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N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists

Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

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PYRIDIZINONE DERIVATIVES

The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof.

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Conversion of nucleophilic halides to electrophilic halides: Efficient and selective halogenation of azinones, amides, and carbonyl compounds using metal halide/lead tetraacetate

AlCl3/Pb(OAc)4 and ZnBr2/Pb(OAc) 4 are efficient electrophilic N- and alpha-C-halogenating agents. A variety of azinones, amides and carbonyl compounds were chemoselectively and regioselectively N-, or alpha-C-halogenated in good to excellent yield using AlCl3/Pb(OAc)4 and ZnBr2/Pb(OAc)4 in acetonitrile. Georg Thieme Verlag Stuttgart.

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2-Cyanopyridazin-3(2H)-ones: Effective and chemoselective electrophilic cyanating agents

2-Cyanopyridazin-3(2H)-ones are novel, effective, selective and electrophilic cyanating agents. A variety of amino, thiol and carbon nucleophiles are chemoselectively N-, S- or C-cyanated in excellent yield using 2-cyanopyridanzin-3(2H)-ones in water or tetrahydrofuran.

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Synthetic studies on isoquinoline derivatives with multidrug resistance (MDR) modulating activity

Tetrahydropyridazino-1,4-oxazinoisoquinoline derivatives with multidrug Resist. (MDR) modulating activity were designed and synthesized. A key step for cyclization of 1,4-oxazine ring was developed using K2CO3 and CH3CN in one-pot. Among prepared compounds, 2-(4-fluorobenzyl)-9,10-dimethoxy-12-methyl-6,7,11b,12-tetrahydropyridazino[4′, 5′,5,6] [1,4]oxazine-[3,4,-a]isoquinolin-1(2H)-one (1f) exhibited significant MDR reversing activity and low toxicity, which might be as potential MDR agent.

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Efficient use of 1,2-dihaloazine synthons in transition-metal-free preparation of diverse heterocycle-fused 1,4-oxazepines

A previously reported condensation reaction of ambiphilic 2-(1H-pyrazol-5-yl)phenols with various o-chloro-substituted nitroaromatic synthons to provide medicinally important tetracyclic pyrazolo[1,5-d][1,4]oxazepines was extended to more readily available and convenient-to-use 1,2-dihaloazines. Although 4,5-dichloropyridazin-3(2H)-ones and 2,3-dichloropyrazine are popular bis(electrophilic) partners in various SNAr-type condensations and also were efficiently used in the reaction reported herein, the facility with which various 3-bromo-2-chloropyridines underwent the same cyclization was unexpected. These reactions are presumed to occur as sequential intermolecular SNAr/Smiles rearrangement/intramolecular SNAr tandem reactions and provide a rare example of the transition-metal-free substitution of a bromine atom at the 3-position of a pyridine ring.

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Pyridazines with Heteroatom Substituents in Position 3 and 5, Part 1: 5-Hydroxy-3(2H)-pyridazinone and Its Derivatives

The synthesis of the title compound 7 was achieved starting with mucochloric acid via the pyridazinones 1,2 and 6.The electrolytic ionisation constants for 7 were found to be 4.81 (+/-0.03) and -0.3 (+/-0.3).Crystal structure analyses were performed for 7 and its “fixed” derivatives 6 and 9. – Keywords.Synthesis of 5-methoxy- and 5-hydroxy-3(2H)-pyridazinones; pKa Values of 5-hydroxy-3(2H)-pyridazinone; Crystal structure of 3(2H)-pyridazinones.

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The present invention provides a compound of Formula (I) or an agronomically acceptable salt thereof, wherein: R2 is selected from the group consisting of (A1), (A2) and (A3) wherein X1 is N or CR7X2 is N or CR8X3 is N or CR9X4 is N or CR6R1, R3, R4, R5 R6, R7, R8 and R9 are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), and to their use for controlling weeds, in particular in crops of useful plants.

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Piperazine and homopiperazine derivatives, pharmaceutical compositions containing them and process for preparing same

This invention relates to novel compounds of the general formula (I) and the pharmaceutically acceptable acid addition salts thereof. In the general formula (I) STR1 wherein Lip, A1, A2, Het and n are defined as in the specification. The compounds of the general formula (I) inhibit the lipid peroxidation and therefore, they are useful for the treatment or prevention of diseases and conditions wherein the inhibition of lipid peroxidation is desirable.

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Liquid reactive dyestuff preparations and their use

The invention relates to liquid reactive dyestuff preparations containing one or several dyestuffs, the chromophore of which has of from 1 to 8 SO3 H groups and of from 1 to 3 fiber-reactive groups, a solubilizer, an anionic dispersing agent and buffer substances and having a pH of from 3 to 7. These preparations are particularly stable to storage and are suitable for dyeing and printing natural and synthetic fiber material.

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