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    5-Cyano-prostacyclin derivatives and use as medicines
    3.
    发明授权
    5-Cyano-prostacyclin derivatives and use as medicines 失效
    5-Cyano-prostacyclin衍生物用作药物

    公开(公告)号：US4364950A

    公开(公告)日：1982-12-21

    申请号：US317621

    申请日：1981-11-02

    申请人： Werner Skuballa ,  Helmut Vorbruggen ,  Bernd Raduchel ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    发明人： Werner Skuballa ,  Helmut Vorbruggen ,  Bernd Raduchel ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    IPC分类号： A61K31/557 ,  A61P7/02 ,  A61P9/12 ,  A61P11/08 ,  A61P43/00 ,  C07D307/935 ,  C07D307/937 ,  C07F7/18 ,  C07F9/40

    CPC分类号： C07D307/935 ,  C07D307/937 ,  C07F7/1856 ,  C07F9/4015

    摘要： 5-cyano-prostacyclins of the formula ##STR1## wherein R.sub.1 is OR.sub.2 or NHR.sub.3 ; R.sub.2 and R.sub.3 each independently is (a) H, (b) C.sub.1-10 -alkyl, (c) C.sub.1-10 -alkyl substituted by halo, C.sub.1-4 -alkoxy or phenyl, 1-naphthyl or 2-naphthyl, each optionally substituted as defined below, (d) C.sub.4-10 -cycloalkyl, (e) C.sub.4-10 -cycloalkyl substituted by C.sub.1-4 -alkyl, (f) phenyl, 1-naphthyl or 2-naphthyl, (g) phenyl, 1-naphthyl or 2-naphthyl substituted by 1-3 halogen atoms, phenyl, 1-3 alkyl groups of 1-4 C atoms each, or a chloromethyl-, fluoromethyl-, trifluoromethyl-, carboxyl-, hydroxy- or alkoxy-group of 1-4 C atoms, or (h) an aromatic, 5- or 6-membered heterocyclic ring containing one hetero atom which is O, N or S, the remaining atoms being carbon; R.sub.3 also possibly being an acyl group of a C.sub.1-15 -hydrocarbon carboxylic or sulfonic acid;B is straight chain or branched alkylene of 2-10 C atoms;W is hydroxymethylene or ##STR2## wherein the OH group may be in the alpha or beta position, and is optionally modified by replacement of the H atom of the OH with an ether or acyl group which is conventional for such replacements in prostaglandins and which is readily cleavable at physiological pH's;R.sub.4 is hydroxy, optionally modified as described for W above;R.sub.5, R.sub.6, R.sub.7 and R.sub.8 each independently is hydrogen, alkyl of 1-5 C atoms or methoxy; andR.sub.9 is alkyl of 1-5 C atoms orfor compounds wherein R.sub.2 is H, the salts thereof with physiologically compatible bases have valuable pharmacalogical properties, e.g., hypertonic and bronchodilatory activities.

    摘要翻译： 其中R1是OR2或NHR3的式“IMAGE”的5-氰基 - 前列环素; R 2和R 3各自独立地为（a）H，（b）C 1-10 - 烷基，（c）被卤素，C 1-4 - 烷氧基或苯基，1-萘基或2-萘基取代的C 1-10 - 烷基， （d）C 4-10 - 环烷基，（e）被C 1-4 - 烷基取代的C 4-10 - 环烷基，（f）苯基，1-萘基或2-萘基，（g）苯基， 萘基或被1-3个卤素原子取代的2-萘基，苯基，1-4个C原子的1-3个烷基，或1个氯甲基 - ，氟甲基 - ，三氟甲基 - ，羧基 - ，羟基或烷氧基 -4个C原子，或（h）含有一个杂原子的芳族的5或6元杂环，它是O，N或S，其余的原子是碳; R3也可能是C1-15-烃羧酸或磺酸的酰基; B是2-10个C原子的直链或支链亚烷基; W是羟基亚甲基或其中OH基团可以在α或β位置，并且任选地通过用在前列腺素中这种替代物常规的醚或酰基取代OH的H原子来任意修饰，并且其是 在生理pH值下易于切割; R4是羟基，任选地按照上述W所述进行改性; R5，R6，R7和R8各自独立地为氢，1-5个C原子的烷基或甲氧基; 并且R 9为1-5个C原子的烷基，或对于其中R 2为H的化合物，其与生理上相容的碱的盐具有有价值的药理学性质，例如高渗和支气管扩张活性。

