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1. 发明授权

US5679652A Amphiphilic nucleosidephosphate analogues 失效
标题翻译：两亲核苷酸类似物
公开(公告)号：US5679652A
公开(公告)日：1997-10-21
申请号：US284683
申请日：1995-01-27
申请人： Herbert Schott , Albert Reto Schwendener , Frederique Guerin
发明人： Herbert Schott , Albert Reto Schwendener , Frederique Guerin
IPC分类号： C07H19/06 , C07H19/10 , A61K31/505
CPC分类号： C07H19/06 , C07H19/10
摘要： 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.
摘要翻译： 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。

2. 发明申请

US20100151001A1 ETHYNYLATED HETERODINUCLEOSIDE PHOSPHATE ANALOGS, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF 审中-公开
标题翻译：乙烯基异丁二酸酯磷酸酯类似物，其生产方法及其用途
公开(公告)号：US20100151001A1
公开(公告)日：2010-06-17
申请号：US12450771
申请日：2008-04-10
申请人： Herbert Schott , Peter Ludwig
发明人： Herbert Schott , Peter Ludwig
IPC分类号： A61K31/7072 , C07H19/10 , A61K9/127 , A61K9/14 , A61P35/00 , A61P31/00
CPC分类号： C07H21/00
摘要： The invention relates to novel ethynylated heterodinucleoside phosphate analogs, the production thereof, substances containing at least one of said compounds, and the use thereof for the treatment of cancer and infectious diseases.
摘要翻译：本发明涉及新型乙炔基异二核苷酸磷酸酯类似物，其生产，含有至少一种所述化合物的物质及其用于治疗癌症和感染性疾病的用途。

3. 发明申请

US20130237494A1 BONE-TARGETING BISPHOSPHONATE DUPLEX DRUGS 有权
标题翻译：骨靶向双磷酸双倍体药物
公开(公告)号：US20130237494A1
公开(公告)日：2013-09-12
申请号：US13814172
申请日：2011-08-03
申请人： Herbert Schott
发明人： Herbert Schott
IPC分类号： C07F9/6512 , A61K45/06 , A61K31/7068
CPC分类号： C07F9/6512 , A61K31/7068 , A61K45/06 , C07D239/54 , C07F9/65586 , C07H15/00 , C07H19/073 , C07H19/09
摘要： The present invention relates to novel bisphosphonate duplex drugs, methods for preparing said compound; pharmaceutical compositions containing the same; as well as the use of said compounds in human and veterinary medicine, and, in particular, for treating tumors, viral infections; or dental disorders.
摘要翻译：本发明涉及新型二膦酸双倍体药物，制备所述化合物的方法; 含有该组合物的药物组合物; 以及所述化合物在人和兽医学中的用途，特别是用于治疗肿瘤，病毒感染; 或牙齿障碍。

4. 发明授权

US06354624B1 Ballast weight arrangement 有权
公开(公告)号：US06354624B1
公开(公告)日：2002-03-12
申请号：US09632437
申请日：2000-08-04
申请人： Herbert Schott
发明人： Herbert Schott
IPC分类号： B60S900
摘要： 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.

5. 发明申请

US20060172997A1 Combinations of inhibitors of reverse transcriptase and inhibitors of virus-encoded DNA polymerase 审中-公开
标题翻译：逆转录酶抑制剂与病毒编码DNA聚合酶抑制剂的组合
公开(公告)号：US20060172997A1
公开(公告)日：2006-08-03
申请号：US11265825
申请日：2005-11-03
申请人： Klaus Hamprecht , Herbert Schott , Elfriede Mikeler , Gerhard Jahn
发明人： Klaus Hamprecht , Herbert Schott , Elfriede Mikeler , Gerhard Jahn
IPC分类号： A61K31/551 , A61K31/522 , A61K31/513
CPC分类号： A61K45/06
摘要： A method for treating viral diseases which are caused by DNA viruses is described comprising administering an effective amount of at least one inhibitor of reverse transcriptase (RTI) in combination with at least one inhibitor of viral DNA polymerase, wherein the at least one RTI and the at least one DNA polymerase inhibitor are present in the form of separate compounds.
摘要翻译：描述了用于治疗由DNA病毒引起的病毒性疾病的方法，其包括将有效量的至少一种逆转录酶（RTI）抑制剂与至少一种病毒DNA聚合酶抑制剂组合施用，其中所述至少一种RTI和至少一种DNA聚合酶抑制剂以分开的化合物的形式存在。

