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11. 发明授权

US5734042A Process for the production of asymmetrical phosphoric acid diesters 失效
标题翻译：生产不对称磷酸二酯的方法
公开(公告)号：US5734042A
公开(公告)日：1998-03-31
申请号：US682571
申请日：1996-07-29
申请人： Einhard Kiegel , Harald Zilch
发明人： Einhard Kiegel , Harald Zilch
IPC分类号： C07H19/06 , C07F9/09 , C07F9/6558 , C07F9/6561 , C07H19/10 , C07H19/20 , C07H1/02 , C07H19/207
CPC分类号： C07H19/10 , C07F9/09 , C07H19/20
摘要： The present invention concerns a process for the production of asymmetrical phosphoric acid diesters. The process is characterized in that a phosphoric acid ester is condensed with a compound containing hydroxy groups in the presence of an arylsulfonic acid chloride and an organic base, the residue of evaporation is stirred out with an organic solvent after the hydrolysis, the arylsulfonic acid pyridine salt which forms is nearly completely crystallized and recycled, the lipid derivative that is formed is precipitated as a sparingly soluble salt by addition of a solution containing alkaline-earth ions and isolated, the sparingly soluble salt is isolated as the free acid in an organic solvent by suspension in a water-immiscible organic solvent and a dilute aqueous mineral acid, the crude product is purified if desired, by means of preparative chromatography on a RP phase and subsequently the free acid is converted if desired into any desired salt.
摘要翻译： PCT No.PCT / EP95 / 00219 Sec。 371日期：1996年7月29日 102（e）日期1996年7月29日PCT提交1995年1月21日PCT公布。公开号WO95 / 20596 日期1995年8月3日本发明涉及不对称磷酸二酯的制造方法。该方法的特征在于，在芳基磺酰氯和有机碱的存在下，将磷酸酯与含有羟基的化合物缩合，水解后用有机溶剂搅拌残余物，芳基磺酸吡啶形成的盐几乎完全结晶并再循环，所形成的脂质衍生物通过加入含有碱土离子的溶液并分离而作为微溶盐沉淀，将微溶盐作为游离酸在有机溶剂中分离通过悬浮在与水不混溶的有机溶剂和稀无机酸水溶液中，如果需要，通过RP相上的制备色谱法纯化粗产物，随后如果需要将游离酸转化成任何所需的盐。

12. 发明授权

US06372725B1 Specific lipid conjugates to nucleoside diphosphates and their use as drugs 失效
标题翻译：特异性脂质偶联物与核苷二磷酸及其作为药物的用途
公开(公告)号：US06372725B1
公开(公告)日：2002-04-16
申请号：US09204497
申请日：1998-12-04
申请人： Harald Zilch , Dieter Herrmann
发明人： Harald Zilch , Dieter Herrmann
IPC分类号： A61K3170
CPC分类号： C07H19/10 , C07H19/207
摘要： The present invention concerns new phospholipid derivatives of nucleosides of the general formula (I) in which R1 represents a straight-chained or branched, saturated or unsaturated aliphatic residue with 9-14 carbon atoms which can optionally be substituted once or several times; R2 can represent a straight-chained or branched, saturated or unsaturated aliphatic residue with 8-12 carbon atoms which can optionally be substituted once or several times; m is 2 or 3; A can represent a methylene group or an oxygen; Nuc can be a nucleoside or a residue derived from a nucleoside derivative; and tautomers thereof and their physiologically tolerated salts of inorganic and organic acids and bases as well as pharmaceutical preparations containing these compounds.
摘要翻译：本发明涉及通式（I）的核苷的新型磷脂衍生物，其中R 1表示具有9-14个碳原子的直链或支链，饱和或不饱和的脂肪族残基，其可任选被取代一次或数次; R2可以表示具有8-12个碳原子的直链或支链，饱和或不饱和的脂肪族残基，其可任选被取代一次或数次; m为2或3; A可以表示亚甲基或氧; Nuc可以是衍生自核苷衍生物的核苷或残基; 及其互变异构体及其生理上耐受的无机和有机酸和碱的盐以及含有这些化合物的药物制剂。

13. 发明授权

US5955452A Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments 失效
标题翻译：共价脂质 - 膦酰 - 羧酸共轭物及其作为抗病毒药物的应用
公开(公告)号：US5955452A
公开(公告)日：1999-09-21
申请号：US077894
申请日：1998-08-26
申请人： Harald Zilch , Dieter Herrmann , Hans-George Opitz , Gerd Zimmermann , Edgar Voss
发明人： Harald Zilch , Dieter Herrmann , Hans-George Opitz , Gerd Zimmermann , Edgar Voss
IPC分类号： A61K31/00 , A61K31/66 , A61K31/662 , A61K47/48 , A61P31/00 , A61P31/12 , C07F9/40 , A01N57/00
CPC分类号： C07F9/4065 , C07F9/4006 , Y10S514/885
摘要： The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.
摘要翻译： PCT No.PCT / EP96 / 05648 Sec。 371日期：1998年8月26日 102（e）1998年8月26日PCT 1996年12月16日PCT公布。出版物WO97 / 22368 日期1996年6月26日本发明涉及通式I的膦酰基羧酸的新的脂质衍生物，其中符号的含义在说明书中阐明，其互变异构体及其生理上耐受的无机和有机碱的盐以及方法用于制备它们和含有这些化合物的药剂。

