摘要 |
The present invention is concerned with novel benzimidazole (thio)carbamates with antiparasitic activity. The present invention provides compounds of the following general formula (I) wherein X<SUP>1</SUP> and X<SUP>2</SUP> are O or S, wherein at least one of X<SUP>1</SUP> and X<SUP>2</SUP> is O, Y<SUP>1</SUP> and Y<SUP>2</SUP> are O or S, wherein at least one of Y<SUP>1</SUP> and Y<SUP>2</SUP> is O, R<SUP>1</SUP> is alkyl of 1-4 carbon atoms, R<SUP>2</SUP>, R<SUP>3</SUP> and R<SUP>4</SUP> are independently of each other hydrogen, or a cation, R<SUP>5</SUP> and R<SUP>6</SUP> may both independently be hydrogen or halogen or alkyl having from 1-8 carbon atoms, or -OR<SUP>7</SUP>, wherein R<SUP>7</SUP> is alkyl having from 1-8 carbon atoms, or -SR<SUP>8</SUP>, wherein R<SUP>8</SUP> may be alkyl having from 1-8 carbon atoms, or aryl, or -CO-R<SUP>9</SUP>, wherein R<SUP>9</SUP> is alkyl having from 1-8 carbon atoms, cycloalkyl having from 3-6 carbon atoms, or R<SUP>9</SUP> is aryl, or -OSO<SUB>2</SUB>-Ar, wherein Ar is aryl, or -S(O)R<SUP>10</SUP>, wherein R<SUP>10</SUP> is alkyl having from 1-8 carbon atoms, or wherein R<SUP>10</SUP> is aryl. The compounds of the invention are highly soluble and stable in water. Moreover, it has been found that the compounds according to the invention are stable for over 8 hours at pH 5 and at pH 9, which are the lower and upper pH limits at which compounds should be stable for over 8 hours in order to be suitable for drinking water application. The compounds of the present invention have excellent antiparasitic, and especially anthelmintic activity in vivo, which is comparable to the state of the art, water insoluble, benzimidazole carbamates such as albendazole and fenbendazole. |
申请人 |
INTERVET INTERNATIONAL B.V.;CHASSAING, CHRISTOPHE, PIERRE, ALAIN |
发明人 |
CHASSAING, CHRISTOPHE, PIERRE, ALAIN |