Patent ID: 6569836
Filing Date: 2003-05-27
Classification: C07H

Abstract:
A compound selected from the group consisting of: or a pharmaceutically acceptable salt thereof, wherein:Rp is hydrogen or a hydroxy protecting group; R1 is selected from the group consisting of: (a) C1-C6 alkyl substituted with one or more substituents selected from the group consisting of: (i) aryl; (ii) substituted aryl; (iii) heteroaryl; (iv) substituted heteroaryl; and (v) Ar1-Ar2, wherein Ar1 and Ar2 are independently selected from the group consisting of aryl, substituted aryl, heteroaryl, and substituted heteroaryl; (b) C1-C6-alkenyl-R2; and (c) C1-C6-alkynyl-R2; R2 is selected from the group consisting of: (a) aryl; (b) substituted aryl; (c) heteroaryl; (d) substituted heteroaryl; and (e) Ar1-Ar2, wherein Ar1 and Ar2 are as defined above; R3 is selected from the group consisting of: (a) hydrogen; (b) OH; (c) F, Cl, Br or I; (d) C1-alkyl substituted with one or more substituents selected from the group consisting of: (i) aryl; (ii) substituted aryl; (iii) heteroaryl; (iv) substituted heteroaryl; (v) â€”NRâ€²Râ€³, wherein Râ€² and Râ€³ are as defined above; and (vi) â€”OR5, wherein R5 is hydrogen or C1-C6 alkyl optionally substituted with one or more substituents selected from the group consisting of: (1) aryl; (2) substituted aryl; (3) heteroaryl; and (4) substituted heteroaryl; (vii) â€”OC(O)R5, wherein R5 is as defined above; (e) C2-C6 alkyl optionally substituted with one or more substituents selected from the group consisting of: (i) aryl; (ii) substituted aryl; (iii) heteroaryl; (iv) substituted heteroaryl; (v) â€”NRâ€²Râ€³, wherein Râ€² and Râ€³ are as defined above; (vi) â€”OR5, wherein R5 is as defined above; and (vii) â€”OC(O)R5, wherein R5 is as defined above; (f) C1-C6-alkenyl; (g) C1-C6-alkenyl-R2, wherein R2 is as defined above; (h) C1-C6-alkynyl; (i) C1-C6-alkynyl-R2, wherein R2 is as defined above; (j) â€”OR5, wherein R5 is as defined above; (k) â€”OC(O)R5, wherein R5 is as defined above; (l) â€”CH2SO2NHR5, wherein R5 as defined above; (m) â€”CH2S(O)xR5, wherein x is 0, 1 or 2, and R5 is as defined above; and (n) â€”CH2NHR5, wherein R5 as defined above; R4 is selected from the group consisting of: (a) hydrogen; (b) OH; (c) NH2; (d) NHR5, wherein R5 is as defined above; (e) PhSe; (f) F, Cl, Br or I; or R3 and R4 taken together with the atoms to which each is attached forms a 3- to 6-membered non-aromatic ring optionally containing a heteroatom, wherein the non-aromatic ring optionally contains one to two double bonds; or R3 and R4 taken together form a &boxH;CH2 (exocyclic methylene), â€”CH2Oâ€” (epoxide) or &boxH;O (oxo);Ra, Rb, Rc and Rd are 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: (i) â€”Lâ€”Mâ€”R6, wherein L is either absent or selected from the group consisting of: (1) â€”C(O)NHâ€”; (2) â€”NHC(O)â€”; (3) â€”NHâ€”; (4) â€”N(CH3)â€”; (5) â€”Oâ€”; (6) â€”S(O)xâ€”, wherein x is as defined above; (7) â€”C(&boxH;NH)NHâ€”; (8) â€”NHC(NH)â€”; (9) â€”C(O)Oâ€”; (10) â€”OC(O)â€”; (11) â€”OC(O)NHâ€”; (12) â€”NHC(O)Oâ€”; and (13) â€”NHC(O)NHâ€”; M is absent or selected from the group consisting of: (1) â€”(CH2)lâ€”, wherein l is 1 to 5; (2) â€”(CH2)mâ€”CH&boxH;CHâ€”, wherein m is 0 to 3; (3) â€”(CH2)nâ€”Câ‰¡Câ€”, wherein n is 0 to 3; R6 is selected from the group consisting of: (1) hydrogen; (2) aryl; (3) substituted aryl; (4) heteroaryl; (5) substituted heteroaryl; and (6) Ar1-Ar2, wherein Ar1 and Ar2 are independently selected from the group consisting of: (a) aryl; (b) substituted aryl; (c) heteroaryl; and (d) substituted heteroaryl; and (ii) halogen; (c) C3-C7 cycloalkyl; (d) heterocycloalkyl; and (e) substituted heterocycloalkyl; or any one pair of substituents selected from the group consisting of RaRb, RaRc, RaRd, RbRc, RbRd, and RcRd taken together with the atom or atoms to which they are attached form a 3- to 7-membered ring optionally containing a hetero function selected from the group consisting of â€”Oâ€”; â€”NHâ€”; â€”N(C1-C6 alkyl-)â€”; â€”N(aryl-C1-C6 alkyl-)â€”; â€”N(substituted aryl-C1-C6 alkyl-)â€”; â€”N(heteroaryl-C1-C6 alkyl-)â€”; â€”N(substituted heteroaryl-C1-C6 alkyl-)â€”; â€”S(O)xâ€”, wherein x is as previously defined above; â€”C(O)â€”NHâ€”; â€”NHâ€”C(O)â€”; â€”C(O)â€”NR12â€”; and â€”NR12â€”C(O)â€”; wherein R12 is hydrogen, C1-C3 alkyl, C1-C3 alkyl substituted with aryl, substituted aryl, heteroaryl, or substituted heteroaryl; andY is selected from the group consisting of:(a) hydrogen; (b) NH2; (c) OH; (d) Zâ€”R7 wherein Z is selected from the group consisting of: (i) â€”NHâ€”(CH2)pâ€”, wherein p is 0 to 5; and (ii) â€”(CH2)pâ€”, wherein p is 0 to 5; and R7 is selected from the group consisting of: (i) hydrogen; (ii) aryl; (iii) substituted aryl; (iv) heteroaryl; (v) substituted heteroaryl; and (vi) Ar1-Ar2, wherein Ar1 and Ar2 are as defined above.