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23 条记录 (耗时 0.021 秒)

    Lipid esters of nucleoside monophosphates and their use as immunosuppressive drugs
    3.
    发明授权
    Lipid esters of nucleoside monophosphates and their use as immunosuppressive drugs 失效
    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。

    Liponucleotides of seco-nucleosides, their production as well as their use as antiviral pharmaceutical agents
    4.
    发明授权
    Liponucleotides of seco-nucleosides, their production as well as their use as antiviral pharmaceutical agents 失效
    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。

    Specific lipid conjugates to nucleoside diphosphates and their use as drugs
    5.
    发明授权
    Specific lipid conjugates to nucleoside diphosphates and their use as drugs 失效
    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。

    Lipid cleavage enzyme
    8.
    发明授权
    Lipid cleavage enzyme 失效
    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。

    Lipid alcohols as new immunosuppressive and antiviral drugs
    9.
    发明授权
    Lipid alcohols as new immunosuppressive and antiviral drugs 失效
    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。