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15 条记录 (耗时 0.018 秒)

    Therapeutically active fluoro substituted benzimidazoles
    3.
    发明授权
    Therapeutically active fluoro substituted benzimidazoles 失效
    治疗活性氟取代的苯并咪唑

    公开(公告)号：US5441968A

    公开(公告)日：1995-08-15

    申请号：US134255

    申请日：1993-10-08

    申请人： Arne E. Brandstrom ,  Per L. Lindberg ,  Gunnel E. Sunden

    发明人： Arne E. Brandstrom ,  Per L. Lindberg ,  Gunnel E. Sunden

    IPC分类号： C07D401/12 ,  A61K31/44

    CPC分类号： C07D401/12

    摘要： The novel compounds of the formulas I and I' ##STR1## wherein F is in 5 or 6 position and ##STR2## wherein in both formulas R is the group --CH.sub.2 OCOOR.sup.1, wherein R.sup.1 is a straight or branched alkyl containing 1-6 carbon atoms or benzyl, or R.sup.1 is the group ##STR3## wherein n is 1-6 and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.

    摘要翻译： 式I和I'的新颖化合物，其中F为5或6位且其中在两式中，R为基团-CH 2 OCOOR 1，其中R 1为含有1- 6个碳原子或苄基，或R1是其中n是1-6的基团，或其生理学上可接受的盐以及中间体，含有这些化合物作为活性成分的药物组合物，以及该化合物的用途 在医学上。

    Method of synthesis of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl-1H-ben zimidazole (omeprazole)
    4.
    发明授权
    Method of synthesis of 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl-1H-ben zimidazole (omeprazole) 失效
    5-甲氧基-2 - [（4-甲氧基-3,5-二甲基-2-吡啶基） - 甲基]亚磺酰基-1H-苯并咪唑（奥美拉唑）的合成方法

    公开(公告)号：US5386032A

    公开(公告)日：1995-01-31

    申请号：US67406

    申请日：1993-05-25

    申请人： Arne E. Brandstrom

    发明人： Arne E. Brandstrom

    IPC分类号： C07D213/68 ,  C07D235/28 ,  C07D401/12 ,  C07D401/00

    CPC分类号： C07D401/12

    摘要： The present invention relates to an improved method for the synthesis of omeprazole, comprising the steps of reacting 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methylthio]-1H-benzimidazole with m-chloroperoxybenzoic acid in a methylene chloride solution at a substantially constant pH of about 8.0 to 8.6; extracting the reaction mixture with aqueous NaOH; separating the aqueous phase from the organic phase; and adding an alkyl formate to the aqueous phase, resulting in crystallization of omeprazole.

    摘要翻译： 本发明涉及一种用于合成奥美拉唑的改进方法，包括以下步骤：使5-甲氧基-2 - [（4-甲氧基-3,5-二甲基-2-吡啶基） - 甲硫基] -1H-苯并咪唑与m - 氯过氧苯甲酸在约8.0至8.6的基本恒定的pH下在二氯甲烷溶液中; 用NaOH水溶液萃取反应混合物; 将水相与有机相分离; 并向水相中加入甲酸烷基酯，导致奥美拉唑结晶。

    2-[8-quinolinyl]-sulphinyl-1H-benzimidazole
    5.
    发明授权
    2-[8-quinolinyl]-sulphinyl-1H-benzimidazole 失效
    2- [8-喹啉基] - 亚磺酰基-1H-苯并咪唑

    公开(公告)号：US4725691A

    公开(公告)日：1988-02-16

    申请号：US913689

    申请日：1986-09-30

    申请人： Arne E. Brandstrom ,  Per L. Lindberg ,  Bjorn Wallmark

    发明人： Arne E. Brandstrom ,  Per L. Lindberg ,  Bjorn Wallmark

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/54 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D513/14 ,  C07D513/16 ,  C07D513/22

    CPC分类号： C07D401/12 ,  C07D513/14

    摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen preferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is a alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.

    Sulphenamides
    6.
    发明授权
    Sulphenamides 失效
    苯甲酰胺

    公开(公告)号：US4636499A

    公开(公告)日：1987-01-13

    申请号：US739425

    申请日：1985-05-30

    申请人： Arne E. Brandstrom ,  Per L. Lindberg ,  Bjorn Wallmark

    发明人： Arne E. Brandstrom ,  Per L. Lindberg ,  Bjorn Wallmark

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/47 ,  A61K31/54 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D401/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D513/14 ,  C07D513/16 ,  C07D513/22 ,  C07D513/04 ,  C07D513/12

    CPC分类号： C07D401/12 ,  C07D513/14

    摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen perferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy, or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is an alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.

    摘要翻译： 新的式IIIa化合物其中R 1a，R 2a，R 3a和R 4a相同或不同，为氢，烷基，任选完全或主要被氟或氯取代的烷氧基，卤素，-CN，-CF 3 - NO 2，-COR，-COOR，芳基，芳氧基或芳烷氧基或相邻基团R 1a，R 2a，R 3a和R 4a与苯并咪唑环中的相邻碳原子一起形成5-，6-或7-元单环或 9,10,10或11元双环，该环可以是饱和或不饱和的，并且可以含有0-3个选自N和O的杂原子，哪些环可以任选被1-4个选自烷基的取代基取代， 3个碳原子，卤素优选为F或Cl，含有4-5个碳原子的烯基，得到螺环化合物，或两个或四个这些取代基一起形成一个或两个氧基“IMAGE”，如果R1a，R2a，R3a和R4a连同 苯并咪唑环中相邻的碳原子形成它们的两个环 相互稠合，R5a为氢或烷基，R6a为氢或烷基或R5a和R6a连接在一起形成亚烷基链，R7a为氢，烷基，烷氧基，烯氧基或炔氧基， R8a是氢或烷基，或R6a和R7a或R7a和R8a与吡啶鎓环中的相邻碳原子一起形成环，其中由R6a和R7a或R7a和R8a构成的部分是-CH = CH-CH = CH-，-O-（CH 2）p - ， - CH 2（CH 2）p - ， - O-CH = CH-，-NH-CH = CH-， 其中p是2,3或4，并且O，S和N原子总是连接到化合物IIIa中的3位，R是烷基，环烷基，芳基或芳基烷基，X是药学上可接受的阴离子， 含有这些化合物的药物组合物及其在药物中的用途。