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1. 发明授权

US4367237A Prostacyclin analogues 失效
公开(公告)号：US4367237A
公开(公告)日：1983-01-04
申请号：US097675
申请日：1979-11-27
申请人： Hirohisa Wakatsuka , Katsuichi Shimoji , Sadahiko Iguchi , Yoshitaka Konishi , Hisashi Suga , Yasuyuki Miyata , Yoichi Iguchi , Hajimu Miyake , Masaki Hayashi
发明人： Hirohisa Wakatsuka , Katsuichi Shimoji , Sadahiko Iguchi , Yoshitaka Konishi , Hisashi Suga , Yasuyuki Miyata , Yoichi Iguchi , Hajimu Miyake , Masaki Hayashi
IPC分类号： C07C405/00 , C07D333/78 , C07D335/04 , A61K31/38
CPC分类号： C07C405/0033 , C07C405/00 , C07D333/78 , C07D335/04
摘要： Prostaglandin analogues of the general formula: ##STR1## [wherein the ring A represents: ##STR2## the ring B represents: ##STR3## (wherein R.sup.6 represents hydrogen, methyl or ethyl, and r is zero, one or two), Y represents ethylene, cis- or trans-vinylene or ethynylene, Z represents a grouping of the formula: --(CH.sub.2).sub.m --, --(CH.sub.2).sub.3 --CHR.sup.7 --, --(CH.sub.2).sub.2 --CHR.sup.7 --CH.sub.2 --, --CH.sub.2 --CHR.sup.7 --(CH.sub.2).sub.2 --, --CHR.sup.7 --(CH.sub.2).sub.3 --, or trans--(CH.sub.2).sub.2 --CH.dbd.CH-- (wherein m is 3, 4 or 5, and R.sup.7 represents methyl or ethyl), R.sup.1 represents a grouping of the formula: --COOR.sup.8, ##STR4## or --CH.sub.2 OR.sup.11 (wherein R.sup.8 represents hydrogen, alkyl, aralkyl, cycloalkyl which is unsubstituted or substituted by at least one alkyl group, or R.sup.8 represents phenyl which is unsubstituted or substituted by halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or phenyl, or represents naphthyl, 2,3- or 1,3-dihydroxypropyl, 2,3- or 1,3-bisalkanoyloxypropyl, a grouping of the formula: -D.sub.1 --COOR.sup.12, ##STR5## -D.sub.2 -R.sup.15 or -D.sub.3 -R.sup.16, wherein D.sub.1 represents alkylene, D.sub.2 represents alkylene, D.sub.3 represents a single bond or alkylene, R.sup.12, R.sup.13 and R.sup.14, each represent alkyl, R.sup.15 represents hydroxy, alkoxy or alkylthio and R.sup.16 represents a heterocyclic ring, or R.sup.8 represents a grouping of the formula: ##STR6## R.sup.9 and R.sup.10, each represent hydrogen, alkyl, alkylsulphonyl, alkanoyl or ##STR7## represents a heterocyclic ring, and R.sup.11 represents hydrogen or alkanoyl, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond or alkylene, R.sup.4 represents hydrogen, alkyl, alkoxy, cycloalkyl or cycloalkyloxy unsubstituted or substituted by alkyl, or represents phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl with the proviso that, when R.sup.3 represents a single bond, R.sup.4 does not represent alkoxy, cycloalkyloxy or phenoxy, R.sup.5 represents hydrogen, methyl or ethyl and with the proviso that, when one of the groups R.sup.5, R.sup.6 and R.sup.7 represents methyl or ethyl the other two groups are hydrogen atoms] and cyclodextrin clathrates, non-toxic salts and non-toxic acid addition salts thereof, possess selective strong stimulatory activity on uterine contraction in female mammals.

2. 发明授权

US4034003A 15-Cycloalkyl-prostaglandins 失效
标题翻译： 15-环烷基 - 前列腺素
公开(公告)号：US4034003A
公开(公告)日：1977-07-05
申请号：US566147
申请日：1975-04-08
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Takashi Yamato , Hisashi Suga
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Takashi Yamato , Hisashi Suga
IPC分类号： C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07D309/12 , C07F9/4018 , Y10S514/822 , Y10S514/962
摘要： 15-Cycloalkyl-prostaglandins of the formula:- ##STR1## wherein A represents a grouping of the formula:- ##STR2## X represents ethylene of cis-vinylene, Y represents ethylene or trans-vinylene, B represents ethylene or trans-vinylene, R represents hydrogen or alkyl of 1 through 4 carbon atoms, R.sup.1 represents cycloalkyl of 4 through 7 carbon atoms, and R.sup.2 represents hydrogen or alkyl of 1 through 12 carbon atoms, are new compounds possessing the useful pharmacological properties typical of prostaglandins; they are of especial interest in the inhibition of blood platelet aggregation.
摘要翻译： 15-环烷基 - 前列腺素，其结构式如下：其中A表示下式的基团：X表示顺式 - 亚乙烯基的亚乙基，Y表示亚乙基或反式亚乙烯基，B表示亚乙基或反式亚乙烯基， R表示氢或1〜4个碳原子的烷基，R1表示4〜7个碳原子的环烷基，R2表示氢或1〜12个碳原子的烷基，是具有典型的前列腺素有用的药理学性质的新化合物; 它们对抑制血小板聚集具有特别的兴趣。

