Abstract: This invention relates to compounds with the formula (I) given below or one of their pharmaceutically acceptable salts, as a medicine; Formula (I) of pharmaceutical compositions comprising one or more compounds with Formula (I) as active constituent, use of compounds with Formula (I) for the preparation of compositions designed to prevent or treat at least one illness involving an abnormal cellular proliferation, pro-apoptotic compositions and/or anti-proliferative compositions comprising at least one compound with Formula (I)/and the use of compounds with formula (I) as pro-apoptotic and/or anti-proliferative agents.

Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: The present invention relates to benzoyl-substituted alanines of the formula I in which the variables R1 to R13 are as defined in the description, and to agriculturally useful salts thereof, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.

Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.

Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.

Abstract: The present invention provides polymeric compositions that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: Disclosed are anthranilic acid derivatives having Formula (I): and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds in the treatment of conditions or diseases such as prostate cancer, and methods of using such compounds in the inhibition of 17?-hydroxysteroid dehydrogenase type 3 enzyme.

Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: The present invention relates to modulators of metalloproteinase activity.

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g. cancer and psoriasis.

Abstract: The present invention concerns novel derivatives of 1-phenylalkanecarboxylic acids, pharmaceutical compositions thereof, a process for their preparation and their use for the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.

Abstract: Compounds of the formula I, in which R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel and antiarrythmic active compounds, in particular for the treatment and prophylaxis of atrial arrythmias, e.g. atrial fibrillation (AF), or atrial flutter.

Abstract: Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

Abstract: The present application describes deuterium-enriched vorinostat, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: Universal supports for oligonucleotide synthesis include a support material represented by the following formula: In this formula, substituent A is selected from H, alkyl, aryl, or a polymeric or silica base material; substituent B is selected from acyl, aroyl, or a polymeric or silica base material; and substituent C is selected from a dimethoxytrityl group or a protecting group removable under acidic or neutral conditions. For the supports, one of substituents A or B constitutes the polymeric or silica base material. In use, an oligonucleotide is attached to the support at substituent C.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)I, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and w

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: Disclosed are novel compound of formula I, As defined herein and their use as pharmaceutically active compounds for reducing blood glucose, and/or treating one or more of type II diabetes, disturbances of lipid and carbohydrate metabolism, arteriosclerotic manifestations, and insulin resistance.

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: This invention is directed to inhibitors of copper-containing amine oxidases (E.C.1.4.3.6) including semicarbazide-sensitive amine oxidase (SSAO; also known as vascular adhesion protein-1, VAP-I), and their therapeutic use in inflammatory diseases, diabetes and its associated complications, atherosclerosis, neurodegenerative diseases, obesity, hypertension and cancer.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.

Abstract: The present invention provides compositions (small molecules, oligomers and polymers) that can be used to modify charge transport across a nanocrystal surface or within a nanocrystal-containing matrix, as well as methods for making and using the novel compositions.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.

Abstract: Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention.

Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

Abstract: Novel acyl urea, thiourea, carbamate, thiocarbamate and related compounds are provided which are effective in inhibiting the cytokine-mediated inflammatory response in cultured cells, in ameliorating bone destruction in an animal model of arthritis and in lowering blood glucose levels in animal models of Type II diabetes mellitus. The compounds are disclosed as useful for a variety of treatments including the treatment of diabetes mellitus, insulin resistance, inflammation, inflammatory, diseases, immunological diseases and cancer.

Abstract: In accordance with the present invention, a high intensity radiopaque contrast agent is disclosed. The agent may be coated on or incorporated within bulk materials, which may then be subsequently utilized to fabricate a radiopaque medical device. Primary effects through chemistry include higher radiopaque concentrations per unit weight of the radiopaque element or agent. Secondary effects include selective placement of the radiopaque elements which may further enhance the radiopacity of the device with reduced requirements of the radiopaque agent. Such a radiopaque contrast agent may be produced in various forms such as a dendrimer and/or incorporated as the end groups of polymeric chain. In addition one can incorporate biological and/or pharmaceutical agents in combination with the present invention.

Abstract: The invention relates to substituted [(phenylethanoyl)amino]benzamides and methods for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of inflammatory disorders such as, for example, cutaneous, respiratory tract and cardiovascular disorders such as, for example, arteriosclerosis and coronary heart disease.

Abstract: Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.

Abstract: Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.

Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.

Abstract: The invention describes fluorescent biomolecule labeling reagents (I-SHark and phI-SHark) and their model compounds. Further described are methods of preparing and using the same.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by -X1-L?-X2-Z or -Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.

Abstract: Compositions, in particular cosmetic compositions, comprising a cyclohexane-based compound defined by formula (I): wherein: R, which may be identical or different, are each chosen from hydrogen atoms and linear and branched, saturated hydrocarbons comprising 1 to 6 carbon atoms; Y, which may be identical or different, are each chosen from —CO—S—R? groups, —CO—NHR? groups, NH—COR? groups and —S—COR? groups, wherein R?, which may be identical or different, are each chosen from hydrogen atoms, aryl groups, optionally substituted with at least one hydrocarbon comprising 1 to 22 carbon atoms, wherein said hydrocarbon is chosen from linear and branched, saturated and unsaturated hydrocarbons, and linear, branched and cyclic, saturated and unsaturated hydrocarbons comprising 1 to 22 carbon atoms, wherein said hydrocarbons may optionally be substituted with at least one group chosen from aryl groups, ester groups, amide groups and urethane groups; wherein said hydrocarbons may optionally comprise at least on

Abstract: A compound of the general formula (I) (wherein the symbols are as defined in the description), or a prodrug or a salt thereof.

Abstract: The present invention is directed to intermediate compounds of mirtazapine and methods for obtaining same. A method is described for obtaining (±)-3-phenyl-1-methylpiperazine, an important intermediate for obtaining mirtazapine, which is based on imposing a cyclization reaction, in the presence of a reducing agent, on new compounds of general formula (1) in which Z is a leaving group capable of undergoing a nucleophilic displacement. A method is also described for obtaining the new compounds of formula (1).

Abstract: The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene group, (C3-C8)alkenylene group or the like, B is —O— or —N(R4)— (wherein R4 is H, (C1-C6)alkyl, halo(C1-C6)alkyl or the like), R1 is H, (C1-C6)alkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, R2 and R3 are each H, (C3-C6)cycloalkyl or —A2—R8 (A2 is —C(?O)—, —C(?S)— or —C(?NR9)—, R8 and R9 are each H, (C1-C6)alkyl or the like), Q1 to Q5 are each carbon or nitrogen, X and Y are each halogen, cyano, nitro, (C3-C6)cycloalkyl, optionally substituted phenyl, optionally substituted heterocyclic group, or the like, n is 0 to 4, m is 1 to 5, and Z1 and Z2 are each O or S] or a salt thereof, an agricultural and horticultural chemical, and a usage of the chemical.

Abstract: The present invention is related to the preparation and pharmaceutical use of novel benzamide derivatives as defined in the specification of formula (I) as histone deacetylase inhibitors (HDACI), their preparations and the methods of using these compounds or their pharmaceutically acceptable salt in the treatment of cell proliferative diseases, e.g.

Abstract: This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor.