Guanidine derivs. X-N(Y)(CH2)nNHC(:N-Q)N(W)-Z [W is H or together with Z may form a ring; X, Y, Z, Q are H, (un)substituted, (un)satd. alkyl, aryl or heteroaryl; X may also be C(:NH)NH-Z1 (Z1 is a group defined for Z) or RCON(Y), where R is a group Z, -OZ or -NZ; n = 0-10], including pharmacol.-acceptable salts, racemates or single isomers, were prepd. as anti-diabetes, serum glucose-lowering and anti-obesity agents. Thus, N-(γ,γ-dimethylallyl)-N'-(6-aminohexyl)guanidine methanesulfonate (ST2370) was prepd. from S-methylisothiourea sulfate by prenylation of the Boc-protected deriv., reaction with 1,6-diaminohexane, and deprotection using a soln. of methanesulfonic acid in anhyd. dioxane.
Giannessi, F., Tassoni, E., Tinti, M.O., Pessotto, P., Botta, M., Corelli, F. (2004)Preparation of guanidine derivatives and their use as medicines with anti-diabetes and/or anti-obesity activity. . Brevetto No. WO 2004054967.
Preparation of guanidine derivatives and their use as medicines with anti-diabetes and/or anti-obesity activity
BOTTA, MAURIZIO;CORELLI, FEDERICO
2004-01-01
Abstract
Guanidine derivs. X-N(Y)(CH2)nNHC(:N-Q)N(W)-Z [W is H or together with Z may form a ring; X, Y, Z, Q are H, (un)substituted, (un)satd. alkyl, aryl or heteroaryl; X may also be C(:NH)NH-Z1 (Z1 is a group defined for Z) or RCON(Y), where R is a group Z, -OZ or -NZ; n = 0-10], including pharmacol.-acceptable salts, racemates or single isomers, were prepd. as anti-diabetes, serum glucose-lowering and anti-obesity agents. Thus, N-(γ,γ-dimethylallyl)-N'-(6-aminohexyl)guanidine methanesulfonate (ST2370) was prepd. from S-methylisothiourea sulfate by prenylation of the Boc-protected deriv., reaction with 1,6-diaminohexane, and deprotection using a soln. of methanesulfonic acid in anhyd. dioxane.
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https://hdl.handle.net/11365/29944
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