Patent ID: 6024937
Filing Date: 2000-02-15
Classification: A61K,C07C,C07D

Abstract:
A compound of the formula: ##STR26## wherein: n=0 or 1;R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, .dbd.O with the proviso that both are not .dbd.O, .paren open-st.CH.sub.2 .paren close-st..sub.m Z where m is 0-10 and Z represents a conjugation group or targeting moiety, and .paren open-st.CH.sub.2 .paren close-st..sub.m W where m is 0-10 and W represents a hydrolyzable group, or R.sub.1 and R.sub.2 are taken together to form a cyclic anhydride or a benzene ring, wherein the conjugation group is an anhydride or active ester, the targeting moiety is a protein or biotin, and the hydrolyzable group is an imidate, ester or carbamate;R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, substituted lower alkyl, alkoxy, perhaloalkyl, halogen, hydroxyl, nitro, .paren open-st.CH.sub.2 .paren close-st..sub.m Z, and .paren open-st.CH.sub.2 .paren close-st..sub.m W;R.sub.4 and R.sub.5 are attached at one or more of the ring positions and are independently selected from the group consisting of hydrogen, lower alkyl, substituted lower alkyl, alkoxy, perhaloalkyl, halogen, hydroxyl, nitro, .paren open-st.CH.sub.2 .paren close-st..sub.m Z, and .paren open-st.CH.sub.2 .paren close-st..sub.m W;A and A' are independently selected from the group consisting of nitrogen and sulfur, where a sulfur may bear a hydrogen or a sulfur protecting group, or where A and A' are both sulfur, A and A' may be joined together by a bond, and where a nitrogen may bear a hydrogen, a hydroxyl or a lower alkyl substituent, or where A and A' are both nitrogen, A and A' may be joined by --CH.sub.2 --(CH.sub.2).sub.n --CH.sub.2 -- where n is 0 or 1;X, Y, X' and Y' are independently selected from the group consisting of carbon and nitrogen;.alpha. and .beta. represent carbon atoms which may bear a carbon-nitrogen double bond; andsaid compound has at least one Z or W.