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    Stabilized choline salicylate compounds
    2.
    发明授权
    Stabilized choline salicylate compounds 失效
    稳定的水杨酸胆碱化合物

    公开(公告)号：US3947491A

    公开(公告)日：1976-03-30

    申请号：US501004

    申请日：1974-09-03

    申请人： William Kelly, deceased ,  by Monica Kelly, representative ,  by John Kelly, representative ,  Alfred Halpern

    发明人： William Kelly, deceased ,  by Monica Kelly, representative ,  by John Kelly, representative ,  Alfred Halpern

    IPC分类号： C07C91/00

    摘要： Choline salicylate sulfite and choline salicylate alkali metal sulfite-containing compounds of the formula, ##SPC1##Wherein Me represents the sodium, potassium or lithium ion and R represents the sulfite, bisulfite, metabisulfite, dithionate, hydrosulfite and hyposulfite groups are described. Said compounds are stable and inhibit the formation of color in pharmaceutical preparations containing the same. The method for the preparation of choline salicylate sulfite and choline salicylate alkali metal sulfite-containing compounds, and pharmaceutical dosage forms containing the same are disclosed together with a method for their use to inhibit color formation.

    摘要翻译： 胆碱水杨酸亚油酸酯和水杨酸胆碱碱金属亚硫酸盐化合物，其中Me代表钠，钾或锂离子，R代表亚硫酸盐，亚硫酸氢盐，偏亚硫酸氢盐，连二硫酸盐，连二亚硫酸盐和亚硫酸氢盐基团。 所述化合物稳定并且抑制含有该化合物的药物制剂中的颜色形成。 公开了用于制备水杨酸胆碱酯亚胺酸酯和水杨酸胆碱盐碱金属亚硫酸盐化合物的方法，以及含有它们的药物剂型及其用于抑制颜色形成的方法。

    Preparation for percutaneous administration
    3.
    发明授权
    Preparation for percutaneous administration 失效
    经皮给药制剂

    公开(公告)号：US4654209A

    公开(公告)日：1987-03-31

    申请号：US765451

    申请日：1985-08-14

    申请人： Stewart T. Leslie ,  Alan Rhodes ,  Cyril Boroda ,  Alfred Halpern

    发明人： Stewart T. Leslie ,  Alan Rhodes ,  Cyril Boroda ,  Alfred Halpern

    IPC分类号： A61K9/107 ,  A61K31/21 ,  A61K31/79

    CPC分类号： A61K9/107 ,  A61K31/21 ,  Y10S514/947 ,  Y10S514/97

    摘要： A preparation for percutaneous administration of nitroglycerine, said preparation comprising nitroglycerine incorporated in a cream base in an amount not less than about 0.05% by weight based on the total weight of the preparation. The composition may also contain other medicaments, the bioavailability of which is enhanced by the nitroglycerine. The action of the preparation against for example angina may be brought about by having an appropriate amount of nitroglycerine or as additional medicament another medicament active against angina. The preparation may contain an hydroxyalkylcellulose which may provide, in combination with a waxy component in the cream, for example a higher aliphatic alcohol, a prolonged release effect. The preparation has advantages particularly as regards bioavailability over prior uniphasic ointments.

    Treatment of hypertension, compounds and compositions for antihypertension and diuresis
    4.
    发明授权
    Treatment of hypertension, compounds and compositions for antihypertension and diuresis 失效
    治疗高血压，化合物和组合物用于抗高血压和利尿

    公开(公告)号：US4898729A

    公开(公告)日：1990-02-06

    申请号：US559755

    申请日：1983-12-09

    申请人： Ronald B. Miller ,  Alfred Halpern ,  Stewart Leslie ,  Peter Hofer

    发明人： Ronald B. Miller ,  Alfred Halpern ,  Stewart Leslie ,  Peter Hofer

    IPC分类号： C07D279/16 ,  A61K31/54 ,  A61K31/5415 ,  A61K47/34 ,  A61K47/48 ,  A61P7/10 ,  A61P9/12 ,  C07D285/26 ,  A61K31/79

    CPC分类号： A61K31/54 ,  A61K47/48184 ,  A61K47/4823 ,  Y10S514/869

    摘要： Antihypertension action is achieved without diuresis by administration of a thiazide diuretic in an amount which while being sufficient to achieve antihypertension is insufficient to achieve diuresis. Such administration in a non-diuretic amount is effected in 4-8 consecutive hourly doses to achieve reduction of blood pressure without high urine output. The invention further relates to complexes of thiazides with mixed cation-anion exchange resins, to insoluble basic metal hydroxy thiazide salts, the salts of thiazide with calcium disodium edetate or disodium edetate, to molecular complexes of thiazides with long chain polymers such as hydroxy alkyl cellulose polymers, carboxy methyl cellulose and polyvinylpyrrolidone, to beta-adrenergic blocking amine-thiazide salts and to amiloride thiazide salts.

