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    • 3. 发明授权
    • Novel carbacyclins, processes for their production and their use as
medicinal agents
    • 新型碳霉素,其生产工艺及其作为药剂的使用
    • US4827017A
    • 1989-05-02
    • US21102
    • 1987-03-03
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenEkkehard SchillingerClaus-Steffen Stuerzebecher
    • Werner SkuballaBernd RaduechelHelmut VorbrueggenEkkehard SchillingerClaus-Steffen Stuerzebecher
    • C07D309/12A61K31/557A61P1/04A61P7/02A61P9/08A61P9/12A61P11/08A61P43/00C07C45/00C07C49/835C07C51/00C07C65/19C07C67/00C07C69/76C07C69/773C07C405/00C07C177/00
    • C07C405/0083
    • 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.
    • 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。
    • 4. 发明授权
    • 9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents
    • 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
    • US06225347B1
    • 2001-05-01
    • US08313667
    • 1994-09-27
    • Bernd BuchmannWerner SkuballaHelmut VorbrueggenBernd RaduechelOlaf LogeWalter ElgerClaus-Steffen StuerzebecherKarl-Heinz Thierauch
    • Bernd BuchmannWerner SkuballaHelmut VorbrueggenBernd RaduechelOlaf LogeWalter ElgerClaus-Steffen StuerzebecherKarl-Heinz Thierauch
    • C07C40500
    • C07C405/0016C07C405/00C07C405/0025
    • 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.
    • 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。