Jacobus Pharmaceutical Company, Inc.

Merck + Co., Inc.

Jacobus Pharmaceuticals Company, Inc.

David Penman Jacobus

Norman P Jensen

Hong-Ming Shieh

Howard Jones

Nathaniel Grier

Gavin David Heffernan

Eugene L Dulaney

Wenyi Zhao

Jacek Terpinski

Conrad P Dorn

Kurt William Saionz

Shu S Yang

Neil J Lewis

Craig Canfield

James Gillin

The present invention relates to antimalarial compounds and their use against protozoa of the genus, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.

Heteroaryl derivatives and uses thereof

The present invention relates to antimalarial compounds and their use against protozoa of the genusincluding drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.

Aryl derivatives and uses thereof

Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.

Biguanide and dihydrotriazine derivatives

Antimalarial N,N&prime;-substituted biguanides derived from hydroxylamines

1-[4-(4'-sulfanilyl)phenyl]urea and its various substituted derivatives can be used to decrease the infectiousness of and reduce the mortality associated with organisms of the genus Leishmania which are responsible for a group of conditions known as Leishmaniasis. This heretofore unrecognized use extends to the known derivatives of ureidodiaminodiphenyl sulfones and includes the novel aryl-ring hydroxylated series of sulfanilylphenylureas of the formula: ##STR1## wherein m and n can be the same or different and may each =0 or 1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are the same or different and are selected from the group consisting of hydrogen, hydroxyl, halo, C.sub.1 to C.sub.6 straight or branch chain alkyl, halo alkyl, polyhalo alkyl, alkoxy, cyano, amino, alkanoylamino, alkoxycarbonylamino, carboxy, alkoxycarbonyl, carbamoyl, acyl, R.sup.7, and R.sup.8 are the same or different and are selected from the group consisting of hydrogen, and C.sub.1 to C.sub.6 straight or branch chain alkyl Z is amino, acylamino, alkoxycarbonylamino, alkylamino, substituted amino or nitro; or its pharmaceutically acceptable salts.

1-[4-(4'-sulfanilyl)phenyl]urea and derivatives for the treatment of

There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.5, Y is oxygen or sulfur, m is 0 or 1, q is 0 or 1, wherein the prefix alk designates moieties which are straight chain or branched chain, and the term lower designates 1-6 carbon atoms and the unmodified term alk signifies 1-24 carbon atoms, the respective tautomers thereof, the pharmaceutically acceptable salts and addition salts thereof and the hydrates of said salts and addition salts. There are further provided methods of protecting subjects liable thereto from infections caused by an organism of the group Plasmodium sp., Mycobacterium sp. and Pneumocystis carinii by administering to a subject liable to such infection, a prophylactically effective amount of a compound of the foregoing formula. These compounds will also reduce the level of infection where said subjects have already been infected.

N,N'-substituted imidodicarbonimidic diamides derived from hydroxylamines

The invention relates to 1-[4-(4-sulfanilyl)phenyl] urea and derivatives thereof in pharmaceutical compositions and in methods of treating rheumatoid arthritis and immune complex diseases such as dermatitis herpetiformis.

1-[4-(4-Sulfanilyl)phenyl] urea and derivatives in compositions and

Combinations of thiopeptin and rumensin are shown to synergistically increase the feed efficiency of ruminant animals. The combination is orally administered to ruminant animals in the feed of the ruminanat or in an orally administered unit dosage form. The combination of thiopeptin and rumensin has a greater effect than the control animals given no medication, and greater than animals given either drug alone.

Combination of thiopeptin and rumensin to improve ruminant feed

Novel cholecalciferol and dihydrotachysterol.sub.3 derivatives produced against metabolic conversions at the 25-position, their preparation, pharmaceutical compositions, methods of treating steroid-induced osteoporosis, senile osteoporosis and secondary hyperparathyroidism, especially that induced by an insufficient amount of calcium in relationship to the amount of phosphate, novel intermediates and their preparation are disclosed.

Blocked cholecalciferol and dihydrotachysterol 3 derivatives

A composition comprising tris-(hydroxymethyl)aminomethane and dicyclohexyl-, dicyclohexenyl- and cyclohexylcyclohexenyl-alkyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.

Broad spectrum antibacterial compositions containing

A composition comprising tris-(hydroxymethyl)aminomethane and diphenyl and loweralkyl substituted diphenyl polyamines, their acid addition salts, and mixtures thereof are useful as antibacterial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.

Broad spectrum antibacterial compositions containing tris

A composition comprising tris-(hydroxymethyl)aminomethane and dibicyclo [3.1.1] and [2.2.1] heptyl and dibicyclo [3.1.1] and [2.2.1] heptenyl polyamines, their acid addition salts, and mixtures thereof are useful as antimicrobial agents. The composition is particularly useful because of the synergistic improvement obtained against strains of the genus Pseudomonas, as well as other genera.

Growing community of inventors

Princeton, NJ, United States of America

David Penman Jacobus