3. 发明授权

US4351846A 3-Hydroxy and 3-oxo-prostaglandin analogues 失效
标题翻译： 3-羟基和3-氧代 - 前列腺素类似物
公开(公告)号：US4351846A
公开(公告)日：1982-09-28
申请号：US262209
申请日：1981-05-08
申请人： Kimiichiro Matsumoto , Hajimu Miyake , Hisashi Suga
发明人： Kimiichiro Matsumoto , Hajimu Miyake , Hisashi Suga
IPC分类号： A61K31/557 , A61K31/5575 , A61K47/48 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： B82Y5/00 , A61K47/48969 , C07C405/00 , Y02P20/55 , Y10S514/843 , Y10S514/899
摘要： Prostaglandin analogues of the formula: ##STR1## [wherein R.sup.1 represents hydrogen or alkyl of 1 to 12 carbon atoms, R.sup.2 represents a single bond or alkylene of from 1 to 5 carbon atoms, R.sup.3 represents hydrogen, alkyl or alkoxy of 1 to 8 carbon atoms, cycloalkyl or cycloalkyloxy of 4 to 7 carbon atoms unsubstituted or substituted by alkyl of 1 to 8 carbon atoms, or phenyl or phenoxy unsubstituted or substituted by halogen, trifluoromethyl or alkyl of 1 to 4 carbon atoms, one of R.sup.4 and R.sup.5 represents hydrogen and the other represents hydroxy or R.sup.4 and R.sup.5 together represent oxo, R.sup.6 represents hydrogen or a hydroxy-protecting group which may be removed under acidic conditions, the double bond between the carbon atoms in positions 13 and 14 is trans, the wavy line attached to the carbon atom in position 15 represents .alpha.- or .beta.- configuration or a mixture thereof and, when one of R.sup.4 and R.sup.5 represents hydrogen and the other represents hydroxy, the configuration of the carbon atom in position 3 is R-- or S or a mixture thereof, provided that, when R.sup.2 represents a single bond, R.sup.3 does not represent alkoxy, cycloalkyloxy or phenoxy and when R.sup.6 represents a hydrogen atom, cyclodextrin clathrates thereof and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, possess selective prostaglandin-like properties.
摘要翻译：具有下式的前列腺素类似物：其中R 1表示氢或1至12个碳原子的烷基，R 2表示单键或1至5个碳原子的亚烷基，R 3表示氢，1至8个碳原子的烷基或烷氧基未取代或被1至8个碳原子的烷基取代的4至7个碳原子的原子，环烷基或环烷氧基，或未取代或被卤素，三氟甲基或1-4个碳原子的烷基取代的苯基或苯氧基，R4和R5之一表示氢另一个表示羟基或R 4和R 5一起代表氧代，R 6表示氢或可在酸性条件下除去的羟基保护基，13和14位的碳原子之间的双键是反式的，波浪线连接到位置15中的碳原子表示α或β-构型或其混合物，当R 4和R 5中的一个代表氢而另一个代表羟基时，位置上的碳原子的构型 n 3为R-或S或其混合物，条件是当R 2表示单键时，R 3不表示烷氧基，环烷氧基或苯氧基，当R6表示氢原子时，环糊精包合，当R1表示氢原子时，其无毒盐具有选择性的前列腺素样特性。

