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Class 514/204 - 3-position substituent contains sulfur


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a substituent in 3-position of the
No. of patents: 159
Last issue date: 04/20/2010


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NumberTitleIssue Date
7700581Cephalosporin compounds comprising a C3 thio-methyl moiety substituted with N-containing heterocyclic group, and a C7 thiourea acetamido group, their preparations and uses thereof
Disclosed herein are a cephalosporin compound of formula I, wherein R1 is selected from the following groups:
04/20/2010
7282221Antiviral product, use and formulation thereof
An antiviral product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antiviral product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosag...
10/16/2007
7128897Aerosolized anti-infectives, anti-inflammatories, and decongestants for the treatment of sinusitis
Pharmaceutical compositions are described that contain one agent for treatment of sinusitis and a surfactant. The compositions are prepared to have a surface tension that renders the composition effective for treatment of sinusitis. ...
10/31/2006
7071329Process for preparing cephalosporins with salified intermediate
Cephalosporins may be conveniently prepared by a process in which a benzathinium salt of formula (V) wherein: Z is benzathine; and X and R2 are as defined in the spec...
07/04/2006
69168017-Alkylidene-3-substituted-3-cephem-4-carboxylates as β-lactamase inhibitors
The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting β...
07/12/2005
6906054Compositions 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
6846492Use of phenylethylamine derivatives for the antimicrobial treatment of surfaces
The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20a...
01/25/2005
67237167-acylamino-3-heteroarylthio-3-cephem carboxylic acid antibiotics and prodrugs thereof
The present invention relates to a cephem prodrug having formula III or formula IV: or a pharmaceutically acceptable salt thereof, wherein R′1 is selected from the group consisting of hydrogen and —C(O)CH(...
04/20/2004
6599893Cephalosporin antibiotics and prodrugs thereof
The present invention relates to chemical compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof. R1 is selected from the group consisting of: ##STR2## R2 is selected from the group consisting of hydroge...
07/29/2003
65998927-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....
07/29/2003
6583133Propenyl cephalosporin derivatives and process for the manufacture thereof
Disclosed are cephalosporin derivatives of the general formula ##STR1## wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfu...
06/24/2003
6531465Antibacterial cephalosporins
A compound of formula ##STR1## wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent....
03/11/2003
6414002Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure ##STR1## wherein Q is C or N, A is 0 or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein...
07/02/2002
6407091ଲ-lactamase inhibiting compounds
The invention provides compounds of formula I and IV: ##STR1## wherein R1 -R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ଲ-lactamase enzyme...
06/18/2002
6329363Cephalosporin antibiotics
The invention provides new fluorinated cephalosporin antibiotics and methods of preventing or treating infection, particularly mastitis in ruminants, using these antibiotics, and veterinary and pharmaceutical formulations comprising these antibiotics....
12/11/2001
6319904Formulation comprising antibacterial substance and antiulcer substance
The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present inv...
11/20/2001
63035927-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
6159706Application of enzyme prodrugs as anti-infective agents
The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate these drugs locally, and to overcome the resistance phenotyp...
12/12/2000
6150351Cephem compounds and pharmaceutical use thereof
This invention relates to new cephem compound represented by the following general formula (I): ##STR1## wherein each symbol is as defined in the specification or a salt thereof, which has antimicrobial activity against Helicobacter pylori, and are ...
11/21/2000
6090801Pharmaceutical compositions containing ceftriaxone and penems
Pharmaceutical formulations comprising ceftriaxone in combination with a penem of formula (I) in which R1 is hydrogen or an organic group; R2 is a ring system of formula (II), wherein R4 and R5 are hydrogen or o...
07/18/2000
6087355Cephalosporin antibiotics
The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R99 is selected from the group consisting of sulfur, SO, SO2, NH, N-a...
07/11/2000
6066630Cephalosporin antibiotics
The present invention includes novel compounds of formula ##STR1## where R99 is selected from the group consisting of sulfur, SO, SO2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R12 is ##STR2##...
05/23/2000
6030965Cephalosporin antibiotics
The present invention includes novel compounds of formula where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R99 is selected from the group consisting of sulfur, SO, S02, NH, N-alkyl, oxygen, ...
02/29/2000
6025352Cephalosporin antibiotics
The present invention includes novel compounds of formula ##STR1## where G, H, J, L and M are carbon or nitrogen, R99 is selected from the group consisting of sulfur, SO, SO2, NH, N-alkyl, oxygen, C.tbd.C (cis or trans), and C.t...
02/15/2000
5994340Azetidinone derivatives as ଲ-lactamase inhibitors
New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial ଲ-lactamases. T...
11/30/1999
5945414Process for the preparation of new intermediates useful in the synthesis of cephalosporins
Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II): R--SH (II) wherein R is 5-me...
08/31/1999
5728691Quinolonylcarboxamidocephalosporin derivatives and pharmaceutical compositions containing them
Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are descr...
03/17/1998
5710146Cephem derivatives and processes for their manufacture
Cephem derivatives of the general formula ##STR1## in which the R2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds....
01/20/1998
5705496Crystalline benzathine salt of cefonicid and its preparation
The present invention relates to benzathine salts of cefonicid, a member of the cephalosporin family of antibiotics, which are crystalline. ##STR1##...
01/06/1998
5698547Cephalosporin antibiotics
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistan...
12/16/1997
5698544Cephem compound, process for producing the compound, and antimicrobial composition containing the same
The present invention provides a cephem compound having a high antimicrobial activity against various pathogenic bacteria. The cephem compound of the invention is represented by the formula ##STR1## wherein Q represents CH or N, R1 represents a...
12/16/1997
5635501Alphalosporins and 1-carba-1-dethia cephalosporins
Compound of formula (I) or salts 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 removable carboxy prote...
06/03/1997
56293067-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
5593986Cephalosporin antibiotics
The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistan...
01/14/1997
55873732-acyloxycephem derivatives
The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical; R1...
12/24/1996
55808652,2-disubstituted cephem sulphones
The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R1 is hydrogen, halogen or an optionally substituted C1
12/03/1996
5571804Cephalosporin antibiotics
Cephalosporin compounds of formula (I): ##STR1## wherein: R1 is a hydrogen or an amino protecting group; R2 and R3 are, independently, a hydrogen or a hydroxy protecting group, or form together a cyclic diol protecting gro...
11/05/1996
54460372-[(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
54399042-spiro(2'-spirocycloalkyl)cyclopropyl cephalosporin sulfones as antiinflammatory and antigenerative agents
2-spiro (2'-spirocycloalkyl) cyclopropyl cephalosporin sulfone compounds, methods of treating patients for elastase inhibition, and processes for preparing such compounds....
08/08/1995
53730007Beta-(thiadiazolyl)-2-iminoacetamido-3cephem compounds
A cephalosporin derivative represented by the formula: ##STR1## wherein R1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R2 and R3 are the same or differ...
12/13/1994
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