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21. 发明授权

US4415746A 16-Aryloxy-17,18,19,20-tetranorprostanoic acids and derivatives 失效
标题翻译： 16-芳氧基-17,18,19,20-四前列醇及其衍生物
公开(公告)号：US4415746A
公开(公告)日：1983-11-15
申请号：US308658
申请日：1981-10-05
申请人： Charles V. Grudzinskas , Martin J. Weiss
发明人： Charles V. Grudzinskas , Martin J. Weiss
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This disclosure describes novel 16-aryloxy-17,18,19,20-tetranoprostanoic acids and derivatives thereof useful as bronchodilators and as hypotensive and contraceptive agents.
摘要翻译：本公开描述了用作支气管扩张剂的新型16-芳氧基-17,18,19,20-四硝基前列腺酸及其衍生物，并且作为降血压和避孕药。

22. 发明授权

US4387241A Novel 16-aryloxy-17,18,19,20-tetranorprostanoic acids and derivatives 失效
标题翻译：新型的16-芳氧基-17,18,19,20-四前列醇及其衍生物
公开(公告)号：US4387241A
公开(公告)日：1983-06-07
申请号：US520064
申请日：1974-11-01
申请人： Charles V. Grudzinskas , Martin J. Weiss
发明人： Charles V. Grudzinskas , Martin J. Weiss
IPC分类号： A61K31/21 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This disclosure describes novel 16-aryloxy-17,18,19,20-tetranorprostanoic acids and derivatives thereof useful as bronchodilators and as hypotensive and contraceptive agents.
摘要翻译：本公开描述了用作支气管扩张剂的新颖的16-芳氧基-17,18,19,20-四 - 前列家酸及其衍生物，并且作为降血压和避孕药。

23. 发明授权

US4358605A 15-Deoxy-16-hydroxy-16-vinyl and cyclopropyl substituted prostanoic acids and congeners 失效
公开(公告)号：US4358605A
公开(公告)日：1982-11-09
申请号：US147910
申请日：1980-05-08
申请人： Middleton B. Floyd, Jr. , Martin J. Weiss , Charles V. Grudzinskas , Sow-Mei L. Chen
发明人： Middleton B. Floyd, Jr. , Martin J. Weiss , Charles V. Grudzinskas , Sow-Mei L. Chen
IPC分类号： C07C29/10 , C07C29/40 , C07C29/42 , C07C45/29 , C07C49/203 , C07C49/227 , C07C49/293 , C07C405/00 , C07F7/18 , C07F7/22 , C07C177/00
CPC分类号： C07F7/2212 , C07C29/10 , C07C29/40 , C07C29/42 , C07C405/00 , C07C45/29 , C07C49/203 , C07C49/227 , C07C49/293 , C07F7/1804 , C07F7/1896 , C07C2102/02
摘要： This disclosure describes novel 15-deoxy-16-hydroxy-16- substituted prostanoic acids and congeners thereof having utility as bronchodilators as hypotensive agents, and as agents for the control of excessive gastric secretion, and particularly, alkyl esters, such as the methyl ester, of such acids.

24. 发明授权

US4328359A 15-Deoxy-16-substituted-19-chloro-20-nor-prostane derivatives of the E and F series 失效
标题翻译： E和F系列的15-脱氧-16-取代-19-氯-20-去 - 前列腺衍生物
公开(公告)号：US4328359A
公开(公告)日：1982-05-04
申请号：US233044
申请日：1981-02-10
申请人： Allan Wissner
发明人： Allan Wissner
IPC分类号： C07C29/42 , C07C45/45 , C07C405/00 , C07F7/08 , C07F7/18 , C07F7/22 , C07C177/00
CPC分类号： C07F7/2212 , C07C29/42 , C07C405/00 , C07C405/0025 , C07C45/45 , C07F7/0818 , C07F7/1804
摘要： The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E and F series wherein C-16 is substituted with hydrogen, methyl, vinyl or ethynyl and C-19 substituted with chloro and the .beta.-chain consists of 7 carbon atoms.
摘要翻译：本文公开的本发明涉及E和F系列的药理学活性前列腺素衍生物，其中C-16被氢，甲基，乙烯基或乙炔基取代，C-19被氯取代，β-链由7个碳原子组成。

