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1. 发明授权

US4004020A Novel prostanoic acid derivatives and process for the preparation thereof 失效
标题翻译：新型前列腺酸衍生物及其制备方法
公开(公告)号：US4004020A
公开(公告)日：1977-01-18
申请号：US534483
申请日：1974-12-19
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07D317/14 , C07D317/46 , C07D317/70 , C07D319/06 , C07D319/08 , C07F9/40 , C07F9/54 , A01N9/28 , A61K31/335
CPC分类号： C07F9/4006 , C07D317/46 , C07D317/70 , C07D319/06 , C07F9/5407
摘要： Prostaglandins of the formula ##STR1## wherein R.sub.1 is hydroxymethyl, carboxy, aryloxycarbonyl, alkoxycarbonyl of 1-8 carbon atoms in the alkoxy group, or the group -COO-CH.sub.2 -U-V wherein U is a direct C-C bond, carbonyl or carbonyloxy and V is phenyl substituted by phenyl, alkoxy of 1-2 carbon atoms or halogen; R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is -CH.sub.2 -CH.sub.2 or trans-CH=CH; B is -CH.sub.2 -CH.sub.2 or CH=CH; one of R.sub.4 and R.sub.5 is hydroxy and the other is a hydrogen atom; R.sub.6 and R.sub.7 each are alkyl of 1-10 carbon atoms or collectively are alkylene of up to 7 carbon atoms and with 2-3 carbon atoms in the chain, phenylene or naphthylene; R.sub.8 is a hydrogen atom or alkyl of 1-5 carbon atoms; ##STR2## when R.sub.2 is hydroxy and R.sub.3 is a hydrogen atom or is ##STR3## or -CH=CH- when R.sub.2 and R.sub.3 collectively are an oxygen atom; or, when R.sub.1 is carboxy, a physiologically acceptable salt thereof with a base, possess the activity of the corresponding natural prostaglandins, including a luteolytic effect, and are useful in triggering abortions and syncronizing the conception cycle of mammals.
摘要翻译：其中R1是羟甲基，羧基，芳氧基羰基，烷氧基中1-8个碳原子的烷氧基羰基或基团-COO-CH2-UV，其中U是直接的CC键，羰基或羰基氧基和V 是被苯基，1-2个碳原子的烷氧基或卤素取代的苯基; R2是羟基，R3是氢原子，R2和R3一起是氧原子; A是-CH 2 -CH 2或反式-CH = CH; B是-CH 2 -CH 2或CH = CH; R4和R5之一是羟基，另一个是氢原子; R6和R7各自为1-10个碳原子的烷基，或者统称为至多7个碳原子的亚烷基，链中有2-3个碳原子，亚苯基或亚萘基; R8是氢原子或1-5个碳原子的烷基; 当R2和R3共同为氧原子时，当R 2为羟基且R 3为氢原子或者为或者-CH = CH-时，或者，当R 1为羧基时，其与碱的生理上可接受的盐具有相应的天然前列腺素的活性，包括溶血性作用，并且可用于触发哺乳动物的受孕循环的流产和同步化。

2. 发明授权

US4154953A Crystalline prostanoic acid esters 失效
标题翻译：结晶前列腺酸酯
公开(公告)号：US4154953A
公开(公告)日：1979-05-15
申请号：US826908
申请日：1977-08-19
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostanoic acid esters of the formulaPG-- CH.sub.2 -- X-- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.
摘要翻译：式PG-CH2-X-Y的前列腺酸，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰氧基，Y是取代的苯基，容易结晶化合物至少与通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素原子，X和Y具有上面给出的值。

3. 发明授权

US3962218A Novel prostanoic acid derivatives and processes for the preparation thereof 失效
标题翻译：新型乳酸衍生物及其制备方法
公开(公告)号：US3962218A
公开(公告)日：1976-06-08
申请号：US472738
申请日：1974-05-23
申请人： Bernd Raduchel , Werner Skuballa , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Bernd Raduchel , Werner Skuballa , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D317/30 , C07D317/54 , C07D319/06 , C07C177/00 , C07D317/12 , C07D317/50 , C07D319/04
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07D317/30 , C07D317/54 , C07D319/06
摘要： Prostaglandins of the formula ##SPC1##Wherein R.sub.1 is HOCH.sub.2, --COOH, a salt thereof or an ester thereof; R.sub.2 is OH; and R.sub.3 is H or R.sub.2 and R.sub.3 collectively are = O. A is --CH.sub. 2 --CH.sub.2 -- or --(trans)--CH=CH--, B is --CH.sub. 2 CH.sub.2 --or --(cis)--CH=CH-- and R.sub.4 --O--O--R.sub.5 is a ketal group, are superior in physiological activity to the corresponding 15-.alpha.-hydroxy-prostaglandins.

