Abstract: The invention relates to novel substituted heteroaryloxyacetanilides of the general formula (I), in which n, R, X, and Z are to intermediates for their preparation and to their use as herbicides.

Abstract: Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonimides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.

Abstract: The present invention relates to novel oxazolidinone compounds of the general formula (I) 1

Abstract: A process for the preparation of 5-(3,5-dimethylphenoxymethyl)-2-oxazolidinone, which includes: a) reacting 3,5-dimethylphonel with epichlorohydrin to obtain a mixture of 1-(3,5-dimethylphenoxy)2,3-epoxy propane (1) and 1-(3,5-dimethylphenoxy)-3-chloro-2-propanol (2); b) reacting the mixture of (1) and (2) obtained from step (a) with benzylamine to obtain a first compound; c) reducing the first compound with hydrogen in presence of ammonia, to obtain a second compound; and d) reacting the second compound with dimethylcarbonate in the presence of a strong base to obtain 5-(3,5-dimethlphenoxymethyl)-2-oxazolidinone.

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: Piperidinyloxy, pyrrolidinyloxyl and azetidinyloxy compounds of the formula: wherein R1 is a piperidinyl, pyrrolidinyl or azetidinyl moiety as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: 3-(alk-2-ynyloxy)carbonyl-5-oxazolidine carboxylic acid and its analogs having a formula and wherein R1 is hydrogen, aryl, heteroaryl, alkyl, alkenyl, alkynyl, R2 and R3 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, R4 is hydrogen, alkyl, alkenyl, alkynyl, aryl, substituted aryl, heteroaryl, R5 and R6 independently selected from hydrogen, alkyl, alkenyl,alkynyl, arly, heteroaryl, alkoxy, alkeyloxy, alkynyloxy, aryloxy, heteroaryloxy.

Abstract: The application relates to a process for preparing a compound of Formula I 1

Abstract: The present application describes novel lactams and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered lactam containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as inhibitors of matrix metalloproteinases, TNF-&agr;, and aggrecanase.

Abstract: The invention concerns compounds of formula (I), wherein, for example, R1 is of the formula —NHC(═O)Ra wherein Ra is (1-4C)alkyl; R2 and R3 are independently hydrogen or fluoro; R5 and R6 are, for example, hydrogen; R4 is —X—Y—Het.; wherein, for example, X is a direct bond and Y is —(CH2)m— or —CONH—(CH2)m—; or X is —(CH2)n— and Y is —S(O)p—(CH2)m—; or X is —CH2O—or —CH2NH— and Y is —CO—(CH2)m—; wherein n is 1, 2 or 3; m is 0, 1, 2 or 3 and p is 0, 1 or 2; wherein Het. is a heterocyclic ring, unsaturated or saturated, optionally substituted by, for example, (1-4C)alkyl, halo, cyano, nitro or amino; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

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 1

Abstract: Compounds of the formula I and their salts, as defined in claim 1, are suitable as safeners for protecting crop plants against the phytotoxic side-effects of herbicides.

Abstract: The present invention relates to a one-step process to prepare pharmacologically active 2-oxo-5-oxazolidinylmethylacetamides.

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 invention relates to a process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that the reaction is a least partially carried out in the presence of an unsaturated organic compound which has one or more ethylenic double bonds, one of the carbon of at least one ethylenic double bond of which is completely substituted by substituents other than halogen atoms. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: 1

Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: The present invention provides a production method of an optically active &bgr;-amino-&agr;-hydroxycarboxylic acid, which includes the following steps (a)-(c):

Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1

Abstract: Compounds represented by formula (I) wherein R is a C3-C5 cycloalkyl group, R1 is a hydrogen atom or a methyl group, or a pharmaceutically acceptable salt thereof; are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

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: The present application discloses a class of antibiotic compounds containing an oxazolidinone ring. These compounds have useful activity against Gram-positive pathogens including MRSA and MRCNS and, in particular, against various strains exhibiting resistance to vancomycin and against E. faecium strains resistant to both aminoglycosides and clinically used &bgr;-lactams. The compounds also possess a favourable toxicological profile. This invention further relates to processes for their preparation, to intermediates useful in their preparation, to their use as therapeutic agents and to pharmaceutical compositions containing them.

