Abstract: Platinum(II) complexes with various selones (L) having the general formula PtL2Cl2 are disclosed. The platinum(II) complexes of the invention inhibit growth of cancer cells in vitro and are useful for treatment of proliferative disorders such as cancers and/or tumors.

Abstract: Provided is a solvent or solvent composition for organic transistor production that is excellent in solubility of an organic semiconductor material and that can form an organic transistor high in crystallinity. The solvent or solvent composition for organic transistor production according to the present invention is a solvent or solvent composition for organic semiconductor material dissolution, including a solvent A represented by the following formula (A). In the formula (A), R1 to R4 are the same or different, and represent a C1-2 alkyl group. R1 and R4 may be bound to each other to form a ring together with —N(R2)—C(?O)—N(R3)— in the formula.

Abstract: Methods for the synthesis of 2-thiohistidine or a derivative thereof of the formula (I), or of a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, from a compound of the formula (II) or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, by cleavage reaction in the presence of a thiol at a temperature higher than or equal to 60° C. The invention also relates to compounds of the formula (II) and a method for the synthesis thereof.

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 of the Formula (I) 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: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

Abstract: Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.

Abstract: The invention relates to a process for the synthesis of N-substituted cyclic alkylene ureas by reacting a multifunctional aliphatic amine A having at least two amino groups which may be primary or secondary, at least one of which is a primary amino group, —NH2, and at least one of which is a secondary amino group, >NH, the other hydrogen group whereof having been substituted by a hydrocarbyl group which in turn may be substituted by a hydroxyl group, or an amino group, or a carboxyl group, or a ketone carbonyl group, or a hydrazide or hydrazone group, or a mercaptan group, and at least one further functional group selected from the group consisting of primary or secondary amino groups and hydroxyl groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA.

Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.

Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.

Abstract: The present invention relates to chemical compounds comprising a [Y(CHRa)n—CH(Ra)SO3]? anion, their preparation and application. The chemical compounds are preferably ionic liquids.

Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

Abstract: The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.

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: 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 present invention relates to novel substituted (thiophenyl-carbonyl)imidazolidinones, methods for their production, their use for the treatment and/or prevention of diseases, as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, especially retroviral diseases, in humans and/or animals.

Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.

Abstract: The present invention provides a compound of formula I: said compound is inhibitor of aldosterone synthase (CYP11B2), and/or 11 beta-hydroxylase (CYP11B1), and/or aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase, aromatase, or CYP11B1. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.

Abstract: There is provided a method for manufacture of 2-oxoimidazolidines of Formula I comprising one or more of the steps of converting an amine to an acylation agent, condensation of the acylation agent with a bi-functional compound of structure L-C(R4)(R5)—C(R2)(R3)—NHR1, wherein L is a leaving group, and ring closure of the resulting urea. In this manner, certain 2-oxoimidazolidines may be manufactured that are useful intermediates for the production of Pramiconazole and structurally related compounds.

Abstract: The present invention provides 3- to 7-membered 1,3-diaza-4-oxo-heterocyclic derivatives, such as imidazolidinone O derivatives, capable of releasing in a controlled manner a biologically active aldehyde or ketone in the surrounding. The invention also relates to the use of these compounds as perfuming or flavoring ingredients, as well as to the perfuming compositions and consumer articles containing such derivatives. It also provides a process for preparing said derivatives of the invention.

Abstract: The present disclosure relates to a method for synthesizing ergothioneine or one of the derivatives thereof of following formula (I): or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in all proportions thereof, from a compound of betaine type of following formula (II): or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in all proportions thereof, by cleavage reaction in the presence of a thiol, at a temperature above or equal to 60° C. The present disclosure also relates to compounds of formula (II) and the method of synthesis thereof.

Abstract: The invention provides a micronized 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid having improved stability. The invention also provides pharmaceutical compositions comprising the stable micronized compound, processes for preparing the stable micronized compound, and methods of using the stable micronized compound to treat diseases such as hypertension.

Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds 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 process and intermediates for preparing such compounds.

Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.

Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.

Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.

Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

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 invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds 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 process and intermediates for preparing such compounds.

Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R6 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.

Abstract: Novel 4-phenylimidazole-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: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These 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 alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These 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 alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These 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 alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.

Abstract: Described are compositions and methods for regulating plant growth that use a complex of an imidazolinone ion and a metal counterion; the compositions and methods include methods of regulation plant growth, optionally in combination with herbicidal, fungicidal, and fertilizer compositions and effects.

Abstract: A disinfecting, nonbleaching N-halamine for use in contact lens soaking solutions. The N-halamine compound is soluble in water and contact lens formulation solutions to the extent necessary to provide disinfection, but not to cause significant bleaching of dye materials incorporated into the contact lenses.

Abstract: The invention provides a method of conditioning azo pigments containing carboxylic ester groups, using glycol monoalkyl ethers or mixtures of glycols and glycol dialkyl ether.

Abstract: Compounds of the invention are disclosed, such as compounds of formulae LX-LXIV, and pharmaceutically acceptable salts, isomers, or prodrugs thereof, which are useful as modulators of the activity of liver X receptors (LXR) and Farnesoid X receptors (FXR), where R00, R200, R400, R500, J11, J21, G1, G21, and Q are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

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: Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

Abstract: A process for producing an ?-hydroxyketone compound, which comprises subjecting an aldehyde compound to a coupling reaction in the presence of an alkoxyimidazolidine compound represented by the formula (1) wherein R1? and R2? independently represent a hydrogen atom, etc., R3? and R4? independently represent a substituted or unsubstituted aryl group, etc. and R5? represents an alkyl group.

Abstract: Chemiluminescent substances are prepared by freezing or lyophilizing a solution of a peroxidized nitrogen-containing five-membered cyclic compound. The chemiluminescent substances have a sensitivity comparable to that of luminol chemiluminescence, are highly water-soluble, have no incorporation of impurities, are not degraded during storage, have high reproducibility in measurement results, and are very suitable for use in the detection and quantification of various substances in many applications, e.g., clinical applications.

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: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.