利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

41 条记录 (耗时 0.024 秒)

    Novel carbacyclin esters, process for the preparation thereof, and their use as medicinal agents
    1.
    发明授权
    Novel carbacyclin esters, process for the preparation thereof, and their use as medicinal agents 失效
    新型卡巴环素酯，其制备方法及其作为药剂的用途

    公开(公告)号：US4618626A

    公开(公告)日：1986-10-21

    申请号：US777535

    申请日：1985-09-16

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael-Harold Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael-Harold Town

    IPC分类号： C07C69/708 ,  A61K31/557 ,  A61P1/04 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  C07C67/10 ,  C07C69/732 ,  C07C405/00 ,  C07C177/00

    CPC分类号： C07C405/0083

    摘要： Carbacyclin esters of Formula I ##STR1## wherein R.sub.1 is an unsubstituted or substituted aromatic residue,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 is an alkyl or cycloalkyl group, or an optionally substituted aryl group, or a heterocyclic group,X is an oxygen atom or the group --CH.sub.2 --,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 the group ##STR3## a straight-chain saturated alkylene group of 1-5 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated alkylene group of 2-5 carbon atoms, which groups can optionally be substituted by fluorine atoms,E is a direct bond, a --C.tbd.C--group, or a --CR.sub.4 .dbd.CR.sub.5 -- group wherein R.sub.2 and R.sub.5 mean a hydrogen atom or an alkyl group of 1-5 carbon atoms;are useful as blood-pressure-lowering agents, inter alia.

    摘要翻译： 式I的卡巴环素酯其中R 1是未取代或取代的芳族残基，R 2是游离或官能改性的羟基，R 3是烷基或环烷基，或任选取代的芳基或杂环基 ，X是氧原子或基团-CH 2 - ，A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3 C C基，W是游离或官能改性的羟基亚甲基， 功能修饰的“IMAGE”，其中OH基可以在α或β位D是基团，即1-5个碳原子的直链饱和亚烷基，支链，饱和或直链 或2-5个碳原子的支链不饱和亚烷基，该基团可任选被氟原子取代，E是直接键，-C 3 C C基或-CR 4 = CR 5 - 基，其中R 2和R 5表示 氢原子或1-5个碳原子的烷基; 作为降血压剂特别有用。

    Novel carbacyclinamides, their preparation and use as medicinal agents
    3.
    发明授权
    Novel carbacyclinamides, their preparation and use as medicinal agents 失效
    新型卡巴胆碱，其制备和用作药物

    公开(公告)号：US4552875A

    公开(公告)日：1985-11-12

    申请号：US510125

    申请日：1983-07-01

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael H. Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Bob Nieuweboer ,  Michael H. Town

    IPC分类号： A61K31/16 ,  A61K31/19 ,  A61K31/535 ,  A61K31/5375 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  C07C67/00 ,  C07C231/00 ,  C07C231/02 ,  C07C231/10 ,  C07C231/12 ,  C07C233/21 ,  C07C235/06 ,  C07C235/08 ,  C07C235/14 ,  C07C235/16 ,  C07C235/30 ,  C07C405/00 ,  C07D295/18 ,  C07H13/04 ,  C07C177/00 ,  A61K31/557

