Malaria

MUKAADIAL ACETATE ISOLATED FROM WARBURGIA SALUTARIS AND THE USE THEREOF AS AN ANTIMALARIAL (Fri, 10 Aug 2018)
The invention relates to compounds and pharmaceutical compositions for use in treating malaria infections. The invention also relates to uses and methods of treating a malaria infection in a subject using the compounds and pharmaceutical compositions described. The invention further relates to methods of preparing the compounds described herein from plant material of Warburgia salutaris.
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USE OF CYMANQUINE COMPOUNDS AS ANTIMALARIAL AGENTS (Fri, 03 Aug 2018)
<p id="p-0001" num="0000">Organometallic compounds comprising a chloroquinoline moiety for use in the prophylaxis and treatment of malaria. The compounds can be manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety.</p>
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Fused Bicyclic Heteroaromatic Derivatives as Kinase Inhibitors (Fri, 20 Jul 2018)
<p id="p-0001" num="0000">A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.</p>
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NEW ANTI-MALARIAL AGENTS (Fri, 13 Jul 2018)
<p id="p-0001" num="0000">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.</p>
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NEW INDOLE COMPOUNDS HAVING ANTIPROTOZOAL ACTIVITY AND ITS USE AS WELL AS METHODS FOR PRODUCING THE SAME (Fri, 13 Jul 2018)
<p id="p-0001" num="0000">In a first aspect, the present invention relates to new compounds as depicted in formula (I). In particular, compounds according to the present invention are bisindolylcyclobuten-dione-based structures having antiprotozoal activity. In a further aspect, pharmaceutical compositions containing the same are provided as well as the use of the compounds and pharmaceutical compositions for the prophylaxis and treatment of parasite based diseases including malaria. Finally, methods for the treatment of parasite diseases including malaria are provided.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.09mm" wi="68.75mm" file="US20180194750A1-20180712-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Quinolone-based compounds, formulations, and uses thereof (Wed, 20 Jun 2018)
<p id="p-0001" num="0000">Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.</p>
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ANTI-MALARIAL AGENT (Fri, 20 Apr 2018)
<p id="p-0001" num="0000">The invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="237.91mm" wi="60.28mm" file="US20180104226A1-20180419-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS AND METHOD FOR BLOCKING TRANSMISSION OF MALARIAL PARASITE (Fri, 20 Apr 2018)
Disclosed are compounds of formula (I) and formula (II): (I) (II) wherein R1, R2, A, and B are as defined herein. Also disclosed is a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula (I) or (II) either alone or in combination with a second compound selected from elesclomol, NSC174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.
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NEW ANTI-MALARIAL AGENT (Fri, 20 Apr 2018)
The present invention is related to new trioxolane derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to trioxolane derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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NEW ANTI-MALARIAL AGENTS (Thu, 19 Apr 2018)
The present invention is related to new trioxolane derivatives of formula (I) in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to trioxolane derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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INACTIVATORS OF TOXOPLASMA GONDII ORNITHINE AMINOTRANSFERASE FOR TREATING TOXOPLASMOSIS AND MALARIA (Fri, 13 Apr 2018)
<p id="p-0001" num="0000">Disclosed are methods, compounds, and compositions for treating infection by an Apicomplexan parasite that include administering a compound that selectively inactivates ornithine aminotransferase of the Apicomplexan parasite. Specifically, the methods, compounds, compounds may be utilized for treating infection by <i>Toxoplasma gondii </i>and toxoplasmosis and for treating infection by <i>Plasmodium falciparum </i>and malaria. The compounds disclosed herein are observed to selectively inactivate <i>Toxoplasma gondii </i>ornithine aminotransferase (TgOAT) relative to human OAT and relative to human γ-aminobutyric aminotransferase (GABA-AT).</p>
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Boron-containing small molecules as antiprotozoal1 agents (Fri, 16 Mar 2018)
<p id="p-0001" num="0000">This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. Formula (I) and (II)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="61.38mm" wi="67.31mm" file="US10011616-20180703-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS (Fri, 09 Mar 2018)
<p id="p-0001" num="0000">The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.</p>
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BIOMARKERS FOR MALARIA DIAGNOSIS (Fri, 23 Feb 2018)
<p id="p-0001" num="0000">Disclosed herein are methods of detecting <i>Plasmodium </i>in a subject (for example, presence of <i>Plasmodium </i>parasite) by detecting the presence and/or amount of one or more metabolites in a sample from the subject. In some embodiments, the methods include detecting in the sample one or more metabolites listed in Table 1, Table 2, and/or Tables 5-8. The amount of the one or more metabolites in the sample is compared to the amount of the one or more metabolites in a control and presence of <i>Plasmodium </i>is determined if the amount of the one or more metabolites is different (for example statistically significantly increased or decreased) compared to the control.</p>
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PI 4-KINASE INHIBITOR AS A THERAPEUTIC FOR VIRAL HEPATITIS, CANCER, MALARIA. AUTOIMMUNE DISORDERS AND INFLAMMATION, AND A RADIOSENSITIZER AND IMMUNOSUPPRESSANT (Fri, 02 Feb 2018)
The present invention provides a plant-based flavonoid pharmaceutical composition and its synthetic for inhibition of phosphau'dylinositol-4-kinases and consequent prevention and treatment of RNA viruses including but not limited to viral hepatitis, as well as activity against cancer, malaria, autoimmune disorders and inflammation, prevent organ transplant rejection and as a radiation sensitizer. A method for isolating specific plant-based flavonoid pharmaceutical compositions from raw plant material as well as a method for synthesizing the compositions are also disclosed.
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PROTEASE TRANSITION STATE INHIBITOR PRODRUGS (Fri, 02 Feb 2018)
Disclosed herein are protease transition state inhibitor/analogue prodrug compounds selected from the group consisting of esters, carbamates, ester phosphates, and pharmaceutically acceptable salts thereof. Compositions containing such prodrugs are also disclosed, along with methods of using such compounds therapeutically or prophylactically against calicivirus, picornavirus, and/or coronavirus infection, as well as other conditions, such as malaria, cancer, stroke, heart attack, neural degeneration, cataracts, and glaucoma through inhibition of the variety of proteases associated with progression of such conditions.
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PLASMODIAL SURFACE ANION CHANNEL INHIBITORS FOR THE TREATMENT OR PREVENTION OF MALARIA (Fri, 19 Jan 2018)
<p id="p-0001" num="0000">The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I:</p> <p id="p-0002" num="0000"> <br/> <?in-line-formulae description="In-line Formulae" end="lead"?>Q—Y—R<sup>1</sup>—R<sup>2</sup>  (I),<?in-line-formulae description="In-line Formulae" end="tail"?> </p> <p id="p-0003" num="0000">wherein Q, Y, R<sup>1</sup>, and R<sup>2 </sup>are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.</p>
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Compounds, compositions and associated methods comprising 3-aryl quinolines (Fri, 12 Jan 2018)
<p id="p-0001" num="0000">Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.</p>
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THIOTRIAZOLE COMPOUND AND ITS USE IN PARASITIC PROTOZOAL INFECTIONS (Fri, 29 Dec 2017)
<p id="p-0001" num="0000">The present invention relates to a compound of Formula (I) or tautomers thereof having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by <i>Plasmodium falciparum. </i></p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="34.46mm" wi="69.26mm" file="US20170368034A1-20171228-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">(R)-2-((3-(3,5-dichloropyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)-1-(1H-indol-3-yl)propan-1-one</p>
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NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS (Sat, 09 Dec 2017)
The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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Animal and human anti-malarial agents (Fri, 08 Dec 2017)
<p id="p-0001" num="0000">Provided herein are Purine Comounds of Formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="20.24mm" wi="59.61mm" file="US10016436-20180710-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R<sup>1</sup>, R<sup>2</sup>, and R<sup>3 </sup>are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.</li> </ul> </li> </ul> </p>
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ANIMAL AND HUMAN ANTI-MALARIAL AGENTS (Fri, 08 Dec 2017)
Provided herein are Purine Comounds of Formula (I) or pharmaceutically acceptable salts, tautomers, isotopologues, or stereoisomers thereof, wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of a Purine Compound, and methods for treating or preventing malaria comprising the administration of an effective amount of a Purine Compound.
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Structure of plasmepsin V in complex with an inhibitor and uses thereof (Fri, 24 Nov 2017)
In one aspect, the present invention relates to the crystal structure of <i>Plasmodium vivax</i> plasmepsin V in complex with an inhibitor, and to methods of using the crystal structure and related structural information to identify, design and/or screen for inhibitors or redesign known inhibitors that interact with and/or modulate plasmepsin V activity. In another aspect, the present invention relates to a class of compounds based on the inhibitor useful in the treatment of malaria.
