1-, and 1,1- disubstituted -6- substituted -2- carbamimidoyl...

Details 1-, and 1,1- disubstituted -6- substituted -2- carbamimidoyl... 1-, and 1,1- disubstituted -6- substituted -2- carbamimidoyl...

C - Chemistry, Metallurgy

07

D

260/299, 260/266

C07D 487/04 (2006.01) C07C 17/275 (2006.01) C07C 45/74 (2006.01) C07D 205/08 (2006.01) C07D 265/14 (2006.01) C07D 409/06 (2006.01) C07D 477/20 (2006.01) C07D 498/04 (2006.01) C07D 519/00 (2006.01) C07F 7/10 (2006.01) C07F 7/18 (2006.01)

Patent

CA 1198427

TITLE OF THE INVENTION 1-, AND 1,1-DISUBSTITUTED-6-SUBSTITUTED-2-CARBAM- IMIDOYL-1-CARBADETHIAPEN-2-EM-3-CARBOXYLIC ACIDS ABSTRACT OF THE DISCLOSURE Disclosed are 1-, and 1,1-disubstituted-6- substituted-2-carbamimidoyl-1-carbadethiapen-2-em-- 3-carboxylic acids having the structure: Image - 2 - wherein R9 and R10 are, inter alia, hydrogen (R9 and R10 are not both hydrogen) alkyl, cycloalkyl, aryl, and aralkyl; R9 and R10 may be joined; R6 and R7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl, aralkyl; A is a direct, single bond connecting the indicated S and C atoms, or A is a cyclic or acylic connecting group selected, inter alia, from alkyl, cycloalkyl, aryl, heteroaryl, heteroalkyl; R1 and R2, which define the carbamimidoyl function, are, inter alia, independently selected from hydrogen, alkyl, aryl; additionally, said carbamimidoyl is characterized by cyclic structures achieved by the joinder of the two nitrogen atoms via their substituents and by their joinder to connecting group A; additionally, "carbamimidiums" are disclosed by quarternization of one of the nitrogen atoms of said carbamimidoyl. Such compounds as well as their pharmaceutically acceptable salt, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

408575

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