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Class 548/232 - 4- or 5-position substituent contains chalcogen


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the substituent on the 4- or 5-position
No. of patents: 175
Last issue date: 08/26/2008


1          
NumberTitleIssue Date
7417156Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers
In only two steps and in 65% overall yield, natural trioxane artemisinin (I) was converted on gram scale into C-10-carba trioxane dimer (3). This new, very stable dimer was then transformed easily in one additional step into four different dimers (4-7). Alcohol and ...
08/26/2008
7358254Method for treating atherosclerosis employing an aP2 inhibitor and combination
A method is provided for treating atherosclerosis and related diseases, employing an aP2 inhibitor or a combination of an aP2 inhibitor and another antiatherosclerotic agent, for example, an HMG CoA reductase inhibitor such as pravastatin. ...
04/15/2008
7348342Heterocyclic compounds process for their preparation and pharmaceutical compositions containing them and their use in medicine
We describe substituted benzenesulfoximine compounds having anti-inflammatory activity, processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of inflammatory diseases. ...
03/25/2008
7259263Method of synthesis of azole-containing amino acids
The invention relates to methods of synthesizing 2-substituted azole compunds of formula (I): The invention is also relates to compounds of formula (I) and to intermediate compounds in the synthesis method. ...
08/21/2007
7217726Antibacterial agents
The present invention provides novel compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically a...
05/15/2007
7193103Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using oxazolidinone derivatives
Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester by treating N-(3,3-dimethylbutyl)-L-aspartic acid with ketones to give oxazolidinone derivatives, which are condensed with L-phenylalanine methyl ester. ...
03/20/2007
7126005Process for preparing florfenicol
The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (...
10/24/2006
7091196Bifunctional heterocyclic compounds and methods of making and using same
The invention provides a family of compounds useful as anti-infective agents and/or anti-proliferative agents, for example, chemotherapeutic agents, anti-fungal agents, anti-bacterial agents, anti-parasitic agents, anti-viral agents, and/or anti-inflammatory agents,...
08/15/2006
7005441Compositions that bind antiterminator RNA and assay for screening such compositions
Compounds that are selective binding agents specific for RNA secondary and tertiary structures and a fluorescence assay for detecting the binding of small molecules to T-box antiterminator model mRNAs. The compounds include novel tri-substituted oxazolidinones and a...
02/28/2006
7002020Oxazolidinone combinatorial libraries, compositions and methods of preparation
Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutica...
02/21/2006
6927229Difluorothioacetamides of oxazolidinones as antibacterial agents
The present invention describes difluororthioacetamide oxazolidinones of formula I: R is —CH2— or —CH2CH2—; R2 and R3 are independently —H or —F; X is ...
08/09/2005
68699682-(3H)-oxazolone derivatives and their use as COX-2 inhibitors
The invention relates to 2-(3H)-oxazolone derivatives. They may be used as COX-2 inhibitors. The compounds may be used in the treatment of colorectal cancer. ...
03/22/2005
6852875Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using oxazolidinone derivatives
Synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester by treating N-(3,3-dimethylbutyl)-L-aspartic acid with ketones to give oxazolidinone derivatives, which are condensed with L-phenylalanine methyl ester. ...
02/08/2005
6743811Oxazalidinone compounds and methods of preparation and use thereof
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readil...
06/01/2004
6699995Process for the preparation of oxazole derivatives
A production method of a compound represented by the formula ##STR1## wherein R1 and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R3 is an electr...
03/02/2004
6617339Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described....
09/09/2003
6602876Adhesion receptor antagonists
Compounds of the formula I ##STR1## wherein R1, R2 and R3 have the meanings defined herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employ...
08/05/2003
6562980Method for producing 5-aryloxymethyl-2-oxazolidinones
The present invention provides a method for making 5-aryloxymethyl-2-oxazolidinone and derivatives thereof having the general formula of: ##STR1## wherein R1 and R2 are hydrogen, alkyl, or alkoxyl group and wherein the alkyl or ...
05/13/2003
6531470Oxazolidinone combinatorial libraries, compositions and methods of preparation
Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as ph...
03/11/2003
6518427Aminoaryl oxazolidinone N-oxides
The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I ##STR1## wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of ...
02/11/2003
6515135Aminoaryl oxazolidinone N-oxides
The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I ##STR1## wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of ...
