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94 条记录 (耗时 0.029 秒)

    Process for the preparation of imidazobenzodiazepines
    11.
    发明授权
    Process for the preparation of imidazobenzodiazepines 失效
    咪唑并二氮杂的制备方法

    公开(公告)号：US4244868A

    公开(公告)日：1981-01-13

    申请号：US123223

    申请日：1980-02-21

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D243/16 ,  C07D487/04 ,  C07D245/06

    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 a disubstituted amineAlso 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。

    Process for the preparation of imidazobenzodiazepines
    12.
    发明授权
    Process for the preparation of imidazobenzodiazepines 失效

    公开(公告)号：US4244867A

    公开(公告)日：1981-01-13

    申请号：US123155

    申请日：1980-02-21

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D243/16 ,  C07D471/04 ,  C07D245/06

    CPC分类号： C07D471/04 ,  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 a disubstituted amineAlso 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.

    Imidazo[1,5-.alpha.][1,4]benzodiazepines
    13.
    发明授权
    Imidazo[1,5-.alpha.][1,4]benzodiazepines 失效
    咪唑（1,5-A）（1,4）苯并嗪

    公开(公告)号：US4166185A

    公开(公告)日：1979-08-28

    申请号：US928628

    申请日：1978-07-27

    申请人： Armin Walser ,  Rodney I. Fryer ,  Louis Benjamin

    发明人： Armin Walser ,  Rodney I. Fryer ,  Louis Benjamin

    IPC分类号： C07D243/16 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D243/16 ,  Y10S514/962

    摘要： Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.

    Process for preparing imidazo[1,5-a][1,5]benzodiazepines
    14.
    发明授权
    Process for preparing imidazo[1,5-a][1,5]benzodiazepines 失效
    制备咪唑并[8,1-a {9 {1,8,5-二唑并[

    公开(公告)号：US4146537A

    公开(公告)日：1979-03-27

    申请号：US874075

    申请日：1978-02-01

    申请人： Armin Walser ,  Rodney I. Fryer

    发明人： Armin Walser ,  Rodney I. Fryer

    IPC分类号： A61K31/55 ,  A61P21/02 ,  A61P25/20 ,  C07D243/12 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D243/12 ,  Y10S514/906

    摘要： The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be different,And the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.

    摘要翻译： 本发明涉及下式的化合物，其中X是氢或卤素; R1是氢，卤素或三氟甲基; R2是氢或低级烷基; 并且R 3是氢，-COO低级烷基或CON（R 4）2，其中R 4是低级烷基或氢并且可以是不同的，并且其药学上可接受的盐。

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    18.
    发明授权
    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂

    公开(公告)号：US06664393B2

    公开(公告)日：2003-12-16

    申请号：US10227222

    申请日：2002-08-26

    申请人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    发明人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    IPC分类号： C07D23924

    CPC分类号： C07D213/30 ,  C07C279/14 ,  C07D213/40 ,  C07D215/48 ,  C07D239/28

    摘要： The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中A，L，Y和k具有说明书和权利要求书中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望的活性的条件或用于治愈或预防其中 旨在抑制因子Xa和/或因子VIIa。 本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical
    19.
    发明授权
    4-fluoro-N-indan-2-yl benzamide and its use as a pharmaceutical 有权
    4-氟-N-茚满-2-基苯甲酰胺及其作为药物的用途

    公开(公告)号：US06617359B2

    公开(公告)日：2003-09-09

    申请号：US10073330

    申请日：2002-02-13

    申请人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    发明人： Paulus Wohlfart ,  Teri Suzuki ,  Ramalinga M. Dharanipragada ,  Alena Safarova ,  Armin Walser ,  Hartmut Strobel

    IPC分类号： A61K3165

    CPC分类号： C07C233/65 ,  A61K31/166 ,  C07C2602/08

    摘要： The present invention relates to the method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan-2-yl benzamide according to the formula (I) to the said mammal. The compound (I) can be used for the therapy and prophylaxis of cardiovascular diseases like stable and unstable angina pectoris, Prinzmetal angina (spasm), acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease PAOD, atherosclerosis, restenosis, endothelial damage after PTCA, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, and the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives, the therapy and prophylaxis of diabetes and diabetes complications (nephropathy, retinopathy), angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, restricted memory performance or a restricted ability to learn.

    摘要翻译： 本发明涉及刺激哺乳动物内皮细胞NO合成酶表达的方法，该方法包括将生理活性量的式（I）的4-氟-N-茚满-2-基苯甲酰胺给予 哺乳动物说 化合物（I）可用于治疗和预防心血管疾病如稳定和不稳定型心绞痛，Prinzmetal心绞痛（痉挛），急性冠状动脉综合征，心力衰竭，心肌梗死，中风，血栓形成，外周动脉闭塞性疾病PAOD，动脉粥样硬化 ，PTCA后再狭窄，内皮损伤，原发性高血压，肺动脉高压，继发性高血压，肾血管性慢性肾小球肾炎，勃起功能障碍，室性心律失常，绝经后妇女心血管危险降低或避孕药物摄入后，糖尿病和糖尿病的治疗和预防 并发症（肾病，视网膜病变），血管生成，哮喘支气管炎，慢性肾功能衰竭，肝硬化，限制性记忆能力或受限的学习能力。

    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
    20.
    发明授权
    N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
    N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂

    公开(公告)号：US06472562B1

    公开(公告)日：2002-10-29

    申请号：US09697188

    申请日：2000-10-27

    申请人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    发明人： Otmar Klingler ,  Gerhard Zoller ,  Elisabeth Defossa ,  Fahad A. Al-Obeidi ,  Armin Walser ,  James Ostrem

    IPC分类号： C07C23305

    CPC分类号： C07D213/30 ,  C07C279/14 ,  C07D213/40 ,  C07D215/48 ,  C07D239/28

    摘要： The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中A，L，Y和k具有说明书和权利要求书中所示的含义。 式I的化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不需要的活性或用于治愈或预防其中 旨在抑制因子Xa和/或因子VIIa。 本发明还涉及制备式I化合物，其用途，特别是药物中的活性成分以及包含它们的药物制剂的方法。