Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.

Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.

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

Abstract: The present invention provides antibacterial agents having the formula I described herein.

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

Abstract: The present invention provides antibacterial agents of formula I described herein and intermediates for their preparation.

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

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, isoxazolidine compounds which have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the isoxazolidine compounds are also taught.

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1

Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.

Abstract: The present invention provides antibacterial agents having the formula I described herein.

Abstract: 1.

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: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: Methods for the preparation of N-arylated oxazolidinone compounds via a copper catalyzed cross coupling reaction are disclosed.

Abstract: The invention relates to novel substituted benzoylpyrazoles of the general formula (I), in which n represents the numbers 0, 1, 2 or 3, A represents a single bond or represents alkanediyl(alkylene), R1 represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, R2 represents hydrogen, cyano, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkoxycarbonyl or cycloalkyl, R3 represents hydrogen, nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, R4 represents nitro, cyano, carboxyl, carbamoyl, thiocarbamoyl, halogen, or represents in each case optionally substituted alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino or dialkylaminosulfonyl, Y represents hydrogen or represents in each case optionally substituted

Abstract: The present invention relates to novel trifluorobutenes of the formula (I) wherein R1 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with halogen, hydroxy, alkoxy, alkylthio, alkylcarbonyloxy, haloalkylcarbonyloxy, or cyano; alkylsulfonyloxy; or phenyl that is unsubstituted or substituted with halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfonyl, haloalkoxy, haloalkylthio, phenyl, phenoxy, cyano, or nitro; R2 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with alkoxy or halogen; or alkoxycarbonyl; and n represents 0, 1 or 2, with the proviso that if R1 represents alkyl, then R2 does not represent halogen. The invention also relates to processes for their preparation and their use as nematicides.

Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them.

Abstract: Compounds of formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolyzable ester thereof, wherein, for example, HET is an optionally substituted C-linked 5-membered heteroaryl ring containing 2 to 4 heteroatoms independently selected from N, O and S; Q is selected from, for example, Q1 and Q2: R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, an N-linked (fully unsaturated) 5-membered heteroaryl ring system or a group of formula (TC5): wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: A methylidene oxazolidinone compound represented by formula (1) or a pharmaceutically acceptable salt thereof, and a preparation method thereof, showing superior antimicrobial activities against gram-positive germs including resistant strains such as methicillic-resistant staphylococcus aureus and vancomycin-resistant enterococcus: 1

Abstract: A process for the preparation of taxanes comprising 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: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: 1

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C•H(OH)—CH2—NH—CO—RN   (VIIIA) and processes for production of pharmacologically useful oxazolidinones.

Abstract: The present invention provides antibacterial agents having the formulae I, II, and III described herein.

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: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

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: The invention concerns a compound of formula (I): 1

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)

Abstract: Condensed heterocyclic compounds of the general formula: 1

Abstract: A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient: 1

Abstract: Compounds of formula (I) 1

Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.

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

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 favorable 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 subject invention involves process for making fuctionalized oxazolidinones having structure (1) wherein: (a) R1 and R2 are each independently selected from hydrogen, alkyl, aryl and heterocycle, or R1 and R2 are attached to form a cycloalkyl, aryl or heterocyclic ring; (b) R3 is selected from primary and secondary alkly (—R6), —SO2—R4, and —C(O)NH—R5; (c) R4 is aryl; and (d) R5 is alkyl or aryl; the process comprising a reaction step carried out in a reaction mixture, wherein an oxazolidinone is reacted with an electrophile selected from R6-Br, R6-I, R4-SO2Cl, and R5-NCO; the reaction mixture comprising a non-protic and non-oxidizing solvent and potassium fluoride on alumina; and without the presence of a substantial amount of a strong base in the reaction mixture. The subject invention also involves libraries of functionalized oxazolidinone compounds and their preparation using such processes.

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

Abstract: The invention relates to the field of blood coagulation.

Abstract: The invention concerns a compound of the formula (I): wherein, for example: T is of the formula (IA), (IB), or (IC); R1 is of the formula —NHC(═O)Rb wherein Rb is (1-4C)alkyl; R2 and R3 are hydrogen or fluoro; >A—B— is >C═CH— (but not when T is (IA)) or >CH—CH2—; wherein when T is of the formula (IA) or (IB); R6 is, for example, (1-4C)alkyl; R5 is hydrogen, R10CO—, R10SO2— or R10CS— wherein R10 is, for example, optionally substituted phenyl, or (1-10C)alkyl, or when T is of the formula (IA), (IB); or (IC): R5 and R6 are linked to give a 5- or 6-membered ring which is fused to the ring shown in (IA), (IB), or (IC) so as to give an optionally substituted bicyclic ring; and pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them, and their use as antibacterial agents.

Abstract: The invention relates to an improved process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid or one of its salts with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that at least a portion of the reaction is carried out under a pressure of less than 1000 mbar. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.

Abstract: Oxazolidinones having a bicyclic[3.1.0] hexane containing moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species.

Abstract: Described herein are compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

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: The present invention relates to novel trifluorobutenes of the formula (I) 1

Abstract: A compound of the formula: 1

Abstract: The invention provides compounds of Formula I: compounds of the Formula I: wherein R1, R2, R4, R6, X, and W are defined herein. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals used to treat diseases or conditions in which &agr;7 is known to be involved.

Abstract: The present invention relates to certain substituted polyketides of formula I, 1

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.