Patent ID: 6656926
Filing Date: 2003-12-02
Classification: A61P,C07F

Abstract:
A compound of formula I: wherein: R1 is a group of formula (III): wherein Rk is hydrogen or (C1-C6)alkyl; Rm is hydrogen or (C1-C6)alkyl, phenyl, benzyl, or phenethyl; and wherein the benz ring is optionally substituted by one or two hydroxy, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, cyano, nitro, mercapto, trifluoromethoxy, or NRfRg; wherein each Rf and Rg is independently hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, phenyl, benzyl, or phenethyl; or Rf and Rg together with the nitrogen to which they are attached are pyrrolidino, piperidino or morpholino; or R1 is a group of formula (IV): wherein Rn is hydrogen or (C1-C6)alkyl; Rp is hydrogen or (C1-C6)alkyl, phenyl, benzyl, or phenethyl; and wherein the benz ring is optionally substituted by one or two hydroxy, halo, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, cyano, nitro, mercapto, trifluoromethoxy, or NRfRg; wherein each Rf and Rg is independently hydrogen, (C1-C6)alkyl, (C1-C6)alkanoyl, phenyl, benzyl, or phenethyl; or Rf and Rg together with the nitrogen to which they are attached are pyrrolidino, piperidino or morpholino; Ra, Rb, Rc, and Rd are each independently hydrogen, (C1-C6)alkyl, or â€”CH2CH2X; and each X is independently halo, (C1-C6)alkylsulfonyl, halo(C1-C6)alkylsulfonyl, or arylsulfonyl, wherein each aryl is optionally substituted with one or more halo, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkanoyloxy, (C1-C6)alkoxycarbonyl, cyano, nitro, or trifluoromethoxy; provided at least two of Ra, Rb, Rc, and Rd are â€”CH2CH2X; or a pharmaceutically acceptable salt thereof.