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11. 发明授权

US5965718A Analogs of sarcodictyin and eleutherobin 失效
标题翻译：讽刺素和eleutherobin的类似物
公开(公告)号：US5965718A
公开(公告)日：1999-10-12
申请号：US145376
申请日：1998-09-01
申请人： Kyriacos C. Nicolaou , Floris VanDelft , Seijiro Hosokawa , Sanghee Kim , Tianhu Li , Takashi Ohshima , Jeff Pfefferkorn , Dionisios Vourloumis , Jin-You Xu , Nicolas Winssinger
发明人： Kyriacos C. Nicolaou , Floris VanDelft , Seijiro Hosokawa , Sanghee Kim , Tianhu Li , Takashi Ohshima , Jeff Pfefferkorn , Dionisios Vourloumis , Jin-You Xu , Nicolas Winssinger
IPC分类号： C07H15/26 , A61K31/34 , A61K31/4164 , A61K31/422 , A61K31/427 , A61K31/443 , A61K31/7028 , A61K31/7048 , A61P35/00 , A61P43/00 , C07D493/08 , C07F7/18 , C07H15/24 , A61K31/70 , C07D307/77
CPC分类号： C07D493/08
摘要： Sarcodictyin A and B, eleutherobin, and bioactive analogs thereof synthesized using solid phase and solution phase chemistries. The synthetic method employs an attachment of common precursors, e.g., compounds 1880 or 200, on a solid support for generating conjugates 230 and 240, followed by standard chemical manipulations. A combinatorial library of sarcodictyins and eletherobin analogs was constructed with modified C-8 ester, C-15 ester and C-4 ketal functionalities and was screened for activity with respect to tubulin polymerization and cytotoxic activity against tumor cells, including Taxol-resistant lines. Compounds 600, 610, 630, 660-700, 730, 760, 850, and 920 were identified to be of equal or superior biological activities as compared to their corresponding natural product.
摘要翻译： Sarcodictyin A和B，eleutherobin及其使用固相和溶液相化学合成的生物活性类似物。合成方法使用常用前体（例如化合物1880或200）在固体支持物上的附着，用于产生共轭物230和240，随后进行标准化学操作。用修饰的C-8酯，C-15酯和C-4缩酮官能团构建了链霉菌素和eletherobin类似物的组合文库，并筛选了关于微管蛋白聚合和抗肿瘤细胞（包括耐紫杉醇系）的细胞毒活性的活性。与其相应的天然产物相比，化合物600,610,630,660-700,730,760,850和920被鉴定为具有相同或优异的生物活性。

12. 发明授权

US5110949A Method of synthesizing leukotriene B.sub.4 and derivatives thereof 失效
标题翻译：白三烯B4及其衍生物的合成方法
公开(公告)号：US5110949A
公开(公告)日：1992-05-05
申请号：US388990
申请日：1989-09-13
申请人： Yoshihiro Abe , Kyriacos C. Nicolaou
发明人： Yoshihiro Abe , Kyriacos C. Nicolaou
IPC分类号： C07C51/09 , C07F7/18
CPC分类号： C07F7/1852 , C07C51/09
摘要： An improved method for synthesizing leukotriene B.sub.4 and derivatives thereof is disclosed, as are novel intermediates used in the process. Unlike prior art processes, the method of this invention involves a step in which 2(R)-[[(1,1-dimethylethyl)diphenylsilyl]oxy]dec-4 (Z)-ene-1-ol or a related compound is coupled with methyl-[5(S)-[[1,1dimethylethyl)-diphenylsilyl]oxy]-dec-8 (E)-10-(dimethylphosphono)-6-ynoate.
摘要翻译：公开了一种用于合成白三烯B4及其衍生物的改进方法，以及该方法中使用的新型中间体。不同于现有技术的方法，本发明的方法涉及2（R） - [[（1,1-二甲基乙基）二苯基甲硅烷基]氧基]癸-4（Z） - 烯-1-醇或相关化合物为与[5（S） - [[1,1-二甲基乙基] - 二苯基甲硅烷基]氧基] -dec-8（E）-10-（二甲基膦酰基）-6-取代物偶联。

13. 发明授权

US5097062A Cyclic conjugated enediynes 失效
标题翻译：环状共轭烯二烯
公开(公告)号：US5097062A
公开(公告)日：1992-03-17
申请号：US214019
申请日：1988-06-30
申请人： Kyriacos C. Nicolaou , Guido Zuccharello , Yuji Ogawa
发明人： Kyriacos C. Nicolaou , Guido Zuccharello , Yuji Ogawa
IPC分类号： C07C33/16 , C07C69/007
CPC分类号： C07C69/007 , C07C33/16
摘要： The synthesis of stable, ten-membered cyclic conjugated enediynes is described. Said compounds were successfully employed to cleave double-stranded DNA spontaneously at ambient temperatures.
摘要翻译：描述了稳定的十元环共轭烯二炔的合成。所述化合物成功应用于环境温度下自发切割双链DNA。

