Abstract: The present invention provides a production method of ?-fluoroacrylate ester, a composition containing a highly-pure fluorocyclopropane derivative and a composition containing highly-pure ?-fluoroacrylate ester.

Abstract: Disclosed is a method for preparing a 2-fluoroacrylate, comprising the steps of: (1) mixing a vinyl ether having the structure of formula A with dichloromonofluoromethane to yield a substituted cyclopropane compound having the structure of formula B; (2) mixing the substituted cyclopropane compound having the structure of formula B with R2OH to yield an acetal product having the structure of formula C, followed by hydrolysis to yield 2-fluoroacrylaldehyde having the structure of formula D; or reacting the substituted cyclopropane compound having the structure of formula B with water to yield 2-fluoroacrylaldehyde having the structure of formula D via hydrolysis; (3) oxidizing 2-fluoroacrylaldehyde having the structure of formula D to yield 2-fluoroacrylic acid having the structure of formula E; and (4) mixing 2-fluoroacrylic acid having the structure of formula E with R3OH to yield a 2-fluoroacrylate having the structure of formula F.

Abstract: To provide a novel method for producing a halogenated acrylic acid derivative. A compound represented by the formula (1): (wherein each of R1 and R2 which are independent of each other, is a hydrogen atom or a monovalent group essentially containing a carbon atom, or R1 and R2 together form a ring, R3 is a monovalent group capable of being desorbed by R3OH removal reaction, and each of R4 and R5 which are independent of each other, is a hydrogen atom or a monovalent group essentially containing a carbon atom) and having a boiling point of at most 500° C.

Abstract: Compositions comprising branched C10 mercaptans selected from the group consisting of 5-methyl-1-mercapto-nonane, 3-propyl-1-mercapto-heptane, 4-ethyl-1-mercapto-octane, 2-butyl-1-mercapto-hexane, 5-methyl-2-mercapto-nonane, 3-propyl-2-mercapto-heptane, 4-ethyl-2-mercapto-octane, 5-methyl-5-mercapto-nonane, and combinations thereof. Compositions comprising C11+ mercaptans, wherein the C11+ mercaptans are characterized by structure R6—SH, wherein R6 is an alkyl group derived from one or more C11+ monoolefins, and wherein the one or more C11+ monoolefins comprise C11 internal monoolefins, C12 internal monoolefins, C13 internal monoolefins, C14 internal monoolefins, 1-tetradecene, 1-hexadecene, or combinations thereof.

Abstract: Disclosed are nucleotide sequences encoding thioesterase enzymes, methods for their production, their use in methods to form thioesters, and their use in methods of screening for other wild type bacteria capable of producing said thioesterase enzymes. Also disclosed are compositions comprising thioesters produced by the methods disclosed herein.

Abstract: The invention provides novel compounds that may be used as intermediates in the preparation of epothilones, epothilone analogs and derivative, as well as new synthetic methods for producing the intermediates and products.

Abstract: Thiol ester compositions, methods of making the thiol ester compositions, and methods of using the thiol ester compositions are provided. In some embodiments, the thiol ester compositions include thiol esters, hydroxy thiol esters and cross-linked thiol esters. The thiol ester composition can be used to produce cross-linked thiol esters, sulfonic acid-containing esters, sulfonate containing esters and thioacrylate containing esters. The thiol ester compositions can be used to produce polythiourethanes. The polythiourethanes can be used in fertilizers and fertilizer coatings.

Abstract: The application discloses thiol ester molecules and ?-hydroxy thiol ester molecules having a thiol group located on one of the final two carbon atoms in a carbon chain or a terminal or ?-hydroxyl groups, respectively. The disclosed thiol ester molecules and or ?-hydroxyl thiol ester molecules es may be made from unsaturated ester molecules having one or more terminal alkene groups. The disclosed techniques also provide methods for making unsaturated ester molecules having one or more terminal alkene groups by the metathesis of unsaturated esters having one or more internal carbon-carbon double bonds (e.g. natural source oils). The thiol ester molecules or ?-hydroxy thiol ester molecule may be used in reactions with isocyanate monomers, epoxide monomer, or material having multiple alkene groups to make sealants, coatings, adhesives, and other products.

Abstract: Thiol ester compositions, methods of making the thiol ester compositions, and methods of using the thiol ester compositions are provided. In some embodiments, the thiol ester compositions include thiol esters, hydroxy thiol esters and cross-linked thiol esters. The thiol ester composition can be used to produce cross-linked thiol esters, sulfonic acid-containing esters, sulfonate containing esters and thioacrylate containing esters. The thiol ester compositions can be used to produce polythiourethanes. The polythiourethanes can be used in fertilizers and fertilizer coatings.

