OXABICYCLOHEPTANE PRODRUGS

摘要

The present invention provides a compound having the structure:;

主权项

1. A compound having the structure: wherein X is OR1, NR2R3, OH, O-alkyl, O-alkenyl, O-alkynyl, O-aryl, O-alkylaryl, O-heteroaryl, wherein R1 is H, alkyl, alkenyl, alkynyl, aryl, alkylaryl, heteroaryl, alkylaryl, (C1-C4 alkyl)-O(CO)R4, (C1-C4 alkyl)-O(CO)OR4, O(C1-C4 alkyl)-OP(O)(OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)R4)2, (C1-C4 alkyl)NR4R5, (C1-C4 alkyl)NC(O)R4, (C1-C4 alkyl)C(O)OR4, (C1-C4 alkyl)OC(O)aryl(C1-C4 alkyl)P(O)(OR4)2, (C1-C4 alkyl)OC(O)(C2-C4 alkenyl)CO2R4, (C1-C4 alkyl)OC(O)(C1-C4 alkyl)NH2, (C1-C4 alkyl)C(O)NR4R5, R2 and R3 are each independently H, alkyl, alkenyl, alkynyl, aryl, alkylaryl, heteroaryl, (C1-C4 alkyl)-O(CO)R4, (C1-C4 alkyl)-O(CO)OR4, O(C1-C4 alkyl)-OP(O)(OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)R)2, (C1-C4 alkyl)NR4R5, (C1-C4 alkyl)NC(O)R4, (C1-C4 alkyl)C(O)OR4, (C1-C4 alkyl)OC(O)aryl(C1-C4 alkyl)P(O)(OR4)2, (C1-C4 alkyl)OC(O)(C2-C4 alkenyl)CO2R4, (C1-C4 alkyl)OC(O)(C1-C4 alkyl)NH2, (C1-C4 alkyl)C(O)NR4R5, R17 is H, alkyl, hydroxyalkyl, alkenyl, alkenyl, alkynyl, aryl, alkylaryl, heteroaryl, alkylheteroaryl, C(O)O-t-Bu or —CH2CN;R18 is H or alkyl;R19 is (C1-C4 alkyl)-O(CO)R4, (C1-C4 alkyl)-O(CO)OR4, (C1-C4 alkyl)-OP(O)(OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)OR4)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)R4)2, (C1-C4 alkyl)NR4R5, (C1-C4 alkyl)NC(O)R4, (C1-C4 alkyl)C(O)OR4, (C1-C4 alkyl)OC(O)aryl(C1-C4 alkyl)P(O)(OR4)2, (C1-C4 alkyl)OC(O)(C2-C4 alkenyl)CO2R4, (C1-C4 alkyl)OC(O)(C1-C4 alkyl)NH2, (C1-C4 alkyl)C(O)NR4R5, wherein each occurrence of R4 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R5 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R6 and R7 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R8 is, independently, H, halogen, alkyl, alkenyl, alkynyl, aryl or heteroaryl; and Y is OR9 or NR10R11,
whereinR9 is H, alkyl, alkenyl, alkynyl, aryl, alkylaryl, heteroaryl, alkylaryl, (C1-C4 alkyl)-O(CO)R2, (C1-C4 alkyl)-O(CO)OR12, (C1-C4 alkyl)-OP(O)(OR12)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)OR12)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)R12)2, (C1-C4 alkyl)NR12R13, (C1-C4 alkyl)NC(O)R12, (C1-C4 alkyl)C(O)OR12, (C1-C4 alkyl)OC(O)aryl(C1-C4 alkyl)P(O)(OR12)2, (C1-C4 alkyl)OC(O)(C2-C4 alkenyl)CO2R12, (C1-C4 alkyl)OC(O)(C1-C4 alkyl)NH2, (C1-C4 alkyl)C(O)NR12R13, R10 is H; andR11 is (C1-C4 alkyl)-O(CO)R12, (C1-C4 alkyl)-O(CO)OR12, (C1-C4 alkyl)-OP(O)(OR12)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)OR12)2, (C1-C4 alkyl)-OP(O)(O(C1-C4 alkyl)-O(CO)R12)2, (C1-C4 alkyl)NR12R13, (C1-C4 alkyl)NC(O)R12, (C1-C4 alkyl)C(O)OR12, (C1-C4 alkyl)OC(O)aryl(C1-C4 alkyl)P(O)(OR12)2, (C1-C4 alkyl)OC(O)(C2-C4 alkenyl)CO2R12, (C1-C4 alkyl)OC(O)(C1-C4 alkyl)NH2, (C1-C4 alkyl)C(O)NR12R13, wherein each occurrence of R12 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R13 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R14 and R15 is, independently, H, alkyl, alkenyl, alkynyl, aryl or heteroaryl;wherein each occurrence of R16 is, independently, H, halogen, alkyl, alkenyl, alkynyl, aryl or heteroaryl,wherein when Y is OR9 where R9 is H, alkyl, alkenyl, alkynyl, aryl, alkylaryl, heteroaryl, alkylaryl, thenX isand
when X iswhere R17 is CH3, then X is other than —O(C4 alkyl)-OP(O)(OEt)2 or —NH(C4 alkyl)-OP(O)(OEt)2,
or a salt or ester of the compound.