Abstract: The novel C7-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

Abstract: The present invention relates to methods of synthesising radiolabelled compounds, to the precursors useful in such methods and to the radiolabelled compounds obtainable by such methods. More particularly, the present invention relate to methods, precursors and radiolabelled compounds useful in Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) especially for imaging neuroreceptors with radiolabelled agonists.

Abstract: A compound of any of formulae (I) to (III) wherein at least one of Y and Z includes a Si atom, is of utility in therapy.

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Abstract: Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting Aurora kinase activity and a method for treating cancer with these compounds.

Abstract: Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

Abstract: The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR/MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

Abstract: The present invention provides methods for preparing complexed diaryl boronic acids from alkyl diarylborinates.

Abstract: The present invention provides a ?-electron-conjugated organice silane compound that give an organic thin film superior in peeling restance, orientation, crystallinity and eletroconductive properties, and a production method thereof. A ?-electron-conjugated organice silane compound represented by General Formula: R1-SiX1X2X3 (R1 represents an organic group having a particular monocyclic heterocyclic unit; and X1 to X3 are a group giving a hydroxyl group by hydrolysis). A method of producing the organic silane compound, comprising allowing a compound represented by General Formula: R1-Li (R1 is the same as above) or a compound represented by General Formula: R1-MgX5 (R1 is the same as above; and X5 represents a halogen atom) with a compound represented by General Formula: X4-SiX1X2X3 (X1 to X3 are the same as above; and X4 represents a hydrogen or halogen atom or a lower alkoxy group).

Abstract: The present invention relates to anthracene derivatives, to the use thereof in organic electroluminescent devices, and to organic electroluminescent devices comprising these compounds.

Abstract: The invention describes a composition comprising a) a naturally occurring or synthetic elastomer susceptible to oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation, b) a white reinforcing filler, and c) as coupling agent, at least one compound of the formula (I) wherein the general symbols are as defined in claim 1, or an oligomeric hydrolysis product of the compound of the formula (I).

Abstract: A compound of any of formulas (I) to (V): wherein at least one of Y and Z includes a Si atom, is of utility in therapy.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: A new nitrogen-containing organosilicon compound contains tertiary amine groups and carbonyl groups wherein the tertiary amine groups are selected from R1R2N— (where R1 and R2 are the same or different univalent hydrocarbon groups of 1-15 carbon atoms), alicyclic amino groups, or heterocyclic amino groups containing in their rings one or more tertiary amine groups.

Abstract: The present invention provides for a composition comprising a silane having the formula: (R1)(R2)(R3)Si—R4—Si(R5)(R6)(R7) wherein R1, R2, R3, R5, and R6 are each independently selected from the group consisting of 1 to 6 monovalent hydrocarbon radicals, aryl, and a hydrocarbon group of 7 to 10 carbons containing an aryl group; R4 is a hydrocarbon group of 1 to 3 carbons; R7 comprises an anionic, cationic or zwitterionic substituent. The silanes of the present invention exhibit resistance to hydrolysis over a wide pH range.

Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.

Abstract: The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders mediated by one or more estrogen receptors and processes for their preparation. The compounds of the invention are useful in the treatment and/or prevention of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Abstract: Novel chemical compounds are disclosed having the general formula L{YXm}n, wherein X is selected from the Group 13 elements, Y is a halide, and L is a chelating ligand containing at least one binding atom contacting the Group 13 element, the atom being selected from the group consisting of C, N, O, and S, and m and n are integers having a value of at least 1. L may be a Schiff base type ligand, such as a salen ligand. The compositions of the present invention may be bidentate, quadridentate, or greater. The compositions may be used in dealkylation of phosphate esters or ethers. Advantageously, the methods of the present invention may be rendered catalytic.

Abstract: This invention relates to new generation triple-targeting, chiral, broad-spectrum antimicrobial 7-substituted piperidino-quinolone carboxylic acid derivatives, to their optical isomers, diastereomers or enantiomers, as well as pharmaceutically acceptable salts, hydrates, prodrugs, polymorphs and pseudopolymorphs thereof, to their preparation, to their compositions and to their use.

Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.

Abstract: The invention relates to chromophores exhibiting semiconductive properties, the production and use thereof as luminophores in organic light-emitting diodes (OLEDs) and organic solar cells. The invention more specifically relates to highly condensed boron complex compounds wherein the boron atoms have improved processability, solubility and the fluorescence quantum efficiency is increased by building up by spirocenters.

