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81. 发明授权

US4247705A 4-Substituted 2-iminoimidazolidine compounds 失效
标题翻译： 4-取代的2-亚氨基咪唑烷化合物
公开(公告)号：US4247705A
公开(公告)日：1981-01-27
申请号：US009899
申请日：1979-02-06
申请人： Albert D. Cale, Jr.
发明人： Albert D. Cale, Jr.
IPC分类号： C07D233/46 , A61K31/415 , A61K31/4427 , A61K31/445 , A61K31/495 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/12 , A61P27/02 , A61P27/12 , C07D233/44 , C07D233/48 , C07D233/50 , C07D401/06
CPC分类号： C07D233/44 , Y10S514/866
摘要： This invention provides a novel class of 2-iminoimidazolidines which include 4-substituted derivatives such as 4-(2-chloroethyl)-1-methyl-2-methylimino-3-phenyl imidazolidine fumarate: ##STR1## This illustrated 4-substituted 2-iminoimidazolidine compound exhibits cardiovascular hypotensive, hypoglycemic (glucose tolerance, and sugar cataract) and anti-inflammatory (pleural effusion) pharmacological activities in test animals.
摘要翻译：本发明提供了一类新的2-亚氨基咪唑烷，其包括4-取代的衍生物如4-（2-氯乙基）-1-甲基-2-甲基亚氨基-3-苯基咪唑烷富马酸盐。亚氨基咪唑烷化合物在试验动物中表现出心血管低血压，低血糖（葡萄糖耐量和糖白内障）和抗炎（胸腔积液）药理活性。

82. 发明授权

US4202129A Insect-combatting device 失效
标题翻译：防虫装置
公开(公告)号：US4202129A
公开(公告)日：1980-05-13
申请号：US857992
申请日：1977-12-06
申请人： Jack Greenberg
发明人： Jack Greenberg
IPC分类号： A01M1/20 , A01N25/18 , A01N57/12 , A01N9/36 , A01N17/00
CPC分类号： A01N25/18 , A01N57/12
摘要： An improved insect-combatting device (e.g., for use against houseflies, gnats and mosquitoes) is disclosed. The device comprises a shaped solid body having a porous surface capable of gradually and continually releasing naled insecticide in an amount sufficient to provide an insecticidally active concentration of said naled over a prolonged period of time and comprises a synthetic resinous matrix material, from about 15 to about 35 weight percent of naled and a minor amount effective to retard spewing of the insecticide of finely divided silica particles and at least one C.sub.14 to C.sub.20 saturated aliphatic carboxylic acid or a salt or ester thereof. The device is formed from a mixture of the said synthetic resin, naled, finely divided silica particles, C.sub.14 to C.sub.20 to aliphatic saturated carboxylic acid or salt or ester thereof and a surface porosity control component that is non-reactive in the mixture and has a boiling point at or below the curing temperature to produce surface openings in communication with pores in said body by vaporization of said porosity control component to provide the release of naled gas at a rate effective to control insects in the vicinity of said body, but insufficient to form as spew on the body.
摘要翻译：公开了一种改进的防虫装置（例如，用于家蝇，g蚊和蚊子）。该装置包括具有多孔表面的成形固体，该多孔表面能够以足以在长时间内提供所述定向的杀昆虫活性浓度的量逐渐且持续释放定向杀虫剂，并且包括合成树脂基质材料，约15至约35重量％的有效量的微量二氧化硅颗粒和至少一种C14至C20饱和脂族羧酸或其盐或酯的杀虫剂的喷雾有效。该装置由所述合成树脂，定形，细碎的二氧化硅颗粒，C14至C20与脂族饱和羧酸或其盐或酯的混合物和在该混合物中不起反应性的表面孔隙率控制组分的混合物形成，沸点等于或低于固化温度，以通过所述孔隙率控制组分的蒸发产生与所述主体中的孔连通的表面开口，以提供有效地控制昆虫在所述身体附近的速率释放定向气体，但不足以形成为身体上的喷雾。

83. 发明授权

US4159381A 4-(P-Fluorobenzoyl)-1-[3-(p-fluorobenzoyl)propyl]piperidine 失效
标题翻译： 4-（对氟苯甲酰基）-1- {8 3-（对氟苯甲酰基）丙基{9哌啶
公开(公告)号：US4159381A
公开(公告)日：1979-06-26
申请号：US850319
申请日：1977-11-10
申请人： Laszlo Baum , Philippe Pochon
发明人： Laszlo Baum , Philippe Pochon
IPC分类号： C07D211/32 , C07D211/62
CPC分类号： C07D211/62 , C07D211/32
摘要： A novel process for the preparation of 4-(p-fluorobenzoyl)-1-[3-(p-fluorobenzoyl)propyl]piperidine and the acid addition salts thereof is disclosed.
摘要翻译：公开了一种制备4-（对氟苯甲酰基）-1- [3-（对氟苯甲酰基）丙基]哌啶及其酸加成盐的新方法。

