Abstract: The present patent discloses a novel, efficient and transition-metal-free room temperature single step process for synthesis of aryl sulfones and substituted aryl sulfones starting from aryl substrates.

Abstract: A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.

Abstract: The invention relates to the use of a derivative compound of 1,3-benzodioxole of formula (I) wherein R is a linear or branched (C4-C10) alkyl substituent as a synergistic compound of insecticidal active ingredients insecticidal compositions comprising at least one compound of Formula (I) and at least one insecticidal active ingredient are also described.

Abstract: Disclosed herein are substituted quinoxaline carboxylic acids of Formula (I): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.

Abstract: The invention provides compounds of formula (I): Said compounds being modulators of Kv3 channels and of use in the prophylaxis or treatment of related disorders.

Abstract: The present invention relates to methods for the treatment of a pathology associated with hyperglycaemia, particularly diabetes, by administering quinoxalinone compounds of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in the claims. The compounds have activity as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone compounds for modulating insulin secretion in insulin-1 cells by contacting the cells with the compounds.

Abstract: Arylpyrazinone derivatives of formula (I), as insulin secretion stimulators, the preparation and use of these pyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

Abstract: The present invention is a method for the treatment of alcohol abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and/or formula (II) as herein defined.

Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

Abstract: A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.

Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.

Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.

Abstract: The present invention relates to quinoxalinone derivatives of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein, as insulin secretion stimulators. Specific such quinoxaline compounds are also an aspect of the invention. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.

Abstract: There is provided a nitrile compound having an excellent controlling effect on arthropod pests represented by the formula (I): wherein m represents in integer of 0 to 4; n represents an integer of 1 to 4; q represents an integer of 0 to 4; Q represents a C1-C4 fluoroalkyl group; Z represents an optionally substituted C2-C6 alkynyl group or a ?N—OR3 group; R1 and R2 independently represent a monovalent C1-C4 chain hydrocarbon group optionally substituted with a halogen atom, etc.; and A represents an optionally substituted monovalent C1-C6 chain hydrocarbon group, etc.

Abstract: A series of derivatives of 6,7-dihydro-3H-oxazolo[3,4-a]pyrazine-5,8-dione, mixtures thereof, their pharmaceutically acceptable salts, which are inhibitors of PDE-5, possessing vasodilatator properties and relaxing effects. In particular, compounds of formula (I), where R1, R2, R3, and R4 are defined herein, processes for the preparation of said compounds, pharmaceutical compositions containing them, as well as uses as inhibitors of the enzyme phosphodiesterase type 5 (PDE-5) in the treatment of the erectile dysfunction and PDE-5 inhibitor treatable disorders.

Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

Abstract: The present invention relates to compounds of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.

Abstract: A production method of fluorinated compounds, for producing a compound represented by formula (3) in a fluorine-based solution in a flow of fluorine gas after reaction of at least one type of compounds represented by formula (1) and at least one type of compounds represented by formula (2). Similarly, fluorinated compounds represented by formula (4) prepared by the fluorination of compounds obtained by the reaction of formula (1) and formula (2)?. The fluorinated polymers obtained by the polymerizations of formula (3) and (4) compounds are useful as an optical or electrical materials. wherein R1, R2, R3, R4, Rff1, Rff2, Rff3, Rff4, X, Y, Z, and n are defined in the specification respectively.

Abstract: This invention relates to a novel compound extracted from antrodia Cinnamomea and related compounds of formula (1), and pharmaceutical compositions comprising the compound of formula (1) and a pharmaceutically acceptable carrier or excipient. The invention further comprises the method of inhibit cancer cells by administering an effective amount of the compound of formula (1).

Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: A method for producing an olefin compound represented by the formula (2): wherein R1 and R2 are the same or different, and independently represent an alkyl group or the like, with the proviso that R1 and R2 are not hydrogen atoms at the same time, R3 represents an alkyl group or the like, which comprises contacting a palladium catalyst with an ?,?-unsaturated aldehyde compound represented by the formula (1): wherein R1, R2 and R3 are the same as defined above, in the presence of an inorganic base.

