Abstract: The present invention relates to a compound of the formula (1): wherein R1 is group of the formula (2): (wherein X is nitrogen atom or C(R5), Y is nitrogen atom or C(R6), R5 and R6 are each independently hydrogen atom, etc.) etc., m is 1 to 6, L1 is single bond, etc., R2 is hydrogen atom, substituted or unsubstituted alkyl group, etc., R3 is hydrogen atom, etc., L2 is single bond, etc., R4 is hydrogen atom, substituted or unsubstituted aryl group, etc., or pharmaceutically acceptable salt thereof, being useful for preventing or treating Alzheimer's disease.

Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

Abstract: The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kv1.5 potassium channel inhibitors, and to methods for treating cardiac arrhythmia.

Abstract: Disclosed herein is a method of treating sensorimotor disorders comprising administering to a subject in need of such treatment an alpha-2 receptor agonist lacking significant alpha-2A receptor activity.

Abstract: The present invention provides heterocyclic derivatives hat modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are used to activate alpha2 adrenergic receptors. The compounds of Formula 1 are incorporated in pharmaceutical compositions and are used as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors.

Abstract: The present invention relates to compounds that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. In certain embodiments, the compounds of the invention relate to aryl oxoimidazolidinyls.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: Imidazolone derivatives, as medicaments, of formula wherein: R1?H, C1 to C5 alkyl, aryl or a 5- or 6-membered heterocyclic group; Ar1=optionally substituted aryl or an aromatic heterocycle; R?R2—S—, R3—HN—, R4COHN or Ar2, with R2=a C1-C5 alkyl, vinyl or vinyl(C1-C5)alkyl, nitrile or nitrile(C1-C5)alkyl, aryl or benzyl radical, which are optionally substituted; R3=the meanings given above and H; Ar2=substituted or unsubstituted aryl.

Abstract: Disclosed herein is a method of treating motor disorders comprising administering to a subject in need of such treatment 4-(1-(2,3-dimethylphenyl)ethyl)-1H-imidazole-2(3H)-thione.

Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.

Abstract: Compositions comprising ergothioneine and a trimethylamine absorber are provided. Also provided are methods for preventing, reducing or minimizing the fishy, amine odor, due to trimethylamine, that is associated with the processing and/or storage of a preparation containing ergothioneine, by combining with the ergothioneine, during processing or prior to storage, a trimethylamine absorber in an amount sufficient to prevent the detection of any trimethylamine odor by the human nose. A method is further provided for ameliorating the methylamine odor associated with an aqueous ergothioneine-containing preparation after it has developed a fishy trimethylamine odor.

Abstract: The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.

Abstract: In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.

Abstract: Novel PDF inhibitors and novel methods for their use are provided.

Abstract: The tyrosinase inhibiting compounds of the following general formula formulated into pharmaceutical or cosmetic compositions, are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.

Abstract: The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2? are independently H or (C1-3)alkyl; or R2 and R2? form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y represents or NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer

Abstract: Novel 4-heteroarylimidazole-2-thione tyrosinase inhibiting compounds corresponding to the following general formula (I): formulated into pharmaceutical or cosmetic compositions are useful for the treatment or prevention of pigmentary disorders, or for preventing and/or treating signs of skin aging, and/or for body or hair hygiene.

Abstract: Certain substituted amino heterocyclic and heteroaryl derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein R, R1, R2, R3, R4, A, B and Q are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of an additional compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: The invention relates to composition and related therapeutic methods including at least one antihyperthyroid drug formulated for transdermal administration. Because the formulation is formulated for transdermal administration, the formulation is easier to administer than existing formulations which are administered orally to animals. Issues surrounding transdermal administration versus oral administration have also been resolved allowing the agent to remain stable during storage and retain a high level of efficacy.

Abstract: Compounds of formula I and a method for their preparation are described, where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or alkyl heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

Abstract: This invention relates to non-natural desamino amino acid compounds, methods of making, and peptides containing these compounds as their N-terminus moieties. A preferred example is neurotensin (8-13) in which the N terminus is an alpha desamino N,N dimethyl homolysine residue.

Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.

Abstract: The present disclosure relates to methods of treating a stimulant addiction of a patient comprising administering to a patient in need a therapeutically effective dose of a selective dopamine ?-hydroxylase inhibitor thereby decreasing stimulant reward, inducing aversion for the stimulant or preventing relapse in the patient. The disclosure further encompasses methods whereby a therapeutically effective dose of a selective dopamine ?-hydroxylase inhibitor is determined by: characterizing the genetic profile of the patient with respect to the gene encoding dopamine ?-hydroxylase, a polymorphism therein correlating to the level of endogenous dopamine ?-hydroxylase activity in the patient before administering the therapeutic agent.

Abstract: The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).

Abstract: Compositions comprising a mixture of (a) a major amount of solid halogen-containing sanitizer material and (b) a minor amount of calcium oxide modified particulate boric acid, the amount of calcium oxide modified particulate boric acid being sufficient to enable the composition to be classified as a class 1 or class 2 NFPA oxidizer are described. Also described is particulate boric acid at least a portion of the particles thereof having on their surface at least a partial coating of calcium oxide, and a method for preparing such coated particulate boric acid.

Abstract: A compound of formula Ia: The present invention relates to novel indazolyl derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments

Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders/diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: The present invention is directed to novel cyclohexylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the prolongation of time until onset of clinical symptoms in patients having an asymptomatic (occult) heart failure or for the reduction of heart size in patients having symptomatic or asymptomatic (occult) heart failure.

Abstract: Compounds corresponding to the following general formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine or else into cosmetic compositions; novel compounds of formula (II) are also thus useful:

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The invention is concerned with novel imidazolidine derivatives of formula (I) wherein R1 to R3, A, D and E are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: The present application relates to novel, substituted 4-arylimidazol-2-ones and 5-aryl-1,2,4-triazolones, processes for the production thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases and the use thereof for the production of medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.

Abstract: The present application describes nitroimidazolic derivative compounds with antibacterial and/or antiprotozoal activity, which are potent urease inhibitors. It also describes the process for preparing those compounds and their use in pharmaceutical compositions and medicines.

Abstract: This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases.

Abstract: Therapeutic and prophylactic treatments of aquatic species and aquatic diseases through the controlled introduction of a heterocyclic N-halamine into an aquatic habitat.

Abstract: The invention relates to a method for inhibiting the biological acidification of water which is in contact with materials containing sulfur in reduced form or with elemental sulfur, susceptible to oxidation on the part of Thiobacilli, comprising putting said materials in contact with soluble inorganic salts at concentrations ranging from 0.4 normal to saturation.

Abstract: The present invention relates to the use of new beta-agonists of general formula (Ia) or (Ib) wherein the groups R1 to R12 and R1 to R7, respectively, have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, for preparing a medicament for the treatment of overactive bladder.

Abstract: A combination comprising at least two components selected from: (i) compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof, wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; the term halogen means fluorine, chlorine, bromine or iodine; and (ii) at least one compound from the following classes of compounds: diuretics; beta-adrenergic antag

Abstract: There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.

Abstract: The present invention is directed to novel imidazolidin-2-one derivatives having a structure according to Formula I wherein a, b, R1, R2, R3, and R4 are as defined above, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R?, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.

Abstract: A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or alkycarboxylate group to provide said 4-substituted imidazole 2-one or thione.

Abstract: The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.

Abstract: The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(?O)—O—R6, C(?O)—NR7aR7b, C(?S)—NR7aR7b, S(?O)2—NR7aR7b or C(?O)—R8; R4 represents hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy or C1-6alkyloxy, C(?O)—O—R6, C(?O)—NR7aR7b, C(?S)—NR7aR7b, S(?O)2—NR7aR7b or C(?O)—R8; or R3 and R4 taken together may form a bivalent radical of formula —C(?O)—NH—NH—C(?O)—; n is 1, 2, 3, 4 or 5; provided that at least one of R3 or R4 is other than hydrogen; and