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    Pharmaceutical compositions based on Diclofenae
    22.
    发明授权
    Pharmaceutical compositions based on Diclofenae 失效
    基于双氯芬酸的药物组合物

    公开(公告)号：US06974595B1

    公开(公告)日：2005-12-13

    申请号：US09524747

    申请日：2000-03-14

    Applicant: Alberto Reiner ,  Giorgio Reiner

    Inventor： Alberto Reiner ,  Giorgio Reiner

    IPC: A61K8/44 ,  A61K9/20 ,  A61K31/196 ,  A61K47/02 ,  A61Q11/00 ,  A61K33/00 ,  A61K45/06

    CPC classification number: A61K31/197 ,  A61K8/44 ,  A61K9/2009 ,  A61K31/196 ,  A61K47/02 ,  A61Q11/00

    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。

    Pharmaceutical compositions having therapeutical activity based on mercaptoethansulphonic arginine salt
    23.
    发明授权
    Pharmaceutical compositions having therapeutical activity based on mercaptoethansulphonic arginine salt 失效
    具有基于巯基乙磺酸精氨酸盐的治疗活性的药物组合物

    公开(公告)号：US5244920A

    公开(公告)日：1993-09-14

    申请号：US960216

    申请日：1992-10-13

    Applicant: Alberto Reiner ,  Giueseppe Vita

    Inventor： Alberto Reiner ,  Giueseppe Vita

    IPC: A61K31/185 ,  A61K31/205

    CPC classification number: A61K31/185 ,  C07C279/14 ,  C07C323/66

    Abstract: The L-arginine salts of the mercaptoethansulphonic acid are active in the therapy of the bladder carcinoma and in the therapy and prevention of the cistinic kidney calculi.The saline derivatives with basic aminoacids and their alkyl esters are moreover devoid of side effects.The latter derivatives are prepared by reacting, in aqueous or aqueous-alcoholic medium, equimolar amounts of mercaptoethansulphonic acid, just prepared from an organic or inorganic salt thereof, and of the desired aminoacid.

    Abstract translation: 巯基乙磺酸的L-精氨酸盐在膀胱癌的治疗和治疗和预防小肠肾结石方面是有活性的。 具有碱性氨基酸及其烷基酯的盐水衍生物还没有副作用。 后一种衍生物通过在水性或含水醇介质中使等摩尔量的由其有机或无机盐制备的巯基乙磺酸和所需的氨基酸反应来制备。

    Process for the preparation of compounds with antiulcer action
    24.
    发明授权
    Process for the preparation of compounds with antiulcer action 失效
    用抗静电剂制备化合物的方法

    公开(公告)号：US5118813A

    公开(公告)日：1992-06-02

    申请号：US597282

    申请日：1990-10-16

    Applicant: Alberto Reiner

    Inventor： Alberto Reiner

    IPC: C07D317/54 ,  C07B31/00 ,  C07B45/06 ,  C07C67/00 ,  C07C319/14 ,  C07C323/25 ,  C07C323/44 ,  C07C325/00 ,  C07C335/08 ,  C07C335/12 ,  C07D307/50 ,  C07D307/52 ,  C07D317/58 ,  C07D407/00 ,  C07D407/12 ,  C07D521/00

    CPC classification number: C07D407/12 ,  C07D317/58

    Abstract: For the preparation of compounds such as ranitidine, niperotidine and cimetidine a urea of the formula:R.sub.1 --NH--C--NH--(CH.sub.2).sub.n --SD--S--(CH.sub.2).sub.n --NH--C--NH--R.sub.1 (I)which is synthesized by reaction with a compound of formula ##STR1##[H.sub.2 N--(CH.sub.2).sub.n --S--] (IX)is converted in a first stage into the corresponding bis-carbodiimideR.sub.1 --N.dbd.C.dbd.N--(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n --N.dbd.C.dbd.N--R.sub.1 (II)by reaction with triphenylphospine and bromine in the presence of a strong base and in a second stage the diimide thus obtained is reacted with nitromethane or a saline derivative of the cyanamide.The product thus obtained is reduced at the disulfide bridge obtaining a compound of formula: ##STR2## which is reacted with: ##STR3## to obtain ranitidine and niperotidine or cimetidine respectively depending on whether the first or the second of the described reactants is used.

