Abstract: The invention relates to a process for preparing chiral imidazolidin-2-ones of the formula I in which R1 is C1-C8-alkyl, cyclohexyl, phenyl, a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, C1-C6-alkylmercapto- or CF3-substituted phenyl radical, naphthyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy- or CF3-substituted naphthyl radical, R2 is C1-C8-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a phenyl-C1-C6-alkyl radical which may be substituted by a nitro, C1-C6-alkoxy, methylenedioxy or CF3 radical, and R3 is C1-C12-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, methylenedioxy-, dialkylamino- or CF3-substituted phenyl radical, by reacting a compound of the formula II or the salt thereof in which R1, R2 and R3 have the abovementioned meaning, with urea in the presence of an involatile ammonium salt, wherein the reaction is carried out in the presence of an aprotic polar organic solvent.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.

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 cardivascular 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 cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: The present invention encompasses compounds or Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as well as methods of using the same in the treatment of disorders, including osteoporosis, associated with enhanced bone turnover which can ultimately lead to fracture.

Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.

Abstract: The present invention describes novel 1,3-dihydro-imidazol-2-one or 1,3-dihydro-imidazol-2-thione compounds of formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate thereof, wherein A, L R1, R2, R3 and R4 are defined in the present specification, which are useful as selective inhibitors of MMP, TACE, aggrecanase or a combination thereof. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.

Abstract: Nonmetallic, chiral organic catalysts are used to catalyze the 1,4-addition of an aromatic nucleophile to an ?,?-unsaturated aldehyde. The aromatic nucleophile may be an N,N-disubstituted aniline compound, or an analog thereof. The reaction is efficient and enantioselective, and proceeds with a variety of substituted and unsubstituted aromatic nucleophiles and aldehydes. The invention also provides a method for the deamination of aromatic N,N-disubstituted amines such as those resulting from the 1,4-addition of an aromatic nucleophile to an ?,?-unsaturated aldehyde.

Abstract: A process for the preparation of benzylimidazole derivatives useful as intermediates for preparation of losartan, novel intermediates for their preparation and a process for the preparation of losartan.

Abstract: This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.

Abstract: The present invention provides a process for recovering 1,3-dimethyl-2-imidazolidinone comprising extracting 1,3-dimethyl-2-imidazolidinone from an aqueous solution containing it with n-butanol in the presence of an inorganic salt to obtain n-butanol layer and, subjecting the n-butanol layer to distillation. As 1,3-dimethyl-2-imidazolidinone can be recoverable at high purity from an aqueous solution containing 1,3-dimethyl-2-imidazolidinone easily and efficiently without using alkali, the present process is industrially advantageous.

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 cardivascular 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 cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: A composition comprising: (a) from 0.1% to 20% of at least one cyclic compound having a nitroxyl group and a thioamide group; and (b) a lubricating oil.

Abstract: This disclosure relates to a method for producing and using catalysts in the production of bisphenols, and in particular to a method for producing catalysts which contain poly-sulfur mercaptan promoters, and using these catalysts in the production of bisphenol-A and its derivatives.

Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.

Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or ?v?5 integrin.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: The present invention relates to novel trifluorobutenyl imidazole thioether derivatives of the following formula (I) wherein R1 represents hydrogen or halogen, R2 represents hydrogen, halogen or alkoxycarbonyl, R3 represents hydrogen, alkyl, alkenyl, cycloalkyl or aralkyl, and n represents 0,1 or 2, with the proviso that R1, R2 and R3 do not all represent hydrogen at the same time, to a process for their preparation and to their use as nematicides.

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

Abstract: A method is provided for the synthesis of nitramines and the recovery of the nitramines from a clathrate.

Abstract: There is provided a process for preparing a 1,3-dialkyl-2-imidazolidinone by using an alkylene oxide as a first component, using at least one of (A) carbon dioxide and a monoalkylamine; (B) a carbon dioxide compound of the monoalkylamine; and (C) an 1,3-dialkylurea, reacting the first and second components by heating at 50° C. or higher to give 1,3-dialkyl-2-imidazolidinone, characterized in that the total molar amount of a molar feed amount of the monoalkylamine included in the component (A), a molar feed amount of the monoalkylamine part of the carbon dioxide compound of monoalkylamine, component (B), and the double of a molar feed amount of the 1,3-dialkylurea, component (C), is at least three folds of a molar feed amount of the alkylene oxide. The preparation process of this invention uses an industrially readily available alkylene oxide as a starting material and can be suitably conducted with a higher yield in an industrial scale.