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COMPOUND FOR USE IN THE TREATMENT AND/OR PREVENTION OF PARASITIC MEDIATED DISEASES (Fri, 15 Sep 2017)
The present invention provides a compound belonging to furanocoumarin derivative having core structure (A) as given below, its pharmaceutically acceptable salt, isomer or a combination thereof for the treatment and/or prevention of a parasitic mediated disease. The present invention also provides a method for manufacturing and isolating said compound as well as method for treatment and prevention of parasitic mediated disease using said compound. In a preferred embodiment, the parasite is Plasmodium falciparum, the disease mediated by the said parasite is malaria and the furanocoumarin derivative having core structure (A) is Anisolactone.
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NITROGEN-CONTAINING ANALOGS OF SALINOMYCIN, SYNTHESIS AND USE AGAINST CANCER STEM CELLS AND MALARIA (Fri, 08 Sep 2017)
<p id="p-0001" num="0000">The present invention concerns compounds of formula (I), enantiomers, mixture of enantiomers, diastereoisomers and mixture of diasteroisomers thereof formula (I): wherein at least one of W, X and Y is selected from the group consisting of —NR<sub>1</sub>R<sub>2</sub>; —NR<sub>3</sub>—(CH<sub>2</sub>)<sub>n</sub>—NR<sub>4</sub>R<sub>5</sub>; —O—(CH<sub>2</sub>)<sub>n</sub>—NR<sub>4</sub>R<sub>5</sub>; —NR<sub>3</sub>—(CH<sub>2</sub>)<sub>n</sub>—N′R<sub>6</sub>R<sub>7</sub>R<sub>8</sub>; and —O—(CH<sub>2</sub>)<sub>n</sub>—N′R<sub>6</sub>R<sub>7</sub>R<sub>8 </sub>and Z is a functional group capable of chelating iron salts. The present invention also concerns the compounds of formula (I) for use as a drug, in particular, in the treatment of cancer and malaria.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.98mm" wi="74.68mm" file="US20170253610A1-20170907-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS FOR THE TREATMENT OF MALARIA (Fri, 25 Aug 2017)
The present invention provides methods of treating malaria by administration of a compound of Formula (I): or a pharmaceutically acceptable salt of said compound, to a subject in need thereof, wherein the variables X, R1, R3, R4, R5, A, B, L, m and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
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N3-SUBSTITUTED IMINOPYRIMIDINONES AS ANTIMALARIAL AGENTS (Fri, 25 Aug 2017)
The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R1, R2, R3, R4, R5, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.
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SILICON BASED CYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR TREATING MALARIA AND TOXOPLASMOSIS (Fri, 25 Aug 2017)
The present invention discloses novel silicon incorporated cyclic compounds of formula I, Wherein Ar1and Ar2 are individually selected from any aryl group which can be optionally substituted; X is selected from any inorganic anion such as halide, carbonate, sulfate, nitrate or any organic anion selected from acetate, tartarate, citrate, carbonate or organosulfonates such as tosylate, mesylate, triflate; R1 and R2 are individually selected from C1-C8 alkyl, cycloalkyl, aryl, heteroaryl, aralkyl, alkoxyalkyl, aminoalkyl, thioalkyl, haloalkyl or hydroxyalkyl. R1 and R2 together may form a ring which optionally may be substituted or may contain heteroatoms; a pharmaceutical composition comprising a therapeutically effective amount of compounds of general formula I, including geometrical isomers and/or salts thereof along with a drug and optionally along with a carrier or diluent or pharmaceutically acceptable excipient for treating malaria and toxoplasmosis.
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TETRAHYDROQUINOLINE SUBSTITUTED HYDROXAMIC ACIDS AS SELECTIVE HISTONE DEACETYLASE 6 INHIBITORS (Fri, 25 Aug 2017)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
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CONJUGATE FOR TREATING MALARIA (Fri, 18 Aug 2017)
<p id="p-0001" num="0000">A peptide-polymer conjugate is provided for use in treating malaria infections, and in particular terminal or drug resistant malaria infections. The conjugate is formed from a polymer to which a peptide having activity against a malaria parasite is co-valently attached. The peptide is a cyclic decapeptide from the closely-related group of tyrocidines, tryptocidines, phenycidines and gramicidin S, and the polymer is a hydrophilic and biocompatible polymer with a terminal thiol, such as poly(N-vinylpyrrolidone) (PVP). The polymer chains can be decorated with a hydrophilic targeting ligand that specifically targets an epitope on red blood cells, and in particular red blood cells infected with a plasmodial parasite. A method for synthesising the peptide-polymer conjugate is also provided.</p>
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ARTEMISININ DERIVATIVES, METHODS FOR THEIR PREPARATION AND THEIR USE AS ANTIMALARIAL AGENTS (Fri, 11 Aug 2017)
<p id="p-0001" num="0000">Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in pharmaceutical compositions intended for the treatment of parasitic infections are provided. Methods are provided for the production of artemisinin derivatives via functionalization of positions C7 and C6a, and optionally, in conjunction with modifications at positions C10 and C9, via chemoenzymatic methods. Recombinant cytochrome P450 polypeptides are also provided for use in the methods. The artemisinin derivatives can be used for the treatment of malaria and other parasitic infections, alone or in combination with other antiparasitic drugs.</p>
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MALARIA ANTIGEN SCREENING METHOD (Fri, 04 Aug 2017)
<p id="p-0001" num="0000">The invention provides a method of identifying an antigen from a pathogen or a disease antigen comprising the use of an adenoviral vector array comprising two or more different adenoviral vectors, wherein each adenoviral vector comprises a nucleic acid sequence encoding a different antigen of a pathogen. The adenoviral vectors are administered to antigen presenting cells (APCs) in vitro or to an animal in vivo. The immunogenicity of the antigen is measured by screening for an immune response from effector T lymphocytes in vitro and by screening for the absence of pathogen-induced disease onset in vivo.</p>
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COMPOUNDS AND METHODS FOR THEIR USE IN THE TREATMENT OF MALARIA (Fri, 28 Jul 2017)
Disclosed herein, in part, are compounds and methods for their use in the treatment of malaria. In at least one specific embodiment, the compounds or salts thereof can include compounds of Formula (I):
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ANTI-PARASITIC COMPOUNDS AND USES THEREOF (Fri, 21 Jul 2017)
The present disclosure provides compounds of Formula (I'), Formula (II), and Formula (III). The compounds described herein may useful in treating and/or preventing protozoan infections in a subject in need thereof, treating and/or preventing trypanosomal infections (e.g., Trypanosoma cruzi (T. cruzi) or Trypanosoma brucei infections) and/or plasmodial infections in a subject in need thereof, treating and/or preventing diseases in a subject in need thereof (e.g., Chagas disease, malaria, and/or sleeping sickness), and may be useful in treating and/or preventing infectious diseases in a subject in need thereof. Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.