4. 发明授权

US3984454A Crystalline prostanoic acid esters 失效
标题翻译：结晶前列腺酸酯
公开(公告)号：US3984454A
公开(公告)日：1976-10-05
申请号：US466173
申请日：1974-05-02
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Wolfgang Losert
IPC分类号： A61K31/557 , A61K31/5575 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostanoic acid esters of the formulaPG -- CH.sub.2 -- X -- Ywherein PG is the prostanoyloxy radical of a prostaglandin, X is a carbon-carbon single bond, carbonyl or carbonyloxy, and Y is substituted phenyl are easily crystallized compounds at least as active as the unesterified prostanoic acid and useful for the purification of the parent prostaglandin are prepared by reacting, in the presence of an agent which splits off hydrogen halide, the unesterified prostaglandin with a halide of the formula Hal--CH.sub.2 --X--Y, wherein Hal is a halogen atom and X and Y have the values given above.
摘要翻译：式PG-CH2-X-Y的前列腺酸酯，其中PG是前列腺素的前烷氧基自由基，X是碳 - 碳单键，羰基或羰基氧基，Y是取代的苯基，其容易结晶化合物至少与通过使未分解的前列腺素与式Hal-CH2-XY的卤化物反应，其中Hal是卤素，其中Hal是卤素原子，X和Y具有上面给出的值。

5. 发明授权

US4088775A 15-Ethylenedioxy-prostanoic acid derivatives and esters thereof and intermediates thereof 失效
标题翻译： 15-亚乙二氧基 - 前列腺酸衍生物及其酯及其中间体
公开(公告)号：US4088775A
公开(公告)日：1978-05-09
申请号：US595015
申请日：1975-07-11
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07D407/04 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D317/00 , C07D317/30 , C07D317/46 , C07F9/535 , C07F9/655 , A61K31/335 , A61K31/36
CPC分类号： C07C405/00 , C07D317/30
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl of 1-10 carbon atoms, aryl or --CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy and V is phenyl or substituted phenyl, e.g. substituted by at least one of phenyl, alkoxy of 1-2 carbon atoms or a halogen atom; one of R.sub.2 and R.sub.3 is hydroxy and the other is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH; B is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH; D and E collectively are a direct bond, or D is alkylene or 1-5 carbon atoms and E is an oxygen or sulfur atom; R.sub.4 is alkyl of 1-10 carbon atoms, alkyl of 1-5 carbon atoms substituted by unsubstituted or substituted aryl, unsubstituted or substituted aryl, or benzodioxol-2-yl-; X--Y is ##STR2## when one of R.sub.2 and R.sub.3 is a hydroxy group and the other is a hydrogen atom or X--Y is ##STR3## or --CH.dbd.CH-- when R.sub.2 and R.sub.3 collectively are an oxygen atom; and when R.sub.1 is a hydrogen atom, the physiologically acceptable salts thereof with bases, have an activity spectrum similar to but stronger and longer lasting activity than the corresponding natural prostaglandins.
摘要翻译：其中R1是氢原子，1-10个碳原子的烷基，芳基或-CH2-U-V，其中U是直接键，羰基或羰氧基，V是苯基或取代的苯基，例如，被苯基，1-2个碳原子的烷氧基或卤素原子中的至少一个取代; R2和R3之一是羟基，另一个是氢原子，R2和R3共同是氧原子; A是-CH 2 -CH 2 - 或反-CH = CH; B是-CH 2 -CH 2 - 或顺式-CH = CH; D和E共同是直接键合，或D是亚烷基或1-5个碳原子，E是氧或硫原子; R4是1-10个碳原子的烷基，1-5个碳原子的烷基被未取代或取代的芳基，未取代或取代的芳基或苯并间二氧杂环戊烯-2-基取代; 当R2和R3中的一个是氧原子时，当R 2和R 3中的一个是羟基，另一个是氢原子或X-Y是<或>时，X-Y是当R1是氢原子时，其与碱的生理上可接受的盐具有与相应的天然前列腺素相似但更强和更持久的活性的活性谱。

