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17 条记录 (耗时 0.023 秒)

    1,5-Diphenylpyrazolin-3-one compounds, process and intermediates for preparation thereof and pharmaceutical compositions containing same
    3.
    发明授权
    1,5-Diphenylpyrazolin-3-one compounds, process and intermediates for preparation thereof and pharmaceutical compositions containing same 失效
    1,5-二苯基吡唑啉-3-酮化合物，其制备方法和中间体以及含有它们的药物组合物

    公开(公告)号：US4442102A

    公开(公告)日：1984-04-10

    申请号：US409631

    申请日：1982-08-19

    申请人： Henning Heinemann ,  Daniel Jasserand ,  Wolfgang Milkowski ,  Dimitri Yavordios ,  Horst Zeugner

    发明人： Henning Heinemann ,  Daniel Jasserand ,  Wolfgang Milkowski ,  Dimitri Yavordios ,  Horst Zeugner

    IPC分类号： A61K31/415 ,  A61K31/495 ,  A61P37/08 ,  C07D231/22 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D498/04 ,  C07D403/06 ,  C07D231/08

    CPC分类号： C07D401/12 ,  C07D231/22 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

    摘要： New 1,5-diphenylpyrazolin-3-one compounds and a method of preparing them are described. The compounds have the general formula I ##STR1## where R.sub.1 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or lower alkanoyloxy radical, R.sub.2 is a hydrogen or halogen atom, or a lower alkyl, or lower alkoxy radical, or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or lower alkanoyloxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, lower alkoxy radical, or R.sub.3 and R.sub.4 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical, Z is an alkylene radical with 2 to 6 carbon atoms and R.sub.5 is an optionally substituted pyridyl radical, a thienyl radical or an optionally substituted phenyl radical. The compounds have pharmacological properties, for example antiallergic properties.

    摘要翻译： 描述了新的1,5-二苯基吡唑啉-3-酮化合物及其制备方法。 该化合物具有通式I，其中R 1是氢或卤素原子，或低级烷基，低级烷氧基，羟基，三氟甲基或低级烷酰氧基，R2是氢或卤素原子，或低级烷基，或 或低级烷氧基，或R 1和R 2与相邻的碳原子键合，并且一起表示亚甲二氧基或亚乙二氧基，R 3是氢或卤原子，或低级烷基，低级烷氧基，羟基，三氟甲基或低级烷酰氧基，R 4是 氢或卤素原子，或低级烷基，低级烷氧基，或者R 3和R 4与相邻的碳原子键合，并且一起表示亚甲二氧基或亚乙二氧基，Z是具有2-6个碳原子的亚烷基，R 5是任意取代的 吡啶基，噻吩基或任选取代的苯基。 这些化合物具有药理学性质，例如抗过敏性质。

    1-Phenylindazol-3-one compounds
    6.
    发明授权
    1-Phenylindazol-3-one compounds 失效
    1-苯基吲哚-3-酮化合物

    公开(公告)号：US4537975A

    公开(公告)日：1985-08-27

    申请号：US564398

    申请日：1983-12-22

    申请人： Henning Heinemann ,  Daniel Jasserand ,  Wolfgang Milkowski ,  Dimitri Yavordios ,  Horst Zeugner

    发明人： Henning Heinemann ,  Daniel Jasserand ,  Wolfgang Milkowski ,  Dimitri Yavordios ,  Horst Zeugner

    IPC分类号： A61K31/415 ,  A61K31/495 ,  A61P37/08 ,  C07D231/56 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D403/06

    CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： Compounds corresponding to the formula: ##STR1## wherein R.sub.1 and R.sub.3 each represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sub.2 and R.sub.4 each represent hydrogen, halogen, lower alkyl or lower alkoxy; Z represents an alkylene radical with 2 to 6 carbon atoms and Y" is halogen, hydroxyl, lower alkanesulphonyl, benzenesulphonyl, or lower alkyl or halogen substituted benzenesulphonyl, and acid addition salts thereof, with the proviso the Y" is other than chlorine if R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each are hydrogen and Z is ethylene or propylene. The claimed compounds are useful intermediates in the synthesis of 1-phenyl-2-[(4-substituted piperazinyl) alkyl]-1,2-dihydro-3H-indazol-3-ones which exhibit antiallergic activity.

