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    Aminoalkyl-substituted benzimidazolidin-2-ones
    13.
    发明授权
    Aminoalkyl-substituted benzimidazolidin-2-ones 失效
    氨基烷基取代的苯并咪唑烷-2-酮

    公开(公告)号：US4215119A

    公开(公告)日：1980-07-29

    申请号：US26608

    申请日：1979-04-03

    申请人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    发明人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    IPC分类号： C07D215/02 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/536 ,  A61P9/08 ,  A61P9/12 ,  A61P11/00 ,  A61P25/24 ,  A61P25/26 ,  C07D215/22 ,  C07D215/227 ,  C07D223/04 ,  C07D233/32 ,  C07D233/36 ,  C07D235/04 ,  C07D235/22 ,  C07D235/26 ,  C07D263/54 ,  C07D263/58 ,  C07D265/22 ,  C07D265/36 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  A61K31/535

    CPC分类号： C07D215/227 ,  C07D233/36 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  Y10S514/929

    摘要： Racemic and optically active compounds of the formulaQ-C.sub.n H.sub.2n -NH-Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl or 1 to 4 carbon atoms,n is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, R.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms, or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --COHN-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译： 其中Q为氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基，三氟甲基或氨基，R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或三氟甲基，R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基，A是-O-，-CH 2 -CH 2 - 或 -NR 3 - ，其中R 3是氢或烷基或1至4个碳原子，n是2-6的整数，包括2和6，R是氢，苄基或者其中R 4是氢，甲基或乙基，R 5，R 6和 R 7可以相同或不同，分别为氢，卤素，羟甲基，三氟甲基，1至4个碳原子的烷基，1至4个碳原子的烷氧基，硝基，氰基，-CONHR 3，-CONHOH， - COOR 3，R8O-，甲基磺酰基甲基，或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时，也可以是-NR 3 R 9，其中R 3具有上述定义，R 8是氢， 1至20个碳原子的烷酰基，1至4个碳原子的烷酰基或芳烷基，R 9是氢，低级烷酰基，甲磺酰基，氨基甲酰基，二甲基氨磺酰基或2至5个碳原子的烷氧基羰基，以及R5和R6， 另一个是-O-CH 2 -O，-O-CH 2 -CH 2 -O - ， - CH = CH-CH = CH-，-O-CH 2 -CONH-，-CH 2 -CH 2 -COOH-或-O-CO -NH-和无毒的药学上可接受的酸加成盐。 化合物及其盐可用作血管扩张剂和CNS刺激剂。

    Aminoalkyl-substituted benzoxazine derivatives
    14.
    发明授权
    Aminoalkyl-substituted benzoxazine derivatives 失效
    氨基烷基取代的苯并恶嗪衍生物

    公开(公告)号：US4154829A

    公开(公告)日：1979-05-15

    申请号：US773394

    申请日：1977-03-02

    申请人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    发明人： Anton Mentrup ,  Kurt Schromm ,  Ernst-Otto Renth ,  Richard Reichl ,  Werner Traunecker ,  Wolfgang Hoefke

    IPC分类号： C07D215/02 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4166 ,  A61K31/4184 ,  A61K31/42 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/536 ,  A61P9/08 ,  A61P9/12 ,  A61P11/00 ,  A61P25/24 ,  A61P25/26 ,  C07D215/22 ,  C07D215/227 ,  C07D223/04 ,  C07D233/32 ,  C07D233/36 ,  C07D235/04 ,  C07D235/22 ,  C07D235/26 ,  C07D263/54 ,  C07D263/58 ,  C07D265/22 ,  C07D265/36 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D265/30 ,  A61K31/535

    CPC分类号： C07D215/227 ,  C07D233/36 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  Y10S514/929

    摘要： Racemic and optically active compounds of the formulaQ--C.sub.n H.sub.2n --NH--Rwherein Q is ##STR1## where R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, trifluoromethyl or amino,R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or trifluoromethyl,R.sub.1 and R.sub.2, together with each other, are methylenedioxy or ethylenedioxy, andA is --O--, --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 -- where the oxygen is bonded to the benzene ring, or --NR.sub.3 -- where R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms,N is an integer from 2 to 6, inclusive, andR is hydrogen, benzyl or ##STR2## where R.sub.4 is hydrogen, methyl or ethyl,R.sub.5, r.sub.6 and R.sub.7, which may be identical to or different from each other, are each hydrogen, halogen, hydroxymethyl, trifluoromethyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, nitro, cyano, --CONHR.sub.3, --CONHOH, --COOR.sub.3, R.sub.8 O--, methylsulfonylmethyl or, when one or two of R.sub.5 through R.sub.7 are other than halogen or trifluoromethyl, also --NR.sub.3 R.sub.9,whereR.sub.3 has the meanings defined above,R.sub.8 is hydrogen, alkanoyl of 1 to 20 carbon atoms, alkyl of 1 to 4 carbon atoms or aralkyl, andR.sub.9 is hydrogen, lower alkanoyl, methanesulfonyl, carbamoyl, dimethylsulfamoyl, or alkoxycarbonyl of 2 to 5 carbon atoms, andR.sub.5 and R.sub.6, together with each other, are --O--CH.sub.2 --O, --O--CH.sub.2 --CH.sub.2 --O--, --CH.dbd.CH--CH.dbd.CH--, --O--CH.sub.2 --CONH--, --CH.sub.2 --CH.sub.2 --CONH-- or --O--CO--NH--,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as vasodilators and CNS-stimulators.

