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1. 发明授权

US4464364A 6.beta.,7.beta.-Methylene-17.alpha.-pregn-4-ene-21,17-carbolactones, their preparation and use as medicinal agents 失效
标题翻译： 6β，7β-亚甲基-17α-孕-4-烯-21,17-碳内酯，它们的制备和用作药物
公开(公告)号：US4464364A
公开(公告)日：1984-08-07
申请号：US502848
申请日：1983-06-09
申请人： Dieter Bittler , Henry Laurent , Rudolf Weichert , Jorge Casals-Stenzel , Ekkehard Schillinger
发明人： Dieter Bittler , Henry Laurent , Rudolf Weichert , Jorge Casals-Stenzel , Ekkehard Schillinger
IPC分类号： A61K31/585 , A61P5/38 , C07J53/00 , A61K31/33
CPC分类号： C07J53/008 , C07J53/007 , Y10S514/869
摘要： Novel 6.beta.,7.beta.-methylene-17.alpha.-pregn-4-ene-21,17-carbolactones of Formula I ##STR1## wherein R and R' each is hydrogen or jointly form a methylene group.These exhibit a good antimineralocorticoid effect with low side effects.
摘要翻译：式I的新型6β，7β-亚甲基-17α-孕-4-烯-21,17-碳内酯其中R和R'各自为氢或共同形成亚甲基。这些表现出良好的抗皮质激素效应，副作用低。

2. 发明授权

US4708963A Novel carbacyclins, their preparation and use 失效
标题翻译：新型碳霉素，其制备和用途
公开(公告)号：US4708963A
公开(公告)日：1987-11-24
申请号：US738545
申请日：1985-05-28
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
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, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;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 a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CH.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
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，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; 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1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CH 7 - ，其中R 6和R 7是氢或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是游离的或官能改性的羟基，当R2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。

3. 发明授权

US4378370A Certain 5-cyano-16-fluoro-prostacyclins and their use as pharmaceuticals 失效
标题翻译：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。

4. 发明授权

US4423067A Carbacyclins, their preparation and use 失效
标题翻译：卡巴菌素，其制备和用途
公开(公告)号：US4423067A
公开(公告)日：1983-12-27
申请号：US333099
申请日：1981-12-21
申请人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduchel , Norbert Schwarz , Helmut Vorbruggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Michael H. Town
IPC分类号： C07C69/708 , A61K31/16 , A61K31/19 , A61K31/20 , A61K31/23 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C51/00 , C07C51/367 , C07C59/125 , C07C67/00 , C07C231/00 , C07C231/02 , C07C235/06 , C07C235/88 , C07C301/00 , C07C303/40 , C07C311/51 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40 , C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D309/12 , C07F9/4015 , Y10S514/927
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, a heterocyclic residue, or NHR.sub.3, wherein R.sub.3 is an acid residue or hydrogen;X is oxygen;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--;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 a straight-chain or branched, saturated or unsaturated aliphatic group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms, 1,2-methylene, 1,1-trimethylene;E is --C.tbd.C-- or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are hydrogen or alkyl of 1-5 carbon atoms;R.sub.4 is an aliphatic group, cycloalkyl, optionally substituted aryl, or a heterocyclic group;R.sub.5 is free or functionally modified hydroxy and,when R.sub.2 is hydrogen, the physiologically compatible salts thereof with bases, have valuable pharmacological properties.
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，杂环残基或NHR 3，其中R 3是酸残基或氢; X是氧; A是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C; 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1-10个碳原子的直链或支链，饱和或不饱和的脂族基团，其可任选被氟原子取代，1,2-亚甲基，1,1-三亚甲基; E是-C 3 C或-CR 6 = CR 7 - ，其中R 6和R 7是氢或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是游离的或官能改性的羟基，当R2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。

5. 发明授权

US4446147A Azaprostacyclins, their preparation and pharmaceutical use 失效
标题翻译：阿沙普罗环素，其制备和药物用途
公开(公告)号：US4446147A
公开(公告)日：1984-05-01
申请号：US350674
申请日：1982-02-22
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.
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。

6. 发明授权

US4954524A Carbacylcins, their preparation and use as medicinal agents 失效
标题翻译：肉桂胆碱，其制备和用作药剂
公开(公告)号：US4954524A
公开(公告)日：1990-09-04
申请号：US333812
申请日：1989-04-06
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Ekkehard Schillinger , Michael H. Town
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Gerda Mannesmann , Ekkehard Schillinger , 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
CPC分类号： C07H13/04 , C07C405/0083
摘要： Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or 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,n is 2, 3, 4, or 5,X is hydrogen or fluorine,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, a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms, all of which can optionally be substituted by fluorine atoms,m 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 and R.sub.7 are different from each other and are hydrogen or alkyl or 1-5 carbon atoms, or are hydrogen or halogen,R.sub.4 is an aliphatic group, cycloalkyl, or 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, have valuable pharmacological properties.