    CPC分类号： C07H13/04 ,  C07C405/0083

    摘要： Carbacyclinamides of Formula I ##STR1## wherein R.sub.1 is NHR.sub.4, wherein R.sub.4 is H, --(CH.sub.2).sub.n --R.sub.8 or straight-chained or branched aliphatic groups of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 each are straight-chained or branched, lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms, or R.sub.4 and R.sub.5 together with the adjoining N-atom form a 5- or 6-membered heterocycle which can optionally contain additional hetero atoms and can be substituted; or R.sub.1 is NR.sub.4 R.sub.5 wherein R.sub.4 is an aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, and R.sub.5 is straight-chained or branched aliphatic group of 1-10 carbon atoms, cycloalkyl of 3-10 carbon atoms, aryl, or lower, mono- or polyhydroxyalkyl of 2-8 carbon atoms;n is 1-4;R.sub.8 is --CONH.sub.2 or --N(C.sub.1 -C.sub.4 -alkyl).sub.2 ;R.sub.2 is a free or functionally modified hydroxy group;R.sub.3 is aliphatic, cycloalkyl, optionally substituted aryl, or a heterocyclic group;X is oxygen or --CH.sub.2 --;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --CH.tbd.--;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position; D is ##STR3## a straight-chain, saturated aliphatic group of 1-5 carbon atoms, or a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-5 carbon atoms, all of which groups can optionally be substituted by fluorine atoms;m is 1-3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --wherein R.sub.6 and R.sub.7 are each a hydrogen atom or an alkyl group of 1-5 carbon atomshave valuable pharmacological properties.

    摘要翻译： 式I的卡拉菌素酰胺其中R 1是NHR 4，其中R 4是H， - （CH 2）n -R 8或1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基， 芳基或2-8个碳原子的低级单 - 或多羟基烷基，或R1是NR4R5，其中R4和R5各自是2-8个碳原子的直链或支链，低级，单 - 或多羟基烷基，或R4和R5连同 邻接的N-原子形成5-或6-元杂环，其可以任选地含有另外的杂原子并且可以被取代; 或R1是NR4R5，其中R4是1-10个碳原子的脂族基团，3-10个碳原子的环烷基，R5是1-10个碳原子的直链或支链脂族基团，3-10个碳原子的环烷基， 芳基或更低级的2-8个碳原子的单或多羟基烷基; n为1-4; R8是-CONH2或-N（C1-C4-烷基）2; R2是游离或官能改性的羟基; R3是脂族，环烷基，任选取代的芳基或杂环基; X是氧或-CH 2 - ; A是-CH 2 -CH 2 - ，反式-CH = CH-或-CH 3 OCH 3 - 。 W是游离的或官能改性的羟基亚甲基或游离或功能改性的“IMAGE”，其中OH-基团可以是α-或β-位; D是1-5个碳原子的直链饱和脂族基团，或2-5个碳原子的支链，饱和或直链或支链不饱和脂肪族基团，所有这些基团可任选地为 被氟原子取代; m为1-3; E是直接键，-C 3 D或-CR 6 = CR 7 - 其中R 6和R 7各自为氢原子或1-5个碳原子的烷基具有有价值的药理学性质。

    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents
    4.
    发明授权
    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents 失效
    3-OXA-5-FLOORO-CARBACYCLINS，其制备和用作药物代理

    公开(公告)号：US5157042A

    公开(公告)日：1992-10-20

    申请号：US713002

    申请日：1991-06-10

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Gerda Mannesmann ,  Michael H. Town

    IPC分类号： C07C69/708 ,  A61K31/225 ,  A61K31/35 ,  A61K31/351 ,  A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  C07C51/00 ,  C07C51/367 ,  C07C59/125 ,  C07C59/62 ,  C07C67/00 ,  C07C67/31 ,  C07C231/00 ,  C07C231/02 ,  C07C231/12 ,  C07C235/06 ,  C07C235/08 ,  C07C235/88 ,  C07C405/00 ,  C07D309/12 ,  C07D317/72

