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PHOENOXYUACIC ACIDS AS ACTIVATORS OF DELIVERY PPAR RECEPTORS

机译:氧磷酸作为递送PPAR受体的活化剂

摘要

1. The compound of formula I! ! or a pharmaceutically acceptable salt thereof,! where X is selected from O, S, OCH2, and SCH2; ! X1 represents O or S; ! R1 is selected from H, C1-8 alkyl, C2-8 alkenyl, aryl, heteroaryl, C3-10 cycloalkyl and heterocyclyl, where each R1 group is substituted with 0-4 R1a; ! R1a in each case is selected from S, substituted 0-1 R1b, O, substituted 0-1 R1b, halogen, NH2, substituted 0-2 R1b, —CN, NO2, C1-6 alkyl, substituted 0-3 R1b, C2-6 alkenyl substituted 0-2 R1b, C2-6 alkynyl, substituted 0-2 R1b, aryl substituted 0-2 R1b, heteroaryl substituted 0-2 R1b, C3-10 cycloalkyl substituted 0-2 R1b, and heterocycle substituted 0-2 R1b; ! R1b in each case is selected from S, substituted 0-1 R1c, O, substituted 0-1 R1c, halogen, methanesulfonyl, NH2, substituted 0-2 R1c, —CN, NO2, C1-6 alkyl, substituted 0-3 R1c, C2 -6 alkenyl substituted with 0-2 R1c, aryl substituted with 0-2 R1c, heteroaryl substituted with 0-2 R1c, C3-10 cycloalkyl substituted with 0-2 R1c, and heterocycle substituted with 0-2 R1c; ! R1c in each case is selected from S, substituted 0-1 R1d, O, substituted 0-1 R1d, halogen, NH2, substituted 0-2 Rd, —CN, NO2, C1-6 alkyl, substituted 0-2 Rd, C2-6 alkenyl substituted 0-2 R1d aryl; substituted 0-2 R1d; heteroaryl; substituted 0-2 R1d; C3-10 cycloalkyl; substituted 0-2 R1d; and a heterocycle substituted 0-2 R1d; ! R1d in each case is selected from OH, SH, S, O, halogen, NH2, —CN, NO2, C1-6 alkyl, C2-6 alkenyl, aryl, CF3 and OCF3; ! R2 is selected from -C≡C-R2a, -CH = CH-R2a, aryl substituted with 0-3 R2a, and heteroaryl substituted with 0-3 R2a; ! R2a in each case is selected from S, substituted 0-1 R2b, O, substituted 0-1 R2b, halogen, NH2, substituted 0-2 R2b, —CN, NO2, C1-6 alkyl, substituted 0-2 R2b, C2-6 alkenyl substituted 0-2 R2b; aryl substituted 0-2 R2b; heteroaryl substituted 0-2 R2b; C3-10 cycloalkyl substituted 0-2 R2b; and heterocycle substituted 0-2; ! R2b in each case is selected from S substituted by 0-1 R2c,
机译:1.式Ⅰ化合物! !或其药学上可接受的盐!其中X选自O,S,OCH2和SCH2; ! X1代表O或S; ! R1选自H,C1-8烷基,C2-8烯基,芳基,杂芳基,C3-10环烷基和杂环基,其中每个R1基团被0-4个R1a取代; ! R 1a在每种情况下均选自S,取代的0-1 R1b,O,取代的0-1 R1b,卤素,NH2,取代的0-2 R1b,-CN,NO2,C1-6烷基,取代的0-3 R1b,C2 -6烯基取代的0-2 R1b,C2-6炔基,取代的0-2 R1b,芳基取代的0-2 R1b,杂芳基取代的0-2 R1b,C3-10环烷基取代的0-2 R1b和杂环取代的0-2 R1b; ! R1b在每种情况下选自S,取代的0-1 R1c,O,取代的0-1 R1c,卤素,甲磺酰基,NH2,取代的0-2 R1c,-CN,NO2,C1-6烷基,取代的0-3 R1c ,被0-2 R1c取代的C 2 -6烯基,被0-2 R1c取代的芳基,被0-2 R1c取代的杂芳基,被0-2 R1c取代的C3-10环烷基,以及被0-2 R1c取代的杂环。 !在每种情况下,R1c选自S,取代的0-1 R1d,O,取代的0-1 R1d,卤素,NH2,取代的0-2 Rd,-CN,NO2,C1-6烷基,取代的0-2 Rd,C2 -6个烯基取代的0-2个R1d芳基;取代0-2 R1d;杂芳基取代0-2 R1d; C3-10环烷基;取代0-2 R1d;和杂环取代的0-2 R1d; ! R 1d在每种情况下选自OH,SH,S,O,卤素,NH 2,-CN,NO 2,C 1-6烷基,C 2-6烯基,芳基,CF 3和OCF 3; ! R2选自-C≡C-R2a,-CH = CH-R2a,被0-3个R2a取代的芳基,和被0-3个R2a取代的杂芳基; !在每种情况下,R 2a选自S,取代的0-1 R2b,O,取代的0-1 R2b,卤素,NH 2,取代的0-2 R2b,-CN,NO 2,C 1-6烷基,取代的0-2 R2b,C2 -6烯基取代的0-2 R2b;芳基取代的0-2 R 2b;杂芳基取代的0-2 R 2b; C3-10环烷基取代的0-2 R2b;杂环取代的0-2; !在每种情况下,R2b均选自被0-1个R2c取代的S,

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