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| Number | Title | Issue Date |
| 7022844 | Amide-based compounds, production, recovery, purification and uses thereof Methods are disclosed of producing and purifying at least one amide. In accordance with one of the methods disclosed herein, the at least one amide is produced by providing an organic liquid comprising at least one oxime, providing at least one catalyst, adding the ... | 04/04/2006 |
| 6949521 | Therapeutic azide compounds Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs... | 09/27/2005 |
| 6414141 | Process for purifying an ampicillin pro-drug ester Applicants have developed a process for purifying an ampicillin pro-drug ester, e.g., bacampicillin, or an acid addition salt thereof of formula I. ##STR1## The process comprises a step wherein a crude solution of the pro-drug ester is subjected to an eva... | 07/02/2002 |
| 6013647 | Benzoxazinedione derivatives, method of producing them and uses thereof This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R1 =H or carboxyalkyl, R2 =H, alkyl or phenyl, and R3 represents different acid groups derived from amino aci... | 01/11/2000 |
| 5607671 | Medical use, a medical method and a pharmaceutical preparation The invention concerns medical use, a medical method and a pharmaceutical preparation. The invention allows the action of ଲ-lactam antibiotics to be targeted and their side effects to be reduced by inactivation of part of the antibiotic in a desired... | 03/04/1997 |
| 5599987 | Integrated process for cyclohexanone oxime production An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein isopropanol is utilized to generate the hydrogen peroxide oxidizing agent. The acetone produced as a co-product is recycled back to the secondary alcohol... | 02/04/1997 |
| 5498729 | Prodrug compositions Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: ##STR1## wherein R' is a residue of a therapeutic bioactive compound, for example, ... | 03/12/1996 |
| 5451701 | Integrated process for cyclohexanone oxime production An integrated process for producing cyclohexanone oxime, a caprolactam precursor, is provided wherein a secondary alcohol is utilized to generate the hydrogen peroxide oxidizing agent and as a reaction medium for ammoximation. The ketone produced as a co-... | 09/19/1995 |
| 5304643 | Process for producing epsilon-caprolactam &3xb5;-Caprolactam is prepared by subjecting cyclohexanone oxime in a gas phase to a catalytic reaction using zeolite catalysts in the presence of water and at least one compound selected from alcohols and ether compounds.... | 04/19/1994 |
| 4889929 | Preparation of 1'-ethoxycarbonyl-oxyethyl esters of penicillins Process for the preparation of 1'-ethoxy carbonyloxy ethyl esters of penicillins, wherein a compound of the formula ##STR1## in which A is phenyl, phenoxy or 4-hydroxyphenyl, B is hydrogen, an amino group or a protected amino group and Z is hydrogen ... | 12/26/1989 |
| 4882325 | Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(d-amino-phenylacetamido)penicillanate napsylate and method of using the same Crystalline 1,1-dioxopenicillanoyloxymethyl 6-(D--amino--phenylacetamido)penicillanate napsylate. The product may be prepared by reacting 1,1-dioxopenicillanoyloxymethyl 6-(D--amino--phenylacetamido)penicillanate or a salt ther... | 11/21/1989 |
| 4866170 | Stable hydrate of penicillin derivative A stable trihydrate of (2S, 5R, 6R)-6-{(2R)-2-[(2R)-2-amino-3-(N-methylcarbamoyl)propionamido]-2-(p-hydrox yphenyl)acetamido}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-c arboxylic acid and process for preparing the same are disclosed.... | 09/12/1989 |
| 4840944 | Antibacterial beta-lactams, pharmaceuticals thereof and methods of using them The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R1 stands for a phenyl, 4-hydroxyphenyl, 1,4-cyclohexadienyl or a 3-thienyl group; R2 represents a primary amino or a carbox... | 06/20/1989 |
