Peripherally-Selective Inhibitors of Dopamine-ß-Hydroxylase And Method Of Their Preparation
    91.
    发明申请
    Peripherally-Selective Inhibitors of Dopamine-ß-Hydroxylase And Method Of Their Preparation 有权
    多巴胺羟脯氨酸的外周选择性抑制剂及其制备方法

    公开(公告)号:US20070015730A1

    公开(公告)日:2007-01-18

    申请号:US11533462

    申请日:2006-09-20

    IPC分类号: A61K31/695 C07F7/02

    摘要: Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

    摘要翻译: 式I化合物:其中R 1,R 2和R 3 3相同或不同,表示氢,卤素,烷基,烷基芳基, 烷氧基,羟基,硝基,氨基,烷基羰基氨基,烷基氨基或二烷基氨基; R 4表示氢,烷基或烷基芳基; X是CH 2,O或S,n是1,2或3,条件是如果X是CH 2,n不为1,并且方法 为他们的准备。 这些化合物具有用于治疗心血管疾病如高血压和慢性心力衰竭的潜在有价值的药物性质。

    Substituted alcohols useful in treatment of Alzheimer's disease
    93.
    发明申请
    Substituted alcohols useful in treatment of Alzheimer's disease 审中-公开
    用于治疗阿尔茨海默病的取代的醇

    公开(公告)号:US20060178345A1

    公开(公告)日:2006-08-10

    申请号:US11324678

    申请日:2006-01-03

    摘要: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.

    摘要翻译: 本发明涉及式(I)的取代醇化合物:其中X,R 1,R 2,R 3,R SUB > N,R 20和R C C在本文中定义。 这些化合物可用于治疗或预防阿尔茨海默氏病,更具体地可用于能够抑制β-分泌酶的化合物,该酶分解淀粉样蛋白前体蛋白以产生淀粉状蛋白β肽(A-β),其是淀粉样蛋白的主要成分 在阿尔茨海默病患者的大脑中发现的斑块。

    Amidino derivatives and their use as thrombin inhibitors
    95.
    发明授权
    Amidino derivatives and their use as thrombin inhibitors 失效
    脒衍生物及其作为凝血酶抑制剂的用途

    公开(公告)号:US07074820B2

    公开(公告)日:2006-07-11

    申请号:US09839609

    申请日:2001-04-23

    申请人: Thomas Antonsson

    发明人: Thomas Antonsson

    IPC分类号: A01N43/06

    摘要: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

    摘要翻译: 提供式I化合物,其中R 1,R 2,R 3,Y,n和B具有在说明书中给出的含义 其可用作胰蛋白酶样蛋白酶(例如凝血酶)的竞争性抑制剂,特别是用于治疗需要凝血酶抑制(例如血栓形成)或作为抗凝剂的条件。