Abstract: 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 acceptable compositions containing them.

Abstract: Synthesis of N-[N-(3,3-dimethylbutyl)-L-?-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.

Abstract: 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, and/or prokinetic (gastrointestinal modulatory) agents, having the formula: or pharmaceutically acceptable salts, esters, or prodrugs thereof.

Abstract: 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 amino alcohols. The assay provides fluorescently labeled model mRNAs that include conserved sequence information typical of antiterminator bulge regions found in the mRNA of T-box gene regulatory systems.

Abstract: 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 pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

Abstract: The present invention describes difluororthioacetamide oxazolidinones of formula I: R is —CH2— or —CH2CH2—; R2 and R3 are independently —H or —F; X is —CH—; Y is —SO—, —SO2—, or —SONR4—; and R4 is —H or —C1-4alkyl. These compounds are useful to treat infectives diseases caused by gram-positive and gram-negative bacteria.

Abstract: 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.

Abstract: Synthesis of N-[N-(3,3-dimethylbutyl)-L-?-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.

Abstract: 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 readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

Abstract: A production method of a compound represented by the formula wherein R1 and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R3 is an electron-withdrawing group, and R4, R5 and R6 are each a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, is provided as an industrially advantageous production. method for forming a carbon-carbon bond at the 5-position of oxazole, which method includes reacting a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, with a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, in the presence of an acid or a base.

Abstract: 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.

Abstract: Compounds of the formula I 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 employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, ischaemias, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1

Abstract: The present invention provides a method for making 5-aryloxymethyl-2-oxazolidinone and derivatives thereof having the general formula of: wherein R1 and R2 are hydrogen, alkyl, or alkoxyl group and wherein the alkyl or alkoxyl group contains no more than three carbon atoms in straight or branched chain. The invention involves the fusion of a triglycidyl isocyanurate (TGIC) with an unsubstituted or a mono- or di-substituted phenol.

Abstract: A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: 1

Abstract: 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 pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: Compounds of the formula I 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 treatment of thromboses, osteoporoses, oncoses, stroke, myocardial infarct, ischemias, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: 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 readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

Abstract: The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.

Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: wherein Y is a radical of the formulae II or III: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: Compounds of the formula 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 compounds, and treatment of diseases using the compounds are disclosed.

Abstract: 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): wherein R1 represents a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, a methoxymethyl group, a benzyloxymethyl group, a benzyloxycarbonylaminomethyl group which may have a substituent or substituents on the benzene ring thereof, an acylaminomethyl group having 3 to 10 carbon atoms, or an alkyloxycarbonylaminomethyl group having 3 to 6 carbon atoms; R2 and R3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, an acetylaminomethyl group, a benzoylaminomethyl group, or a benzyl group; and * indicates an asymmetric carbon atom, and subjecting the resulting hydrazide to Curtius rearrangement.

Abstract: 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 use of defined compounds of formula I as thrombin inhibitors.

Abstract: The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R1, R2 and n are as defined in thereof.

Abstract: A compound of the formula: 1

Abstract: The invention relates to an amine derivative represented by the general formula (1): wherein R1 is a C1-C30 hydrocarbon group which may be interrupted by an ether linkage, with the proviso that phenyl and benzyl groups are excluded; one of A and B is and the other of them is —OR4; R2 and R3 are individually H, amidino group, alkanoyl group, C1-C20 hydrocarbon group, or the like; R4 and R5 are individually H, phosphoryl group, or the like, and an external skin care composition containing the same. The external skin care composition exhibits excellent preventing effects on aging of the skin, etc.

Abstract: 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 industry especially in the areas of antimicrobials and behavioral disorders.

Abstract: 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 pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

Abstract: Compounds of the formula I 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 employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, ischaemias, inflammations, arteriosclerosis and osteolytic disorders.

Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is NR.sub.1 ; R.sub.1 is H, C.sub.1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R.sub.1 is --(CH.sub.2).sub.h -aryl, --COR.sub.1-1, --COOR.sub.1-2, --CO--(CH.sub.2).sub.h --COR.sub.1-1, C.sub.1-6 alkyl sulfonyl, --SO.sub.2 --(CH.sub.2).sub.h -aryl, or --(CO).sub.i --Het; R.sub.2 is H, C.sub.1-6 alkyl, --(CH.sub.2).sub.h -aryl, or halo; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.

Abstract: Compounds derived from 3-(benzofuran-5-yl) oxazolidin-2-one, of general formula (I) ##STR1## in which: R.sub.1 represents a phenyl group, a phenylmethyl group, an alkyl group or a fluoroalkyl group, and R.sub.2 represents a hydrogen atom or a methyl group. Application in therapeutics.

