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    Process for the manufacture of racemic (R,R; S,S) asocainol
    12.
    发明授权
    Process for the manufacture of racemic (R,R; S,S) asocainol 失效
    用于制备外消旋（R，R; S，S）asocainol的方法

    公开(公告)号：US4649196A

    公开(公告)日：1987-03-10

    申请号：US730124

    申请日：1985-05-03

    申请人： Wolfgang Herrmann ,  Gerhard Satzinger

    发明人： Wolfgang Herrmann ,  Gerhard Satzinger

    IPC分类号： A61K31/395 ,  A61P9/06 ,  C07D225/08

    CPC分类号： C07D225/08

    摘要： A process for the preparation of racemic asocainol in the (R,R; S,S)-form and (-)-asocainol in the (S,S)-form as well as the pharmacologically compatible salts thereof is herein described on the basis of a thermal rearrangement of the inactive (R,S)-diastereomer to the (S,S)-form.Racemic (.+-.)-asocainol and the (-)-enantiomer are potent antiarrhythmic agents and local anesthetics.

    摘要翻译： 在（S，S）形式的（R，R; S，S）形式和（ - ） - 焦氨醇中制备外消旋asocainol以及其药理学上相容的盐的方法在此基于 的非活性（R，S） - 非对映体与（S，S） - 形式的热重排。 外消旋（+/-） - asocainol和（ - ） - 对映异构体是有效的抗心律失常药和局部麻醉药。

    Process for the preparation of 4-hydroxy-3-(heterocyclocarbamoyl)-2H-1,2-benzothiazine-1,1-dioxides
    13.
    发明授权
    Process for the preparation of 4-hydroxy-3-(heterocyclocarbamoyl)-2H-1,2-benzothiazine-1,1-dioxides 失效
    制备4-羟基-3-（杂环氨基甲酰基）-2H-1,2-苯并噻嗪-1,1-二氧化物的方法

    公开(公告)号：US4477661A

    公开(公告)日：1984-10-16

    申请号：US478763

    申请日：1983-03-25

    申请人： Wolfgang Herrmann ,  Wolfram Geibel ,  Gerhard Satzinger

    发明人： Wolfgang Herrmann ,  Wolfram Geibel ,  Gerhard Satzinger

    IPC分类号： C07D417/12 ,  C07D401/12

    CPC分类号： C07D417/12

    摘要： The present invention provides a process for the preparation of 4-hydroxy-3-(heterocyclocarbamoyl)-2H-1,2-benzothiazine-1,1-dioxides of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl radical, R.sub.2 is a nitrogen-containing heterocyclic radical and R.sub.3 is a hydrogen or halogen atom or a methyl radical, and of the alkali metal, alkaline earth metal and amine salts thereof, by the reaction of an amine-substituted, nitrogen-containing heterocyclic compound with a halo-acetyl halide, reaction of the intermediate thus obtained with sodium benzoic acid sulphimide, ring expansion of the benzoisothiazole ring to give a benzothiazine ring and, in case R.sub.2 is to be an isoxazolyl radical, reverse rearrangement of the oxadiazole-ring formed by ring expansion to the isoxazolyl ring, wherein (in a one-pot reaction A) the reaction of an amine-substituted, nitrogen-containing heterocyclic compound with a halo-acetyl halide is carried out, without the addition of a base, in boiling ethyl acetate, the intermediate formed is, without isolation, reacted with sodium benzoic acid sulphimide and the reaction product isolated, whereafter, in a one-pot reaction B, the reaction product from the one-pot reaction A is reacted in a dipolar aprotonic solvent under an atmosphere of a protection gas with a strongly basic alkali-alkohole and thereafter with so much acid that about 2 equivalents of base remained unneutralized in the reaction solution and, if desired, the benzothiazine ring is N-methylated in the usual manner and the product obtained is, if desired, converted in known manner into an alkali metal, alkaline earth metal or amine salt.

    摘要翻译： 本发明提供了制备下列通式的4-羟基-3-（杂环氨基甲酰基）-2H-1,2-苯并噻嗪-1,1-二氧化物的方法：其中R 1是氢原子或甲基 自由基，R2是含氮杂环基，R3是氢或卤素原子或甲基，以及其碱金属，碱土金属和胺盐，通过胺取代的含氮杂环 与卤代 - 乙酰卤的化合物，由此获得的中间体与苯甲酸亚磺酰亚胺的反应，苯并异噻唑环的环扩展得到苯并噻嗪环，并且在R2为异恶唑基的情况下，恶二唑环的反向重排 通过环扩展形成异恶唑环，其中（在一锅反应A）中，胺取代的含氮杂环化合物与卤代 - 乙酰卤的反应在不加碱的情况下进行 沸腾等 乙酸乙酯，形成的中间体不经分离，与苯甲酸亚磺酰亚胺反应，分离出反应产物，然后在一锅反应B中，来自一锅反应A的反应产物在偶极非质子溶剂 在具有强碱性碱性碱性气体的保护气体的气氛下，然后用如此多的酸使约2当量的碱在反应溶液中保持未中和，如果需要，苯并噻嗪环以常规方式进行N-甲基化，并且 如果需要，获得的产物以已知的方式转化为碱金属，碱土金属或胺盐。

    Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis
    16.
    发明授权
    Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis 失效
    使用1,6-萘啶酮衍生物治疗肺血栓形成

    公开(公告)号：US4698341A

    公开(公告)日：1987-10-06

    申请号：US753758

    申请日：1985-07-11

    申请人： Gerhard Satzinger ,  Johannes Hartenstein ,  Karl Mannhardt ,  Jurgen Kleinschroth ,  Manfred Herrmann ,  Edgar Fritschi ,  Horst-Dietmar Tauschel ,  Bernd Wagner ,  Gunter Wolf

    发明人： Gerhard Satzinger ,  Johannes Hartenstein ,  Karl Mannhardt ,  Jurgen Kleinschroth ,  Manfred Herrmann ,  Edgar Fritschi ,  Horst-Dietmar Tauschel ,  Bernd Wagner ,  Gunter Wolf

    IPC分类号： C07D211/90 ,  C07D471/04 ,  A61K31/455 ,  A61K31/535

    CPC分类号： C07D471/04 ,  C07D211/90

    摘要： New 1,6-naphthyridinone derivatives of the formula I ##STR1## are herein described wherein R.sup.1 represents an unsubstituted or substituted aromatic or heteroaromatic ring;R.sup.2 is hydrogen, a straight-chained or branched alkyl, alkoxyalkyl, or a substituted or unsubstituted aminoalkyl group with up to ten carbon atoms;R.sup.3 is hydrogen, a straight-chained or branched alkyl group, or an alkoxycarbonyl radical with up to four carbon atoms;R.sup.4 is hydrogen, or a morpholinoethyl group;R.sup.5 is a straight-chained or branched alkyl group with up to four carbon atoms, or an amino group; andR.sup.6 is a carboxyl group, or an alkyl- or alkyloxyalkyl carbonyl radical, containing up to 12 carbon atoms and optionally interrupted by an oxygen, sulphur, or nitrogen atom;as well as optionally the pharmacologically acceptable salts thereof; processes for the preparation of these derivatives and their use in the control of vascular diseases.

    摘要翻译： 本文描述了式I（I）的新的1,6-萘啶酮衍生物，其中R 1表示未取代或取代的芳族或杂芳族环; R2是氢，直链或支链烷基，烷氧基烷基或具有至多10个碳原子的取代或未取代的氨基烷基; R3是氢，直链或支链烷基或具有至多四个碳原子的烷氧基羰基; R4是氢或吗啉代乙基; R5是具有至多4个碳原子的直链或支链烷基或氨基; 并且R 6是含有至多12个碳原子并任选被氧，硫或氮原子中断的羧基或烷基 - 或烷氧基烷基羰基; 以及任选地其药理学上可接受的盐; 这些衍生物的制备方法及其在血管疾病控制中的应用。

    Benzo(b)thiophene derivatives
    19.
    发明授权
    Benzo(b)thiophene derivatives 失效
    BENZO（B）噻吩衍生物

    公开(公告)号：US4056526A

    公开(公告)日：1977-11-01

    申请号：US691109

    申请日：1976-05-28

    申请人： Peter Johannes Stoss ,  Manfred Franz Reinhold Herrmann ,  Gerhard Satzinger

    发明人： Peter Johannes Stoss ,  Manfred Franz Reinhold Herrmann ,  Gerhard Satzinger

    IPC分类号： C07D413/04 ,  C07D413/02

    CPC分类号： C07D413/04

    摘要： The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 R.sup.3, wherein R' is an alkyl radical of 1 to 5 carbons which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.3 represents either a hydroxyl or an amino group which may be substituted by lower alkyl, dialkyl, alkylidene, phenyl or acyl groups or a lower alkyl group which may be substituted by hydroxy, lower alkoxy, phenoxy, dialkylamino, pyrrolidino, piperidino or morpholino groups; R.sup.3 further is a cycloalkyl or phenyl group, which may be substituted by a halogen or a lower alkoxy radical; or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, may form an aziridine, pyrrolidine, piperidine, morpholine or piperazine ring which may be substituted by lower alkyl, hydroxyalkyl, phenylalkyl, phenyl or acetyl groups; or A and B together with the C.dbd.N group may form a 5, 6, or 7-membered heterocyclic ring.