4. 发明授权

US4128720A Prostaglandin analogues 失效
标题翻译：前列腺素类似物
公开(公告)号：US4128720A
公开(公告)日：1978-12-05
申请号：US657125
申请日：1976-02-11
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： A61K31/23 , A61K31/557 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F1/00 , C07F1/02 , C08B37/16 , C07C177/00
CPC分类号： C07D307/935 , C07C321/00 , C07C405/00 , C07C405/0033 , C07F1/00 , C07F1/02
摘要： Prostaglandins of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, R.sup.2 represents a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms, or a grouping of the formula: ##STR3## wherein R.sup.4 and R.sup.5 each represents a hydrogen or halogen atom, a trifluoromethyl group or an alkyl group containing from 1 to 3 carbon atoms, or R.sup.2 and R.sup.3 together represent an ethylene or trimethylene group and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, non-toxic salts of such acids, are disclosed.These compounds exhibit characteristic prostaglandin activity, in particular, inhibitory activity on gastric secretion, luteolytic activity and so on.
摘要翻译：下式的前列腺素：其中A代表下式的组：其中X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基，R表示氢原子或直链，或含有1至12个碳原子的支链烷基，R 1表示氢原子或含有1至10个碳原子的直链或支链烷基，R 2表示直链或支链烷基， 1至4个碳原子，R 3表示含有1至4个碳原子的直链或支链烷基，含有4至7个碳原子的环烷基，或下式的组：其中R 4和 R5各自表示氢或卤素原子，三氟甲基或含有1至3个碳原子的烷基，或者R 2和R 3一起表示这些酸和酯的乙烯或三亚甲基和环糊精包合物，当R表示氢原子公开了这种酸的有毒盐。

5. 发明授权

US4140712A 20-Hydroxy-prostaglandins 失效
标题翻译： 20-羟基 - 前列腺素
公开(公告)号：US4140712A
公开(公告)日：1979-02-20
申请号：US547293
申请日：1975-02-05
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： C07D317/72 , B01J31/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D309/12 , C07F9/4006 , Y10S514/826 , Y10S514/929 , Y10S514/957 , Y10S514/962
摘要： The present invention relates to 20-hydroxy prostaglandins of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## and X represents ethylene or cis-vinylene and Y represents trans-vinylene, or X and Y each represent ethylene, R represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.1 , R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a methyl or ethyl group, and n represents zero or an integer from 1 to 3 inclusive, and cyclodextrin clathrates of such acids and esters and, when R represents a hydrogen atom, the non-toxic salts thereof.These compounds exhibit characteristic prostaglandin activity.
摘要翻译：本发明涉及下式的20-羟基前列腺素：其中A代表下式的组：其中X表示亚乙基或顺式 - 亚乙烯基，Y表示反式亚乙烯基，或X和Y各自表示乙烯，R表示氢原子或含有1至12个碳原子的直链或支链烷基，可以相同或不同的R 1，R 2，R 3，R 4和R 5各自表示氢原子或甲基或乙基，n表示0或1〜3的整数，以及这些酸和酯的环糊精包合物，当R表示氢原子时，为无毒性盐。

6. 发明授权

US4110341A Dithio prostaglandin derivatives 失效
标题翻译： Dithio前列腺素衍生物
公开(公告)号：US4110341A
公开(公告)日：1978-08-29
申请号：US765580
申请日：1977-02-04
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： A61K31/23 , A61K31/215 , A61K31/385 , A61K31/70 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07D339/04 , C08B37/16
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0033 , C07D309/12 , C07D339/04
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R.sup.1 represents a straight- or branched-chain alkyl group containing from 4 to 10 carbon atoms, and R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms and cyclodextrin clathrates of such acids and esters and, when R.sup.2 represents a hydrogen atom, non-toxic salts thereof, the bonds attaching the epidithio radical to the carbon atoms in the 9- and 11-positions in the grouping of formula VA being either botn in .alpha.-configuration or both in .beta.-configuration are disclosed.These compounds exhibit characteristic prostaglandin properties.
摘要翻译：（IV）的前列腺素类似物：其中A表示下式的基团：（VI）或（IMA）（VB）X表示亚乙基或顺式亚乙烯基，Y表示亚乙基或反式亚乙烯基， R1表示含有4至10个碳原子的直链或支链烷基，R2表示氢原子或含有1至12个碳原子的直链或支链烷基和这些酸和酯的环糊精包合物并且当R2表示氢原子时，其无毒盐，附加硫代自由基与式VA组中9-和11位中的碳原子的键或者是以α-构型或两者均为β - 配置。

