Patent ID: 6548679
Filing Date: 2003-04-15
Classification: A61K,A61P,C07C,C07D,C07K,Y02A

Abstract:
A compound of formula I: whereinR1 is â€”(CH2)nâ€”(X)â€”(Y); n is 1; X is thio; Y is a 2 to 6 membered branched or unbranched carbon chain; wherein said chain is substituted on carbon with 1, 2, or 3, oxo, heteroaryl; and wherein said chain may optionally be saturated or unsaturated; R2 is hydrogen or (C1-C6)alkyl; R3 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, aryl, heteroaryl, aryloxy, or heteroaryloxy; R4 is hydrogen or (C1-C6)alkyl; and R5 is hydroxy, (C1-C6)alkoxy, or (C1-C6)alkanoyloxy; or R4 and R5 taken together are ethylenedioxy; R6 is hydrogen, carboxy, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, halo(C1-C6)alkyl, â€”C(&boxH;O)NRfRg, or (C1-C6)alkyl optionally substituted by 1 or 2 hydroxy, (C1-C6)alkoxy, (C1-C6)alkanoyloxy, carboxy, or â€”C(&boxH;O)NRfRg; Ra is hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, phenyl or benzyl; and Rb, Rc, Rf and Rg are each independently hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, phenyl or benzyl; or Rb and Rc or Rf and Rg, together with the nitrogen to which they are attached, are pyrrolidino, piperidino, or morpholino; wherein any aryl, heteroaryl, aryloxy, or heteroaryloxy of Y, or R3 may optionally be substituted by 1, 2, or 3 ((C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, hydroxy (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy, halo, carboxy, mercapto, nitro, or â€”N(Rh)(Rj); wherein each Rh and Rj is independently hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, phenyl or benzyl; or Rh and Rj together with the nitrogen to which they are attached are pyrrolidino, piperidino, or morpholino; or a pharmaceutically acceptable salt thereof.