首页> 外国专利> The use of the derivatives as inhibiting protein apolipoprotein B protein (or) of (apo B) secretion and production of isoquinoline-6-ylamide derivatives, birds and agent glycerides microsomal transfer protein - biphenyl-2-carboxylic acid - tetrahydro

The use of the derivatives as inhibiting protein apolipoprotein B protein (or) of (apo B) secretion and production of isoquinoline-6-ylamide derivatives, birds and agent glycerides microsomal transfer protein - biphenyl-2-carboxylic acid - tetrahydro

机译:衍生物作为抑制载脂蛋白B蛋白(或)(载脂蛋白B)分泌和生产异喹啉-6-基酰胺衍生物,禽类和甘油三酯制剂微粒体转移蛋白-联苯-2-羧酸-四氢

摘要

The compounds of the summary formula 1, formula, X, or (57) CH 2, CO, CS, 2 SO; (ie, covalent bond) Y is an aliphatic hydrocarbylene of up to 20 carbon atoms direct bond is a radical, the radical is mono substitution hydroxy, (C 1 ~C 10) alkoxy, (C 1 ~C 10) acyl, or (C 1 ~C 10) acyloxy, a (C 6 ~C 10) allyl radicals which may, NH, and one which is selected from O, X if is CH 2, then, is a direct bond Y; the Z, is selected from the following group: (1) H, halo , cyano, (2) hydroxy, (C 1 ~C 10) alkoxy, (C 1 ~C 10) alkylthio, (C 1 ~C 10) acyl, thiophenylcarbonyl, (C 1 ~C 10) alkoxycarbonyl, ( (C 1 ~C 10) alkylamino, di (C 1 ~C 10) alkylamino, (C 6 ~C 10) aryl (C 1 ~C 10) alkylamino, Y is not a NH or O, 3) ( condensation benz derivatives thereof 4) non-substituted vinyl, (C 6 ~C 10) aryl, and (C 3 ~C 8) cycloalkyl, (C 7 ~C 10) poly-cycloalkyl, (C 4 ~C 8) cyclo alkenyl, (C 7 ~C 10) poly cycloalkenyl, (5) (C 6 ~C 10) aryloxy, (C 6 ~C 10) arylthio, (C 6 ~C 10) aryl (C 1 ~C 10) The condensed multi-alkoxy, (C 6 ~C 10) aryl (C 1 ~C 10) alkylthio, (C 3 ~C 8) Cycloalkyloxy, (C 4 ~C 8) cycloalkenyloxy, (6) and one annular radical saturated heterocyclyl selected from the group consisting of the cyclic radicals, the radical is not the individual rings of the radicals of oxygen, nitrogen, and also contains a ring 4 heteroatoms total 1 is independently selected from sulfur Well, X if is CH 2, then even an aromatic ring or a saturated, or group H (4) and Z is one selected from (6), when Z contains one or more rings, Each separately, said ring from halo, hydroxy, cyano, nitro, oxo (O =), thioxo (S =), aminosulfonyl, phenyl, phenoxy, phenylthio, halo-phenylthio, benzyl, benzyloxy, (C 1 ~C 10) alkyl, (C 1 ~C 10) alkoxy, (C 1 ~C 10) alkoxycarbonyl, (C 1 ~C 10) alkylthio, (C 1 ~C 10) alkylamino, (C 1 ~C 10) alkyl aminocarbonyl, di (C 1 ~C 10) alkylamino, di (C 1 ~C 10) alkylaminocarbonyl, di (C 1 ~C 10) alkylamino (C 1 ~C 10) alkoxy, (C 1 ~C 3) perfluoroalkyl, (C 1 ~C 3) perfluoroalkoxy, (C 1 ~C 10) acyl, (C 1 ~C 10) acyloxy, (C 1 ~C 10) acyloxy (C 1 ~C 10) alkyl, and its salts 0 is selected from pyrrolidinyl individually to it, and may have a substituent 4, pharmaceutically acceptable. The present invention, useful atherosclerosis and to prevent and treat its clinical sequelae thereby triglyceride transfer protein of microsomes and also is an inhibitor B protein protein apolipoprotein (or) of (apo B) secretion on a compound. And compositions containing said compounds The present invention relates to a method of treating a compound of structure (or) atherosclerosis, obesity, and related diseases.
机译:通式1,通式,X或(57)CH 2, CO,CS, 2 SO的化合物; (即共价键)Y是最多20个碳原子的脂族亚烃基,直接键是一个基团,该基团是单取代羟基,(C 1 〜C 10)烷氧基,(C 1 〜C 10)酰基,或(C 1 〜C 10)酰氧基, a(C 6 〜C 10)烯丙基,可以是NH,如果是CH 2,则选自O,X则是一个,那么,是直接键Y; Z选自以下基团:(1)H,卤素,氰基,(2)羟基,(C 1 〜C 10)烷氧基,(C < Sub> 1 〜C 10)烷硫基,(C 1 〜C 10)酰基,硫代苯基羰基,(C 1 〜C 10)烷氧羰基,((C 1 〜C 10)烷基氨基,二(C 1 < / Sub>〜C 10)烷基氨基,(C 6 〜C 10)芳基(C 1 〜C 10)烷基氨基,Y不是NH或O,3)(其缩合苯并衍生物4)未取代的乙烯基,(C 6 〜C 10) 芳基和(C 3 〜C 8)环烷基,(C 7 〜C 10)聚环烷基,(C 4 〜C 8)环烯基,(C 7 〜C 10)聚环烯基,(5)(C 6 〜C 10)芳氧基,(C 6 〜C 10)芳硫基,(C 6 〜C 10)芳基(C 1 〜C 10)稠合多烷氧基,(C 6 〜C < Sub> 10)芳基(C 1 〜C 10)烷硫基,(C 3 〜C 8)< / Sub>环烷氧基(C 4 〜C 8)环烯氧基(6)和一个选自环状基团的环基饱和杂环基,该基团为而不是氧,氮自由基的单个环,并且还包含一个环4个杂原子,总共1个独立地选自硫井,X如果是CH 2 ,那么即使是芳环或饱和环,或基团H(4),并且Z是选自(6)的一个,当Z包含一个或多个环时,每个环分别由卤素,羟基,氰基,硝基,氧代(O =),硫代(S =)表示,氨基磺酰基,苯基,苯氧基,苯硫基,卤代苯硫基,苄基,苄氧基,(C 1 〜C 10)烷基,(C 1 〜 C 10)烷氧基,(C 1 〜C 10)烷氧基羰基,(C 1 〜C 10)烷硫基,(C 1 〜C 10)烷氨基,(C 1 〜C < Sub> 10)烷基氨基羰基二(C 1 〜C 10)烷基氨基羰基二(C 1 〜C 10)烷基氨基羰基,二(C 1 〜C 10)烷基氨基(C 1 〜C 10)< / Sub>烷氧基,(C 1 〜C 3)全氟烷基,(C 1 〜C 3)全氟烷氧基,(C 1 〜C 10)酰基,(C 1 〜C 10)酰氧基,(C < Sub> 1 〜C 10)酰氧基(C 1 〜C 10)烷基,其盐0选自吡咯烷基可以单独地被取代,并且可以具有可药用的取代基4。本发明可用于动脉粥样硬化并预防和治疗其临床后遗症,从而使微粒体的甘油三酸酯转移蛋白,并且也是化合物上的(或)(apo B)分泌的抑制剂B蛋白(载脂蛋白)。以及包含所述化合物的组合物本发明涉及治疗具有结构(或)动脉粥样硬化,肥胖症和相关疾病的化合物的方法。

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