    CPC分类号： C07D317/72 ,  C07C405/0083

    摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2 ;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 aliphatic group of 1-10 carbon atoms; or a branched, saturated or straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms; all of which are substituted by fluorine atoms;n is 1, 2, or 3;E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 --, wherein R.sub.6 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.7 is hydrogen, halogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group; andR.sub.5 is a free or functionally modified hydroxy group; andwhen R.sub.1 is OH, the salts thereof with physiologically compatible bases,are valuable pharmacological 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，烷基，环烷基，芳基，杂芳基或杂环残基; 或R1是NHR3，其中R3是酸残基（酰基）或R2; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH基可以是α-或β-位; D是1-10个碳原子的直链饱和脂族基团; 或2-10个碳原子的支链，饱和或直链或支链的不饱和脂族基团; 所有这些都被氟原子取代; n为1,2或3; E是直接键，-C 3 D或-CR 6 = CR 7 - ，其中R 6是氢或1-5个碳原子的烷基，R 7是氢，卤素或1-5个碳原子的烷基; R4是脂族基团，环烷基，任选取代的芳基或杂环基; R5是游离或官能改性的羟基; 当R1是OH时，其与生理上相容的碱的盐是有价值的药剂。

    Certain pyrrole analogs of prostacyclin derivatives
    6.
    发明授权
    Certain pyrrole analogs of prostacyclin derivatives 失效
    某些前列环素衍生物的吡咯类似物

    公开(公告)号：US4315013A

    公开(公告)日：1982-02-09

    申请号：US122794

    申请日：1980-02-19

    申请人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Wolfgang Losert ,  Jorge Casals

    发明人： Werner Skuballa ,  Bernd Raduechel ,  Helmut Vorbrueggen ,  Gerda Mannesmann ,  Wolfgang Losert ,  Jorge Casals

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/557 ,  A61K31/5585 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07C405/00 ,  C07D209/52 ,  A61K31/435 ,  C07D401/12 ,  C07D405/12

    CPC分类号： C07D209/52 ,  C07C405/00 ,  C07C405/0041

    摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 alkylammonium; (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;W is hydroxymethylene or RO-methylene; or ##STR2## wherein OH or OR is in the .alpha.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently hydrogen or alkyl of 1-5 carbon atoms,R.sub.2 is OH or OR, R being as defined above,or, when R.sub.1 is H, a physiologically compatible salt thereof with a base.

    摘要翻译： 其中R 1为（a）氢，（b）C 1-10烷基，（c）被卤素取代的C 1-10烷基; C 1-4烷氧基; C6-10芳基; 被1-3个卤素原子取代的C 6-10芳基，苯基，1-3个C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基; 二-C 1-4 - 烷基氨基; 或三-C 1-4烷基铵; （d）C 4-10环烷基，（e）被C 1-4烷基取代的C 4-10环烷基，（f）C 6-10芳基，（g）被1-3个卤素原子取代的C 6-10芳基，苯基， -3 C 1-4烷基或氯甲基，氟甲基，三氟甲基，羧基，羟基或C 1-4烷氧基，或（h）5或6个环原子的芳族杂环，其中一个为O，N或S; W是羟基亚甲基或RO-亚甲基; 或其中OH或OR位于α位且R是体内可水解和生理上可接受的醚或酰基，其是常规用于改变前列腺素中的OH基团; R 3，R 4，R 5和R 6各自独立地是氢或1-5个碳原子的烷基，R 2是OH或OR，R如上定义，或者当R 1是H时，其与碱的生理上相容的盐。

    Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals
    7.
    发明授权
    Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals 失效
    某些5-氰基-16-氟前列环素及其作为药物的用途

    公开(公告)号：US4378370A

    公开(公告)日：1983-03-29

    申请号：US309967

    申请日：1981-10-06

    申请人： Helmut Vorbrueggen ,  Bernd Raduechel ,  Werner Skuballa ,  Gerda Mannesmann ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger

    发明人： Helmut Vorbrueggen ,  Bernd Raduechel ,  Werner Skuballa ,  Gerda Mannesmann ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger

    IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/557 ,  A61P43/00 ,  C07D307/93 ,  C07D307/937 ,  C07F7/18

