Carbamylguanidine antimicrobial compounds

A - Human Necessities – 61 – K

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260/538.2, 260/5

A61K 31/35 (2006.01) A61K 31/13 (2006.01) A61K 31/135 (2006.01) A61K 31/16 (2006.01) A61K 31/165 (2006.01) A61K 31/17 (2006.01)

Patent

CA 1070684

ABSTRACT OF THE DISCLOSURE: Antimicrobial compounds are disclosed having the formula: Z-B-Y-B'-Z 'nHA wherein B is carbamylguanidino, or thiocarbamylguanidino and B' is B or biguanidino provided that B' is biguanidino only when B is carbamylguanidino bonded to Y through the guanidino portion of the group, Y is a bivalent organic radical selected from the group con- sisting of C2-C12 alkylene, C5-C12 cycloalkylene, C5-C12 cyclo- alkylenebis(loweralkyl), C6-C12 arylene and loweralkylarylene, C7-C12 aryleneloweralkyl, and C8-C12 arylenebis(loweralkyl) and Z is selected from the group consisting of C1-C12 alkyl; C4-C12 dialkylaminoalkyl; C3-C12 alkenyl; C3-C12 alkynyl; C3-C12 cycloalkyl, C4-C12 cycloalkylalkyl; C1-C10 alkoxy C10-C2 alkyl having a total carbon content of C3-Cl4; C1-C10 alkylthio C10-C2 alkyl having a total carbon content of C3-C14; phenoxy C2-C6 alkyl; phenylthio C2-C6 alkyl; C6-C14 aryl; C7-C14 aralkyl, and arylcycloalkyl; and C6-C14 aryl and aralkyl substituted with one or more radicals selected from the group con- sisting of loweralkyl, trifluoromethyl, loweralkoxy, trifluoro- methoxy, phenoxy, loweralkylthio, halo, nitro, cyano, C2-C6 acyl, benzoyl, alkoxycarbonyl, diloweralkylamino, loweralkylsulfonyl, fluorosulfonyl and alkylsulfinyl; n=0, 1/3, 1/2, 2/3, 1, 2 and HA is an inorganic or organic acid. These compounds are useful in controlling the micro organisms that produce dental plaque.

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