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29 条记录 (耗时 0.02 秒)

    Multilayer matrix systems for the controlled release of active principles
    4.
    发明授权
    Multilayer matrix systems for the controlled release of active principles 失效
    用于控制释放有源原理的多层矩阵系统

    公开(公告)号：US5549913A

    公开(公告)日：1996-08-27

    申请号：US153437

    申请日：1993-11-16

    申请人： Paolo Colombo ,  Antonio C. Cardona ,  Giorgio Pifferi

    发明人： Paolo Colombo ,  Antonio C. Cardona ,  Giorgio Pifferi

    IPC分类号： A61J3/10 ,  A61K9/20 ,  A61K9/24 ,  A61K9/48 ,  A61K47/04 ,  A61K47/10 ,  A61K47/12 ,  A61K47/32 ,  A61K47/34 ,  A61K47/36 ,  A61K47/38 ,  A61K47/42

    CPC分类号： A61K9/2086 ,  A61K9/209

    摘要： This invention concerns systems for the release of active principles which are capable of releasing active principle(s) into an aqueous medium at a controlled rate.More precisely, the invention concerns a monolithic system for the controlled release of active principles, consisting of:a) at least one swelling layer containing one or more active principles, in a matrix of swellable, hydrophilic polymers;b) at least one erodible and/or soluble layer comprising excipients and/or water soluble polymers, possibly containing one or more active principles, either the same or different from those present in the layer a), the said erodible and/or soluble layer being in contact with the swelling layer(s) a).

    摘要翻译： 本发明涉及释放能够以受控速率将有效原理释放到水性介质中的活性原理的系统。 更准确地说，本发明涉及用于控制释放活性成分的整体系统，其包括：a）在可溶胀亲水性聚合物基质中含有一种或多种活性成分的至少一种溶胀层; b）至少一个包含赋形剂和/或水溶性聚合物的可侵蚀和/或可溶性层，其可能含有一个或多个与层a）中存在的活性成分相同或不同的活性成分，所述可侵蚀和/或可溶层 与膨胀层a）接触。

    4-Cyclopropylmethyleneoxy-3-chlorophenylacetic acid and salts thereof
    5.
    发明授权
    4-Cyclopropylmethyleneoxy-3-chlorophenylacetic acid and salts thereof 失效
    4-环丙基亚甲基氧基-3-氯苯基乙酸及其盐

    公开(公告)号：US3976673A

    公开(公告)日：1976-08-24

    申请号：US539912

    申请日：1975-01-09

    申请人： Giorgio Pifferi

    发明人： Giorgio Pifferi

    IPC分类号： A61K31/19 ,  A61P25/04 ,  A61P29/00 ,  C07C51/00 ,  C07C59/64 ,  C07C59/72 ,  C07C65/00 ,  C07C67/00 ,  C07C63/52 ,  C07C87/14 ,  C07F1/08

    CPC分类号： C07C59/72

    摘要： The compound 4-cyclopropylmethyleneoxy-3-chlorophenylacetic acid and its non-toxic pharmaceutically acceptable salts have activity as anti-inflammatory, antipiretic and analgesic agents. It is prepared by reacting a lower alkyl ester of 3-chloro-4-hydroxyphenyl acetic acid with a cyclopropylmethylene halide and subsequently saponifying the ester obtained. The acid obtained is optionally salified to give corresponding non-toxic, inorganic or organic pharmaceutically acceptable salts.

    摘要翻译： 化合物4-环丙基亚甲基氧基-3-氯苯基乙酸及其无毒的药学上可接受的盐具有作为抗炎，止痒和止痛剂的活性。 其通过使3-氯-4-羟基苯基乙酸的低级烷基酯与环丙基亚甲基卤反应并随后皂化所得的酯来制备。 获得的酸任选盐化以产生相应的无毒，无机或有机的药学上可接受的盐。

    Preparation of pyrrolidine and pyrrolidin-2-one derivatives
    6.
    发明授权
    Preparation of pyrrolidine and pyrrolidin-2-one derivatives 失效
    吡咯烷和吡咯烷-2-酮衍生物的制备

    公开(公告)号：US4173569A

    公开(公告)日：1979-11-06

    申请号：US876169

    申请日：1978-02-08

    申请人： Silvano Banfi ,  Renato Pellegata ,  Giorgio Pifferi ,  Mario Pinza

    发明人： Silvano Banfi ,  Renato Pellegata ,  Giorgio Pifferi ,  Mario Pinza

    IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61P25/00 ,  B43K24/08 ,  C07D207/26 ,  C07D207/273 ,  C09J115/00

    CPC分类号： C07D207/273 ,  B43K24/084 ,  C09J115/00 ,  Y10S514/87

    摘要： Preparation of compounds of the formula: ##STR1## wherein n is 1, 2 or 3, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or alkyl containing 1 to 3 carbon atoms and the asterisk indicates the center of asymmetry of the molecule, and compounds of the formula ##STR2## wherein R" is a saturated or unsaturated aliphatic hydrocarbon containing 1 to 6 carbon atoms, R.sub.3 is hydrogen or acyl containing 1 to 7 carbon atoms and the asterisk indicates the center of asymmetry of the molecule. The compounds produced by the present invention improve learning memory and display a protecting effect against the E.E.G. consequence of an overdose of barbiturates and against the reduced performance following brain damage (e.g. cerebral edema).