25. 发明授权

US4322435A Prostacyclin compounds 失效
标题翻译：前列环素化合物
公开(公告)号：US4322435A
公开(公告)日：1982-03-30
申请号：US153825
申请日：1980-05-27
申请人： Koichi Kojima , Kiyoshi Sakai , Shinsaku Kobayashi
发明人： Koichi Kojima , Kiyoshi Sakai , Shinsaku Kobayashi
IPC分类号： C07C69/732 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/23 , A61K31/557 , A61P7/02 , C07C29/147 , C07C47/198 , C07C49/633 , C07C49/743 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/38 , C07C67/00 , C07C69/73 , C07C69/757 , C07C405/00 , C07D309/12 , C07D317/72 , C07D407/12 , C07C177/00
CPC分类号： C07D317/72 , C07C29/147 , C07C309/00 , C07C405/00 , C07C405/0083 , C07C49/633 , C07C49/743 , C07C62/38 , C07D309/12 , C07C2101/16 , Y02P20/55
摘要： Prostacyclin derivatives of formula (I): ##STR1## (wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an alkenyl group having from 8 to 12 carbon atoms; and n represents an integer of from 1 to 8, inclusive) and pharmaceutically acceptable salts thereof, are valuable pharmaceuticals, showing excellent thrombocyte agglutination inhibitory, coronary blood vessel dilatory and bronchodilatory effects, and may be prepared by introducing the .dbd.CH(CH.sub.2).sub.n COOR.sup.1 side chain onto an appropriate compound by means of a Wittig reaction.
摘要翻译：式（I）的前列环素衍生物：其中，R1表示氢原子或低级烷基，R2表示碳原子数为8〜12的烯基，n表示1〜8的整数，包括）和其药学上可接受的盐是有价值的药物，显示优异的凝血细胞凝集抑制，冠状动脉血管扩张和支气管扩张作用，并且可以通过将= CH（CH 2）n COOR 1侧链通过维蒂希反应。

26. 发明授权

US4321405A 15,16-Dioxy prostenoic acids and esters 失效
标题翻译： 15,16-二氧基前列腺酸和酯
公开(公告)号：US4321405A
公开(公告)日：1982-03-23
申请号：US142593
申请日：1980-04-21
申请人： Martin J. Weiss
发明人： Martin J. Weiss
IPC分类号： C07C405/00 , C07D309/12 , C07D317/12 , C07D317/16 , C07D317/30 , C07F7/18 , C07C177/00
CPC分类号： C07D317/16 , C07C405/00 , C07D309/12 , C07D317/12 , C07D317/30 , C07F7/1804
摘要： This disclosure describes novel erythro 15,16-dioxy prostenoic acids and esters useful as bronchodilators, hypotensives and gastric acid secretion inhibitors.
摘要翻译：本公开描述了用作支气管扩张剂，低血糖剂和胃酸分泌抑制剂的新型的赤式15,16-二氧基前列腺酸和酯。

27. 发明授权

US4315032A Process for preparation of adjacently disubstituted ketones 失效
标题翻译：相邻二取代酮制备方法
公开(公告)号：US4315032A
公开(公告)日：1982-02-09
申请号：US149584
申请日：1980-05-14
申请人： Ryoji Noyori , Masaaki Suzuki , Seizi Kurozumi
发明人： Ryoji Noyori , Masaaki Suzuki , Seizi Kurozumi
IPC分类号： C07B37/02 , A61K31/557 , C07B31/00 , C07C45/00 , C07C45/69 , C07C45/70 , C07C45/72 , C07C45/75 , C07C49/493 , C07C49/517 , C07C49/743 , C07C49/747 , C07C49/753 , C07C67/00 , C07C225/20 , C07C401/00 , C07C405/00 , C07D309/12 , C07F7/18 , C07C177/00
CPC分类号： C07F7/1856 , A61K31/557 , C07C225/20 , C07C405/00 , C07C405/0025 , C07C45/70 , C07C45/72 , C07C45/75 , C07C49/493 , C07C49/743 , C07C49/747
摘要： A novel 7-hydroxyprostaglandin E.sub.1, or a stereoisomer thereof, or a protected derivative thereof, having the following formula: ##STR1## wherein R.sup.8 represents H, CH.sub.3 or C.sub.2 H.sub.5, R.sup.9 represents H or CH.sub.3, R.sup.10 and R.sup.11 are identical or different, and each represents H, tetrahydropyranyl or t-butyldimethylsilyl. Also provided is a process for producing an adjacently disubstituted ketone including the above compounds, i.e. 7-oxoprostaglandin, etc. which comprises reacting an .alpha.,.beta.-unsaturated carbonyl compound with a cuprous salt and an organolithium compound in an aprotic inert organic medium in the presence of trialkylphosphine, the amounts of said cuprous salt and said organolithium compound being substantially equimolar, and reacting the product with a protected acetal derivative of an organic carbonyl compound or an aldehyde in the presence of a Lewis acid, if necessary, followed by reacting the product with a proton donor.
摘要翻译：具有下式的新颖的7-羟基前列腺素E1或其保护的衍生物：其中R 8表示H，CH 3或C 2 H 5，R 9表示H或CH 3，R 10和R 11相同或不同，各自表示H，四氢吡喃基或叔丁基二甲基甲硅烷基。还提供了制备包括上述化合物即7-氧代前列腺素等的相邻二取代的酮的方法，其包括使α，β-不饱和羰基化合物与亚硝酸盐和有机锂化合物在非质子惰性有机介质中反应存在三烷基膦，所述亚铜盐和所述有机锂化合物的量基本上是等摩尔的，并且如果需要，在路易斯酸存在下，使产物与有机羰基化合物或醛的保护缩醛衍生物反应，然后使产品与质子供体。

