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21.发明授权
公开(公告)号：US4092427A
公开(公告)日：1978-05-30
申请号：US696245
申请日：1976-06-15
IPC分类号： C07C405/00 , C07F9/40 , C07F9/54 , A61K31/19 , A61K31/215
CPC分类号： C07F9/5407 , C07C405/00 , C07F9/4006
摘要： 15- And/or 16-alkyl derivatives of 9,15-dioxygenated prost-13-enoic, prosta-4,13-dienoic and prosta-5,13-dienoic acid, lower alkyl esters thereof and homologs thereof, as well as a process for preparing these derivatives are disclosed. The compounds possess hypotensive, anti-hypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. The compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及 公开了制备这些衍生物的方法。 该化合物具有降血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节特性。 该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。 还公开了它们的使用方法。
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公开(公告)号：US4048329A
公开(公告)日：1977-09-13
申请号：US696328
申请日：1976-06-15
IPC分类号： C07C405/00 , C07F9/40 , C07F9/54 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07F9/4006 , C07C405/00 , C07F9/5407
摘要： 15- And/or 16-alkyl derivatives of 9,15-dioxygenated prost-13-enoic, prosta-4,13-dienoic and prosta-5,13-dienoic acid, lower alkyl esters thereof and homologs thereof, as well as a process for preparing these derivatives are disclosed. The compounds possses hypotensive, antihypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. The compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及 公开了制备这些衍生物的方法。 化合物降血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节性质。 该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。 还公开了它们的使用方法。
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公开(公告)号：US4036856A
公开(公告)日：1977-07-19
申请号：US741096
申请日：1976-11-11
IPC分类号： C07C405/00 , C07D307/88
CPC分类号： C07C405/00
摘要： A process for preparing 11-deoxyprostaglandin E.sub.1, E.sub.2 and E.sub.3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared from a Wittig reagent of formula (AlkO).sub.2 POCH.sub.2 CO-(c)-CH.sub.3 in which Alk is an alkyl containing one to three carbon atoms and (c) is either (CH.sub.2).sub.q wherein q is an integer from 1 to 6 or cis CH.sub.2 CH=CH(CH.sub.2).sub.r wherein r is an integer from 0 to 3 to obtain the corresponding compound of formula: ##STR1## in which R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl, R.sup.4 is lower alkyl and (c) is as defined herein. The latter compound is reduced with an alkali metal borohydride to yield the corresponding alcohol derivative. Condensation of this alcohol derivative or preferably its corresponding tetrahydropyran-2-yl ether derivative with a triester of formula CH(COOR.sup.6).sub.2 --(a)-(CH.sub.2)pCOOR in which R and R.sup.6 are lower alkyl, (a) is CH.sub.2 CH.sub.2, cis CH=CH or C.tbd.C and p is an integer from 2 to 4, gives the corresponding cyclopentanonetriester of formula ##STR2## in which (a), (c), p, R, R.sup.4 and R.sup.6 are as defined herein, R.sup.5 is hydrogen or tetrahydropyran-2-yl, respectively, and R.sup.7 is hydrogen or lower alkyl; the lactonized form of the cyclopentanonetriester being obtained from said alcohol derivative in which R.sup.2 is CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl. In the instance when R.sup.5 is tetrahydropyran-2-yl the cyclopentanonetriester is treated with an acid to give the corresponding compound in which R.sup.5 is hydrogen. The instant compound is then treated with a base under aqueous conditions, followed by optional esterification and acylation to give the desired 11-deoxyprostaglandin derivatives of formula ##STR3## in which (a), (c) and p, are as defined herein, (b) is trans CH=CH, R is hydrogen or lower alkyl, R.sup.1 is hydrogen or lower alkanoyl and R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is hydrogen or lower alkanoyl. The derivatives possess prostaglandin-like biological activity and methods for their use are given.
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公开(公告)号：US4006136A
公开(公告)日：1977-02-01
申请号：US489856
申请日：1974-07-19
IPC分类号： C07C45/67 , C07C49/20 , C07C49/203 , C07C405/00 , C07C69/74
CPC分类号： C07C405/00 , C07C45/673 , C07C49/20 , C07C49/203
摘要： A process for preparing 11-deoxyprostaglandin E.sub.1, E.sub.2 and E.sub.3 and analogs thereof is realized by treating an appropriate di(lower)alkyl 3-(optionally substituted)-2-formylcyclopropane-1,1-dicarboxylate with an ylid prepared from a Wittig reagent of formula (AlkO).sub.2 PCCH.sub.2 CO-(c)-CH.sub.3 in which Alk is an alkyl containing one to three carbon atoms and (c) is either (CH.sub.2).sub.q wherein q is an integer from 1 to 6 or cis CH.sub.2 CH=CH(CH.sub.2).sub.r wherein r is an integer from 0 to 3 to obtain the corresponding compound of formula: ##STR1## in which R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl, R.sup.4 is lower alkyl and (c) is as defined herein. The latter compound is reduced with an alkali metal borehydride to yield the corresponding alcohol derivative. Condensation of this alcohol derivative or preferably its corresponding tetrahydropyran-2-yl ether derivative with a triester of formula CH(COOR.sup.6).sub.2 -(a)-(CH.sub.2)pCOOR in which R and R.sup.6 are lower alkyl, (a) is CH.sub.2 CH.sub.2, cis CH=CH or CaC and p is an integer from 2 to 4, gives the corresponding cyclopentanonetriester of formula ##STR2## in which (a), (c), p, R, R.sup.4 and R.sup.6 are as defined herein, R.sup.5 is hydrogen or tetrahydropyran-2-yl, respectively, and R.sup.7 is hydrogen or lower alkyl; the lactonized form of the cyclopentanone-triester being obtained from said alcohol derivative in which R.sup.2 is CH.sub.2 OR.sup.3 wherein R.sup.3 is lower alkanoyl. In the instance when R.sup.5 is tetrahydropyran-2-yl the cyclopentanonetriester is treated with an acid to give the corresponding compound in which R.sup.5 is hydrogen. The instant compound is then treated with a base under aqueous conditions, followed by optional esterification and acylation to give the desired 11-deoxy-prostaglandin derivatives of the formula ##STR3## in which (a), (c) and p, are as defined herein, (b) is trans CH=CH, R is hydrogen or lower alkyl, R.sup.1 is hydrogen or lower alkanoyl and R.sup.2 is hydrogen, lower alkyl or CH.sub.2 OR.sup.3 wherein R.sup.3 is hydrogen or lower alkanoyl. The derivatives possess prostaglandin-like biological activity and methods for their use are given.
