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    Azepine derivatives and their anti-thrombotic compositions and methods
    5.
    发明授权
    Azepine derivatives and their anti-thrombotic compositions and methods 失效
    Azepine衍生物及其抗血栓形成和方法

    公开(公告)号：US4414225A

    公开(公告)日：1983-11-08

    申请号：US348496

    申请日：1982-02-12

    申请人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    发明人： Robert Sauter ,  Gerhart Griss ,  Wolfgang Grell ,  Rudolf Hurnaus ,  Bernhard Eisele ,  Walter Haarmann ,  Eckhard Rupprecht

    IPC分类号： C07D487/02 ,  A61K31/55 ,  A61P3/06 ,  A61P7/02 ,  C07D223/06 ,  C07D487/04 ,  C07D491/02 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/40

    CPC分类号： C07D487/04 ,  C07D223/06 ,  C07D491/04 ,  C07D495/04

    摘要： Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.

    摘要翻译： 其中n和m各自为1,2或3，并且n + m的和为4; R1是烷基; 烯基; 未取代的，单或二取代的芳烷基; 未取代的，单或二取代的苯甲酰基; 烷氧基羰基 芳烷氧羰基; 或者当m和n各自为2和/或R 2和R 3不同时为氢时，也为氢; R2和R3之一是氢或氨基，另一个是羧基或烷氧基羰基; 或当R3为氢时，R2为氢; 氨基; 烷氧基羰基 - 氨基; （未取代或单取代的苯基） - 氨基羰基 - ; （未取代或单取代的苯基）乙基氨基羰基; 叠氮羰基; 或肼基羰基; X是氧，硫或者其中R 4是氢; 烷基; 苯基 - 烷基; 或苯基; 无毒，药理学上可接受的酸加成盐; 并且当R 2或R 3为羧基时，与无机或有机碱形成的无毒的药学上可接受的盐。 化合物及其盐可用作抗血栓形成剂。

    Fused-ring amino-pyrazines as bradycardiac agents
    6.
    发明授权
    Fused-ring amino-pyrazines as bradycardiac agents 失效
    稠环氨基吡嗪作为心动过缓剂

    公开(公告)号：US4409220A

    公开(公告)日：1983-10-11

    申请号：US297024

    申请日：1981-08-27

    申请人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    发明人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    IPC分类号： A61K31/495 ,  A61K31/55 ,  A61P9/02 ,  A61P9/06 ,  A61P9/12 ,  A61P25/02 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    摘要翻译： 其中A和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基 ），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基， 苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。

    Fused-ring amino-pyrazines as bradycardiacs
    7.
    发明授权
    Fused-ring amino-pyrazines as bradycardiacs 失效
    融合环氨基吡嗪作为心动过缓

    公开(公告)号：US4486433A

    公开(公告)日：1984-12-04

    申请号：US501437

    申请日：1983-06-06

    申请人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    发明人： Rudolf Hurnaus ,  Gerhart Griss ,  Robert Sauter ,  Wolfgang Grell ,  Walter Kobinger ,  Ludwig Pichler

    IPC分类号： A61K31/495 ,  A61K31/55 ,  A61P9/02 ,  A61P9/06 ,  A61P9/12 ,  A61P25/02 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    摘要翻译： 其中A和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基 ），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基， 苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。

    Tetrahydro-azepinoquinolines
    8.
    发明授权
    Tetrahydro-azepinoquinolines 失效
    四氮唑腈

    公开(公告)号：US3987047A

    公开(公告)日：1976-10-19

    申请号：US520965

    申请日：1974-11-05

    申请人： Gerhart Griss ,  Rudolf Hurnaus ,  Wolfgang Grell ,  Robert Sauter ,  Richard Reichl

    发明人： Gerhart Griss ,  Rudolf Hurnaus ,  Wolfgang Grell ,  Robert Sauter ,  Richard Reichl