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MODIFICATION OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 23 Jun 2017)
<p id="p-0001" num="0000">The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half-life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cell</p>
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NOVEL BISAMINOQUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS PREPARED THEREFROM AND THEIR USE (Fri, 16 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.</p>
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TRICYCLIC MOSQUITOCIDES AND METHODS OF MAKING AND USING THEREOF (Fri, 16 Jun 2017)
<p id="p-0001" num="0000">Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.</p>
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HEXAHYDROPYRAZINOTRIAZINONE DERIVATIVES AS KINASE INHIBITORS (Fri, 16 Jun 2017)
A series of 1,2,6,7,9,9a-hexahydropyrazino[1,2-d][1,2,4]triazin-4-one derivatives, substituted in the 8-position by an optionally substituted fused bicyclic heteroaromatic group, and in the 3-position by a range of functional groups,being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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BINDING INHIBITOR BETWEEN TCTP DIMER TYPE IGE-DEPENDENT HISTAMINE RELEASING FACTOR AND RECEPTOR THEREOF, AND USE THEREOF (Fri, 09 Jun 2017)
<p id="p-0001" num="0000">The present invention relates to a receptor-binding domain of an IgE-dependent histamine releasing factor (HRF), and a use thereof, and more specifically, ascertains, as an HRF structual region, and a FL domain and an H2 domain which bind to a receptor of HRF existing in a cell membrane, ascertains the C-terminus domain of the HRF, and ascertains that a material binding thereto inhibits IL-8 secretion, thereby determining that the FL and H2 domains and the C-terminus domain can be utilized in: the development of a therapeutic agent for treatment and prevention of HRF-related disease including allergic diseases such as asthma, bronchitis, chronic obstructive pulmonary disease, bronchiectasis, rhinitis, atopic dermatitis, hives (urticaria), hay fever, conjunctivitis, and anaphylaxis; inflammatory diseases such as bronchitis, pneumonia, arthritis, nephritis, psoriasis, dermatitis, Crohn's disease, enteritis, gingivitis, arteriosclerosis, coronary arteritis, hepatitis, Behcet's disease, bladder cancer, prostatitis, pyelonephritis, glomerulonephritis, osteomyelitis, thyroiditis, uveitis, abdominal cavity inflammation, meningitis, pulmonary fibrosis and rheumatoid arthritis; and malaria, and a method for screening for the HRF-related diseases.</p>
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Azepanyl-derivatives and pharmaceutical compositions comprising the same with antiparasitic activity (Fri, 19 May 2017)
<p id="p-0001" num="0000">The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i), for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="49.02mm" wi="61.04mm" file="US09994577-20180612-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Fused bicyclic heteroaromatic derivatives as kinase inhibitors (Fri, 12 May 2017)
<p id="p-0001" num="0000">A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.</p>
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PPAR MODULATORS (Fri, 05 May 2017)
<p id="p-0001" num="0000">The present application relates to amorfrutin analogs and uses as PPAR modulators for the treatment of metabolic syndrome, obesity, hyperlipidemia, elevated fasting blood glucose, elevated blood pressure, low HDL cholesterol, type 2 diabetes, cardiovascular disease, a neurodegenerative disease, malaria or irritable bowel syndrome.</p>
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Fused bicyclic heteroaromatic derivatives as kinase inhibitors (Fri, 05 May 2017)
<p id="p-0001" num="0000">A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.40mm" wi="52.32mm" file="US10000497-20180619-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HDAC inhibitors and therapeutic methods using the same (Fri, 05 May 2017)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
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PYRAZINE COMPOUNDS FOR USE IN THE TREATMENT OF PARASITIC PROTOZOAL INFECTIONS (Fri, 28 Apr 2017)
The present invention relates to compounds of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasiticprotozoalinfections such as malaria, in particular infection by Plasmodium falciparum. Formula (I), wherein R is methyl or fluoro.
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SUBSTITUTED AMINOALKYLAZOLES AS MALARIAL ASPARTIC PROTEASE INHIBITORS (Fri, 28 Apr 2017)
The present invention relates to novel aminoalkylazoles acting as inhibitors of malarial protease plasmepsin II. These can be used as medicines or as constituent of medicines for the treatment of malaria infection.
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SUBSTITUTED AMINOALKYLAZOLES AS MALARIAL ASPARTIC PROTEASE INHIBITORS (Fri, 28 Apr 2017)
The present invention relates to novel aminoalkylazoles acting as inhibitors of malarial protease plasmepsin II. These can be used as medicines or as constituent of medicines for the treatment of malaria infection.</p>
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BINDING INHIBITOR BETWEEN TCTP DIMER TYPE IGE-DEPENDENT HISTAMINE RELEASING FACTOR AND RECEPTOR THEREOF, AND USE THEREOF (Thu, 20 Apr 2017)
The present invention relates to a receptor-binding domain of an IgE-dependent histamine releasing factor (HRF), and a use thereof and, more specifically, ascertains, as an HRF framework region, an FL domain and an H2 domain which bind to a receptor of an HRF existing in a cell membrane, ascertains the C-terminus of the HRF, and ascertains that a material binding thereto inhibits IL-8 secretion, thereby determining that the FL and H2 domains and the C-terminus can be utilized in: the development of a therapeutic agent for and prevention of HRF-related diseases including malaria and inflammatory diseases such as asthma, bronchitis, chronic obstructive pulmonary disease, bronchiectasis, rhinitis, atopic dermatitis, hives, hay fever, conjunctivitis, anaphylactic allergic diseases, pneumonia, arthritis, nephritis, psoriasis, dermatitis, Crohn's disease, enteritis, gingivitis, arteriosclerosis, coronary arteritis, hepatitis, Behcet's disease, bladder cancer, prostatitis, pyelonephritis, glomerulonephritis, osteomyelitis, thyroiditis, uveitis, abdominal cavity inflammation, meningitis, pulmonary fibrosis and rheumatoid arthritis; and a method for screening for the HRF-related diseases.
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BICYCLIC AND TRICYCLIC CAP BEARING MERCAPTOACETAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS (Fri, 31 Mar 2017)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
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Fused bicyclic heteroaromatic derivatives as kinase inhibitors (Thu, 16 Mar 2017)
A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III beta (PI4KIII beta) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 10 Mar 2017)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed
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Triaminopyrimidine compounds useful for preventing or treating malaria (Fri, 24 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to triaminopyrimidines and to pharmaceutically acceptable salts thereof, to their use in the treatment and/or prevention of malaria caused by <i>plasmodium </i>species, and to their methods of preparation.</p>
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METHODS OF DETECTING PLASMODIUM INFECTION (Fri, 17 Feb 2017)
<p id="p-0001" num="0000">The present invention relates to a method of identifying a subject with a <i>Plasmodium </i>infection. The present invention also relates to a method for monitoring a subject with a <i>Plasmodium </i>infection, for example, following treatment with an anti-malaria compound. Also provided are methods of identifying a compound to treat a <i>Plasmodium </i>infection.</p>
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Azepanyl-derivatives and pharmaceutical compositions comprising the same with antiparasitic activity (Fri, 17 Feb 2017)
The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i), for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases.
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QUINOLONE-3-DIARYLETHERS (Fri, 27 Jan 2017)
<p id="p-0001" num="0000">Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.</p>
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QUINOLONE-3-DIARYLETHERS (Fri, 27 Jan 2017)
Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.
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USE OF CYMANQUINE COMPOUNDS AS ANTIMALARIAL AGENTS (Fri, 27 Jan 2017)
Organometallic compounds comprising a chloroquinoline moiety for use in the prophylaxis and treatment of malaria. The compounds can be manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety.
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NEW ANTI-MALARIAL AGENTS (Fri, 20 Jan 2017)
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.
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NEW INDOLE COMPOUNDS HAVING ANTIPROTOZOAL ACTIVITY AND ITS USE AS WELL AS METHODS FOR PRODUCING THE SAME (Fri, 20 Jan 2017)
In a first aspect, the present invention relates to new compounds as depicted in formula (I). In particular, compounds according to the present invention are bisindolylcyclobuten-dione-based structures having antiprotozoal activity. In a further aspect, pharmaceutical compositions containing the same are provided as well as the use of the compounds and pharmaceutical compositions for the prophylaxis and treatment of parasite based diseases including malaria. Finally, methods for the treatment of parasite diseases including malaria are provided.
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ANTI-MALARIAL AGENTS (Thu, 19 Jan 2017)
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.
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Autophagy Inhibitors (Fri, 06 Jan 2017)
<p id="p-0001" num="0000">The present invention relates to compounds of Formula III, Formula 111(a), Formula V, Formula V(a), Formula A, Formula A 1, Formula A2, Formula A 3, or a pharmaceutically acceptable salt thereof that are useful as pharmaceutical agents, individually and/or in a combination with a chemotherapeutic agent: PLX-4032 (vemurafenib), or the catalytic mTOR inhibitor AZD8055, to treat a cancer and/or a cancer metastasis, for example a cancer harboring a BRAF protein kinase mutation and/or a HRAS protein mutation. Also, a method of treating and/or preventing malaria in a subject, the method comprising administering a therapeutically effective amount of a compound of Formula A, Formula A 1, Formula A2, Formula A 3, or a pharmaceutically acceptable salt thereof to the subject in need.</p>
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COMPOUNDS AND THEIR USE AS INHIBITORS OF N-MYRISTOYL TRANSFERASE (Fri, 06 Jan 2017)
This invention provides compounds of formula (I) and salts thereof, which have activity as inhibitors of N-myristoyl transferase (NMT). The invention also relates to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of N-myristoyl transferase provides a therapeutic or prophylactic effect, including protozoan infections (such as malaria and leishmaniasis), viral infections (such as human rhinovirus and HIV), and hyperproliferative disorders (such as B-cell lymphoma).
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TREATMENT OF INFECTIOUS DISEASES WITH GLUCOSE UPTAKE INHIBITORS (Fri, 30 Dec 2016)
Provided are methods of treating infectious diseases in mammals comprising administering a compound that inhibits glucose uptake. Particular infectious diseases that may be treated include malaria, leishmaniasis, African trypanosomiasis, tuberculosis, HIV, HCMV or herpes virus. In a first aspect, the invention features a method of treating infectious diseases in a mammal, comprising administering to a mammalian subject in need thereof a therapeutically effective amount of a compound or prodrug thereof, or pharmaceutically acceptable salt or ester of said compound or prodrug, wherein the compound is an inhibitor of glucose uptake.
