Method for producing amidinopenicillanoyloxyalkyl...

C - Chemistry – Metallurgy – 07 – D

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260/102, 260/103

C07D 501/20 (2006.01) C07D 499/00 (2006.01)

Patent

CA 1118412

ABSTRACT OF THE DISCLOSURE Novel esters of the formula 1, salts of the esters of such for- mula I with pharmaceutically acceptable acids, and processes for producing such new compounds are provided herein. The novel esters have the for- mula I Image I in which R1 and R2 represent C1-7 alkyl or together with the nitrogen form a heterocyclic radical having 4 to 8 carbon atoms; R3 represents hydrogen or benzyl; R5 represents hydrogen acyloxy, carbamoyloxy, or SR8, where R8 stands for a heterocyclic ring; R6 represents methyl substituted by cyano, pyridylthio, trifluoromethyl or by a 5-membered heterocyclic ring, or simultaneously by a 5-membered heterocyclic ring and by methoximino or represents benzyl substituted by azido, amino and/or hydroxy or represents 1,4-cyclohexadienylmethyl substitued by amino; and R7 represents hydrogen or methoxy. The novel compounds described above posses valuable in vivo antibacterial activity and their toxicity is low, even when administered parenterally.

272706

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