主权项 |
1. A thieno[3,2-d]pyrimidin-4-one compound of structural formula I, an enantiomer, a diastereoisomer, a racemate and mixtures thereof, and a pharmaceutically acceptable salt thereof, wherein, n is an integer from 1 to 3; R1 and R2 are identical or different, and not hydrogen simultaneously, and each of R1 and R2 is independently H, a halogen, CBr2H, CCl2H, CF2H, a cyano, CF3, an aldehyde group, (CH2)mOR6, (CH2)mNR6R7,(CH2)mCOOR8, CONR9R10, orwherein,
R1 and R2 can be linked together to form C3-C6 alkylidene, but not necessarily; m is an integer from 0 to 3; R6 and R7 are identical or different, and each of R6 and R7 is independently selected from H, a linear or branched saturated or unsaturated C1-C6 hydrocarbyl, a C3-C7 cyclic hydrocarbyl, a C1-C3 alkoxy, a 4-7 member heterocyclic group, a C1-C4 alkyloyl RCO, a C5-C7 aroyl ArCO, a C1-C4 alkylsulfonyl RSO2, a C5-C7 arylsulfonyl ArSO2, a C5-C7 aroylmethylene, a 5-7 member heteroaroylmethylene, a benzyl, a pyridinedimethylene, a C5-C7 aryl Ar or a 5-7 member heteroaryl; wherein, the linear or branched saturated or unsaturated C1-C6 hydrocarbyl is substituted by one or more substituents selected from a methylsulfonyl, a cyclopropyl, a hydroxy, a C1-C3 alkoxy, a C1-C3 alkoxycarbonyl, and an epoxypropyl, but not necessarily; the heterocyclic group contains 1-3 heteroatoms selected from O, S and N, the methylene of the heterocyclic group is substituted by carbonyl or sulfonyl, but not necessarily, or the heterocyclic group is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a C1-C4 alkoxy carbonyl, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar, but not necessarily; the aryl or the benzyl is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar, but not necessarily; the heteroaryl contains 1-3 heteroatoms selected from O, S and N, is combined with a phenyl or a C5-C7 heteroaryl, but not necessarily, or is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar; R8 is selected from H, a linear or branched saturated or unsaturated C1-C6 hydrocarbyl, a C3-C7 cyclic hydrocarbyl; R9 and R10 are identical or different, and each is independently selected form H,a linear or branched saturated or unsaturated C1-C6 hydrocarbyl, a C3-C7 cyclic hydrocarbyl, a C4-C7 heterocyclic group, a C5-C7 aroylmethylene, a 5-7 member heteroaroylmethylene, a benzyl, a pyridinedimethylene, a C5-C7 aryl Ar or a 5-7 member heteroaryl; wherein the linear or branched saturated or unsaturated C1-C6 hydrocarbyl is substituted by one or more substituents selected from a methylsulfonyl, a cyclopropyl, a hydroxy, a C1-C3 alkoxy, a C1-C3 alkoxycarbonyl, and an epoxypropyl, but not necessarily; the heterocyclic group contains 1-3 heteroatoms selected from O, S and N, the methylene of the heterocyclic group is substituted by carbonyl or sulfonyl, but not necessarily, or the heterocyclic group is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar, but not necessarily; the aryl or the benzyl is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar, but not necessarily; the heteroaryl contains 1-3 heteroatoms selected from O, S and N, is combined with a phenyl or a C5-C7 heteroaryl, but not necessarily, or is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar;
P is an integer from 0 to 2; R11, R12 and R13 are identical or different, each of which is independently selected form H, a linear or branched saturated or unsaturated C1-C6 hydrocarbyl, a C3-C7 cyclic hydrocarbyl, a phenyl or a benzyl; wherein the phenyl or the benzyl is substituted by one or more substituents selected from a halogen, a linear or branched C1-C3 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, and a C1-C4 alkoxy, but not necessarily;is a 3-7 member nitrogen-containing heterocyclic group, the heterocyclic group further contains 1-3 heteroatoms selected from O, S and N, and the methylene of the heterocyclic group is substituted by carbonyl or sulfonyl, but not necessarily, and the heterocyclic group is substituted by 1-5 substituents selected from H, a linear or branched C1-C6 hydrocarbyl, a halogen, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, an acylamino, a carboxylate group, C1-C4 alkoxy carbonyl, a mercapto, a C1-C4 alkoxy and hydroxamino, but not necessarily;
R3 is selected from NR14R15 orwherein R14 and R15 are identical or different, and each of R14 and R15 is independently H, a linear or branched saturated or unsaturated C1-C6 hydrocarbyl and hydrocarboxyl, a C3-C7 cyclic hydrocarbyl, a C1-C6 hydrocarbyl amino, a C1-C6 hydrocarbyl amino hydroxy, a C1-C6 hydrocarbyl amidino, a C1-C6 hydrocarbyl guanidyl, a benzyl, a C5-C7 aryl Ar or a 5-7 member heteroaryl, and the heteroaryl contains 1-3 heteroatoms selected from O, S and N, is combined with a phenyl or a C5-C7 heteroaryl, but not necessarily, or is substituted by one or more substituents selected from a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl and a C5-C7 aryl Ar;is a 3-7 member nitrogen-containing heterocyclic group, and the heterocyclic group further contains 1-4 heteroatoms selected from O, S and N, and is substituted by 1-5 substituents selected from H, a linear or branched C1-C6 hydrocarbyl, a halogen, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, an acylamino, a carboxylate group, a C1-C4 alkoxy carbonyl, a mercapto, an amidino, a guanidyl and hydroxamino;
R4, and R5 are identical or different, and each of R4 and R5 is independently H, a halogen, a linear or branched C1-C6 hydrocarbyl, a cyano, a nitro, an amino, a hydroxy, a hydroxymethyl, a trifluoromethyl, a trifluoromethoxy, a carboxyl, a C1-C4 alkoxy, a mercapto, a C1-C4 acyl, a C1-C4 sulfonyl, a C1-C4 sulfonyl amino, an aminoacyl or a C1-C4 linear or branched alkyl substituted sulfonyl; the halogen is a fluoro, a chloro, a bromo or an iodo. |