    摘要翻译： 其中Q为氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基，三氟甲基或氨基，R 2为式Q-C n H 2n-NH-R的外消旋和旋光活性化合物 氢，卤素，1至4个碳原子的烷基，1至4个碳原子的烷氧基或三氟甲基，R 1和R 2彼此一起是亚甲二氧基或亚乙二氧基，A是-O-，-CH 2 -CH 2 - ， - O-CH2-，其中氧与苯环结合，或-NR 3 - ，其中R 3是氢或1至4个碳原子的烷基，N是2至6，INCLUSIVE和R R的整数是氢，苄基或 其中R 4是氢，甲基或乙基，R 5，R 6和R 7可以彼此相同或不同，各自为氢，卤素，羟甲基，三氟甲基，1至4个碳原子的烷基，1至 4个碳原子，硝基，氰基，-CONHR 3，-CONHOH，-COOR 3，R 8 O - ，甲基磺酰基甲基，或当R 5至R 7中的一个或两个不同于卤素或三氟甲基时，也可以是-NR 3 R 9， R 3具有上述定义，R 8为氢，1至20个碳原子的烷酰基，1至4个碳原子的烷基或芳烷基，R 9为氢，低级烷酰基，甲磺酰基，氨基甲酰基，二甲基氨磺酰基或烷氧基羰基2至5 碳原子和R 5和R 6彼此一起是-O-CH 2 -O，-O-CH 2 -CH 2 -O - ， - CH = CH-CH = CH-，-O-CH 2 -CONH-， - CH2-CH2-CONH-或-O-CO-NH-，及其无毒的药学上可接受的酸加成盐; 化合物及其盐可用作血管扩张剂和CNS刺激剂。

    Pharmaceutical compositions containing 1,1-azo bis-(1h-imidazo(1,2-a)pyridinium)dibromide compounds and the use thereof
    15.
    发明授权
    Pharmaceutical compositions containing 1,1-azo bis-(1h-imidazo(1,2-a)pyridinium)dibromide compounds and the use thereof 失效
    含有1,1-AZO BIS-（1H-IMIDAZO（1,2-A）PYRIDINIUM）二溴化碳化合物的药物组合物及其用途

    公开(公告)号：US3849557A

    公开(公告)日：1974-11-19

    申请号：US31226172

    申请日：1972-12-05

    申请人： ALLEN & HANBURYS LTD

    发明人： JACK D ,  GLOVER E

    IPC分类号： C07D235/22 ,  C07D519/00 ,  A61K27/00

    CPC分类号： C07D235/22 ,  Y10S514/906

    摘要： 1. AN INJECTABLE COMPOSITION IN DOSAGE UNIT FORM COMPRISING AS ACTIVE INGREDIENT A COMPOUND OF THE FORMULA:

    1-R4,2-R3,3-(1-R4,2-R3,4-R1,5-R2-IMIDAZOL-3-YLIUM-N=N-),

    4-R1,5-R2-IMIDAZOLIUM 2X(-)

    WHEREIN: R1 AND R2, WHICH ARE THE SAME OR DIFFERENT, ARE EACH HYDROGEN, LOWER ALKYL, HALOGEN, PHENYL, PHENYL SUBSTITUTED BY HALOGEN, PHENYL SUBSTITUTED BY HYDROXY, PHENYL SUBSTITUTED BY LOWER ALKOXY, PHENYL SUBSTITUTED BY TRIFLUOROMETHYL, PHENYL SUBSTITUTED BY NITRO; OR TOGETHER WITH THE ADJACENT CARBON ATOMS TO WHICH THEY ARE ATTACHED FORM PHENYL; R3 AND R4, WHICH ARE THE SAME OR DIFFERENT, ARE EACH LOWER ALKYL OR PHENYL, OR TOGETHER WITH THE ADJACENT NITROGEN ATOM FORM PYRIDINIUM OR TETRAHYDROPYRIDINIUM; AND X IS A PHYSIOLOGICALLY ACCEPTABLE ANION, IN ASSOCIATION WITH A PHARMACEUTICALLY ACCEPTABLE CARRIER, WHEREIN EACH DOSAGE UNIT CONTAINS FROM 2 TO 100 MGS. OF ACTIVE INGREDIENT.