首页> 外国专利> AMIDA DERIVATIVES OF ACID N- (PHENYL-OXAZOL-4-ILMETOXIMETIL) -CICLOHEXIL-SUCCINICO AND RELATED COMPOUNDS AS PPAR LIGANDS (ACTIVATED RECEPTORS FOR PEROXISOM PROLIFERATORS) FOR THE TREATMENT OF HYPERLIPETEM.

AMIDA DERIVATIVES OF ACID N- (PHENYL-OXAZOL-4-ILMETOXIMETIL) -CICLOHEXIL-SUCCINICO AND RELATED COMPOUNDS AS PPAR LIGANDS (ACTIVATED RECEPTORS FOR PEROXISOM PROLIFERATORS) FOR THE TREATMENT OF HYPERLIPETEM.

机译:酸性N-(PHENYL-OXAZOL-4-ILMETOXIMETIL)-CICLOHEXIL-SUCCINICO及其相关化合物作为PPAR配体(过氧化物酶体增殖剂的活化受体)用于高脂血症的治疗。

摘要

Compounds of formula I ** see formula ** in which they mean: ring A cycloalkanediyl- (C3-C8), cycloalkenodiyl- (C3-C8), in which in the rings of cycloalkanediyl or cycloalkenodiyl one or more carbon atoms they can be substituted by oxygen atoms; R1 and R2, independently of each other, H, F, Cl, Br, CF3, OCF3, alkyl- (C1-C6), O-alkyl- (C1-C6), SCF3, SF5, OCF2-CHF2, aryl- ( C6-C10), aryloxy- (C6-C10), OH, NO2; or R1 and R2, together with the phenyl, pyridine, 1-H-pyrrole, thiophene or furan, aryl- (C6-C10), heteroaryl- (C5-C11) bicyclic ring partially saturated or unsaturated; R3 H, alkyl- (C1-C6), cycloalkyl- (C3-C8), alkyl- (C1-C3) -cycloalkyl- (C3-C8), phenyl, alkyl- (C1-C3) -phenyl, heteroaryl- ( C5-C6), alkyl- (C1-C3) -heteroaryl- (C5-C6) or alkyl- (C1-C3) which is totally or partially substituted by F; W CH, N, if o = 1; W O, S, NR9, if o = 0; X-alkanediyl- (C1-C6), in which in the alkanediyl group one or more carbon atoms may be replaced by oxygen atoms; And CO, SO, SO2; n 0-2; R4 H, F, alkyl- (C1-C6); R5 H, F, alkyl- (C1-C6); R6 H, F, alkyl- (C1-C6); R5 and R6, together with the C atoms that carry them, cycloalkane- (C3-C8) -1,2-diyl; R7 H, alkyl- (C1-C6), alkenyl- (C2-C6), alkynyl- (C2-C6), O-alkyl- (C1-C6), O-alkenyl- (C2-C6), Oalkynyl- ( C2-C6), cycloalkyl- (C3-C8), aryl- (C6-C10), heteroaryl- (C5-C11), O-cycloalkyl- (C3-C8), O-phenyl, NR10R11 which may be substituted by O -alkyl- (C1-C6), O-alkenyl- (C2-C6), O-alkynyl- (C2-C6), O-cycloalkyl- (C3-C8), O-phenyl, O-heteroaryl- (C5- C11), and in which cycloalkyl- (C3-C8), phenyl and heteroaryl- (C5-C11) may also be substituted by alkyl- (C1-C6), optionally unsubstituted or totally or partially substituted by F, O- alkyl- (C1-C6), optionally unsubstituted or totally or partially substituted by F, Cl, Br, I, OH, NR10R11, CO-alkyl- (C1-C6), CO-aryl- (C6-C10), COheteroaryl - (C5-C11), C (O) -O-alkyl- (C1-C6), C (O) -O-aryl- (C6-C10), C (O) -O-heteroaryl- (C5-C11 ), SO2-alkyl- (C1-C6), SO2-aryl- (C6-C10), SO2-heteroaryl- (C5-C11), and the