Abstract: The invention concerns a method for preparing an oxysulphide and fluorinated derivative, said method comprising the reacting, in the presence of an organic solvent, of: i) at least one compound of formula Ea-COOR (I), in which Ea represents the fluorine atom or a group having 1 to 10 carbon atoms chosen from fluoroalkyls, perfluoroalkyls and fluoroalkenyls and R represents hydrogen, a monovalent cation or an alkyl group, and ii) a sulphur oxide, said method being such that the initial molar ratio (sulphur oxide/compound of formula (I)) is less than 0.4 and the concentration of sulphur oxide dissolved in the reaction medium is kept constant for the entire duration of the reaction to a value of between 0.2% and 3% by weight by means of continually adding said sulphur oxide to the reaction medium.

Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

Abstract: There is provided a method for preparing oligomers and co-oligomers of highly fluorinated sulfuric acids and salts thereof.

Abstract: Useful processes for isolating the fluorinated products formed by reaction with 4-tert-butyl-2,6-dimethylphenylsulfur trifluoride (Fluolead) are disclosed. The processes comprise the conversion of the byproduct (formula I) to sulfinate ester (formula V), and to sulfonate eater (formula VI), and then to the water-soluble sulfonate salt (formula IV) in the presence of the fluorinated products.

Abstract: The present invention provides new ruthenium complexes of Formula (1), which contain a chelate ring created by a halogen atom X. The invention concerns also a method for the preparation of the new ruthenium complexes and their application in metathesis reactions.

Abstract: The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.

Abstract: There is provided a method for preparing oligomers and co-oligomers of highly fluorinated sulfuric acids and salts thereof.

Abstract: A method for preparing fluoroalkanesulphinic acid esters is described. The preparation of esters of trifluoromethanesulphinic acid, commonly referred to as “triflinic acid,” is also described. A method for preparing a fluoroalkanesulphinic acid ester is also described wherein the method includes reacting a fluoroalkanesulphinic acid with an organic carbonate leading to the formation of a fluoroalkanesulphinic acid ester and carbon dioxide, which is removed during the reaction.

Abstract: According to the method for producing fluorine-containing N-alkylsulfonylimide compound, the fluorine-containing N-alkylsulfonylimide compound can be produced safely with a high recovery rate by alkylating fluorine-containing sulfonylimide acid or fluorine-containing sulfonylimide acid salt with dialkylsulfuric acid or dialkylcarbonic acid.

Abstract: Oxysulfide and fluorinated organic compounds, for example, perfluoroalkanesulfinic and sulfonic acids, and preferably trifluoromethanesulfinic and trifluoromethanesulfonic acids in salt form, are prepared by reacting, in the presence of an aprotic polar organic solvent: (i) a fluorocarboxylic acid having the formula Ea-CF2—COOH (I), wherein Ea is an atom or an electroattracting group at least partially forming a salt with an organic or inorganic cation; with (ii) a sulfur oxide, preferably sulfur dioxide, and further wherein the ratio of the number of moles of sulfur oxide to the number of moles of fluorocarboxylic acid is less than 1, preferably less than 0.99.

Abstract: A method for preparing fluoroalkanesulphinic acid esters is described. The preparation of esters of trifluoromethanesulphinic acid, commonly referred to as “triflinic acid,” is also described. A method for preparing a fluoroalkanesulphinic acid ester is also described wherein the method includes reacting a fluoroalkanesulphinic acid with an organic carbonate leading to the formation of a fluoroalkanesulphinic acid ester and carbon dioxide, which is removed during the reaction.

Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).

Abstract: Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or builing blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.

Abstract: A method for covalently binding target molecules to carbon nanoparticles via at least one bridge molecule includes converting carbon nanoparticles to acyl carbon nanoparticles using a carbonyl compound of the at least one bridge molecule in the presence of a Lewis acid under Friedel-Crafts conditionsm, where the acyl carbon nanoparticles include a nucleofuge in the omega position. The target molecule is covalently bound to the acyl carbon nanoparticles via nucleophilic substitution of the nucleofuge in the omega position.

Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.

Abstract: Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or building blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.

Abstract: Aspects of the present invention relate to compounds for preparing fluorocarbon compounds, methods for preparing fluorocarbon compounds, and methods for purifying a mixture of compounds. One aspect of the present invention relates to a trivalent iodonium fluorocarbon. The trivalent iodonium fluorocarbon compound of the invention is useful for attaching a fluorocarbon group to a compound that has a nucleophilic functional group. Another aspect of the present invention relates to a method of preparing a trivalent iodonium fluorocarbon. Another aspect of the present invention relates to a method of preparing a fluorocarbon by treating a compound bearing a nucleophilic functional group with a trivalent iodonium fluorocarbon compound.

