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1. 发明授权

US4159343A Prostane derivatives 失效
标题翻译：前列腺衍生物
公开(公告)号：US4159343A
公开(公告)日：1979-06-26
申请号：US883428
申请日：1978-03-03
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： C07C405/00 , C07D309/12 , C07C69/34 , A61K31/225
CPC分类号： C07C405/0025 , C07C405/0016 , 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。

2. 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。

3. 发明授权

US4105792A Prostane dervatives 失效
标题翻译：前列治罪
公开(公告)号：US4105792A
公开(公告)日：1978-08-08
申请号：US689849
申请日：1976-05-25
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 , C07C69/34 , A61K31/225 , C07C177/00
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。

4. 发明授权

US4073934A Novel acetylenic prostaglandin analogs 失效
标题翻译：新型炔类前列腺素类似物
公开(公告)号：US4073934A
公开(公告)日：1978-02-14
申请号：US677861
申请日：1976-04-16
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
IPC分类号： A61K31/23 , C07C67/00 , C07C401/00 , C07C405/00 , C07D213/30 , C07D213/55 , C07D307/38 , C07D307/54 , C07D307/935 , C07D333/06 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00
摘要： Optically active and racemic prostaglandin derivatives of the formula ##STR1## wherein R.sub.1 is --OR.sub.5 ; --NHSO.sub.2 CH.sub.3 ; or --O--CH.sub.2 --U--V; R.sub.5 is hydrogen, alkyl, aryl, or a heterocyclic group; U is a direct bond, carbonyl or carbonyloxy; and V is phenyl substituted by 1-3 phenyl, alkoxy of 1-2 carbon atoms, or halogen, preferably bromine;R.sub.2 is hydrogen or alkyl of 1-5 carbon atoms;R.sub.3 is alkyl, substituted or unsubstituted cycloalkyl, straight-chain or branched alkyl of 1-5 carbon atoms substituted by aryl or substituted aryl, when R.sub.1 is as above; or R.sub.3 is aryl or substituted aryl group when R.sub.1 is --OR.sub.5 ', --NHSO.sub.2 CH.sub.3, or --O--CH.sub.2 --U--V and R.sub.5 ' is aryl or a heterocyclic group and U and V are as above;R.sub.4 is hydrogen or an ether or acyl residue;A is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--;D is a direct bond, oxygen, or sulfur;Z is carbonyl or >CH OR.sub.4 wherein OR.sub.4 is in the .alpha.- or .beta.-position; andX y is ##STR2## when Z is >CH OR.sub.4 --, or ##STR3## or --CH.dbd.CH-- when Z is carbonyl; AND, WHEN R.sub.1 is hydroxy, the physiologically compatible salts thereof with bases, have more prolonged activity than naturally-occurring prostaglandins.
摘要翻译：式（Ⅰ）的光学活性和外消旋前列腺素衍生物，其中R1为-OR5; -NHSO 2 CH 3; 或-O-CH 2 -U-V; R5是氢，烷基，芳基或杂环基; U是直接键，羰基或羰氧基; 并且V是被1-3个苯基，1-2个碳原子的烷氧基或卤素，优选溴取代的苯基; R2是氢或1-5个碳原子的烷基; R 3为烷基，取代或未取代的环烷基，被芳基或取代芳基取代的1-5个碳原子的直链或支链烷基，当R 1如上所述时; 或当R 1为-OR 5'，-NHSO 2 CH 3或-O-CH 2 -U-V且R 5'为芳基或杂环基时，R 3为芳基或取代的芳基，U和V如上所述; R4是氢或醚或酰基残基; A是-CH 2 -CH 2 - 或顺式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-; D是直接键合，氧或硫; Z是羰基或> CH OR 4，其中OR 4在α或β-位; 当Z为羰基时Z为> CH OR4-或或-CH = CH-时，X Y为当R1是羟基时，其与碱的生理上相容的盐比天然存在的前列腺素具有更长的活性。

5. 发明授权

US4346228A Novel 11-oxoprostaglandin derivatives 失效
标题翻译：新型11-氧代前列腺素衍生物
公开(公告)号：US4346228A
公开(公告)日：1982-08-24
申请号：US677420
申请日：1976-04-15
申请人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
发明人： Werner Skuballa , Bernd Raduechel , Helmut Vorbrueggen , Walter Elger , Olaf Loge , Eckehard Schillinger
IPC分类号： A61K31/23 , C07C67/00 , C07C401/00 , C07C405/00 , C07D213/30 , C07D307/20 , C07D307/935 , C07D309/12 , C07D521/00 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12
摘要： 11-Oxoprostaglandin derivatives of the formula ##STR1## wherein R.sub.2 is a hydrogen atom or alkyl of 1-5 carbon atoms,R.sub.3 is alkyl of 1-5 carbon atoms, alkylaryl, cycloalkyl of 5-6 ring carbon atoms and a total of 5-10 carbon atoms; benzodioxol-2-yl, phenyl, naphthyl or phenyl or naphthyl substituted by phenyl, halogen, alkyl of 1-4 carbon atoms, chloromethyl, fluoromethyl, carboxyl or hydroxy;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, or trans--CH.dbd.CH--;B is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH--,D and E collectively are a direct bond or D is alkylene of 1-5 carbon atoms and E is an oxygen or sulfur atom; esters thereof; readily cleavable 9,15 and 9,15 ethers thereof; methanesulfonylamides thereof, and physiologically acceptable salts thereof with bases; possess the activity of the corresponding natural prostaglandins with a surprisingly longer duration of effectiveness, greater selectivity, and better effects, and can be produced, e.g., by oxidation of the corresponding 9-hydroxy prostaglandins.
摘要翻译：其中R2是氢原子或1-5个碳原子的烷基，R3是1-5个碳原子的烷基，烷基芳基，5-6个环碳原子的环烷基和总共5个碳原子的11-前列酰乳糖衍生物 -10个碳原子; 苯基二氧杂环戊烯-2-基，苯基，萘基或被苯基，卤素，1-4个碳原子的烷基取代的苯基或萘基，氯甲基，氟甲基，羧基或羟基; A是-CH 2 -CH 2 - ，顺式-CH = CH-或反式-CH = CH-; B是-CH 2 -CH 2 - 或反式-CH = CH-，D和E共同是直接键或D是1-5个碳原子的亚烷基，E是氧或硫原子; 其酯; 易于切割的9,15和9,15醚; 甲磺酰胺及其与碱的生理学上可接受的盐; 具有相当的天然前列腺素的活性，具有惊人的更长的有效期，更高的选择性和更好的效果，并且可以例如通过相应的9-羟基前列腺素的氧化来产生。

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