Patent ID: 6617425
Filing Date: 2003-09-09
Classification: A61K,A61P,C07C

Abstract:
A compound of formula I whereineach R is H, â€”R5, â€”OR5, â€”C(O)R5, â€”R5C(O)R6, â€”C(O)OR5, â€”R5C(O)OR6, â€”R5OC(O)R6, â€”R5OC(O)OR6, â€”R5NR6C(O)R7, â€”R5C(O)NR6R7, â€”C(O)NR6R7, â€”R6OC(O)NR6R7, â€”R5NR6C(O)NR7R8, â€”R5NR6C(O)OR7, â€”R5â€”Oâ€”R6, â€”R5â€”NR6R7, â€”R5â€”Sâ€”R6, â€”R5â€”SOmâ€”R6, â€”R5OR6â€”Oâ€”R7, â€”R5NR6R7â€”Oâ€”R8, â€”R5SOmR6â€”Oâ€”R7, â€”C(O)R5â€”Oâ€”R6, â€”C(O)OR5â€”Oâ€”R6, â€”R5C(O)R6â€”Oâ€”R7, â€”R5C(O)OR6â€”Oâ€”R7, â€”R5OC(O)R6â€”Oâ€”R7, â€”R5OC(O)OR6â€”Oâ€”R7, â€”R5NR6C(O)R7â€”Oâ€”R8, â€”C(O)NR5R6â€”Oâ€”R7, â€”R5C(O)NR6R7â€”Oâ€”R8, â€”R5OC(O)NR6R7â€”Oâ€”R8, â€”R5NR6C(O)NR7R8â€”Oâ€”R9, â€”R5NR6C(O)OR7â€”Oâ€”R8, â€”R5OR6â€”Sâ€”R7, â€”R5NR6R7â€”Sâ€”R8, â€”R5SOmR6â€”Sâ€”R7, â€”C(O)R5â€”Sâ€”R6, â€”C(O)OR5â€”Sâ€”R6, â€”R5C(O)R6â€”Sâ€”R7, â€”R5C(O)OR6â€”Sâ€”R7, â€”R5OC(O)R6â€”Sâ€”R7, â€”R5OC(O)OR6â€”Sâ€”R7, â€”R5NR6C(O)R7â€”Sâ€”R8, â€”C(O)NR5R6â€”Sâ€”R7, â€”R5C(O)NR6R7â€”Sâ€”R8, â€”R5OC(O)NR6R7â€”Sâ€”R8, â€”R5NR6C(O)NR7R8â€”Sâ€”R9, â€”R5NR6C(O)OR7â€”Sâ€”R8, â€”R5OR6â€”NR7R8, â€”R5NR6R7â€”NR8R9, â€”R5SOmR6â€”NR7R8, â€”C(O)R5â€”NR6R8, â€”C(O)OR5â€”NR6R8, â€”R5C(O)R6â€”NR7R8, â€”R5C(O)OR6â€”NR7R8, â€”R5OC(O)R6â€”NR7R8, â€”R5OC(O)OR6â€”NR7R8, â€”R5NR6C(O)R7â€”NR8R9, â€”C(O)NR5R6â€”NR7R8, â€”R5C(O)NR6R7â€”NR8R9, â€”R5OC(O)NR6R7â€”NR8R9, â€”R5NR6C(O)NR7R8â€”NHR9, or â€”R5NR6C(O)OR7â€”NR8R9â€², where R5, R6, R7, R8 and R9 are each independently C1-10alkyl, C1-10alkenyl, C1-10alkynyl, C6-10aryl, C6-14aralkyl, C6-14aralkenyl or C6-14aralkynyl and m is 1,2,3 or 4; and where R5, R6, R7, R8 and R9 are each unsubstituted or substituted with up to 6 substituents selected from halo, NO2, â€”OH, C1-4alkyl, â€”SH, â€”SO3, â€”NH2, C1-4acyl, C1-4acyloxy, C1-4alkylamino, C1-4dialkylamino, trihalomethyl, â€”CN, C1-4alkylthio, C1-4alkylsulfinyl, or C1-4alkylsulfonyl, provided that all the R substituents are not identical, or R forms a cyclic structure, with itself, with R3 or with the carbonyl group attached to the immediately adjacent nitrogen atom; X is hydrogen or an O-protecting group or as defined above for R, with the exception that X is not OR5; R1 and R2, which may be the same or different, are H, an N-protecting group or as defined above for R, or R1 and R2 are linked together in a 3 to 7 membered heterocyclic ring structure, or either R1 or R2 together with OX signify an amide bond to form a cyclic structure of formula wherein Y is H, an amino protecting group or is as defined above for R, Z is â€”NHâ€”CH(R)â€”CH(R3)â€”COâ€” and m is 1, 2, 3, 4, 5, 6, 7, 8 or 9; each R3, which may be the same or different, is as defined above for R, or R3 forms a cyclic structure with the amino group which is alpha to the carbon bearing R3, provided that R and R3 are not both H; and n is 3, 4, 5, 6, 7, 8, 9, or 10.