US Government as Represented by the Secretary of the Army

Calspan Corporation

Other

West Laboratories, Inc.

Edward A Nodiff

Andrew J Saggiomo

Abraham Cantor

Eugene H Chen

Improvement in the treatment of malaria has been demonstrated with 5-[(aryl)alkoxy] primaquine compounds and 5[(heterocycle)alkoxy] primaquine compounds. These primaquine related compounds are effective in malarial chemotherapy. The 5-arylalkoxy primaquine compounds of the invention are at least as effective in malarial treatment as the prior are 5-alkoxy primaquine compounds, but are not as toxic as the 5-alkoxy compounds at higher dosage ranges. The 5[(heterocycle)alkoxy] primaquine compounds show less toxicity than primaquine in blood schizonticidal studies and are comparable to the 5-arylalkoxy primaquine compounds in efficacy.

5-(phenylalkoxy)primaquine and 5[(heterocycle)alkoxy] primaquine

Improvement in the treatment of malaria has been demonstrated with 5-arylalkoxy primaquine compounds of the formula ##STR1## wherein R.sub.2 represents H or methyl, R represents an alkylene group having from about 2 to about 12 carbon atoms, R' represents a substituted or non-substituted aryl moiety, such as phenyl and napthyl, and pharmaceutically acceptable salts thereof, wherein the salt forming acid may be organic or inorganic in nature. These primaquine related compounds are effective in malarial chemotherapy, by exerting plasmodicidal activity on malarial parasites present in both the blood and formed tissues of the mammalian host. The 5-arylalkoxy primaquine compounds of the invention are at least as effective in malarial treatment as the prior art 5-alkoxy primaquine compounds, but are not as toxic as the 5-alkoxy compounds at higher dosage ranges.

5-(phenylalkoxy)primaquine compounds and their use for treatment of

Improved means for the chemotherapy of malaria have been achieved with 5-oxy-primaquine analogues having the formula: ##STR1## wherein R.sub.4 represents hydrogen or a methyl grouping, and R represents an alkyl group containing 3 to 12 carbon atoms and pharmaceutically acceptable salts thereof, wherein the salt-forming acid may be organic or inorganic in nature. These primaquine-related compounds afford improvement in the chemotherapy of malaria by exerting plasmodicidal action on malaria parasites which may be present in either the blood, formed tissues, or blood and formed tissues of the mammalian host. Such broad and practical spectrum of effectiveness distinguishes the said primaquine analogues, which may be administered parenterally or perorally to infected animals.

5-(Straight chain 3-12 carbon alkoxy)-8-quinolinamines and their use for

An improved process for producing 8-NHR quinolines from 8-aminoquinolines disclosed. The process comprises reacting 8-aminoquinolines with a substituted alkyl halide in the presence of an amine having a boiling point of 80.degree.-90.degree. C. The amine functions as an acid acceptor whereby the amine salt formed may be efficiently separated from the 8-NHR quinoline formed without expensive or time consuming purification steps. The reaction may be carried out in the presence of a solvent such as an alcohol.

Process for production of 8-NHR quinolines

An epoxy adhesive sealant composition comprised of an uncured epoxy resin composition and a composition capable of curing the epoxy resin composition, one of said compositions containing a coloring agent effective to impart latently transient color to said composition unlike the color of the non-colored composition. Substantially equal amounts of each of said compositions are combined to form a substantially uniformly colored composition which becomes essentially colorless with curing of the epoxy resin composition.

Epoxy adhesive sealant

A new group of compounds, generically classed as phenothiazinyl sulfides, are described having the formula: ##STR1## wherein n is 1 or 2, x and/or y and/or z represent 0, 1 or 2; R.sub.1 may be H, alkyl, aryl, alkaryl, acyl, haloacyl and biologically activating aminoalkyl groups known in the medicinal arts, such as --(CH.sub.2).sub.3 --N(CH.sub.3).sub.2, ##STR2## and -[2-(1-methyl-2-piperidyl)ethyl]; and R.sub.2 and/or R.sub.3 and/or R.sub.4 and/or R.sub.5 and/or R.sub.6 and/or R.sub.7 represent H, OH, Cl, Br, F, CF.sub.3, SH, NO.sub.2, CN, COOH, alkyl, alkoxy, sulfamoyl, dimethylsulfamoyl, dimethyl amino, aryl, alkaryl, acyl, aryloxy, methyl sulfonyl, methyl thio, and -S-phenothiazinyl substitutents; and as charge-transfer complexes of iodine therewith in which the number of moles of iodine associated with the molecule equals 1.5 (range 0.75 to 3.0) times the number of phenothiazinyl groups in the molecule. Methods for the preparation of the compounds are described. The phenothiazinyl sulfides appear to be active in the same industrial and biological applications as phenothiazine and its corresponding derivatives, and show distinctive activity in various uses and as charge-transfer complexes of novel electrochemical properties as illustrated, in-vitro, in combination with iodine as a cathode material.

Growing community of inventors

Philadelphia, PA, United States of America

Edward A Nodiff