Abstract: The invention provides a method of identifying an inhibitor of LtaS comprising: (a) providing bacteria which comprise a mutation in the mbl gene or homologue thereof; (b) culturing the bacteria of (a) in the presence of a test substance under conditions of low magnesium; (c) monitoring the growth of the bacteria; wherein growth or more rapid growth of the bacteria compared to growth in the absence of the test substance is indicative that the test substance is an inhibitor of LtaS.

Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: A method for producing a fermentation product from a lignocellulose-containing material comprises pre-treating the lignocellulose-containing material; introducing a cationic polysaccharide to the pre-treated lignocellulose-containing material; exposing the pre-treated lignocellulose-containing material to an effective amount of a first hydrolyzing enzyme; and fermenting with a fermenting organism to produce a fermentation product. The cationic polysaccharide may be a cationic starch.

Abstract: The present invention is directed to attaching drugs 11 and other functional groups to surfaces of nano-sized diamond particles (NDs) 20 to enhance their efficacy. The method involves hydrating a plurality of nanodiamond (ND) particles 20 having a plurality of carbon chain surface molecules 23 on its surface. Cations 40 are embedded within the lattice structure 21 of the surface molecules 23 of the ND particles 20. The embedded cations 40 attract anions that cause crystalline growth. The anion form of drug molecules 11 are then grown on the crystal to cause the NDs 20 to be coated such that the active sites of said drug molecules 11 point away from the ND particle 20 exposing them for enhanced activity and enhanced drug efficacy. The efficacy of antimicrobial drugs 11, as well as other drugs 11 are enhanced by their attachment to the NDs 20.

Abstract: 1

Abstract: The present invention provides anhydrous crystals of &bgr;-lactam compound represented by the formula: 1

Abstract: A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.

Abstract: The crystal of the invention is the crystal of diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate 1,1-dioxide which is stable substantially without decomposition or degradation of properties even when left to stand at a temperature of 5 to 35° C. for a period of 1 year.

Abstract: The crystal of the invention is crystal of diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate which is stable substantially without decomposition or degradation of properties even when left to stand at room temperature for 1 year.

Abstract: The present invention provides processes for making compounds of the structure(Q--L.sup.1)--L--(L.sup.2 --B)wherein(I) Q is a quinolone moiety;(II) B is a lactam moiety; and(III) L, L.sup.1, and L.sup.2 together comprise a linking moiety;comprising the steps of:(1) coupling a compound of Formula (III) with a lactam-containing compound to form an intermediate compound; and(2) cyclizing the intermediate by reaction with an organosilicon compound to give a compound of the formula (Q--L.sup.1)--L--(L.sup.2 --B).Preferably, the process additionally comprises a step prior to the coupling step, wherein protected forms of the compound of Formula (III) and the lactam compound are formed; and deprotection steps after the cyclization step, wherein the protecting groups are removed. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem, a carbapenem, a cephem, or a carbacephem. Also preferred are those compounds where L.sup.1, L, and L.sup.

Abstract: The present invention provides a novel process for the preparation of 5-arylhydantoins as an important intermediate of (D)-arylglycines (e.g., (D)-p-hydroxyphenyl-glycine) useful for the synthesis of semisynthetic penicillines and cephalosporins, the process comprising (i) reacting a 5-unsubstituted hydantoin compound with a halogenating agent and (ii) reacting the resulting product with a p-unsubstituted phenol compound, the hydroxy group of which may be protected, to substitute the 5-position of the hydantoin compound with the phenol compound at the para position.

Abstract: The present application discloses a process for the conversion of penicillin-1-(R)-sulfoxide(s) and/or cephalosporin-1-(R)-sulfoxides in solution, to their corresponding 1-(S)-sulfoxides comprising the step of treating said 1-(R)-sulfoxide with a sufficient amount of an acid anhydride to convert at least some of said 1-(R)-sulfoxide to its corresponding 1-(S)-sulfoxide. Also disclosed is a process for the production of 1-(S)-sulfoxide from penicillin and/or cephalosporin by oxidizing the penicillin or cephalosporin with an oxidizing agent and simultaneously or subsequently adding a sufficient amount of an acid anhydride to convert at least some 1-(R)-sulfoxide to its corresponding 1-(S)-sulfoxide over a time period of from 5 minutes to 2 hours so as to maintain the pH above 3.5 and produce a solution of the corresponding 1-(S)-oxide. In a preferred embodiment, a buffer is incorporated in the solution to provide additional pH control during the reaction.

Abstract: There is described a process for the manufacture of carboxylic acid amides by acylating amines with 2-benzothiazolyl thioesters of carboxylic acids, which process comprises reacting the amine in the form of an acid addition salt. This process is especially of great advantage when the amine is not particularly stable in the form of the free base, which is frequently the case especially with 7-aminocephalosporin derivatives. 7-Acylamino-cephalosporin derivatives can be manufactured in good yield and in high purity with the novel process.

