Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p

Abstract: Lidocaine analogs, latex particle-analog conjugates, and methods of making and using the same. The analogs have the formula: wherein Z comprises a nucleophilic group and optionally a protecting group; L is a linker; R1, R2, R3, R4, R5 are each independently H, a protecting group, or C1 to C6 alkyls, provided that R1 and R3 may form a six membered ring with the nitrogen and carbon atom to which R1 and R3 are attached; R6 and R7 are each independently H or C1 to C20 alkyls; and including salts thereof. The analogs are immobilized on latex particles and prepared for use in assays for lidocaine.

Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like].

Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases

Abstract: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC 3.4.21.31) of the aryl guanidine type.

Abstract: N-Benzoylureidocinnamic acid derivatives, processes for preparing them and their use The invention relates to N-benzoylureidocinnamic acid derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention thus relates to compounds of formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetic agents.

Abstract: In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor.

Abstract: Compound of formula (I): and medicinal products containing the same are useful as dual ?2/5-HT2c antagonist receptors.

Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to ?-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Abstract: A method of successfully controlling sea lice in commercial fish farming, in an efficient and environmentally friendly way, with the compounds named in claim 1, preferably by injection, and a method of automating this type of control, are described.

Abstract: The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXR? selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXR?-selective antagonist.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: Compositions and methods of using the same for the treatment of diabetes and other disorders of glucose metabolism are provided. Compositions may include an anti-diabetic agent and one or more of a bioavailable source of chromium and vanadium.

Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.

Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.

Abstract: The present invention relates to injecting a high specificity p38 kinase inhibitor into a diseased intervertebral disc.

Abstract: Compound of formula (I): 1

Abstract: A compound according to formula one that is useful as a fungicide is provided. Additionally, processes to make and use same are provided.

Abstract: The invention relates to carboxamide-substituted phenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.

Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: This invention provides compounds of formula I having the structure wherein: B, D, C, and R1 as defined herein.

Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: The invention relates a compound represented by the formula (1):

Abstract: The present invention relates to compounds of the formula wherein R1 independently represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro, provided that when R1 represents one substituent, it is in the ortho position, and when R1 represents more than one substituent, at least one R1 substituent is in the ortho position; R2 is one substituent in the ortho position, said substituent being selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl and nitro; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1

Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: The present invention relates to novel naphthalene derivatives of formula (I), wherein R1, R2, R3 and X are as defined in the description, and preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: Disclosed herein are methods for the treatment or prevention of photoaging or skin cancer in a patient. These methods include administering a compound that inhibits a component of the kallikrein inflammatory pathway in an amount sufficient to reduce one or more symptoms of photoaging or skin cancer.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.

Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.

Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: Described herein are novel 1-aryl-3-(2-chloroalkanylureas derivatives. These derivatives are useful anticaner agents having excellent specifilty towards cell targets and potent antineoplastic activity without systemic toxicity derivatives mutagenicity. More specifically, the invention is directed to novel derivatives of the following formula: wherein R1 is C1-C6 alkyl, C3-C7 cycloalkyl, C1-C6 alkoxy, C1-C6 hydroxy alkyl, or C1-C6 halide; R2 is H, C1-C6 alky, C3-C7 cycloalkyl, C1-C6 I alkoxy, C1-C6 hydroxy alkyl or C1-C6 halide, di-halide or tri-halide; R1 and R2 may also be part of cyclic structures.

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: The invention provides compounds of Formula I: 1

Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: This invention relates to novel phenyl ureas useful in the treatment of disease states mediated by the chemokine, Interleukin-3 (IL-3)

Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.

Abstract: The present invention relates to a urea derivative of the formula (1) 1

Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Abstract: Pharmaceutical compositions containing as an active ingredient compounds of the general formula (I), prodrugs of the same, pharmaceutically acceptable salts of both, or solvates of them and exhibiting thrombopoietin receptor agonism:

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: A heat sensitive recording material, comprising a) at least one colour forming compound, and b) at least one developer of the formula  wherein R1 is unsubstituted or substituted phenyl, naphthyl or C1-C20alkyl, X is a group of the formula A is unsubstituted or substituted phenylene, naphthylene or C1-C12alkylene, or is an unsubstituted or substituted heterocyclic group, B is a linking group of formula —O—SO2—, —SO2—O—, —NH—SO2—, —SO2—NH—, —S—SO2—, —O—CO—, —O—CO—NH—, —NH—CO—, —NH—CO—O—, —S—CO—NH—, —S—CS—NH—, —CO—NH—SO2—, —O—CO—NH—SO2—, —NH═CH—, —CO—NH—CO—, —S—, —CO—, —O—, —SO2—NH—CO—, —O&m

Abstract: A compound selected from the group consisting of a compound of formula I a compound of formula II and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: Disclosed are novel aromatic compounds of the formula(I) wherein G, E, W, Ar, X, Y and Z. The compounds are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.