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公开(公告)号：US4220654A
公开(公告)日：1980-09-02
申请号：US45545
申请日：1979-06-04
IPC分类号： A61K31/415 , A61P1/04 , C07C45/63 , C07D233/54 , C07D233/64 , C07D233/90 , C07D333/42 , C07D403/06 , C07D409/04 , C07D409/06
CPC分类号： C07D233/64 , A61K31/415 , C07C205/45 , C07C45/63 , C07D233/90 , C07D333/42
摘要： There are disclosed novel compounds described as imidazole cyanoguanidines in which the imidazole moiety is connected to the cyanoguanidine moiety through a cyclic group which may optionally contain one or two alkylene linkages. The cyclic groups may be phenyl, cyclohexyl, thienyl and the like. Processes for the preparation of such compounds are also disclosed. The compounds are useful for the suppression of gastric acid secretion in mammals, and compositions for such uses are also disclosed.
摘要翻译： 公开了描述为咪唑氰基胍的新化合物，其中咪唑部分通过可任选地含有一个或两个亚烷基键的环状基团连接到氰基胍部分。 环状基团可以是苯基，环己基，噻吩基等。 还公开了制备这些化合物的方法。 该化合物可用于抑制哺乳动物中的胃酸分泌，并且还公开了用于这些用途的组合物。
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公开(公告)号：US4196292A
公开(公告)日：1980-04-01
申请号：US811011
申请日：1977-06-29
IPC分类号： A61K31/495 , A61P7/10 , C07D241/26 , C07D241/30 , C07D241/32 , C07D241/34
CPC分类号： C07D241/26 , A01N31/02 , Y10S514/869
摘要： N-amidino-3,5-diamino-6-substituted-2-pyrazinecarboxamides and a process for their synthesis.
摘要翻译： N-脒基-3,5-二氨基-6-取代-2-吡嗪甲酰胺及其合成方法。
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53.发明授权2,3-Dihydro-6,7-disubstituted-5-furoyl benzofuran-2-carboxylic acids 失效2,3-二氢-6,7-二取代-5-糠酰基苯并呋喃-2-羧酸
公开(公告)号：US4163794A
公开(公告)日：1979-08-07
申请号：US873023
申请日：1978-01-27
IPC分类号： A61K31/34 , A61K31/343 , A61P7/10 , A61P9/12 , C07D307/80 , C07D307/85 , C07D307/83
CPC分类号： C07D307/85 , C07D307/80 , Y10S514/869 , Y10S514/87
摘要： 2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
摘要翻译： 公开了2,3-二氢-6,7-二取代-5-（酰基）苯并呋喃-2-羧酸，其药学上可接受的盐，酯和酰胺衍生物以及这些化合物与抗利尿剂的组合，其具有利尿钠盐，尿酸 和抗高血压活动。
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公开(公告)号：US4150235A
公开(公告)日：1979-04-17
申请号：US751831
申请日：1976-12-17
IPC分类号： C07C69/66 , A61K31/16 , A61K31/165 , A61K31/19 , A61K31/215 , A61P7/10 , A61P9/08 , A61P9/12 , A61P37/06 , A61P43/00 , C07C45/46 , C07C51/00 , C07C51/08 , C07C51/29 , C07C59/125 , C07C59/48 , C07C59/68 , C07C59/70 , C07C59/84 , C07C59/90 , C07C63/04 , C07C65/01 , C07C65/32 , C07C65/40 , C07C67/00 , C07C69/612 , C07C69/76 , C07C231/00 , C07C235/10 , C07C235/20 , C07C235/34 , C07C235/42 , C07C235/78 , C07C235/84 , C07C241/00 , C07C243/32 , C07C243/38 , C07C255/32 , C07D309/12
CPC分类号： C07D309/12 , C07C243/38 , C07C255/00 , C07C403/20 , C07C45/46 , C07C51/08 , C07C59/90 , C07C65/01 , C07C65/40 , C07C2101/14
摘要： Novel interphenylene derivatives of 11,12-secoprostaglandins are prepared by the stepwise alkylation of the ethyl ester or the t-butyl ester of acetoacetic acid. One such method involves treatment of the t-butyl ester of acetoacetic acid with a strong base to form the anion followed by treatment with ethyl p-(3-bromopropyl)benzoate to produce ethyl 4-(4-tert-butoxycarbonyl-5-oxo-hexyl)benzoate, subsequently reacting the anion of the thus-formed benzoate with 1-chloro-4-acetoxynonane to produce ethyl 4-(4-acetyl-4-tert-butoxycarbonyl-8-acetoxytridecyl)benzoate followed by decarboxylation and alkaline hydrolysis to produce the desired product 4-(4-acetyl-8-hydroxytridecyl)benzoic acid which is useful as pharmaceutical in the treatment of patients with renal failure and in the prevention of transplant rejection.
