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1. 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。

2. 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。

3. 发明授权

US5002937A Diphosphonic acid compounds and use for calcium metabolism disorders 失效
标题翻译：二膦酸化合物和用于钙代谢紊乱
公开(公告)号：US5002937A
公开(公告)日：1991-03-26
申请号：US375747
申请日：1989-07-05
申请人： Elmar Bosies , Harald Zilch
发明人： Elmar Bosies , Harald Zilch
IPC分类号： A61K31/66 , A61K31/675 , A61P3/00 , A61P3/14 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/59 , C07F9/60 , C07F9/6506 , C07F9/6509 , C07F9/6533 , C07F9/6544
CPC分类号： C07F9/5721 , C07F9/386 , C07F9/3873 , C07F9/5722 , C07F9/5728 , C07F9/591 , C07F9/592 , C07F9/60 , C07F9/65062 , C07F9/650958 , C07F9/6533 , C07F9/6544
摘要： The present invention provides compounds of the formula: ##STR1## The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them useful in treatment and prophylaxis of disorders of calcium metabolism.
摘要翻译：本发明提供下式的化合物：（I）本发明还提供制备这些化合物的方法和含有它们的药物组合物，它们可用于治疗和预防钙代谢紊乱。

4. 发明授权

US5446139A Purine analog nucleoside and nucleotide compounds 失效
标题翻译：嘌呤类似物核苷和核苷酸化合物
公开(公告)号：US5446139A
公开(公告)日：1995-08-29
申请号：US809506
申请日：1992-02-21
申请人： Frank Seela , Werner Bourgeouis , Rainer Gumbiowski , Angelika Roling , Helmut Rosemeyer , Alfred Mertens , Harald Zilch , Bernhard Konig , Edith Koch
发明人： Frank Seela , Werner Bourgeouis , Rainer Gumbiowski , Angelika Roling , Helmut Rosemeyer , Alfred Mertens , Harald Zilch , Bernhard Konig , Edith Koch
IPC分类号： A61K31/40 , A61K31/435 , A61K31/505 , A61K31/53 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61P31/12 , C07D405/04 , C07D471/04 , C07D487/04 , C07F9/09 , C07F9/6561 , C07H19/04 , C12Q1/68 , C07H19/16
CPC分类号： C07H19/04
摘要： The invention concerns nucleoside derivatives of the formula I ##STR1## in which Ba signifies an indolyl (A), benzimidazolyl (B), pyrrolopyridinyl (C), imidazopyridinyl (D), triazolopyrimidinyl (E), imidazotriazinyl (F) or imidazopyrimidinyl (G) group substituted by R.sup.1, R.sup.2 and R.sup.3, in which R.sup.1, R.sup.2 and R.sup.3, which can be the same or different, signify hydrogen, halogen, a C.sub.1 -C.sub.7 -alkyl, C.sub.2 -C.sub.7 -alkenyl, hydroxy, mercapto, C.sub.1 -C.sub.7 -alkylthio, C.sub.1 -C.sub.7 -alkoxy, C.sub.2 -C.sub.7 -alkenyloxy, ar-C.sub.1 -C.sub.5 -alkyl, ar-C.sub.2 -C.sub.5 -alkenyl, ar-C.sub.1 -C.sub.5 -alkoxy, ar-C.sub.2 -C.sub.5 -alkenyloxy, aryloxy, nitro, amino-C.sub.1 -C.sub.7 -alkyl, C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, di-C.sub.1 -C.sub.7 -alkylamino-C.sub.1 -C.sub.7 -alkyl, amino, a substituted amino group --NMR.sup.4 or --N(R.sup.4).sub.2 or an imino group --N.dbd.CH--R.sup.4, and R.sup.4 has the meaning given in the description, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each signify hydrogen or one or two of the radicals R.sup.5, R.sup.6, R.sup.7 and R.sup.8 a hydroxyl, halogen, cyano, azido or a substituted amino group --NHR.sup.4 or --N(R.sup.4).sub.2 or R.sup.5 and R.sup.7 can together represent a further bond between C-2' and C-3' and Y represents hydrogen or a C.sub.1 -C.sub.7 -alkylcarbonyl, monophosphate, diphosphate or triphosphate group, whereby "aryl" signifies a phenyl or naphthyl group and "hetaryl" a furanyl, thienyl or pyridyl group, as well as their possible anomers, N.sup.7 - or N.sup.9 -regioisomers (purine nomenclature), tautomers and salts.
摘要翻译： PCT No.PCT / EP90 / 00650 Sec。一九九二年二月二十一日 102（e）日期1992年2月21日PCT提交1990年4月23日PCT公布。第WO91 / 01325号公报 1991年2月7日，本发明涉及式Ⅰ（I）的核苷衍生物，其中Ba表示吲哚基（A），苯并咪唑基（B），吡咯并吡啶基（C），咪唑并吡啶基（D），三唑并嘧啶基（E ），被R1，R2和R3取代的咪唑并吡嗪基（F）或咪唑并嘧啶基（G）基团，其中可以相同或不同的R 1，R 2和R 3表示氢，卤素，C 1 -C 7 - 烷基， C7-烯基，羟基，巯基，C1-C7-烷硫基，C1-C7-烷氧基，C2-C7-烯氧基，芳基-C1-C5-烷基，ar-C2-C5-烯基，ar-C1-C5-烷氧基，芳基氧基，硝基，氨基-C 1 -C 7 - 烷基，C 1 -C 7 - 烷基氨基-C 1 -C 7 - 烷基，二-C 1 -C 7 - 烷基氨基-C 1 -C 7 - 烷基，氨基，取代的氨基-NMR4或-N（R4）2或亚氨基-N = CH-R4，R4具有说明书中给出的含义，R5，R6，R7和R8各自表示氢或一个或两个基团R 5 ，R6，R7和R8是羟基，卤素，氰基，叠氮基或取代的氨基-NHR4或-N（R4）2或R5和R7可以一起代表另一个b C-2'和C-3'之间，Y表示氢或C1-C7-烷基羰基，一磷酸，二磷酸或三磷酸基，其中“芳基”表示苯基或萘基，“杂芳基”是呋喃基，噻吩基或吡啶基组，以及它们可能的端基异构体，N7-或N9-区域异构体（嘌呤命名法），互变异构体和盐。

