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| Number | Title | Issue Date |
| 7728126 | Purification of beta-lactam products Method for purifying 7α-methoxy-cephalosporins containing as impurity the corresponding 7α-methylthio analogue, which is transformed into its methoxy analogue by treatment with a halogenating agent in methanol. In this way the complete conversion of the sulphurate... | 06/01/2010 |
| 7705142 | Process for the preparation of cefixime There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and wate... | 04/27/2010 |
| 7662955 | Process for the preparation of cefoxitin A process for the preparation of cefoxitin of formula (I) The process includes treating the compound of formula (II) with a halogenating agent in an organic solvent, followed by t... | 02/16/2010 |
| 7605256 | Process for preparing sodium cefoxitin Cefalotin is methoxylated in position 7α, desacetylated and then carbamoylated in position 3, to provide acid cefoxitin without any isolation of intermediate products. The acid cefoxitin is then transformed into the sodium salt by means of ion exchange resin. ... | 10/20/2009 |
| 7071330 | Process for carbapenem synthesis A process for synthesizing a compound represented by formula I: or a pharmaceutically acceptable salt thereof, wherein deprotection is conducted using a prereduced metal catalyst is disclosed. ... | 07/04/2006 |
| 7022503 | Process for the stereoselective preparation of functionalized vicinal diols The present invention relates to a process for the kinetic resolution of racemic functionalized epoxides in the presence of microorganisms, crude or pure preparations thereof comprising a polypeptide having epoxide hydrolase activity. Preferred microorganisms are ye... | 04/04/2006 |
| 6906054 | Compositions for inhibiting beta-lactamase The invention provides pharmaceutical compositions comprising compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and ... | 06/14/2005 |
| 6303592 | 7-alkylidene cephalosporanic acid derivatives and methods of using the same Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of ଲ-lactamase enzymes.... | 10/16/2001 |
| 6288086 | N-hydroxy-2-(alkyl, aryl, or heteroaryl, sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenase... | 09/11/2001 |
| 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 |
| 6001997 | Cephalosporins and homologues, preparations and pharmaceutical compositions ଲ-Lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy or formamido; R2 is an acyl group; CO2 R3 is a carboxy group or a carboxylate anion, or R3 is a readily rem... | 12/14/1999 |
| 5929233 | Cyclization for preparing halo-cephems The invention provides a process for preparing an allenyl ଲ-lactam of formula (4), by reacting the hydroxyl group of a ଲ-lactam of formula (1) with a reactive derivative of sulfonic acid of formula (2) to convert the compound of formula (1) to... | 07/27/1999 |
| 5856474 | Cephalosporin synthesis Cephalosporin derivatives of formula ##STR1## wherein R1 signifies hydrogen or a silyl protecting group, processes for their production and their use as intermediate products.... | 01/05/1999 |
| 5840885 | Processes for the production of 6--aminoacyl-penicillin and 7-.alpha . A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a derivative thereof in a halogen-free solvent.... | 11/24/1998 |
| 5804577 | Cephalosporin derivatives The present invention relates to compounds of formula I ##STR1## wherein R1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily hydroyzable esters thereof, pharmaceutically ... | 09/08/1998 |
| 5750684 | Process for the preparatin of ଲ-lactam compounds The present invention provides a process for the substitution of an acylamino ଲ-lactam compound at the carbon atom carrying the acylamino group, which process comprises reacting the ଲ-lactam compound with an halogenating agent and a nucleophil... | 05/12/1998 |
| 5719276 | Beta lactam production A new process is described for the production of 6-alpha-amino-penicillins and 7-alpha-amino-desacetoxy-cephalosporins free from halogen-containing solvents by acylating 6-APA, 7-ADCA or a derivative thereof in a halogen-free solvent.... | 02/17/1998 |
| 5693791 | Antibiotics and process for preparation A group of reagents, as diisocyanates, dianhydrides, diacidchlorides, diepoxides, carbodiimides and the like are utilized to link a wide variety of antibiotic moities, reacted two at a time with said reagents, the said antibiotic moieties containing group... | 12/02/1997 |
| 5686604 | Cephalosporines The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of formula ##STR1## wherein R is hydrogen, a negative charge... | 11/11/1997 |