6. 发明授权

US4219479A 5-Cyano-prostacyclin derivatives 失效
标题翻译： 5-氰基前列环素衍生物
公开(公告)号：US4219479A
公开(公告)日：1980-08-26
申请号：US963240
申请日：1978-11-24
申请人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
发明人： Helmut Vorbruggen , Werner Skuballa , Bernd Raduchel , Wolfgang Losert , Olaf Loge , Bernd Muller , Gerda Mannesmann
IPC分类号： A61K31/557 , A61K31/34 , A61K31/343 , A61K31/5575 , A61P1/04 , A61P7/02 , A61P9/12 , A61P11/00 , C07C405/00 , C07D307/935 , C07D307/937 , A61K31/335 , C07D307/93
CPC分类号： C07D307/937
摘要： Stabilized prostacyclins having a wide range of pharmacological activity and long duration of such activity, have the formula ##STR1## wherein R.sub.1 is (a) OR.sub.3, wherein R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl or a heterocyclic residue; or (b) NHR.sub.4 wherein R.sub.4 is an acid residue;B is straight-chain or branched alkylene of 2-10 carbon atoms;A is --CH.sub.2 --CH.sub.2 --, cis--CH.dbd.CH--, 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 and E together are a direct bond; orD is straight-chain or branched alkylene of 1-5 carbon atoms; andE is oxygen or sulfur or a direct bond,R.sub.2 is alkyl, cycloalkyl, optionally substituted aryl or a heterocyclic group; andR.sub.5 is free or functionally modified hydroxy; and when R.sub.3 is hydrogen, the salts thereof with physiologically compatible bases.
摘要翻译：具有广泛的药理活性和长时间的这种活性的稳定的前列环素具有下式（IMAGE），其中R1是（a）OR3，其中R3是氢，烷基，环烷基，芳基或杂环残基; 或（b）NHR 4，其中R 4是酸残基; B是2-10个碳原子的直链或支链亚烷基; A是-CH 2 -CH 2 - ，顺式-CH = CH-，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，其中OH-基团可以是在alpha或beta位置; D和E一起是直接的债券; 或D是1-5个碳原子的直链或支链亚烷基; 并且E是氧或硫或直接键，R 2是烷基，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; 并且当R3是氢时，其盐与生理上相容的碱基。

7. 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。

8. 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。

9. 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。

10. 发明授权

US4699920A 9-halo-2-prostaglandin derivatives, processes for the preparation thereof and use thereof as medicinal agents 失效
标题翻译： 9-卤-2-前列腺素衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4699920A
公开(公告)日：1987-10-13
申请号：US770350
申请日：1985-09-17
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge
IPC分类号： C07C401/00 , A61K31/557 , A61K31/5575 , A61P1/04 , A61P7/02 , A61P9/08 , A61P9/12 , A61P11/08 , A61P13/02 , A61P15/00 , C07C67/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0041 , C07C405/00
摘要： The invention relates to 9-halo-.DELTA..sup.2 -prostane derivatives of general Formula I ##STR1## wherein Hal is a fluorine or chlorine atom in the .alpha.- or .beta.-position,R.sub.1 is the residue OR.sub.2 with R.sub.2 meaning a hydrogen atom, alkyl, cycloalkyl, aryl or a heterocyclic residue; or the residue NHR.sub.3 wherein R.sub.3 means an acid residue or the residue R.sub.2 andA is a --CH.sub.2 --CH.sub.2 -- or cis-CH.dbd.CH--group,B is a --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH-- or --C.tbd.C--group,W is a free or functionally modified hydroxymethylene or ##STR2## wherein the respective OH-groups can be in the .alpha.- or .beta.-position,D and E jointly mean a direct bond orD is a straight- or branched-chain alkylene group of 1-10 carbon atoms, which can optionally be substituted by fluorine atoms,E is an oxygen or sulfur atom, a direct bond, a --C.tbd.C--bond or a --CR.sub.6 .dbd.CR.sub.7 --group wherein R.sub.6 is a hydrogen atom or an alkyl group and R.sub.7 is a hydrogen atom, an alkyl group or a halogen atom,R.sub.4 is a free or functionally modified hydroxy group,R.sub.5 is a hydrogen atom, an alkyl group, a halogen-substituted alkyl group, a cycloalkyl group, an optionally substituted aryl group, or a heterocyclic group,and, if R.sub.2 means a hydrogen atom, the salts thereof with physiologically compatible bases.
摘要翻译： PCT No.PCT / DE84 / 00280 Sec。 371日期：1985年9月17日 102（e）日期1985年9月17日PCT提交1984年12月21日PCT公布。出版物WO85 / 02841 日期：1985年7月4日本发明涉及通式Ⅰ（I）的9-卤代-TATA 2-前列腺衍生物，其中Hal是α-或β-位中的氟或氯原子，R1是残基OR2与R2表示氢原子，烷基，环烷基，芳基或杂环残基; 或残基NHR 3，其中R 3表示酸残基或残基R2和A是-CH 2 -CH 2 - 或顺式-CH = CH-基团，B是-CH 2 -CH 2 - 或反式-CH = CH-或-C 第三个C基团，W是游离的或官能改性的羟基亚甲基或者其中相应的OH基团可以是α-或β-位，D和E共同指直接键或D是直链或支链可以任选被氟原子取代的1-10个碳原子的链状亚烷基，E是氧或硫原子，直接键，-C 3 C C键或-CR 6 = CR 7 - 基，其中R 6是氢原子或烷基，R 7为氢原子，烷基或卤素原子，R 4为游离或官能改性的羟基，R 5为氢原子，烷基，卤素取代的烷基，环烷基，任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱的盐。

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