Abstract: Oxysulfide and fluorinated organic compounds, for example, perfluoroalkanesulfinic and sulfonic acids, and preferably trifluoromethanesulfinic and trifluoromethanesulfonic acids in salt form, are prepared by reacting, in the presence of an aprotic polar organic solvent: (i) a fluorocarboxylic acid having the formula Ea-CF2—COOH (I), wherein Ea is an atom or an electroattracting group at least partially forming a salt with an organic or inorganic cation; with (ii) a sulfur oxide, preferably sulfur dioxide, and further wherein the ratio of the number of moles of sulfur oxide to the number of moles of fluorocarboxylic acid is less than 1, preferably less than 0.99.

Abstract: The present invention relates to a bridge compound with N,N-dialkylamino group, represented by the following formula (I), wherein, R, R?, R?, R1, R2, B, B?, i, j, m, and n are defined the same as the specification. The novel bridge compound of the present invention is suitable for being used as a bridge group between dyestuffs, ultraviolet absorbers, or one dyestuff and one ultraviolet absorber. In addition, the present invention further provides a dyestuff compound provided from the aforementioned bridge compound.

Abstract: Aspects of the present invention relate to compounds for preparing fluorocarbon compounds, methods for preparing fluorocarbon compounds, and methods for purifying a mixture of compounds. One aspect of the present invention relates to a trivalent iodonium fluorocarbon. The trivalent iodonium fluorocarbon compound of the invention is useful for attaching a fluorocarbon group to a compound that has a nucleophilic functional group. Another aspect of the present invention relates to a method of preparing a trivalent iodonium fluorocarbon. Another aspect of the present invention relates to a method of preparing a fluorocarbon by treating a compound bearing a nucleophilic functional group with a trivalent iodonium fluorocarbon compound.

Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R? and R? are each independently C1-C10 alkyl; R1 is CH3; and X is O; or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

Abstract: The present application relates to a compound of formula where X is selected from the group CF3SO3, C4F9SO3, N(SO2C2F5)2, N(SO2CF3SO2C4F9), N(SO2C3F7)2, N(SO2C4F9)2, CF3CHFO(CF2)2SO3, and CH3CH2CH2O(CF2)4SO3. A photoresist composition comprising a polymer containing an acid labile group, the above compounds, and one or more additional photoacid generators is also provided for.

Abstract: The present invention is directed to 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 prevention or treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: The invention provides the combined use of an inhibitor of formation or release of ?-amyloid and a nitric oxide releaser for the treatment or prevention of Alzheimer's disease.

Abstract: The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (4R,5R)-3-acetyl-2,2-dimethyl-4-hydroxymethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine; and (4S,5R)-3-acetyl-2,2-dimethyl-4-fluoromethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine.

Abstract: The invention relates to a process for the preparation of organic boronic acid derivatives involving the reaction of an organic compound with diboronic acid in the presence of a Group 8-11 metal catalyst.

Abstract: A blocked mercaptosilane of the structure: G-C(?O)—S—CH2CH2CH2SiX3 is disclosed wherein each X is an independently selected RO— group or R— group wherein each R is independently selected from the group consisting of hydrogen, alkyl that may or may not contain unsaturation, alkenyl groups, aryl groups, and aralkyl groups, such moieties other than hydrogen having from 1 to 18 carbon atoms, at least one X is RO—, and G is a monovalent alkyl group.

Abstract: This invention concerns olefins having a terminally disposed fluorocyclobutyl ring bearing an ionic functionality or a precursor thereto, a process for the production thereof, and polymers formed therefrom.

Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Abstract: The present invention relates to a novel 3,4-dihydro-1H-naphthalene derivative having a structure of formula 1 or formula 2, its pharmaceutically acceptable salts and their geometric isomers as a highly selective cyclooxygenase-2 inhibitor. Wherein R1, R2, X, A and Q are defined in this specification respectively.

Abstract: Phosphinoamidite carboxylates and analogs are provided that have the structure of formula (I) wherein R1, R2, R3, R4, X, Y, Z and n are as defined herein. The compounds are useful as phosphitylating agents, e.g., in the phosphitylation of 3′ and 5′ hydroxyl groups of nucleosides and oligonucleotides. Also provided are phosphonocarboxylate and H-phosphonite carboxylate analogs of the compounds of formula (I). The compounds enable synthesis of phosphinocarboxylate and phosphonocarboxylate oligonucleotides having reduced internucleotide charge and enhanced nuclease resistance.

