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71. 发明授权

US4734411A Pyrrolizidine compounds, salts thereof, process for the preparation of same and pharmaceutical agents comprising same 失效
标题翻译：吡咯烷啶化合物，其盐，其制备方法和包含其的药剂
公开(公告)号：US4734411A
公开(公告)日：1988-03-29
申请号：US895099
申请日：1986-08-11
申请人： Masayasu Kurono , Yasuaki Kondo , Takuji Yamaguchi , Toshinao Usui , Ryoichi Unno , Hiromoto Kimura , Masato Fukushima , Mitsuru Oka , Shinichi Ikeda , Noboru Kuboyama , Takashi Ito , Seiji Miyano , Kunihiro Sumoto
发明人： Masayasu Kurono , Yasuaki Kondo , Takuji Yamaguchi , Toshinao Usui , Ryoichi Unno , Hiromoto Kimura , Masato Fukushima , Mitsuru Oka , Shinichi Ikeda , Noboru Kuboyama , Takashi Ito , Seiji Miyano , Kunihiro Sumoto
IPC分类号： A61K31/40 , A61K31/54 , A61P1/04 , C07D487/04 , C07D519/00 , C07F7/08 , A61K31/55 , C07D521/00
CPC分类号： C07D487/04 , C07F7/0814
摘要： Novel pyrrolizidine compounds represented by the formula ##STR1## wherein R is a radical of ##STR2## R.sup.1 is hydrogen, halogen, alkyl group, alkoxy group, alkanoyl group, trifluoromethyl radical, trimethylsilyl radical or ##STR3## R.sup.2 and R.sup.3 are same or different and are hydrogen or alkyl group, respectively, R.sup.4 is hydrogen, halogen, alkyl group or alkoxy group and m is an integer of 0 to 5,salts thereof, a process for the preparation of same as well as a pharmaceutical agent comprising same.
摘要翻译：由式（I）表示的新型吡咯烷酮化合物，其中R是R 1的基团是氢，卤素，烷基，烷氧基，烷酰基，三氟甲基，三甲基甲硅烷基或者R 2是相同或不同，分别为氢或烷基，R4为氢，卤素，烷基或烷氧基，m为0-5的整数，其盐，其制备方法以及药剂，其包含相同。

72. 发明授权

US4131747A Process for preparing .alpha.-substituted phenylalkanecarboxylic acid 失效
标题翻译：制备{60-取代的苯基烷羧酸的方法
公开(公告)号：US4131747A
公开(公告)日：1978-12-26
申请号：US743258
申请日：1976-11-19
申请人： Masayasu Kurono , Masaaki Toda , Haruki Niwa , Syunji Kosuge , Takahumi Iida , Kenichi Narita
发明人： Masayasu Kurono , Masaaki Toda , Haruki Niwa , Syunji Kosuge , Takahumi Iida , Kenichi Narita
IPC分类号： C07C51/00 , C07C51/29 , C07C51/377 , C07C57/30 , C07C57/38 , C07C57/46 , C07C57/52 , C07C57/58 , C07C59/64 , C07C59/76 , C07C67/00 , C07D303/48 , C07C63/52 , C07C63/33 , C07C65/02
CPC分类号： C07C255/00 , C07C57/30 , C07C57/38 , C07D303/48
摘要： A process for preparing an .alpha.-substituted phenylalkanecarboxylic acid, having useful pharmaceutical properties such as analgesic, anti-inflammatory and anti-pyretic properties, from the corresponding ethylidenecyanoacetate by oxidation, hydrolysis, decarboxylation and oxidation.
摘要翻译：通过氧化，水解，脱羧和氧化从相应的亚乙基亚乙酸酯制备具有有用的药学性质如镇痛，抗炎和抗热解性能的α-取代的苯基烷羧酸的方法。