Abstract: The invention relates to novel substituted benzoylcyclohexanediones of the general formula (I) in which A1 represents a single bond or represents alkanediyl (alkylene) having 1 to 3 carbon atoms, A2 represents alkanediyl (alkylene) having 1 to 3 carbon atoms, and R1, R2, R3, R4 and R5 are each as defined in the description, and to novel intermediates, to processes for their preparation and to their use as herbicides.

Abstract: Compounds of Formula 1 1

Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr;,&bgr;-unsaturated aldehydes. The catalysts are chiral imidazolidinone compounds having the structure of formula (IIA) or (IIB) or are acid addition salts thereof, wherein, in one preferred embodiment, R1 is C1-C6 alkyl, R2 is tri(C1-C6 alkyl)-substituted methyl, R3 and R4 are hydrogen, and R5 is phenyl optionally substituted with 1 or 2 substituents selected from the group consisting of halo, hydroxyl, and C1-C6 alkyl. The chiral imidazolidinones are useful in catalyzing a wide variety of reactions, including cycloaddition reactions, Friedel-Crafts alkylation reactions, and Michael additions.

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): 1

Abstract: Compounds of formula I: t,0010

Abstract: Compounds which are 3-arylsulfonyl-2-methyl propanoic acid derivatives of formula (I): wherein X is HO—NH— or HO—, R1 is selected from phenyl, 4-chlorophenyl, 4-florophenyl, 4-cyanophenyl, benzamido (i.e., —NH—CO-Ph) and benzamido substituted on the terminal phenyl ring by C1-C4 alkyl, fluoro, chloro, cyano or C1-4 alkoxy; R2 is selected from (a) —S—Ar or —S—CH2—Ar wherein Ar is an aromatic moiety; (b) —O—Ar wherein Ar is as defined above; (c) —S-Het or —S—CH2-Het wherein Het is a heterocyclic ring; and (d) 2,5-dioxo-1-imidazolidinyl or 2,4-dioxo-1-imidazolinyl; and the pharmaceutically acceptable salts thereof; have potent and selective inhibitory activity against matrix metalloproteinases (MMPs) and can thus be used in the treatment and prevention of diseases mediated by MMPs.

Abstract: This invention discloses and claims diary heterocycles of formula (I) 1

Abstract: Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

Abstract: A dye-forming coupler and compound of formula (I): formula (I) 1

Abstract: The invention relates to 2-thio-substituted imidazole derivatives of the formula I 1

Abstract: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.

Abstract: A composition comprising a compound of formula I: wherein W represents O, S—A2, or two groups, R3 and R4; bonds a and b are single or double bonds, provided that one of a and b is a single bond and the other is a double bond; c is a single or double bond, and d is a single bond, double bond, or two single bonds, provided that d is a single bond when c is a double bond, d is not a single bond when c is a single bond, and W is R3 and R4 when d is two single bonds; A1, A2, B1 and B2 are independently hydrogen, alkyl, alkenyl, aralkyl or one of the groups depicted in Scheme 1: and a dithiophosphate.

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 o

Abstract: This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at

Abstract: The continuous production of acetylene diurea takes place by means of the reaction of glyoxal with urea in the presence of mineral acids. The reaction is carried out in at least one reactor having a mixing device, into which glyoxal, urea, and mineral acid are continuously fed, and from which a suspension of acetylene diurea in mother liquor is discharged. The acetylene diurea is mechanically removed from the mother liquor, and the remaining mother liquor is recycled back into the reactor, in whole or in part.

Abstract: A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders.

Abstract: Heterocyclic compound represented by the formula I 1

Abstract: A convenient one step synthesis of N-substituted 2-sulfanylimidazole from an isothiocyanate, an &agr;-aminocarbonyl compound and an alkyl halide or an activated aryl halide is described. Reaction of an isothiocyanate with an &agr;-aminocarbonyl compound affords a thiourea acetal intermediate, which without isolation or purification affords the desired N-substituted 2-sulfanylimidazole upon treatment with an alkyl halide or an activated aryl halide.

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: Nonmetallic, chiral organic catalysts are used to catalyze the 1,4-addition of an aromatic nucleophile to an &agr;,&bgr;-unsaturated aldehyde. The aromatic nucleophile may be an N,N-disubstituted aniline compound, or an analog thereof. The reaction is efficient and enantioselective, and proceeds with a variety of substituted and unsubstituted aromatic nucleophiles and aldehydes. The invention also provides a method for the deamination of aromatic N,N-disubstituted amines such as those resulting from the 1,4-addition of an aromatic nucleophile to an &agr;,&bgr;-unsaturated aldehyde.

Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereosomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Compounds of the formula: 1

Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.

Abstract: Nonmetallic organic catalysts are provided that facilitate the enantioselective reaction of &agr;,&bgr;-unsaturated ketones.

Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.

Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.