Abstract: The present invention relates to a pharmaceutical composition, a food composition or a cosmetic composition, containing one or more kinds of a compound represented by the following formula (I?) wherein R1 is a hydrogen atom, a hydroxyl group, a methoxy group or an ethoxy group, R2 is a hydroxyl group, a methoxy group or an acetoxy group, or R1 and R2 in combination optionally form a methylenedioxy group, R is represented by the following formula wherein Y is an ethylene group or a vinylene group, m and n are each an integer of 0 to 7, which satisfy m+n=2 to 8, and R3 and R4 are each independently a hydrogen atom, a methyl group or an ethyl group, provided that, (1) when R1 is a methoxy group, then R2 is not a hydroxyl group; and (2) when R1 is a hydroxyl group, then R2 is not a hydroxyl group and an acetoxy group.

Abstract: A compound has Formula VIII where, X is —C(O)R, —C(O)OR, —CN, —NO2, —S(O)2R?, —P(O)(OR)2; each R is individually H, alkyl, or alkenyl; R? is alkyl or akenyl; R1 is aryl, alkenyl, arylalkenyl, heterocyclyl, or heteroaryl; and R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are individually H, alkoxy, or hydroxy. In some cases, X is NO2. Pharmaceutical compositions of the compound of Formula VIII with a pharmaceutically acceptable carrier may be prepared. The compounds may be used for inhibition of cyclooxygenase-2.

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: A ?-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X?N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The ?-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: A compound of the formula I in which X and Y are selected as follows: (i) X is H and Y is selected from the group consisting of (ii) X and Y together form a bivalent radical selected from the group consisting of —O—CH2—O—, —N?CH—O— and —N?CH—S— thus forming together with the carbon atoms to which the radical is attached a 5-membered ring. The compounds have cooling properties and are useful in, for example, foodstuffs, dentifrices and cosmetics.

Abstract: The invention relates to a method for producing optionally substituted methylenedioxybenzene. The invention particularly relates to the production of methylenedioxybenzene. The inventive production method is characterized by the fact that it involves the reaction of an optionally substituted catechol with an aldehyde in the presence of a solid acid catalyst selected among: a titanium silicalite and a zeolite that is doped with tin and/or titanium.

Abstract: Compounds of formula I, wherein X, a, b, R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.

Abstract: A positive resist composition including a base component (A) which exhibits increased solubility in an alkali developing solution under the action of acid and an acid generator component (B) which generates acid upon exposure, wherein the base component (A) includes a polymeric compound (A1) having a structural unit (a0) containing an acid-dissociable, dissolution-inhibiting group, and the acid-dissociable, dissolution-inhibiting group has a 1,3-dioxole skeleton.

Abstract: The present invention provides appropriately substituted chalcones, such as, for example, represented by the structural formula as shown herein below Wherein R1, R2 and R3 are selected from the group consisting of H, OH, O-alkyl, O-phenyl and O-substituted phenyl; B represents Ar—Z—O or RO; where Z is an alkane having up to 5 carbon atoms; R is substituted propanol amino, wherein substituted amino groups are selected from the group consisting of t-butyl, n-butyl, i-butyl, i-propyl, 4-phenyl piperazine-1-yl, 4-(2-methoxyphenyl)-piperazin-1-yl and 3,4-dimethoxy phenethyl; and Ar is thiazolidine-dione methylene phenoxy. The compounds prepared have been demonstrated to exhibit significant antidiabetic effect in various animal models indicating potential for further exploitation.

Abstract: Methods for removing safrole from a sample, molecular imprinted copolymers that bind safrole, and methods of making the same are provided.

Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.

Abstract: Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.

Abstract: The present invention relates to new amino acid derivatives, process for the production, their use, in particular in transplantation, and pharmaceutical compositions containing them.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: Provided herein are substituted PDE5 inhibitors of Formula 1, and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function.

Abstract: 7-substituted fused ring tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted fused ring tetracycline compounds are described.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

Abstract: A process for the production of a substance or composition for the therapeutic or prophylactic treatment of erectile dysfunction or the enhancement of libido in a male human or animal subject comprises the step of formulating the substance or composition from at least one of plant material and an extract of plant material of at least one plant species of the family Geraniaceae.

Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.

Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.

Abstract: The invention relates to a process for preparing difluorobenzo-1,3-dioxole-5-carboxylic acid and derivatives thereof, and to the use thereof for preparing medicaments and crop protection agents.

Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.

Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.