Patent ID: 6486350
Filing Date: 2002-11-26
Classification: A61P,C07C,C07K,G01N

Abstract:
An intermediate useful in the preparation of biological reagents that inhibit &bgr;-amyloid peptide release and/or its synthesis, wherein said intermediate is represented by formula VIAâ€”Bâ€²â€ƒâ€ƒVI wherein A is represented by formula V whereinR41 is selected from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, heteroaryl and heterocyclic; R42 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, aryl, heteroaryl and heterocyclic; each R43 is independently selected from the group consisting of hydrogen and methyl and R43 together with R44 can be fused to form a cyclic structure of from 3 to 8 atoms which is optionally fused with an aryl or heteroaryl group; each R44 is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclic, substituted alkyl, substituted alkenyl and substituted alkynyl; each R45 is selected from hydrogen and methyl or together with R43 forms a cycloalkyl group of from 3 to 6 carbon atoms; X is selected from oxygen, sulfur and NH; Xâ€² is hydrogen, hydroxy or fluoro; and Xâ€³ is hydrogen, hydroxy or fluoro, or Xâ€² and Xâ€³ together form an oxo group; Z is selected from the group consisting of a bond covalently linking R41 to â€”CXâ€²Xâ€³â€”, oxygen and sulfur; n is an integer equal to 1 to 3; and Bâ€² is selected from the group consisting of a) (CH2CH(R)Q)nH b) alkylene-Qâ€”H c) substituted alkylene-Qâ€”H wherein R is selected from hydrogen, alkyl or aryl and Q is selected from the group consisting of â€”Oâ€”, â€”Sâ€” and â€”NHâ€”.