Abstract: The invention provides a method for the synthesis of an 18F-labelled product comprising deprotected of a protected 18F-labelled compound using a deprotection agent comprising a weak acid and wherein neutralisation and buffering of the deprotected product are carried out by the addition of a neutralisation agent. The deprotected product is buffered in a pH range suitable for subsequent autoclaving and formulation into an injectable radiopharmaceutical.

Abstract: The present invention discloses novel methods and solid supports for the synthesis of 3?-amino oligonucleotides. The novel supports are based on an unsubstituted or ring-substituted hydroxymethylbenzoyl linker element wherein the hydroxymethyl group is esterified to a solid phase bound carboxylic acid and the carbonyl group is linked to an amino alcohol as an amide. Oligonucleotides are conveniently synthesized on the novel supports with no modifications in the standard phosphoramidite synthesis scheme. The ester function of the support is cleaved under the alkaline deprotection conditions for oligonucleotides to provide a free hydroxymethyl group that aids in the release of the 3?-amino oligonucleotide products with a free amino group through neighbor group participation. The free amino group of the oligonucleotides is available for further conjugation reactions to haptens, reporter groups, surfaces or other small molecules or biomolecules.

Abstract: The invention describes fluorescent biomolecule labeling reagents (I-SHark and phI-SHark) and their model compounds. Further described are methods of preparing and using the same.

Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.

Abstract: A fungicide can be provided by using, as an active ingredient, a diamine derivative of the following general formula (1): wherein R1 to R7 represent a specific substituent such as an alkyl group with 1 to 6 carbon atoms, and R8 represents an aryl group, which may be substituted or a heteroaryl group, which may be substituted.

Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.

Abstract: An advantageous process is provided for preparing methyl 4-(aminomethyl)benzoate by esterifying 4-(aminomethyl)benzoic acid and subsequently obtaining the methyl 4-(aminomethyl)benzoate, this process proceeding under specific pH and temperature control and isolation of the hydrochloride of methyl 4-(aminomethyl)benzoate formed as an intermediate being avoidable.

Abstract: A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.

Abstract: Novel acetylamino benzoic acid compounds, methods of using and pharmaceutical compositions comprising an acetylamino benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Abstract: Provided is an arylene derivative including a polar functional group represented by Formula 1: An arylene derivative including a polar functional group has excellent solubility in an organic solvent. A soluble compound of the arylene derivative can be used to form a thermally stable organic layer which can be used to form an organic light emitting device having low operating voltage, high efficiency, and excellent brightness.

Abstract: Novel platform mesogens, intermediates, and polymerizable mesogens made therefrom.

Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticals The invention relates to arylcycloalkyl derivatives having branched side chains and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.

Abstract: The invention provides methods and compositions useful for making synthetic peptide conjugates. In one embodiment, the invention provides compositions comprising the structure: wherein R is selected from lower substituted or unsubstituted alkyl, O, NH and S and P is an amine protection group. In more particular embodiments, the compositions comprise ?-amine protected 4,5-dehydroleucine or ?-amine protected (2S)-aminolevulinic acid and/or P is F-moc. These compounds may be incorporated into peptides, for example, peptides comprising a substituted or unsubstituted (2S)-aminolevulinic acid residue, such as (2S)-aminolevulinic acid residue is substituted with an O- or N-linked glycoconjugate, or a detectable label.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: The invention relates to compounds of the formula I in which the radicals are defined as specified, and also to their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: Disclosed are novel colorant compounds which contain one or more ethylenically-unsaturated (vinyl), photopolymerizable radicals which may be copolymewrized (or cured) with ethylenically-unsaturated monomers to produce colored compositions such as colored acrylic coatings and polymers, e.g., coatings and polymers produced from acrylate and methacrylate esters, colored polystyrenes, and similar colored polymeric materials derived from other ethylenically-unsaturated monomers. The present invention also pertains to processes for the preparation of certain of the photopolymerizable colorant compounds.

Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.

Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.

Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.

Abstract: Radiolabeled fluorinated compounds useful for imaging in the diagnosis of Parkinson's Disease are disclosed. Methods and kits for their synthesis are also disclosed.

Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.

Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases

Abstract: A method of preparing a 2-alkyl amino acid involves the aziridination of an alkylacrylate and the opening of the aziridine ring by addition of a side chain. This method can result in the preparation of enantiomeric excess of a 2-alkyl amino acid. The invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

Abstract: The present invention relates to a compound formula [I]: wherein Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

Abstract: Compounds having the formula are useful for treating conditions which arise from or are exacerbated by angiogenesis. Also disclosed are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.

Abstract: A compound represented by the following formula (1) or a salt thereof: wherein R1 represents a C1-12 alkyl group, phenyl group, 1-naphthyl group and the like, R2 represents a C2-12 alkyl group, (R3)b represents 0 to 4 substituents such as a halogen atom, R4 represents a lower alkyl group, R5 represents hydrogen atom or a lower alkyl group, n represents an integer from 2 to 4, and X represents —NH— or —O—, which has superior hypoglycemic action, hypolipidemic action and total cholesterol reducing action, and is useful as an active ingredient of a medicament for prophylactic and/or therapeutic treatment of diseases including diabetes mellitus, hyperlipidemia and the like.

Abstract: Compositions including a conjugate of ?-difluoromethylornithine can be applied topically to reduce hair growth.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.

Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: The invention provides methods and compositions useful for making synthetic peptide conjugates. In one embodiment, the invention provides compositions comprising the structure: wherein R is selected from lower substituted or unsubstituted alkyl, O, NH and S and P is an amine protection group. In more particular embodiments, the compositions comprise ?-amine protected 4,5-dehydroleucine or ?-amine protected (2S)-aminolevulinic acid and/or P is F-moc. These compounds may be incorporated into peptides, for example, peptides comprising a substituted or unsubstituted (2S)-aminolevulinic acid residue, such as (2S)-aminolevulinic acid residue is substituted with an O- or N-linked glycoconjugate, or a detectable label.

Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).

Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Abstract: Derivatives of fluorene, including ester derivatives of cyano(9H-fluoren-9-ylidene) acetic acid, and sunscreen compositions including a mixture of a photoactive compound and an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid are disclosed herein. Also disclosed are methods for terminating a polymer chain with an ester derivative of cyano(9H-fluoren-9-ylidene) acetic acid and methods of filtering out ultra-violet light from a substrate by the use of one or more such derivatives.

Abstract: Positionally isomeric diethyloctanediol dicarbamates and diethyloctanediol diallophanates, processes for preparing them, and their use as synthesis building blocks and constituents of adhesives, sealing compounds, and coating materials.

Abstract: The novel compound of the disclosure is 4-chloro-4-(4-ethoxy-phenyl)-2-(fluoren-9-ylidene-hydrazono)-but-3-enoic acid methyl ester (3F-19), and it alone or in combination with 4-(4-Ethoxy-phenyl)-2-(N?-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester (OF-13), appears useful in humans as therapeutic means for the eradication of tumors from the human's colon.

Abstract: A novel norbornene derivative represented by a general formula (1m) shown below is provided. By conducting a ring opening polymerization of this norbornene derivative, or by performing a subsequent hydrogenation following the ring opening polymerization, a ring opening polymer or a hydrogenated product thereof with an excellent low birefringence can be obtained. [wherein, at least one of R1 to R4 is a group selected from the group consisting of groups represented by a general formula (1-1) shown below and groups represented by a general formula (1-2) shown below] [wherein, at least one of RA, RB and Z is a group represented by the formula —C(O)O—].

Abstract: A new ligands that include a benzene ring in the backbone can be combined with a metal or metal precursor compound or formed into a metal-ligand complex catalyze a number of different chemical transformations, including olefin polymerization reactions. The ligands, complexes formed with the ligands and compositions including the ligands are useful catalysts, depending on the reaction.

Abstract: Mesogens having the following general formula: 1

Abstract: A polyisocyanate compound obtained by highly converting a bis(isocyanatomethyl)cyclohexane into a urethodione compound, a process for producing the compound, a polyisocyanate polyaddition composition obtained by polyaddition of the compound, a compound having at least two hydroxyl groups and a compound having one hydroxyl group, and a powder coating material using the composition as the curing agent. The powder coating material is advantageous for safety and health due to the absence of dissociation of blocking agents and for economy due to a content of latent NCO greater than conventional urethodione-based powder coating materials.

Abstract: Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals.

Abstract: The invention relates to the inhibition of histone deactylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.