5. 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。

6. 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。

7. 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。

8. 发明授权

US5756711A Phospholipid derivatives of nucleosides and their use as anti-viral medicaments 失效
标题翻译：核苷的磷脂衍生物及其作为抗病毒药物的用途
公开(公告)号：US5756711A
公开(公告)日：1998-05-26
申请号：US661038
申请日：1996-06-10
申请人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
发明人： Harald Zilch , Herbert Leinert , Alfred Mertens , Dieter Herrmann
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/10 , C07H19/20 , C12P19/28 , C12P19/30
CPC分类号： C07H19/10 , C07H19/20 , C12P19/28
摘要： Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 represent a possibly substituted C.sub.8 -C.sub.15 -alkyl chain, n the number 0, 1 or 2 and A the residue of a nucleoside, processes for their preparation, as well as antiviral medicaments which contain these compounds.
摘要翻译：其中R1和R2代表可能被取代的C 8 -C 15烷基链，数字0,1或2，A是核苷的残基，其制备方法以及抗病毒药物的式I的化合物其中含有这些化合物。

9. 发明授权

US6025343A Lipid esters of nucleoside monophosphates and their use as immunosuppressive drugs 失效
标题翻译：核苷单磷酸酯的脂质酯及其作为免疫抑制药物的用途
公开(公告)号：US6025343A
公开(公告)日：2000-02-15
申请号：US753633
申请日：1996-11-27
申请人： Dieter Herrmann , Hans-Georg Opitz , Harald Zilch , Alfred Mertens
发明人： Dieter Herrmann , Hans-Georg Opitz , Harald Zilch , Alfred Mertens
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P35/00 , A61P37/06 , C07H19/04 , C07H19/10 , C07H19/20 , C07H19/207 , A01N43/04
CPC分类号： C07H19/10 , C07H19/20 , Y10S514/885 , Y10S514/908
摘要： The present invention is directed to new nucleoside monophosphate derivatives of lipid ester residues of general formula (I) ##STR1## wherein R.sup.1 represents an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.2 represents hydrogen, an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, hydroxy, azido, amino, cyano, or halogen;X represents a valence dash, oxygen, sulfur, a sulfinyl or sulfonyl group;Y represents a valence dash, an oxygen or sulfur atom;B represents a purine and/or pyrimidine base;with the proviso that at least one of the residues R.sup.3 or R.sup.5 is hydrogen;to their tautomers and their physiologically acceptable salts of inorganic and organic acids and/or bases, as well as to processes for their preparation, and to drugs containing said compounds.
摘要翻译：本发明涉及通式（I）的脂质酯残基的新的核苷单磷酸酯衍生物，其中R 1表示任选取代的具有1-20个碳原子的烷基链; R 2表示氢，任选取代的具有1-20个碳原子的烷基链; R3，R4和R5代表氢，羟基，叠氮基，氨基，氰基或卤素; X表示化合价，氧，硫，亚磺酰基或磺酰基; Y表示化合价，氧或硫原子; B代表嘌呤和/或嘧啶碱基; 条件是残基R3或R5中的至少一个是氢; 其互变异构体及其生理上可接受的无机酸和有机酸和/或碱的盐，以及其制备方法，以及含有所述化合物的药物。

10. 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。

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