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| Number | Title | Issue Date |
| 7241885 | Process for the isolation of crystalline imipenem The present invention relates to a cost effective and industrially advantageous process for the preparation of imipenem of high purity comprising the steps of treating an aqueous solution containing imipenem with an organic solvent, wherein the imipenem is not lyoph... | 07/10/2007 |
| 6903211 | Process for the preparation of 3-propenyl cephalosporin DMF solvate The present invention relates to an improved process for the preparation of cefprozil DMF solvate of formula (I), which is useful for the preparation of cefprozil, comprising: i) reac... | 06/07/2005 |
| 6232305 | Substituted amino bicyclic-ଲ-lactam penam and cepham derivatives as cysteine protease inhibitors The present invention provides substituted amino bicyclic-ଲ-lactam penam derivatives and substituted amino bicyclic-ଲ-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of... | 05/15/2001 |
| 6127355 | High molecular weight polymer-based prodrugs The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; (n) is zero (0) or a positive integer, preferably from 1 to ... | 10/03/2000 |
| 6107481 | De-esterification process A process to prepare the E isomer of a 3-substituted (6R,7R)-7-phenyl-acetamido-ceph-3-em-4-carboxylic acid from a mixture of the E and Z-isomer of either the corresponding tert-butyl or the corresponding 4-methoxybenzyl ester of a 3-substituted (6R,... | 08/22/2000 |
| 6015808 | Synthesis of pharmaceutical compositions with lactams and ଲ-lactams/oxo thia azabicyclo compounds Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and ଲ-lactam compo... | 01/18/2000 |
| 5955458 | Penicillin glycolate New solvates of penicillin, in particular amoxycillin glycolate has been provided for together with a simple one-step process to prepare the same.... | 09/21/1999 |
| 5922861 | De-esterification process An efficient process for de-esterification has been provided for by application of special tetrahalogenides. By applying this process a new compound, viz. cefesone, and especially the E-isomer thereof, has been prepared.... | 07/13/1999 |
| 5880111 | Therapeutic derivations of diphosphonates Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeut... | 03/09/1999 |
| 5854227 | Therapeutic derivatives of diphosphonates Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are obtained by combining chemically a diphosphonate compound wit... | 12/29/1998 |
| 5821362 | Method of desilylating silylether compounds Method of desilylating a silylether compound by reacting a silylether compound of the general formula (I): ##STR1## or a salt thereof with an amine hydrogen fluoride salt or a pyridine hydrogen fluoride salt in an organic solvent to produce a compoun... | 10/13/1998 |
| 5801242 | Process for making quinolonyl lactam antimicrobials and novel intermediate compounds The present invention provides processes for making compounds of the structure (Q--L1)--L--(L2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L1, and L2 together comprise a linking moiet... | 09/01/1998 |
| 5644053 | Penam derivatives The present invention discloses compounds having the formula ##STR1## wherein one of R1 and R2 is --COR4, --CN, --CH2 R5, halogen, --CH.dbd.CHR6 or Q and the other is hydrogen or lower... | 07/01/1997 |
| 5637580 | Antimicrobial penem-quinolones Compounds of structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzables esters, and hydrates thereof, are effective antiinfective agents, useful in treating and preventing infection.... | 06/10/1997 |
| 5474993 | Lactam inhibitors of cholesterol esterase The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R1 is H or C1-6 alkyl; R2 is H or C1-6 alkyl; R3 is H or C... | 12/12/1995 |
| 5387578 | New linker for bioactive agents Conjugate of general formula 1: [A--O--W-Z]a -T 1 wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is... | 02/07/1995 |
| 5300497 | Penam derivatives and salts thereof, process for producing the same and antibacterial agent comprising the same A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R1 represents a hydrogen atom, an amino-protecting group or an acyl group; R2 represents a hydrogen atom or a lower alkyl group;... | 04/05/1994 |
| 5281703 | Process for making antimicrobial quinolonyl lactams The present invention provides methods of making compounds of the structure [Q-L1 ]-L-[L2 -B[ wherein (I) Q is a quinolone moiety; (II) B is a beta-lactam moiety; (III) L, L1, and L2 together comprise a carbamate-containing ... | 01/25/1994 |
| 5185330 | Penam derivatives and salts thereof, and antibacterial agent comprising the same A penam derivative represented by the following general formula or a salt thereof: ##STR1## wherein R1 represents a hydrogen atom, an amino-protecting group or an acyl group; R2 represents a hydrogen atom or a lower alkyl group;... | 02/09/1993 |
| 5132300 | Beta-lactam elastase inhibitors Novel beta lactam compounds having potent elastrase inhibition activity are disclosed. These compounds are characterized by the general structural formulae I, II, and III: ##STR1## These compounds are further characterized such that X and Y are each ... | 07/21/1992 |
