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94 条记录 (耗时 0.039 秒)

    Indole derivatives as inhibitors or factor Xa
    86.
    发明授权
    Indole derivatives as inhibitors or factor Xa 有权
    吲哚衍生物作为抑制剂或因子Xa

    公开(公告)号：US06337344B1

    公开(公告)日：2002-01-08

    申请号：US09582344

    申请日：2000-08-14

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose ,  Hans Matter

    IPC分类号： A61K3144

    CPC分类号： C07D401/06 ,  C07D209/42 ,  C07D401/12 ,  C07D403/10 ,  C07D471/04

    摘要： The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.

    摘要翻译： 本发明涉及抑制血液凝固蛋白质，更具体地说，涉及式（I）的吲哚衍生物，其中R1a，R1b，R1c R1d，R2，R3，R4和A如权利要求中所示定义。 式（I）的化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式（I）化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式（I）化合物治疗和预防可以 通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防，以及式（I）化合物在制备用于这些疾病的药物中的用途。 本发明还涉及包含与惰性载体混合或以其它方式结合的式（I）化合物的组合物，特别是含有式（I）化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。

    Chromanes and their pharmaceutical compositions and methods
    88.
    发明授权
    Chromanes and their pharmaceutical compositions and methods 失效

    公开(公告)号：US5015661A

    公开(公告)日：1991-05-14

    申请号：US367082

    申请日：1989-06-16

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D491/048 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/435 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/535 ,  A61P3/06 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D311/70 ,  C07D311/72 ,  C07D405/06 ,  C07D405/10 ,  C07D407/04 ,  C07D409/00 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D491/04

    CPC分类号： C07D405/06 ,  C07D311/72 ,  C07D405/10 ,  C07D407/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D491/04

    摘要： Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.7 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl-lower alkoxy of 2-7 carbon atoms, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, amino, amino-lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy or pyridyl, or on adjacent carbons can be ##STR4## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.8, R.sub.9, R.sub.10, independently, are hydrogen, hydroxy, lower alkyl, lower alkoxy, hydroxy lower alkyl, fluorine, chlorine or lower alkanoyl provided that no more than one of R.sub.8, R.sub.9, and R.sub.10 is hydroxy, lower alkoxy, lower hydroxyalkyl, fluorine, chlorine or lower alkanoyl, and Y is CH or N, and their enantiomer and salts thereof are described.The compounds of formula I exhibit activity as inhibitors of 5-lipoxygenase and inhibit lipid peroxidation. They are, therefore, useful in the treatment of diseases caused or aggravated by excess oxidative metabolism of arachidonic acid via the 5-lipoxygenase pathway and in the treatment of inflammation, arthritis, allergies, asthma and psoriasis. The compounds of formula I can also be used to prevent peroxidation of lipids and thus protect lipid membranes from oxidative stress.

    Benzodiazepine intermediates for the preparation of imidazobenzodiazepines
    89.
    发明授权
    Benzodiazepine intermediates for the preparation of imidazobenzodiazepines 失效
    苯二氮卓中间体用于制备咪唑并二氮杂

    公开(公告)号：US4257946A

    公开(公告)日：1981-03-24

    申请号：US123525

    申请日：1980-02-21

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D243/16 ,  C07D487/04 ,  C07D401/06 ,  C07D403/06

    CPC分类号： C07D487/04 ,  C07D243/16

    摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.

    摘要翻译： 提出了一种用于制备下式的咪唑并二氮杂的多步骤方法，其中X选自氢，卤素，硝基和三氟甲基; Y选自氢，卤素或三氟甲基; R1是氢或低级烷基，R2是二取代的胺。 还提出了在该方法中使用的新型中间体。 终产物和中间体可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。 最终产品在用于术前麻醉的静脉内组合物中特别有用。

    Imidazobenzodiazepines
    90.
    发明授权
    Imidazobenzodiazepines 失效
    咪唑并二氮杂卓

    公开(公告)号：US4250095A

    公开(公告)日：1981-02-10

    申请号：US139531

    申请日：1980-04-11

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D243/16 ,  C07D487/04 ,  C07D498/04

    CPC分类号： C07D487/04 ,  C07D243/16 ,  Y10S514/906

    摘要： A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and aryl.Also presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.

    摘要翻译： 提出了一种多步骤方法，用于制备下式的咪唑并二氮杂其中X选自氢，卤素，硝基和三氟甲基，Y选自氢，卤素和三氟甲基，R 1选自 由氢，低级烷基和芳基组成的组。 还提出了在该方法中使用的新型中间体。 最终产品可用作镇静剂，抗焦虑药，肌肉松弛剂和抗惊厥药。 最终产品在用于术前麻醉的静脉内组合物中特别有用。