6. 发明申请

US20050187183A1 Use of amphiphilic nucleoside phosphonoformic acid derivatives for the treatment of viral infectious diseases 失效
标题翻译：使用两亲核苷磷酰甲酸衍生物治疗病毒性传染病
公开(公告)号：US20050187183A1
公开(公告)日：2005-08-25
申请号：US11015209
申请日：2004-12-16
申请人： Klaus Hamprecht , Gerhard Jahn , Herbert Schott
发明人： Klaus Hamprecht , Gerhard Jahn , Herbert Schott
IPC分类号： A61K31/047 , A61K31/7072 , A61P31/12
CPC分类号： A61K31/7072 , A61K31/047
摘要： The invention relates to a method for treating infectious diseases which are elicited by viruses which are pathogenic to humans comprising the step of administering an amphiphilic nucleoside-phosphonoformic acid derivative having an esterified or unesterified carboxyl group, preferably of a nucleoside-glycerol-(hydroxycarbonyl)-phosphonate, as an active compound.
摘要翻译：本发明涉及一种治疗感染性疾病的方法，所述感染性疾病是由对人体致病的病毒引起的，包括施用具有酯化或未酯化羧基的两亲核苷 - 膦酰甲酸衍生物的步骤，优选核苷 - 甘油 - （羟基羰基）膦酸酯，作为活性化合物。

7. 发明授权

US08916536B2 Bone-targeting bisphosphonate duplex drugs 有权
标题翻译：骨靶向双磷酸双倍体药物
公开(公告)号：US08916536B2
公开(公告)日：2014-12-23
申请号：US13814172
申请日：2011-08-03
申请人： Herbert Schott
发明人： Herbert Schott
IPC分类号： A01N43/04 , A61K31/70 , C07H19/09 , C07F9/6558 , C07H19/073 , C07H15/00 , A61K45/06 , A61K31/7068 , C07F9/6512 , C07D239/54
CPC分类号： C07F9/6512 , A61K31/7068 , A61K45/06 , C07D239/54 , C07F9/65586 , C07H15/00 , C07H19/073 , C07H19/09
摘要： The present invention relates to novel bisphosphonate duplex drugs, methods for preparing said compound; pharmaceutical compositions containing the same; as well as the use of said compounds in human and veterinary medicine, and, in particular, for treating tumors, viral infections; or dental disorders.
摘要翻译：本发明涉及新型二膦酸双倍体药物，制备所述化合物的方法; 含有该组合物的药物组合物; 以及所述化合物在人和兽医学中的用途，特别是用于治疗肿瘤，病毒感染; 或牙齿障碍。

8. 发明授权

US07279465B2 Use of amphiphilic nucleoside phosphonoformic acid derivatives for the treatment of viral infectious diseases 失效
标题翻译：使用两亲核苷磷酰甲酸衍生物治疗病毒性传染病
公开(公告)号：US07279465B2
公开(公告)日：2007-10-09
申请号：US11015209
申请日：2004-12-16
申请人： Klaus Hamprecht , Gerhard Jahn , Herbert Schott
发明人： Klaus Hamprecht , Gerhard Jahn , Herbert Schott
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H21/00
CPC分类号： A61K31/7072 , A61K31/047
摘要： The invention relates to a method for treating infectious diseases which are elicited by viruses which are pathogenic to humans comprising the step of administering an amphiphilic nucleoside-phosphonoformic acid derivative having an esterified or unesterified carboxyl group, preferably of a nucleoside-glycerol-(hydroxycarbonyl)-phosphonate, as an active compound.
摘要翻译：本发明涉及一种治疗感染性疾病的方法，所述感染性疾病是由对人体致病的病毒引起的，包括施用具有酯化或未酯化羧基的两亲核苷 - 膦酰甲酸衍生物的步骤，优选核苷 - 甘油 - （羟基羰基）膦酸酯，作为活性化合物。

9. 发明授权

US06787525B1 Glyceryl nucleotides, method for the production thereof and their use 失效
标题翻译：甘油核苷酸，其制备方法及其用途
公开(公告)号：US06787525B1
公开(公告)日：2004-09-07
申请号：US09856165
申请日：2001-09-12
申请人： Herbert Schott , Peter Stephan Ludwig
发明人： Herbert Schott , Peter Stephan Ludwig
IPC分类号： A61K3170
CPC分类号： C07H19/06 , C07H19/16 , C07H19/207
摘要： 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.
摘要翻译：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

US06471245B1 Ballast weight arrangement 失效
标题翻译：镇流器重量排列
公开(公告)号：US06471245B1
公开(公告)日：2002-10-29
申请号：US09632437
申请日：2000-08-04
申请人： Herbert Schott
发明人： Herbert Schott
IPC分类号： B60S900
CPC分类号： B62D49/085
摘要： 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.
摘要翻译：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。

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