Methods of treating acute pain using diclofenac
    41.
    发明申请
    Methods of treating acute pain using diclofenac 审中-公开
    使用双氯芬酸治疗急性疼痛的方法

    公开(公告)号:US20060013896A1

    公开(公告)日:2006-01-19

    申请号:US11180996

    申请日:2005-07-13

    CPC classification number: A61K8/44 A61K9/2009 A61K31/196 A61K47/02 A61Q11/00

    Abstract: New pharmaceutical compositions for oral use containing diclofenac preferably together with alkali metal bicarbonates in amounts of from about 20 to about 80 by weight with respect to diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other, side effects; in particular, these formulations permit to obtain in human patients higher Cmax of the active principle and shorter Tmax together with a lower coefficient of variation.

    Abstract translation: 描述了相对于双氯芬酸,含有双氯芬酸的新型口服用药物组合物,优选与碱金属碳酸氢盐相当于约20至约80重量%。 这些组合物完全可口,没有任何不愉快的味道或其他副作用; 特别地,这些制剂允许在人类患者中获得较高的活性成分的最大值和更短的最大最小值以及更低的变异系数。

    Pharmaceutical compositions based on diclofenac
    42.
    发明申请
    Pharmaceutical compositions based on diclofenac 审中-公开
    基于双氯芬酸的药物组合物

    公开(公告)号:US20050147671A1

    公开(公告)日:2005-07-07

    申请号:US11030537

    申请日:2005-01-05

    Abstract: New pharmaceutical compositions for oral use containing Diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to Diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other side effects; in particular, these formulations permit to obtain in human patients higher Cmax of the active principle and shorter Tmax together with a lower coefficient of variation.

    Abstract translation: 描述了相对于双氯芬酸,含有重量比为20至80的新型双氯芬酸口服用药物组合物和碱金属碳酸氢盐。 这些组合物完全可口,没有任何不愉快的味道或其他副作用; 特别地,这些制剂允许在人类患者中获得较高的活性成分的最大值和更短的最大最小值以及更低的变异系数。

    Synthesis of antiulcer compounds
    43.
    发明授权
    Synthesis of antiulcer compounds 失效
    抗溃疡化合物的合成

    公开(公告)号:US5030738A

    公开(公告)日:1991-07-09

    申请号:US527680

    申请日:1990-05-22

    Applicant: Alberto Reiner

    Inventor: Alberto Reiner

    CPC classification number: C07D407/12 C07D317/58

    Abstract: To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R.sub.1 is hydrogen or together with R.sub.2 represents the rest of a cycloaliphatic or heterocyclic optionally substituted ring with 5 or 6 carbon atoms, R.sub.2 represents H, alkyl, alkyl substituted with a simple or substituted aromatic ring or with a single or substituted heterocyclic ring, Ar represents a simple or substituted phenyl group, a simple or substituted heterocyclic aromatic group, N=1, 2, 3, 4, 5 or 6 and X represents CH--NO.sub.2, S, N--C.tbd.N, the compound (II) is prepared through the following process sequence: ##STR2## wherein Z=H, NO.sub.2, halogen and R.sub.3 =--(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n, --(CH.sub.2).sub.n --S--CH.sub.2 Ar Y being halogen.The urea of formula ##STR3## is converted in a first stage into the corresponding carbodiimide ##STR4## by reaction with triphenylphosphine and bromine in the presence of a strong base and in a second stage is obtained the desired compound by reaction with nitromethane or with a saline derivative of cynamide.

    Abstract translation: 为了合成具有抗溃疡作用的分子,特别是具有以下分子式的雷尼替丁,尼泊替定和西咪替丁:其中R1是氢或与R2一起代表其余的具有5或6个碳原子的脂环族或杂环任意取代的环, R 2表示H,烷基,被简单或取代的芳环或单取代的杂环取代的烷基,Ar表示简单或取代的苯基,简单或取代的杂环芳基,N = 1,2,3,4 ,5或6,X表示CH-NO 2,S,NC 3 N N,化合物(II)通过以下方法制备:其中Z = H,NO2 卤素和R 3 = - (CH 2)n Ar, - (CH 2)n -SH, - (CH 2)nSS-(CH 2)n - ,(CH 2)n S-CH 2 Ar Y是卤素。 通过在强碱的存在下,通过与三苯基膦和溴反应,将式(II)的脲在第一阶段转化成相应的碳二亚胺(VI),并且在第二阶段中通过 与硝基甲烷或与cynamide的盐水衍生物反应。

    Water soluble derivatives of cephalex and process for their preparation
    46.
    发明授权
    Water soluble derivatives of cephalex and process for their preparation 失效
    头孢氨苄的水溶性衍生物及其制备方法

    公开(公告)号:US4471115A

    公开(公告)日:1984-09-11

    申请号:US452159

    申请日:1982-12-22

    Applicant: Alberto Reiner

    Inventor: Alberto Reiner

    CPC classification number: C07D501/22

    Abstract: The water soluble derivatives of cephalexin, having general formula: ##STR1## wherein X represents an alkali metal or the organic nitrogen containing cation of a basic aminoacid, combine the typical antibiotic action of cephalexin with the water solubility and form essentially neutral, aqueous solutions. The process for the preparation of the above derivatives comprises a first step in which the methylol derivative of cephalexin is prepared and a second step in which the treatment with a suitable base is carried out.

    Abstract translation: 具有以下通式的头孢氨苄的水溶性衍生物:其中X表示碱金属或碱性氨基酸的有机含氮阳离子,其结合了头孢氨苄的典型抗生素作用与水溶性,形成基本中性的水溶液。 制备上述衍生物的方法包括制备头孢氨苄羟甲基衍生物的第一步骤和进行用合适碱处理的第二步骤。

    Therapeutically active d-glucosamine salts
    48.
    发明授权
    Therapeutically active d-glucosamine salts 失效
    治疗活性的D-葡糖胺盐

    公开(公告)号:US4157440A

    公开(公告)日:1979-06-05

    申请号:US560236

    申请日:1975-03-20

    CPC classification number: C07H19/20

    Abstract: For the treatment of cardiac hypertrophy, d-glucosamine salts of the 3',5'-adenosine monophosphoric cyclic acid (AMP-c) and of the dibutyl ester thereof are disclosed, these salts having a reduced acute toxicity and an improved activity on the mitochondria of hypertrophic heart with respect to the cyclic AMP acid alone or its dibutyl ester. The compounds in question are useful for the treatment of cardiac hypertrophy and alteration of the energetic muscular metabolism.

    Abstract translation: 为了治疗心脏肥大,公开了3',5'-腺苷单磷酸环状酸(AMP-c)及其二丁基酯的d-葡糖胺盐,这些盐具有降低的急性毒性和对 相对于单独的环状AMP酸或其二丁酯,肥大心脏的线粒体。 所讨论的化合物可用于治疗心脏肥大和改变能量肌肉代谢。

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