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Synthesis and substance P antagonist activity of naphthimidazolium derivatives

The synthesis of unsymmetrical naphth[2,3-d]imidazolium and bridged naphth[2,3-d]imidazolium derivatives and their substance P (SP) antagonist activity are described. All compounds were evaluated for their ability to displace SP from neurokinin-1 (NK-1) receptor sites using standard receptor binding methodology (rat forebrain membrane). 1,3-Diethyl-2-[3-(1,3-dihydro- 1,3,3-trimethyl-2H-indol-2-ylidene)-1-propenyl]-1H-naphth[2,3-d]imidazolium chloride (7a), a representative compound in this series, was further evaluated for SP antagonist activity in a guinea pig ileum contractility assay. In vivo SP antagonist activity of 7a was demonstrated using SP-induced salivation and paw edema models performed in rats.

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Synthesis of 2-(phenylselanyl)tetrahydrofurans from gamma-lactones and of gamma-hydroxydiselenoacetals from gamma-lactols

A known one-pot procedure for the synthesis of 2-(phenylselanyl)tetrahydrofurans could be applied to the transformation of gamma-lactones 3a-c into 2-(phenylselanyl)tetrahydrofurans 1a-c. Surprisingly, formation of gamma-hydroxydiselenoacetals 5b and 5c was observed when gamma-lactols 4b and 4c were treated with selenophenol and boron trifluoride etherate.

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Novel HMG-CoA reductase inhibitors

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): STR1 wherein: n is 1 to 5; R is hydrogen or STR2 R1 is hydrogen or methyl; R2 is hydrogen or methyl; and R3 is hydrogen, C1-5 alkyl or C1-5 alkyl substituted with a member of the group consisting of phenyl, dimethylamino, or acetylamino; and the dotted lines at a, b and c represent optional double bonds and pharmaceutically acceptable salts of the compounds (II) in which R3 is hydrogen are disclosed.

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1679-47-6, Name is 3-Methyldihydrofuran-2(3H)-one, belongs to Tetrahydrofurans compound, is a common compound. COA of Formula: C5H8O2In an article, once mentioned the new application about 1679-47-6.

Pyrrolo[1,2b]pyridazine compounds and their uses

Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): [image] including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

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Metal-Free Synthesis of N-Aryl Amides using Organocatalytic Ring-Opening Aminolysis of Lactones

Catalytic ring-opening of bio-sourced non-strained lactones with aromatic amines can offer a straightforward, 100 % atom-economical, and sustainable pathway towards relevant N-aryl amide scaffolds. Herein, the first general, metal-free, and highly efficient N-aryl amide formation is reported from poorly reactive aromatic amines and non-strained lactones under mild operating conditions using an organic bicyclic guanidine catalyst. This protocol has high application potential as exemplified by the formal syntheses of drug-relevant molecules.

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PROCESS FOR MANUFACTURING POLYAMIDE

In one or a plurality of embodiments, a process for manufacturing polyamide without using PrO (propylene oxide) in synthesis is provided. In one or a plurality of embodiments, provided is a process for manufacturing polyamide, including steps (a) to (c): (a) reacting diacid dichloride monomer with at least two kinds of diamine monomers in a solvent so as to generate polyamide; and (b) removing hydrochloric acid physically out of a reaction system, the hydrochloric acid being generated during the reaction in the step (a); or (c) adding a trapping reagent capable of trapping hydrochloric acid, at any time at least before the step (a), at the same time of starting the step (a), or during the step (a), wherein at least one of the diamine monomers is a diamine monomer containing a carboxyl group, and the trapping reagent does not include propylene oxide.

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Tetrahydrofuran – Wikipedia,
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TRICYCLIC COMPOUNDS

The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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Alpha-methyl-production of gamma-butyrolactone (by machine translation)

PROBLEM TO BE SOLVED: alpha-methyl-gamma-butyrolactone of high purity is obtained. SOLUTION: alpha-methyl-gamma is expressed by the following eq. (1) in the production of-butylolactone, reactive soln. org. base or its salt is added to the process, and including the step of distilling the reaction liquid, alpha-methyl-production of gamma-butyrolactone. Selected drawing: no (by machine translation)

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POLY-ADP RIBOSE POLYMERASE (PARP) INHIBITORS

The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.

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A METALLIC NANOPARTICLE DISPERSION

A metallic nanoparticle dispersion includes metallic nanoparticles, a binder, and a liquid carrier, characterized in that the binder is a copolymer of vinyl chloride and a hydroxyfunctional monomer.

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Tetrahydrofuran – Wikipedia,
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