84. 发明授权

US4144245A 4-Hydroxymethyl-2-pyrrolidinones 失效
公开(公告)号：US4144245A
公开(公告)日：1979-03-13
申请号：US892539
申请日：1978-02-03
申请人： Albert D. Cale, Jr.
发明人： Albert D. Cale, Jr.
IPC分类号： C07D203/08 , C07D207/26 , C07D307/33 , C07D207/44
CPC分类号： C07D203/08 , C07D207/26 , C07D307/33
摘要： 1-Hydrocarbon-3,3-diphenyl-4-hydroxymethyl-2-pyrrolidinones and methods for making them from 4,5-dihydro-3,3-diphenyl-4-hydrocarbylaminomethylfuran-2(3H)ones are disclosed. Methods for making the 4,5-dihydro-3,3-diphenyl-4-hydrocarbylaminomethylfuran-2(3H)ones are also disclosed. The novel compounds are useful intermediates for the preparation of pharmacologically active 4-(4,4-disubstitutedpiperidinylmethyl)-3,3-diphenyl-2-pyrrolidinones.

85. 发明授权

US4143150A Derivatives of oxanilic acid 失效
标题翻译：氨基酸衍生物
公开(公告)号：US4143150A
公开(公告)日：1979-03-06
申请号：US826032
申请日：1977-08-19
申请人： William J. Welstead, Jr. , Albert D. Cale, Jr.
发明人： William J. Welstead, Jr. , Albert D. Cale, Jr.
IPC分类号： A61K31/40 , A61P11/08 , A61P37/08 , C07D207/14
CPC分类号： C07D207/14
摘要： Oxanilic acid derivatives having the formula: ##STR1## are disclosed wherein R is lower-alkyl, cycloalkyl, phenylalkyl or phenyl; R.sup.1 is hydrogen, lower-alkyl or phenyl; R.sup.2 is hydrogen, lower-alkyl, or lower-alkoxy; R.sup.3 is hydrogen, fluoro, chloro or bromo; X is oxygen or sulfur; and M is hydrogen, lower-alkyl or a physiologically acceptable cation. The compounds are useful for ameliorating and controlling symptoms associated with asthma.

86. 发明授权

US4115587A Fatty acid amides of norfenfluramine and compositions and methods thereof 失效
标题翻译：诺氟氟胺的脂肪酸酰胺及其组成及方法
公开(公告)号：US4115587A
公开(公告)日：1978-09-19
申请号：US751294
申请日：1976-12-16
申请人： Carl D. Lunsford , Albert D. Cale, Jr.
发明人： Carl D. Lunsford , Albert D. Cale, Jr.
IPC分类号： C07C233/02 , A61K31/165 , C09F5/00
CPC分类号： C07C233/02
摘要： Novel amides of norfenfluramine having the formula ##STR1## wherein R is selected from the group consisting of alkyl and alkenyl radicals having 12 to 22 carbon atoms and compositions and methods for combating atherosclerosis and hypercholesteremia, with beneficial side effects useful for combating obesity in atherosclerotic subjects are disclosed. The compounds lower lipid values and simultaneously inhibit appetite and reduce weight gain from ingested food with minimal side effects.
摘要翻译：具有式“IMAGE”的诺氟氟胺的新型酰胺，其中R选自具有12至22个碳原子的烷基和烯基，以及用于对抗动脉粥样硬化和高胆固醇血症的组合物和方法，具有用于对抗动脉粥样硬化受试者的肥胖症的有益副作用被披露。该化合物降低脂质含量，同时抑制食欲，减少摄入食物的体重增加，副作用最小。

87. 发明授权

US4073796A N-(1-substituted-3-pyrrolidinyl)-1-naphthalene carboxamides 失效
标题翻译： N-（1-取代-3-吡咯烷基）-1-萘甲酰胺
公开(公告)号：US4073796A
公开(公告)日：1978-02-14
申请号：US683605
申请日：1976-05-05
申请人： Albert D. Cale, Jr.
发明人： Albert D. Cale, Jr.
IPC分类号： A61K31/40 , A61K31/47 , A61P1/08 , C07D207/14 , C07D401/12
CPC分类号： C07D207/14 , Y10S514/872
摘要： Novel N-(1-substituted-3-pyrrolidinyl)-1-naphthalene- and 4-quinolinecarboxamides of the formula: ##STR1## wherein R is lower cycloalkyl, R.sup.1 is hydrogen, lower alkyl or aryl, R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, amino or nitro, R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkoxy, amino or nitro, Y is carbon or nitrogen and pharmaceutically acceptable acid addition salts thereof having anti-emetic properties are disclosed.
摘要翻译：新型的具有下式的N-（1-取代-3-吡咯烷基）-1-萘和4-喹啉甲酰胺：其中R是低级环烷基，R 1是氢，低级烷基或芳基，R 2是氢，低级烷基卤素，低级烷氧基，氨基或硝基，R 3为氢，低级烷基，卤素，低级烷氧基，氨基或硝基，Y为碳或氮，并且其药学上可接受的酸加成盐具有抗呕吐性质。

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