    摘要翻译： 对应于下式的化合物：其中R 1和R 3各自代表氢，卤素，低级烷基，低级烷氧基或三氟甲基; R2和R4各自表示氢，卤素，低级烷基或低级烷氧基; Z代表具有2至6个碳原子的亚烷基，Y“是卤素，羟基，低级链烷磺酰基，苯磺酰基或低级烷基或卤素取代的苯磺酰基，及其酸加成盐，条件是Y”不是氯 如果R1，R2，R3和R4各自为氢，Z为乙烯或丙烯。 要求保护的化合物是合成具有抗过敏活性的1-苯基-2 - [（4-取代哌嗪基）烷基] -1,2-二氢-3H-吲唑-3-酮的有用中间体。

    3-Amino-1-benzoxepine derivatives and their salts and pharmaceutical compositions thereof
    7.
    发明授权
    3-Amino-1-benzoxepine derivatives and their salts and pharmaceutical compositions thereof 失效
    3-氨基-1-苯并恶庚因衍生物及其盐及其药物组合物

    公开(公告)号：US4279904A

    公开(公告)日：1981-07-21

    申请号：US173075

    申请日：1980-07-28

    申请人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

    发明人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

    IPC分类号： A61K31/335 ,  A61K31/35 ,  A61K31/55 ,  A61P1/00 ,  A61P1/14 ,  C07D313/08

    CPC分类号： C07D313/08

    摘要： Novel 3-amino-1-benzoxepine derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another arehydrogen,C.sub.1 -C.sub.5 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4-ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.7 R.sub.8 ;R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.7 and R.sub.8 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or nitrogen, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring or said ring having heterogeneous oxygen, sulfur or NR.sub.9 ;R.sub.9 is hydrogen, methyl, benzyl, or phenyl;one of R.sub.3 and R.sub.4 is hydrogen and the other hydroxy, orR.sub.3 and R.sub.4 together are oxygen;R.sub.5 and R.sub.6 independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.5 and R.sub.6 is trifluoromethyl or nitro and the other is hydrogen; the stereo isomers and the acid addition salts thereof. These compounds have a favorable effect upon the motility of the gastro-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of motility disorders.

    摘要翻译： 公开了新的3-氨基-1-苯并恶庚因衍生物及其生产方法。 这些衍生物对应于式I其中：R1和R2彼此独立地是氢，C1-C5烷基，被末端苯基取代的C1-C5烷基或含有一个或两个卤素的苯基，甲基或甲氧基 基团，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C 2 -C 5烷基或C 3 -C 4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 7 R 8取代的C 2 -C 5烷基; R 7和R 8彼此独立地是氢或C 1 -C 5烷基; 或R 7和R 8一起为5至7元环或所述具有异质氧，硫或氮的环，或R 1和R 2一起为5至7元环或所述具有异质的氧，硫或NR 9的环; R9是氢，甲基，苄基或苯基; R3和R4之一是氢，另一个羟基或R3和R4一起是氧; R 5和R 6彼此独立地是氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 5和R 6中的一个是三氟甲基或硝基，另一个是氢; 立体异构体及其酸加成盐。 这些化合物对胃肠道的运动性具有有利的作用，因此构成用于治疗运动障碍的药物组合物和方法的活性成分。

    2,3,4,5-Tetrahydro-1-benzoxepin-3,5-dione derivatives
    8.
    发明授权
    2,3,4,5-Tetrahydro-1-benzoxepin-3,5-dione derivatives 失效
    2,3,4,5-四氢-1-苯并氧杂胨-3,5-二酮衍生物