Abstract: The present invention relates to a novel 3,4-dihydro-1H-naphthalene derivative having a structure of formula 1 or formula 2, its pharmaceutically acceptable salts and their geometric isomers as a highly selective cyclooxygenase-2 inhibitor. Wherein, R1, R2, X, A and Q are defined in this specification respectively.

Abstract: A blocked mercaptosilane of the structure: G—C(═O)—S—CH2CH2CH2SiX3 is disclosed wherein each X is an independently selected RO— group wherein each R is independently selected from the group consisting of hydrogen, alkyl that may or may not contain unsaturation, alkenyl groups, aryl groups, and aralkyl groups, such moieties other than hydrogen having from 1 to 18 carbon atoms, and G is a monovalent alkyl of from 2 to 12 carbon atoms.

Abstract: A process is provided for the preparation of cyclohexene derivatives of general formula I or II: in which the substituents R1 and R2 independently of one another are defined as follows: R2 is OH or a protective group convertible to a hydroxyl group by hydrolysis, R3 and R4 are hydrogen or C1-C4-alkyl, and R5 is hydrogen or C1-C4-acyl, by the reduction or alkyne compounds of general formula III or IV: wherein the reducing agent used is at least one salt of hyposulfurous acid or hydroxymethanesulfinic acid or a mixture of at least one salt of hyposulfurous acid and at least one salt of hydroxymethanesulfinic acid.

Abstract: A flame retardant composition is produced by mixing a flammable organic material with an organic phosphorus-inorganic phosphorus oxyacid compound or its salts. The organic phosphorus-inorganic phosphorus oxyacid compounds are produced by reacting an organic phosphorus compound with an inorganic phosphorus oxyacid. The organic phosphorus-inorganic phosphorus oxyacid compound may be reacted with a basic salt forming compound. The flammable organic material such as thermoplastic resins are made less flammable by melting-kneading the flammable material with the organic phosphorus-inorganic phosphorus oxyacid compound or it's basic salt, carbonization auxiliaries, a metal-containing compound having a carbonization acceleration effect, a comb-like polymer and a filler.

Abstract: This invention relates to a compound that is represented by the following Structure I: R1—SO2—C(R2)R3—(CO)m—(L)n—SG  I wherein R1 is an aliphatic or cyclic group, R2 and R3 are independently hydrogen or bromine as long as at least one of them is bromine, L is an divalent linking group, m and n are independently 0 or 1, SG is a solubilizing group with a pKa of 8 or less, with the proviso that when m and n are both 0, SG is not a sulfo (or salt thereof) or a sulfonamido (or salt thereof) and when m is 0 and n is 1, either L is not an alkylene group or SG is not a carboxy (or salt thereof).

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The invention relates to compounds of the formula (I): CF2═CX—CH2—CH2—S(O)—R wherein X represents hydrogen, halogen or lower alkyl, and R represents a group OR1 or NR2R3 wherein R1, R2 and R3 are as defined in the description. The compounds are useful for controlling insect and like pests of agriculture.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: This invention discloses an efficient process for selectively sulfonating the primary alcohol of a diol containing both primary and secondary alcohols.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolernia, or as lead compounds for the development of such agents.

Abstract: The invention concerns a novel process for preparing racemic phenethylamines of formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meanings given in the description. According to this process: a) in a first step, optically active phenethylamines of formula (I*) ##STR2## are reacted with acetophenone derivatives of formula (II), ##STR3## the optically active phenethylamine used and the acetophenone derivative used each being substituted in an identical manner in the phenyl part, optionally in the presence of a diluting agent and optionally in the presence of a catalyst; b) in a second step, the resultant optically active Schiff bases of formula (III*) ##STR4## are reacted with metallic hydroxides containing between 0.1 and 50 wt. % water; and c) in a third step, the resultant racemic Schiff bases are reacted with acids in the presence of water.

Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.

Abstract: The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: A thermosensitive reversible color-developing and disappearing agent includes an aromatic compound having at least one group of the formula, --SO.sub.2 NHCXNH--, wherein X.dbd.O or S atom, and at least one straight chain alkyl group with 11 or more carbon atoms, and is reactive with a dye precursor in a thermosensitive recording material to thereby record colored images on the recording material upon heating imagewise, and make the colored images disappear upon heating to a temperature lower than the colored image-forming temperature.

Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.

Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Abstract: D,L-, L- and D-phenyl alanine derivatives of formula (I) defined in claim 1 in which R.sub.1 is an amidino-, guanidino-, oxamidino-, aminomethyl- or amino group have been discovered which effectively prevent blood coagulation or thrombosis. The antithrombotically active compounds have low toxicity and may be administered by mouth, subcutaneously or intravenously.