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: Compounds of formula I wherein A is R3, OR3, SR3, and NR3R4; and R1, R2, R3 and R4 are as defined. The compounds of the invention are reversible inhibitors of acyl-CoA dehydrogenase, and are useful in treating disorders such as diabetes, heart diseases (including angina and congestive heart failure), and peripheral vascular disease in patients suffering from these diseases or conditions resulting thereof.

Abstract: A thiol carboxylate ester as shown by general formula (I) below, which has a half ester content of 0.0001 to 2 mass %, and favorably, which has a halogen content of not more than 2 mass % and/or to which a polymerization inhibitor such as a catechol family member is added.

Abstract: The invention relates to compounds of the general formula (I) 1

Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: A process comprising the steps of a) reacting in an esterification reaction (i) a plurality of different plyols with; (ii) a plurality of different polycarboxylic acids and/or precursors therefor; in a manner to retain a plurality of free hydroxy groups in the resultant polyester(s) and retain substantial amounts of un-crosslinked polyesters in the resultant product; followed by b) reacting substantially all of the free hydroxy groups present in the resultant mixture of polyesters with an acrylating agent; to form a mixture having a hydroxy (OH) number (measured using ASTM E222-73) of no more than about 100 mg KOH/g. Use of the mixture as a composition for lithographic or flexographic inks.

Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound contains one or more protected sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substituents bearing at least one terminal —ONO2 group. The present invention further provides pharmaceutical compositions comprising one or more of said compounds as an active ingredient.

Abstract: A 2-methoxyphenol derivative may be used as an ultraviolet (UV) light absorbing dispersant and, an ink composition may include the 2-methoxyphenol derivative as a light-resistant dispersant. The 2-methoxyphenol derivative absorbs UV light and thus provides light resistance to outputs. The 2-methooxyphenol derivative also improves dispersibility. When the 2-methoxyphenol derivative is used to prepare an ink composition, the ink composition has improved dispersibility and light resistance, and there is no need to add a light-resistant additive.

Abstract: Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions.

Abstract: Thioester and selenoester generators, precursors thereof, thioester and selenoester compounds produced therefrom, and related methods for their production are provided. The subject thioester and selenoester generators include an amino acid synthon having an N-terminal group joined to a C-terminal group through an organic backbone comprising one or more carbons. The organic backbone contains a backbone nitrogen, anchored to a support through a nucleophile-stable linker that lacks reactive functional groups. The organic backbone may include a target molecule of interest, such as an amino acid, peptide, polypeptide or other organic compound of interest, and/or the N- and/or C-termini can be elaborated using a variety of synthesis approaches to provide a target molecule of interest. The compounds and methods find a wide variety of uses, including use in thioester- or selenoester-based chemical ligation techniques.

Abstract: This invention relates to compounds of the Formula (I): 1

Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.

Abstract: This invention is directed to novel and known stufur containing compounds and pharmaceutically acceptable salts thereof that have utility as antifungals and as antiproliferative agents against mammalian cells, in particular cancer cells and most particularly leukemia-derived cells. The invention provides a method for synthesizing certain of the sulfur containing compounds that is more efficient than previously known methods.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of GABA analogs following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Polymers and copolymers synthesized by means that yield a narrow range of molecular weights can have different properties than polymers synthesized by conventional means. In order to obtain such polymers, however, polymerization must be controlled. One type of controlled polymerization is the reversible addition-fragmentation chain transfer (RAFT) process, which has characteristics of a living polymerization. The present invention discloses a group of dithioesters and trithioesters suitable as chain transfer agents for RAFT polymerization. The present invention also discloses RAFT polymerizations conducted in aqueous media.

Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

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: The present invention discloses aminothiol compounds and acylated derivatives thereof, which respectively have general formula I and formula II wherein R1-R6 are substitutable ligands. Such compounds can perform as superior catalysts in asymmetric addition reactions of organic zinc and aldehyde. According to the present invention, the compounds is needed only less than 0.02% of main reactants to obtain enantioselectivity higher than 99% enantiomeric excess, whereby the asymmetric reactions can become very economic.

