首页> 外国专利> Derivatives of 2 - (4 - (4 - (3, 5 - bis - (trifluoromethyl benzyl) - 2 - methyl - 2h-tetrazol-5-yl) - amino - 2 - ethyl - 2 - trifluoromethyl - 3,4-dihydro - 2H - quinoline - 1 - carbonyl} - cyclohexyl) - acetamide as CETP inhibitors

Derivatives of 2 - (4 - (4 - (3, 5 - bis - (trifluoromethyl benzyl) - 2 - methyl - 2h-tetrazol-5-yl) - amino - 2 - ethyl - 2 - trifluoromethyl - 3,4-dihydro - 2H - quinoline - 1 - carbonyl} - cyclohexyl) - acetamide as CETP inhibitors

机译:2-(4-(4-(3,5-[双-(三氟甲基苄基)-2-甲基-2h-四唑-5-基)-氨基]-2-乙基-2-三氟甲基-3,4的衍生物-二氢-2H-喹啉-1-羰基}-环己基)-乙酰胺作为CETP抑制剂

摘要

Refers to compounds of 4 - amino - 2 - 1,2,3,4 - Tetrahidroquinolina of formula (i) wherein R1 is and W - O - W and - and or; where W is carbonyl; and Z is (C1 - C10) or alkyl, optionally substituted amino oxo Halo, amido, alkoxy (C1 - C6), carboxy, among others; Z is a ring, such as Cyclohexyl substituted, optionally with amido or carboxy alkyl (C1 - C6)Among others, R2 is alkyl (c1-c4) or cycloalkyl (C1 - C6); R4 is V, - cooalquilo (c1-c4), among others, where V is tetrazolilo, oxadiazolilo, among others, optionally substituted; R5, R6, R7 and R8 are independently h, halogen, alkyl, cyano, (c1-c4) or alkoxy optionally substituted with has Logeno.Are preferred: acid ethyl ester ({4 - [4 - (3,5-bis - (trifluoromethyl) - benzyl) - 2 - methyl - 2h-tetrazol-5-yl) - amino] - 2 - ethyl - 2 - trifluoromethyl - 3,4-dihydro - 2H - quinoline - 1 - carbonyl) cyclohexyl] Acid, (2R, 4S) - {{2 - (4 - [4 - (3,5-bis - (trifluoromethyl) - benzyl) - 2 - methyl - 2h-tetrazol-5-yl) - amino] - 2 - ethyl - 4 - trifluoromet Il - 3,4-dihydro - 2H - quinoline - 1 - carbonyl) - cyclohexyl) - acetamide, among others.It also relates to a Pharmaceutical composition or kit can also understand another Agent as an inhibitor of HMG CoA reductase or a Modulator of PPAR.These compounds are inhibitors of the colesterilico ester transfer protein (CETP), and are useful in the treatment of diseases exacerbated by low levels of HDL cholesterol and / or high levels of LDL and TG, such as atherosclerosis or Cardiovascular Diseases
机译:指式(i)的4-氨基-2-2-1、2、3、4-四羟基喹啉的化合物,其中R 1为-,W-O-W和-和或;或其中W是羰基; Z是(C1-C10)或烷基,任选地被取代的氨基氧代卤代,酰胺基,烷氧基(C1-C6),羧基等。 Z为环,例如环己基,任选被酰胺基或羧基烷基(C1-C6)取代,其中R2为烷基(c1-c4)或环烷基(C1-C6); R4是V,-库拉基洛基(c1-c4),等等,其中V是四唑基,恶二唑基,等等,任选地被取代; R 5,R 6,R 7和R 8独立地为h,卤素,烷基,氰基,(c1-c4)或任选被取代的烷氧基具有Logeno.A优选的是:酸乙酯({4- [4-(3,5-双- (三氟甲基)-苄基)-2-甲基-2h-四唑-5-基)-氨基]-2-乙基-2-三氟甲基-3,4-二氢-2H-喹啉-1-羰基)环己基]酸,( 2R,4S)-{{2-(4-[4-(3,5-双-(三氟甲基)-苄基)-2-甲基-2h-四唑-5-基)-氨基]-2-乙基-4 -三氟乙二胺-3,4-二氢-2H-喹啉-1-羰基)-环己基)-乙酰胺等,它还涉及药物组合物或试剂盒,也可以理解为HMG CoA还原酶抑制剂或PPAR的调节剂。这些化合物是可考酯酯转移蛋白(CETP)的抑制剂,可用于治疗低水平的HDL胆固醇和/或高水平的LDL和TG所加剧的疾病,例如动脉粥样硬化或心血管疾病

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