：US938756
申请日：1992-09-01
申请人： Kyriacos C. Nicolaou , Aijun Liu
发明人： Kyriacos C. Nicolaou , Aijun Liu
IPC分类号： C07C39/23 , C07C49/747 , C07C49/755 , C07C50/14 , C07C50/32 , C07C50/34 , C07C50/38 , C07C69/00 , C07C69/017 , C07F7/18 , C07C50/06 , C07C50/20
CPC分类号： C07F7/1852 , C07C39/23 , C07C49/747 , C07C49/755 , C07C50/14 , C07C50/32 , C07C50/34 , C07C50/38 , C07C69/30 , C07C2102/32 , C07C2103/24
摘要： Quinone- and hydroquinone-containing cyclic enediyneols and enediyneones having 10-carbon atoms in the enediyne-containing ring that cleave DNA are disclosed, as are methods of making and using the same.
摘要翻译：公开了在含有烯烃的环中具有10个碳原子的含喹啉酮和氢醌的环烯炔酮和烯ene酮，其制备和使用它们的方法。

8. 发明授权

US4317935A Bicyclo aldehyde and process for preparation 失效
标题翻译：双环醛和制备方法
公开(公告)号：US4317935A
公开(公告)日：1982-03-02
申请号：US194399
申请日：1980-10-06
申请人： Kyriacos C. Nicolaou , Ronald L. Magolda , David A. Claremon
发明人： Kyriacos C. Nicolaou , Ronald L. Magolda , David A. Claremon
IPC分类号： C07C29/62 , C07C45/51 , C07C45/54 , C07C45/67 , C07C45/68 , C07C59/46 , C07C405/00 , C07C47/44 , C07C45/27
CPC分类号： C07C405/0091 , C07C29/62 , C07C45/51 , C07C45/512 , C07C45/54 , C07C45/67 , C07C45/68 , C07C59/46 , C07C2102/40
摘要： Stable biologically active thromboxane A.sub.2 analogues having the formula: ##STR1## wherein R.sup.1 is OR.sup.3, where R.sup.3 represents hydrogen or a pharmaceutically acceptable cation or lower alkyl group; orR.sup.1 is NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 are the same or different substituents selected from the group consisting of hydrogen and lower alkyl group; andR.sup.2 is hydrogen or an -OH group.The thromboxane analogues are potent thrombotic agents, useful in cardiovascular treatment.
摘要翻译：具有下式的稳定的生物活性凝血恶烷A2类似物：其中R1是OR3，其中R3代表氢或药学上可接受的阳离子或低级烷基; 或R 1是NR 4 R 5，其中R 4和R 5是相同或不同的选自氢和低级烷基的取代基; R2为氢或-OH基。血栓素类似物是有效的血栓形成剂，可用于心血管治疗。

9. 发明授权

US08003801B2 Chemical synthesis of a highly potent epothilone 失效
标题翻译：化学合成高效埃坡霉素
公开(公告)号：US08003801B2
公开(公告)日：2011-08-23
申请号：US12092038
申请日：2006-11-09
申请人： Kyriacos C. Nicolaou , Benjamin Pratt , Stellios Arseniyadis
发明人： Kyriacos C. Nicolaou , Benjamin Pratt , Stellios Arseniyadis
IPC分类号： C07D277/04 , C07D277/60 , C07D257/04 , C07D231/00 , C07D233/00 , C07D249/08
CPC分类号： C07D493/04 , C07D405/06 , C07D417/06 , C07D519/00
摘要： A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
摘要翻译：作为包含合成埃坡霉素的药物组合物，公开了一种高活性的合成埃坡霉素化合物，其活性超过了埃博霉素EpoA或EpoB的活性，当被测定为对癌细胞系的细胞毒性剂时。

10. 发明授权

US07652033B2 HIF-1 inhibitors 有权
标题翻译： HIF-1抑制剂
公开(公告)号：US07652033B2
公开(公告)日：2010-01-26
申请号：US10550286
申请日：2004-03-29
申请人： Erwin G Van Meir , Chalet Tan , Anthony Roecker , Kyriacos C. Nicolaou
发明人： Erwin G Van Meir , Chalet Tan , Anthony Roecker , Kyriacos C. Nicolaou
IPC分类号： A61K31/44
CPC分类号： C07D471/04 , A61K31/352 , A61K31/4178 , A61K31/4188 , A61K45/06 , C07D311/14 , C07D405/06 , C07D405/12 , A61K2300/00
摘要： HIF-1 inhibitors and methods of their use are provided. In particular, 2,2-dimethylbenzopyran based compounds and methods of their use, for example in the treatment or prevention of hypoxia-related pathologies are provided.
摘要翻译：提供HIF-1抑制剂及其使用方法。特别地，提供了基于2,2-二甲基苯并吡喃的化合物及其用途的方法，例如用于治疗或预防缺氧相关病症。

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