| 4831025 | Crystalline penicillin derivative tosylate hydrates The present invention relates to a crystalline hydrate of a salt of the antimicrobial agent 1,1-dioxopenicillanoyloxymethyl 6-(D--amino--phenylacetamido)penicillanate with p-toluenesulfonic acid, more particularly the mono- and dihydrate. Th... | 05/16/1989 |
| 4820857 | -bromodiethylcarbonate The novel compound -bromodiethylcarbonate, novel methods for the preparation thereof, its use in the preparation of 1-ethoxycarbonyloxyethyl esters of penicillins and cephalosporins, and improvements in the method for preparing such esters.... | 04/11/1989 |
| 4626532 | Process for stabilization of bacampicillin hydrochloride A new process for the stabilization of bacampicillin hydrochloride against degradation by humidity characterized by the incorporation of between 3 to 9% by weight of straight-chain alkanes, alkenes, fatty acids, alcohols, and esters of fatty acids and alc... | 12/02/1986 |
| 4457924 | 1,1-Alkanediol dicarboxylate linked antibacterial agents Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula ##STR1## where A is the residue of certain dicarboxyic acids, R3 is H or (C1 -C | 07/03/1984 |
| 4410458 | Process for providing an oxidized penam This invention relates to a process for preparing an oxidized penam derivative of the formula: ##STR1## wherein R1 represents an amino or protected amino radical, and R3 represents a radical selected from the group consisting of carb... | 10/18/1983 |
| 4400509 | Silylation process An improved process for the trimethylsilylation of organic compounds with at least one active hydrogen atom with hexamethyldisilazane, the improvement comprising effecting the reaction in the presence of 0.001 to 10 mole percent of a catalyst of the formu... | 08/23/1983 |
| 4389408 | Novel ampicillin esters and production thereof A novel Ampicillin ester of the general formula ##STR1## wherein R1 represents a hydrogen atom, a methyl group or an aryl group, and R2 represents a hydrogen atom or may be taken together with R1 to form a divalent ca... | 06/21/1983 |
| 4381307 | Soft tertiary amine esters of bio-affecting carboxylic acids Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C1 -C4 alkyl; n is 0 or 1; R1 and R2 ar... | 04/26/1983 |
| 4381263 | Process for the preparation of penicillanic acid esters A process for the preparation of chloromethyl esters of penicillanic acids, using iodochloromethane or bromochloromethane and a tetraalkylammonium salt of the penicillanic acid, and their use in processes for the synthesis of penicillanic acid esters, usi... | 04/26/1983 |
| 4342693 | 1,3-Dioxolen-2-one derivatives and process for production thereof A 1,3-dioxolen-2-one derivative of the general formula ##STR1## wherein R1 represents a hydrogen atom, a methyl group, or an aryl group, R2 represents a hydrogen atom, or may be taken together with R1 to form a divale... | 08/03/1982 |
| 4293560 | Talampicillin 2-methoxyphenoxyacetate and pharmaceutical compositions containing it Talampicillin 2-methoxyphenoxyacetate; a process for its preparation by acid hydrolysis of the metampicillin phthalidyl ester in a biphasic aqueous-organic solvent and treatment of the resulting aqueous phase with an alkali metal salt of the 2-methoxyphen... | 10/06/1981 |
| 4255330 | Process for preparing 6-substituted amino-2-substituted-pen-2-em-3-carboxylic acid Disclosed are 6-substituted amino-2-substituted-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein R1 is hydrogen or acyl, R2 is hydrogen or methoxyl, and R3 is, inter alia, hydrogen, --R, --OR, ... | 03/10/1981 |
| 4185015 | Methoxymethyl 6-[D-2,2-dimethyl-4-(4-hydroxyphenyl)-5-oxo-1-imidazolyl]penicillanate There is disclosed a process for preparing methoxymethyl 6-aminopenicillanate, its conversion to methoxymethyl amoxicillin and the use of the latter compound as an intermediate in the preparation of the methoxymethyl ester of p-hydroxyhetacillin which is ... | 01/22/1980 |
