Patent ID: 6710034
Filing Date: 2004-03-23
Classification: A61P,C07H

Abstract:
A compound represented by the Formula: whereinA is selected from the group consisting of: (1) â€”CHO or a protected aldehyde; (2) â€”CN; (3) â€”CH&boxH;Nâ€”NR5R6, wherein R5 and R6 are each independently selected from the group consisting of: a. hydrogen, b. C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, c. C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, d. C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocylic and substituted heterocyclic, and e. R5 and R6 taken together with the nitrogen atom to which they are connected form a 3- to 7-membered ring which may optionally contain one or more heterofunctions selected from the group consisting of: â€”Oâ€”, â€”NHâ€”, â€”N(C1-C6-alkyl)â€”, â€”N(aryl)â€”, â€”N(heteroaryl)â€”, â€”Sâ€”, â€”S(O)â€” and â€”S(O)2â€”; (4) â€”CH&boxH;Nâ€”OR5, wherein R5 is as previously defined; (5) â€”CH3X, wherein X is selected from the group consisting of: (a) hydroxy or protected hydroxy; (b) halogen; (c) â€”NR5R6, wherein R5 and R6 are as previously defined; (d) â€”NR5C(O)â€”R7, where R5 is as previously defined and R7 is selected from the group consisting of: i. hydrogen; ii. C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic; iii. C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocylic and substituted heterocyclic; iv. C2-C6-alkynyl, optionally substituted with one or more substitueuts selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic; v. aryl; vi. substituted aryl; vii. heterocyclic; and viii. substituted heterocyclic; (e) â€”NR5C(O)â€”NR6R7, where R5, R6, and R7 are as previously defined; (f) â€”NR5â€”NR6R7, where R5, R6 and R7 are as previously defined; (g) â€”NR5â€”NR6C(O)â€”R7, where R5, R6 and R7 are as previously defined; (h) â€”S(O)nâ€”R8, where R8 is selected from the group consisting of: aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n=0, 1 or 2; (i) â€”S(O)nâ€”(C1-C6-alkyl), optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; (j) â€”S(O)nâ€”(C2-C6-alkenyl), optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; (k) â€”S(O)nâ€”(C2-C6-alkynyl), optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; and (l) â€”Oâ€”Mâ€”Y, where M is: i. absent, ii. â€”C(O)â€”, iii. â€”C(O)N(R5)â€”, where R5 is as previously defined, iv. C1-C6-alkyl-N(R5)â€”, where R5 is as previously defined, v. C2-C6-alkenyl-N(R5)â€”, where R5 is as previously defined, or vi. C2-C6-alkynyl-N(R5)â€”, where R5 is as previously defined, and Y is: i. hydrogen, ii. C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, â€”OR5, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where R5 is as previously defined, iii. C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, â€”OR5, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where R5 is as previously defined. iv. C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of halogen, â€”OR5, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where R5 is as previously defined, v. aryl, vi. substituted aryl, vii. heterocylic, or viii. substituted heterocyclic; and (6) heterocyclic or substituted heterocyclic; B is selected from the group consisting of: (1) â€”CHO or a protected aldehyde; (2) â€”CN; (3) â€”CH&boxH;Nâ€”NR5R6, wherein R5 and R6 are as previously defined; (4) â€”CH&boxH;Nâ€”OR5, wherein R5 is as previously defined; (5) â€”CH2Z, wherein Z is selected from the group consisting of: a. halogen; b. â€”NR5C(O)â€”R7, where R5 and R7 are as previously defined; c. â€”NR5C(O)â€”NR6R7, where R5, R6, and R7 are as previously defined; d. â€”NR5â€”NR6R7, where R5, R6 and R7 are as previously defined; e. â€”NR5â€”NR6C(O)â€”R7, where R5, R6 and R7 are as previously defined; f. â€”S(O)nâ€”R8, where R8 and n are as previously defined; g. â€”S(O)nâ€”(C1-C6-alkyl), optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; h. â€”S(O)nâ€”(C2-C6-alkenyl), optionally substituted with one or more substituents selected from the group consisting of; halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; i. â€”S(O)nâ€”(C2-C6-alkynyl), optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined; and j. â€”NR9R10, where R9 and R10 are each independently selected from the group consisting of: (i) hydrogen; (ii) C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, â€”Oâ€”R5 and â€”NR5R6, where R5 and R6 are as previously defined; (iii) C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, â€”Oâ€”R5 and â€”NR5R6, where R5 and R6 are as previously defined; (iv) C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, Oâ€”R5 and NR5R6, where R5 and R6 are as previously defined; and (v) â€”Wâ€”R11, where W is selected from the group consisting of: 1. â€”C(O)â€”; 2. â€”C(O)Oâ€”; 3. â€”C(S)â€”; 4. â€”C(S)â€”Sâ€”; 5. â€”C(S)â€”Oâ€”; 6. â€”C(S)â€”NR5, where R5 is as previously defined; 7. â€”C(O)NR5, where R5 is as previously defined; 8. â€”C(&boxH;NR5)â€”Oâ€”, where R5 is as previously defined; and 9. â€”C(&boxH;NR11)â€”NR5R6, where R5 and R6 are as previously defined, and where R11 is selected from the group consisting of: (a) hydrogen; (b) C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic; (c) C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic; (d) C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic; (vi) R9 and R10 taken together with the nitrogen atom they are attached to represent the carbon or hetero atoms necessary to form a heterocyclic or substituted heterocyclic moiety; and (vii) R9 and R10 taken together with the nitrogen atom they are attached to form a 4 to 8 membered ring which contains one or more W moieties, and optionally may contain one or more heteromoieties selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”S(O)2â€” and â€”NR5â€”, where W and R5 are as previously defined; provided that when R3 and R4 are hydrogen, Z cannot be â€”NR9R10;R1 and R2 are each independently selected from the group consisting of: (1) hydrogen; (2) hydroxy; (3) protected hydroxy; (4) â€”OC(O)â€”C1-C13-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, Oâ€”R5 and NR5R6 where R5 and R6 are as previously defined; (5) â€”Oâ€”R5, where R5 is as previously defined; (6) halogen; (7) â€”NR5R6, where R5 and R6 are as previously defined; and (8) R1 and R2 taken together are oxo; R3 is selected from the group consisting of: (1) hydrogen; (2) a hydroxy protecting group; (3) â€”C(O)â€”C1-C12-alkyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, â€”OR5 and â€”NR5R6, where R5 and R6 are as previously defined; (4) C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, â€”OR5 and â€”NR5R6, where R5 and R6 are as previously defined; (5) C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, â€”OR5 and â€”NR5R6, where R5 and R6 are as previously defined; and (6) C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of: halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, â€”OR5 and â€”NR5R6, where R5 and R6 are as previously defined; R4 is â€”Mâ€”Y, where M and Y are as previously defined; provided that when M is absent Y can not be mycarosyl or substituted mycarosyl; and Rp is hydrogen or a hydroxy protecting group.