28. 发明授权

US4309351A Chemical synthesis 失效
标题翻译：化学合成
公开(公告)号：US4309351A
公开(公告)日：1982-01-05
申请号：US118266
申请日：1980-02-04
申请人： Josef Fried
发明人： Josef Fried
IPC分类号： C07C29/42 , C07C271/06 , C07C405/00 , C07D307/935 , C07C177/00
CPC分类号： C07D307/935 , C07C271/06 , C07C29/42 , C07C405/00 , C07C405/0016 , C07C405/0033 , C07C2101/10
摘要： This invention relates to compounds of the formulae ##STR1## wherein n is an integer from 2 to 5; M is H, acyl, lower alkyl, or lower alkoxy alkyl; Q is H or lower alkyl; R is alkyl, alkenyl or analkyl; A is H; Y is OH, acyloxy or alkoxy, and when taken together, Y and A is oxo (O.dbd.), and to novel intermediates therefore.
摘要翻译：本发明涉及下式化合物：其中n为2至5的整数; M是H，酰基，低级烷基或低级烷氧基烷基; Q是H或低级烷基; R是烷基，烯基或烷基; A是H; Y是OH，酰氧基或烷氧基，当Y和A一起是氧代（O =）时，因此也是新的中间体。

29. 发明授权

US4306095A Prostane derivatives 失效
标题翻译：前列腺衍生物
公开(公告)号：US4306095A
公开(公告)日：1981-12-15
申请号：US95306
申请日：1979-11-19
申请人： Jean Bowler
发明人： Jean Bowler
IPC分类号： A61K31/075 , A61K31/12 , A61K31/19 , A61P43/00 , B01J31/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C07C177/00
CPC分类号： C07D309/12 , C07C405/00 , C07C405/0016 , C07C405/0025 , Y10S514/822
摘要： The disclosure relates to novel 4-cis-prostenoic acid derivatives, for example 16-(3-chlorophenoxy)-9.alpha.,11.alpha.,15-trihydroxy-17,18,19,20-tetranor-4-cis, 13-trans-prostadienoic acid, to chemical processes for their manufacture, to pharmaceutical and veterinary compositions containing them, and to the use of the compounds in a method of luteolysis, a method of inhibiting blood platelet aggregation, and a method of inhibiting gastric acid production.
摘要翻译：本公开涉及新的4-顺式 - 前列宁酸衍生物，例如16-（3-氯苯氧基）-9α，11α，15-三羟基-17,18,19,20-四去甲-4-顺式，13-反式 - 前列腺素酸，其制备的化学方法，含有它们的药物和兽用组合物，以及在骨溶解方法中使用该化合物，抑制血小板聚集的方法以及抑制胃酸生产的方法。

30. 发明授权

US4304926A Phenacyl-type esters of PGE-types compounds 失效
标题翻译： PGE型化合物的苯甲酰型酯
公开(公告)号：US4304926A
公开(公告)日：1981-12-08
申请号：US497244
申请日：1974-08-14
申请人： Walter Morozowich
发明人： Walter Morozowich
IPC分类号： A61K31/21 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Phenacyl-type esters of PGE.sub.2, PGE.sub.1, and 13,14-dihydro-PGE.sub.1 and their 15-methyl, 16,16-dimethyl, and 17-phenyl analogs, including the respective 15(R)epimers, are disclosed, represented by the formula ##STR1## wherein M is ##STR2## wherein R.sub.3 is hydrogen or methyl; wherein Q is ##STR3## wherein each of R.sub.4 and R.sub.5 is hydrogen or methyl, being the same or different, or ##STR4## wherein the moiety--C.sub.t H.sub.2t -- represents a valence bond or alkylene of one to 10 carbon atoms, inclusive, with one to 7 carbon atoms, inclusive, between ##STR5## and the phenyl ring; wherein R.sub.1 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl; wherein R.sub.2 is hydrogen or benzoyl; and wherein (a) X is --CH.sub.2 CH.sub.2 -- or trans--CH.dbd.CH-- and Y is --CH.sub.2 CH.sub.2 --, or (b) X is trans--CH.dbd.CH-- and Y is cis--CH.dbd.CH--. The products are useful for the same pharmacological and medical purposes as the corresponding prostaglandins and analogs, and are also useful as a means for obtaining highly purified products.
摘要翻译： PGE2，PGE1和13,14-二氢-PGEE及其15-甲基，16,16-二甲基和17-苯基类似物（包括相应的15（R）差向异构体）的苯甲酰基型酯被公开，由其中M为，其中R 3为氢或甲基; 其中Q为（1），其中R 4和R 5各自为氢或甲基，相同或不同，或其中部分-CtH 2 t表示价键或1至10碳的亚烷基含有1到7个碳原子的原子，包括端值在＆lt; IMAGE＆gt;和苯环之间; 其中R1是苯基，对溴苯基，对联苯基，对硝基苯基，对苯甲酰胺基苯基或2-萘基; 其中R2是氢或苯甲酰基; 并且其中（a）X是-CH 2 CH 2 - 或反式-CH = CH-，Y是-CH 2 CH 2 - ，或（b）X是反式-CH = CH-，Y是顺式-CH = CH-。该产品可用于与相应的前列腺素和类似物相同的药理和医学目的，并且也可用作获得高纯度产品的手段。

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