    Azaprostacyclins, their preparation and pharmaceutical use
    5.
    发明授权
    Azaprostacyclins, their preparation and pharmaceutical use 失效
    阿沙普罗环素，其制备和药物用途

    公开(公告)号：US4567195A

    公开(公告)日：1986-01-28

    申请号：US591719

    申请日：1984-03-21

    申请人： Norbert Schwarz ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    发明人： Norbert Schwarz ,  Werner Skuballa ,  Helmut Vorbrueggen ,  Jorge Casals-Stenzel ,  Ekkehard Schillinger ,  Michael H. Town

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/557 ,  A61P7/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  C07C57/03 ,  C07C57/13 ,  C07C57/26 ,  C07C57/52 ,  C07C405/00 ,  C07D209/52 ,  C07D307/935 ,  C07F9/40

    CPC分类号： C07D307/935 ,  C07C405/00 ,  C07C405/0041 ,  C07C57/03 ,  C07C57/13 ,  C07C57/26 ,  C07C57/52 ,  C07D209/52 ,  C07F9/4015 ,  C07F9/4018

    摘要： Azaprostacyclins of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic residue, or a phenacyl residue optionally substituted on the phenyl ring by bromine, phenyl, alkoxy, or dialkoxy,W is a free or functionally modified carbonyl group or a ##STR2## wherein R.sub.8 is hydrogen or alkyl of 1-5 carbon atoms and R.sub.9 is hydrogen or a readily cleavable ether or acyl residue and wherein the OR.sub.9 -group can be in the .alpha.- or .beta.-position,R.sub.2 is a free or functionally modified hydroxy group,R.sub.3 and R.sub.4 each independently is hydrogen, alkyl of 1-5 carbon atoms, or fluorine,D is alkylene of 1-2 carbon atoms which can be substituted by alkyl groups of 1-5 carbon atoms,R.sub.5 is hydrogen or alkyl of 1-2 carbon atoms or, when D is alkylene of 1 or 2 carbon atoms, R.sub.5, together with R.sub.6, represents a bond,R.sub.6 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms, whereinR.sub.6 (R.sub.7) is halogen when R.sub.7 (R.sub.6), respectively, is alkyl of 1-2 carbon atoms orR.sub.5 and R.sub.7 each independently is hydrogen or alkyl of 1-2 carbon atoms whenD and R.sub.6 together form a carbocyclic ring closed via (CH.sub.2).sub.1-3 with D as --CH

    摘要翻译： 式I的阿沙普罗环素其中R 1是氢，烷基，环烷基，芳基，杂环残基或任选在苯环上被溴，苯基，烷氧基或二烷氧基取代的苯甲酰甲基残基，W是游离或 官能改性的羰基或其中R8是氢或1-5个碳原子的烷基，R9是氢或易裂解的醚或酰基残基，其中OR9-基团可以是α-或β-位， R2是游离的或官能改性的羟基，R 3和R 4各自独立地是氢，1-5个碳原子的烷基或氟，D是可以被1-5个碳原子的烷基取代的1-2个碳原子的亚烷基 原子，R5是氢或1-2个碳原子的烷基，或当D是1或2个碳原子的亚烷基时，R5与R6一起代表键，R6和R7各自独立地是氢或1-2碳的烷基 原子，其中当R 7（R 6）分别为1-2个碳原子的烷基或R 5和R 7 eac时，R 6（R 7）为卤素 h独立地为氢或1-2个碳原子的烷基，当D和R6一起形成通过（CH 2）1-3封闭的碳环，其中D为-CH 3且R 6为-CH 2 - ，当R 1为氢时， 其与碱的生理上相容的盐具有有价值的药理学性质，例如降血压和支气管扩张活性。