Abstract: 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 to four nitrogen atoms where R.sup.1 is independentlyl H, OCH.sub.3, F, or Cl; and R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl (optionally substituted with one or more of F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy), C.sub.3 -C.sub.6 cycloalkyl, amino, C.sub.1 -C.sub.8 alkylamino, C.sub.1 -C.sub.8 dialkylamino, C.sub.1 -C.sub.8 alkoxy.

Abstract: 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.

Abstract: The present invention provides compounds of formula I and formula II useful as antimicrobial agents wherein R.sub.1 is methyl, ethyl, cyclopropyl, or dichloromethyl; R.sub.2 and R.sub.3 are independently hydrogen or fluoro; R.sub.4 is ethyl or dichloromethyl. The invention also relates to a novel assay for determining the inhibitory activity of oxazolidinones to human monoamine oxidase.

Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## A is alkyl having from 1 to 6 C atoms, R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.

Abstract: This invention relates to (R)-(-)-methylphenyloxazolidinone derivatives, a process for their production and their use as pharmaceutical agents.

Abstract: Pharmaceutical preparations for the local treatment of inflammations are claimed herein, characterized in that they contain as the active ingredient one or two compounds of general Formula I ##STR1## wherein X is an oxygen atom or a methylene group,R.sub.1 and R.sub.2 represent a hydrogen atom or a hydrocarbon residue of maximally eight carbon atoms, optionally interrupted by an oxygen atom,R.sub.3 is a hydrogen atom or a hydrocarbon residue of maximally eight carbon atoms, optionally substituted by an oxo group, andR.sub.4 is a hydrogen atom or an alkyl group of maximally four carbon atoms.

Abstract: Compounds derived from oxazolidin-2-one of formula (I) ##STR1## in which: R.sub.1 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a fluoroalkyl group, a hydroxyfluoroalkyl group, a cyanoalkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylmethyl group or an R.sub.3 A- group in which R.sub.3 is a cycloalklyl or cyclooxyalkyl group which is unsubstituted or substituted by a hydroxyl group and A is a --CH.sub.2 or --CH.sub.2 --CH.sub.2 radical,R.sub.2 represents a hydrogen atom or a methyl group,X represents an oxygen or sulphur atom or an NR.sub.4 group where R.sub.4 is an alkyl group or a hydrogen atom, andZ represents an oxygen atom or a --CH.dbd.CH or --CH.sub.2 --CH.sub.2 group,their process of preparation and their applications in therapeutics.

Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.

Abstract: The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as anti-bacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (.+-.)-5-(acetamidomethyl)-3-?4-(3-pyridyl)-3,5-difluorophenyl!-2-oxazolid inone.

Abstract: Derivatives of oxazolidin-2-one of general formula (I) ##STR1## in which: n is equal to 0 or 1,R.sub.1 represents a cyano group, an alkyl group or a fluoroalkyl group,R.sub.2 represents a hydrogen atom or a hydroxyl group, andR.sub.3 represents a hydrogen atom or a methyl group.Application in therapeutics.

Abstract: A process for preparing a compound of formula (I) ##STR1## wherein R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX4 is --OH, fluorine or --O--SO.sub.2 R6 where R6 is methyl, trifluoromethyl, phenyl or p-methylphenyl which comprises contacting of a compound of formula (III) ##STR2## where R2 is C.sub.1-4 alkyl; and R and X4 have the above mentioned meanings, with a strong base selected from the group consisting of alkali earth metal alcoholates, alkaline earth metal alcoholates, and tertiary amines in an aprotic solvent, to obtain the compound of formula (I).

Abstract: Cyclic N-halamine biocidal monomers and polymers and methods of using the same as biocides, wherein the functional group, halogenated oxazolidinones, may be homo- and copolymerized, are provided. The copolymerizations are effected with inexpensive monomers such as acrylonitrile, styrene, vinyl acetate, vinyl chloride, and the like. Grafting reactions were also accomplished with the N-halamine monomers and commercial polymers such as poly-acrylonitrile, poly-styrene, poly-vinyl acetate, poly-vinyl alcohol, poly-vinyl chloride, and cellulose. These N-halamine compounds are stable biocides which release small amounts of free halogen and other impurities. They will be useful as disinfectants for swimming pools, oil and water based paints, preservatives, medical and dental coatings, industrial and commercial coatings, fabrics, sterile bandages, liners of containers, and the like.

Abstract: The present invention relates to antimicrobial phenyloxazolidinone compounds having a pyrrolidinyl or azetidinyl moiety.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.