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Triaminopyrimidine compounds useful for preventing or treating malaria (Thu, 22 Dec 2016)
The present invention relates to triaminopyrimidines and to pharmaceutically acceptable salts thereof, to their use in the treatment and or prevention of malaria caused by plasmodium species, and to their methods of preparation.
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STRUCTURE OF PLASMEPSIN V IN COMPLEX WITH AN INHIBITOR AND USES THEREOF (Fri, 16 Dec 2016)
In one aspect, the present invention relates to the crystal structure of Plasmodium vivax plasmepsin V in complex with an inhibitor, and to methods of using the crystal structure and related structural information to identify, design and/or screen for inhibitors or redesign known inhibitors that interact with and/or modulate plasmepsin V activity. In another aspect, the present invention relates to a class of compounds based on the inhibitor useful in the treatment of malaria.
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Compounds and compositions for the treatment of parasitic diseases (Fri, 18 Nov 2016)
<p id="p-0001" num="0000">The present invention provides compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.21mm" wi="68.16mm" file="US09926314-20180327-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a <i>Plasmodium </i>parasite, such as malaria. </p>
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ANTI-MALARIAL AGENT (Thu, 17 Nov 2016)
The objective of the present invention is to prevent and/or treat malaria with an anti-malarial agent comprising, as an active ingredient, a metal chelator such as Tris(2-pyridylmethyl)amine represented by formula (I), (III), (IV), (V), (VI), or (VII). (I) (III) (IV) (V) (VI) (VII)
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Anti-malarial agent (Fri, 11 Nov 2016)
<p id="p-0001" num="0000">The present invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="191.35mm" wi="60.28mm" file="US09861626-20180109-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compound (S) and (R)-N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide and use (Fri, 28 Oct 2016)
<p id="p-0001" num="0000">The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by <i>Plasmodium falciparum</i>.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.57mm" wi="67.06mm" file="US09624219-20170418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> (S)—N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide. </p>
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2,4-DIOXO-1,2-DIHYDROPYRIDO[3,4-D]PYRIMIDINE DERIVATIVES (Fri, 28 Oct 2016)
The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (S)-N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.
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URACIL DERIVATIVES FOR THE TREATMENT OF MALARIA (Fri, 28 Oct 2016)
The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. R1 is morpholinyl or pyridyl; R2 is fluoro or hydrogen when R1 is morpholinyl; and R2 is hydrogen when R1 is pyridyl or a pharmaceutically acceptable salt thereof.
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PLASMODIAL SURFACE ANION CHANNEL INHIBITORS FOR THE TREATMENT OR PREVENTION OF MALARIA (Fri, 21 Oct 2016)
The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (1): Q-Y-R1-R2 (1), wherein Q, Y, RI, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (1) in combination with any one or more compounds represented by formulas 11, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
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Desferrithiocin analogs and uses thereof (Fri, 07 Oct 2016)
<p id="p-0001" num="0000">Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).</p>
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COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 07 Oct 2016)
<p id="p-0001" num="0000">Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of malaria.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="36.32mm" wi="58.00mm" file="US20160289235A1-20161006-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Application of piperaquine nitrogen oxide in preparation of medicines for resisting malaria (Thu, 06 Oct 2016)
The invention discloses application of piperaquine mono-nitrogen oxide and/or piperaquine dinitrogen oxide or pharmaceutically acceptable salt in preparation of medicines for resisting malaria. According to the unexpected discovery, piperaquine mono-nitrogen oxide and piperaquine dinitrogen oxide have a remarkable inhibition effect on growth of plasmodium and development of agamont. In-vitro tests prove that the piperaquine mono-nitrogen oxide and piperaquine dinitrogen oxide show the activity of inhibiting development of plasmodium agamont at a relatively low concentration (7.8nM); and in-vivo tests prove that oral piperaquine mono-nitrogen oxide and piperaquine dinitrogen oxide have a remarkable effect on inhibiting plasmodium falciparum.
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NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS (Fri, 30 Sep 2016)
The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS (Fri, 30 Sep 2016)
The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.</p>
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NEW SUBSTITUTED TRIAZOLOPYRIMIDINES AS ANTI-MALARIAL AGENTS (Thu, 29 Sep 2016)
The present invention is related to a use of triazolopyrimidine derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to triazolopyrimidine derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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BIOMARKERS FOR MALARIA DIAGNOSIS (Fri, 23 Sep 2016)
Disclosed herein are methods of detecting Plasmodium in a subject (for example, presence of Plasmodium parasite) by detecting the presence and/or amount of one or more metabolites in a sample from the subject. In some embodiments, the methods include detecting in the sample one or more metabolites listed in Table 1, Table 2, and/or Tables 5-8. The amount of the one or more metabolites in the sample is compared to the amount of the one or more metabolites in a control and presence of Plasmodium is determined if the amount of the one or more metabolites is different (for example statistically significantly increased or decreased) compared to the control.
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METHOD OF BLOCKING TRANSMISSION OF MALARIAL PARASITE (Fri, 16 Sep 2016)
<p id="p-0001" num="0000">The invention provides a method of blocking transmission of a <i>Plasmodium </i>parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula I: wherein A, B, R<sup>1</sup>, R<sup>2</sup>, R<sup>10</sup>, and R<sup>11 </sup>are described herein, either alone or in combination with a second compound selected from elesclomol, NSC 174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1 152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="32.60mm" wi="55.20mm" file="US20160264570A1-20160915-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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MALARIA VACCINATION (Fri, 02 Sep 2016)
<p id="p-0001" num="0000">The invention relates to an antigenic composition or vaccine comprising a viral vector, the viral vector comprising nucleic acid encoding <i>Plasmodium </i>protein PfLSA1, or a part or variant of <i>Plasmodium </i>protein PfLSA1; PfLSAP2, or a part or variant of <i>Plasmodium </i>protein PfLSAP2; PfUIS3, or a part or variant of <i>Plasmodium </i>protein PfUIS3; PfI0580c, or a part or variant of <i>Plasmodium </i>protein PfI0580c; and PfSPECT-1, or a part or variant of <i>Plasmodium </i>protein PfSPECT-1.</p>
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CHLOROQUINOLINE TRIAZOLE COMPOUNDS, COMPOSITION AND USES (Fri, 15 Jul 2016)
Chloroquinoline triazole compounds are provided, as are compositions comprising the compounds, and methods relating to them, including methods of inhibiting autophagy in biological systems and treatment of diseases, disorders or conditions in which autophagy inhibition can provide benefit, including treatment of cancer, rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease.
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Plasmodial surface anion channel inhibitors for the treatment or prevention of malaria (Fri, 08 Jul 2016)
<p id="p-0001" num="0000">The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: <br/> <?in-line-formulae description="In-line Formulae" end="lead"?>Q-Y—R<sup>1</sup>—R<sup>2</sup>  (I),<?in-line-formulae description="In-line Formulae" end="tail"?> <br/> wherein Q, Y, R<sup>1</sup>, and R<sup>2 </sup>are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions. </p>
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Therapeutically active pyrazolo-pyrimidine derivatives (Fri, 08 Jul 2016)
<p id="p-0001" num="0000">A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4-position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.</p>
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Anti-malarial agents (Fri, 08 Jul 2016)
<p id="p-0001" num="0000">The present invention is related to a use of pyrazole derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to pyrazole derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.</p>
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THIOTRIAZOLE COMPOUND AND ITS USE IN PARASITIC PROTOZOAL INFECTIONS (Fri, 01 Jul 2016)
The present invention relates to a compound of Formula (I) or tautomers thereof having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by Plasmodium falciparum. (R)-2-((3-(3,5-dichloropyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)-1-(1H-indol-3-yl)propan-1-one
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Thiotriazole compound and its use in parasitic protozoal infections (Fri, 01 Jul 2016)
The present invention relates to a compound of Formula (I) or tautomers thereof having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by <i>Plasmodium falciparum</i>. (<i>R</i>)-2-((3-(3,5-dichloropyridin-4-yl)-1H-1,2,4-triazol-5-yl)thio)-1-(1H-indol-3-yl)propan-1-one
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NOVEL BISAMINOQUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS PREPARED THEREFROM AND THEIR USE (Fri, 17 Jun 2016)
<p id="p-0001" num="0000">The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.</p>
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Oxone-Aceton Mediated Metal Free Preparation of Syn-Diols (Fri, 17 Jun 2016)
<p id="p-0001" num="0000">The present invention disclose a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of benzo fused olefins of formula (II) to obtain library of dioxolo compounds of formula (I). The invention further disclose a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of stilbene and its derivatives of formula (III) thereof. Also disclosed herein is Wacker-type oxidation of benzo-fused olefins of formula (X). The invention further disclose compounds of formula (I) which can be useful for the treatment of HIV, cancer or malaria.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.62mm" wi="54.86mm" file="US20160168114A1-20160616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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MONOCARBOXYLATE TRANSPORT MODULATORS AND USES THEREOF (Fri, 27 May 2016)
The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
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NEW ANTI-MALARIAL AGENTS (Thu, 26 May 2016)
The present invention is related to a use of pyrazole derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to pyrazole derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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Compounds and compositions for the treatment of parasitic disease (Fri, 22 Apr 2016)
<p id="p-0001" num="0000">The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.</p>
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NITROGEN-CONTAINING ANALOGS OF SALINOMYCIN, SYNTHESIS AND USE AGAINST CANCER STEM CELLS AND MALARIA (Fri, 18 Mar 2016)
The present invention concerns compounds of formula (I), enantiomers, mixture of enantiomers, diastereoisomers and mixture of diasteroisomers thereof formual (I): wherein at least one of W, X and Y is selected from the group consisting of -NR1R2; - NR3-(CH2)n-NR4R5; -O-(CH2)n-NR4R5; -NR3-(CH2)n-N+R6R7R8; and -O-(CH2)n-N+R6R7R8 and Z is a functional group capable of chelating iron salts. The present invention also concerns the compounds of formula (I) for use as a drug, in particular, in the treatment of cancer and malaria.