    Carbacyclins, process for the preparation thereof, and use thereof as medicinal agents
    7.
    发明授权
    Carbacyclins, process for the preparation thereof, and use thereof as medicinal agents 失效
    卡巴菌素，其制备方法及其作为药剂的用途

    公开(公告)号：US5124343A

    公开(公告)日：1992-06-23

    申请号：US141233

    申请日：1988-01-06

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

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

    IPC分类号： C07C45/59 ,  C07C57/26 ,  C07C57/60 ,  C07C405/00 ,  C07D263/14 ,  C07D317/72 ,  C07F9/40

    CPC分类号： C07D317/72 ,  C07C405/0083 ,  C07C45/59 ,  C07C57/26 ,  C07C57/60 ,  C07D263/14 ,  C07F9/4018

    摘要： The invention relates to carbacyclins of general Formula I ##STR1## wherein R.sub.1 is the residue CH.sub.2 OH or ##STR2## with R.sub.2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl residue, a ##STR3## or heterocyclic residue, or R.sub.1 is the residue ##STR4## with R.sub.3 meaning an alkanoyl or alkanesulfonyl residue of respectively 1-10 carbon atoms or the residue R.sub.2, orR.sub.1 is the residue ##STR5## wherein m is the number 1 or 2, X is an oxygen atom or a CH.sub.2 -group,A is a trans--CH.dbd.CH- or --.tbd.C--group,W is a free or functionally modified hydroxymethylene group wherein the OH-group can be in the .alpha.- or .beta.- position,n is the number 1, 2, or 3,D is a straight-chain alkylene group of 1-5 carbon atoms,E is a --C.tbd.C---bond or a --CR.sub.6 =CR.sub.7 --group wherein R.sub.6 and R.sub.7 are different from each other and mean a hydrogen atom or an alkyl group of 1-5 carbon atoms or a hydrogen atom or a halogen atom, preferably chlorine,R.sub.4 is an alkyl, cycloalkyl, or optionally substituted arly group, or a heterocyclic group,R.sub.5 is a free or functionally modified hydroxy group, andif R.sub.2 means a hydrogen atom, the salts thereof with physiologically compatible bases;to processes for the preparation thereof, and to the use thereof as blood-pressure-lowering agents.

    摘要翻译： 本发明涉及通式I的碳霉素，其中R 1是残基CH 2 OH或R 2，其中R 2表示氢原子，烷基，环烷基，芳基，芳基或杂环残基，或者R 1是 残基其中R3表示分别为1-10个碳原子的烷酰基或烷磺酰基残基或残基R2，或R1为残基，其中m为数1或2，X为氧原子或CH2- 基团，A是反式-CH = CH-或 - 3BOND C-基团，W是游离或官能改性的羟基亚甲基基团，其中OH-基团可以是α或β位置，n是数1，2 或3，D是1-5个碳原子的直链亚烷基，E是-C3OND C键或-CR6 = CR7-基团，其中R6和R7彼此不同，意指氢 原子或1-5个碳原子的烷基或氢原子或卤素原子，优选氯，R4是烷基，环烷基或任选取代的芳基或杂环基团 p，R5是游离或功能改性的羟基，如果R 2表示氢原子，则其与生理上相容的碱的盐; 其制备方法及其作为降血压剂的用途。

    3-oxa-5-fluoro-carbacyclins, their preparation and use as medicinal agents
    8.
    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。

    Novel carbacyclinamides, their preparation and use as medicinal agents
    10.
    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。