73. 发明授权

US4045468A 16-Cyclobutyl-prostaglandins 失效
标题翻译： 16-环丁基 - 前列腺素
公开(公告)号：US4045468A
公开(公告)日：1977-08-30
申请号：US557437
申请日：1975-03-11
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07D309/12 , C07F9/4018 , Y10S514/927
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.
摘要翻译：其中A表示下式的组：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示氢或1至12个碳原子的烷基，R 1 R 2和R 3表示氢或1〜12个碳原子的烷基或芳基，条件是R1，R2和R3中的至少一个表示烷基或芳基，是具有有用药理特性的新化合物; 它们特别适用于治疗胃溃疡。

74. 发明授权

US4971799A Percutaneous-administration-type pharmaceutical preparation of nitroglycerin 失效
标题翻译：硝酸甘油经皮给药型药物制剂
公开(公告)号：US4971799A
公开(公告)日：1990-11-20
申请号：US175820
申请日：1988-03-31
申请人： Takashi Nakagawa , Masayasu Kurono , Makoto Sato , Tsutomu Ishida , Kazushi Tokita , Katsuhiko Takahashi , Masato Azuma , Satoshi Uenoyama
发明人： Takashi Nakagawa , Masayasu Kurono , Makoto Sato , Tsutomu Ishida , Kazushi Tokita , Katsuhiko Takahashi , Masato Azuma , Satoshi Uenoyama
IPC分类号： A61K9/70 , A61K31/21 , A61L15/58 , A61P9/08 , A61P9/10
CPC分类号： A61K9/7061 , A61K31/21 , A61K9/7076 , A61L15/58
摘要： A percutaneous-administration-type pharmaceutical preparation of nitroglycerin comprising a backing that is impervious to medicines, and a pressure-sensitive adhesive layer that is disposed on one surface of the backing, wherein the pressure-sensitive adhesive layer contains alkyl (meth)acrylate copolymer in the concentration of 80-95% by weight and the nitroglycerin in the concentration of 5-20% by weight, said copolymer contains as major copolymer components alkyl (meth)acrylate with alkyl groups having 6 or more carbon atoms, which alkyl (meth)acrylates include 2-ethylhexylmethacrylate in the concentration of 40-90% by weight based on the total weight of said alkyl (meth)acrylates, and the copolymer has a rolling ball tack value of 2 or less. The preparation obtained makes it possible for nitroglycerin to be absorbed percutaneously at a controlled rate for long periods of time.

75. 发明授权

US4560679A Organosilicon compounds and antitumor agents containing the compound as effective component 失效
标题翻译：含有化合物作为有效成分的有机硅化合物和抗肿瘤剂
公开(公告)号：US4560679A
公开(公告)日：1985-12-24
申请号：US542439
申请日：1983-10-17
申请人： Shigeshi Toyoshima , Masayasu Kurono , Ryoichi Unno , Koichi Ito
发明人： Shigeshi Toyoshima , Masayasu Kurono , Ryoichi Unno , Koichi Ito
IPC分类号： A61K31/695 , A61P35/00 , C07F7/08 , C07F7/10
CPC分类号： C07F7/0812 , C07F7/0818
摘要： A novel organosilicon compound represented by a formula ##STR1## wherein A is methylene, carbonyl or sulfonyl group; R, R.sub.1 and R.sub.2 are alkyl group, respectively; R.sub.3 is alkyl, substituted alkyl, alkenyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, pyridyl, substituted pyridyl, furyl, substituted furyl, thienyl, substituted thienyl group or cycloalkyl group together with the substituent A; R.sub.4 is hydrogen, alkyl or alkenyl group; and R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are hydrogen, alkyl or substituted alkyl, respectively,a non-toxic salt thereof, a process for the preparation of said compound or salt, as well as an antitumor agent comprising as an effective agent at least one of said compound and salt.
摘要翻译：一种由下式表示的新型有机硅化合物，其中A是亚甲基，羰基或磺酰基; R，R 1和R 2分别是烷基; R 3是烷基，取代的烷基，烯基，苯基，取代的苯基，萘基，取代的萘基，吡啶基，取代的吡啶基，呋喃基，取代的呋喃基，噻吩基，取代的噻吩基或环烷基与取代基A一起; R4是氢，烷基或烯基; R 5，R 6，R 7，R 8，R 9，R 10，R 11和R 12分别为氢，烷基或取代的烷基，其无毒盐，制备所述化合物或盐的方法，以及抗肿瘤剂包括所述化合物和盐中的至少一种作为有效剂。