Abstract: The present invention provides oxazolidinones having a benzannelated 6- or 7-membered heterocycle as antibacterial agents.

Abstract: Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: Molecules containing a chiral 1,2-diol unit are synthesized from reactions between aldehydes and N-acyl selones. A chilled N-acyl selone is reacted with a Lewis acid such as TiCl4 and mixed with a tertiary amine such as diisopropylethylamine to generate an enolate solution. Upon further chilling of the enolate solution a desired aldehyde is added and after an acceptable reaction period a quencher is introduced and the product isolated.

Abstract: Compound represented by the structural formula 1

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I 1

Abstract: Compounds of formula (I) 1

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.

Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I 1

Abstract: Novel sulphonyloxazolones of the formula 1

Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising:

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to a process for producing 4-alkoxycarbonyl-2-oxazolidinone compound represented by the formula (III): wherein R1 represents H, an alkyl group, an cycloalkyl group, an alkenyl group or a phenyl group, R2 represents H, an alkyl group, a phenyl group or an alkenyl group, R3 represents an alkyl group, a cycloalkyl group, an alkenyl group, or a phenyl group, and R4 represents H, an alkyl group, an alkenyl group, acycloalkyl group, alkynyl group, an aryl group, a 5- or 6-membered heteroaromatic ring group, an alkoxycarbonyl group, an acetyl group or a benzoyl group, which comprises reacting a 5-alkoxy-2(3H)oxazolone compound represented by the formula (I): wherein R1, R2 and R3 have the same meanings as defined above, and an aldehyde compound represented by the formula (II): R4CHO  (II) wherein R4 has the same meaning as defined above, in the presence of a Lewis acid catalyst.

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: 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: Disclosed are multibinding compounds which inhibit cyclooxygenase-2 (COX-2), an enzyme which catalyzes the first committed step in the biosynthesis of prostaglandins. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to COX-2. The multibinding compounds of this invention are useful in the treatment inflammation, pain, fever and the like.

Abstract: Compounds of the formula: 1

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

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

Abstract: Compounds of the formula 1

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: The invention concerns a compound of the formula (I): wherein, for example: R1 is of the formula —NHC(═O)Rb wherein Rb is, for example, (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; R2 and R3 are hydrogen or fluoro; D is O; R4 and R5 are hydrogen, (1-4C)alkyl or AR-oxymethyl; AR is phenyl or phenyl(1-4C)alkyl; R6 is hydrogen; >A—B— is of the formula >C═C(Ra)—, >CHCHRa—, or >C(OH)CHRa— (> represents two single bonds) wherein Ra is hydrogen or (1-4C)alkyl; and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: The invention concerns compounds of formula (I), wherein: A is a 5 membered heteroaryl ring, a bicyclic benzo system containing such a 5 membered heteroaryl ring or a bicyclic or tricyclic heteroaryl ring system with at least one bridgehead nitrogen and optionally a further 1-3 heteroatoms chosen from oxygen, sulfur and nitrogen; R1 is, for example, hydroxy, halo, amino, nitro, cyano, carboxy, thiol, C1-4alkanoyloxy, C1-4alkoxycarbonyl, dimethylaminomethyleneaminocarbonyl, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, optionally substituted phenyl, an optionally substituted 5- or 6-membered heteroaryl ring or hydroxyC1-4alkyl; n is 0-6; R2 and R3 are independently hydrogen or fluoro; R4 is, for example, C1-4alkyl; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.

Abstract: Amide compounds of formula (I), combinatorial libraries of amide compounds and methods of preparing the same are provided. Libraries of the invention are useful for screening in biological assays in order to identify pharmaceutically useful compounds.