    摘要翻译： 下式化合物的制备：其中n为1,2或3，可以相同或不同的R 1和R 2为氢或含有1至3个碳原子的烷基，并且星号表示中心的化合物 的分子的不对称性和式（Ia）的化合物，其中R“是含有1至6个碳原子的饱和或不饱和脂族烃，R 3是氢或含有1至7个碳原子的酰基，而星号表示 分子的不对称中心。 本发明生产的化合物改善了学习记忆并显示出对E.E.G.的保护作用。 过量巴比妥类药物和脑损伤（例如脑水肿）后降低性能的后果。

    7-.alpha.Hydrazinoacetamido derivatives of cephalosporanic
    7.
    发明授权
    7-.alpha.Hydrazinoacetamido derivatives of cephalosporanic 失效
    7- {60头孢菌素的肼基-N-乙酰氨基衍生物

    公开(公告)号：US3998950A

    公开(公告)日：1976-12-21

    申请号：US563135

    申请日：1975-03-28

    申请人： Renato Broggi ,  Giuseppe Libassi ,  Giorgio Pifferi

    发明人： Renato Broggi ,  Giuseppe Libassi ,  Giorgio Pifferi

    IPC分类号： A61K20060101 ,  A61K31/545 ,  C07D20060101 ,  C07D205/08 ,  C07D213/04 ,  C07D279/06 ,  C07D333/04 ,  C07D501/06 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26 ,  C07D501/32 ,  C07D501/34 ,  C07D501/38 ,  C07D501/42 ,  C07D501/60

    CPC分类号： C07D501/20 ,  Y02P20/55

    摘要： Derivatives of 7-aminocephalosporanic acid of the formula: ##STR1## wherein the carbon atom marked with an asterisk represents an asymmetry center of the molecule, A represents an aromatic nucleus, preferably phenyl which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms, or a heterocyclic nucleus, preferably 2- or 3-thiophene which may be, for example, substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R.sub.1 represents a hydrogen atom, a hydroxy group, an acetoxy or pyridinium group. The invention includes the compounds as such or in the form of separated epimers as well as the corresponding pharmaceutically acceptable salts with alkali or alkaline-earth metals, with suitable organic bases or corresponding suitable organic or inorganic acid addition salts. Also method of preparing same. The compounds have powerful antibacterial action against gram-positive and gram-negative bacteria.

    摘要翻译： 7-氨基头孢烷酸的衍生物，具有下式：其中标有星号的碳原子代表分子的不对称中心，A代表芳香核，优选苯基，其可被具有1-4个碳原子的烷基取代 碳原子，卤素，羟基或具有1-4个碳原子的烷氧基，或杂环核，优选可以被卤素取代的2-或3-噻吩，R表示氢原子或直链或支链低级 烷基，R 1表示氢原子，羟基，乙酰氧基或吡啶鎓基。 本发明包括这样的化合物或分离的差向异构体的形式，以及与碱金属或碱土金属的相应的药学上可接受的盐，以及合适的有机碱或相应​​的合适的有机或无机酸加成盐。 还有制备方法。 这些化合物对革兰氏阳性和革兰氏阴性细菌具有强大的抗菌作用。

    3-0-(Beta-carbobenzyloxypropionyl)-11-oxo-18-beta-olean-12-en-30-oic acid
    8.
    发明授权
    3-0-(Beta-carbobenzyloxypropionyl)-11-oxo-18-beta-olean-12-en-30-oic acid 失效
    3-0-（β-苄酯基丙酰基）-11-氧代-18-β-烯​​烃-12-烯-30-酸

    公开(公告)号：US3984461A

    公开(公告)日：1976-10-05

    申请号：US220695

    申请日：1972-01-25

    申请人： Giorgio Pifferi

    发明人： Giorgio Pifferi

    IPC分类号： C07C69/40 ,  A61K31/19

    CPC分类号： A61K31/19 ,  Y02P20/582

    摘要： A two-step method for the preparation of 3-0-(beta-carboxypropionyl-18-beta-glycyrrhetic acid (carbenoxolone) is disclosed, which comprises the steps of condensing beta-glycyrrhetic acid with anhydrous beta-carbobenzyloxypropionic acid (or a derivative thereof such as its chloride or anhydride), the result being 3-O-(beta-carbobenzyloxypropionyl)-11-oxo-18-beta-olean-12-en-30-oic acid, the latter compound being then debenzylated with hydrogen under normal temperature and pressure conditions, in an alcoholic solvent (alcohols having from C.sub.1 to C.sub.5) and in the presence of catalytic amounts of a noble metal (e.g. palladium), thus obtaining the expected compound.

    摘要翻译： 公开了制备3-0-（β-羧基丙酰基-18-β-甘草次酸（carbenoxolone）的两步法，其包括将β-甘草次酸与无水β-苄酯基丙酸（或衍生物）缩合的步骤 其结果是3-O-（β-苄氧基丙酰基）-11-氧代-18-β-烯​​烃-12-烯-30-酸，然后将后一种化合物用氢气去氢化， 在常温和常压条件下，在醇溶剂（具有C1至C5的醇）和催化量的贵金属（例如钯）的存在下，从而得到预期的化合物。