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NITROGEN-CONTAINING ANALOGS OF SALINOMYCIN, SYNTHESIS AND USE AGAINST CANCER STEM CELLS AND MALARIA (Fri, 18 Mar 2016)
The present invention concerns compounds of formula (I), enantiomers, mixture of enantiomers, diastereoisomers and mixture of diasteroisomers thereof formual (I): wherein at least one of W, X and Y is selected from the group consisting of -NR1R2; - NR3-(CH2)n-NR4R5; -O-(CH2)n-NR4R5; -NR3-(CH2)n-N+R6R7R8; and -O-(CH2)n-N+R6R7R8 and Z is a functional group capable of chelating iron salts. The present invention also concerns the compounds of formula (I) for use as a drug, in particular, in the treatment of cancer and malaria.</p>
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MACROLIDE COMPOUNDS AND THEIR USE IN LIVER STAGE MALARIA AND RELATED DISEASE (Fri, 04 Mar 2016)
A novel quantum-based computational process for drug discovery and design was used to identify potential novel liver-stage anti-malarial therapeutic molecules. The approach combined the latest big-data advances in high-throughput bioassay development with fundamental scientific knowledge to generate new pharmaceutical leads. Several molecules with no previous association with anti-parasitical activity were identified. These molecules and there use in prevention and/or treatment of Plasmodium infections are provided.
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CONJUGATE FOR TREATING MALARIA (Fri, 19 Feb 2016)
A peptide-polymer conjugate is provided for use in treating malaria infections, and in particular terminal or drug resistant malaria infections. The conjugate is formed from a polymer to which a peptide having activity against a malaria parasite is covalently attached. The peptide is a cyclic decapeptide from the closely-related group of tyrocidines, tryptocidines, phenycidines and gramicidin S, and the polymer is a hydrophilic and biocompatible polymer with a terminal thiol, such as poly(N-vinylpyrrolidone) (PVP). The polymer chains can be decorated with a hydrophilic targeting ligand that specifically targets an epitope on red blood cells, and in particular red blood cells infected with a plasmodial parasite. A method for synthesising the peptide-polymer conjugate is also provided.
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Antiprotozoal compounds (Fri, 12 Feb 2016)
<p id="p-0001" num="0000">The invention is directed to a compound of formula I, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of formula I, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria.</p>
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Substituted piperidines with antiparasitic activity (Fri, 05 Feb 2016)
<p id="p-0001" num="0000">The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="18.71mm" wi="42.93mm" file="US09688633-20170627-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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HDAC6 INHIBITORS AND USES THEREOF (Thu, 28 Jan 2016)
The present invention relates to Histone deacetylases 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, a viral disease, malaria, or a combination thereof, also are disclosed.
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HDAC6 inhibitors and uses thereof (Fri, 15 Jan 2016)
<p id="p-0001" num="0000">Histone deacetylases 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, a viral disease, malaria, or a combination thereof.</p>
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TRICYCLIC MOSQUITOCIDES AND METHODS OF MAKING AND USING THEREOF (Fri, 15 Jan 2016)
Compounds that inhibit digestion in blood-ingesting pests are described herein. In one embodiment, the compounds described herein block entry of blood into the midgut and thereby inhibit digestion and nutrient processing. In another embodiment, the compounds described herein prevent pathogens contained in the blood meal from entering the midgut where they could cross the epithelial cell layer and infect the mosquito. The compounds can be administered to a population of blood-ingesting pests, such as mosquitos, directly or indirectly in an effective amount to prevent mosquitoes from transmitting diseases such as malaria, dengue fever, West Nile virus and lymphatic filariasis. Preferably, the compounds are lethal to blood-ingesting pests. The compounds can be combined with one or more excipients to prepare compositions.
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AZEPANYL-DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME WITH ANTIPARASITIC ACTIVITY (Fri, 08 Jan 2016)
The present invention provides compounds of Formula (i). Furthermore, pharmaceutical compositions are provided comprising at least one compound of Formula (i), for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases.
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Piperidinylcarbazoles (Fri, 25 Dec 2015)
<p id="p-0001" num="0000">The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R<sup>3</sup>, R<sup>4</sup>, X and Y have the meaning given in claim <b>1</b>.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="22.44mm" wi="57.32mm" file="US09908863-20180306-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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FUSED BICYCLIC HETEROAROMATIC DERIVATIVES AS KINASE INHIBITORS (Thu, 24 Dec 2015)
A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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FUSED BICYCLIC HETEROAROMATIC DERIVATIVES AS KINASE INHIBITORS (Thu, 24 Dec 2015)
A series of fused bicyclic heteroaromatic derivatives of formula (I), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.
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Two-carbon linked artemisinin-derived trioxane dimers (Fri, 18 Dec 2015)
<p id="p-0001" num="0000">Two-carbon linked artemisinin-derived trioxane dimers and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.</p>
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Compounds and compositions for the treatment of parasitic diseases (Fri, 04 Dec 2015)
<p id="p-0001" num="0000">The present invention provides compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.28mm" wi="67.31mm" file="US09556169-20170131-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a <i>Plasmodium </i>parasite, such as malaria. </p>
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Use of inhibitors of the activity or function of PI3K (Fri, 04 Dec 2015)
<p id="p-0001" num="0000">The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.</p>
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PPAR MODULATORS (Fri, 27 Nov 2015)
The present application relates to amorfrutin analogs and uses as PPAR modulators for the treatment of metabolic syndrome, obesity, hyperlipidemia, elevated fasting blood glucose, elevated blood pressure, low HDL cholesterol, type 2 diabetes, cardiovascular disease, a neurodegenerative disease, malaria or irritable bowel syndrome.
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Ruthenium carbon monoxide releasing molecules and uses thereof (Fri, 13 Nov 2015)
<p id="p-0001" num="0000">The present invention provides novel ruthenium compounds of Formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.63mm" wi="59.27mm" file="US09611286-20170404-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or salts, isomers, hydrates, or solvates thereof, or combinations thereof; wherein E, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, X<sub>1</sub>, and X<sub>2 </sub>are as defined herein, and pharmaceutical compositions thereof. Also provided are methods of use and treatment. Such compounds have been found useful in the treatment of malaria infection. Such compounds may also be useful in the treatment of inflammatory conditions, such as acute lung injury and acute resipiratory distress syndrome, which optionally may be associated with a malaria infection. </p>
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TRIAMINOPYRIMIDINE COMPOUNDS USEFUL FOR PREVENTING OR TREATING MALARIA (Fri, 06 Nov 2015)
The present invention relates to triaminopyrimidines and to pharmaceutically acceptable salts thereof, to their use in the treatment and or prevention of malaria caused by plasmodium species, and to their methods of preparation.
