Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

Abstract: The disclosure relates to a bituminous composition comprising at least one bitumen and at least one organogelling molecule taken alone or as a mixture, said organogelling molecule being represented by the following general formula (I): where: A represents an acyclic, cyclic or polycyclic, saturated or unsaturated, linear or branched hydrocarbon-based group having 3 to 92 carbon atoms, resulting from the polymerization of the side chains of at least one unsaturated fatty acid, X represents an NH group or an oxygen atom O, R1 represents a group chosen from: a linear or branched hydrocarbon-based group having 2 to 40 carbon atoms, optionally comprising one or more heteroatoms and optionally comprising one or more unsaturations, or a substituted or unsubstituted aromatic group, R2 represents a group chosen from: a hydrogen atom, a linear or branched hydrocarbon-based group having 1 to 40 carbon atoms, comprising one or more heteroatoms and optionally comprising one or more unsaturations, or a substituted or unsub

Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R1-3 are as defined in the specification.

Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.

Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4 and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.

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: The claimed invention relates to a process for preparing (meth)acrylates of N-hydroxyalkylated amides, in which open-chain N-hydroxyalkylated amides are esterified with (meth)acrylic acid or transesterified with at least one (meth)acrylic ester in the presence of at least one heterogeneous catalyst selected from the group consisting of an inorganic salt and an enzyme.

Abstract: Process for catalytically preparing (meth)acrylates of N-hydroxyalkylated amides and use thereof.

Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present invention provides HIV protease inhibitors of formulas I, IA, IB, Ib or II, or pharmaceutically acceptable salts thereof, wherein R2 may be, for example, 2-pyridyl-CH2—, 3-pyridyl-CH2—, 4-pyridyl-CH2—, a sulfonyl group as described in the formulas herein including benzenesulfonyl or thiophenesulfonyl groups, R2a—CO)—, R2a being selected from the group consisting of piperonyl, 2-pyranzinyl (unsubstituted or substituted with H, or an alkyl of 1 to 4 carbon atoms) or a picolylamine group as described herein, wherein R3 may be, for example, a phenyl group or diphenylmethyl group as described herein, and wherein Cx may be, for example, COOH, CONR5R6, CH2OH or CH2OR7.

Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The invention provides a crystalline freebase form 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 compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.

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: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them.

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 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 invention is a mitochondria-targeted antioxidant prodrug useful for the prevention or treatment of diseases or conditions associated with mitochondrial dysfunction resulting from changes in the mitochondrial redox environment. Antioxidant prodrugs of the invention are produced by modifying an antioxidant to a fatty acid so that the resulting prodrug is targeted to and activated by an enzyme of mitochondrial fatty acid beta-oxidation.

Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.

Abstract: The present invention is directed to imidazolidinone compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: This invention relates to a novel process for the preparation of optically pure L-(+)-ergothioneine. The process for the chemical synthesis of L-ergothioneine comprises steps which consist of reacting L-histidine alkyl ester with an acid halide, chloroformate or pyrocarbonate in the presence of a base, hydrolysis of the alkyl-(S,Z)-2,4,5-triamidopent-4-enoate to obtain a (S)-alkyl 2,5-diamido-4-oxopentanoate, acid catalyzed hydrolysis of the (S)-alkyl 2,5-diamido-4-oxopentanoate followed by reaction with a metal thiocyanate to obtain the thiohistidine, protection of the sulfur of thiohistidine as the tert-butyl thioether, dialkylation of the primary amine to obtain a tertiary amine, quaternization of the tertiary amine, and removal of the protecting group to obtain the desired (S)-3-(2-mercapto-1H-imidazol-5-yl)-2-(trialkylammonio)propanoate (I). This process affords a better yield and is capable of practical application at large scale.

Abstract: The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.

Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.

Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).

Abstract: This invention relates to benzonitrile derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R3 are defined in the description, to their use in medicine, and to compositions containing them. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof.

Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by inhibiting the activity of KSP are disclosed.

Abstract: The invention relates to new compounds, being 3-phenylpropionic acid derivatives of formula I wherein W represents COOH group or its bioisosters, or —COO—C1–C4-alkyl group; Y represents NH, N—C1–C10-alkyl, O, or S; Z represents NH, N—C1–C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N—C1–C10-alkyl, N-aryl, NSO2—C1–C10-alkyl, N—SO2-aryl, or N—SO2-heteroaryl; R1, to R6 each independently represent hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive; and pharmaceutically acceptable salts thereof. The compounds are the ligands of PPAR-gamma receptor and are useful as medicaments.

