Abstract: Phosphoramidate alkylator prodrugs can be used to treat cancer when administered along or in combination with one or more anti-neoplastic agents.

Abstract: A phosphorus compound of formula (1): wherein R1 denotes a hydrogen atom or a hydroxy protective group; R2 denotes a group defined by the following formula (R2-1) or (R2-2); R3, R4, R5, and R6 may be the same or different and independently denote a hydrogen atom, an alkyl group, an alkoxy group, an acyloxy group, a halogen atom, a haloalkyl group, or a dialkylamino group; two among R3, R4, R5, and R6 may form an aromatic ring optionally having a substituent group, and two among R3, R4, R5, and R6 may form a methylene chain optionally having a substituent group or a (poly)methylenedioxy group optionally having a substituent group: wherein (R2-1) and (R2-2), R7 denotes an alkyl group, a cycloalkyl group, an aryl group, an alkoxy group, or an aryloxy group; R8 and R9 independently denote a hydrogen atom, an alkyl group, or an aryl group; z denotes a divalent group; and a denotes an integer of 0 or 1.

Abstract: A thiophene compound having a phosphate group, for example, one represented by the formula [1]. The compound has high resistance to heat and oxidation and can be improved in solubility or dispersibility in various solvents. (In the formula, R1 and R2 each independently represents, e.g., hydrogen, halogeno, cyano, or phenyl optionally substituted by W; and R3 to R6 each independently represents —OR7, SR8, or —NR92, provided that R7 to R9 each independently represents hydrogen, C1-10 alkyl, or phenyl optionally substituted by W and W represents halogeno, cyano, nitro, hydroxyl, mercapto, amino, formyl, carboxy, C1-10 alkyl, etc.

Abstract: An organic semiconductor compound based on a 2,7-bis-(vinyl)[1]benzothieno[3,2-b]benzothiophene backbone, an organic semiconductor thin film, an organic thin film transistor and methods of forming the same are provided, the organic semiconductor compound including a vinyl group derived from a phosphonate derivative represented by Formula 1 and an aldehyde derivative represented by Formula 2 below:

Abstract: The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: A compound of the formula (I): wherein X is hydroxy or the like; Y is —C(?R2)—R3—R4 wherein R2 and R3 is oxygen atom or the like, R4 is hydrogen, optionally substituted alkyl, optionally substituted heteroaryl or the like; Z is hydrogen or the like; Z1 and Z3 each is independently a bond, alkylene or the like; Z2 is a bond, alkylene, —O— or the like; R1 is optionally substituted aryl, optionally substituted heteroaryl or the like; p is 0 to 2 and ring (A) is optionally substituted aromatic heterocycle, a tautomer of itself, a prodrug thereof, a pharmaceutically acceptable salt thereof or a solvate thereof has an integrase-inhibiting activity.

Abstract: Methods of imaging tissue of a mammal which expresses chymase include administering to the mammal an effective amount of a radiolabeled chymase inhibitor.

Abstract: The present invention is directed to an improved process for synthesizing phosphonic and phosphinic acid chymase inhibitor compounds.

Abstract: Compounds of the following formula (I), for example: (1), wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.

Abstract: Oligonucleotides comprising one or more 4?-thioarabinonucleotides are described, as well as uses thereof for applications such as antisense- and RNAi-based gene silencing. 4?-thioarabinose-based phosphoramidite and H-phosphonate compounds are also described, as well as uses thereof for the synthesis of oligonucleotides comprising one or more 4?-thioarabinonucleotides.

Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

Abstract: The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.

Abstract: The present invention concerns novel bidentante optionally N-containing P-ligands of general Formula (I) embracing a two-ring-system and processes for synthesizing them, transition metal complexes of these compounds and their use as catalysts.

Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.

Abstract: Disclosed is a method of fabricating an organic thin film transistor including a substrate, a gate electrode, a gate insulating layer, metal oxide source/drain electrodes, and an organic semiconductor layer, in which the surface of the metal oxide source/drain electrodes or of the metal oxide source/drain electrodes and gate insulating layer is treated with a self assembled monolayer-forming compound containing a dichlorophosphoryl group. According to the method of example embodiments, the work function of the metal oxide of the source/drain electrodes may be increased to be higher than that with no SAM-forming electrode, thus making it possible to fabricate an improved organic thin film transistor having increased charge mobility.

