Patent ID: 6660246
Filing Date: 2003-12-09
Classification: A61K,C07B,C07C,C07F

Abstract:
A compound of the following formula I: whereQ is the group â€”(C(RR))m1â€”(Y1)nâ€”(C(RR))m2â€”(Y2â€”(C(RR))m3)n1â€”, where Y1 and Y2 are each independently â€”NRâ€”, â€”Oâ€”, â€”Sâ€”, â€”SOâ€”, â€”SO2â€” or â€”Seâ€”; n and n1 are each independently 0 or 1; and m1, m2 and m3 are each independently 0 or an integer from 1 to 4; provided that m1 and m2 are not both 0, that m1+m2+n+n1 is less than 6 and that a carbon atom bearing an R group is not directly bonded to more than one heteroatom; each R and R* group is independently: (i) R1; (ii) alkoxy; (iii) hydroxy; (iv) halogen; (v) haloalkyl; (vi) â€”OR1; (vii) â€”C(O)â€”OR1; (viii) â€”C(O)â€”N(R1)2; (ix) â€”N(R1)2â€”; (x) â€”N(R1)â€”COR1; (xi) -alkyl-C(O)â€”OR1; (xii) -alkyl-C(O)â€”N(R1)2; (xiii) -alkyl-N(R1); (xiv) -alkyl-N(R1)â€”COR1; (xv) -aryl-C(O)â€”OR1; (xvi) -aryl-C(O)â€”N(R1)2; (xvii) -aryl-N(R1)2; (xviii) -aryl-N(R1)â€”COR1; (xix) nitrile; (xx) acyl; (xxi) acyloxy; (xxii) heterocyclo; (xxiii) hydroxyalkyl; (xxiv) alkoxyalkyl; (xxv) hydroxyaryl; (xxvi) arylalkyl; (xxvii) â€”SO2â€”R1; (xxviii) -alkyl-SO2â€”R1; (xxix) â€”(A)pâ€”R1, where A is a linking group which is bound to Ra via a carbon, oxygen, nitrogen or sulfur group, p is 0 or a positive integer, and Ra is a bioactive moiety or a reactive group which forms a covalent bond to a bioactive moiety; or (xxx) two of the groups, taken together with one or more atoms to which they are bonded, form a saturated or unsaturated, spiro or fused, carbocyclic or heterocyclic ring which may be unsubstituted or substituted by one or more groups selected from the groups (i) to (xxix) above; each R1 is independently hydrogen, alkyl, alkenyl, alkynyl or aryl; and G1 and G2 are each independently â€”OH or â€”N(R2)2, provided that at least one of G1 and G2 is â€”N(R2)2, where each R2 is independently hydrogen, alkyl, aryl, acyl or â€”(A)pâ€”Ra, further provided; each alkyl is substituted or unsubstituted and has 1 to 12 carbon atoms; each alkoxy is substituted or unsubstituted and has 1 to 12 carbon atoms; each alkenyl is substituted or unsubstituted and has 2 to 10 carbon atoms; each alkenyl is substituted or unsubstituted and has 2 to 10 carbon atoms; each cycloalkyl is substituted or unsubstituted and is a 2- to 3-ring system where each ring contains 3 to 7 carbon atoms; each aryl is substituted or unsubstituted and is a homocyclic aromatic group which contains 1 or 2 rings where each ring contains 6 to 12 carbon atoms; each heterocycl is substituted 1 or 2 is where or unsaturated, aromatic or non-aromatic cyclic group containing at least one oxygen, nitrogen or sulfur atom; and each bioactive moiety is a group selected from the list consisting of a group which can function a s a metabolic substrate, catalyst or inhibitor; a group which can preferentially be taken up at a selected biological site; a group which contains reactive groups for coupling to a protein; or a group which can preferentially localize at a selected biological site.