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1. 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。

2. 发明授权

US4468395A Prostaglandins and prostacyclins, processer 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：US4468395A
公开(公告)日：1984-08-28
申请号：US380326
申请日：1982-05-20
申请人： VorbruHelmut , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
发明人： VorbruHelmut , 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 -alkylaminocarbonyl;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。

3. 发明授权

US4235930A Novel acetylenic prostaglandins and processes for the preparation thereof 失效
标题翻译：新型炔类前列腺素及其制备方法
公开(公告)号：US4235930A
公开(公告)日：1980-11-25
申请号：US920523
申请日：1978-06-29
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Ekkehard Schillinger
IPC分类号： A61K31/18 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/435 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/20 , C07D307/935 , C07D309/12 , C07D333/32 , C07F9/40 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4015 , Y02P20/55
摘要： Prostane derivatives of the formula ##STR1## wherein R.sub.1 is the residue OR.sub.2 and R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, or a heterocyclic residue; or is NHR.sub.3 wherein R.sub.3 is an acyl group derived from a hydrocarbon carboxylic or sulfonic acid of up to 15 carbon atoms;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--Z is carbonyl or ##STR2## wherein the OR.sub.4 group can be in the .alpha.- or .beta.-position and R.sub.4 is H or a hydroxy-protective groupX Y is ##STR3## wherein R.sub.4 is as defined above, --CH.sub.2 -- CH.sub.2 -- or --CH.sub.2 --CH-- wherein R.sub.5 is alkyl or 1-5 carbon atoms, if Z is R.sub.5 carbonyl or ##STR4## X Y represents --CH.dbd.CH-- if Z is carbonyl: R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 each independently is hydrogen or an alkyl group of 1-5 carbon atoms; andR.sub.11 is alkyl of 1-5 carbon atoms;and if R.sub.2 is hydrogen, the salts thereof with physiologically compatible bases are prostaglandins having prolonged duration of activity and increased selectivity of effectiveness.
摘要翻译：其中R1是残基OR2，R2是氢，烷基，环烷基，芳基或杂环残基的式或者是NHR 3，其中R 3是衍生自至多15个碳原子的烃羧酸或磺酸的酰基; A是-CH 2 -CH 2 - 或顺式-CH = CH-Z是羰基或者其中OR 4基团可以是α或β-位，R 4是H或羟基保护基团XY是其中R 4如上定义，-CH 2 -CH 2 - 或-CH 2 -CH-，其中R 5是烷基或1-5个碳原子，如果Z是R 5羰基或如果Z是羰基，则X代表-CH = CH- R6，R7，R8，R9和R10各自独立地为氢或1-5个碳原子的烷基; R11为1-5个碳原子的烷基; 并且如果R 2是氢，则其与生理上相容的碱的盐是具有延长的活性持续时间和增加的有效性选择性的前列腺素。

4. 发明授权

US5079259A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药物活性9氯罗丹明
公开(公告)号：US5079259A
公开(公告)日：1992-01-07
申请号：US96232
申请日：1987-09-08
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： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： A 9-chloroprostane of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha. or .beta.-position and R.sub.1, R.sub.4, R.sub.5, A, B, W, D and E are as described hereinafter which are useful as medical agents.

5. 发明授权

US5204371A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：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。

6. 发明授权

US4444788A Pharmaceutically active 9-chloroprostaglandins 失效
标题翻译：药用活性9-氯前列腺素
公开(公告)号：US4444788A
公开(公告)日：1984-04-24
申请号：US387140
申请日：1982-06-10
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： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： Compounds of the formula ##STR1## wherein the 9-chlorine atom can be in the .alpha.- or .beta.-position,R.sub.1 is OR.sub.2, or NHR.sub.3 wherein R.sub.3 is H or the acyl group ofa C.sub.1-15 hydrocarbon carboxylic or sulfonic acid;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--, ##STR2## wherein the OH-group in each case can be in the .alpha.- or .beta.-position, and can be etherified or esterified by tetrahydropyranyl, tetrahydrofuranyl, .alpha.-ethoxyethyl, trimethylsilyl dimethyl, tert-butylsilyl, tribenzylsilyl, acetyl, propionyl, butyryl or benzoyl;D 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 pharmacological properties.
摘要翻译：其中9-氯原子可以是α-或β-位，R1是OR2或NHR3，其中R3是H或C1-15烃羧酸或磺酸的酰基; A是-CH 2 -CH 2 - 或顺式-CH = CH-，B是-CH 2 -CH 2 - ，反式-CH = CH-或-C 3位C，，其中每种情况下的OH-基团可以是四氢呋喃基，α-乙氧基乙基，三甲基甲硅烷基二甲基，叔丁基甲硅烷基，三苄基甲硅烷基，乙酰基，丙酰基，丁酰基或苯甲酰基可以醚化或酯化。 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R 4是羟基或羟基醚化或酯化如上述W所定义; R5是C1-10烃脂族基团; C1-10烃基，被芳基取代的脂族基团，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。

7. 发明授权

US4789685A 9-fluoroprostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： 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。

8. 发明授权

US4560786A .DELTA..sup.8,9 -Prostaglandin derivatives, their preparation and use as medicinal agents 失效
标题翻译： 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. 发明授权

US4454339A 9-Fluoroprostaglandin derivatives, and use as medicinal agents 失效
标题翻译： 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。

10. 发明授权

US4256745A New prostane derivatives and process for their preparation 失效
标题翻译：新的前列腺衍生物及其制备方法
公开(公告)号：US4256745A
公开(公告)日：1981-03-17
申请号：US882687
申请日：1978-03-02
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Eckehard Schillinger
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Eckehard Schillinger
IPC分类号： A61K31/21 , A61K31/27 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C07C177/00 , C07C69/02
CPC分类号： C07C405/0016 , C07C405/0025 , C07D309/12
摘要： Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.
摘要翻译：描述了用于其制备的丙烷-1-醇酯和中间体; 前者的化合物表现出改善的器官特异性和较低的剂量比相应的未酯化的前列腺素更长的活性持续时间，并且尤其用于触发流产，诱导劳动和调节月经周期。

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