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    Cyclodextrin clathrates of carbacyclin derivatives and their use as medicinal agents
    1.
    发明授权
    Cyclodextrin clathrates of carbacyclin derivatives and their use as medicinal agents 失效
    碳环糊精衍生物的环糊精包合物及其作为药物的用途

    公开(公告)号：US4886788A

    公开(公告)日：1989-12-12

    申请号：US23506

    申请日：1987-03-09

    申请人： Werner Skuballa ,  Helmut Vorbrueggen ,  Helmut Dahl ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    发明人： Werner Skuballa ,  Helmut Vorbrueggen ,  Helmut Dahl ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    IPC分类号： C07C59/46 ,  A61K31/557 ,  A61K47/48 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C51/00 ,  C07C51/347 ,  C07C59/125 ,  C07C59/62 ,  C07C67/00 ,  C07C69/732 ,  C07C405/00 ,  C07D521/00 ,  C08B37/00 ,  C08B37/16

    CPC分类号： B82Y5/00 ,  A61K47/48969 ,  C07C405/0083 ,  C08B37/0015

    摘要： Cyclodextrin clathrates of carbacyclin analogs of general Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkenyl of up to 10 carbon atoms,A is a --CH.sub.2 CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C-- group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position,D is ##STR3## alkylene, or unsaturated alkylene each of which can optionally be substituted by fluorine atoms,m is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group, or --CR.sub.4 .dbd.CR.sub.5 -- group, wherein R.sub.4 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen, halogen, or an alkyl group of 1-5 carbon atoms,R.sub.2 is alkyl or alkenyl of up to 10 carbon atoms, cycloalkyl of 3-10 carbon atoms or an optionally substituted aryl group of 6-10 carbon atoms, or a heterocyclic group, andR.sub.3 is a free or functionally modified hydroxy group,n is 1, 2, 3, 4 or 5, andX is --CH.sub.2 -- or oxygenas valuable crystalline pharmaceuticals.

    摘要翻译： 通式Ⅰ的碳霉酸类似物的环糊精包合物其中R 1是氢，至多10个碳原子的烷基或链烯基，A是-CH 2 CH 2 - ，反式-CH = CH-或-C 3位C- 基团，W是游离或官能改性的羟基亚甲基基团或游离或官能改性的“IMAGE”，其中OH基团可以在α或β-位，D是亚烷基，或不饱和亚烷基，其各自可以 任选被氟原子取代，m为1,2或3，E为直接键，-C 3位C基或-CR 4 = CR 5 - 基，其中R 4为氢或1-5碳烷基 原子，R5为氢或1-5个碳原子的烷基，R5为氢，卤素或1-5个碳原子的烷基，R2为至多10个碳原子的烷基或烯基，环烷基为3 -10个碳原子或任选取代的6-10个碳原子的芳基或杂环基，R3是游离或官能改性的羟基，n是1,2,3,4或5，X是-CH 2 - 或氧作为有价值的结晶药物。

    9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    2.
    发明授权
    9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
    9-卤素 - （Z） - 前列腺素衍生物，其制备方法及其作为药剂的用途

    公开(公告)号：US06225347B1

    公开(公告)日：2001-05-01

    申请号：US08313667

    申请日：1994-09-27

    申请人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    发明人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    IPC分类号： C07C40500

    CPC分类号： C07C405/0016 ,  C07C405/00 ,  C07C405/0025

    摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a —CR6═CR7 group, and R6 and R7 are different and mean a hydrogen atom, a chlorine atom or a C1-C4 alkyl group, R4 resents a free or functionally modified hydroxy group, R5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group, and if R2 means a hydrogen atom, its salts with physiologically compatible bases or its cyclodextrin chlathrates, process for their production and their pharmaceutical use.

    摘要翻译： 本发明涉及式Iin的9-卤素 - （Z）前列腺衍生物，其中Z代表基团.Hal表示α或β位上的氯或氟原子，R 1表示R 2表示氢原子，烷基，环烷基，芳基或 杂环基或R 1表示基团，其中R 3表示酸基或基团R 2且A表示-CH 2 -CH 2 - ，反式-CH = CH或-C = C基团，W表示游离或功能修饰基团， OH基可以是α或β位，D和E一起代表直接键或D表示具有1-10个C原子的直链亚烷基，具有2-10个C原子的支链亚烷基或环状亚烷基 具有3-10个C原子的基团，其任选地可以被氟原子取代，E表示氧或硫原子，直接键合，C = C键或-CR 6 = CR 7基团，并且R 6和R 7不同， 一个氢原子，一个氯原子或一个C 1 -C 4烷基，R 4是一个游离的 或官能改性的羟基，R 5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱或其环糊精的盐 chlathrates，生产过程及其药物用途。

    9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    3.
    发明授权
    9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
    9-卤素 - （Z）前列腺素衍生物，其制备方法及其作为药剂的用途

    公开(公告)号：US5891910A

    公开(公告)日：1999-04-06

    申请号：US467888

    申请日：1995-06-06

    申请人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    发明人： Bernd Buchmann ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Bernd Raduechel ,  Olaf Loge ,  Walter Elger ,  Claus-Steffen Stuerzebecher ,  Karl-Heinz Thierauch

