- BETA-LACTAMASE INHIBITORS
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Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof.
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Page/Page column 108
(2010/12/17)
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- Process for the preparation of crystalline (Z)-2-(2-tert.-butoxycarbonylprop-2-oxyimino)-2-(2-triphenylmethylaminothiazol-4-yl) acetic acid in association with N,N-dimethylformamide
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The present invention relates to the preparation of crystalline (Z)-2-(2-tert.-butoxycarbonyl prop-2-oxyimino)-2-(2-triphenylmethylaminothiazol-4-yl) acetic acid of the following formula which is useful in the synthesis of β-lactam antibiotics such is ceftazidime.
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- Antibiotic derivatives, derived from cephalosporins with thiazolyl substituents, pharmaceutical preparations and salts thereof
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The present invention relates to derivatives of the family of cephalosporins, of formula: STR1 in which STR2 is an acid, a salt or an ester of this acid, R1 is a group of form STR3 in which RA and RB are H or alkyl or form a saturated cyclobutyl or cyclopentyl ring and RC is H or COOH, R2 is a thiazolium salt or a OCOCH2 RD group in which RD is a 1,3-thiazol-4-yl group. The invention also relates to a process for preparing the products of formula (I) and to drugs containing said products.
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- (6R,7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimino)acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4-carboxylate and salts thereof
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Cephalosporin antibiotics of the general formula STR1 (wherein Ra and Rb, which may be the same or different, each represent a C1-4 alkyl group or Ra and Rb together with the carbon atom to which they are attached form a C3-7 cycloalkylidene group; and R4 represents hydrogen or a 3- or 4-carbamoyl group) exhibit broad spectrum antibiotic activity, the activity being unusually high against gram-negative organisms such as strains of Pseudomonas organisms. A particular antibiotic compound of formula (I) possessing excellent antibacterial activity against strains of Pseudomonas organisms, as well as other valuable therapeutic properties, is (6R,7R)-7-[(Z)-2-(2-aminothiazol-4-yl)-2-(2-carboxyprop-2-oxyimono) acetamido]-3-(1-pyridiniummethyl)-ceph-3-em-4 carboxylate. The invention also includes the non-toxic salts and non-toxic metabolically labile esters of compounds of formula (I). Also described are compositions containing the antibiotics of the invention and processes for the preparation of such antibiotics.
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