ANALOGUES OF AZACYTIDINE AND THEIR APPLICATION

摘要

1. The compound of formula (I) !! where R represents H, R5C (O), R5CH2OC (O) or R5CH2NHC (O); ! R1 represents! ! where the crossed dashed line shows the bond formed by the addition of R1 to the molecule of formula (I); ! R2 and R3 independently represent OH or H, provided that R2 and R3 are not simultaneously OH; ! R4 is H, R5C (O), R5CH2OC (O) or R5CH2NHC (O), provided that R and R4 are not both H; ! R5 has a general formula! CH3- (CH2) n- (CH = CH-CH2) m-CH = CH- (CH2) k-,! k represents an integer from 0 to 7; ! m is an integer from 0 to 2; and! n is an integer from 0 to 10,! or a pharmaceutically acceptable salt thereof. ! 2. The compound according to claim 1, where k is 4.! 3. The compound according to claim 2, where n is 10.! 4. The compound according to claim 1, where R1 represents! ! 5. The compound according to claim 4, where R4 represents N.! 6. The compound according to claim 1, where R represents R5C (O); R1 represents! ! R2 is H; R3 is OH; R4 represents H; k is 4; m is 0; and n is 10.! 7. A pharmaceutical composition comprising:! connection according to claim 1 and! pharmaceutical excipient, diluent and / or carrier. ! 8. A method of treatment in a subject of a neoplasm, comprising:! the choice of a subject with a neoplasm and! introduction to the subject of a compound of the formula! ! where R represents H, R5C (O), R5CH2OC (O) or R5CH2NHC (O); ! R1 represents! ! where the crossed dashed line shows the bond formed by the addition of R1 to the molecule of formula (I); ! R2 and R3 independently represent OH or H, provided that R2 and R3 are not simultaneously OH; ! R4 is H, R5C (O), R5CH2OC (O) or R5CH2NHC (O), provided that R and R4 are not both H; ! R5 has a general formula! CH3- (CH2) n- (CH = CH-CH2) m-CH = CH- (CH2) k-,!