摘要翻译： 通过乙酸乙酯或乙酸乙酯的叔丁酯的逐步烷基化制备11,12-前列腺素的新型间苯二酚衍生物。 一种这样的方法包括用强碱处理乙酰乙酸的叔丁酯以形成阴离子，然后用对 - （3-溴丙基）苯甲酸乙酯处理，得到4-（4-叔丁氧基羰基-5-氧代 - 己基）苯甲酸酯，随后将由此形成的苯甲酸酯的阴离子与1-氯-4-乙酰氧基壬烷反应，生成4-（4-乙酰基-4-叔丁氧基羰基-8-乙酰氧基十三烷基）苯甲酸乙酯，然后脱羧和碱水解 以产生所需产物4-（4-乙酰基-8-羟基十三烷基）苯甲酸，其可用作治疗肾衰竭患者和预防移植排斥的药物。
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公开(公告)号：US4133885A
公开(公告)日：1979-01-09
申请号：US816617
申请日：1977-07-18
IPC分类号： A61K31/435 , A61P1/04 , C07D471/04 , A01N9/22 , C07D213/00
CPC分类号： C07D471/04 , Y10S514/819
摘要： Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
摘要翻译： {PG，1]公开了基于萘啶分子的有机化合物，其具有有效的胃分泌抑制性质。 萘啶酮在1位被取代的氨基烷基取代，并在其余位置被不同地取代。 这些化合物对胃肠道胃分泌物的抑制具有深远的影响，并且还公开了用于这些用途的组合物。
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56.发明授权9-Thia- and oxothia- and 9-dioxothia-11,12-seco-prostaglandins 失效9-Thia-和oxothia-和9-dioxothia-11,12-seco-prostaglandins
公开(公告)号：US4128564A
公开(公告)日：1978-12-05
申请号：US844687
申请日：1977-10-25
IPC分类号： C07C317/46 , C07C317/48 , C07C143/90 , C11D1/28
CPC分类号： C07C317/46 , C07C317/48 , C07C2101/14
摘要： This invention relates to 9-thia-, 9-oxothia, and 9-dioxothia-11,12-seco-prostaglandins and processes for their manufacture. These compounds have prostaglandin-like biological activity and are particularly useful for the treatment of skin diseases such as psoriasis, for the prevention of thrombus formation, in stimulating the production of growth hormone in intact animals, and as regulators of the immune response.
摘要翻译： 本发明涉及9-硫杂，9-氧代硫代和9-二氧硫杂十一-11,12-前列腺素及其制备方法。 这些化合物具有前列腺素样生物活性，并且特别可用于治疗皮肤疾病如牛皮癣，用于预防血栓形成，刺激完整动物中生长激素的产生，以及作为免疫应答的调节剂。
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公开(公告)号：US4126629A
公开(公告)日：1978-11-21
申请号：US721733
申请日：1976-09-09
摘要： This invention relates to aryloxy-, alkoxy-, arylthio-, and alkylthio-11,12-seco-prostaglandins and to processes for their manufacture. These compounds have prostaglandin-like activity and are particularly useful in fertility control such as for estrus synchronization in animals and postcoital contraceptive agents in humans.
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58.发明授权
公开(公告)号：US4115402A
公开(公告)日：1978-09-19
申请号：US807478
申请日：1977-06-17
IPC分类号： C07D333/34 , C07D333/24 , A01N9/00
CPC分类号： C07D333/34 , Y10S514/869
摘要： 2,3-Dichloro-4-[(substituted sulfonyl)phenoxyl]-acetic acids and their salt, ester and amide derivatives thereof. The products are useful diuretic, saluretic and uricosuric agents. The acid products are prepared by treating a 2,3-dichloro-4-(2-substituted sulfonyl)phenol with a haloalkanoic acid or ester thereof and if the ester is employed hydrolyzing the ester.
摘要翻译： 2,3-二氯-4 - [（取代的磺酰基）苯氧基] - 乙酸及其盐，酯和酰胺衍生物。 该产品是有用的利尿剂，盐水和尿酸剂。 通过用卤代链烷酸或其酯处理2,3-二氯-4-（2-取代的磺酰基）苯酚，并且如果使用酯水解酯，则制备酸产物。
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公开(公告)号：US4102888A
公开(公告)日：1978-07-25
申请号：US789047
申请日：1977-04-20
IPC分类号： C07C45/29 , C07C45/51 , C07C47/277 , C07D209/48 , C07D277/14 , C07D309/06 , C07F9/09 , C07F9/40
CPC分类号： C07D209/48 , C07D277/14 , C07D309/06 , C07F9/091 , C07F9/4059 , Y10S514/885 , Y10S514/929
摘要： This invention relates to novel 8-aza-9-oxo-11-thia-, -11-oxothia-, and -11-dioxothia-prostanoic acid compounds, salts, and derivatives thereof and also to processes for the preparation of such compounds. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, for the treatment of certain autoimmune diseases, and in preventing thrombus formation.
摘要翻译： 本发明涉及新的8-氮杂-9-氧代-11-硫杂-11-氧代硫代和-11-二氧噻吩 - 前列腺烷酸化合物，其盐及其衍生物，还涉及制备这些化合物的方法。 这些化合物具有前列腺素样生物活性，并且特别可用作肾血管扩张剂，用于治疗某些自身免疫性疾病和预防血栓形成。
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60.发明授权5-(Hydroxy (substituted) methyl)-2,3-dihydrobenzo furan-2-carboxylic acid and its derivatives 失效5-（羟基（取代的）甲基）-2,3-二氢苯并呋喃-2-羧酸及其衍生物
公开(公告)号：US4100294A
公开(公告)日：1978-07-11
申请号：US747840
申请日：1976-12-06
IPC分类号： A61K31/34 , A61K31/343 , A61K31/38 , A61K31/41 , A61P7/10 , A61P9/12 , A61P19/06 , C07D307/80 , C07D307/85 , C07D409/04 , C07D417/06 , C07D307/82 , A61K31/18 , A61K31/425
CPC分类号： C07D307/80 , C07D307/85
摘要： 5-[Hydroxy(substituted)methyl]-2,3-dihydrobenzo-furan-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
摘要翻译： 5- [羟基（取代的）甲基] -2,3-二氢苯并呋喃-2-羧酸，其药学上可接受的盐，酯和酰胺衍生物以及这些化合物与抗利尿剂的组合公开了具有利尿钠盐，尿酸和 抗高血压活动。
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