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    • 1. 发明授权
    • S-oxide lipid lowering compounds
    • S-氧化物降脂化合物
    • US06451802B1
    • 2002-09-17
    • US09857838
    • 2001-06-08
    • Cornelus Gerardus Maria JanssenPeter Walter Maria RoevensJozef Bertha August Thijssen
    • Cornelus Gerardus Maria JanssenPeter Walter Maria RoevensJozef Bertha August Thijssen
    • A61K31496
    • C07D405/14C07D417/14
    • The present invention relates to compounds of formula (I) the N-oxides, the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts, wherein n is 1 or 2, R1 is hydrogen, C1-6alkyl or halo; R2 is hydrogen or halo; R3 is C1-8alkyl or C3-6cycloalkyl; Hetis an optionally substituted triazole, imidazole, or thiazole; and —A—B— is a bivalent radical of formula —CH═CH—, —N═CH—, —CH═N—, wherein optionally one of the hydrogen atoms is replaced by C1-4alkyl; having apolipoprotein B inhibiting activity and concomitant lipid lowering activity. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating disorders caused by an excess of very low density lipoproteins (VLDL) or low density lipoproteins (LDL), and especially disorders caused by the cholesterol associated with said VLDL and LDL, such as, for example, hyperlipidemia, obesitas or atherosclerosis.
    • 本发明涉及式(I)化合物的N-氧化物,其立体化学异构形式和药学上可接受的酸加成盐,其中n为1或2,R 1为氢,C 1-6烷基或卤素; R2是氢或卤素; R3是C1-8烷基或C3-6环烷基; Hetis是任选取代的三唑,咪唑或噻唑; 并且-A-B-是式-CH = CH-,-N = CH-,-CH = N-的二价基团,其中任选地一个氢原子被C 1-4烷基取代; 具有载脂蛋白B抑制活性和伴随的降脂活性。 公开了用于制备所述产品的方法,包含所述产品的制剂及其作为药物的用途,特别是用于治疗由过量非常低密度脂蛋白(VLDL)或低密度脂蛋白(LDL)引起的疾病,特别是由 与所述VLDL和LDL相关的胆固醇,例如高脂血症,肥胖或动脉粥样硬化。