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    9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    4.
    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
    5.
    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。

    Cyclodextrin clathrates of carbacyclin derivatives and their use as medicinal agents
    7.
    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。

    Treatment of cardiomyopathy and of endothelial dysfunction
    8.
    发明申请
    Treatment of cardiomyopathy and of endothelial dysfunction 审中-公开
    治疗心肌病和内皮功能障碍

    公开(公告)号：US20050276785A1

    公开(公告)日：2005-12-15

    申请号：US11147492

    申请日：2005-06-07

    申请人： Georg Groetzbach ,  Joachim-Friedrich Kapp ,  Uwe Kuehl ,  Heinz-Peter Schultheiss ,  Olaf Sowade ,  Claus-Steffen Stuerzebecher

    发明人： Georg Groetzbach ,  Joachim-Friedrich Kapp ,  Uwe Kuehl ,  Heinz-Peter Schultheiss ,  Olaf Sowade ,  Claus-Steffen Stuerzebecher

    IPC分类号： A61K38/00 ,  A61K38/21

    CPC分类号： A61K38/215

    摘要： The present invention relates to pharmaceutical compositions comprising a therapeutically effective dose of an isolated interferon (IFN) or IFN mutein for treatment of cardiomyopathy and of endothelial dysfunction, and to methods of treating cardiomyopathy and methods of treating endothelial dysfunction using such pharmaceutical compositions. Particularly, the pharmaceutical compositions of the present invention comprise a therapeutically effective dose of an isolated, human IFN, or IFN mutein that is a variant of an isolated human IFN, e.g., an isolated, native, human IFNβ or an isolated, native, human IFNα.

    摘要翻译： 本发明涉及包含治疗有效剂量的用于治疗心肌病和内皮功能障碍的分离的干扰素（IFN）或IFN突变蛋白的药物组合物，以及使用这种药物组合物治疗心肌病的方法和治疗内皮功能障碍的方法。 特别地，本发明的药物组合物包含治疗有效剂量的分离的人IFN或IFN突变蛋白，其是分离的人IFN的变体，例如分离的天然人IFNBeta或分离的天然人 IFNalpha。

    Carbacyclins, processes for their preparation, and their use as medicinal agents
    9.
    发明授权
    Carbacyclins, processes for their preparation, and their use as medicinal agents 失效