76. 发明授权

US4275075A 15-cylobutyl-trans-.DELTA..sup.2 -prostaglandin analogues 失效
标题翻译： 15-cylobutyl-trans-DELTA 2-prostaglandin类似物
公开(公告)号：US4275075A
公开(公告)日：1981-06-23
申请号：US915493
申请日：1978-06-14
申请人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
发明人： Masayasu Kurono , Hisao Nakai , Shigeru Sakuyama
IPC分类号： A61K31/557 , A61K31/19 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/40 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07F9/4018
摘要： The present invention relates to prostaglandin analogues of the general formula: ##STR1## [wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents a group of the formula --COOR.sup.4, in which R.sup.4 represents hydrogen or straight- or branched-chain alkyl of 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.5, in which R.sup.5 represents hydrogen or alkylcarbonyl of 2 to 5 carbon atoms and R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent hydrogen, straight- or branched-chain alkyl of 1 to 12 carbon atoms, or an aryl group unsubstituted or substituted by one, two or three substituents selected from alkyl, alkoxy, alkylthio, monoalkylamino and dialkylamino groups and halogen atoms, the alkyl groups or moieties of the said groups containing from 1 to 5 carbon atoms in a straight- or branched-chain, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 is other than hydrogen and the double bond between C.sub.2 -C.sub.3 is trans] and cyclodextrin clathrates of such prostaglandin analogues and, when R.sup.4 in the group - COOR.sup.4 represents hydrogen, non-toxic salts thereof, which exhibit characteristic prostaglandin-like activities.
摘要翻译：本发明涉及以下通式的前列腺素类似物：其中A表示下式的基团：X表示反式亚乙烯基或亚乙基，Y表示顺式亚乙烯基或亚乙基，R表示式-COOR4，其中R 4表示氢或1至12个碳原子的直链或支链烷基，或式-CH 2 OR 5的基团，其中R 5表示氢或2至5个碳原子的烷基羰基，R 1，R 2 和可以相同或不同的R 3各自表示氢，1至12个碳原子的直链或支链烷基，或未取代或被1,2或3个选自烷基，烷氧基，烷硫基的取代基取代的芳基，单烷基氨基和二烷基氨基和卤素原子，所述基团的直链或支链含有1至5个碳原子的烷基或部分，条件是R1，R2和R3中的至少一个符号是除了氢和 C2-C3之间的双键是反式]和这种前列腺素类似物的环糊精包合物，当组COOR4中的R4表示氢时，其无毒性盐显示出特征性的前列腺素样活性。

77. 发明授权

US4117119A 15-Cyclobutyl-prostaglandins 失效
标题翻译： 15-CYCLOBUTYL-PROSTAGLANDINS
公开(公告)号：US4117119A
公开(公告)日：1978-09-26
申请号：US794580
申请日：1977-05-06
申请人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
发明人： Masayasu Kurono , Hisao Nakai , Takashi Muryobayashi
IPC分类号： C07C51/353 , C07C51/60 , C07C61/04 , C07C405/00 , C07D307/935 , C07D309/12 , C07F9/40 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07D307/935 , C07C405/00 , C07C51/353 , C07C51/60 , C07C61/04 , C07D309/12 , C07F9/4018 , Y10S514/899 , Y10S514/925
摘要： Prostaglandin analogues of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## X represents trans-vinylene or ethylene and Y represents cis-vinylene or ethylene, R represents hydrogen or alkyl of 1 through 12 carbon atoms, R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, or alkyl of 1 through 12 carbon atoms or an aryl group, with the proviso that at least one of the symbols R.sup.1, R.sup.2 and R.sup.3 represents an alkyl or aryl group, are new compounds possessing useful pharmacological properties; they are especially useful for the treatment of gastric ulceration.

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