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Treatment and inhibition of protozoal diseases with nandrolone and its derivatives (Wed, 04 Nov 2015)
<p id="p-0001" num="0000">This invention provides new therapeutic potential of nandrolone or a derivative thereof, against protozoal diseases. More specifically, nandrolone or a derivative thereof exhibits anti-protozoal activity against <i>Leishmania major</i>. Anti-protozoal potential of nandrolone derivatives, such as compounds 1-8, can contribute in the development of effective therapies against protozoal diseases, such as leishmaniasis, trypanosomiasis, malaria, toxoplasmosis, babeosis, amoebic dysentery and lambliasis. Another aspect of the invention is a method of testing derivatives of nandrolone for anti-protozoal activity comprising growing <i>Leishmania </i>in the presence of the test derivative and determining the IC<sub>50 </sub>value.</p>
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Saponins and chromans derivatives mixture compositions against leishmaniasis, Trypanosomiasis americana, malaria, Trypanosomiasis africana and <i>Fasciola hepatica</i> (Wed, 28 Oct 2015)
<p id="p-0001" num="0000">SAPONINS AND CHROMANS DERIVATIVES MIXTURE COMPOSITIONS AGAINST LEISHMANIASIS, TRYPANOSOMIASIS AMERICANA, MALARIA, TRYPANOSOMIASIS AFRICANA AND <i>FASCIOLA HEPATICA</i>, is a composition of saponins and chromans derivatives. The saponins are triterpene types and chromans are hydrazones derivatives. This composition is a therapeutic agent against tropical diseases.</p>
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Antiprotozoal amidine compounds (Wed, 28 Oct 2015)
<p id="p-0001" num="0000">The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, malaria and Leishmaniasis, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.</p>
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Artemisinin derivatives, methods for their preparation and their use as antimalarial agents (Fri, 23 Oct 2015)
<p id="p-0001" num="0000">Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in pharmaceutical compositions intended for the treatment of parasitic infections are provided. Methods are provided for the production of artemisinin derivatives via functionalization of positions C7 and C6a, and optionally, in conjunction with modifications at positions C10 and C9, via chemoenzymatic methods. Recombinant cytochrome P450 polypeptides are also provided for use in the methods. The artemisinin derivatives can be used for the treatment of malaria and other parasitic infections, alone or in combination with other antiparasitic drugs.</p>
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Compounds for use in the treatment of parasitic diseases (Fri, 23 Oct 2015)
<p id="p-0001" num="0000">The present invention relates to compounds useful for treating parasitic diseases, which are infectious diseases caused or transmitted by a parasite. Compounds of the invention are particularly active against the causative pathogens in malaria. Such compounds are selective inhibitors of parasitic histone deacetylase (PfHDAC) and suppress the growth of parasites, such as <i>Plasmodium falciparum</i>, at a lower concentration than the concentration required for the inhibition of the growth of mammalian cells.</p>
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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 16 Oct 2015)
<p id="p-0001" num="0000">The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a <i>Plasmodium </i>parasite.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.72mm" wi="66.29mm" file="US20150291598A1-20151015-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Thu, 08 Oct 2015)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
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Biphenyl compounds for use in treating malaria and other parasitic disorders (Fri, 02 Oct 2015)
<p id="p-0001" num="0000">The present invention relates to a compound of formula (I)</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.43mm" wi="72.56mm" file="US09499471-20161122-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">as defined herein.</li> </ul> </li> </ul> </p>
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COMPOUNDS FOR USE IN THE TREATMENT OF PARASITIC DISEASES (Thu, 10 Sep 2015)
The present invention relates to compounds useful for treating parasitic diseases, which are infectious diseases caused or transmitted by a parasite. Compounds of the invention are particularly active against the causative pathogens in malaria. Such compounds are selective inhibitors of parasitic histone deacetylase (PfHDAC) and suppress the growth of parasites, such as <i>Plasmodium falciparum</i>, at a lower concentration than the concentration required for the inhibition of the growth of mammalian cells.
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Piperidinylcarbazole as antimalarial (Fri, 21 Aug 2015)
The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R<sp>3</sp>, R<sp>4</sp>, X and Y have the meaning given in claim 1.
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Cycloalkyl-diamines (Fri, 31 Jul 2015)
<p id="p-0001" num="0000">The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal, especially a human, in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting Human African Trypanosomiasis (HAT), Chagas Disease, Malaria, Leishmaniasis, and other infectious diseases transmitted to humans and animals by exposure to parasites, the method comprising administering to a human or mammal in need of such treatment a compound of formula I as described above.</p>
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NOVEL COMPOUNDS HAVING A TETRACYCLIC IRIDOID SKELETON AND AN ANTI-TRYPANOSOMAL, ANTI-LEISHMANIAL AND ANTI-PLASMODIAL AGENTS COMPRISING THE SAME AS AN ACTIVE INGREDIENT (Fri, 17 Jul 2015)
The present invention provides anti-trypanosomal, anti-leishmanial or anti-plastmodial agent for treating, preventing trypanosomiasis, leishmaniasis or malaria, respectively, of mammals, which comprises a compound having the tetracyclic iridoid skeleton represented by a general formula (I).
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Therapeutically active pyrazolo-pyrimidine derivatives (Fri, 10 Jul 2015)
A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4- position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseasesand malaria; and organ and cell transplant rejection.
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Compounds and application thereof in preparation of anti-parasitosis drugs (Thu, 09 Jul 2015)
The invention discloses compounds and an application thereof in preparation of anti-parasitosis drugs. The compounds have a structural formula represented by the formula I or the formula II. The compounds provided by the invention have rich functional group diversity and modificability, and the products are relatively easy to separate and purify. The compounds provided by the invention have quite good inhibitory effect on pernicious malaria NDH protein activity and are new anti-malarial action targets and mechanisms, and thus the compounds also have quite good inhibitory effect on many plasmodium species and strains generating resistance to traditional drugs, thereby providing a new breakthrough for current increasingly-serious plasmodium drug resistance aspect. At the same time, the plasmodium NDH and human NADH oxidordeuctase belong to different species, so that the compounds can be expected to produce fewer side effects on human. In summary, the compounds have broad development and application prospects.
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Method for producing a plant extract and fraction, pharmaceutical compositions and use thereof (Thu, 25 Jun 2015)
The present invention describes the method for producing the dichloromethane fraction and subfractions of Eleutherine plicata, commonly known as "marupazinho, marupari, palmeirinha, coquinho, marupai, marupau, marupa-piranga, lirio-folha-de-palmeira". The invention further includes the preparation of pharmaceutical compositions that contain the dichloromethane fraction and/or naphthoquinone, as well as the use thereof for the treatment of malaria. The extract and fractions described were tested and showed antiplasmodium activity, in particular against chloroquine-resistant Plasmodium falciparum (W2).
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AUTOPHAGY INHIBITORS (Fri, 12 Jun 2015)
The present invention relates to compounds of Formula III, Formula 111(a), Formula V, Formula V(a), Formula A, Formula A 1, Formula A2, Formula A 3, or a pharmaceutically acceptable salt thereof that are useful as pharmaceutical agents, individually and/or in a combination with a chemotherapeutic agent: PLX-4032 (vemurafenib), or the catalytic mTOR inhibitor AZD8055, to treat a cancer and/or a cancer metastasis, for example a cancer harboring a BRAF protein kinase mutation and/or a HRAS protein mutation. Also, a method of treating and/or preventing malaria in a subject, the method comprising administering a therapeutically effective amount of a compound of Formula A, Formula A 1, Formula A2, Formula A 3, or a pharmaceutically acceptable salt thereof to the subject in need.
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DESFERRITHIOCIN ANALOGS AND USES THEREOF (Fri, 29 May 2015)
Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).
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METHOD OF BLOCKING TRANSMISSION OF MALARIAL PARASITE (Fri, 22 May 2015)
The invention provides a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing malaria comprising administering to an animal an effective amount of a first compound of formula I: wherein A, B, R1, R2, R10, and R11 are described herein, either alone or in combination with a second compound selected from elesclomol, NSC 174938, NVP-AUY922, Maduramicin, Narasin, Alvespimycin, Omacetaxine, Thiram, Zinc pyrithione, Phanquinone, Bortezomib, Salinomycin sodium, Monensin sodium, Dipyrithione, Dicyclopentamethylene-thiuram disulfide, YM155, Withaferin A, Adriamycin, Romidepsin, AZD-1 152-HQPA, CAY10581, Plicamycin, CUDC-101, Auranofin, Trametinib, GSK-458, Afatinib, and Panobinostat.
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METHOD FOR PRODUCING A PLANT EXTRACT AND FRACTION, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF (Fri, 15 May 2015)
<p id="p-0001" num="0000">The present invention describes the obtaining process of the dichloromethane fraction and subfractions from <i>Eleutherine plicata</i>, popularly known as “marupazinho, marupari, palmeirinha, coquinho, marupaí, marupaú, marupá-piranga, and lirio-folha-de-palmeira”. This invention comprises the obtaining process of pharmaceutical compositions that contain the dichloromethane fraction and/or naphthoquinone, as well as its use for malaria treatment. Extract and fractions were assayed and presented antiplasmodial activity, particularly against chloroquine-resistant <i>Plasmodium falciparum </i>(clone W2).</p>
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COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 15 May 2015)
Provided herein are compounds of the formula (I) : as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of malaria.