| 4155905 | 6-Substituted penicillanic acid and derivatives thereof Disclosed herein are penicillanic acids and derivatives thereof which are substituted in the 6-position, processes for preparing such compounds and the utility thereof. The compounds of the invention have been found to be useful as antibacterial agents.... | 05/22/1979 |
| 4102882 | Process to prepare novel antibiotic compounds A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-acylaminocephalosporin, or 6-acylaminopenicillin, then the latter compounds are treated with an organolithium compound, followed with t-butyl-hypoc... | 07/25/1978 |
| 4082745 | Process for the preparation of phosphorus derivatives of secondary ammonium salts of penam and cephem compounds An improvement in the conversion of penam and cephem compounds to secondary ammonium salts of phosphite amides thereof by reacting as follows: ##STR1## wherein --R, is the non-reacting balance of the penam or cephem compound and ##STR2## AR... | 04/04/1978 |
| 4081443 | Penicillin oxides Compounds of the formula: ##STR1## (where COB is carboxy or protected carboxy and X is hydrogen or nucleophilic group) preparable by oxidation of the corresponding N-nitrosopenicillin derivatives are useful as starting materials for synthesizing know... | 03/28/1978 |
| 4081546 | 3-Substituted aminocycloalkyl esters of penicillin antibiotics A class of substituted aminocycloalkyl esters of penicillins have improved pharmacokinetic properties and are hydrolysed to the antibacterially active penicillin.... | 03/28/1978 |
| 4072710 | Process for preparing acid chlorides A process for preparing acid chlorides, wherein a silyl ester having an aliphatic, aromatic, alkanoaromatic or heterocyclic group which may support substituents, and having a low molecular weight alkyl or phenyl group is reacted with thionyl chloride in a... | 02/07/1978 |
| 4070477 | 2-Penem compounds The invention relates to 6-amino-2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R1a denotes hydrogen or an amino protective group R1A and R1b represents hydrogen ... | 01/24/1978 |
| 4062842 | Method for preparing 7-substituted cephalosporins and 6-substituted penicillins by replacement of sulfur-containing groups Disclosed is a method for replacing 7-lower alkylthio and 7-arylthio groups from cephalosporins with lower alkanoyloxy,lower alkoxy, aryloxy, aroyloxy, amino, lower alkylamino and azido moieties, and for replacing 6-lower alkylthio and 6-arylthio groups f... | 12/13/1977 |
| 4036829 | Lactonyl esters of penicillins Lactonyl esters of Penicillins of the formula ##STR1## WHEREIN R1 is an antibacterially active penicillin-completing side chain; R is hydrogen, methyl or phenyl; and Ra, Rb, Rc, Rd are hydrogen, lower alkyl, lower alkoxy, halo, and nitro, ... | 07/19/1977 |
| 4035359 | 6, ଲ-Substituted penicillin derivatives Novel 6-methoxy and 6-thioalkyl-6-acylamido-penicillanic acids and their non-toxic pharmaceutically-acceptable salts, esters and amides which are useful as antibiotics. The products are prepared by treating an ester of 6-substituted-6-aminopenicillanic ac... | 07/12/1977 |
| 4000129 | 6-Aminopenicillanic acid sulfoxide silyl esters Novel 6-substituted amino-penicillanic sulfoxide silyl esters useful as intermediates for the preparation of 7-aminodesacetoxycephalosporanic acids derivatives.... | 12/28/1976 |
| 3997532 | Intermediates for producing semi-synthetic cephalosporins Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a... | 12/14/1976 |
| 3980793 | Carbonate esters of penicillins and compositions and methods for treatment of bacterial infections New carbonate esters of penicillins, having the formula ##EQU1## wherein R.sup. 1 is substituted or unsubstituted alkyl, alkenyl, aryl, aryloxy or heterocyclic group, R2 is ##EQU2## in which formula R3 is H or -CH3 | 09/14/1976 |
| 3965093 | 6-Arylthio penicillanic acid and derivatives thereof Disclosed herein are penicillanic acids and derivatives thereof which are substituted in the 6-position, processes for preparing such compounds and the utility thereof. The compounds of the invention have been found to be useful as antibacterial agents.... | 06/22/1976 |