Abstract: Triazabutadiene molecules, such as those according to Formula B, which can yield aryl diazonium species, and methods of use of triazabutadiene molecules, for example methods and compositions for yielding an aryl diazonium species from a triazabutadiene molecule, e.g., a protected aryl diazonium species in the form of a triazabutadiene. In some embodiments, an enzyme catalyzes the reaction yielding the aryl diazonium species from the triazabutadiene molecule. As an example, the methods and compositions herein may be used for delivery of drugs.

Abstract: Triazabutadiene molecules for use in applications. e.g., those involving fluorogenic molecules, e.g., triazabutadiene molecules configured to generate a fluorescent compound when combined with a second molecule, e.g., upon reaction with a tyrosine molecule or other appropriate molecule; and protected triazabutadiene molecules that are stable in acidic conditions and are adapted to release an active (e.g., acid-labile} triazabutadiene molecule upon appropriate conditions, and methods for producing and using said protected or releasable triazabutadiene molecules (and products of cleavage).

Abstract: The invention includes a selective method of modifying the N-terminus of a protein using an aminoacyl tRNA transferase. In certain embodiments, the method comprises contacting a solution of the protein or peptide with a transferase and a derivative of a molecule, whereby the N-terminus of the protein or peptide is derivatized with the molecule.

Abstract: A photosensitive compound represented by formula (1) or formula (2). (Chemical formula 1) (In formula (1) and formula (2), n is an integer of 1-3; R1 is a linear or branched alkyl group having 1-6 carbon atoms or an alkylene group having 2-6 carbon atoms formed from two R1 together; R2 is —NR3R4; R3 and R4 are each independently a linear or branched alkyl group or alkenyl group having 1-6 carbon atoms, a linear or branched alkylene group having 2-6 carbon atoms formed by R3 and R4 together, or a linear or branched alkylene group or alkenylene group having 3-8 carbon atoms optionally containing an oxygen atom or nitrogen atom.

Abstract: The design, modeling, synthesis, biological evaluation, and photoaffinity labeling studies of a series of photoreactive potent and selective HDACs 1 and 2 benzamide based probes are disclosed herein.

Abstract: The present disclosure sets forth the compound 3-azidopicric acid and a method of making the same. The method of producing 3-azidopicric acid is a two step reaction process of first reacting 3-aminopicric acid with sulfuric acid and sodium nitrite, and then reacting the result of the first step with phosphoric acid and sodium azide. Additionally described is a method of producing KDNP (4,6-dinitro-7-hydroxybenzofuroxan, potassium salt), by reacting 3-AzPA with potassium bicarbonate.

Abstract: The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5? end or 3? end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same.

Abstract: The invention relates to carbon surfaces modified with one or more azide groups. The invention also relates to methods of modifying carbon surfaces with one or more azide groups.

Abstract: The invention provides compounds of the formulas described herein and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.

Abstract: Azido-diarylpyrimidine (azido-DAPY) compounds, and compositions containing such compounds, are provided. In addition, methods of using azido-diarylpyrimidines to inactivate reverse transcriptases, prepare inactivated viruses, and treat or prevent viral infections are also provided.

Abstract: A cross-linking moiety having a general formula I: N3—ArF—W, wherein ArF comprises a fluorinated phenyl azide group having at least one non-fluorine substituent that is bulkier than fluorine at a meta position relative to the azide group, and W comprises an electron-withdrawing group.

Abstract: Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Abstract: There is provided a class of crosslinking compound, said compound comprising (i) one or more fluorinated aromatic group; and (ii) one or more ionizable group, wherein the crosslinking compound is soluble in at least one polar solvent. Methods of preparing the crosslinking compounds are also disclosed. There is further provided devices obtainable from the methods of preparing the crosslinking compounds.

Abstract: Azido-diarylpyrimidine (azido-DAPY) compounds, and compositions containing such compounds, are provided. In addition, methods of using azido-diarylpyrimidines to inactivate reverse transcriptases, prepare inactivated viruses, and treat or prevent viral infections are also provided.

Abstract: The invention relates to carbon surfaces modified with one or more azide groups. The invention also relates to methods of modifying carbon surfaces with one or more azide groups.

Abstract: To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH?CH.