Abstract: This invention provides a method for identifying one or more complexes from a library of complexes, wherein said complex or complexes are selected for their ability to perform a preselected or desired function on a target molecule or by having a pre-selected structure, each complex being designated a morphatide, said method comprising: (a) preparing a library of morphatides, comprised of: (i) a scaffolding component selected from the group consisting of nucleic acid, nucleic acid like molecule or nucleic acid analog having one or more regions of randomized sequence; (ii) one or more linker components; and (iii) one or more agent molecules or type of agent molecules, linked to the scaffolding component by one or more type of linker components; and (b)screening the library of morphatides prepared in step (a) by contacting, binding, or associating the morphatides with one or more suitable target molecules upon which a morphatide performs a preselected or desired function or to which a morphatide binds or associa

Abstract: In accordance with the present invention, there are provided novel benzoxazine compounds and thermosetting resin compositions prepared therefrom. Invention compositions are particularly useful for increasing adhesion at interfaces within microelectronic packages. Invention benzoxazines are useful for the preparation of invention compositions with properties which are associated with increased adhesion at interfaces, such as, for example, low shrinkage on cure and low coefficient of thermal expansion (CTE). In another aspect of the invention, there are provided die-attach pastes having increased interfacial adhesion. Invention die-attach pastes include benzoxazine-containing thermosetting resin compositions. In further aspects of the invention, there are provided methods for enhancing adhesive strength of thermosetting resin compositions and methods for enhancing adhesion of a substrate bound to a metallic surface by a thermosetting resin composition.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Process for preparing arylboron and alkylboron compounds of the formulae (II) and (III) by reacting lithioaromatics and lithiated aliphatics of the formula (I) with boron compounds in microreactors in accordance with equation I or equation II, 1

Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R3 is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, CORC; RC is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R5 is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR6 and containing one or two independent substituents from the group including H, halogen, CN, N02, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 a

Abstract: Compounds of formula I wherein R1, R2, and R3 independently of one another are hydrogen; C1-C20alkyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-8alkyl)O—(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R1, R2, and R3 independently of one another are C3-C6alkenyl; phenyl which is unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/— and di(C1-C4alkyl)amino; or R1 and R2 together are C2-C9alkylene, o-xylylene, 2-butenylene, C3-C9oxaalkylene or C3-C9azaalkylene; R4, R5, R6, and R7 independently of one another are sec-C3-C20alkyl, tert-C4-C20alkyl or phenyl wherein these radicals are unsubstituted or substituted by OH, C1-C4alkoxy, C1-C4alkylthio, phenylthio, F, Cl, Br, I, CN, (C1-C8alkyl)O(CO)—, (C1-C4alkyl)—(CO)O— or/and di(C1-C4alkyl)amino; or R4 and R5, and/or R6 and R7

Abstract: A high char yield polybenzoxazine is formed by mixing (i) a benzoxazine compound, (ii) a furan compound, (iii) a benzoxazine-furan compound or combinations thereof, wherein the mixture has a benzoxazine ring to furan ring ratio from about 0.001 to about 10 and then heating the mixture for a sufficient time to form the polybenzoxazine.

Abstract: The present invention is directed to new, energy-efficient, photoinitiators having the general formula: 1

Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

Abstract: A compound of formula wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H2 or F2; A is N or C(R2); G is N or C(R3); D is N or C(R4); with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO; R1 is hydrogen or C1 to C4 alkyl; R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3 or R2 and R3, or R3 and R4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, aryl, heteroaryl, OH, OC1-C4 alkyl, CO2R1, —CN, —NO2, —NR5R6, —CF3, —OSO2CF3; R5 and R6

Abstract: A light modulator (1) is proposed which has a photochromic layer (15), which can be activated optically by control light, for modulating signal light, and at least one optically transparent substrate (13) for the photochromic layer (15), in which the light modulator (1) has at least one filter layer (14), which reflects the control light in a wavelength-selective fashion for the purpose of retroreflecting control light which has penetrated the photochromic layer (15). The reflecting filter layer (14) ensures that the control light is utilized efficiently for the photochemical conversion (photoconversion) of the photochromic material, since the control light passes twice through the photochromic layer (15). The reflecting filter layer (14) has the function, furthermore, of separating the control light from the modulated signal light such that the modulated signal light can be evaluated without significant interference from the control light.

Abstract: For preparing bis-silyl carboxamides in a semi-continuous, reacting an amide or the N-trimethylsilyl derivative thereof with a silylating agent and, at the same time, extracting the bis-silyl carboxamide formed by distillation under reduced pressure.

