Oread Laboratories, Inc.

Merck + Co., Inc.

Iprx, Inc.

Takeru Higuchi, Deceased

Arnold J Repta

Larry A Sternson

Pierre M De Montigny

By Kenji Higuchi, Co-executor

Jose Alexander

John F Stobaugh

Ooi Wong

Kenji W Higuchi, Co-executor

John F Stabaugh

By Martin Dickinson, Jr, Co-executor

The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.

Pyroglutamic acid esters used as dermal penetration enhancers for drugs

There is provided a fluorescent adduct which is amenable to detection by fluorometric and electrochemical techniques. The adduct is of the formula: ##STR1## wherein X is a radical derived from a primary amine of the formula X--NH.sub.2 and where R.sub.1 --R.sub.6 are selected from various organic or inorganic substituents.

Polycyclic nitriles

A compound having the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are independently selected from hydrogen; hydroxy; fluorine; bromine; chlorine; C.sub.1 -C.sub.20 alkyl; C.sub.2 -C.sub.20 alkenyl; C.sub.2 -C.sub.20 alkynyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.2 -C.sub.20 (monohydroxy or polyhydroxy)alkyl; C.sub.1 -C.sub.20 (monohalo or polyhalo)alkyl; carboxy; C.sub.1 -C.sub.20 alkylcarboxy; C.sub.1 -C.sub.20 alkenylcarboxy; C.sub.1 -C.sub.20 carboxyalkyl; C.sub.1 -C.sub.20 alkanoyl; C.sub.1 -C.sub.20 alkanoyloxy; C.sub.1 -C.sub.20 alkoxycarbonyl; carbamoyl; carbamyl; C.sub.1 -C.sub.20 alkylcarbamyl; sulfo; C.sub.1 -C.sub.20 alkylsulfonyl; C.sub.1 -C.sub.20 alkylsulfinyl; C.sub.1 -C.sub.20 alkylsulfoxide; C.sub.1 -C.sub.20 alkylsulfone; thio; C.sub.1 -C.sub.20 alkylthio; amino; nitro; C.sub.1 -C.sub.20 alkylamino; C.sub.1 -C.sub.20 aminoalkyl; substituted or unsubstituted phenyl or benzyl, the substituents being selected from hydroxy, fluorine, bromine, chlorine, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 (monohydroxy or polyhydroxy)alkyl, X is methyl or oxygen and n is 0 to 20. The invention is also directed to a method for increasing the topical penetration of a physiologically active agent across the skin or membrane of a mammalian organism. Also claimed is a pharmaceutical composition and a novel method for preparing 1-substituted-4-imidazolin-2-one.

Imidazolin-2-ones

A method of assaying primary amines or cyanide is disclosed. The process is carried out by reacting a substituted or unsubstituted naphthalene-2,3-dicarboxaldehyde or o-phthalaldehyde, reactive with primary amines and cyanide, with cyanide ions and at least one primary amine to form an adduct amenable to fluorometric or electrochemical assaying techniques. The adduct is then fluorometrically or electrochemically assayed. Also disclosed are 1-cyano-benz[f]isoindole adducts.

Assaying method for primary amines using aromatic dialdehydes

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Lawrence, KS, United States of America

Takeru Higuchi, Deceased