| 主权项 |
1. A compound of the formula (I): wherein: R1 is H, a halogen (F, Cl, Br, I, especially F, Cl, or Br), CN, NO2, an optionally substituted alkyl group, preferably a C1-C6 alkyl group (preferably CH3 and including CF3); R3 is H, OH, a C1-C3 alkyl group which is optionally substituted with up to 3 halogens (preferably F), a halogen (preferably F, Cl or Br), NO2 or CN; Rp is an optionally substituted five- or six-membered heterocycle, including pyrimidine derivatives preferably linked at the 1-position of the pyrimidine, more often a uracil moiety linked at the 1-position which is optionally substituted at the 5- or 6-position (often the 5-position) with a substituent R2a; R2a is H, halogen (preferably F, Cl or Br), optionally substituted C1-C3 alkyl (preferably methyl, ethyl or trifluoromethyl), optionally substituted —O—(C1-C3) alkyl (methyl, ethyl, propyl, isopropyl), including O—CF3, CN; W is N or C; X1 isO or N—RX when W is C, andwhen W is N;
Z is(the double bond can be on either side of the carbon depending on X1 and Y1);
Y1 isO or N—RY when W is C, andwhen W is N;
R2 is H, a C1-C6 alkyl (preferably C1-C3 alkyl, including cyclopropyl) or a C2-C6 alkenyl optionally substituted with up to three fluorines (e.g. CF3), CN or halogen (F, Br, Cl, I), C1-C6alkoxy; C1-C6 hydroxyalkyl, C1-C6 alkoxyalkyl, C1-C6 polyoxyalkyl (e.g., methoxyethoxy) or a vinyl-R2 (substituted on the first or second carbon of the vinyl group, preferably on the second carbon cis or trans, more preferably trans); and RX and RY are each independently H or a C1-C6 alkyl (or a C1-C3 alkyl) group, optionally substituted with one or two hydroxyl groups; m is 0, 1, 2, 3 or 4 and n is 0, 1, 2 or 3; and the pharmaceutically acceptable salts, solvates and polymorphs thereof; with the proviso that the following compounds are excluded: (1) the compound of formula I where Rp is uracil, W is C, X1 is N—RX, RX is H, Y1 iswhere R2 is H, R1 is 4-H, R3 is 6-H, Z iswhere R2 is H and m and n are 1;
(2) the compound of formula I where Rp is uracil, W is N, X1 iswhere R2 is H, Y1 iswhere R2 is H, R1 is 4-H, R3 is 6-H, m and n are 1, Z isand R2 bound to the Z carbon is either CH3 or CN;
(3) the compound of formula I where Rp is uracil, W is C, X1 is O, Y1 isR2 is H, Z ism and n are 1, R1 is 4-Cl, R3 is 6-H and R2 bound to the Z carbon is H or CH3; and
(4) the compound of formula I where Rp is uracil, W is C, X1 iswhere R2 is H, Z iswhere R2 is H, Y1 is O, R1 is 4-Cl, R3 is 6-H and m and n are 1. |