14. 发明授权

US6080734A Liponucleotides of seco-nucleosides, their production as well as their use as antiviral pharmaceutical agents 失效
标题翻译：仲核苷的脂质体，其生产以及它们作为抗病毒药剂的用途
公开(公告)号：US6080734A
公开(公告)日：2000-06-27
申请号：US209484
申请日：1998-12-11
申请人： Harald Zilch , Dieter Herrmann
发明人： Harald Zilch , Dieter Herrmann
IPC分类号： C07F9/6561 , A61K31/675
CPC分类号： C07F9/65616
摘要： The present invention is directed to new phospholipid derivatives of acyclovir and ganciclovir that link a lipid moiety, which represents a substituted C3 backbone, to acyclovir or ganciclovir via phosphate or thiophosphate. The compounds are particularly suitable for the therapy of viral infections.
摘要翻译：本发明涉及通过磷酸盐或硫代磷酸酯将代表取代的C3骨架的脂质部分与阿昔洛韦或更昔洛韦连接的阿昔洛韦和更昔洛韦的新型磷脂衍生物。该化合物特别适用于病毒感染的治疗。

15. 发明授权

US5543561A Acyclic amidine group-containing diphosphonic acid derivatives, processes for their preparation and medicaments containing these compounds 失效
标题翻译：含有无环脒基的二膦酸衍生物，其制备方法和含有这些化合物的药物
公开(公告)号：US5543561A
公开(公告)日：1996-08-06
申请号：US367325
申请日：1995-03-28
申请人： Harald Zilch , Frieder Bauss
发明人： Harald Zilch , Frieder Bauss
IPC分类号： A61K31/685 , A61K31/66 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/40
CPC分类号： C07F9/3873
摘要： Compounds of the formula I ##STR1## in which R.sup.1 signifies hydrogen, a straight-chained, branched, saturated or unsaturated alkyl radical with 1-9 carbon atoms possibly substituted by phenyl or a phenyl ring which is possibly substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 -alkoxy or halogen, R.sup.2 signifies hydrogen or C.sub.1 -C.sub.3 -alkyl, whereby the two radicals can be the same or different, R represents hydrogen or a straight-chained or branched alkyl radical with 1-4 carbon atoms, X signifies an alkylene chain with 1-6 carbon atoms which can be substituted one or more times by C.sub.1 -C.sub.3 -alkyl and can possibly be interrupted by oxygen, whereby 1 or 2 carbon stems of the alkylene chain can possibly be part of a cyclopentyl or cyclohexyl ring and Y signifies hydrogen, hydroxyl or amino group possibly substituted by alkyl groups with 1-6 carbon atoms, as well as their pharmacologically acceptable salts, processes for their preparation, as well as medicaments for the treatment of calcium metabolism disturbances.
摘要翻译： PCT No.PCT / EP93 / 01833 Sec。 371日期：1995年3月28日 102（e）1995年3月28日PCT PCT 1993年7月13日PCT公布。出版物WO94 / 02492 日期1994年2月3日，式I（I）的化合物，其中R 1表示可以被苯基或苯环取代的具有1-9个碳原子的氢，直链，支链，饱和或不饱和的烷基，可能被C 1 -C 3烷基，C 1 -C 3 - 烷氧基或卤素取代，R 2表示氢或C 1 -C 3 - 烷基，由此两个基团可以相同或不同，R表示氢或直链或支链烷基， -4个碳原子，X表示具有1-6个碳原子的亚烷基链，其可以被C 1 -C 3 - 烷基取代一次或多次，并且可能被氧中断，由此亚烷基链的1或2个碳原子可能是环戊基或环己基环的一部分，Y表示可能被具有1-6个碳原子的烷基取代的氢，羟基或氨基，以及它们的药理学上可接受的盐，它们的制备方法，以及用于治疗钙代谢骚动

