Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.

Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Abstract: The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.

Abstract: The present invention provides compounds that can inhibit the activity of soluble epoxide hydrolases. In particular, the present invention provides compounds of Formula I.

Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.

Abstract: Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions.

Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: The present invention is directed to compositions which contain a combination of at least one histone deacetylase inhibitor (HDAC inhibitor) and a retinoid. The composition is in particular a cosmetic preparation. It was found that the combination of an HDAC inhibitor and retinol or a derivative thereof is in particular useful for treating wrinkles but also for thickening the epidermis and for improving hair growth.

Abstract: The use of a compound of formula (I) wherein X is (i), (ii) or (iii), where the substituents have the meanings assigned to them in claim 1, or compositions containing them in controlling insects, acarines, nematodes or molluscs. Novel compounds are also provided.

Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.

Abstract: The present invention provides new compounds of formula I, wherein Q, R1, R2, R4, R5, R6, Xi, R7, R8, M and G1n are defined as in formula I; invention compounds are modulators of follicle-stimulating hormone—(“FSH”) which are useful for male and female contraception as well as other disorders modulated by FSH receptor.

Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Abstract: A method for treating a cytotoxic disease by administrating compounds having a general formula X-(A)n-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an RaCO, RaOCO, RaNHCO or RaSO2 group, Ra being an alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl group, the groups being substituted or not, on condition that X is different from H when n is equal to 6; A denotes either a group having formula (I) or (II), wherein Ri is a hydrogen atom, an amino acid side chain, an alkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl group, said groups being substituted or not, i being an integer of between 1 and n; Y is an NRbRc, Rb and Rc group having the same meaning as given earlier for Ra.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as Parkinson's disease, and the manufacture of medicaments for such treatment.

Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.

Abstract: The present invention relates to new sulfonylurea inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-car-boxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl.

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: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.

Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans,trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.

Abstract: This invention relates to the use of a combination of selected substances in paint to prevent the settlement and growth of different biofouling organisms with a reduced negative effect on the ecosystems compared to present methods.

Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Abstract: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The invention relates to sulfonamido derivatives of formula (I) wherein R1-R7 are as defined in the description. Compounds (I) antagonize the vanilloid receptor and can be used for the preparation of medicaments for the treatment of inflammatory states.

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: One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.

Abstract: Biphenyl derivatives represented by the following formula (1): wherein R1 represents a C5-7 alkyl group, R2 represents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, R3 represents a tetrazolyl group, —NHCOCF3, —NHSO2CF3 or —SO2NHCONHR4 in which R4 represents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a C1-4 alkylene group or —SO2NH—, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.

Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.

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: 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: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.

Abstract: Highly concentrated, water-based dispersions of certain lipophilic and/or hydrophobic antimicrobially active materials are stabilized to a surprising degree by a surfactant combination including a nonionic acrylic graft copolymer surfactant and a alkoxylated polyarylphenol phosphate ester surfactant. The active materials may be present in dispersion concentrates of the present invention singly or in useful combinations. The active materials are selected from the group of fungicides and bactericides consisting of 1,2-benzisothiazol-3(2H)-one; 2-octyl-2H-isothiazol-3-one; 5-chloro-2-methyl-2H-isothiazol-3 -one; 2-methyl-2H-isothiazol-3-one; pyrithione zinc; 3-iodo-2-propynyl butylcarbamate; 2-methylthio-4-ethylamino-6-tert-butylamino-s-triazine; and 3-(4-isopropylphenyl)-1,1-dimethylurea, and mixtures thereof. The dispersion concentrates may be efficiently shipped and stored, and subsequently diluted with water to produce less concentrated dispersions when desired.

Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antinflammatory, antiarthritic and antiviral activity.

Abstract: Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A? and A? are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.

Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receotor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.

Abstract: Methods for evaluating the antiviral activity of test compounds are provided. Further aspects of the methods involve the retroviral capsid protein of HIV-1. In another aspect, methods of reducing mortality associated with AIDS with a compound that binds to the apical cleft near the C-terminal end of the N-terminal domain of the HIV-1 capsid protein are provided. Derivatives of CAP-1, CAP-2, CAP-3, CAP-4, CAP-5, CAP-6 and CAP-7 are described that bind to the apical cleft of the N-terminal domain of the HIV-1 capsid protein and inhibit proper assembly of the core particle.

Abstract: The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.

Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.

Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.

Abstract: The present invention describes compounds comprising new and useful peptides and peptidomimetics that can bind to CD23. They are capable of reducing inflammatory responses associated with auto-immune diseases, chronic inflammatory diseases, allergies and other inflammatory conditions such as those mediated by the mammalian immune system. Compounds of the present invention relate to a CD23-binding peptide wherein said peptide comprises an amino-acid sequence of X1,-X2- X3-X4-X5-X6-X7-X8, wherein: X1 is Phe, or is absent; X2 is His or Ala; X3 is Glu, Ser, Ala, Asn, Lys, or Cys; X4 is Asn, Phe, Gln, Pro, Ser, or Ala; X5 is Trp; X6 is Pro, Arg, Glu, Gly, Cys, or Lys; X7 is Ser, Pro, Leu, Thr Ala, Gly, Asn, or absent; and X8 is Phe, Gly, or is absent.

Abstract: Compounds of the formula or a pharmaceutically acceptable salt thereof or a tautomer thereof, wherein A and B are as described herein, are useful for treating conditions afflicting mammals.

Abstract: The present invention relates to novel selective inhibitors of the urokinase plasminogene activator (uPA, EC3,4.21.31) of the aryl guanidine type.

Abstract: The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment.

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: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.