http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CA-2374555-A1

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filingDate 2000-06-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a11b0989fc06a6dc9046ee62fef10245
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc3770bab8c74fb43fbb2144db7bc1e4
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_06d6b46c885f1a616cf934591aa5d53c
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b33f35b8c10333ed6684d81d16411915
publicationDate 2000-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CA-2374555-A1
titleOfInvention Thiol derivative, metallo-beta-lactamase inhibitors
abstract Thiol derivative compounds, pharmaceutically acceptable salts, and biolabile esters thereof, useful for inhibiting metallo-.beta.-lactamases, bacterial enzymes which confer resistance to clinically relevant ~-lactam antibiotics, characterized by general formula (I): wherein: R1 is selected from straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 Rx groups; and (CH2)nAr, where Ar is an aryl selected from the group consisting of phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; R2 is selected from hydrogen; and a group of formula (II): wherein: R3 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with from 1 to 3 Rx groups; (CH2)nAr, where Ar is an aryl selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where Ar is optionally substituted with 1 to 3 Rx groups, and where n is 0, 1, 2 or 3; and a group of formula (III): wherein: R4 is selected from hydrogen; and straight or branched alkyl; R5 is selected from hydrogen; straight, branched, unsaturated or alicyclic alkyl, optionally substituted with 1 to 3 Rx groups, where the alkyl group is optionally interrupted by X, where X is selected from O, S, NH and N(COCH3); allyloxy and 9-fluorenylmethyloxy; and (CH2)nAr, where Ar is selected from phenyl, furanyl, thienyl, pyridyl, naphthyl, biphenyl, dibenzofuranyl, dibenzothienyl, fluorenyl and fluorenonyl, where n is 0, 1, 2 or 3, and where Ar is optionally substituted with 1 to 3 Rx groups; and Rx is selected from OR, CN, C(O)NH2, C(O)NHR, C(O)N(R)2, OC(O)NH2, OC(O)R, CHO, SO2NH2, SOR, CF3, C(O)R, COOR, F, Cl, Br, I, OCH2Ph, NHR, N(R)2, NHCOR, NHCO2t-Bu, NHCO2allyl, NH2, and R, where R is hydrogen, C1 to C15 alkyl, or aryl. The invention is further directed to a pharmaceutical composition containing the compound, as well as a method for treating bacterial infections in animals or humans, wherein the composition can be administered in combination with a .beta.-lactam antibiotic.
priorityDate 1999-06-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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