Abstract: The invention is directed to nucleophile-stable thioester generating compounds comprising an orthothioloester or a carboxyester thiol, methods of production and use. The compounds and methods have wide applicability in organic synthesis, including the generation of peptide-, polypeptide- and other polymer-thioesters. The invention is particularly useful for generating activated-thioesters from precursors that are made under conditions in which strong nucleophiles are employed, such as peptides or polypeptides made using Fmoc SPPS, as well as multi-step ligation or conjugation schemes that require (or benefit from the use of) compatible selective approaches for directing a specific ligation or conjugation reaction of interest.

Abstract: Provided are fluorine-containing compounds, and polymers derived therefrom, for use in compositions used for treating textile substrates. Also provided are methods of making fluorine-containing compounds and polymers derived therefrom, compositions comprising the compounds and/or polymers of the present invention, methods of treating substrates, and the treated products derived therefrom.

Abstract: The present invention includes 16-HETE analogs which are agonists and antagonists of 16-HETE. The compositions may be formulated in pharmaceutically acceptable formulations. The invention also includes methods and products for inhibiting neutrophil adhesion and neutrophil aggregation using the 16-HETE agonists. One method of the invention involves the administration of a 16-HETE agonist in combination with a thrombolytic agent to a patient suffering from thromboembolic stroke.

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The invention comprises a novel lactate compound for two unique purposes: (1) cardiac energy resuscitation and the treatment or prevention of reperfusion injury following ischemia, and (2) the provision of a fuel energy source to humans and other mammals during exercise and recovery. The novel lactate compound is particularly a lactate thiolester. Preferably, the thiol is selected from a cysteine or a methionine amino acid. In a particularly preferred form, the compound is a lactate N-acetyl ethyl ester of the cysteine or methionine amino acid. The most preferred compound is lactate N-acetyl cysteine thiolester (LNACE): Further, the invention involves use of mixtures of lactate- and pyruvate compounds as well as hexoses (glucose and fructose), maltodextrins and electrolytes as adjutants to support LNACE in its specific purposes.

Abstract: Benzene butyric acid compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.

Abstract: Compounds of the formula 1

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds represented by general Formula (I) and a pharmaceutically acceptable salt or an oxide or a hydrate thereof, that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

Abstract: Compounds of the formula I 1

Abstract: Acrylates having a high degree of halogenation, as well as polymers that include one or more mer units derived from such acrylates provide materials having tailorable optical and physical properties. The polymers find utility particularly in optical devices including optical waveguides and interconnecting devices.

Abstract: A method is provided which facilitates and enables the production of a wide range of complex conjugates composed of similar or dissimilar units linked together by amide bonds. Said method for the production of acylthio derivatives, R′—CO—SA, involves reaction of a carboxylate, R′—CO—O− (or carboxylic acid R′—CO—OH) with an iso-thiouronium derivative (bearing SA) in the presence of base. Nucleophilic counterion forms of the iso-thiouronium salts confer significant rate enhancement. The processes are simple, generally applicable, efficient, and do not require the employment of noxious reagents. The production of complex protein-like products by the intermediary of acylthio esters generated by the process of this invention, provides a method which is compatible with mild methods of chain assembly; and is preferably applied when the second component in the ligation bears an amino terminal cysteine residue.

Abstract: A catalyst used for preparing thiochloroformates by reacting thiols with phosgene is a cyclic urea or cyclic thiourea which may be in the form of a salt obtainable by reaction with a hydrohalic acid or phosgene.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.

Abstract: Compounds of the formula: ##STR1## wherein n is 1, 2, 3, or 4;X.sup.1 and X.sup.2 are each, independently, chlorine or bromine;A is O or S;R.sup.1 is hydrogen or C.sub.1 -C.sub.16 alkyl;R.sup.2 is C.sub.1 -C.sub.16 alkyl, C.sub.6 -C.sub.16 aryl, C.sub.1 -C.sub.4 alkylidene, or CH.sub.2 OR.sup.5 ;R.sup.3 is hydrogen, chlorine, bromine, or OR.sup.6 ;R.sup.4 is C.sub.1 -C.sub.16 alkyl, C.sub.7 -C.sub.16 aralkyl, C.sub.2 -C.sub.16 alkenyl, or C.sub.6 -C.sub.18 aryl;R.sup.5 is hydrogen, C.sub.1 -C.sub.16 alkyl, C.sub.7 -C.sub.16 aralkyl, C.sub.2 -C.sub.16 alkenyl, or C.sub.6 -C.sub.18 aryl; andR.sup.6 is hydrogen or C.sub.1 -C.sub.16 alkyl.These compounds by themselves and in combination with certain halo-but-2-enoic acids and esters are useful as catalyst promoters in ethylene polymerization processes.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.

Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.