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Biomedical subjects

R J Borgman

Publications and source records attributed to R J Borgman.

14 recordsLinked to original sources
PubMed1992

Development of an orphan drug by a start-up company. MetroGel for rosacea.

The Orphan Drug Act of 1983, along with the discovery of a new use for a known drug and an investor willing to assume the necessary risk, brought about the formation of a start-up pharmaceutical company. The primary incentive of the Orphan Drug Act of seven years of marketing exclusivity provided the protection from competition necessary for recovery of the significant research and development and marketing costs. The orphan product, MetroGel, for the treatment of rosacea, required approximately five years of development before it was approved for marketing by the Food and Drug Administration. MetroGel has become the number one drug in the United States for the treatment of rosacea. It currently is marketed in other countries through a licensing agreement with a major pharmaceutical company.

Administration, Topical↗
PubMed1984

[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.

Novel [(arylcarbonyl)oxy]propanolamines were synthesized and investigated as potential ultrashort-acting beta-adrenergic receptor blockers. Many of these analogues exhibited good potency and short duration. The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog. It has been selected as a candidate for further clinical study. Structure-activity relationships and structure-duration relationships for these new beta-blockers are also discussed.

Adrenergic beta-Antagonists↗
PubMed1982

Ultra-short acting beta-blockers: a proposal for the treatment of the critically ill patient.

Beta-blockade is of proven value in the therapy of acute myocardial infarction but, unfortunately, may produce cardiac failure by removal of needed sympathetic support. The long duration of action of available blockers (hours) makes reversal of failure a complicated problem and precludes rapid modification of therapy to match changing autonomic conditions. To improve the safety and efficacy of beta-blockade in this setting we have developed the concept of ultra-short beta-blockade and have identified a novel beta-blocker (ASL-8052) which possesses a duration of action less than 15 minutes. This compound is cardioselective and possesses efficacy in an animal model of acute myocardial infarction. It, therefore, appears to be suitable for rapid attainment of controlled levels of beta-blockade via intravenous infusion and rapid recovery from beta-blockade if required by the clinical situation. The compound should, therefore, be useful for safe therapy in critically ill cardiac patients.

Adrenergic beta-Antagonists↗
PubMed1979

Synthesis and pharmacology of potential beta-blockers.

Several 1-(4-substituted phenoxyl)-2-hydroxy-3-isopropylaminopropanes and 1-(4-substituted phenoxy)-2-hydroxy-3-[3,4-dimethoxyphenethyl]aminopropanes were synthesized for possible beta-adrenergic receptor blockage. The compounds were synthesized by reaction of the 4-substituted phenol with epichlorohydrin and subsequent opening of the resulting epoxide with either N-isopropylamine or N-3,4-dimethoxyphenethylamine. Preliminary biological testing indicated a decrease in the beta-blocking potency and the duration of action.

Adrenergic beta-Antagonists↗
PubMed1976

Diester derivatives as apomorphine prodrugs.

A series of diesters of apomorphine was synthesized to serve as prodrugs. They were converted in vivo to free apomorphine, which could be detected in the brain. Stereotyped gnawing behavior and unilateral rotation similar to that produced by apomorphine were induced by all of the diesters but the time course of action of the latter was prolonged. The duration of action generally increased with the size of the ester substituent and appeared to correlate inversely with the rate of hydrolysis of the esters by liver extracts. It is concluded that the diesters serve as prodrugs of apomorphine and their prolonged duration is partly explained by a decreasing rate of hydrolysis attributable to increased steric hindrance at the acyl carbon atoms.

Animals↗