Patent ID: 6641798
Filing Date: 2003-11-04
Classification: A61K,A61P

Abstract:
A compound of formula wherein W4 and X4 are â€”CR1R2; Y4 is selected from the group consisting of â€”(CH2)aâ€”CONHâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”Bm, â€”(CH2)aâ€”NHCOâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”Bm, â€”(CH2)aâ€”N(R3)â€”(CH2)bâ€”CONHâ€”Bm, (CH2)aâ€”N(R3)â€”(CH2)câ€”NHCOâ€”Bm, â€”(CH2)aâ€”N(R3)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”Bm, â€”(CH2)aâ€”N(R3)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”(CH2)aâ€”CONHâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”(CH2)aâ€”NHCOâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”CH2â€”(CH2OCH2)dâ€”CONHâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”CH2â€”(CH2OCH2)dâ€”NHCOâ€”Bm, â€”(CH2)aâ€”NR3R4, and â€”CH2(CH2OCH2)bâ€”CH2NR3R4; Z4 is selected from the group consisting of â€”(CH2)aâ€”CONHâ€”Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2CONHâ€”Dm, â€”(CH2)aâ€”NHCOâ€”Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”Dm, â€”(CH2)aâ€”N(R3)â€”(CH2)bâ€”CONHâ€”Dm, (CH2)aâ€”N(R3)â€”(CH2)câ€”NHCOâ€”Dm, â€”(CH2)aâ€”N(R3)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”Dm, â€”(CH2)aâ€”N(R3)â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”(CH2)aâ€”CONHâ€”Dm, â€”CH2-(CH2OCH2)bâ€”CH2â€”N(R3)â€”(CH2)aâ€”NHCOâ€”Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”CH2â€”(CH2OCH2)dâ€”CONHâ€”Dm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”N(R3)â€”CH2â€”(CH2OCH2)dâ€”NHCOâ€”Dm, â€”(CH2)aâ€”NR3R4, and â€”CH2(CH2OCH2)bâ€”CH2NR3R4; A2 is a single or a double bond; B2, C2, and D2 are independently selected from the group consisting of â€”Oâ€”, â€”Sâ€”, â€”Seâ€”, â€”Pâ€”, â€”CR1R2, â€”CR1, alkyl, NR3, and â€”C&boxH;O; A2, B2, O2, and D2 may together form a 6- to 12-membered carbocyclic ring or a 6- to 12-membered heterocyclic ring optionally containing one or more oxygen, nitrogen, or sulfur atom; a4 and b4 are independently from 0 to 5; R1 to R4, and R45 to R57 are independently selected from the group consisting of hydrogen, C1-C10 alkyl, C5-C20 aryl, C1-C10 alkoxyl, C1-C10 polyalkoxyalkyl, C1-C20 polyhydroxyalkyl, C5-C20 polyhydroxyaryl, C1-C10 aminoalkyl, cyano, nitro, halogen, saccharide, peptide, â€”CH2(CH2OCH2)bâ€”CH2â€”OH, â€”(CH2)aâ€”CO2H, â€”(CH2)aâ€”CONHâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”CONHâ€”Bm, â€”(CH2)aâ€”NHCOâ€”Bm, â€”CH2â€”(CH2OCH2)bâ€”CH2â€”NHCOâ€”Bm, â€”(CH2)aâ€”OH and â€”CH2â€”(CH2OCH2)bâ€”CO2H; Bm and Dm are independently selected from the group consisting of a bioactive peptide, a protein, a cell, an antibody, an antibody fragment, a saccharide, a glycopeptide, a peptidomimetic, a drug, a drug mimic, a hormone, a metal chelating agent, a radioactive or nonradioactive metal complex, and an echogenic agent; a and c are independently from 1 to 20; and b and d are independently from 1 to 100.