    Abstract translation: 为了制备化合物如雷尼替丁，哌啶啶和西咪替丁，下式为：R 1 -NH-C-NH-（CH 2）n-SD-S-（CH 2）n -NH-C-NH-R 1（I） 其通过与式（VIII）化合物反应合成[H 2 N-（CH 2）n -S - （IX））在第一阶段转化为相应的双碳二亚胺R 1 -N = C = N- ）nSS-（CH 2）n N = C = N-R 1（II），通过在强碱的存在下与三苯膦和溴反应，并且在第二阶段中将由此获得的二酰亚胺与硝基甲烷或氨基氰的盐水衍生物反应。 由此获得的产物在二硫键下还原，得到与下式反应的式（Ⅳ）化合物：ⅩⅥ或Ⅶ（Ⅶ），分别得到雷尼替丁和西咪替丁 关于所使用的第一种或第二种反应物是否被使用。

    Quinuclidinic ester and derivatives of phenoxycarboxylic acids
    26.
    发明授权
    Quinuclidinic ester and derivatives of phenoxycarboxylic acids 失效
    喹喔啉酯和苯氧基羧酸的衍生物

    公开(公告)号：US4355166A

    公开(公告)日：1982-10-19

    申请号：US245273

    申请日：1981-03-19

    Applicant: Alberto Reiner

    Inventor： Alberto Reiner

    IPC: C07D213/803 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/52 ,  A61K31/522 ,  A61P3/06 ,  A61P7/10 ,  A61P25/02 ,  A61P29/00 ,  C07C53/124 ,  C07C57/12 ,  C07C59/68 ,  C07D213/55 ,  C07D213/80 ,  C07D453/02 ,  C07D473/08

    CPC classification number: C07D213/80 ,  C07C53/124 ,  C07C57/12 ,  C07C59/68 ,  C07D213/55 ,  C07D453/02 ,  C07D473/08

    Abstract: The invention relates to esters of 3-hydroxy-quinuclidine with phenoxycarboxylic acids, and their salts having general formula: ##STR1## wherein R.sub.1 represents H,CH.sub.3, and R.sub.2 represents H, Cl,Br or a radical of an acid of the group comprising oleic, pivalic, nicotinic, clofibric, pyridineacetic and teophyllineacetic acid.The compounds of the invention jointly show hypocholesteremizing and hypotriglyceridimizing activity, combined with other therapeutically interesting properties, such as beta-blocking, diuretic, anti-inflammatory activity.The invention furthermore relates to the pharmaceutical compositions containing the compounds of the invention as the active ingredients.

    Abstract translation: 本发明涉及3-羟基 - 奎宁环与苯氧基羧酸的酯及其盐，具有以下通式：其中R 1表示H，CH 3，R 2表示H，Cl，Br或酸的基团 该组包括油酸，新戊酸，烟酸，氯仿，吡啶乙酸和茶碱乙酸。 本发明的化合物联合显示低胆固醇和低甘油三酯化活性，结合其它治疗上有趣的性质，如β-阻断，利尿，抗炎活性。 本发明还涉及含有本发明化合物作为活性成分的药物组合物。

    Amide derivatives of p-isobutyl-phenyl-propionic acids and related pharmaceutical compositions
    27.
    发明授权
    Amide derivatives of p-isobutyl-phenyl-propionic acids and related pharmaceutical compositions 失效
    对异丁基苯基 - 丙酸的酰胺衍生物和相关的药物组合物

    公开(公告)号：US4341798A

    公开(公告)日：1982-07-27

    申请号：US283430

    申请日：1981-07-15

    Applicant: Alberto Reiner

    Inventor： Alberto Reiner

    IPC: C07C233/45 ,  A61K31/195 ,  C07C101/22

    CPC classification number: C07C233/45

    Abstract: The amide derivatives of p-isobutyl-phenyl-propionic acid, having general formula ##STR1## wherein X is the radical of a substituted amine, of the group comprising lysine, metatrifluorotoluidine, glutamic acid and aspartic acid, show a good anti-inflammatory activity, accompanied by favourable side properties. For the preparation of the compounds of the invention, the p-isobutyl-phenyl-propionic acid is chlorinated, and the chlorinated derivative is reacted with the proper substituted amine.

    Abstract translation: 具有通式为“IMAGE”的对异丁基苯基 - 丙酸的酰胺衍生物，其中X为赖氨酸，偏三氟甲苯胺，谷氨酸和天冬氨酸的基团，其中X为取代的胺基，显示出良好的抗炎活性 伴随着有利的边缘性质。 为了制备本发明的化合物，将对异丁基苯基 - 丙酸氯化，氯化衍生物与适当的取代胺反应。

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