Pfizer Corporation

Anacor Pharmaceuticals, Inc.

Celgene Corporation

University of Cape Town

Mmv Medicines for Malaria Venture

Michael John Witty

Jacob J Plattner

Yong-Kang Zhang

Tsutomu Akama

Robert Toms Jacobs

Yang Liu

David Scott Carter

Paul R McGuirk

Jason S Halladay

Paul J Gilligan

David Waterson

Natalie Anne Hawryluk

Stacie S Canan

Kelly Chibale

Bernard Joseph Banks

Stephen Paul Gibson

Christopher J Dutton

Michael Snarey

Peter J Swift

Diego Gonzalez Cabrera

Yassir Younis

Tanya Paquet

Leslie Street

The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.

Oxaborole esters and uses thereof

Provided herein are Aminopurine compounds of Formula I: 

Animal and human anti-trypanosomonal and anti-leishmania agents

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.

Anti-malarial agents

The present invention is related to a use of aminopyrazine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyrazine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation. In one embodiment, the invention provides aminopyrazine derivatives having the following formula: 

The present invention is related to a use of aminopyridine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to aminopyridine derivatives useful for the preparation of a pharmaceutical foimulation for the inhibition of malaria parasite proliferation.

Antiparasitic avermectin derivatives of formula (I), where the broken line represents an optional bond, R.sup.1 and R.sup.4 are independently H, OH, halo, oximino, or an organic radical, R.sup.2, R.sup.6 and R.sup.7 are organic radicals and R.sup.3 is alpha-oleandrosyl or 4'-(alpha-oleandrosyl)-alpha-oleandrosyl optionally substituted at the 4'- or 4'-position, and R.sup.12 and R.sup.13 are independently H, CN, CONH.sub.2, C.sub.1 -C.sub.8 alkyl or aryl optionally substituted with at least one halo, OH, C.sub.1 -C.sub.8 alkylthio group.

Antiparastic auermectin derivatives

Antiparasitics comprising Avermectin derivatives of formula (I): ##STR1## wherein X represents a single or a double bond; R.sup.1 is H or OH; provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond, R.sup.1 is absent; R.sup.2 is an alkyl group substituted by one oxo or one or more hydroxy groups or by a single oxygen atom on two adjacent carbon atoms to form an oxirane ring, or R.sup.2 is an alkyl group substituted by an alkoxycarbonyl group, said substituents on R.sub.2 being attached to either or both a terminal carbon atom and a carbon atom adjacent to a terminal carbon atom of R.sup.2 ; and R.sup.3 is H or CH.sub.3 ; or, when R.sup.2 is oxo-substituted alkyl, an alkyl acetal or ketal derivative thereof.

Antiparasitic agents

6-Fluoro-7-pyridylquinolone carboxylic esters and acids having antibacterial activity are prepared by coupling of a 2-fluorophenyl-metallic compound with a pyridyl bromide or iodide in the presence of a transition metal catalyst, nitrating and hydrogenating the pyridyl-2-fluorophenyl compound formed, introducing a substituent on the nitrogen of the amine formed, and cyclizing after reacting with a dialkyl or dibenzyl ethoxymethylene malonate to form a 6-fluoro-7-pyridyl-1,4-dihydroquinol-4-one 3-carboxylate, and hydrolyzing to the corresponding acid.

Process for the preparation of 3-(2'-fluorophenyl)pyridine

1-Alkyl-6,8-difluoro-7-heterocyclic-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by conventional cyclization methods.

7-heterocyclic-1,4-dihydroquinolones

1-Substituted-6-fluoro-7-aryl-(8-fluoro)-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by reacting the corresponding alkyl 1-substituted-6-fluoro-7-bromo-(8-fluoro)-1,4-dihydroquinol-4-one-3-carbox ylate with an arylmetallic compound and hydrolyzing the ester formed.

Antibiotic derivatives of

L-pyroglutamyl-pyridylalanyl-L-prolinamides of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.8 alkoxyalkyl or aryl; and X is H, halo, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; and their physiologically acceptable salts and feed compositions thereof are useful for improving the efficiency of feed utilization and/or growth of animals especially poultry.

Growing community of inventors

Dover, United Kingdom

Michael John Witty