| 5053502 | Anhydro penicillin derivatives There is disclosed a compound represented by the formula ##STR1## where P is a hydroxy protecting group.... | 10/01/1991 |
| 5008257 | Brain-specific drug delivery The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are: (a) compounds of the formula [D-DHC] (I) wherein [D] is a centrally acting drug ... | 04/16/1991 |
| 4933444 | Process for preparing 2ଲ-substituted-methylpenicillin derivatives Disclosed is a process for preparing 2ଲ-substituted-methylpenicillin derivative of the formula ##STR1## wherein R is H or carboxyl protecting group, R1 is H or halo, R2 is H, lower alkyl, lower alkoxy, halogen, azido, lowe... | 06/12/1990 |
| 4877783 | ଲ-lactam antibacterial agents ଲ-Lactam antibiotics having an -formamido substituent on the carbon atom adjacent to the carbonyl group of the ଲ-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes fo... | 10/31/1989 |
| 4861768 | 2 ଲ-substituted thiomethylpenicillin derivatives and their preparation and use Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R1 is a hydrogen atom, a lower ... | 08/29/1989 |
| 4767853 | Synthesis of 1-(allyloxycarbonyl)-methyl-3-(hydroxyethyl)-4-beta-naphthoxythiocarbony lthio-2-azetidinones and hydroxy protected analogs thereof A multi-step stereospecific process for preparing (3S,4R,5R)-1-(allyloxycarbonyl)-methyl-3-(1-hydroxyethyl)-4-beta-naphthoxy thiocarbonylthio-2-azetidinones, stereoisomers thereof or hydroxy protected analogs thereof from anhydropenicillin. The azetidinone... | 08/30/1988 |
| 4675186 | 6-(1-acyl-1-hydroxymethyl)penicillanic acid derivatives 6-(1-Acyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.... | 06/23/1987 |
| 4668514 | Penicillin derivatives This invention provides a penicillin derivative of the formula ##STR1## wherein R1 and R2 are the same or different and represent hydrogen, C1-6 alkyl, C1-6 hydroxyalkyl, C3-9 acyloxyalkyl, C | 05/26/1987 |
| 4663451 | Process for the synthesis of penems and penams Described is a novel process for the preparation of penams and penems useful as antibacterial agents, which comprises the reaction of an appropriate 4-substituted-azetidin-2-one with a base, followed by reaction of the thereby formed penam compound with a... | 05/05/1987 |
| 4654331 | Oral absorption enhancement of carboxylic acid pharmaceuticals using (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl ester group 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 ... | 03/31/1987 |
| 4639335 | Stereocontrolled acetoxyazetidinone process A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl... | 01/27/1987 |
| 4596677 | Anhydropenicillin intermediates A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl... | 06/24/1986 |
| 4431658 | Aza penem compounds Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline ... | 02/14/1984 |
| 4304779 | 6-(Nitrogen-containing heterocyclic)hydroxymethylpenicillanic acids, compounds related thereto and processes for their preparation 6-(Heterocyclic)hydroxymethylpenicillanic acids and compounds related thereto are prepared by reaction of a 6,6-dihalopenicillanic acid with a Grignard reagent and a heterocyclic aldehyde in an anhydrous aprotic solvent. The compounds possess useful antib... | 12/08/1981 |
| 4272439 | 6-(Substituted-hydroxymethylene penams) ଲ-Lactams having a substituted hydroxymethylene group at the position to the lactam carbonyl group are prepared by reaction of an -halo-ଲ-lactam with zinc or zinc amalgam in an anhydrous aprotic medium to produce an intermediate... | 06/09/1981 |
| 4172832 | Mercaptoalcohols and process for their manufacture The invention concerns 3-amino-4-(2-hydroxyethylthio)-2-oxo-azetidine compounds of the formula ##STR1## wherein R1a represents hydrogen or an amino protective group R1A, R1b represents... | 10/30/1979 |
| 4136096 | 6-Amino-2,2-dimethyl-3-(5-tetrazolyl)penam process and intermediates therefor 6-Amino and 6-(N-protected amino)-2,2-dimethyl-3-cyanopenams, intermediates therefor, and a process for the conversion of the 3-cyano penams, by reaction with a source of azide ion in a reaction inert solvent, to 6-amino-and 6-(N-protected amino)-2,2-dime... | 01/23/1979 |
| 4105668 | Process for 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam Certain 6-amino-2,2-dimethyl-3-(1-substituted tetrazol-5-yl)penam and 6-(protected amino)-2,2-dimethyl-3-(1-substituted tetrazolyl-5-yl)penam compounds react with hydrogen fluoride to produce 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, a useful intermedia... | 08/08/1978 |
| 4081455 | 6-Amino-2,2-dimethyl-3-cyanopenams 6-AMINO AND 6-(N-protected amino)-2,2-dimethyl-3-cyanopenams, intermediates therefor, and a process for the conversion of the 3-cyano penams, by reaction with a source of azide ion in a reaction inert solvent, to 6-amino-and 6-(N-protected amino)-2,2-dime... | 03/28/1978 |
| 4036846 | 3-Hydroxy and 3-acetoxy-6-triphenyl-methylaminopenams The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reac... | 07/19/1977 |