Abstract: Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Abstract: Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Abstract: A process of synthesizing hyperbranched polytriazoles, linear and hyperbranched poly(aroyltriazoles) by Huisgen 1,3-dipolar cycloaddition. The polytriazoles were prepared by A2+B3 method to avoid self-polymerization during monomer preparation and storage. The polymers are light emissive and can be crosslinked to generate well-resolution photopatterns upon UV irradiation. White light emission patterns were observed with fluorescence microscopy. The high molecular weight poly(aroyltriazoles) (up to 26000 Da) are prepared in high yields (up to 92.0%) and with high regioselectivity (the ratio of 1,4- and 1,5-disubstituted 1,2,3-triazole is equal or larger than 9:1). The polycyclomerization is not moisture or oxygen sensitive and therefore, no special precautions are necessary before and during the reaction. All the polymers are processible, easily film-forming, and curable into thermosets by heat or irradiation. The hyperbranched polymers can act as fluorescent adhesive materials with large tensile strength.

Abstract: The invention provides compounds of formula I and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.

Abstract: Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Abstract: The present invention describes a bioconjugation strategy and compounds that are useful therein in which a fluorescent signal is produced when two molecular or supramolecular entities are linked by chemoselective combination of one linker having an azido or halide substituent group with another linker having a cyano or an alkyne substituent group. A kit is also provided.

Abstract: The invention provides a photosensitive resin which can readily form, through photo-crosslinking, a surface coating which has hydrophilicity and high bioadaptability; a photosensitive composition containing the photosensitive resin; and a photo-crosslinked structure obtained from the photosensitive composition.

Abstract: Pyrocatechin derivatives of formula I wherein R illustrates a group of formulae Ia, Ib, Ic or Id R1 is 4-halogen-but-2-enyl, R2 is lower alkyl or cycloalkyl, R3 is lower alkoxy and R4 is lower alkoxy lower alkoxy, or, where R is a group of formula (Ia), it is hydroxy, hydroxy lower alkoxy or a group of formula Ie R5 is reactive esterified hydroxy, R6 is azido and R7 is lower alkyl, lower alkenyl, cycloalkyl or aryl lower alkyl, and their salts, are valuable intermediates in the production of active ingredients for medicaments.

Abstract: There is provided a class of crosslinking compound, said compound comprising (i) one or more fluorinated aromatic group; and (ii) one or more ionisable group, wherein the crosslinking compound is soluble in at least one polar solvent. Methods of preparing the crosslinking compounds are also disclosed. There is further provided devices obtainable from the methods of preparing the crosslinking compounds.

Abstract: Azidoaryl-substituted cyclooctene monomers and synthesized and used in the preparation of various copolymers. Among these copolymers are those prepared from ring-opening metathesis polymerization of cyclooctene, polyethylene glycol-substituted cyclooctene, and azidoaryl-substituted cyclooctene. These copolymers are useful in the formation of crosslinked films that reduce fouling of water purification membranes.

Abstract: The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV, its production method, an intermediate compound useful for its production and a pharmaceutical composition containing these compounds, and the present invention relates to a compound represented by the formula (I): (wherein A represents —(CH2)n—, etc.; B represents —(C?O)—, etc.; D represents —(CH2)m—R?, etc.; E represents a hydrogen atom, etc.; G represents —(CH2)p-J, etc.; bond Q represents a single bond or double bond; and R1, R2 and R3 may be the same or different and each represent a hydrogen atom, etc.), a prodrug thereof or a pharmaceutically acceptable salt thereof.

Abstract: Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove ?-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified.

Abstract: The present invention relates to a water-soluble photosensitive compound represented by the general formula (1): or by the general formula (2): in the formula, X represents a direct bond, an alkylene group containing 1 to 5 carbon atoms, —CH2O—, —OCH2—, —CH2OCH2—, —O—, —S— or —SO2—, and Z represents —SO3?.Q+, —COO?.Q+ or —SO2NR2, in which Q+ represents Li+, Na+, K+ or N+R4 and R represents a hydrogen atom and/or an alkyl group containing 1 to 5 carbon atoms, said alkyl group optionally having one hydroxy, ether, carbonyl, carbonyloxy or oxycarbonyl group, wherein a photosensitive group has an absorption maximum wavelength of not longer than 305 nm in the ultraviolet absorption spectrum thereof.