    IPC分类号： C07D471/04 ,  C07D491/14 ,  C07D491/147

    CPC分类号： C07D471/04 ,  C07D491/14 ,  Y10S514/96 ,  Y10S514/966

    摘要： Compounds of the formula ##SPC1##Wherein ##EQU1## where R.sub.1 is hydrogen, straight or branched aliphatic acyl of 1 to 12 carbon atoms, methoxy-substituted straight or branched aliphatic acyl of 1 to 12 carbon atoms, benzoyl, halo-benzoyl, carbalkoxy of 2 to 7 carbon atoms, carbcycloalkoxy of 4 to 7 carbon atoms, benzyl, methylbenzyl, phenylsulfonyl, halo-phenylsulfonyl, tolylsulfonyl, alkenyl of 2 to 6 carbon atoms, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl, methylsulfonyl or--B -- XwhereB is straight or branched alkylene of 1 to 6 carbon atoms, andX is hydrogen, hydroxyl, methoxy, carboxyl, cyano, dimethylaminocarbonyl, morpholino-carbonyl or carbalkoxy of 2 to 6 carbon atoms,R.sub.2 is hydrogen, hydroxyl, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkanoyloxy of 1 to 3 carbon atoms, alkoxycarbonyloxy of 2 to 4 carbon atoms, amino, dimethylamino, morpholino or halogen,R.sub.3 is hydrogen, halogen, hydroxyl, carboxyl, straight or branched alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms, phenyl-alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms -- alkoxy of 1 to 3 carbon atoms, carbalkoxy of 2 to 4 carbon atoms, hydroxymethyl, phenyl, phenoxy, amino, pyrrolidino or morpholino,R.sub.4, r.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen, halogen, methyl, hydroxyl, methoxy, cyano, amino, nitro, trifluoromethyl, carboxyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, or any two of R.sub.4, R.sub.5 and R.sub.6 together are methylenedioxy, andX.sub.1 and X.sub.2 are hydrogen or together form a double bond,6-N-oxides thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anoretics.

    1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1)
    10.
    发明授权
    1-Phenyl-2,2,4,4-C.sub.1 -C.sub.2 alkyl-3-[4-(phenyl or pyridyl)-piperazino]-cyclobutanols-(1) 失效
    1-苯基-2,2,4,4-C（HD 1 {B -C {HD 2 {B烷基-3- {8 4-（苯基或吡啶基） - 哌嗪基{9-环丁烷醇 - （1）

    公开(公告)号：US3931185A

    公开(公告)日：1976-01-06

    申请号：US413233

    申请日：1973-11-06

    申请人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    发明人： Manfred Kleemann ,  Joachim Kahling ,  Gerhart Griss ,  Rudolf Hurnaus

    IPC分类号： C07D295/08 ,  A61K31/495 ,  A61K31/496 ,  C07D213/74 ,  C07D213/79 ,  C07D295/00 ,  C07D295/04 ,  C07D295/096 ,  C07D295/135 ,  C07D405/08 ,  C07D295/12

    CPC分类号： C07D295/096 ,  A61K31/495 ,  C07D295/135 ,  Y10S514/906

    摘要： This invention relates to cyclobutane derivatives having the formula ##SPC1##Wherein R.sub.1 to R.sub.3, which may be the same or different, represent hydrogen atoms, halogen atoms, hydroxy, trifluoromethyl, benzyloxy, acyloxy groups, alkyl groups with 1 to 6 carbon atoms, alkoxy groups with 1 to 3 carbon atoms, phenyl, cyclohexyl, or 2 of the radicals R.sub.1 to R.sub.3 together represents a methylenedioxy group,R.sub.4 represents a hydrogen atom or an alkyl group with 1 or 2 carbon atoms,R.sub.5 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms andR.sub.6 represents a phenyl group, which may be mono- or disubstituted by halogen atoms, trifluoromethyl, hydroxy, nitro, amino, benzyloxy, acyloxy groups, alkyl groups with 1 to 3 carbon atoms, alkoxy groups with 1 to 3 carbon atoms or alkylthio groups with 1 to 3 carbon atoms; or a pyridyl group, optionally substituted by a halogen atom, a hydroxy, nitro, amino, benzyloxy, acyloxy, carboxy group, a carbalkoxy group with 1 to 3 carbon atoms in the alkoxy, an alkyl group with 1 to 3 carbon atoms or an alkoxy group with 1 to 3 carbon atoms;To salts thereof with physiologically compatible inorganic or organic acids or bases as well as to processes for their preparation.The cyclobutane compounds of the above general formula show valuable pharmacological properties, especially a sedative and muscle relaxing activity.

    摘要翻译： 本发明涉及具有式WHEREIN R 1至R 3的环丁烷衍生物，其可以相同或不同，表示氢原子，卤素原子，羟基，三氟甲基，苄氧基，酰氧基，具有1-6个碳原子的烷基， 1至3个碳原子，基团R 1至R 3的苯基，环己基或2一起表示亚甲二氧基，R 4表示氢原子或具有1或2个碳原子的烷基，R 5表示氢原子或 1至3个碳原子，R 6表示可被卤素原子，三氟甲基，羟基，硝基，氨基，苄氧基，酰氧基，具有1至3个碳原子的烷基，1至3个碳原子的烷基， 3个碳原子或1〜3个碳原子的烷硫基; 或任选被卤素原子取代的吡啶基，羟基，硝基，氨基，苄氧基，酰氧基，羧基，烷氧基中具有1至3个碳原子的烷氧基，具有1至3个碳原子的烷基或 具有1至3个碳原子的烷氧基; 与生理学兼容的有机酸或有机酸或基础同样适用于其制备方法。