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NOVEL SUBSTITUTED 2-AMINOQUINAZOLIN-4(3H)-ONE DERIVATIVES AS MALARIAL ASPARTIC PROTEASE INHIBITORS (Fri, 08 May 2015)
The present invention discloses novel substituted 2-aminoquinazolin-4(3H)-one derivatives and their use as inhibitors of malarial aspartic protease plasmepsin I,II,IV or related malarial aspartic proteases, as well as pharmaceutical compositions thereof for treatment of malaria.
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Orally bioavailable pentamidine prodrugs for the treatment of diseases (Fri, 24 Apr 2015)
<p id="p-0001" num="0000">The present invention relates to prodrug derivatives of pentamidine, their use in the treatment and/or prophylaxis of diseases such as tumor diseases, as well as leishmaniasis, trypanosomiasis, pneumocystis carinii pneumonia (PcP), and malaria.</p>
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MALARIA VACCINATION (Fri, 17 Apr 2015)
The invention relates to an antigenic composition or vaccine comprising a viral vector, the viral vector comprising nucleic acid encoding Plasmodium protein Pf LSA1, or a part or variant of Plasmodium protein PfLSA1; PfLSAP2, or a part or variant of Plasmodium protein PfLSAP2; PfUIS3, or a part or variant of Plasmodium protein PfUIS3; PfI0580c, or a part or variant of Plasmodium protein PfI0580c; and PfSPECT-1, or a part or variant of Plasmodium protein Pf SPECT-1.
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METHOD FOR PRODUCING A PLANT EXTRACT AND FRACTION, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF (Thu, 26 Mar 2015)
The present invention describes the obtaining process of the dichloromethane fraction and subfractions from Eleutherine plicata, popularly known as "marupazinho, maruparí, palmeirinha, coquinho, marupaí, marupaú, marupá-piranga, and lírio-folha-de-palmeira". This invention comprises the obtaining process of pharmaceutical compositions that contain the dichloromethane fraction and/or naphthoquinone, as well as its use for malaria treatment. Extract and fractions were assayed and presented antiplasmodial activity, particularly against chloroquine-resistant Plasmodium falciparum (clone W2).
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HALOFUGINOL DERIVATIVES AND THEIR USE IN COSMETIC AND PHARMACEUTICAL COMPOSITIONS (Fri, 27 Feb 2015)
<p id="p-0001" num="0000">The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="80.01mm" wi="76.20mm" file="US20150057297A1-20150226-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ANTI-MALARIAL AGENTS (Thu, 19 Feb 2015)
The present invention relates to a novel class of quinolone-4-carboxamide <i>Pf</i>3D7 inhibitors of general formula (I) (Formula (I)) wherein R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, R<sp>4</sp>, R<sp>5</sp>, R<sp>6</sp>, R<sp>7</sp>, R<sp>8</sp> and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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Anti-malarial agents (Fri, 13 Feb 2015)
<p id="p-0001" num="0000">The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8 </sup>and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="41.06mm" wi="70.19mm" file="US09115088-20150825-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Antiprotozoal compounds (Fri, 06 Feb 2015)
<p id="p-0001" num="0000">The invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by administration of the compound, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of Human African Trypanosomiasis (HAT), Chagas disease, Leishmaniasis and malaria, the method comprising administering to a mammal, including a human, in need of such treatment a compound of formula I as described above.</p>
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Anti-malarial agents (Fri, 30 Jan 2015)
<p id="p-0001" num="0000">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:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.67mm" wi="62.65mm" file="US09266842-20160223-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Low anticoagulant heparins (Fri, 30 Jan 2015)
<p id="p-0001" num="0000">The present invention relates to a chemically modified heparin, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa. Also disclosed is a method of preparing the heparin and its medical use, including treatment of malaria.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="25.32mm" wi="51.05mm" file="US09480701-20161101-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Trioxane thioacetal monomers and dimers and methods of use thereof (Fri, 30 Jan 2015)
<p id="p-0001" num="0000">Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.</p>
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NEW ANTI-MALARIAL AGENTS (Fri, 23 Jan 2015)
The present invention is related to a use of pyrazole derivatives in the manufacture of a medicament for preventing or treating malaria. Specifically, the present invention is related to pyrazole derivatives useful for the preparation of a pharmaceutical formulation for the inhibition of malaria parasite proliferation.
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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 09 Jan 2015)
<p id="p-0001" num="0000">The present invention provides compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.72mm" wi="67.39mm" file="US20150011522A1-20150108-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a <i>Plasmodium </i>parasite, such as malaria.</p>
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OXONE-ACETONE MEDIATED METAL FREE PREPARATION OF SYN-DIOLS (Thu, 01 Jan 2015)
The present invention disclose a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of benzo fused olefins of formula (II) to obtain library of dioxolo compounds of formula (I). The invention further disclsoe a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of stilbene and its derivatives of formula (III) thereof. Also disclosed herein is Wacker-type oxidation of benzo-fused olefins of formula (X). The invention further disclose compounds of formula (I) which can be useful for the treatment of HIV, cancer or malaria.
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ANTI-MALARIAL AGENTS (Thu, 25 Dec 2014)
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.
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Compounds, compositions and associated methods comprising 3-aryl quinolines (Fri, 28 Nov 2014)
<p id="p-0001" num="0000">Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.</p>
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Multi-fluorescent substance including novel coumarin derivative, and LED light source-based microfluorescent quantitative biosensor for diagnosis using same (Fri, 28 Nov 2014)
<p id="p-0001" num="0000">The present invention relates to a novel coumarin derivative, to a method for preparing the same, and a multi-fluorescent substance that includes a plurality of the coumarin derivatives and is able to emit light using an LED light source. A novel coumarin derivative multi-fluorescent substance according to the present invention has an optimal emission wavelength band of 512 nm to 590 nm and thereby is effective in improving a signal intensity and stability since light emission using an LED light source is possible.</p> <p id="p-0002" num="0000">In addition, higher fluorescence reactivity is exhibited compared to coumarin fluorescent substances known in the related arts since one molecule has a plurality of fluorescent substances, and the problem of the coumarin fluorescent substance possibly binding to a binding site of the antigen of the antibody is solved since fluorescence detection is possible even when a minimum number of fluorescent substance molecules bind to an antibody.</p> <p id="p-0003" num="0000">Moreover, the novel coumarin derivative multi-fluorescent substance according to the present invention is suitably used in a fluorescent-linked immunosorbent assay (FLISA) and a rapid fluorescent immunochromatographic test (FICT) as an LED-based microfluorescent quantitative biosensor for diagnosis, therefore, diseases such as malaria may be rapidly and quantitatively analyzed.</p>
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INDOLE DERIVATIVES INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) (Fri, 21 Nov 2014)
<p id="p-0001" num="0000">The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="35.64mm" wi="66.97mm" file="US20140343001A1-20141120-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Adenoviral vector-based malaria vaccines (Fri, 14 Nov 2014)
<p id="p-0001" num="0000">The invention provides a method of inducing an immune response against malaria in a mammal. The method comprises intramuscularly administering to a mammal a composition comprising a pharmaceutically acceptable carrier and either or both of (a) a first adenoviral vector comprising a nucleic acid sequence encoding a <i>P. falciparum </i>circumsporozoite protein (CSP) operably linked to a human CMV promoter, and/or (b) a second adenoviral vector comprising a nucleic acid sequence encoding a <i>P. falciparum </i>apical membrane antigen 1 (AMA-1) antigen operably linked to a human CMV promoter.</p>
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DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES (Fri, 31 Oct 2014)
<p id="p-0001" num="0000">The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="50.38mm" wi="51.05mm" file="US20140323488A1-20141030-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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LOW ANTICOAGULANT HEPARINS (Thu, 30 Oct 2014)
The present invention relates to a chemically modified heparin, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa. Also disclosed is a method of preparing the heparin and its medical use, including treatment of malaria.