Abstract: Metallic catalysts of the general formula (I) and their precursors, suitable for chemo- regio- and stereoselective reactions, derived from ortho-bis-(1-phospholanyl)-heteroarenes.

Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.

Abstract: Disclosed herein are compounds of the formula wherein R1 is independently H or alkyl of 1 to 6 carbons; R2 is optional and is defined as lower alkyl of 1 to 6 carbons, F, Cl, Br, I, CF3, fluoro substituted alkyl of 1 to 6 carbons, OH, SH, alkoxy of 1 to 6 carbons, or alkylthio of 1 to 6 carbons; n is an integer of between 0 and 2; o is an integer between 0 and 3; R3 is hydrogen, lower alkyl of 1 to 6 carbons, F, Cl, Br or I; R4 is heteroaryl or (R5)p-heteroaryl where the heteroaryl group is 5-membered or 6-membered and has 1 to 3 heteroatoms selected from the group consisting of O, S, and N; p is an integer having the values of 0–5; R5 is F, Cl, Br, I, NO2, N(R8)2, N(R8)CORO8, N(R8)CON(R8)2, OH, OCOR8, OR8, CN, COOH, COOR8, C1-10 alkyl, fluoro substituted C1-10 alkyl, C2-10 alkenyl having 1 to 3 double bonds, C2-10 alkynyl having 1 to 3 triple bonds, or a (trialkyl)silyl or (trialkyl)silyloxy group where the alkyl groups independently have 1 to 6 carbons; A is (CH2)q where q is 0–5, C3-6 branched alkyl,

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.

Abstract: The invention relates to a process for the manufacture of bidentate ligands of the formula IA and IIA, characterized in that N,N-(optionally substituted)dialkylamino phosphines bound to an aromatic carbon are lithiated in ortho-position and the lithiated compounds are further converted to said bidentate ligands: wherein X1 is NR, O or S; X2 is CHR1 or CR1; X3 is CHR2 or NR2, or, if X2is CR1, X3 is CR2 or N; and R, R1 and R2 are radicals such as alkyl groups or R1 and R2 together form an annealed ring; Y1*, Y2* and Y1?* are, independently of each other, an element of the fifth group of the periodic table of elements as such or in thioxo or oxo form; Z1*, Z2*, Z3*, Z4*, Z1?*, Z2?* are, independently of each other, for example halogen, hydrogen, or an unsubstituted or substituted moiety selected from radicals such as alkyl groups; the substituents have otherwise the meanings given in the specification; and the ligands are capable of forming metal complexes, which can be used as catalysts in stereoselective s

Abstract: The present invention concerns novel unsymmetrical chiral diphosphines of a mixed aliphatic-aromatic type and processes for synthesizing them, complexes of these compounds and their use as catalysts.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1–8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R5 denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.

Abstract: A novel photoacid generator containing a structure of the following formula (I), wherein R is a monovalent organic group with a fluorine content of 50 wt % or less, a nitro group, a cyano group, or a hydrogen atom, and Z1 and Z2 are individually a fluorine atom or a linear or branched perfluoroalkyl group having 1-10 carbon atoms, is provided. When used in a chemically amplified radiation-sensitive resin composition, the photoacid generator exhibits high transparency, comparatively high combustibility, and no bioaccumulation, and produces an acid exhibiting high acidity, high boiling point, moderately short diffusion length in the resist coating, and low dependency to mask pattern density.

Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The invention relates to pharmaceutically active substances from the group comprising midazolam and compounds with a methyl-substituted nitrogen atom that is the ring atom of a nitrogenous heterocycle. These substances are used to reduce the oxygen consumption during a physical activity. They can be administered together with an effective amount of D-glucose, D-maltose, ethanol, a glucogenic amine, a glucogenic amino acid or an amino acid metabolizable via glyoxylate or a dipeptide or a pharmaceutically acceptable salt of such an amino acid and an effective amount of thiamine, of a pharmaceutically acceptable thiamine salt or of a combination of folic acid and cyanocobalamine, with the proviso that the third component is thiamine or a pharmaceutically acceptable thiamine salt if the second component is D-glucose, D-maltose, a glucogenic amine, a glucogenic amino acid non-metabolizable via glyoxylate, or a dipeptide or a pharmaceutically acceptable salt of such an amino acid.

