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11. 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。

12. 发明授权

US5135949A Pharmaceutical compositions containing phenylamides 失效
标题翻译：含有苯甲酸的药物组合物
公开(公告)号：US5135949A
公开(公告)日：1992-08-04
申请号：US402185
申请日：1989-09-05
申请人： Wolfgang von der Saal , Alfred Mertens , Harald Zilch , Erwin Boehm
发明人： Wolfgang von der Saal , Alfred Mertens , Harald Zilch , Erwin Boehm
IPC分类号： A61K31/165 , A61K31/275 , A61K31/357 , A61K31/36 , A61P7/00 , A61P9/00 , A61P9/12 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/76 , C07C233/80 , C07C233/81 , C07C235/22 , C07C235/38 , C07C235/56 , C07C237/22 , C07C237/30 , C07C237/40 , C07C255/40 , C07C255/41 , C07C255/42 , C07C255/46 , C07C255/60 , C07C309/66 , C07C311/05 , C07C311/06 , C07C311/09 , C07C317/40 , C07C317/44 , C07C323/42 , C07C323/44 , C07C323/62 , C07D213/65 , C07D317/66
CPC分类号： C07C309/66 , A61K31/165 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C235/22 , C07C235/38 , C07C235/56 , C07C237/22 , C07C237/40 , C07C255/41 , C07C255/46 , C07C255/60 , C07C323/42 , C07D213/65 , C07D317/66 , C07C2101/14 , Y10S514/822
摘要： Pharmaceutical compositions for inhibiting the aggregation of erthyrocytes or thrombocytes which include phenylamides which conform to the formula: ##STR1## with R.sub.1-6, X, A and B being as defined. Processes for the preparation of novel phenylamides coming within the above formula are also discussed.
摘要翻译：用于抑制红细胞或血栓细胞聚集的药物组合物，其包括符合下式的苯酰胺：R1-6，X，A和B的定义如下。还讨论了在上述配方中制备新型苯酰胺的方法。

13. 发明授权

US4985448A Ureidoindoles, pharmaceutical compositions and methods for erythrocyte and thrombocyte aggregation inhibition 失效
标题翻译：脲基吲哚，用于红细胞和血小板聚集抑制的药物组合物和方法
公开(公告)号：US4985448A
公开(公告)日：1991-01-15
申请号：US307417
申请日：1989-02-06
申请人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
发明人： Harald Zilch , Alfred Mertens , Wolfgang Von Der Saal , Erwin Boehm , Klaus Strein
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61P7/02 , C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D209/34 , C07D209/54 , C07D215/38 , C07D215/54 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Lactam compounds of the formula ##STR1## in which: R is hydrogen, alkyl or cycloalkyl;R.sup.1 is hydrogen, alkyl, alkenyl or cycloalkyl;R.sup.2 is alkyl, alkenyl, cyano or a carbonyl substituted hydroxyl, alkyl, alkoxy, amino, alkylamino or hydrazino; orR.sup.1 and R.sup.2 together represent alkylidene cycloalkylidene; orR.sup.1, R.sup.2 and the adjacent carbon atom form a spirocyclic ring;n is 0 or 1;A is a --Co--NH--, --NH--CO--NH-- or --O--CO--NH--;X is a valency bond, alkylene or alkenylene; andR.sup.3 is optionally substituted phenyl, pyridyl, methylenedioxyphenyl or a five-membered heterocycle; or when X is a valency bond, R.sup.3 can also be an optionally substituted alkyl or alkino group, or cycloalkyl. The compounds are useful for the inhibition of erythrocyte and thrombocyte aggregation.
摘要翻译：式（I）的内酰胺化合物，其中：R为氢，烷基或环烷基; R1是氢，烷基，烯基或环烷基; R2是烷基，烯基，氰基或羰基取代的羟基，烷基，烷氧基，氨基，烷基氨基或肼基; 或者R1和R2一起表示亚烷基亚环烷基; 或R 1，R 2和相邻碳原子形成螺环; n为0或1; A是-Co-NH-，-NH-CO-NH-或-O-CO-NH-; X是价键，亚烷基或亚烯基; 并且R 3是任选取代的苯基，吡啶基，亚甲二氧基苯基或五元杂环; 或当X是价键时，R 3也可以是任选取代的烷基或烷基或环烷基。该化合物可用于抑制红细胞和血小板聚集。

