Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

Abstract: A method for producing an optically active piperidine carboxylic acid derivative, which comprises subjecting a piperidine carboxylic acid derivative of the formula (1): wherein Z is a protecting group for the carboxyl group, to optical resolution by means of an optical resolution agent of the formula (2): wherein symbol * indicates that the designated carbon atom is asymmetric.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.

Abstract: A 1,7-disubstituted perylene-3,4,9,10-tetracarboxylic diimide of the general formula VI: Compositions or products comprising the compound of formula VI. Compositions comprising 1,7-diaroxy- or 1,7-diarylthio-substituted perylene-3,4,9,10-tetracarboxylic dianhydrides (I) or 1,7-diaroxy- or 1,7-diarylthio-substituted perylene-3,4,9,10-tetracarboxylic acids (Ia).

Abstract: A new gamma-I type quinacridone pigment characterized by C.I.E color space values in masstone, and a process for its preparation is disclosed. The new gamma quinacridone pigment is especially useful for coloring coating compositions, such as automotive paints, and plastics.

Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

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: A process for the preparation of trifluoroethoxy benzoic acid derivatives, in particular Flecainide, and their pharmaceutically acceptable salts, starting with commercially available halobenzoic acids and involving the use of simple reagents and low cost solvents, to afford high overall yield of the product. The above object is achieved in accordance with the present invention which, in one aspect thereof, provides a process for preparing a compound of formula (A): and pharmaceutically acceptable salts thereof, which process comprises the steps of: a) reacting a halobenzoic acid or a salt thereof of the formula [II ]  with 2,2,2-trifluoroethanol in the presence of a strong base and a copper containing material, if desired followed by acidification to obtain a compound of formula [I] b) converting the product obtained in step a) above into the compound of formula (A) or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

Abstract: Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.

Abstract: A compound of formula (I), wherein R1 is carboxy or protected carboxy, R2 and R3 are each independently hydrogen, hydroxy, or protected hydroxy, R4 is hydrogen or halogen, R5 is aryl substituted with halogen, amino, hydroxy or protected hydroxy, R6 is aryl optionally substituted with halogen, amino, hydroxy or protected hydroxy, A1 and A2 are each independently lower alkylene, and (II) is (III), (IV), (V) or (VI) or its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.

Abstract: Compound of the formula (I): wherein Ar is a group of the following formula (Ar-1) or (Ar-2): A is a group of the formula: —Z—N(Q1)(Q2), —CO—R7 or —(CH2)p—CH(R8)—COR9, or a pharmaceutically acceptable acid addition salt thereof, a process for preparing the same, a pharmaceutical composition containing the same, and intermediates therefor. The compounds of the present invention show a potent affinity for 5-HT4 receptors, and they are useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent.

Abstract: A &bgr;,&ggr;-dihydropolyprenyl alcohol derivative having the formula: wherein n is an integer of 5 to 7 and R is hydrogen, a lower alkyl group or an aliphatic or aromatic acyl group, is new and useful as a prophylactic therapeutic agent for human and animal immuno-deficiency deseases and phylactic agent against human and animal infectious deseases. Another disclosed polyprenyl compound is also useful as the same agent.

Abstract: An process for epoxidizing diversely functionalized olefins by oxorhenium catalysis employs conditions which control water concentration. By controlling water concentration, one can maximize monoperoxo complex formation and increase turnover which subsequently reduces diol side products obtained from epoxide ring opening and increases the yield of the desired epoxide product. The optimal range of water concentrations is 0.50-80.0 mol %. Using less than 0.5 mol % water does not result in practical turnovers and 1.0 equivalent of water (or more) is detrimental to the lifetime of the active catalytic species formed.

Abstract: Compounds of general formula (I) wherein: R1 is H or optionally joined with R2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl rings, R2 and R3 are independently H, HET, aryl, C1-12 aliphatic, CN, NO2, halogen, R10, —OR10, —SR10, —S(O)R10, —SO2R10, —NR10R11, —NR11R12, —NR12COR11, —NR12CO2R11, —NR12CONR11R12, —NO12SO2R11, —NR12C(NR 12)NHR11, —COR11, —CO2R11, —CONR12R11, —SO2NR12R11, —OCONR12R11, C(NR12)NR12R11, R6 and R7 are independently halogen, CN, NO2, —CONR10R11, —SO2NR10R11, —NR10R11, or —OR11, where R10 and R11 are as defined below; R8 is OH, NHSO2R12 or NHCOCF3; and their use in therapy, especially in the treatment of disorders mediated by cRaf1 kinase.

Abstract: The present invention relates to a compound represented by Formula [I] wherein represents an aromatic carbo- or heterocyclic ring which may have a substituent; Cy represents a mono-, bi- or tricyclic aliphatic carbocyclic group having 3 to 20 carbon atoms, which may have a substituent; represents a mono- or bicyclic aliphatic nitrogen-containing heterocyclic group having 3 to 14 carbon atoms, which may have a substituent; R1 represents a hydrogen atom, a lower alkenyl group, a lower alkynyl group, a cyclo(lower alkyl) group, an amino group, a lower alkylamino group, a di(lower alkyl)-amino group, a hydroxyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group or a di(lower alkyl)carbamoyl group, or a lower alkyl group which may have a substituent; and R2 represents a hydrogen atom or a lower alkyl group, a salt or ester thereof, a production process for the same, and an analge

Abstract: This invention relates to novel compounds, pharmaceutical compositions comprising these compounds and their use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: There is disclosed a process for the preparation of sulfenimides comprising: mixing, in a hydrocarbon solvent, a sulfenamide of the formula with an aldehyde of the formula R4CHO where X is a sulfur atom, a —C═N— group, or a —C═C— group, R1 and R2 are independently selected from the group consisting of hydrogen, alkyl, and aryl or may be joined to form a saturated or unsaturated ring or aromatic ring, R3 is alkyl or cycloalkyl, and R4 is a hydrocarbon radical wherein the carbon bearing the aldehyde function is bonded only to other carbon atoms, a substituted or unsubstituted aryl ring, or a heteroaromatic ring; and heating the mixture at a temperature and for a period of time sufficient to convert the sulfenamide to the sulfenimide.

Abstract: A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.