Patent ES-8604232-A1 (ES)
Title: Beta-lactam antibiotics.
IPC: A61P31/04
Filed: 1983-12-28
Abstract: EP--93564 A 6-(2-(3,4-Dihydroxyphenyl) 2-(aminocarbonylamino)) acetamido bisnorpenicillanic acid derivs. of formula (I) and their salts and in vivo hydrolysable esters are new. In (I) R is H, 2-7C alkanoyl or 1-6C alkyl R1 is H or hydrocarbyl R2 is H, opt. substd. hydrocarbyl, opt. substd. heterocyclyl or CXR3 X is O or S R4 is H, opt. substd. hydrocarbyl or opt. substd. heterocyclyl NR1R2 is opt. substd. heterocyclyl. - (I) are broad-spectrum antibacterials useful as therapeutic agents in man and animals they may be administered alone or with a beta-lactamase inhibitor. Dose is 0.1-3 g daily in adults, esp. 1-5g. EPAB- EP--93564 B 6-(2-(3,4-Dihydroxyphenyl) 2-(aminocarbonylamino)) acetamido bisnorpenicillanic acid derivs. of formula (I) and their salts and in vivo hydrolysable esters are new. In (I) R is H, 2-7C alkanoyl or 1-6C alkyl R1 is H or hydrocarbyl R2 is H, opt. substd. hydrocarbyl, opt. substd. heterocyclyl or CXR3 X is O or S R4 is H, opt. substd. hydrocarbyl or opt. substd. heterocyclyl NR1R2 is opt. substd. heterocyclyl. - (I) are broad-spectrum antibacterials useful as therapeutic agents in man and animals they may be administered alone or with a beta-lactomase inhibitor. Dose is 0.1-3 g daily in adults, esp. 1-5g. (39ppDwg.No.0/0) - EP--93564 B A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein R is hydrogen, C1-6 alkylcarbonyl R1 is hydrogen or a C1-6 alkyl R2 is hydrogen, a C1-6 alkyl optionally substituted by heterocyclyl, a heterocyclic group, or CXRd where X is O or S and Rd is hydrogen, C1-6 alkyl optionally substituted by heterocyclyl, or a heterocyclyl group or R1 and R2 together with the nitrogen to which they are attached form a heterocyclyl group the aforementioned heterocyclyl groups comprising single or fused rings having up to four hetero atoms in the ring selected from oxygen, nitrogen and sulphur and optionally substituted with up to three halogen, C1-6 alkyl, C1-6 alkoxy, halo-(C1-6)-alkyl, hydroxy, amino, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl(C1-6)alkyl, oxo, phenyl optionally substituted with up to three groups selected from halogen, C1-6 alkyl, phenyl, C1-6 alkoxy, halo(C1-6)alkyl, alkoxycarbonyloxy, or C1-6 alkylcarbonyl, or naphthyl, optionally substituted as for phenyl, groups. (15pp) - EP--93564 B 6-(2-(3,4-Dihydroxyphenyl) 2-(aminocarbonylamino)) acetamido bisnorpenicillanic acid derivs. of formula (I) and their salts and in vivo hydrolysable esters are new. In (I) R is H, 2-7C alkanoyl or 1-6C alkyl R1 is H or hydrocarbyl R2 is H, opt. substd. hydrocarbyl, opt. substd. heterocyclyl or CXR3 X is O or S R4 is H, opt. substd. hydrocarbyl or opt. substd. heterocyclyl NR1R2 is opt. substd. heterocyclyl. - (I) are broad-spectrum antibacterials useful as therapeutic agents in man and animals they may be administered alone or with a beta-lactamase inhibitor. Dose is 0.1-3 g daily in adults, esp. 1-5g. (Dwg.0/0) USAB- US4540688 A Beta-lactam antibiotics of formula (I) are claimed, where R is H, 1-6C alkyl or 1-6C alkyl carbonyl, R1 is H or hydrocarbyl, R2 is H or opt. substd. hydrocarbyl or opt. substd. heterocyclyl or is CXRd in which X is O or S and Rd is H or opt. substd. heterocyclyl, or R1 and R2, together with the N atom to which they are attached, form an opt. substd. heterocyclyl gp. Salts and esters which are hydrolysable in vivo are also claimed. - A typical cpd. is 6-beta- D-2-(4-ethyl -2,3-dioxopiperazine-1-carbony lamino) -2-(2,4-dihydroxyphenyl) acetamidobisnorpenicillanic acid.