| 摘要 |
The present invention belongs to the field of pharmaceutical chemistry, and specifically relates to compounds having an alkynyl heteroaromatic ring structure and pharmaceutically acceptable salts, stereoisomers, N-oxides, solvates, or prodrugs thereof, and pharmaceutical compositions comprising these compounds, as well as uses of these compounds and compositions in the manufacture of a medicament. The compounds of the present invention and the pharmaceutically acceptable salts, stereoisomers, N-oxides, solvates or prodrugs thereof and the pharmaceutical compositions comprising the compounds have better anti-tumor activity. |
| 主权项 |
1. A compound of general formula I,or a pharmaceutically acceptable salt, stereoisomer, N-oxide, solvate or prodrug thereof,wherein
L is selected from —C(O)NH—, —NHC(O)NH— and —NHC(O)—; Z is selected from (CH2)n and O, wherein n is selected from 0, 1, 2, 3 and 4; A is selected from substituted and unsubstituted 5-, 6- and 7-membered nitrogen-containing heterocyclic groups; R1 is selected from H, alkyl, alkoxy, halo-substituted alkyl, halo-substituted alkoxy, —OH, —NH2, halogen and —CN; R2 is selected from H, alkyl, alkoxy, halo-substituted alkyl, halo-substituted alkoxy, —OH, —NH2, halogen and —CN; and B is selected from groups represented by the formula wherein B′ is a 5- to 7-membered saturated or unsaturated heteroaromatic ring containing 1 to 3 nitrogen atoms;
R3 is selected from H, alkyl, alkoxy, halo-substituted alkyl, halo-substituted alkoxy, —OH, —NH2, halogen and —CN;R5 is selected from H, —NR6R7, —NHCOR8, —SO2R8, alkyl, alkoxy, halo-substituted alkyl, halo-substituted alkoxy, —OH, halogen, oxo, —CN, hydrazino and alkyl substituted hydrazino, wherein R6 and R7 are independently selected from H, alkyl, 4-methylsulphonylanilino and 4-aminosulphonylanilino, and R8 is selected from H and alkyl;p is selected from 1, 2 and 3; andq is selected from 1 and 2. |
