Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1

Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: 1 2

Abstract: Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e.g., eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.

Abstract: The invention relates to a compound of formula (I): 1

Abstract: Compounds of the formula (I) wherein X is O, CH2, S or NH, or the moiety X—R1 is hydrogen; V is CH or N; R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heterocyclyl, hererocyclylC1-6alkyl, heteroaryl, or heteroarylC1-6alkyl any of which except hydrogen may be optionally substituted; R2 and R3 independently represent hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, arylC1-6alkyl, heteroaryl, heteroarylC1-6alkyl, heterocyclyl, or heterocyclylC1-6alkyl any one of which except hydrogen may be optionally substituted, or R2 and R3 together with the nitrogen atom to which they are attached form a 4- to 10-membered optionally substituted monocyclic or bicyclic ring; Ar is an aryl or heteroaryl ring either of which may be optionally substituted; one of X1 and X2 is N and the other is NR4, wherein R4 is hydrogen, C1-6alkyl, or arylC1-6alkyl; or pharmaceutically acceptable salts thereof; their use as inhibitors of Raf kinases and pharmaceutical compositions containing them.

Abstract: Compounds of formula (I) 1

Abstract: The present invention is a heteroaromatic substituted amide showing antagonist activity to neurokinin 1 (NK-1, substance P) receptors.

Abstract: 3-(amino- or aminoalkyl) pyridinone derivatives having the formula (1) 1

Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: A process for preparing a compound of the formula 1

Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases.

Abstract: A new series of derivatives of 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid and their synthesis have been discovered. Surprisingly, by modifying the substituent of the 3-carboxylic acid group, new compounds were produced with high activity as PAF receptor antagonists. These compounds were shown to protect neurons from brain damage that normally occurs in response to stroke and other cerebrovascular diseases. These compounds are also protective against edema generation resulting from traumatic breakdown of the blood-brain barrier. Moreover, these compounds were found to be non-toxic and cytoprotective of cells undergoing oxidative stress that would normally trigger apoptotic cell death; and to have activity as (a) antagonists of an intracellular platelet activating factor (“PAF”)-binding site, (b) inhibitors of PAF- and cytokine-mediated c-aminoterminal jun kinase (JNK) and extracellular regulated kinase (ERK), and (c) transcriptional inhibitors of COX-2 expression.

Abstract: Aspects of the present invention are directed towards compounds of Formula I for the treatment of human erectile disorders including erectile dysfunction in men.

Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.

Abstract: Compounds are provided which have the structure 1

Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.

Abstract: Compounds I-III wherein U is CH, O, or S; Z is mono- or di-substituted carbon; R is (CH2)nCO2H, (CH2)nSO3H, (CH2)nPO3H2, (CH2)nNO2, CH(SCH3)3, esters; R1 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl; RR1 is O; n is 0-4; R2, R3 is H, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkyl; R4 is (CH2)nOH, (CH2)nNH2, substituted alkyl were prepd. as neuraminidase inhibitors. Thus, (1R,3R,4R,1′S)-(−)-(1′-acetylamino-2 ′-ethyl)butyl-4-(aminoimino)methylaminocyclopentan-1-carboxylic acid was prepd. and tested in vitro as neuraminidase inhibitor (IC50<1.mu.M).

Abstract: The present invention relates to 1-(2-chloro-5-methyl-3-pyridylmethyl)-2-nitroiminoimadozolidine of the formula 1, a novel compound of class nitroimino pyridyl derivatives and to a process for the preparation thereof 1

Abstract: Compounds of the formula (I), in which M, A1, A2, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.

Abstract: The invention provides a method for synthesis of compounds of formula 1

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: Peptide analogs formed by replacing one or more, but not all, amino acids of a peptide chain with 1,2-dihydro-3(6H)-pyridinone, display an unusually strong tendency to assume a &bgr;-strand conformation and to enter into &bgr;-sheet-like interactions with peptides and other peptide analogs that engage in &bgr;-sheet-like interactions with peptides. The peptide analogs of this invention therefore have utility has &bgr;-strand mimics offering advantages over native peptides as well as &bgr;-strand mimics of the prior art.

Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: 1

Abstract: The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions containing a therapeutically effective amount of at least one of these analogues. In accordance with the present invention, the pyridoxal and pyridoxine analogues can be used in the treatment of undesired platelet aggregation, and in the treatment of symptoms thereof.

Abstract: Novel 1,4,5 substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.

Abstract: Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.

Abstract: This invention relates aryl substituted pyridines of Formula I: 1

Abstract: Compositions and methods for inhibiting and controlling the growth of microbes are disclosed. The composition comprises at least one chemically-modified peptide with antimicrobial activity and at least one carrier. The method comprises of administering an amount, effective for the prevention, inhibition and termination of microbial growth for industrial, pharmaceutical, household and personal care use.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: The present invention relates to a process for preparing tetrasubstituted imidazole derivatives of the general formula (I) 1

Abstract: N-Heterocyclic derivatives selected from the group consisting of the following formulae: where Z1, Z2, Z3, R1, R2, R3, R4, R5 and R6 are described herein, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: The present invention discloses novel substituted imidazole compounds which have either or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.

Abstract: Novel agents acting as co-factors for replacement of NAD(P)+/NAD(P)H co-enzyme systems in enzymatic oxido-reductive reactions. Agents mimicking the action of NAD(P)+/NAD(P)H system in enzymatic oxidation/reduction of substrates into reduced or oxidized products. A method for selection and preparation of the mimicking agents for replacement of NAD(P)+/NAD(P)H system and a device comprising co-factors for replacement of NAD(P)+/NAD(P)H system.

Abstract: The present invention provides a genus of pyridine-substituted benzanilides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Abstract: The present invention relates to bisarylimidazolyl derivatives and pharmaceutical compositions comprising said compounds inhibiting fatty acid amide hydrolase and useful for the treatment of pain, particularly neuropathic pain, psychomotor disorder, hypertension, cardiovascular disease, eating disorder, nausea, AIDS-related complex, glaucoma, inflammation, psoriasis or multiple sclerosis, and other conditions the treatment of which can be effected by inhibiting fatty acid amide hydrolase.

Abstract: Provided is a method of treating or ameliorating certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I:

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor (“CRF receptor”) and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be effected by the antagonism of the CRF-1 receptor.

Abstract: Compounds having Formula 4 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1, R2 and R3 are various substituent groups; and one of X1 and X2 is N or CR′, and the other is NR′ or CHR′ wherein R′ is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR′ then the other may be S or O; and their use as pharmaceuticals.

Abstract: Certain imidazo pyridines/quinolines of the formula: where n is 0, 1, 2; X is independently selected from the group consisting of C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2, nitro, and two adjacent X may be fused to form the moiety:  whereby a saturated, partially unsaturated or aromatic six-membered fused ring is formed; Y is independently selected from the group consisting of hydrogen, hydroxy, C1-4alkyl, C1-4alkoxy, trifluoromethyl and phenyl; and Z is independently selected from the group consisting of hydroxy, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2 and nitro; are &agr;2-adrenoceptor modulators which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, Parkinsonism, the need for anesthesia, cardiac arrythmia or the need for analgesia.

Abstract: The invention relates to certain heterocyclic compounds useful for the treatment of cancer and other diseases, having the Formula (I): 1

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

Abstract: Novel fluorescent derivitization reagents are described that are suitable for coupling to biomolecules that contain aldehyde or ketone functional groups. The method of treating a sample with the derivativization reagents is described. The reagents are particularly useful for labeling glycoproteins or glycopeptides, nucleic acids, and lipopolysaccharides in electrophoresis gels.