Joseph P Yevich

SYNTHESIS AND EVALUATION OF N-SUBSTITUTED 1-(5-FLUORO-2-PYRIMIDINYL)PIPERAZINE DERIVATIVES AS POTENTIAL ANTI-ISCHEMIC AGENTS

Abstract A number of N-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives were prepared and evaluated for binding to sigma and serotonin 5-HT 1A and 5-HT 2 receptor subtypes as well as for their protection against nitrogen anoxia-induced lethality in rats. Although various compounds exhibited good binding affinity and/or anti-anoxic effects, there was no obvious correlation between their receptor binding and in vivo effects.

Antimigraine agents: July 1995 - December 1996

The patent literature pertaining to agents for the treatment of migraine headache and related disorders has been reviewed for the period of July 1, 1995 to December 31, 1996. Included are patents on serotonergic agents, such as 5-hydroxytryptamine 1D (5-HT1D) receptor subtype agonists and 5-HT2 and 5-HT3 antagonists. Also covered are patents describing chemical entities that may be effective in migraine therapy based on their pharmacological actions as adrenergic agents, tachykinin receptor antagonists or inhibitors of nitric oxide synthetase (NOS). Selected references from the recent scientific literature have also been cited.

Chemistry in the Pharmaceutical Industry

This chapter will discuss the role of chemistry within the pharmaceutical industry. Although the focus will be upon the industry within the United States, much of the discussion is equally relevant to pharmaceutical companies based in other first world nations such as Japan and those in Europe. The major objective of the pharmaceutical industry is the discovery, development, and marketing of efficacious and safe drugs for the treatment of human disease. Of course drug companies do not exist as altruistic, charitable organizations but like other share-holder owned corporations within our capitalistic society must achieve profits in order to remain viable and competitive. Thus, there exists a conundrum between the dual goals of enhancing the quality and duration of human life and that of increasing stock-holder equity. Much has been written and spoken in the lay media about the high prices of prescription drugs and the hardships this places upon the elderly and others of limited income.

Patent Update: Central & Peripheral Nervous Systems: Antimigraine agents: July 1994 - June 1995

The patent literature pertaining to agents for the treatment of migraine headache and related disorders has been reviewed for the period of July 1, 1994 to June 30, 1995. Included are patents on serotonergic agents, i.e. 5-HT1D agonists, 5-HT2 receptor ligands and 5-HT3 antagonists as well as patents disclosing chemical entities claimed to have potential antimigraine activity via non-serotonergic mechanisms, e.g. tachykinin receptor antagonists and nitric oxide synthetase inhibitors. Relevant references from the recent scientific literature have also been cited.