16. 发明授权

US5158942A Process of using phospholipid derivatives to inhibit multiplication of the human immunodeficiency virus 失效
标题翻译：使用磷脂衍生物抑制人类免疫缺陷病毒的繁殖方法
公开(公告)号：US5158942A
公开(公告)日：1992-10-27
申请号：US572475
申请日：1990-08-23
申请人： Dieter Herrmann , Elmar Bosies , Harald Zilch , Edith Koch
发明人： Dieter Herrmann , Elmar Bosies , Harald Zilch , Edith Koch
IPC分类号： A61K31/685 , A61P31/12 , C07F9/09 , C07F9/10
CPC分类号： C07F9/10
摘要： The present invention is concerned with the use of compounds of the general formula: ##STR1## and of the pharmacologically acceptable salts thereof, as well as of the optical isomers thereof for the preparation of pharmaceutical compositions with antiviral action.The present invention also provides new phospholipid derivatives.
摘要翻译：本发明涉及以下通式的化合物及其药学上可接受的盐及其旋光异构体在制备具有抗病毒作用的药物组合物中的用途。本发明还提供了新的磷脂衍生物。

17. 发明授权

US07176011B2 Lipid cleavage enzyme 失效
标题翻译：脂质切割酶
公开(公告)号：US07176011B2
公开(公告)日：2007-02-13
申请号：US10211260
申请日：2002-08-05
申请人： Dieter Herrmann , Hans-George Opitz , Harald Zilch
发明人： Dieter Herrmann , Hans-George Opitz , Harald Zilch
IPC分类号： C12N9/20 , C12N9/18
CPC分类号： A61K31/7052 , C07H19/10 , C07H19/20 , C12N9/16 , C12Q1/44
摘要： A membranous enzyme not yet described in the state-of-the-art can be extracted from cellular membrane fractions of blood leukocytes or monocytes/macrophages. Also disclosed is the use of substrates of this enzyme to prepare medicaments that contain these substrates as pharmaceutical active substance. These medicaments are useful to direct pharmacologically active substances to target cells and to enrich target cells with said substances. Also disclosed are in-vitro research systems containing this enzyme used to detect other substrates of this enzyme.
摘要翻译：在现有技术中尚未描述的膜状酶可以从血液白细胞或单核细胞/巨噬细胞的细胞膜级分中提取。还公开了使用该酶的底物来制备含有这些底物作为药物活性物质的药物。这些药物可用于将药理学活性物质引导至靶细胞并用所述物质富集靶细胞。还公开了含有用于检测该酶的其它底物的酶的体外研究系统。

18. 发明授权

US06177469B1 Lipid alcohols as new immunosuppressive and antiviral drugs 失效
标题翻译：脂质醇作为新的免疫抑制和抗病毒药物
公开(公告)号：US06177469B1
公开(公告)日：2001-01-23
申请号：US09051088
申请日：1998-06-22
申请人： Harald Zilch , Dieter Herrmann , Hans-Georg Opitz
发明人： Harald Zilch , Dieter Herrmann , Hans-Georg Opitz
IPC分类号： A61K3700
CPC分类号： C07C323/25 , A61K31/08 , A61K31/10 , C07C317/18
摘要： The present invention concerns new immunosuppressive and antiviral pharmaceutical agents using lipid alcohols of the general formulae I and II in which R1 represents a straight-chained or branched, saturated or unsaturated alkyl chain with 1-30 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl, carboxy, C1-C6 alkylsulfinyl or C1-C6 alkylsulfonyl groups, R2 represents hydrogen, a straight-chained or branched, saturated or unsaturated alkyl chain with 1-20 carbon atoms which can optionally be substituted once or several times by halogen, C1-C6 alkoxy, C1-C6 alkylmercapto, C1-C6 alkoxycarbonyl or C1-C6 alkylsulfonyl groups, X represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group Y represents a valency dash, oxicarbonyl, carbonyloxy, amidocarbonyl, carbonylamido, oxygen, sulphur, a sulfinyl or sulfonyl group n represents an integer value from 1 to 5 inclusive as well as tautomers thereof and combinations containing these compounds with other active substances.
摘要翻译：本发明涉及新的免疫抑制和抗病毒药物，其使用通式I和IIin的脂质醇，其中R1表示具有1-30个碳原子的直链或支链，饱和或不饱和的烷基链，其可以任选被一次或多次取代一次或几次卤素，C 1 -C 6烷氧基，C 1 -C 6烷基巯基，C 1 -C 6烷氧基羰基，羧基，C 1 -C 6烷基亚磺酰基或C 1 -C 6烷基磺酰基，R 2表示氢，直链或支链，饱和或不饱和的具有1-20 碳原子，其可任选被卤素，C 1 -C 6烷氧基，C 1 -C 6烷基巯基，C 1 -C 6烷氧基羰基或C 1 -C 6烷基磺酰基取代一次或几次，X表示化合价，氧羰基，羰基氧基，酰氨基羰基，羰基酰氨基，氧，硫，亚磺酰基或磺酰基Y表示化合价，氧羰基，羰氧基，酰氨基羰基，羰基酰氨基，氧，硫，亚磺酰基或磺酰基，代表整数va 从1到5，以及其互变异构体和含有这些化合物与其它活性物质的组合。