alkyl, aryl and heteroaryl can also be substituted by alkyl- (C1-C6) or phenyl; R6 and R7, along with the atom of C that carry them. cycloalkane- (C3-C8) -1,1-diyl; R8 H, alkyl- (C1-C6); R9 H, alkyl- (C1-C6) which is unsubstituted or substituted by phenyl and phenyl; R10 H, alkyl- (C1-C6), phenyl, CO-alkyl- (C1-C6), CO-aryl- (C6-C10), CO-alkyl- (C1-C6) -aryl- (C6-C10) , CO-heteroaryl- (C5-C11), C (O) -O-alkyl- (C1-C6), C (O) -O-alkyl- (C1-C6) -aryl- (C6-C10), C (O) -O-aryl- (C6-C10), C (O) -O-heteroaryl- (C5-C11), SO2-alkyl- (C1-C6), SO2-alkyl- (C1-C6) -aryl - (C6-C10), SO2-alkyl- (C1-C6) -SO2-alkyl- (C1-C6), SO2-aryl- (C6-C10), SO2-heteroaryl- (C5-C11), and may also be alkyl, aryl and heteroaryl substituted by (C 1 -C 6) alkyl or phenyl. R11 H, alkyl- (C1-C6) which is eventually substituted by phenyl, phenyl; R12 H, benzyl; as well as its physiologically acceptable salts and solvates.
机译:式I **的化合物参见式**,其中它们的含义是:环A环烷二基-(C3-C8),环烯二基-(C3-C8),其中在环烷二基或环烯二基的环中一个或多个碳原子可以是被氧原子取代; R1和R2彼此独立地为H,F,Cl,Br,CF3,OCF3,烷基-(C1-C6),O-烷基-(C1-C6),SCF3,SF5,OCF2-CHF2,芳基-( C6-C10),芳氧基-(C6-C10),OH,NO2; R1和R2与苯基,吡啶,1-H-吡咯,噻吩或呋喃,芳基-(C6-C10),杂芳基-(C5-C11)双环部分饱和或不饱和; R 3 H,烷基-(C 1 -C 6),环烷基-(C 3 -C 8),烷基-(C 1 -C 3)-环烷基-(C 3 -C 8),苯基,烷基-(C 1 -C 3)-苯基,杂芳基-( C 5 -C 6),全部或部分被F取代的烷基-(C 1 -C 3)-杂芳基-(C 5 -C 6)或烷基-(C 1 -C 3)。 W CH,N,如果o = 1;如果o = 0,则W O,S,NR9; X-烷二基-(C1-C6),其中在烷二基中一个或多个碳原子可以被氧原子取代;还有CO,SO,SO2; n 0-2; R4H,F,烷基-(C1-C6); R 5 H,F,烷基-(C 1 -C 6); R6 H,F,烷基-(C1-C6); R5和R6,连同携带它们的C原子,是环烷烃-(C3-C8)-1,2-二烷基; R 7 H,烷基-(C 1 -C 6),烯基-(C 2 -C 6),炔基-(C 2 -C 6),O-烷基-(C 1 -C 6),O-烯基-(C 2 -C 6),O炔基-( C2-C6),环烷基-(C3-C8),芳基-(C6-C10),杂芳基-(C5-C11),O-环烷基-(C3-C8),O-苯基,可被O取代的NR10R11 -烷基-(C1-C6),O-烯基-(C2-C6),O-炔基-(C2-C6),O-环烷基-(C3-C8),O-苯基,O-杂芳基-(C5- C11),其中环烷基-(C3-C8),苯基和杂芳基-(C5-C11)也可以被烷基-(C1-C6)取代,可选地未被取代或全部或部分被F,O-烷基-取代。 (C1-C6),任选未被取代或完全或部分被F,Cl,Br,I,OH,NR10R11,CO-烷基-(C1-C6),CO-芳基-(C6-C10),CO杂芳基-(C5 -C11),C(O)-O-烷基-(C1-C6),C(O)-O-芳基-(C6-C10),C(O)-O-杂芳基-(C5-C11),SO2 -烷基-(C1-C6),SO2-芳基-(C6-C10),SO2-杂芳基-(C5-C11),并且烷基,芳基和杂芳基也可以被烷基-(C1-C6)或苯基取代; R6和R7,以及携带它们的C原子。环烷-(C3-C8)-1,1-二基; R8H,烷基-(C1-C6); R9H,烷基-未被取代或被苯基和苯基取代的烷基-(C1-C6); R10H,烷基-(C1-C6),苯基,CO-烷基-(C1-C6),CO-芳基-(C6-C10),CO-烷基-(C1-C6)-芳基-(C6-C10) ,CO-杂芳基-(C5-C11),C(O)-O-烷基-(C1-C6),C(O)-O-烷基-(C1-C6)-芳基-(C6-C10),C (O)-O-芳基-(C6-C10),C(O)-O-杂芳基-(C5-C11),SO2-烷基-(C1-C6),SO2-烷基-(C1-C6)-芳基-(C6-C10),SO2-烷基-(C1-C6)-SO2-烷基-(C1-C6),SO2-芳基-(C6-C10),SO2-杂芳基-(C5-C11),并且也可以是被(C 1 -C 6)烷基或苯基取代的烷基,芳基和杂芳基。 R 11 H,烷基-(C 1 -C 6),其最终被苯基取代; R 12 H,苄基;以及其生理上可接受的盐和溶剂化物。

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