Abstract: Borane-trialkylamines of the formula H3B.NRR1R2 wherein R is a tertiary alkyl group having 4 to 8 carbon atoms, and R1 and R2 are the same or different straight or branched chain alkyl from 1 to 4 carbon atoms are provided. The compounds are new hydroboration agents.

Abstract: The use of linear or cyclic silicon compounds containing at least one chromophoric group of quinone or azo type as direct dyes in dye compositions intended for dyeing human keratin fibres and in particular the hair. The invention also relates to novel silicon compounds and dye compositions containing them, as well as to the corresponding direct dyeing process.

Abstract: The use of linear or cyclic silicon compounds containing at least one chromophoric group of quinone or azo type as direct dyes in dye compositions intended for dyeing human keratin fibers and in particular the hair. The invention also relates to novel silicon compounds and dye compositions containing them, as well as to the corresponding direct dyeing process.

Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.

Abstract: Arylamines with electron donating groups such as alkyl and alkoxy groups in the meta position on the aromatic ring change the polymerization temperature of the benzoxazine prepared therefrom and offer an opportunity for an additional crosslinking site (the para position on the aromatic amine can couple to a Mannich base generated by the opening of the oxazine ring of the benzoxazine or a methylene bridge generated by a degradation reaction). Naphthenic amines with an alkyl or alkoxy substituent on the 5.sup.th through the 8.sup.th carbon atom on the naphthalene ring can function similarly. The polymers for benzoxazines prepared from at least 10% substituted aromatic or naphthenic amines are useful due to low polymerization temperatures and higher Tg (glass transition temperature).

Abstract: Novel organosilicon compounds containing organooxysilyl and sulfenamide groups in the molecule are provided. They are useful as interfacial binders between inorganic materials and organic materials, adhesion modifiers for organic resins and rubber, primers, etc.

Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.

Abstract: Disclosed herein are boronic ester and acid compounds, their synthesis and uses. More specifically, disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds.

Abstract: Pyrroloindole derivatives having antimicrobial and antitumor activities and having a carbamoyloxy group represented by the following general formula (1), optical isomers thereof, and pharmacologically acceptable salts thereof; and intermediates for production thereof: ##STR1## where R.sup.1 is OH, or a pyrrolidinyl group; n is 1 or 2; R.sup.2 is a lower alkyl group of C.sub.1 -C.sub.4 ; X--Y or Y--X is CH.sub.2, CHOH, CH.sub.2 -CH.sub.2, O--CH.sub.2, or NMe--CH.sub.2 ; Z.sup.1 is Cl or Br; and Ar.sup.1 is ##STR2## wherein Z.sup.2 and Z.sup.3 are O or NH; m is 0 or an integer of 1 to 4; and Ar.sup.2 is any of the above groups a, b, c, and d.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: The use of linear or cyclic silicon compounds containing at least one chromophoric group of quinone or azo type as direct dyes in dye compositions intended for dyeing human keratin fibres and in particular the hair. The invention also relates to novel silicon compounds and dye compositions containing them, as well as to the corresponding direct dyeing process.

Abstract: Benzoxazine monomers, oligomers and polymers are desirably modified by adding pendant functional groups to either the amine or phenolic reactants. These pendant functional groups can be activated at temperatures generally from about 25.degree. C. to about 300.degree. C. to form chemical bonds between said benzoxazine monomers, oligomers and polymers. The additional chemical bonds increase the thermal stability of benzoxazine polymers such that they can withstand higher use temperature, act as more effective flame barriers, or result in higher amounts of char if used as a precursor to high temperature (600-1000.degree. C. reaction condition) chars.

Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.

Abstract: Polysiloxane copolymers containing both photochromic and lightstabilizing groups with enhanced UV-fatigue resistance can be used as coatings for devices with variable optical density, including lenses, glazing, textiles and the like, to provide light-sensitive darkening effects. The photochromic groups are spironaphtooxazine groups and the lightstabilizing groups are hindered amine light stabilizing (HALS) groups.

Abstract: The invention relates to new 1,3,4-oxadiazine derivatives of the formula (I) ##STR1## in which Ar.sup.1 represents in each case optionally substituted aryl or hetaryl,Ar.sup.2 represents in each case optionally substituted aryl or hetaryl andX represents the group --(CHR.sup.1).sub.m --(CHR.sup.2).sub.n in whichR.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,m represents 0 or 1 andn represents 0 or 1,to a plurality of processes for their preparation, and to their use for combating animal pests.

Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.