19. 发明授权

US6136797A Phospholipid derivatives of phosphono-carboxylic acids, the production of said derivatives and the use of said derivatives as antiviral medicaments 失效
标题翻译：膦酰羧酸的磷脂衍生物，所述衍生物的制备以及所述衍生物作为抗病毒药物的用途
公开(公告)号：US6136797A
公开(公告)日：2000-10-24
申请号：US77891
申请日：1998-08-27
申请人： Harald Zilch , Dieter Herrmann , Hans-George Opitz , Gerd Zimmermann
发明人： Harald Zilch , Dieter Herrmann , Hans-George Opitz , Gerd Zimmermann
IPC分类号： A61K31/661 , A61K31/662 , A61P29/00 , A61P31/12 , A61P31/14 , A61P31/18 , A61P35/00 , A61P37/06 , C07F9/40 , A61K31/66
CPC分类号： C07F9/4065 , C07F9/4006 , C07F9/4075
摘要： The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.
摘要翻译： PCT No.PCT / EP96 / 05647 Sec。 371日期1998年8月27日第 102（e）1998年8月27日PCT PCT 1996年12月16日PCT公布。公开号WO97 / 22613 PCT 日期1996年6月26日本发明涉及通式I的膦酰基羧酸的新脂质衍生物，其中符号的含义在说明书中阐明，其互变异构体及其生理上耐受的无机或有机碱的酯和盐作为其制备方法和含有这些化合物的药剂。

20. 发明授权

US5366969A Amidine group containing monocycloheteracyclic or bicycloheterocyclic diphosphonic acid derivatives and medicaments containing these compounds 失效
标题翻译：含有单环杂环或双环杂环二膦酸衍生物的脒基和含有这些化合物的药物
公开(公告)号：US5366969A
公开(公告)日：1994-11-22
申请号：US829019
申请日：1992-03-06
申请人： Elmar Bosies , Harald Zilch
发明人： Elmar Bosies , Harald Zilch
IPC分类号： A61K31/675 , A61P3/00 , C07F9/6512 , C07F9/6561 , A61K31/66 , C07F9/38 , C07F9/40
CPC分类号： C07F9/65126 , C07F9/6561
摘要： Compounds of the formula I ##STR1## in which R can be hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.1 hydrogen, C.sub.1 -C.sub.6 -alkyl, aryl, aryl-C.sub.1 -C.sub.4 -alkyl, amino-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -dialkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.7 -alkenyl, R.sup.2 R.sup.1 or C.sub.2 -C.sub.7 -alkenyl, C.sub.1 -C.sub.6 -alkylmercapto, C.sub.1 -C.sub.6 -alkoxy, phenoxy-C.sub.1 -C.sub.4 -alkyl,amino, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, morpholino, thiomorpholino, pyrrolidino, piperidino, hexamethyleneimino, pyrasolino, imidazolino, n 0, 1 or 2 and R.sup.1 and R.sup.2, together with the carbon and the nitrogen atom to which they are attached, can form a heterocyclic five-, six- or seven-membered ring with 1-4 heteroatoms, whereby the heteroatoms can be the same or different and signify oxygen, nitrogen or sulphur and the annelated ring can possibly be substituted by one or more C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylmercapto groups, hydroxyl, amino, nitro, halogen or halomethyl, as well as their pharmacologically acceptable salts, processes for their preparation, as well as medicaments which contain these compounds for the treatment of calcium metabolism disturbances.
摘要翻译：其中R可以是氢或C 1 -C 4烷基，R 1氢，C 1 -C 6烷基，芳基，芳基-C 1 -C 4烷基，氨基-C 1 -C 6烷基，C 1 -C 4烷基， C 1-6 - 烷基氨基-C 1 -C 4 - 烷基，C 1 -C 6 - 二烷基氨基-C 1 -C 4烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷硫基-C 1 -C 4烷基，C 3 -C 7 - 烯基，R 2 R 1或C 2 -C 7 - 烯基，C 1 -C 6烷基巯基，C 1 -C 6 - 烷氧基，苯氧基-C 1 -C 4烷基，氨基，C 1 -C 4烷基氨基，二-C 1 -C 4烷基氨基，吗啉代，硫代吗啉代，吡咯烷子基，哌啶子基，六亚甲基亚氨基，吡咯烷基，咪唑啉，n 0,1或者2，并且R 1和R 2与它们所连接的碳原子和氮原子一起可以形成杂环的五，六或七元具有1-4个杂原子的环，其中杂原子可以相同或不同，表示氧，氮或硫，并且环状环可以被一个或多个C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基巯基，羟基，氨基，硝基，卤素或卤代甲基，以及它们的药理学上可接受的盐，其制备方法以及含有这些化合物用于治疗钙代谢紊乱的药物。

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