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    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。

    Novel carbacyclins, processes for their production and their use as medicinal agents
    6.
    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。

    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents
    8.
    发明授权
    9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
    9-氟前列腺素衍生物，其制备和用作药物

    公开(公告)号：US4789685A

    公开(公告)日：1988-12-06

    申请号：US4733

    申请日：1987-01-20

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Norbert Schwarz ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Michael-Harold Town

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07C405/0016 ,  C07C405/0041

    摘要： 9-fluoroprostane derivatives of Formula I ##STR1## wherein R.sub.1 is CH.sub.2 OH or ##STR2## wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or R.sub.1 is the residue ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 and A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,D and E jointly are a direct bond orD is straight-chain or branched alkylene or alkenylene of 1-10 carbon atoms which can optionally be substituted by fluorine atoms, and E is oxygen or sulfur, a direct bond, --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 differ from each other and each is hydrogen, chlorine, or alkyl,R.sub.4 is a free or functionally modified hydroxy group, andR.sub.5 is hydrogen, an optionally substituted aliphatic group, e.g., alkyl or halosubstituted alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group, and, when R.sub.2 is H, the physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g., as luteolytics or abortifacients.

    摘要翻译： 其中R 1是CH 2 OH或其中R 2是氢，烷基，环烷基，芳基或杂环残基的式I的α-氟仿烷基衍生物。 或R1是残基，其中R3是酸残基或R2和A是-CH2-CH2-或顺式-CH = CH-，B是-CH2-CH2-，反式-CH = CH-或-C3BOND C，W是游离的或官能改性的羟基亚甲基，其中OH基可以是α或β位，D和E共同是直接键，或D是1-10的直链或支链亚烷基或亚链烯基 可以任选被氟原子取代的碳原子，E是氧或硫，直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自是氢，氯或烷基 R4是游离的或官能改性的羟基，R5是氢，任意取代的脂族基团，例如烷基或卤代取代的烷基，环烷基，任选被取代的芳基或杂环基，当R2是H时，生理上相容的盐 具有有价值的药理学性质，例如作为骨质疏松症或流产者。

    Pharmaceutically active 9-chloroprostaglandins
    9.
    发明授权
    Pharmaceutically active 9-chloroprostaglandins 失效
    药用活性9-氯前列腺素

    公开(公告)号：US5204371A

    公开(公告)日：1993-04-20

    申请号：US792574

    申请日：1991-11-15

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Ekkehard Schillinger

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Walter Elger ,  Olaf Loge ,  Ekkehard Schillinger

    IPC分类号： C07C405/00

    CPC分类号： C07C405/0041 ,  C07C405/00

    摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.-or .beta.-position,A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--,B is --CH.sub.2 --CH.sub.2,--, trans--CH.dbd.CH--, or --CH.tbd.C--, W is hydroxymethylene orD and E together represent a direct bond orD is a straight-chain or branched alkylene group of 1-10 carbon atoms, optionally substituted by fluorine, andE is oxygen or sulfur or a direct bond, andR.sub.4 is hydroxy or hydroxy etherified or esterified as defined for W above;R.sub.5 is a C.sub.1-10 hydrocarbon aliphatic group; a C.sub.1-10 hydrocarbon aliphatic group substituted by aryl, a substituted aryl as defined for R.sub.2 above, or halogen; or cycloalkyl, substituted cycloalkyl, aryl, substituted aryl or aromatic heterocyclic, all as defined for R.sub.2 above;or a physiologically acceptable salt thereof with a base when R.sub.1 is OH,have valuable pharmacologoical properties.

    摘要翻译： 其中9-氯原子可以是α-或β-位的式为“IMAGE”的化合物，A为-CH 2 -CH 2 - 或顺式-CH = CH-，B为-CH 2 -CH 2， - ， CH = CH-或-CH 3 B - ，W是羟基亚甲基或D和E一起代表直接键，或D是1-10个碳原子的直链或支链亚烷基，任选被氟取代，E是 氧或硫或直接键，并且R4是如上定义的羟基或羟基醚化或酯化; R5是C1-10烃脂族基团; 被芳基取代的C1-10烃脂族基，对上述R2定义的取代芳基或卤素; 或环烷基，取代的环烷基，芳基，取代的芳基或芳族杂环，全部如上述R2所定义; 或其生理上可接受的盐，当R1为OH时，具有有价值的药理学性质。