14. 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。

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

US5414088A 2-bicyclobenzimidazoles, processes for their preparation and medicaments containing these compounds 失效
标题翻译： 2-二环苯并咪唑，它们的制备方法和含有这些化合物的药物
公开(公告)号：US5414088A
公开(公告)日：1995-05-09
申请号：US847060
申请日：1992-04-14
申请人： Wolfgang Von Der Saal , Harald Zilch , Erwin Bohm
发明人： Wolfgang Von Der Saal , Harald Zilch , Erwin Bohm
IPC分类号： A61K31/415 , A61K31/47 , A61P7/02 , C07D401/04 , C07D403/04 , C07D487/04 , C07D215/227 , C07D235/18
CPC分类号： C07D401/04 , C07D403/04 , C07D487/04
摘要： The invention concerns compounds of formula I ##STR1## where R.sup.1 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl, R.sup.2 is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, cyano, carboxy [carbonyl substituted by hydroxyl], C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or hydrazino or R.sup.1 and R.sup.2 together are C.sub.2 -C.sub.6 -alkylidene or C.sub.3 -C.sub.6 -cycloalkylidene or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, form a C.sub.3 -C.sub.7 -spirocycle, n is 0 or 1, R.sup.3 is hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, C.sub.3 -C.sub.7 -cycloalkyl, benzyl, carboxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkyloxycarbonyl-C.sub.1 -C.sub.6 -alkyl or di-C.sub.1 -C.sub.6 -alkyloxophosphinyl-C.sub.1 -C.sub.6 -alkyl and R.sup.4 -R.sup. 6 are as in the specification. These compounds of formula I serve for the preparation of medicaments to inhibit erythrocyte and thrombocyte aggregation. Therefore, these compounds are useful for the treatment of diseases where these aggregations occur such as arterial occlusive or ischaemic conditions, venous insufficiency or diabetes mellitus.
摘要翻译： PCT No.PCT / EP90 / 01663 Sec。 371日期：1992年4月14日 102（e）日期1992年4月14日PCT 1990年9月4日PCT PCT。出版物WO91 / 04974 1991年4月18日，本发明涉及式I化合物（Ⅰ）其中R1是氢，C1-C6-烷基，C2-C6-烯基或C3-C7-环烷基，R2是C1-C6-烷基，C 2 -C 6 - 烯基，氰基，羧基[被羟基取代的羰基]，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6烷基氨基或肼基或R 1和R 2 一起是C 2 -C 6亚烷基或C 3 -C 6亚环烷基或R 1和R 2与它们连接的碳原子一起形成C 3 -C 7 - 螺环，n是0或1，R 3是氢，C 1 -C 8 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 7 - 环烷基，苄基，羧基-C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基羰基-C 1 -C 6烷基或二-C 1 -C 6烷氧基氧膦 -C 1 -C 6烷基和R 4 -R 6如说明书中所述。这些式I化合物用于制备抑制红细胞和血小板聚集的药物。因此，这些化合物可用于治疗发生这些聚集的疾病，例如动脉闭塞或缺血性疾病，静脉功能不全或糖尿病。

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

US5563257A Phospholipid derivatives of nucleosides 失效
标题翻译：核苷的磷脂衍生物
公开(公告)号：US5563257A
公开(公告)日：1996-10-08
申请号：US438240
申请日：1995-05-09
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： C07H19/10 , C07H19/20 , C12P19/28
CPC分类号： C07H19/10 , C07H19/20 , C12P19/28
摘要： Liponucleotides containing an ether linkage in the 2-position and a thioether, sulfoxide, or sulfone linkage in the 3-position. The nucleoside component of said liponucleotide is AZT or 3'-deoxy-3'-fluorothymidine. These compounds exhibit antiviral activity.
摘要翻译：在2位上含有醚键的脂核苷酸和3位的硫醚，亚砜或砜键。所述脂核苷酸的核苷组分是AZT或3'-脱氧-3'-氟胸苷。这些化合物表现出抗病毒活性。

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