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    Crystalline sodium (5R, 6S, 8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate and process for making same
    6.
    发明授权
    Crystalline sodium (5R, 6S, 8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate and process for making same 失效
    结晶钠（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯酸甲酯及其制备方法

    公开(公告)号：US4634556A

    公开(公告)日：1987-01-06

    申请号：US732533

    申请日：1985-05-10

    申请人： John K. Jenkins ,  John S. Chiu ,  Charles G. Eckhart ,  Paul E. McNamara ,  Stanley Rosenhouse ,  Richard E. Youngstrom

    发明人： John K. Jenkins ,  John S. Chiu ,  Charles G. Eckhart ,  Paul E. McNamara ,  Stanley Rosenhouse ,  Richard E. Youngstrom

    IPC分类号： C07D499/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/88

    摘要： A novel, stable, crystalline sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate (designated as Form II) is prepared by forming a homogenous solution of sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylate combined with stirring the homogenous solution for a time and at a temperature sufficient to produce Form II and recovering Form II. Form II may also be prepared by contacting a first solution obtained by dissolving (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxylic acid in dimethylacetamide with a second solution obtained by dissolving a sodium salt of an organic acid having a pKa of up to about 5, e.g., sodium 2-ethylhexanoate in acetone, in the presence of at least 5 volume percent water while stirring the reaction mixture so formed at a temperature and for a time sufficient to produce Form II followed by recovering Form II.Form II exhibits a greater physical stability and increased solid state chemical stability and reduced hygroscopicity over that of the amorphous form (e.g., Form I) which renders Form II greatly superior to Form I as a clinically suitable antibacterial agent.

    摘要翻译： 通过形成均匀的溶液来制备新的稳定的结晶的（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯氧基化钠（命名为II型） 的（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 庚-3-烯酰氧基化合物与搅拌均匀溶液一段时间并在足以产生II型 并恢复II型。 形式II也可以通过将通过将（5R，6S，8R）-6-（1-羟乙基）-2-（2-氨基甲酰氧基乙硫基） - 亚氨基-3-碳氧基酸溶解在二甲基乙酰胺中获得的第一溶液与第二溶液 通过在至少5体积％的水的存在下，将具有高达约5的pKa的有机酸的钠盐例如2-乙基己酸酯溶解在丙酮中而获得的溶液，同时搅拌在温度下形成的反应混合物， 一段时间足以生产II型，然后恢复II型。 II型具有更大的物理稳定性和增加的固态化学稳定性，并且比非晶形式（例如，形式I）的吸湿性降低，其使得II型作为临床合适的抗菌剂大大优于I型。

    Antihypertensive agents
    9.
    发明授权
    Antihypertensive agents 失效
    抗高血压药

    公开(公告)号：US4559340A

    公开(公告)日：1985-12-17

    申请号：US555311

    申请日：1983-11-25

    申请人： Bernard R. Neustadt ,  David R. Andrews ,  Paul E. McNamara

    发明人： Bernard R. Neustadt ,  David R. Andrews ,  Paul E. McNamara

    IPC分类号： A61K38/00 ,  C07D285/32 ,  C07K5/02 ,  C07D417/12 ,  A61K31/54

    CPC分类号： C07K5/0222 ,  C07D285/32 ,  A61K38/00 ,  Y10S530/80

    摘要： There are disclosed benzothiadiazinyl and quinazolinyl substituted carboxylalkyl dipeptides, wherein the benzothiodiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group. Compounds of this invention are useful as antihypertensive agents, in the treatment of congestive heart failure and in the treatment of glaucoma. In addition, compounds of this invention have diuretic activity.

    摘要翻译： 公开了苯并噻二嗪基和喹唑啉基取代的羧基烷基二肽，其中苯并二氮嗪基或喹唑啉基部分通过氨基羰基连接到二肽部分。 本发明化合物可用作抗高血压药，用于治疗充血性心力衰竭和治疗青光眼。 此外，本发明的化合物具有利尿活性。