Compositions, systems and methods that allow for the detection of the actual physical delivery of a pharmaceutical agent to a body are provided. Embodiments of the compositions include an identifier and an active agent. The invention finds use in a variety of different applications, including but not limited to, monitoring of therapeutic regimen compliance, tracking the history of pharmaceutical agents, etc.

Pharma-informatics system

Publisher Summary This chapter focuses on pharmacologically active pyridazine derivatives. This chapter describes that the cardiovascular diseases occupy first place as causa mortis in civilized countries continues to influence strongly the research in the field of bioactive pyridazine derivatives, as shown by the enormous number of patents and papers dealing with pyridazines useful as cardiovascular drugs. Cardiovascular active pyridazines are divided into the following classes: cardiotonics (including pyridazines exhibiting both positive inotropic and systemic vasodilator activity—that is, inodilators), coronary vasodilators, antiarrhythmics, cardioselective P-blockers, antihypertensive agents, antihypotensive agents, and hypocholesterolaemic agents. The increasing interest in the chemistry and in biological activities of pyridazines as observed within the past 15 years has resulted in the development of a wide variety of interesting novel drugs and pharmacological tools. It is hoped that this chapter will not only facilitate the access to the literature on pharmacologically interesting pyridazines but also stimulate further research in this field.

Pharmacologically active pyridazine derivatives. Part 1.

New 3- and 4-hydroxyfuranones as anti-oxidants and anti-inflammatory agents.

Publisher Summary This chapter discusses the synthetic methods for the synthesis of pyridazine. Numerous syntheses of pyridazines follow the well-known approaches, but there are some significant developments and new methods, such as syntheses of pyridazines by cycloaddition, which have become powerful synthetic tools in the hands of organic chemists. Pyridazines have been investigated intensely, from a theoretical standpoint, by spectroscopic methods. Several aspects of pyridazine chemistry and activity are included in this chapter. The chapter deals with aromaticity and antiaromaticity of azines and substituent effects in azines. The chapter covers unusual organic compounds including azoalkanes, cycloadditions of azadienes, diazoquinones, thermal and photochemical decomposition of azoalkanes, and one-electron oxidations. The pyridazine nucleosides, some biologically active pyridazines, antihypertensive 3-hydrazinopyridazines, and pyridazines with antimicrobial activity are also reviewed in the chapter

Advances in Pyridazine Chemistry

The invention relates to methods of targeted drug delivery of compounds, including, chemical agents, (poly)peptides and nucleic acid based drugs (like DNA vaccines, antisense oligonucleotides, ribozymes, catalytic DNA (DNAzymes) or RNA molecules, siRNAs or plasmids encoding thereof). Furthermore, the invention relates to targeted drug delivery of compounds to extravascular and intracellular target sites within cells, tissues and organs, in particular to target sites within the central nervous system (CNS), into and across the blood-brain barrier, by targeting to glutathione transporters present on these cells, tissues and organs. Thereto, the compounds, or the pharmaceutical acceptable carrier thereof, are conjugated to glutathione-based ligands that facilitate the specific binding to and internalization by these glutathione transporters.

Glutathione-based drug delivery system

1. The properties of a new antihypertensive agent, SK&F 92657, dl-3-[2-(3-t-butylamino-2-hydroxypropoxy)phenyl]-6-hydrazinopyridazine, have been studied. 2. The compound caused a sustained fall in blood pressure in several species as a result of precapillary vasodilatation, particularly in the renal and coronary vasculatures. 3. The β-adrenoreceptor-blocking actions of SK&F 92657 prevent reflex cardiac stimulation.

SK&F 92657, a Novel Antihypertensive Acting by Precapillary Vasodilatation and β-Adrenoreceptor Blockade

Efficient preparations of 4- and 5-phenyl-4,5-dihydropyridazin-3(2H)-ones have been developed, the main reactions of these compounds have been studied, and the synthetic routes have been used to give analogues with substituents in the phenyl rings.In the best synthesis of the 4-phenyldihydropyridazinone (72% overall yield) the product was obtained from phenylacetic acid by three simple stages. This approach was applied in preparations of the 2- and 4-hydroxyphenyl compounds and, in conjunction with a recent method for amine protection, the 4-aminophenyl analogue. A four stage synthesis starting from benzaldehyde gave the 5-phenyl-dihydropyridazinone in 47% overall yield; hydroxybenzaldehydes were similarly converted into 5-(allyloxyphenyl)dihydropyridazinones.Oxidation to phenylpyridazinones occurred more readily with the 4- and 5-phenyldihydropyridazin-ones than with the 6-phenyl isomer. The 4- and 5-dihydropyridazinones were smoothly reduced to tetrahydropyridazinones by hydrogenation over platinum but were unaffected by palladium in the presence of hydrazine or cyclohexene.

Preparation and some reactions of 4- and 5-aryl-4,5-dihydropyridazin-3(2H)-ones

The compounds are 6-(3-substituted amino-2-hydroxypropoxyaryl)-4,5-dihydro-3(2H)-pyridazinones which are β-adrenergic blocking agents.

Pharmaceutical compositions and methods of inhibiting β-adrenergic receptors

The compounds are 3-(3-(3-substituted amino-2-hydroxypropoxy)phenyl)-6-hydrazino pyridazines which have β-adrenergic blocking and vasodilator activity.

3-(3-(3-Substituted amino-2-hydroxypropoxy)phenyl)-6-hydrazino pyridazines and their use as vasodilators and β-adrenergic blocking agents

Substituted derivatives of 3-chloro-6-phenylpyridazine which are useful intermediates in the preparation of substituted phenylhydrazinopyridazines which have β-adrenergic blocking and vasodilator activity.

Anthony Maitland Roe

Papers

SK&F 92657, a Novel Antihypertensive Acting by Precapillary Vasodilatation and β-Adrenoreceptor Blockade

Preparation and some reactions of 4- and 5-aryl-4,5-dihydropyridazin-3(2H)-ones

Pharmaceutical compositions and methods of inhibiting β-adrenergic receptors

3-(3-(3-Substituted amino-2-hydroxypropoxy)phenyl)-6-hydrazino pyridazines and their use as vasodilators and β-adrenergic blocking agents

3-chloro-6-phenylpyridazine compounds