7. 发明授权

US4567195A Azaprostacyclins, their preparation and pharmaceutical use 失效
标题翻译：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。

8. 发明授权

US4497830A Carbacyclins, their preparation and pharmacological use 失效
标题翻译：卡巴菌素，其制备和药理学用途
公开(公告)号：US4497830A
公开(公告)日：1985-02-05
申请号：US381609
申请日：1982-05-24
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Gerda Mannesmann , Bob Nieuweboer
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Jorge Casals-Stenzel , Ekkehard Schillinger , Gerda Mannesmann , Bob Nieuweboer
IPC分类号： A61K31/557 , A61P43/00 , C07C29/147 , C07C33/05 , C07C33/12 , C07C41/26 , C07C43/178 , C07C405/00 , C07D309/12 , C07D317/72 , C07F9/40
CPC分类号： C07D317/72 , C07C33/12 , C07C405/0083 , C07C43/178 , C07D309/12 , C07F9/4015
摘要： Compounds of Formula I ##STR1## wherein X is oxygen or CH.sub.2 ;A is CH.sub.2 --CH.sub.2, trans-CH.dbd.CH or C.tbd.C;W is free or functionally modified hydroxymethylene or free or functionally modified ##STR2## and the OH groups may be in the .alpha.- or the .beta.-position; D is straight chain or branched, saturated or unsaturated hydrocarbon aliphatic of from 1 to 10 carbon atoms, which may be substituted by fluorine;E is C.tbd.C or CR.sub.3 .dbd.CR.sub.4, R.sub.3 and R.sub.4 being different and being hydrogen or alkyl of 1 to 5 carbon atoms;R.sub.1 is free or functionally modified hydroxy; andR.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or heterocyclic,have valuable pharmacological properties, e.g., hypotensive and bronchodilatory characteristics. They can furthermore be used for prophylaxis and therapy of coronary infarct and as a treatment for stroke. They are produced by means of reduction of the corresponding 1-carbonic acid derivatives.
摘要翻译：式I的化合物其中X是氧或CH 2; A是CH 2 -CH 2，反式-CH = CH或C 3 C; W是游离或官能改性的羟基亚甲基或游离或功能修饰的“IMAGE”，OH基可以是α或β位; D是可以被氟取代的具有1至10个碳原子的直链或支链，饱和或不饱和的烃脂族; E为C 3或C 3或CR 3 = CR 4，R 3和R 4不同，为氢或1至5个碳原子的烷基; R1是游离或官能改性的羟基; 和R2是烷基，环烷基，任选取代的芳基或杂环，具有有价值的药理学性质，例如降血压和支气管扩张特征。它们还可用于冠状动脉梗塞的预防和治疗以及中风治疗。它们是通过还原相应的1-碳酸衍生物生产的。

9. 发明授权

US4364950A 5-Cyano-prostacyclin derivatives and use as medicines 失效
标题翻译： 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。

10. 发明授权

US4631276A Prostaglandins and prostacyclins, process for their preparation and their use as medicaments 失效
标题翻译：前列腺素和前列腺素，其制备过程及其用作药物
公开(公告)号：US4631276A
公开(公告)日：1986-12-23
申请号：US627572
申请日：1984-07-03
申请人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
发明人： Helmut Vorbruggen , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
IPC分类号： C07C405/00 , C07D263/14 , C07D277/10 , C07D417/12 , C07F7/18 , C07D233/14 , A61K31/42
CPC分类号： C07D417/12 , C07C405/0041 , C07D263/14 , C07D277/10 , C07F7/1856
摘要： Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.
摘要翻译：式I的化合物其中R 1是前列腺素或前列环素残基; Y是氧，硫，亚氨基或N-（C 1 -C 4 - 烷基）亚氨基; Q是（CR 6 R 7）p，其中p是0至3的整数; R2是氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; C 1 -C 4烷氧基羰基; 苄氧羰基氰基; 或二-C 1 -C 4烷基氨基 - 羰基; R3，R4，R5，R6和R7各自独立地为氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; 或芳基; 当R 2和R 5一起代表直接键时，R 3和R 4一起形成三亚甲基，四亚甲基或1,3-丁二烯基; 具有有价值的药理学性质，例如作为降血压药或降血糖药。

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