14. 发明授权

US4977286A Glycolipids 失效
标题翻译：糖脂
公开(公告)号：US4977286A
公开(公告)日：1990-12-11
申请号：US242723
申请日：1988-09-09
申请人： Kyriacos C. Nicolaou , Thomas J. Caulfield
发明人： Kyriacos C. Nicolaou , Thomas J. Caulfield
IPC分类号： C07F7/18 , C07H15/10
CPC分类号： C07H15/10 , C07F7/1852
摘要： Novel, optically active azido alcohols are synthesized from N-haloacetyl oxazolidinone and are coupled with protected, activated carbohydrate residues in stereoselective glycosidic fashion to provide glycolipids in substantially pure stereochemical form. In accordance with certain preferred embodiments, the glycosphingolipids globotriaosylceramide, lactosyl ceramide, and galactosyl ceramide are synthesized in substantially pure stereochemical form from alkenyl, C-18 azido alcohols and protected fluoroglycosides and are employed as antigens in the production of antibodies useful, for example, in the treatment of disease.
摘要翻译：新的旋光活性叠氮醇由N-卤代乙酰基恶唑烷酮合成并与保护的活性碳水化合物残留物以立体选择性糖苷方式偶联，以提供基本上纯的立体化学形式的糖脂。根据某些优选实施方案，糖基脂蛋白球三烯酰神经酰胺，乳糖基神经酰胺和半乳糖基神经酰胺以基本上纯的立体化学形式由烯基，C-18叠氮基醇和被保护的氟代糖苷合成，并且在制备抗体中被用作抗体，在治疗疾病。

15. 发明授权

US4759880A Alkanoarachidonic acids 失效
标题翻译：藻糖酸
公开(公告)号：US4759880A
公开(公告)日：1988-07-26
申请号：US655196
申请日：1984-09-27
申请人： Kyriacos C. Nicolaou , Nicos A. Petasis , Wen-Sen Li , Tamara Ladduwahetty , Jared L. Randall , Stephen E. Webber , Pedro E. Hernandez
发明人： Kyriacos C. Nicolaou , Nicos A. Petasis , Wen-Sen Li , Tamara Ladduwahetty , Jared L. Randall , Stephen E. Webber , Pedro E. Hernandez
IPC分类号： C07C47/225 , C07C47/45 , C07C57/26 , C07C57/52 , C07C61/35 , C07C62/16 , C11C1/00 , A61K31/045 , C07C33/05 , C07C47/21
CPC分类号： C07C57/26 , C07C47/225 , C07C47/45 , C07C57/52 , C07C61/35 , C07C62/16
摘要： A series of alkanoarachidonic acids have been prepared as modulators of the arachidonic acid cascade to increase the production of biologically desirable compounds and minimize the production of biologically undesirable compounds. Examples of desirable compounds in this respect comprise postaglandins and thromboxanes whereas undesirable compounds comprise the mono- and polyhydroxyarachidonic acids and leukotrienes. The alkanoarachidonic acids and their intermediates are of the general formula: ##STR1## and at least one of X, Y, and Z is lower alkano and is hydrogen when not lower alkano; the esters and salts of the acids are also prepared. The acids, esters and salts may be used as anti-anaphylaxis or anti-thrombosis agents.
摘要翻译：已经制备了一系列链烷二糖酸作为花生四烯酸级联的调节剂，以增加生物需要的化合物的产生并使生物学不需要的化合物的产生最小化。所需化合物在这方面的实例包括Postaglandin和血栓素，而不希望的化合物包括单羟基和多羟基花生四烯酸和白三烯。链烷二酸及其中间体具有以下通式：其中R 1 =低级烷基（低级烷基）（低级亚烷基）OH（低级亚烷基）CHO CHO，其中R 2 = COO（低级烷基）（低级烷基）亚烷基）OH（低级亚烷基）CHO CHO其中R3 = COO（低级烷基）（低级亚烷基）OH（低级亚烷基）CHO CHO，X，Y和Z中的至少一个为低级烷基，当不为低级烷还制备了酸的酯和盐。酸，酯和盐可用作抗过敏反应或抗血栓形成剂。

16. 发明授权

US4429166A Method of preparing bicyclo(3.1.1)hept-2-one 失效
标题翻译：双环（3.1.1）庚-2-酮的制备方法
公开(公告)号：US4429166A
公开(公告)日：1984-01-31
申请号：US289965
申请日：1981-08-04
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 , C07C45/45
CPC分类号： C07C405/0091 , C07C29/62 , C07C45/51 , 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。

17. 发明授权

US4308396A Thromboxane A.sub.2 analogues 失效
标题翻译：血栓素A2类似物
公开(公告)号：US4308396A
公开(公告)日：1981-12-29
申请号：US019932
申请日：1979-03-12
申请人： Kyriacos C. Nicolaou , Ronald L. Magolda
发明人： Kyriacos C. Nicolaou , Ronald L. Magolda
IPC分类号： C07C59/46 , C07C405/00 , C07C57/26 , C07C69/608 , C07C103/19
CPC分类号： C07C405/0091 , C07C59/46 , Y10S514/929
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.
摘要翻译：具有式“IMAGE”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。

18. 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。

19. 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。

20. 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。

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