Abstract: The present invention provides methods of making compounds of the structure[Q-L.sup.1 ]-L-[L.sup.2 -B[wherein(I) Q is a quinolone moiety;(II) B is a beta-lactam moiety;(III) L, L.sup.1, and L.sup.2 together comprise a carbamate-containing linking moietycomprising the steps of:(1) Reacting a lactam compound of the formula B-L.sup.4 -H with phosgene to form an intermediate compound of the formula B--L.sup.4 --C(=O)--Cl, where L.sup.4 is oxygen; and(2) Coupling said intermediate compound with a quinolone compound of the formula Q-L.sup.3 -R.sup.44 ; wherein L.sup.3 is nitrogen; R.sup.44 is hydrogen, Si(R.sup.45).sub.3, or Sn(R.sup.45).sub.3 ; and R.sup.45 is lower alkyl.Preferably, the process additionally comprises steps prior to the reacting and coupling steps where esters of the lactam and quinolone compounds are made. Also preferably, the coupling step comprises adding a solution containing the quinolone compound to a solution containing the intermediate compound.

Abstract: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.

Abstract: A new compound called N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine of Formula I ##STR1## A process for the preparation thereof based on the reaction of 4-ethyl-2,3-dioxo-piperazine or a trimethylsilyl derivative thereof with carbonyl chloride or a derivative thereof.The use of the compound of Formula I as an intermediate in the preparation of compounds of Formula II ##STR2## where R is a radical, substituted in alpha position, of a molecule of an acid selected from the group formed by phenylacetic acid, p-hydroxy phenylacetic acid, a 6-(phenylacetamido)-penicillanic acid and a 7-(phenylacetamido)-cephalosporanic acid.

Abstract: A process is described for producing pure crystalline products, in particular penicillin and cephalosporin, wherein the desired product, prepared according to a known method, is treated with ethanol in one or two steps, whereby the crystallization of the pure product and impurity separation are achieved.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.

Abstract: Disclosed are an optically active, ethylenically unsaturated monomer represented by the following structural formula: ##STR1## wherein: A stands for S, SO or SO.sub.2 ; X and Y each stand for a hydrogen atom or a substituent selected from the group consisting of alkyl groups and acyl groups; Z stands for a substituent selected from the group consisting of alkoxy, alkylamino, hydroxyl and silyloxy groups; and X and Y can be bonded together to form a ring with the nitrogen atom to which they are bonded or X and Y can be a single group bonded to said nitrogen atom through a double bond, with the proviso that at least one of X and Z is an alkenyl equivalent to said group, and polymers of this monomer. One typical instance of the monomer is benzyl 6-acrylaminopenicillanate.

Abstract: Diphenylmethyl esters of cephalosporins, and processes for synthesizing such, are described and disclosed.

Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.

Abstract: There are presented compounds of the formula ##STR1## wherein R.sub.2, R.sub.3, R.sub.4 and m are as described herein.

Abstract: 2-(Allenyl)penicillins antibiotics and intermediates thereto are disclosed. A process for making the 2-(allenyl)penicillins and the starting materials for the process are also disclosed.

Abstract: A compound having the partial structure (A): ##STR1## wherein n is 1 or 2.

Abstract: 6.beta.-(L-.alpha.-Aminoadipoyl)-2.alpha.-vinyl-2.beta.-methylpenam-3-carbo xylic acid is provided in an enzymatic process converting .delta.-(L-.alpha.-aminoadipoyl)-L-cysteinyl-D-.gamma.,.delta.-didehydrois oleucine with isopenicillin N synthetase. The 2.alpha.-vinylpenam product is converted by known methods to the 6.beta.-amino-2.alpha.-vinyl-2.beta.-methylpenam-3-carboxylic acid nucleus and the latter is N-acylated to provide corresponding 6.beta.-acylaminopenams.

Abstract: The (5-R-2-oxo-1,3-dioxolen-4-yl)methyl moiety: ##STR1## wherein R is loweralkyl of 1-6 carbon atoms, especially methyl or t-butyl; when utilized as an ester on a pharmaceutical having a carboxylic acid functionality, enhances oral absorption of the pharmaceutical. This effect is applicable to a broad range of pharmaceutically active substances, including antibiotics, and antihypertensives as well as other classes of therapeutic agents.

Abstract: This invention relates to the hybridization of streptolydigin, tirandamycin and sorbic acid to penicillin and cephalosporin nuclei.

Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.

Abstract: Substituted 1,3-dithietane-2-carboxylic acid derivatives useful as intermediates for the preparation of highly effective penicillin and cephalosporin derivatives and the preparation thereof.