    公开(公告)号：US5162353A

    公开(公告)日：1992-11-10

    申请号：US570446

    申请日：1990-08-21

    申请人： Helmut Vorbrueggen ,  Bob Nieuweboer ,  Claus-Steffen Stuerzebecher

    发明人： Helmut Vorbrueggen ,  Bob Nieuweboer ,  Claus-Steffen Stuerzebecher

    IPC分类号： C07C59/62 ,  C07C405/00

    CPC分类号： C07C59/62 ,  C07C405/0083

    摘要： The invention relates to carbacyclin derivatives with general formula I: ##STR1## in which Y.sub.1 stands for the radical --CH.sub.2 --X--(CH.sub.2).sub.n --R.sub.1 or the radical ##STR2## n, 1 or 3, R.sub.1, the radical ##STR3## the radical ##STR4## R.sub.9 stands for the radical --(CH.sub.2).sub.m --R.sub.6 or the radical --(CH.sub.2).sub.m-o --[Z.sub.1 --(CH.sub.2).sub.m-p ].sub.x --[Z.sub.2 --(CH.sub.2).sub.m-q ].sub.y --R.sub.6,m=2-20,o, p, and q are less than or equal to 19,x, y=0, 1 or 2,Z.sub.1 stands for a cis--CH.dbd.CH group, a trans--CH.dbd.CH group of a --C.dbd.C group, and each of these groups must be separated at least by a methylene group from the C-9 carbon atom of the carbacyclin bicyclic compound,Z.sub.2 stands for oxygen, sulfur, an NH or an N methyl group,R.sub.6 stands for amino, methylamino, hydroxy, carboxy or mercapto,X an oxygen atom or a methylene group,Y.sub.2 hydrogen or fluorine,A a --CH.sub.2 --CH.sub.2, trans--CH.dbd.CH or --C.dbd.C group,W a free or functionally modified hydroxy methylene group,D a straight-chain, saturated alkylene group with 1-5 C atoms,E stands for a direct bond, a --C.tbd.C group or a --CH.dbd.CR.sub.7 group,R.sub.4 stands for an alkyl group with 1-10 C atoms,R.sub.5 stands for a free or functionally modified hydroxy group.The invention also relates to carbacyclin derivatives of general Formula I' ##STR5## wherein n is 1 or 3R.sub.1 is the residue ##STR6## the residue ##STR7## the residue COOR.sub.2 wherein R.sub.2 can mean hydrogen or alkyl of 1-10 carbon atoms optionally substituted by halogen, phenyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -dialkylamino; cycloalkyl, aryl, or a heterocyclic residue, or is the residue CONHR.sub.3 with R.sub.3 meaning hydrogen or an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms,R.sub.9 is an alkyl group of 1-10 carbon atoms or the group --C.tbd.C--(CH.sub.2).sub.m --R.sub.6 whereinm is 1 to 16 andR.sub.6 is hydrogen, hydroxy, amino or trimethylsilyl,X is an oxygen atom or, if R.sub.9 means an alkyl group of 5-10 carbon atoms, a methylene group, andY is hydrogen or fluorine, to processes for their preparation, and to medicinal agents containing these compounds.

    Novel carbacyclins, processes for their production and their use as medicinal agents
    10.
    发明授权
    Novel carbacyclins, processes for their production and their use as medicinal agents 失效
    新型碳霉素，其生产工艺及其作为药剂的使用

    公开(公告)号：US4827017A

    公开(公告)日：1989-05-02

    申请号：US21102

    申请日：1987-03-03

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Ekkehard Schillinger ,  Claus-Steffen Stuerzebecher

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Ekkehard Schillinger ,  Claus-Steffen Stuerzebecher

    IPC分类号： C07D309/12 ,  A61K31/557 ,  A61P1/04 ,  A61P7/02 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C45/00 ,  C07C49/835 ,  C07C51/00 ,  C07C65/19 ,  C07C67/00 ,  C07C69/76 ,  C07C69/773 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/0083

    摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2 wherein R.sub.2 is hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, ##STR2## or a heterocyclic residue, or R.sub.1 is R.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.6 -C.sub.10 -aryl, C.sub.7 -C.sub.14 -aralkyl or a heterocyclic residue,A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated alkylene group of 1-10 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-10 carbon atoms, each of which can optionally by substituted by fluorine atoms,n is the number 1, 2 or 3,E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and one is hydrogen and the other alkyl of 1-5 carbon atoms, or one is hydrogen and the other is halogen, orE can also be --CH.sub.2 CH.sub.2 -- when R.sub.1 is R.sub.3,R.sub.4 is C.sub.1-10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, optionally substituted C.sub.6 -C.sub.10 -aryl or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group and, when R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases;are useful as medicinal agents.

    摘要翻译： 式I的卡巴环素衍生物其中R 1是OR 2，其中R 2是氢，C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，或者杂环残基，或者R 1是R 3 其中R 3是C 1 -C 10 - 烷基，C 3 -C 10 - 环烷基，C 6 -C 10 - 芳基，C 7 -C 14 - 芳烷基或杂环残基，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C - ，W是游离或官能改性的羟基亚甲基或游离的或功能上被修饰的“IMAGE”，其中OH基可以是α或β-位，D是直链，饱和的亚烷基 1-10个碳原子，或2-10个碳原子的支链，饱和或直链或支链不饱和的亚烷基，其各自可任选被氟原子取代，n为数1,2或3， E是-C 3位C或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，一个是氢，1-5个碳原子的另一个烷基，或一个是氢，另一个是卤素，或者也可以是 当R 1为R 3，R 4为C 1-10时为-CH 2 CH 2 - 烷基，C 3 -C 10 - 环烷基，任选取代的C 6 -C 10 - 芳基或杂环基，R 5是游离或官能改性的羟基，并且当R 2是氢时，其与生理上相容的碱的盐; 作为药剂有用。