Abstract: The present invention relates to a one pot process for preparing a compound of formula I: I; from a compound of formula II and III: I; III.

Abstract: Novel lipid compounds and compositions comprising carbohydrate backbones are used to make supramolecular structures such as vesicles, liposomes (single lamellar, multilamellar, and giant), micelles, hexagonal phases, microemulsions and others. The novel compositions and supramolecular structures may be combined with active agents such as contrast agents and bioactive agents (e.g., therapeutic and diagnostic agents) in delivery methods.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: A class of novel benzo(b)thiophene is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.

Abstract: The invention concerns a resolution method for a racemic mixture of aldehyde of formula (I). The aldehydes of formula I are useful in their enantiomeric form or their racemic form for preparing transition metal complexes useful as catalysts in hydroformylation reactions of olefins.

Abstract: Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include (R,S,S,R)-DIOP*. The ruthenium complex reduces enamide to the corresponding amine with up to 99% enantioselectivity. The transition metal complexes of the chiral ligands are useful in asymmetric reactions such as asymmetric hydrogenation, hydride transfer, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, hydrocarboxylation, isomerization, allylic alkylation, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition and epoxidation reactions.

Abstract: The present invention relates to unsymmetric bidendate organophosphorus ligands of the formula (I) which have a modular structure and have a trivalent phosphine function and a second trivalent phosphorus group which is bound via a heteroatom to a chiral ligand framework, R1R2PZC*HR3XP(YR4)(YR5)  (I) where X is —O—, —S— or —NR6—, Y is a direct phosphorus-carbon bond, —O— or —NR7—, Z represents 1 to 6 carbon atoms which are joined by single or double bonds and link the phosphine unit PR1R2 to the carbon center C*, and P is trivalent phosphorus. The invention also relates to complexes comprising such a chiral ligand system of the formula (I).

Abstract: The present invention relates to a compound with aryl-amidines, particularly amidinoaryl-cyclopropanes, amidinoarylmethyl-pyrroles, amidinoaryl-benzenes, amidinoaryl-pyridines, or amindonoaryl-alanines, represented by formula (1), a pharmaceutically acceptable salt, a prodrug, a hydrate, a solvate or an isomer thereof, which are inhibitors of coagulation enzyme, factor Xa (FXa). The present invention also relates to a pharmaceutical composition containing the compound, and a method of using the same as an anticoagulant agent for treatment and prevention of thrombosis disorders.

Abstract: The present invention provides amidophosphate derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

Abstract: New oxime derivatives of formula (I) or. (II), wherein m is 0 or 1; R1 inter alia is phenyl, naphthyl, anthracyl, phenanthryl or a heteroaryl radical; R′1 is for example C2-C12alkylene, phenylene, naphthylene; R2 is CN; R3 is C2-C6haloalkanoyl, halobenzoyl, a phosphoryl or an organosilyl group; R4, R5, R10 and R11 inter alia are hydrogen, C1-C6alkyl, C1-C6alkoxy; R6 inter alia is hydrogen phenyl, C1-C12alkyl; R7 and R8 inter alia are hydrogen, C1-C12alkyl; or R7 and R8, together with the nitrogen atom to which they are bonded, form a 5-, 6 or 7-membered ring; R9 is for example C1-C12alkyl; and A inter alia is S, O, NR7a; are useful as latent acids, especially in photoresist applications.

Abstract: The present invention is concerned with a novel process for the preparation of a hydroxybenzothiophene that is an intermediate for synthesizing pharmaceutically active substances, e.g. 5-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-7-benzothiophenylmethyl]-2,4-thiazolidinedione and the corresponding sodium salt which are useful in the treatment of diabetes.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: This invention provides compounds of Formula I having the structure wherein R1 and R2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy; R3 and R4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, perfluoroalkoxy of 1-6 carbon atoms, alkanoyloxy of 2-7 carbon atoms, perfluoroalkanoyloxy of 2-7 carbon atoms, arylalkoxy of 7-15 carbon atoms, aryloxy of 6-12 carbon atoms, aroyloxy of 6-12 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, nitrile, nitro, amino, —NHSO2CF3, carbamoyl, carbo

Abstract: Novel monocyclic L-Nucleoside compounds have the general formula 1

Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: 1

Abstract: Compounds of the formula I 1

Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.