    公开(公告)号：US4320061A

    公开(公告)日：1982-03-16

    申请号：US243745

    申请日：1981-03-16

    申请人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

    发明人： Heinrich-Wilhelm Ohlendorf ,  Klaus-Ullrich Wolf ,  Wilhelm Kaupmann ,  Henning Heinemann

    IPC分类号： A61K31/335 ,  A61K31/37 ,  A61P1/00 ,  A61P1/14 ,  C07D313/08

    CPC分类号： C07D313/08

    摘要： Novel, 3-amino-1-benzoxepin-5(2H)-one derivatives and methods for their production are disclosed. These derivatives correspond to the Formula I: ##STR1## wherein: R.sub.1 and R.sub.2 independently of one another are hydrogen,C.sub.1 -C.sub.3 alkyl,C.sub.1 -C.sub.5 alkyl substituted with a terminal phenyl, or a phenyl containing one or two halogens, methyl or methoxy groups, a 3,4-methylenedioxy or a 3,4 -ethylenedioxy group,C.sub.2 -C.sub.5 alkyl substituted with terminal hydroxy or methoxy or,C.sub.3 -C.sub.4 alkenyl; orone of R.sub.1 and R.sub.2 are hydrogen or a C.sub.1 -C.sub.5 alkyl and the other is a C.sub.2 -C.sub.5 alkyl substituted with a terminal NR.sub.5 R.sub.6 ;R.sub.5 and R.sub.6 independently of one another are hydrogen or C.sub.1 -C.sub.5 alkyl; orR.sub.5 and R.sub.6 are together a 5 or 7 member ring, orR.sub.5 and R.sub.6 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or nitrogen;R.sub.1 and R.sub.2 are together a 5 to 7 member ring, orR.sub.1 and R.sub.2 are together a 5 to 7 member ring having heterogeneous oxygen, sulfur or NR.sub.7 ;R.sub.7 is hydrogen, methyl, benzyl or phenyl;R.sub.3 and R.sub.4 are independently of one another are hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; orone of R.sub.3 and R.sub.4 is trifluoromethyl or nitro and the other is hydrogen;and the acid addition salts thereof. These compounds have a favorable effect on the treatment of spasms of the stomach-intestinal tract and, therefore, constitute the active ingredient of pharmaceutical compositions and methods for the treatment of disorders of the stomach and intestinal tract. Processes for the preparation of the derivatives and their acid addition salts and intermediate products for their preparation are also described.

    摘要翻译： 公开了3-氨基-1-苯并氧杂-5（2H） - 酮衍生物及其生产方法。 这些衍生物对应于式I：其中：R 1和R 2彼此独立地是氢，C 1 -C 3烷基，被末端苯基取代的C 1 -C 5烷基或含有一个或两个卤素的苯基，甲基或 甲氧基，3,4-亚甲二氧基或3,4-亚乙二氧基，被末端羟基或甲氧基取代的C2-C5烷基，或C3-C4烯基; 或R 1和R 2中的一个为氢或C 1 -C 5烷基，另一个为被末端NR 5 R 6取代的C 2 -C 5烷基; R 5和R 6彼此独立地是氢或C 1 -C 5烷基; 或R 5和R 6一起为5或7元环，或者R 5和R 6一起是具有异质氧，硫或氮的5至7元环; R 1和R 2一起为5至7元环，或者R 1和R 2一起为具有异质氧，硫或NR 7的5至7元环; R7是氢，甲基，苄基或苯基; R 3和R 4彼此独立地为氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基或C 1 -C 4烷硫基; 或者R 3和R 4中的一个是三氟甲基或硝基，另一个是氢; 及其酸加成盐。 这些化合物对胃肠道痉挛的治疗具有有利的作用，因此构成了用于治疗胃肠道疾病的药物组合物和方法的活性成分。 还描述了制备衍生物及其酸加成盐和中间产物用于制备的方法。