    摘要翻译： 通过施用噻嗪类利尿剂可以实现抗高血压作用，其量足以达到抗高血压的量不足以达到利尿。 这种非利尿剂量的施用是以4-8个连续的小时剂量进行的，以达到降低血压而没有高尿量。 本发明还涉及噻嗪类与混合的阳离子 - 阴离子交换树脂，不溶性碱金属羟基噻嗪盐，噻嗪类与依地酸二钠盐或乙二胺四乙酸二钠盐的配合物，与噻唑烷与长链聚合物如羟烷基纤维素的分子复合物 聚合物，羧甲基纤维素和聚乙烯吡咯烷酮，β-肾上腺素能阻断胺 - 噻嗪盐和阿米洛利噻嗪盐。

    Percutaneous administration of nitroglycerine
    6.
    发明授权
    Percutaneous administration of nitroglycerine 失效
    经皮给药硝酸甘油

    公开(公告)号：US4322433A

    公开(公告)日：1982-03-30

    申请号：US203481

    申请日：1980-11-03

    申请人： Stewart T. Leslie ,  Alan Rhodes ,  Cyril Boroda ,  Alfred Halpern

    发明人： Stewart T. Leslie ,  Alan Rhodes ,  Cyril Boroda ,  Alfred Halpern

    IPC分类号： A61K9/107 ,  A61K31/21

    CPC分类号： A61K9/107 ,  A61K31/21 ,  Y10S514/947 ,  Y10S514/97

    摘要： A preparation for percutaneous administration of nitroglycerine, said preparation comprising nitroglycerine incorporated in a cream base in an amount not less than about 0.05% by weight based on the total weight of the preparation. The composition may also contain other medicaments, the bioavailability of which is enhanced by the nitroglycerine. The action of the preparation against for example angina may be brought about by having an appropriate amount of nitroglycerine or as additional medicament another medicament active against angina. The preparation may contain an hydroxyalkylcellulose which may provide, in combination with a waxy component in the cream, for example a higher aliphatic alcohol, a prolonged release effect. The preparation has advantages particularly as regards bioavailability over prior uniphasic ointments.

    摘要翻译： 一种用于经皮给药硝酸甘油的制剂，所述制剂包含以不低于制剂总重量的约0.05重量％的量掺入乳膏基质中的硝酸甘油。 组合物还可以含有其它药物，其生物利​​用度由硝酸甘油增强。 制备例如心绞痛的作用可以通过使用适量的硝酸甘油或另外的药物来治疗心绞痛。 该制剂可以含有羟烷基纤维素，其可以与霜中的蜡状组分组合，例如高级脂族醇，延长的释放效果。 该制剂在生物利用度方面特别优于以前的非相软膏。

    Ultra-violet filtration with certain aminosalicylic acid esters
    8.
    发明授权
    Ultra-violet filtration with certain aminosalicylic acid esters 失效
    用某些氨基水杨酸酯进行紫外线过滤

    公开(公告)号：US4036951A

    公开(公告)日：1977-07-19

    申请号：US649891

    申请日：1976-01-16

    申请人： Alfred Halpern ,  Ernest J. Sasmor

    发明人： Alfred Halpern ,  Ernest J. Sasmor

    IPC分类号： A61K8/44 ,  A61Q17/04 ,  A61K7/44

    CPC分类号： A61Q17/04 ,  A61K8/445 ,  Y10S424/13 ,  Y10S514/939

    摘要： Alkyl esters of aminosalicylic acid, said alkyl group having from 1 to 18 carbon atoms in chain length; alkenyl esters of aminosalicylic acid, said alkenyl group selected from the group consisting of vinyl, allyl, undecenyl, oleyl and linolenyl groups, and cyclic esters of aminosalicylic acid, said cyclic group being the cyclohexyl, phenyl and menthyl groups, having ultra-violet screening properties to absorb light rays within the wave-length range of 2950 A. to 3200 A. while transmitting the light rays beyond the 3200 A. range to permit the desirable tanning of the skin without solar burn. The respective esters of aminosalicylic acid are prepared by the reduction of the appropriate nitro-salicylic acid ester with Raney nickel and hydrogen in the presence of ethyl acetate. The respective esters are obtained as oils or solid crystalline substances and are soluble in alcohols, chloroform, acetone and benzene but insoluble in water. The ultra-violet absorption spectra for the respective compounds are described. Compositions comprising the above compounds together with the method for their preparation and the method for the use to achieve an ultraviolet filtering action on the skin of humans and animals are described.

    摘要翻译： 氨基水杨酸的烷基酯，所述烷基具有1至18个碳原子的链长; 所述烯基选自乙烯基，烯丙基，十一碳烯基，油烯基和亚麻基，氨基水杨酸的环状酯，所述环状基团是环己基，苯基和薄荷基，具有紫外线筛选 在2900A至3200A的波长范围内吸收光线的特性，同时将光线透射超过3200A的范围，以允许期望的鞣制皮肤而不需要太阳能燃烧。 氨基水杨酸的各自酯通过在乙酸乙酯存在下用阮内镍和氢还原适当的硝基 - 水杨酸酯来制备。 各酯是作为油或固体结晶物质得到的，可溶于醇，氯仿，丙酮和苯，但不溶于水。 描述各化合物的紫外吸收光谱。 描述了包含上述化合物的组合物及其制备方法以及用于在人和动物的皮肤上实现紫外线过滤作用的方法。