02/04/2003
6512112Aminoaryl oxazolidinone N-oxides
The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I ##STR1## wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of ...
01/28/2003
6455529Adhesion receptor antagonists
Compounds of the formula I ##STR1## in which R1, R2 and R3 have the stated meanings, and their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be used for the treat...
09/24/2002
6441005Oxazolidinone compounds and compositions, and methods of using the same
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein ca...
08/27/2002
6441188Aminoaryl oxazolidinone N-oxides
The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I ##STR1## wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of ...
08/27/2002
6441189Process for the preparation of matrix metalloproteinase inhibitors
The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors....
08/27/2002
6413981Bicyclic heterocyclic substituted phenyl oxazolidinone antibacterials, and related compositions and methods
Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: ##STR1## wherein Y is a radical of the formulae II or III: ##STR2## in which the substituents have the meaning indicated in the description. These compounds are useful a...
07/02/2002
6410728Oxazolidinone chemotherapeutic agents
Compounds of the formula ##STR1## or therapeutically acceptable salts or prodrugs thereof, are useful for treating bacterial infections, psoriasis, arthritis, and toxicity due to chemotherapy. Preparation of the compounds, compositions containing the ...
06/25/2002
6403804Process for preparing optically active oxazolidinone derivative
Disclosed is a process for preparing an optically active oxazolidinone derivative comprising allowing hydrazine to react on an optically active ester having a hydroxyl group at the 3-position which is represented by formula (II): ##STR1## wherein R
06/11/2002
6391901Thrombin inhibitors
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the ...
05/21/2002
6387896Bicyclic oxazolidinones as antibacterial agents
The present invention provides compounds of formula I useful as antimicrobial agents ##STR1## wherein W, X, Y, R1, R2 and n are as defined in thereof....
05/14/2002
6329409Amine derivatives and skin preparations for external use containing the same
The invention relates to an amine derivative represented by the general formula (1): ##STR1## wherein R1 is a C1 -C30 hydrocarbon group which may be interrupted by an ether linkage, with the proviso that phenyl and benzyl ...
12/11/2001
62882395-trityloxymethyl-oxazolidinones and process for the preparation thereof
A method for preparing protected, preferably chiral, 5-trityloxymethyl-oxazolidinone in one step directly from optically active 3-hydroxy-4-trityloxy butyramide is described. Oxazolidinones are an important class of molecules in the pharmaceutical industr...
09/11/2001
6239152Oxazolidinone combinatorial libraries, compositions and methods of preparation
Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as ph...
05/29/2001
6204280Adhesion receptor antagonists
Compounds of the formula I ##STR1## wherein R1, R2 and R3 have the meanings defined herein, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employ...
03/20/2001
6166056Phenyloxazolidinones having a C-C bond to 4-8 membered heterocyclic rings
A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR1 ; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is --(CH2)
12/26/2000
6143772Compounds derived from 3-(benzofuran-5-yl)oxazolidin-2-one, preparation method therefor and therapeutical use thereof
Compounds derived from 3-(benzofuran-5-yl) oxazolidin-2-one, of general formula (I) ##STR1## in which: R1 represents a phenyl group, a phenylmethyl group, an alkyl group or a fluoroalkyl group, and R2 represents a hydrogen atom ...
11/07/2000
6124334Hetero-aromatic ring substituted phenyloxazolidinone antimicrobials
A hetero-aromatic (Q) substituted phenyloxazolidinone antimicrobial of Formula I ##STR1## wherein Q is a 5-member hetero-aromatic having from one to four nitrogen atoms or alternatively a benzoannulated 5-member hetero-aromatic having from one t...
09/26/2000
6090820Spirocyclic and bicyclic diazinyl and carbazinyl oxazolidinones
A compound of structural Formula I or II which is useful for treating microbial infections in humans or other warm-blooded animals, or pharmaceultically acceptable salts thereof as defined herein. ##STR1##...
07/18/2000
6083967S-oxide and S,S-dioxide tetrahydrothiopyran phenyloxazolidinones
The present invention provides compounds of formula I and formula II useful as antimicrobial agents wherein R1 is methyl, ethyl, cyclopropyl, or dichloromethyl; R2 and R3 are independently hydrogen or fluoro; R4...
07/04/2000
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