| 摘要 |
FIELD: medicine, pharmaceutics. ^ SUBSTANCE: present invention refers to compounds of formula VIII suitable in medicine as T3 mimetic drugs: VIII, where G is O, -S(=O)2- or -CH2-; R2 is halogen, alkyl, -CF3, -OCF3, alkoxy or cyano; R3 and R4 are H, halogen, alkyl or -(CRaÇè2)maryl; T is selected from -(CRaÇè2)k-, -CRb=CRb-(CRaÇè2)n-, -(CRaÇè2)n-CRb=CRb, -(CRaÇè2)-CRb=CRb-(CRaÇè2)-, O(CRaÇè2)(CRaÇè2)n-, -S(CRaÇè2)(CRaÇè2)n-, -N(Rc)(CRbÇè2)(CRaÇè2)n-, -N(Rb)C(O)(CRaÇè2)n-, -(CRaÇè2)nCH(NRbRc) -C(O)(CRaÇè2)m-, -(CRaÇè2)mC(O)-, -(CRaÇè2)C(O)(CRaÇè2)n-, -(CRaÇè2)n C(O)(CRaÇè2)- and -C(O)NH(CRbÇè2)(CRaÇè2)p-; Ra, Rb, Rc, R1, R6, R7, R8 and R9 are H, halogen or alkyl; or R6 and T with C atom form a 5-6-members ring with 0-2 groups -NRi-, -O- or -S-; Ri is H, -C(O)alkyl, alkyl or aryl; R5 is OH, alkoxy, -OC(O)Re, -OC(O)ORh, -F, -NHC(O)Re, -NHS(=O)Re, -NHS(=O)2Re, -NHC(S)NH(Rh) or -NHC(O)NH(Rh); Re is alkyl, -(CRa2)n-aryl, -(CRaÇè2)n-cycloalkyl or -(CRaÇè2)n- heterocycloalkyl; Rh is H or alkyl; X is P(O)YRllY'Rll; Y and Y' are O or -NRv-; R11 is H, alkyl, -C(Rz)2-OC(O)Ry, -C(RZ)2-O-C(O)ORy, -alkyl-S-C(O)Ry, -[C(Rz)2]q-COORy, -cycloalkylene-COORy, aryl, -C(Rz)2OC(O)SRy, -C(Rx)2COORy or two R11 and R11 form a cycle; k is within 1 to 4; m is within 0 to 3; n is within 0 to 2; p is within 0 to 1; q is 2 or 3; Rv, Rz, Ry and Rx are H or alkyl, or two Rx and Rx form a cycle. ^ EFFECT: production of new thymomimetic drugs. ^ 19 cl, 80 ex, 10 tbl, 13 dwg |
