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40 条记录 (耗时 0.023 秒)

    Carboxylic acid derivatives
    1.
    发明授权
    Carboxylic acid derivatives 失效
    羧酸衍生物

    公开(公告)号：US5229418A

    公开(公告)日：1993-07-20

    申请号：US691399

    申请日：1991-04-25

    申请人： Eric W. Collington ,  John W. Clitherow ,  David E. Bays

    发明人： Eric W. Collington ,  John W. Clitherow ,  David E. Bays

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61K31/555 ,  A61P1/00 ,  A61P1/04 ,  A61P31/04 ,  C07C59/255 ,  C07C59/265 ,  C07D307/52 ,  C07D405/06 ,  C07D405/12

    CPC分类号： C07D405/12 ,  C07D307/52

    摘要： The invention relates to a salt of a basic histamine H.sub.2 -receptor antagonist of formula (I) ##STR1## and a complex of bismuth with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, or a solvate of such a salt, whereinR.sup.1 represents a group of formula ##STR2## where R.sup.3 represents methyl or the group (CH.sub.2).sub.2 CONR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 both represent ethyl groups;R.sup.2 represents a hydrogen atom or, when R.sup.1 is the group --C(.dbd.CHNO.sub.2)NHCH.sub.3, R.sup.2 may also represent a methyl group; andn is 3 and X is oxygen, or n is 2 and X is CH.sub.2 or sulphur;with the provisos that(i) when R.sup.1 represents ##STR3## then X is sulphur and n is 2: (ii) when R.sup.1 represents --C(.dbd.CHNO.sub.2)NHCH.sub.3 and R.sup.2 is hydrogen, then X is oxygen and n is 3 or X is CH.sub.2 and n is 2; and(iii) when R.sup.1 represents --C(.dbd.CHNO.sub.2)NHCH.sub.3 and R.sup.2 is methyl, then X is oxygen and n is 3 or X is sulphur and n is 2.The salts and solvates thereof are useful in the treatment of gastro-intestinal disorders, such as peptic ulcer disease, gastritis and non-ulcer dyspepsia.

    Carboxylic acid derivatives
    2.
    发明授权
    Carboxylic acid derivatives 失效
    羧酸衍生物

    公开(公告)号：US5399556A

    公开(公告)日：1995-03-21

    申请号：US938301

    申请日：1992-03-02

    申请人： John W. Clitherow ,  Eric W. Collington

    发明人： John W. Clitherow ,  Eric W. Collington

    IPC分类号： A61K31/315 ,  A61K31/34 ,  A61K31/341 ,  A61P1/00 ,  C07D307/52 ,  A61K31/555

    CPC分类号： C07D307/52

    摘要： The invention relates to salts formed between ranitidine and a complex of zinc with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, and to solvates of such salts. The salts and solvates thereof are useful in the treatment of gastro-intestinal disorders, such as peptic ulcer disease and non-ulcer dyspepsia.

    摘要翻译： 本发明涉及雷尼替丁和锌与选自酒石酸，柠檬酸和烷基柠檬酸的羧酸络合物之间形成的盐，以及这些盐的溶剂合物。 其盐和溶剂化物可用于治疗胃肠道疾病，例如消化性溃疡疾病和非溃疡性消化不良。

    Process for the preparation of a furan derivative
    6.
    发明授权
    Process for the preparation of a furan derivative 失效
    制备呋喃衍生物的方法

    公开(公告)号：US4399294A

    公开(公告)日：1983-08-16

    申请号：US335686

    申请日：1981-12-30

    申请人： David E. Bays ,  John W. Clitherow ,  Duncan B. Judd

    发明人： David E. Bays ,  John W. Clitherow ,  Duncan B. Judd

    IPC分类号： C07D307/46 ,  C07D307/52 ,  C07D405/14

    CPC分类号： C07D405/14 ,  C07D307/46 ,  C07D307/52

    摘要： Ranitidine is prepared by treating an aldehyde of formula (II) ##STR1## with dimethylamine and a reducing agent which is capable of effecting reductive alkylation to introduce the group Me.sub.2 NCH.sub.2 -- but which does not reduce the nitroethene group. The reaction is carried out in a suitable solvent, preferably in the presence of an acid or followed by treatment with an acid. Suitable reducing agents include, diborane, aluminium hydride and alkali or alkaline earth metal borohydrides.The aldehyde (II) may be generated in situ from an acetal of formula (III) ##STR2## where R.sub.1 and R.sub.2 are both alkyl groups or R.sub.1 OCHOR.sub.2 forms a cyclic acetal.

    摘要翻译： 雷尼替丁通过用能够进行还原性烷基化以引入基团Me2NCH2-但不降低硝基乙烯基团的二甲胺和还原剂处理式（II）的醛制备。 该反应在合适的溶剂中进行，优选在酸的存在下进行，或者随后用酸处理。 合适的还原剂包括乙硼烷，氢化铝和碱金属或碱土金属硼氢化物。 醛（II）可以由式（III）的缩醛（III）原位产生，其中R 1和R 2都是烷基或R 1 OCHOR 2形成环状缩醛。

    Heterocyclic derivatives
    10.
    发明授权
    Heterocyclic derivatives 失效

    公开(公告)号：US4410523A

    公开(公告)日：1983-10-18

    申请号：US199522

    申请日：1980-10-22

    申请人： William D. Ollis ,  Barry J. Price ,  Linda Carey ,  Roger Hayes ,  John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon

    发明人： William D. Ollis ,  Barry J. Price ,  Linda Carey ,  Roger Hayes ,  John W. Clitherow ,  John Bradshaw ,  John W. M. Mackinnon

    IPC分类号： C07D249/14 ,  A61K31/395 ,  C07D249/10

    CPC分类号： C07D249/14 ,  Y10S514/927

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in whichR.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, aralkyl, trifluoroalkyl, heteroaralkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkyamino or cycloalkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups, or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur;Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms and is attached to the cyclohexadiene ring at either the 4- or 5- position;X represents --CH.sub.2 or --O--;m represents 2, 3, 4 or 5 and when X is --O-- the chain (CH.sub.2).sub.m may be interrupted by an oxygen atom provided that there are at least two methylene groups between any two heteroatoms in the moiety --X(CH.sub.2).sub.m NH--;R.sub.3 represents hydrogen, alkyl, alkenyl, aralkyl, or C.sub.2-6 alkyl substituted by hydroxy or alkoxy; andR.sub.4 represents hydrogen, alkyl, alkenyl, aralkyl, hydroxyalkyl, acyloxyalkyl, alkoxyalkyl, aryloxyalkyl, aralkyloxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxy or alkoxy or the group NR.sub.5 R.sub.6 whereR.sub.5 represents hydrogen, alkyl, alkyl substituted by hydroxy or C.sub.1-3 alkoxy, alkenyl, aralkyl or heteroaralkyl and R.sub.6 represents any of the groups defined for R.sub.5 or may represent the group COR.sub.7 where R.sub.7 represents hydrogen, alkyl, aryl, aralkyl, alkoxy, heteroaryl or monocyclic heteroaralkyl or R.sub.6 represents the group SO.sub.2 R.sub.8 where R.sub.8 represents alkyl or aryl, or R.sub.6 represents the group ##STR2## where Y is oxygen or sulphur and R.sub.9 represents hydrogen, alkyl, cycloalkyl, aryl or aralkyl,or R.sub.5 and R.sub.6 taken together may represent the group .dbd.CR.sub.10 R.sub.11 where R.sub.10 represents aryl or heteroaryl and R.sub.11 represents hydrogen or alkyl.The compounds show activity as selective histamine H.sub.2 -antagonists.