| 5683996 | 4-thia-1-aza-bicyclo4,2,0!oct-2-ene antibiotics A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and Rb --NH--, Ra is an organic radical, Ri and Rj are individually selected from the grou... | 11/04/1997 |
| 5648346 | Antimicrobial carbacephem-quinolones A substantially flat collapsed plastic bag with an evacuation form unit insert positioned therein as manufactured to serve as a form about which the filled bag will collapse as it is emptied. The form unit comprises a ring for mounting the unit on the spo... | 07/15/1997 |
| 5644052 | Process for the production of cephalosporines and novel intermediates in this process The invention relates to a new economical and simple process, using a new intermediate compound, for the production of 3'-substituted 7-amino-3-propenyl-4-cephem-carboxylic acid derivatives of formula ##STR1## wherein R is hydrogen, a negative charge... | 07/01/1997 |
| 5639877 | Intermediates in the synthesis of cephalosporins Novel amidine salts of 7-Amino-3-hydroxymethyl-3-cephem-4-carboxylic acid (=HACA), particular guanidine and diaza-bicyclo-alkylene salts, are useful as intermediates in the synthesis of cephalosporins.... | 06/17/1997 |
| 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 |
| 5631367 | E-rotamers of 3-hydroy cephem derivatives A process for the manufacture of 7-acylamino-3-hydroxy-cephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with ozone in an inert organic solvent in the presence of... | 05/20/1997 |
| 5629306 | 7-alkylidene cephalosporanic acid derivatives and methods of using the same Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of ଲ-lactamase enzymes.... | 05/13/1997 |
| 5602117 | Cephalosporin compounds ଲ-lactam antibiotics of formula (I) or a salt thereof, wherein R1 is hydrogen, methoxy of formamido; R2 is an acyl group, in particular that of an antibacterially active cephalosporin; CO2 R3 is a carboxy ... | 02/11/1997 |
| 5597817 | 7-vinylidene cephalosporins and methods of using the same Cephalosporins with an exocyclic allene in the 7-position and their pharmaceutically active salts are potent inhibitors of ଲ-lactamases and are therefore useful in the treatment of penicillin resistant infections.... | 01/28/1997 |
| 5530116 | Antimicrobial quinolonyl lactams Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A1, A2, A3, R1, and R4 generally form any of a v... | 06/25/1996 |
| 5523400 | Cephalosporin antibiotics The present invention relates to compounds of the formula ##STR1## wherein R1 is an acyl group derived from a carboxylic acid, hydrogen, or an amino protecting group; R2 is hydrogen, hydroxy, lower alkyl-Qp -, cycloalkyl, ... | 06/04/1996 |
| 5514561 | Fluorogenic and chromogenic ଲ-lactamase substrates Chromogenic and fluorogenic substrates for ଲ-lactamase, methods for synthesis thereof and methods for detecting ଲ-lactamase in a sample are provided. The substrates are substantially colorless or substantially nonfluorescent ଲ-lactam com... | 05/07/1996 |
| 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 |
| 5446037 | 2-[(substituted) methylene]cephalosporin sulfones as antiinflammatory, antidegenerative and antithrombin agents This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as well as effective thrombin inhibitors and therefore are use... | 08/29/1995 |
| 5412093 | 3-heterocyclic thiomethyl cephalosporins Cephalosporin compounds having a 3-position substituent of the formula (I) are described: --CH2 --S--Q--(Y)n --P wherein Q is a 5- or 6-membered heterocyclic ring, P is a benzene ring substituted by groups R1 and R2 ... | 05/02/1995 |
| 5410044 | Process for preparing Z and E-rotamers of 3-hydroxy cephem derivatives A process for the manufacture of 7-acylamino-3-hydroxycephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with ozone in an inert organic solvent in the presence of ... | 04/25/1995 |
| 5397779 | Cephalosporins A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R1, Rc, Rb, A and A' are defined as in the following specification and their ... | 03/14/1995 |
| 5385897 | 4-thia-1-aza-bicyclo[4,2,0]oct-2-ene derivatives A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of ##STR2## and Rb --NH--, Ra is an organic radical, Ri and Rj are individually selected from the grou... | 01/31/1995 |
| 5366970 | Cephem compounds and pharmaceutically acceptable salts thereof The invention relates to a compound of the formula: ##STR1## of antimicrobial activity.... | 11/22/1994 |
| 5364848 | Substituted cephalosporin sulfones as anti-inflammatory and antidegenerative agents New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.... | 11/15/1994 |
| 5359057 | Acylation of amines 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 especiall... | 10/25/1994 |
