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    • 1. 发明授权
    • Amphiphilic nucleosidephosphate analogues
    • 两亲核苷酸类似物
    • US5679652A
    • 1997-10-21
    • US284683
    • 1995-01-27
    • Herbert SchottAlbert Reto SchwendenerFrederique Guerin
    • Herbert SchottAlbert Reto SchwendenerFrederique Guerin
    • C07H19/06C07H19/10A61K31/505
    • C07H19/06C07H19/10
    • Amphiphilic nucleoside phosphate analogues of formula I ##STR1## wherein R.sup.1 denotes a hydroxyl or amino group or an acylated or alkylated or polyoxyethylene-substituted amino group, the acyl or alkyl group of which is straight-chained or branched, has 1 to 24 carbon atoms and up to 2 double bonds and may be substituted by an aromatic group; R.sup.2 denotes H, F, a 2-bromo vinyl group or a straight-chained or branched C.sub.1-24 -alkyl group; R.sup.3 and R.sup.4 are identical or different and denote H, hydroxyl, halogen and azido; R.sup.5 denotes a nucleoside group of formula II ##STR2## wherein R.sup.6 denotes a hydroxyl or amino group or an acylated or alkalized amino group, the acyl or alkyl group of which is straight-chained or branched, contains 1 to 24 carbon atoms and up to 2 double bonds and may be substituted by an aromatic group, whilst R.sup.6 and R.sup.1 are different and one of the groups denotes acylamino or alkylamino groups having 12 to 24 carbon atoms, R.sup.1, R.sup.2, R.sup.6 and R.sup.7 are selected so that, together, they impart an amphiphilic nature to a dinucleotide phosphate analogue; and the corresponding salts of the acid forms of these compounds.
    • PCT No.PCT / EP93 / 00346 Sec。 371日期:1995年1月27日 102(e)日期1995年1月27日PCT提交1993年2月12日PCT公布。 公开号WO93 / 16093 日期:1993年8月19日式I的亲核性核苷磷酸酯类似物(I)其中R1表示羟基或氨基或酰化或烷基化或聚氧乙烯取代的氨基,其酰基或烷基是直链或 具有1至24个碳原子和至多2个双键并且可以被芳基取代; R2表示H,F,2-溴乙烯基或直链或支链C 1-14烷基; R3和R4相同或不同,表示H,羟基,卤素和叠氮基; R5表示式II的核苷酸(II)其中R6表示羟基或氨基或酰基或碱化的氨基,其酰基或烷基是直链或支链的,含有1至24个碳原子 并且可以被芳基取代,而R6和R1不同,其中一个表示酰基氨基或具有12-24个碳原子的烷基氨基,R1,R2,R6和R7被选择, 一起,它们赋予二核苷酸磷酸酯类似物两亲性质; 和这些化合物的酸形式的相应盐。
    • 9. 发明授权
    • Glyceryl nucleotides, method for the production thereof and their use
    • 甘油核苷酸,其制备方法及其用途
    • US06787525B1
    • 2004-09-07
    • US09856165
    • 2001-09-12
    • Herbert SchottPeter Stephan Ludwig
    • Herbert SchottPeter Stephan Ludwig
    • A61K3170
    • C07H19/06C07H19/16C07H19/207
    • The invention relates to glyceryl nucleotides of the formula Ia in which a) one of the radicals A1, A2 and A3 is a hydrogen atom or a radical selected from hydroxyl, mercapto, alkyl, alkenyl, polyoxyalkenyl, aryl, acyl, alkyloxy, alkenyloxy, polyoxyalkenyloxy, acyloxy, aryloxy, alkylthio, alkenylthio, acylthio and arylthio, where the alkyl, alkenyl and acyl radicals are optionally substituted by from 1 to 3 aryl radicals; and b1) two of the remaining radicals A1, A2 and A3 are two nucleoside groups which are different from each other; or b2) one of the remaining radicals A1, A2 and A3 is a nucleoside group and the other of the remaining radicals is a hydroxycarbonyl group, where at least one of the nucleoside groups is not a naturally occurring nucleoside group; to processes for preparing these compounds, to pharmaceutical remedies which comprise these compounds, and to the use of these compounds for treating cancer diseases and infectious diseases.
    • 本发明涉及式Iain的甘油基核苷酸,其中a 1,A 2和A 3之一是氢原子或选自羟基,巯基,烷基,烯基,聚氧乙烯基,芳基 酰基,烷氧基,烯氧基,聚氧乙烯氧基,酰氧基,芳氧基,烷硫基,烯硫基,酰硫基和芳硫基,其中烷基,链烯基和酰基任选被1至3个芳基取代; 和b1)剩余的基团A 1,A 2和A 3中的两个是彼此不同的两个核苷酸基团; orb2)剩余基团A 1,A 2和A 3中的一个是核苷基团,剩余的基团中的另一个是羟基羰基,其中至少一个核苷基团不是天然存在的 核苷类;制备这些化合物的方法,包含这些化合物的药物治疗剂以及这些化合物用于治疗癌症疾病和感染性疾病的用途。
    • 10. 发明授权
    • Ballast weight arrangement
    • 镇流器重量排列
    • US06471245B1
    • 2002-10-29
    • US09632437
    • 2000-08-04
    • Herbert Schott
    • Herbert Schott
    • B60S900
    • B62D49/085
    • A ballast weight arrangement for a working vehicle has an interlocking connection between a ballast weight and a ballast weight support in the transverse plane of the vehicle, wherein interlocking is brought about by at least one projection on the ballast weight engaging in a recess on an adjacent ballast weight. Interlocking is achieved by controlled movement of a locking member on lifting up ballast weight 8 from a deposit block 22 and be released on putting down ballast weight 8 on deposit block 22.
    • 用于工作车辆的压载重量装置在车辆的横向平面中的压载重量和压载重量支撑件之间具有互锁连接,其中通过至少一个突出部在联接在邻近的凹部上的压载重物上引起互锁 镇流器重量。通过锁定构件在从沉积块22提升压载重量8时受到控制的移动来实现锁定,并且在将沉重块8放在沉积块22上时被释放。