首页> 外国专利> IDENTIFICATION OF HUMAN T2R RECEPTORS, BINDING WITH Bitter COMPOUNDS, GIVING A HOT TASTE TO COMPOSITIONS, AND THEIR APPLICATION IN ANALYSIS FOR DETERMINING COMPOUNDS, INHIBITION INHIBIBILITY

IDENTIFICATION OF HUMAN T2R RECEPTORS, BINDING WITH Bitter COMPOUNDS, GIVING A HOT TASTE TO COMPOSITIONS, AND THEIR APPLICATION IN ANALYSIS FOR DETERMINING COMPOUNDS, INHIBITION INHIBIBILITY

机译:人T2R受体的识别,与苦味化合物的结合,赋予成分以热味,并将其用于分析化合物,抑制抑制性

摘要

1. The compound of structural Formula (I) indicated below! ! or its salt, hydrate, solvate or N-oxide, where! Ar1 represents a five- or six-membered aryl, heteroaryl or cycloalkyl ring; ! m is 0, 1, 2 or 3; ! R1 is SO2; C is O; C = S; or C = NOR4; ! X is selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, acyl, substituted acyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, substituted heteroaryl, NO, heteroaryl , OR6, S (O) bR6, NR6R7, CONR6R7, CO2R6, NR6CO2R7, NR6CONR7R8, NR6CSNR7R8, NR6C (= NH) NR7R8, SO2NR5R6, NR5SO2R6, NR5SO2NR6R7) OR (P5) OR6) and P (O) (R5) (OR6); ! each R1 ′ is independently selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, acyl, substituted acyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, CN, NO2, OR6, S (O) bR6, NR6R7, CONR6R7, CO2R6, NR6CO2R7, NR6CONR7R8, NR6CSNR7R8, NR6C (= NH) NR7R8, SO2NR5R6, NR5SO2R6, NR5SO6 (OR) OR OR5) (OR6) and P (O) (R5) (OR6); ! or, alternatively, X and / or at least one R1 ′ together with the atoms to which they are attached form an aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl or substituted cycloheteroalkyl ring, where this ring is, optionally fused to another aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl or substituted cycloheteroalkyl ring; ! R
机译:1.下述结构式(I)的化合物! !或其盐,水合物,溶剂化物或N-氧化物! Ar 1代表五元或六元芳基,杂芳基或环烷基环; ! m为0、1、2或3; ! R1是SO2; C是O; C = S;或C = NOR4; ! X选自氢,卤素,烷基,取代的烷基,芳基,取代的芳基,芳基烷基,取代的芳基烷基,酰基,取代的酰基,杂烷基,取代的杂烷基,杂芳基,取代的杂芳基,杂芳基烷基,取代的杂芳基烷基,取代的杂芳基, NO,杂芳基,OR6,S(O)bR6,NR6R7,CONR6R7,CO2R6,NR6CO2R7,NR6CONR7R8,NR6CSNR7R8,NR6C(= NH)NR7R8,SO2NR5R6,NR5SO2R6,NR5SO2R6(5)(5) )(OR6); !每个R 1'独立地选自氢,卤素,烷基,取代的烷基,芳基,取代的芳基,芳基烷基,取代的芳基烷基,酰基,取代的酰基,杂烷基,取代的杂烷基,杂芳基,取代的杂芳基,杂芳基烷基,CN,NO 2 ,OR6,S(O)bR6,NR6R7,CONR6R7,CO2R6,NR6CO2R7,NR6CONR7R8,NR6CSNR7R8,NR6C(= NH)NR7R8,SO2NR5R6,NR5SO2R6,NR5SO6(OR)和(或)OR5 P (OR6); !或者,X和/或至少一个R 1'与它们所连接的原子一起形成芳基,取代的芳基,杂芳基,取代的杂芳基,环烷基,取代的环烷基,环杂烷基或取代的环杂烷基环,其中该环为,任选地稠合至另一个芳基,取代的芳基,杂芳基,取代的杂芳基,环烷基,取代的环烷基,环杂烷基或取代的环杂烷基环; ! [R

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