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1. 发明授权

US3978229A Synergistic composition comprising PGF.sub.2.sub..alpha. and PGE.sub.2 失效
标题翻译：包含PGF'2“+ 0和PGE'2的协同组合物
公开(公告)号：US3978229A
公开(公告)日：1976-08-31
申请号：US566146
申请日：1975-04-08
申请人： Kimiichiro Matsumoto , Tsuneo Fujita , Toshitaka Sakai , Takeshi Tsuda
发明人： Kimiichiro Matsumoto , Tsuneo Fujita , Toshitaka Sakai , Takeshi Tsuda
IPC分类号： A61K47/48 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , A61K31/19 , A61K31/215 , A61K31/715
CPC分类号： C07D307/935 , A61K47/48969 , B82Y5/00 , C07C405/00 , C07D309/12 , C07F9/4006 , C07F9/4015 , C07F9/4018
摘要： A synergistic composition comprising as active ingredients a PGF.sub.2.sub..alpha. compound or its cyclodextrin clathrate thereof and a PGE.sub.2 compound or its cyclodextrin clathrate thereof, at a weight ratio of from about 1:0.33 to about 1:1.

2. 发明授权

US4390548A Trans-.DELTA..sup.2 -pge alkylsulphonyl amides 失效
标题翻译：经DELTA 2-pge烷基磺酰胺
公开(公告)号：US4390548A
公开(公告)日：1983-06-28
申请号：US257102
申请日：1981-04-24
申请人： Takashi Yamato , Hirofumi Endo , Kimiichiro Matsumoto , Hajimu Miyake
发明人： Takashi Yamato , Hirofumi Endo , Kimiichiro Matsumoto , Hajimu Miyake
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C143/75 , A61K31/18
CPC分类号： C07C405/0041 , C07C405/0033 , Y02P20/55
摘要： Prostaglandin analogues of the formula: ##STR1## (wherein R.sup.1 represents an alkyl group containing from 1 to 4 carbon atoms, R.sup.2 represents a single bond or an alkylene group containing from 1 to 5 carbon atoms, R.sup.3 represents a hydrogen atom, an alkyl or alkoxy group containing from 1 to 8 carbon atoms, a cycloalkyl or cycloalkyloxy group containing from 4 to 7 carbon atoms and being unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or a phenyl or phenoxy group unsubstituted or substituted by at least one halogen atom, trifluoromethyl group or alkyl group containing from 1 to 4 carbon atoms, R.sup.4 represents a hydrogen atom or a hydroxy-protecting group which may be removed under acidic conditions, X represents an ethylene group or a cis-vinylene group, the double bonds between the carbon atoms in positions 2 and 3 and between the carbon atoms in positions 13 and 14 are both in trans-configuration, and the wavy line attached to the carbon atom in position 15 represents .alpha.- or .beta.-configuration or a mixture thereof, provided that, when R.sup.2 represents a single bond, R.sup.3 does not represent an alkoxy group, a cycloalkoxy group or a phenoxy group) and cyclodextrin clathrates thereof are useful compounds: those in which R.sup.4 represents a hydrogen atom 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表示含有1至4个碳原子的烷基，R 2表示单键或含有1至5个碳原子的亚烷基，R 3表示氢原子，烷基或含有1至8个碳原子的烷氧基，含有4至7个碳原子的环烷基或环烷氧基，未被取代或被至少一个含有1至8个碳原子的烷基取代，或未取代或取代的苯基或苯氧基通过至少一个卤素原子，三氟甲基或含有1至4个碳原子的烷基，R 4表示氢原子或可在酸性条件下除去的羟基保护基，X表示亚乙基或顺式 - 亚乙烯基位置2和3之间的碳原子之间以及位置13和14之间的碳原子之间的双键都是反式构型，并且连接在p中的碳原子上的波浪线环状15表示α-或β-构型或其混合物，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）和环糊精包合物是有用的化合物：其中R4表示氢原子，具有选择性前列腺素样特性。

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

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。

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