    IPC分类号： C07C405/00 ,  A61K31/557

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0025

    摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I ##STR1## in which ##STR2## Z represents the radicals Hal represents a chlorine or fluorine atom,R.sub.1 represents ##STR3## A represents a --CH.sub.2 --CH.sub.2 --, a trans--CH=CH or --C.ident.C, W represents a free or a functionally modified ##STR4## group, D and E together represent a direct bond orD represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, andE represents an oxygen or sulfur atom, a direct bond, a C.ident.C bond or a --CR.sub.6 =CR.sub.7 group, and R.sub.6 and R.sub.7 are different and mean a hydrogen atom, a chlorine atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.4 represents a free or functionally modified hydroxy,R.sub.5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group.

    摘要翻译： 本发明涉及式I的9-卤代 - （Z）前列腺衍生物，其中，Z表示基团，Hal表示氯或氟原子，R1表示A表示 -CH 2 -CH 2 - ，反式-CH = CH或-C = C，W表示游离或官能改性的基团，D和E一起表示直接键或D表示直链亚烷基，其中1 -10个C原子，具有2-10个碳原子的支链亚烷基或具有3-10个C原子的环状亚烷基，其任选可以被氟原子取代，E表示氧或硫原子，直接键 ，C = C键或-CR6 = CR7基，R6和R7不同，表示氢原子，氯原子或C1-C4烷基，R4表示游离或官能改性的羟基，R5表示氢 原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基。

    6-oxoprostaglandin E derivatives, process for their production and their pharmaceutical use
    5.
    发明授权
    6-oxoprostaglandin E derivatives, process for their production and their pharmaceutical use 失效
    6-氧代前列腺素E衍生物，其制备方法及其药物用途

    公开(公告)号：US5023273A

    公开(公告)日：1991-06-11

    申请号：US276502

    申请日：1988-11-23

    申请人： Ulrich Klar ,  Werner Skuballa ,  Helmut Vorbruggen ,  Claus-Steffen Sturzebecher ,  Karl-Heinz Thierauch ,  Ekkehard Schillinger

    发明人： Ulrich Klar ,  Werner Skuballa ,  Helmut Vorbruggen ,  Claus-Steffen Sturzebecher ,  Karl-Heinz Thierauch ,  Ekkehard Schillinger

    IPC分类号： C07D213/00 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/50 ,  C07D213/63 ,  C07D309/00 ,  C07D309/12 ,  C07D521/00

    CPC分类号： C07C405/00

    摘要： The invention relates to 6-oxo-prostaglandin E.sub.1 derivatives of formula I, ##STR1## in which R.sup.1 means the radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom, C.sub.1 -C.sub.10 alkyl, a C.sub.5 -C.sub.6 cycloalkyl or a C.sub.6 -C.sub.10 aryl group or a heterocyclic radical, or the radical CONHSO.sub.2 R.sup.5 as C.sub.1-10 alkyl, C.sub.5-6 cycloalkyl or C.sub.6-10 aryl,A means an E-configuration CH.dbd.CH or a --C.dbd.C group,W means a free or functionally modified hydroxymethylene group or a free or functionally modified group, and the OH group in each case can be in the alpha or beta position,D means a straight-chain or branched-chain alkylene group with 1-5 C atoms,E means a --C.dbd.C group or a C.sub.2 -C.sub.4 alkenylene group,R.sup.3 means C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl or an optionally substituted C.sub.6 -C.sub.10 aryl group or a heterocyclic group,R.sup.4 means a free or functionally modified hydroxy group, and if R.sup.2 means a hydrogen atom, its salts with physiologically compatible bases as well as alpha, beta or gamma cyclodextrin clathrates of the compounds of formula I, process for their production and their pharmaceutical use.

    摘要翻译： PCT No.PCT / DE88 / 00151 Sec。 371日期1988年11月23日第 102（e）日期1988年11月23日PCT提交1988年3月11日PCT公布。 出版物WO88 / 07037 本发明涉及式I的6-氧代 - 前列腺素E1衍生物，其中R1表示具有R2的基团COOR2，其表示氢原子，C1-C10烷基，C5- C6环烷基或C6-C10芳基或杂环基，或基团CONHSO2 R5为C1-10烷基，C5-6环烷基或C6-10芳基，A表示E构型CH = CH或-C = C 基团，W表示游离或官能改性的羟基亚甲基或游离或官能改性的基团，并且每种情况下OH基团可以在α或β位置，D表示具有1-位的直链或支链亚烷基， 5 C原子，E表示-C = C基或C 2 -C 4亚烯基，R 3表示C 1 -C 10烷基，C 3 -C 10环烷基或任选取代的C 6 -C 10芳基或杂环基，R 4表示游离或 官能改性的羟基，并且如果R 2表示氢原子，则其与生理相容性碱的盐以及化合物的α，β或γ环糊精包合物 的式I，其生产过程及其药物用途。