Abstract: This invention utilizes a mixed salt transesterification catalyst in a transesterification process for the production of esters of alkyl(meth)acrylate monomers.

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: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): that are prepared by reacting at least one (meth)acrylate of formula (II): with a heterocyclic alcohol of formula (III): in the presence of a catalyst comprising at least one compound (a) which is a chelate formed of lithium and of a 1,3-dicarbonyl compound. The invention also relates to a composition comprising compound (I) in solution in (meth)acrylate (II). Finally, the invention involves the use of the abovementioned composition in the preparation of polymers that can be used as coatings and adhesives, in the treatment of paper and of textiles, as agent for leather treatment and in the production of paints with high wet adhesion characteristics.

Abstract: A method for making a compound of formula (I) wherein 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; one of B1 and B2 is —CHR5—CHR6—C(Y)ZR7 and the other is absent; B3 is hydrogen; Y is O or S; Z is O, S or NR9; R5 is hydrogen or C1–C4 alkyl; R6 is hydrogen or C1–C4 alkyl; R7, R9 are independently hydrogen, alkyl, alkenyl, aryl or aralkyl. The method comprises steps of: (a) preparing an imidazolidinethione having formula by combining a cyanide source, a sulfide salt, and at least one ketone or aldehyde; and (b) adding to the imidazolidinethione, without isolation of the imidazolidinethione, CHR5?CR6—C(O)OR7.

Abstract: The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

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: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.

Abstract: The present invention is directed to a compound of Formula I: wherein A, R1, and R2 are defined herein. The present invention is also directed to compositions comprising compounds of Formula I, methods of using compounds of Formula I, and methods of making compounds of Formula I.

Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): that are prepared by reacting at least one (meth)acrylate of formula (II): with a heterocyclic alcohol of formula (III): in the presence of a catalyst comprising at least one compound (a) which is a chelate formed of lithium and of a 1,3-dicarbonyl compound. The invention also relates to a composition comprising compound (I) in solution in (meth)acrylate (II). Finally, the invention involves the use of the abovementioned composition in the preparation of polymers that can be used as coatings and adhesives, in the treatment of paper and of textiles, as agent for leather treatment and in the production of paints with high wet adhesion characteristics.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R1, R2, R3, R4, R5, R6, G and Z have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: The invention relates to a process for the preparation of alkylimidazolidone (meth)acrylates, generally expressed as compound (I): 1

Abstract: A dye-forming method comprising: reacting a dye-forming coupler and a color developing agent precursor represented by the following general formula (I): wherein A3 represents a group other than a hydrogen atom which leaves, accompanied by the bonding electron pair with the nitrogen atom in general formula (I), to thereby form a color developing agent; A2 represents a group which leaves in association with a dye-formation; and A1 represents a group which forms a dye together with the nitrogen atom and the coupler.

Abstract: The present invention discloses a method for producing angiotensin converting enzyme inhibitor of the following formula (I) and pharmaceutically acceptable salts thereof, in which a compound of the following formula (II), wherein R and R1 are defined as in the specification, is subjected to a de-protective reaction of silyl group in non-aqueous medium. This reaction is easily carried out only in the non-aqueous medium, so that by-product is minimized and the yield is high.

Abstract: An improved transesterification process is disclosed for forming certain (meth)acrylates by the transesterification of an alkyl (meth)acrylate with a hydroxyl alkyl imidazolidin-2-one using a transesterification catalyst in the presence of a polymerization inhibitor.

Abstract: It is provided carbapenem compounds represented by the following formula (I): wherein R is hydrogen atom, or substituted or unsubstituted lower alkyl group; and, n is an integer of 1 or 2, or a pharmaceutically acceptable salt thereof, and an antibacterial compositions containing these compounds as an active ingredient. These carbapenem compounds exhibit potent antibacterial activities and are excellent in the resistance against renal dehydropeptidase.

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: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X,  are as defined herein.

Abstract: The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.

Abstract: Substituted imidazolidine derivatives of the formula I, 1

Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Five-membered heterocycles having biphenylsulfonyl substitution, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the formula I in which the symbols have the meanings indicated in the claims, have outstanding antiarrhythmic properties and exhibit a cardioprotective component. They can preventively inhibit or greatly decrease the pathophysiological processes in the formation of ischemically induced damage, in particular in the elicitation of ischemically induced cardiac arrhythmias. Moreover, they have a potent inhibitory action on the proliferation of cells.