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Class 514/201 - 7,7-di-substituted


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo octane ring system contains
No. of patents: 163
Last issue date: 03/11/2008


1          
NumberTitleIssue Date
7341993Cross-linked glycopeptide—cephalosporin antibiotics
This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacteria...
03/11/2008
7279487Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
Hydroxynaphthyridinone carboxamides of formula: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein L, R1a, R1b, R1c, R2a, R2b
10/09/2007
7262183Substituted 5-membered n-heterocyclic compounds and their uses for treating or preventing neurodegenerative diseases
This invention relates to substituted 5-membered N-Herterocyclic neurotrophic compounds of formula (I) or pharmaceutically acceptable salts or hydrates thereof, wherein R1, R2, R3, R4, V, W, X, Y, and Z are as defined in t...
08/28/2007
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
6613807Therapeutic polyanhydride compounds for drug delivery
Polyanhydrides which link low molecular weight drugs containing a carboxylic acid group and an amine, thiol, alcohol or phenol group within their structure into polymeric drug delivery systems are provided. Also provided are methods of producing polymeric...
09/02/2003
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
6489319Neurotherapeutic use of carboxypeptidase inhibitors
Administration of inhibitors of carboxypeptidase E provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition. Certain ଲ-Lactam antibiotics, most signif...
12/03/2002
6486214Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby
Polyanhydrides which link low molecular weight drugs containing a carboxylic acid group and an amine, thiol, alcohol or phenol group within their structure into polymeric drug delivery systems are provided. Also provided are methods of producing polymeric...
11/26/2002
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
6013647Benzoxazinedione 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
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
5994086Method for assessing infertility by binding of mannose to sperm cells
Methods for labeling mannose lectins on the surface of mammalian sperm cells are described, and methods of categorizing and quantifying the numbers of cells exhibiting particular labeling patterns are also provided. These methods provide ways of detecting...
11/30/1999
56815637-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....
10/28/1997
5663162Cephem derivatives
Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted imidazo[5,1-b]thiazolium-6-yl as a substituent at the 3-position of the cephem ring: ##STR1## wherein X represents CH or N, R
09/02/1997
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
5602117Cephalosporin 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
55978177-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
5514561Fluorogenic 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
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
5436250Isatineoxime derivatives, their preparation and use
A compound having the formula ##STR1## wherein R4 and R5 independently are hydrogen, halogen, CF3, CN, NO2 or SO2 NR1 R2 wherein R1 is hydrogen or C1-6 -alk...
07/25/1995
5409917Topical treatment of acne with cephalosporins
A method and composition for topically treating acne and acneiform dermal disorders includes applying an amount of a cephalosporin antibiotic effective to treat the acne and acneiform dermal disorders. The antibiotic is blended with a carrier suitable for...
04/25/1995
5364848Substituted 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
5348951Cephalosporins
Cephalosporin compounds having a 3-position substituent of the formula (I) are described, --CH2 --Y--Q (I) wherein Y is a bond or a linking group --NR4 --Y'--, --O--Y'--, --S--Y'-- wherein R4
09/20/1994
5312813Biofilm reduction method
A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated...
05/17/1994
5275816Cephalosporin derivatives
7 ଱-formamido cephalosporin derivatives having a 3[N-(optionally substituted)aminothiopyridinium thiomethyl] substituent have anti-bacterial activity and are of use in anti-bacterial therapy. Processes for the preparation thereof and intermediates f...
01/04/1994
52644292-spirocyclopropyl cephalosporin sulfone derivatives
Derivatives of 2-spirocyclopropyl cephalosporin sulfone of the structural formula I ##STR1## are provided which are useful as potent elastase inhibitors....
11/23/1993
52624103-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 ...
11/16/1993
52583772-spirocyclopropyl 4-acylcephems
Derivatives of 2-spirocyclopropyl 4-acylcephem sulfones of the formula (I) ##STR1## are provided which are useful as potent elastase inhibitors and hence are useful in the prevention, control and treatment of inflammatory conditions, especially arthr...
11/02/1993
5246926Cephalosporin derivatives
ଲ-Lactam compounds of the formula (Ia) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R1 is hydrogen, methoxy or formamido; ...
09/21/1993
5232918Cephalosporin derivatives
Cephalosporin derivatives having a 3-position substituent of formula I are described: ##STR1## wherein R1 is hydrogen, alkenyl or optionally substituted alkyl, Het is a 5- or 6-membered heterocyclic ring bonded via a carbon atom to the ...
08/03/1993
5219848Cephem compounds
Cephalosporin antibiotics having a 3-position substituent of the formula: ##STR1## are described, wherein X is --CO--, --SO2 -- or --COCH2 --; Y is --CO--, --SO2 -- or --CH2 --; Q is a benzene, pyridine or ...
06/15/1993
5214037Thioalkylthio cephalosporin derivatives
A novel thioalkylthio cephalosporin antibiotic compound of formula I: ##STR1## wherein Acyl is C1 -C12 acyl; Het is optionally substituted monocyclic heteroaromatic group containing one or more hetero atoms; R1 is a s...
05/25/1993
5190748Absorption enhancement of antibiotics
The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C6 to C18
03/02/1993
5158946Cephalosporin derivatives and pharmaceutical compositions
ଲ-Lactam compounds of the formula (I) including pharmaceutically acceptable salts and in vivo hydrolysable esters, processes for their preparation and their use as antibiotics: ##STR1## wherein R1 is hydrogen, methoxy or formamido; R...
10/27/1992
5147871Anti-bacterial cephalosporin compounds
There are presented anti-bacterial cephalosporins having broad antimicrobial activity of the formula ##STR1## wherein R1 is an antibiotically active quinolonyl; R2 is selected from the group consisting of hydrogen, lower alkoxy,...
09/15/1992
5143910Piperaziniocephalosporins
Antibacterial hydroxyarylpiperazinocephalosporins of the formula: ##STR1## wherein R1 is amino or acylamino; R2 is H or methoxy; R3 is alkyl; R4 is --(P--C--Q)n --, where P and Q each are H, alkyl or ...
09/01/1992
5134138Phenacylpyridiniothiocephalosporins
An antibacterial 3-vic-dihydroxyaroylmethylpyridiniothiomethyl cephalosporin (I) and its salts represented by the following formula: ##STR1## (wherein, R1 is amino group or acylamino; R2 is hydrogen or methoxy; R3 is ...
07/28/1992
5132301Substituted cephalosporin sulfones as anti-inflammatory and anti-degenerative agents
New substituted cephalosporin sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents....
07/21/1992
5114933Cephalosporin compounds
Cephalosporin compounds having a 3-position substituent of the formula (I) are described: --CH2 --Y--Q (I) wherein Y is a bond or a linking group --NR4 --Y'--, --O--Y'--, 13 S--Y'-- wherein R4...
05/19/1992
5106842Antibiotic C-3 cyclobutenedione substituted (1-carba)cephalosporin compounds, compositions, and methods of use thereof
A compound of formula I ##STR1## wherein X is sulfur or CH2 ; R1 is hydrogen, hydroxy, amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, phenyl optionally substituted with one to three C1-6
04/21/1992
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