Patent ID: 6372744
Filing Date: 2002-04-16
Classification: A61K,C07K

Abstract:
A compound having the structure: or a pharmaceutically acceptable salt thereof, whereinA is selected from â€”C(&boxH;O)â€”, â€”(CH2)0-4â€”, â€”C(&boxH;O)(CH2)1-3â€”, â€”(CH2)1-2Oâ€” and â€”(CH2)1-2Sâ€”; B is selected from N and CH; C is selected from â€”C(&boxH;O)â€”, â€”C(&boxH;O)(CH2)1-3â€”, â€”(CH2)0-3â€”, â€”Oâ€”, â€”Sâ€”, â€”Oâ€”(CH2)1-2â€” and â€”S(CH2)1-2â€”; D is selected from N and C(R4), E is selected from F is a direct bond or a carbonyl moiety; R1, R3â€² and R4 are independently selected from amino acid side chain moieties and derivatives thereof; R2 is selected from an amino acid side chain moiety and derivatives thereof, or taken together with C forms a fused substituted or unsubstituted homocyclic or heterocyclic ring; R3 is independently selected from an amino acid side chain moiety and derivatives thereof, or taken together with C forms a bridging moiety selected from â€”(CH2)1-2â€”, â€”Oâ€” and â€”Sâ€”; Y and Z represent the remainder of the molecule; and any two adjacent CH groups of the bicyclic ring do or do not form a double bond; and wherein when F is a carbonyl moiety, Y is anached to F by a C(&boxH;O)N bond, with the proviso that Y is not NH2; and when F is a direct bond, Y is selected from â€ƒâ€”CH(OH)CH&boxH;CHC(&boxH;O)OH, â€”CH(OH)CH&boxH;CHC(&boxH;O)R, â€”CH(OH)CH&boxH;CHC(&boxH;O)OR, â€”CH(OH)CH&boxH;CHC(&boxH;O)NRR, â€”CH&boxH;CHC(&boxH;O)SO2R and â€”SO2CH&boxH;CHR, wherein each occurrence of R is independently selected from a lower chain alkyl moiety, a lower chain aryl moiety, a lower chain aralkyl moiety and a heterocyclic moiety; with the proviso that the compound is not 7-methoxy-1,3-dioxo-2-phenyl-N-[(1S)-1-phenylethyl]-2,3,5,8-tetrahydro-1H-[1,2,4]triazolo[1,2-&agr;]pyridazine-5-carboxamide; 7-methoxy-2-phenyl-5-(1-piperidinylcarbonyl)-5,8-dihydro-1H-[1,2,4]triazolo[1,2-&agr;]pyridazine-1,3(2H)dione; (3aR,7aS)-6-methoxy-2-phenyl-4-(1-pyrroldinylcarbonyl)-3a,4,7,7a-tetrahydro-1H-isoindole-1,3(2H)-dione; (3aR,7aS)-6-methoxy-2-phenyl-4-(1-piperidinylcarbonyl)-3a,4,7,7a-tetrahydro-1H)-isoindole-1,3(2H)-dione; 2-phenyl-8-(1-piperidinylcarbonyl)-5,8-dihydro-1H-[1,2,4]triazolo[1,2-&agr;]pyridazine-1,3,6(2H,5H)trione; or (3aR,7aS)-2-phenyl-7-(1-piperidinylcarbonyl)-tetrahydro-1H-isoindole-1,3,5(2H,4H)-trione.