    CPC分类号： C07D307/937 ,  C07F7/1856 ,  Y10S514/826

    摘要： Prostacyclin derivatives of the formula ##STR1## wherein R.sub.1 is OR.sub.3 wherein R.sub.3 is hydrogen or alkyl of 1-10 carbon atoms, or R.sub.1 is NHR.sub.4 wherein R.sub.4 is alkanoyl or alkanesulfonyl,B is alkylene of 1-5 carbon atoms,A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--,W is hydroxymethylene or ##STR2## wherein the OH-group is optionally substituted by alkanoyl of 1-4 carbon atoms and the free or substituted OH-group can be in the .alpha.- or .beta.- position,R.sub.2 is alkyl of 1-6 carbon atoms optionally substituted by phenyl, or R.sub.2 is phenyl,R.sub.5 is hydroxy optionally substituted by alkanoyl of 1-4 carbon atoms,R.sub.6 is hydrogen, fluorine, or alkyl of 1-4 carbon atomsor when R.sub.3 is hydrogen, a salt thereof with a physiologically compatible base,have pharmacological activity e.g., blood pressure-lowering and bronchodilatory effects.

    摘要翻译： PCT No.PCT / DE81 / 00031 Sec。 371日期1981年10月6日 102（e）日期1981年10月6日PCT提交1981年2月5日PCT公布。 出版物WO81 / 02296 日本1981年8月20日。其中R 1为OR 3的式（I）其中R 3为氢或1-10个碳原子的烷基，或R 1为NHR 4，其中R 4为烷酰基或链烷磺酰基，B为1- 5个碳原子，A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-，W是羟基亚甲基或其中OH基任选被1-4个碳原子的烷酰基取代 并且游离或取代的OH基团可以在α或β位，R 2是任选被苯基取代的1-6个碳原子的烷基，或者R 2是苯基，R 5是任选被1-4碳的烷酰基取代的羟基 原子，R6是氢，氟或1-4个碳原子的烷基，或当R3是氢时，其与生理上相容的碱的盐具有药理活性，例如降血压和支气管扩张作用。

    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。

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

    公开(公告)号：US4560786A

    公开(公告)日：1985-12-24

    申请号：US391734

    申请日：1982-06-24

    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： A61K31/045 ,  A61K31/557 ,  A61K31/5575 ,  A61P25/04 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07C177/00

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

    摘要： .DELTA..sup.8,9 -Prostane 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 ##STR3## wherein R.sub.3 is an acid residue or R.sub.2 ; 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 or free or functionally modified ##STR4## 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, 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 free or functionally modified hydroxy andR.sub.5 is an optionally substituted aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group, and when R.sub.2 is hydrogen, physiologically compatible salts thereof with bases,have valuable pharmacological properties, e.g. luteolytic and abortifacient activities.

    摘要翻译： DELTA 8,9-式I的前驱体衍生物其中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; 或R 1为，其中R 3为酸残基或R 2; A是-CH 2 -CH 2 - 或顺式-CH = CH; B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3BOND C-W是游离或官能改性的羟基亚甲基或游离或官能改性的“IMAGE”，其中OH-基团可以是α或β - 位置 D和E共同是直接键合，或D是可以任选被氟原子取代的1-10个碳原子的直链或支链亚烷基或亚烯基，并且E是氧，硫，直接键，-C 3 D或 -CR 6 = CR 7 - ，其中R 6和R 7彼此不同，各自为氢，氯或烷基; R4是游离的或官能改性的羟基，R 5是任选取代的脂族基，环烷基，任选取代的芳基或杂环基，当R 2是氢时，其与碱的生理上相容的盐具有有价值的药理学性质。 luteolytic和流产活动。

    9-Fluoroprostaglandin derivatives, and use as medicinal agents
    10.
    发明授权
    9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
    9-氟前列腺素衍生物，用作药物

    公开(公告)号：US4454339A

    公开(公告)日：1984-06-12

    申请号：US395448

    申请日：1982-07-06

    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, 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1-氟代衍生物（Ⅰ） 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，任选取代的芳基或杂环基，当R 2是H时，其生理上相容的盐 具有碱性，具有有价值的药理学性质，例如作为纤溶素或流产。