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25.发明授权Resolution of (.+-.)-1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid using cinchonine 失效使用辛可宁拆分（+/-） - 1,8-二乙基-1,3,4,9-四氢吡喃并[3,4-b]吲哚-1-乙酸
公开(公告)号：US4520203A
公开(公告)日：1985-05-28
申请号：US523987
申请日：1983-08-16
IPC分类号： C07D491/04 , C07D491/052 , C07D493/04
CPC分类号： C07D491/04
摘要： Racemic (.+-.)-1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid is resolved with cinchonine to obtain directly the pure salt of the (+)-enantiomer with cinchonine and converting the latter salt to the pure (+)-enantiomer.
摘要翻译： 外消旋（+/-） - 1,8-二乙基-1,3,4,9-四氢吡喃并[3,4-b]吲哚-1-乙酸用辛可宁解决，直接得到（+） - 对映异构体与辛可宁，并将后一种盐转化为纯（+） - 对映异构体。
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公开(公告)号：US4048328A
公开(公告)日：1977-09-13
申请号：US696453
申请日：1976-06-15
IPC分类号： C07C405/00 , C07F9/40 , C07F9/54 , A61K31/19 , A61K31/215 , C07C177/00
CPC分类号： C07F9/4006 , C07C405/00 , C07F9/5407
摘要： 15- And/or 16-alkyl derivatives of 9,15-dioxygenated prost-13-enoic, prosta-4,13-dienoic and prosta-5,13-dienoic acid, lower alkyl esters thereof and homologs thereof, as well as a process for preparing these derivatives are disclosed. The compounds possess hypotensive, anti-hypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. The compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及 公开了制备这些衍生物的方法。 该化合物具有降血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节特性。 该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。 还公开了它们的使用方法。
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公开(公告)号：US4011212A
公开(公告)日：1977-03-08
申请号：US641128
申请日：1975-12-15
CPC分类号： C07J41/0094
摘要： There are disclosed herein the 3.beta.,14-dihydroxy-, 3.beta.,5,14-trihydroxy-, 3.beta.,12.beta.,14-trihydroxy- and 3.beta.,14,16.beta.-trihydroxy-21,23-epoxy-23-methoxy-24-nor-5.beta.,14.beta.-chola-20,22-diene-22-carbonitriles, as well as their corresponding 3-acetates, 3-propionates and 3-butyrates and their 3-digitosides and 3.beta.-cyamarosyl-glucosides as encountered in naturally-occuring starting materials. The compounds possess useful cardiotonic activity. Also included are the corresponding 22-cyano-5.beta.-card-20(22)-enolides, useful as intermediates in the preparation of the compounds of this invention and also as cardiotonic agents.
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公开(公告)号：US4007171A
公开(公告)日：1977-02-08
申请号：US567036
申请日：1975-04-10
IPC分类号： C07C405/00 , C07F9/40 , C07F9/54 , C07C69/74
CPC分类号： C07F9/5407 , C07C405/00 , C07F9/4006
摘要： 15- And/or 16-alkyl derivatives of 9,15-dioxygenated prost-13-enoic, prosta-4,13-dienoic and prosta-5,13-dienoic acid, lower alkyl esters thereof and homologs thereof, as well as a process for preparing these derivatives are disclosed. The compounds possess hypotensive, antihypertensive, bronchospasmolytic, gastric acid secretion inhibiting, abortifacient, estrus synchronizing and ovulation regulating properties. The compounds also inhibit the aggregation of platelets and promote the disaggregation of aggregated platelets. Methods for their use are also disclosed.
摘要翻译： 9,15-双加氧前列腺-13-烯酸，前列腺-4,13-二烯酸和前列腺-5,13-二烯酸的15-和/或16-烷基衍生物，其低级烷基酯及其同系物，以及 公开了制备这些衍生物的方法。 该化合物具有低血压，抗高血压，支气管痉挛，胃酸分泌抑制，流产，发情同步和排卵调节特性。 该化合物还抑制血小板的聚集并促进聚集的血小板的解聚。 还公开了它们的使用方法。
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