Abstract: The present invention provides a novel photosensitive compound having an azido group suitable for exposure to light of a short wavelength; a photosensitive resin containing the photosensitive compound; and a photosensitive composition containing the photosensitive compound or photosensitive resin. The photosensitive compound containing a photosensitive unit represented by formula (1): wherein R is selected from among the following groups, R: X is selected from among the following groups, X: and each of Y and Z represents a hydrogen atom, an alkyl group, an acetal-group-containing alkyl group, an aryl group, an aralkyl group, or a substituent containing a base-forming nitrogen atom, wherein at least one of R and X contains an azido group.

Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1

Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: 1

Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.

Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

Abstract: The invention provides a novel azidocinnamaldehyde compound which, when used as an intermediate for providing a photosensitive moiety of a photoresist, introduces a photosensitive moiety having high sensitivity and attaining high contrast between the exposed portion and the unexposed portion, and which per se can serve as a photosensitive moiety.

Abstract: This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interteukin-8 (IL-8).

Abstract: The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.

Abstract: The invention relates top a light sensitive, aqueous alkali developing, negatively acting resist, comprising a phenolic resin as a binder, and a diazostilbene disulfonic acid ester light sensitive component, a solvent or mixture of solvents, and film forming and/or film stabilizing additives, and to a process for preparing the light sensitive component.

Abstract: Indane compounds of general formulas (7) and (8) and their pharmaceutical use particularly to achieve smooth muscle relaxing activity and/or mast cell stabilizing activity and/or anti-inflammatory activity as described, wherein in formula (7) R2 to R13, in formula (8) R1 and R3 and R13 are selected from one or more of the same or different of: H, halo, hydroxy, alkoxy, aryloxy, acetoxy, carboxy, alkyl carbonyl, hydro carbonyl, amino, amido, alkylamino, hydroxylamino, amine oxide groups, azo groups, cyano, hydrazino groups, hydrazide groups, hydrazone groups, imide groups, iminoether groups, ureyl groups, oxime, nitro, nitrate, nitrite, nitroso groups, nitrile, heterocyclic groups containing heretro atoms containing one or more of N, O or S, aralkyl groups, mono and polybenzoid aryl groups, substituted aryl groups, thiol, thioureyl, phenylthiol groups, sulphonic acid groups, sulphoxide groups, sulphone groups, alkyl containing 1 to 10 carbon atoms or cycloalkyl groups containing 3 to 8 carbon atoms which may s

Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The invention is directed to a novel compounds comprising 4-azidotetrafluoroaniline and the alkyl, acyl and sulfonamide derivatives thereof and to methods of making and using the same. The novel compounds are useful as a photoaffinity probe to study protein structure and function. Two methods for preparing 4-azidotetrafluoroaniline are disclosed, each employing a stable carbamate intermediate from which the 4-azidotetrafluoroaniline is derived.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: The photosensitive compound of the present invention contains the following unit: ##STR1## and is particularly expressed by the following formula: ##STR2## Different photosensitive resin compositions can be prepared from this novel photosensitive resin compound, and the resulting photosensitive resin compositions do not raise the problem of environmental pollution, exhibit high resolution, possess a high level of sensitivity, and exhibit excellent adhesion with substrates, coating characteristics and storage stability.

Abstract: The present invention provides a compound having the structure: ##STR1## wherein R.sub.1 is a saturated or unsaturated linear or branched chain alkyl group, or a cholestanyl group; wherein R.sub.2 is a 2-indolyl, 3-indolyl, 4-indolyl, 5-indolyl, 4-hydroxyphenyl, 4-(arylalkyloxy)phenyl, 3,4-dihalophenyl, 4-hydroxy-3,5-dihalophenyl, 4-azidophenyl or 4-halophenyl group; wherein R.sub.3 is H, a linear or branched chain alkyl or alkenyl group, or a phenyl, 2-azidophenyl, 3-azidophenyl, 4-azidophenyl group, or an a alkenylacyl, 3-amino-3-butylpropyl, N-[N-(N-{4-azidobenzoyl}aminopropyl) aminopropyl], cis- or trans-cinnamyl, 2-amino-2-[(4'-azidophenyl)acetyl, (trifluoromethyl)aminoacetyl or D- or L-arginyl group bonded through the .alpha.-carbonyl moiety thereof; R.sub.4 is H, or a linear or branched chain alkyl group; wherein R.sub.5, R.sub.6 and R.sub.

Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.