7. 发明授权

US4065632A 16-Phenoxy and phenylthio prostaglandin derivatives 失效
标题翻译： 16-苯氧基和苯硫基前列腺素衍生物
公开(公告)号：US4065632A
公开(公告)日：1977-12-27
申请号：US713941
申请日：1976-08-12
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Takanori Okada
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Takanori Okada
IPC分类号： A61K31/12 , A61K31/19 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C69/76
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0033 , C07D309/12 , C07F9/4006 , Y10S514/822 , Y10S514/826 , Y10S514/869 , Y10S514/927
摘要： The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents an oxygen or sulphur atom, R.sup.1 and R.sup.2, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group, or a straight- or branched-chain alkyl or alkoxy group containing from 1 to 4 carbon atoms, R represents a group of the formula --COOR.sup.3, in which R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.4, in which R.sup.4 represents a hydrogen atom or an alkylcarbonyl group containing from 2 to 5 carbon atoms and the double bonds depicted in positions C.sub.2 -C.sub.3, C.sub.5 -C.sub.6 and C.sub.13 -C.sub.14 are trans, cis and trans respectively, the cyclodextrin clathrates thereof and, when R.sup.3 in the group --COOR.sup.3 represents a hydrogen atom, non-toxic salts thereof. These compounds exhibit characteristics of prostaglandin-like activity.
摘要翻译：本发明涉及下式的化合物：其中A表示下式的基团：IV B表示氧或硫原子，R 1和R 2可以是相同或不同，各自表示氢或卤素原子，三氟甲基或含有1至4个碳原子的直链或支链烷基或烷氧基，R表示式-COOR 3的基团，其中R 3 表示氢原子或含有1至12个碳原子的直链或支链烷基，或式-CH 2OR 4基团，其中R 4表示氢原子或含有2至5个碳原子的烷基羰基，位置C2-C3，C5-C6和C13-C14中所示的双键分别是反式，顺式和反式，环糊精包合，当-COOR3基团中的R3表示氢原子时，其无毒盐。这些化合物表现出前列腺素样活性的特征。

8. 发明授权

US4018812A 16-METHYLENE-PROSTAGLANDIN COMPOUNDS 失效
标题翻译： 16-METHYLENE-PROSTAGLANDIN化合物
公开(公告)号：US4018812A
公开(公告)日：1977-04-19
申请号：US685953
申请日：1976-05-13
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： A61K31/23 , A61K9/08 , A61K31/215 , A61P43/00 , B01J31/00 , C07B61/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C08B37/16 , C12P31/00 , C07C177/00
CPC分类号： C07D309/12 , C07C405/00
摘要： A compound of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## , R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms, R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, X represents trans-vinylene or ethylene, and the wavy line indicates attachment of the hydroxy radical in .alpha.- or .beta.-configuration and cyclodextrin clathrates thereof and, when R.sup.2 represents a hydrogen atom, non-toxic salts thereof. These compounds exhibit characteristic prostaglandin activity.
摘要翻译：下式的化合物：其中A表示下式的基团：其中R 1表示氢原子或含有1至6个碳原子的直链或支链烷基原子，R 2表示氢原子或含有1至12个碳原子的直链或支链烷基，X表示反式亚乙烯基或亚乙基，波浪线表示羟基自由基以α-或β-构型的连接和环糊精包合物，当R 2表示氢原子时，其无毒性盐。这些化合物表现出特征性前列腺素活性。

9. 发明授权

US4070537A 17-Oxo-17-phenyl-prostaglandins 失效
标题翻译： 17-氧代-17-苯基 - 前列腺素
公开(公告)号：US4070537A
公开(公告)日：1978-01-24
申请号：US679299
申请日：1976-04-22
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Kimiichiro Matsumoto
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake , Kimiichiro Matsumoto
IPC分类号： C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07C69/76
CPC分类号： C07D307/935 , C07C405/00
摘要： The present invention relates to 17-oxo-17-phenyl-prostaglandins having the following structural formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, R.sup.1 represents a hydrogen atom or a methyl or ethyl group, R.sup.2 and R.sup.3, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group or a straight- or branched-chain alkyl group containing from 1 to 3 carbon atoms, and R.sup.4 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms and cyclodextrin clathrates of such acids and esters, and when R.sup.4 represents a hydrogen atom, non-toxic salts thereof.These compounds exhibit characteristic prostaglandin activity, e.g., abortifacient activity, stimulation activity on uterine contraction, and so on.
摘要翻译：本发明涉及具有以下结构式的17-氧代-17-苯基 - 前列腺素：（VI）其中A代表下式的基团：X表示亚乙基或顺式亚乙烯基，Y代表乙烯或反式亚乙烯基，R 1表示氢原子或甲基或乙基，可以相同或不同的R 2和R 3各自表示氢或卤素原子，三氟甲基或含有直链或支链烷基的 1〜3个碳原子，R4表示氢原子或含有1〜12个碳原子的直链或支链烷基和这些酸和酯的环糊精包合物，当R4表示氢原子时，无毒的盐。

10. 发明授权

US3953495A 16-Methylene PGE.sub.2 失效
标题翻译： 16-亚甲基PGE {HD 2
公开(公告)号：US3953495A
公开(公告)日：1976-04-27
申请号：US501548
申请日：1974-08-29
申请人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
发明人： Masaki Hayashi , Seiji Kori , Hajimu Miyake
IPC分类号： C12P31/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C61/38
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4006
摘要： The present invention relates to 16-methylene prostaglandins. These compounds are useful as anti-ulcer agents, bronchodilators and so on.
摘要翻译：本发明涉及16-亚甲基前列腺素。这些化合物可用作抗溃疡剂，支气管扩张剂等。

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