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Malaria antigen screening method (Fri, 24 Oct 2014)
<p id="p-0001" num="0000">The invention provides a method of identifying an antigen from a pathogen or a disease antigen comprising the use of an adenoviral vector array comprising two or more different adenoviral vectors, wherein each adenoviral vector comprises a nucleic acid sequence encoding a different antigen of a pathogen. The adenoviral vectors are administered to antigen presenting cells (APCs) in vitro or to an animal in vivo. The immunogenicity of the antigen is measured by screening for an immune response from effector T lymphocytes in vitro and by screening for the absence of pathogen-induced disease onset in vivo.</p>
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SYK KINASE INHIBITORS AS TREATMENT FOR MALARIA (Fri, 17 Oct 2014)
<p id="p-0001" num="0000">The disclosure relates to methods, compositions, and kits for treatment of parasite-mediated disease. In one embodiment, the disclosure relates to compounds, compositions, methods and kits for the treatment of malaria. In still another embodiment, the disclosure relates to a method for treating malaria comprising the use of a Syk kinase inhibitor.</p>
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Sphingosine Analogs, Compositions, and Methods Related Thereto (Fri, 17 Oct 2014)
<p id="p-0001" num="0000">The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of or diagnosed with a malaria infection.</p>
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SAPONINS AND CHROMANS DERIVATIVES MIXTURE COMPOSITIONS AGAINST LEISHMANIASIS, TRYPANOSOMIASIS AMERICANA, MALARIA, TRYPANOSOMIASIS AFRICANA AND FASCIOLA HEPATICA (Fri, 17 Oct 2014)
Saponins and chromans derivatives mixture compositions against leishmaniasis, trypanosomiasis americana, malaria, trypanosomiasis africana and fasciola hepa tica, is a composition of saponins and chromans derivatives. The saponins are triterpene types and chromans are hydrazones derivatives. This composition is a therapeutic agent against tropical diseases.
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Compositions and methods for the treatment of malaria (Fri, 03 Oct 2014)
<p id="p-0001" num="0000">The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.</p>
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COMPOSITIONS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 03 Oct 2014)
The present invention provides aminohydantoin anti-malarial agents. In some embodiments, these agents have the property of functions of targeting malarial aspartic proteases while at the same time having low activity against human BACE. Methods of employing such agents are also provided.
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Microparticle vaccine against malaria (Fri, 03 Oct 2014)
Multilayer films comprise polypeptide epitopes from <i>Plasmodium falciparum</i>, specifically a circumsporozoite T1, B or T* epitope. The multilayer films are capable of eliciting an immune response in a host upon administration to the host. The multilayer films can include at least one designed peptide that includes one or more polypeptide epitopes from a <i>Plasmodium protozoan. </i>
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COMPOSITIONS AND METHODS TO CONCURRENTLY TREAT AND/OR PREVENT MULTIPLE DISEASES WITH CUPREDOXINS (Fri, 26 Sep 2014)
<p id="p-0001" num="0000">The present invention relates to compositions and methods to administer compositions comprising cupredoxin and/or cytochrome and/or variants, derivatives, truncations and structural equivalents of cupredoxin and cytochrome to treat and/or prevent two or more conditions in a mammalian cell. The invention also relates to compositions and methods to administer compositions comprising cupredoxin and/or cytochrome and/or variants, derivatives, truncations and structural equivalents of cupredoxin and cytochrome to concurrently treat and/or prevent two or more conditions in a patient such as HIV, cancer, malaria and inappropriate angiogenesis.</p>
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HDAC6 INHIBITORS AND USES THEREOF (Fri, 26 Sep 2014)
The present invention relates to Histone deacetylases 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an autoimmune or inflammatory disorder, a neurodegenerative disease, a viral disease, malaria, or a combination thereof, also are disclosed.
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Small molecule malarial Aldolase-TRAP enhancers and glideosome inhibitors (Fri, 19 Sep 2014)
<p id="p-0001" num="0000">In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231-269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310, 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed.</p>
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NEW ARYLAMINOALCOHOL DERIVATIVES WITH ANTIPLASMODIAL ACTIVITY (Fri, 19 Sep 2014)
The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: I The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
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NEW ARYLAMINOALCOHOL DERIVATIVES WITH ANTIPLASMODIAL ACTIVITY (Fri, 19 Sep 2014)
The present invention relates to new arylaminoalcohol derivatives of formula (I), and to a method for the preparation of such compounds: The invention also relates to the use of these compounds as medicaments, and in particular for the prevention and/or the treatment of parasitic diseases caused by apicomplexan parasites such as malaria and toxoplasmosis. Finally, the invention relates to pharmaceutical compositions containing such compounds of formula (I) as active principles.
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Substituted 2-alkyl-1-OXO-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies (Fri, 22 Aug 2014)
<p id="p-0001" num="0000">In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl -1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.</p>
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Ruthenium carbon monoxide releasing molecules and uses thereof (Fri, 08 Aug 2014)
<p id="p-0001" num="0000">The present invention provides novel ruthenium compounds of Formula (I): or salts, isomers, hydrates, or solvates thereof, or combinations thereof; wherein E, R<sup>1</sup>, R<sup>2</sup>, R<sup>3</sup>, R<sup>4</sup>, R<sup>5</sup>, X<sub>1</sub>, and X<sub>2 </sub>are as defined herein, and pharmaceutical compositions thereof. Also provided are methods of use and treatment. Such compounds have been found useful in the treatment of malaria infection. Such compounds may also be useful in the treatment of inflammatory conditions, such as acute lung injury and acute respiratory distress syndrome, which optionally may be associated with a malaria infection.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.63mm" wi="59.27mm" file="US09062089-20150623-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Halofuginol derivatives and their use in cosmetic and pharmaceutical compositions (Fri, 08 Aug 2014)
The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
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TWO-CARBON LINKED ARTEMISININ-DERIVED TRIOXANE DIMERS (Fri, 01 Aug 2014)
Two-carbon linked artemisinin-derived trioxane dimers and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
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Anti-malarial compounds from marine natural products (Fri, 18 Jul 2014)
<p id="p-0001" num="0000">Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.</p>
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PIPERIDINYLCARBAZOLE AS ANTIMALARIAL (Fri, 18 Jul 2014)
The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R3, R4, X and Y have the meaning given in claim 1.
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Use of inhibitors of the activity or function of PI3K (Fri, 04 Jul 2014)
The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.
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SUBSTITUTED 2-ALKYL-1-OXO-N-PHENYL-3-HETEROARYL-1,2,3,4-TETRAHYDROISOQUINOLINE-4-CARBOXAMIDES FOR ANTIMALARIAL THERAPIES (Thu, 03 Jul 2014)

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THERAPEUTICALLY ACTIVE PYRAZOLO-PYRIMIDINE DERIVATIVES (Fri, 27 Jun 2014)
A series of pyrazolo[3,4-d]pyrimidine derivatives that are substituted at the 4- position by a diaza monocyclic, bridged bicyclic or spirocyclic moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseasesand malaria; and organ and cell transplant rejection.
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SYK KINASE INHIBITORS AS TREATMENT FOR MALARIA (Fri, 27 Jun 2014)
The disclosure relates to methods, compositions, and kits for treatment of parasite- mediated disease. In one embodiment, the disclosure relates to compounds, compositions, methods and kits for the treatment of malaria. In still another embodiment, the disclosure relates to a method for treating malaria comprising the use of a Syk kinase inhibitor.
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Hybrid Compounds And Methods Of Making And Using The Same (Fri, 20 Jun 2014)
<p id="p-0001" num="0000">The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a <i>Mycobacterium </i>infection; killing or inhibiting the growth of a <i>Plasmodium </i>species; inhibiting the growth of a <i>Mycobacterium </i>species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.</p>
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HYBRID COMPOUNDS AND METHODS OF MAKING AND USING THE SAME (Fri, 20 Jun 2014)
The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the gr 5 owth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.
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Compounds and compositions for the treatment of parasitic diseases (Fri, 06 Jun 2014)
<p id="p-0001" num="0000">The present invention provides compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="23.71mm" wi="66.89mm" file="US08871754-20141028-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a <i>Plasmodium </i>parasite, such as malaria. </p>
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Low anticoagulant heparins (Fri, 06 Jun 2014)
The present invention relates to a chemically modified heparin, with an antifactor II activity of less than 10 IU/mg, an antifactor Xa activity of less than 10 IU/mg and an average molecular weight (Mw) between about 6.5 and 9.5 kDa. Also disclosed is a method of preparing the heparin and its medical use, including treatment of malaria.
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Imidazo[1,2a]pyrazines and compositions comprising them for the treatment of parasitic diseases (Thu, 05 Jun 2014)
The invention provides compounds of formula Ia, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
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RUTHENIUM CARBON MONOXIDE RELEASING MOLECULES AND USES THEREOF (Thu, 29 May 2014)
The present invention provides novel ruthenium compounds of Formula (I): or salts, isomers, hydrates, or solvates thereof, or combinations thereof; wherein E, R<sp>1</sp>, R<sp>2</sp>, R<sp>3</sp>, R<sp>4</sp>, R<sp>5</sp>, X<sb>1</sb>, and X<sb>2</sb> are as defined herein, and pharmaceutical compositions thereof. Also provided are methods of use and treatment. Such compounds have been found useful in the treatment of malaria infection. Such compounds may also be useful in the treatment of inflammatory conditions, such as acute lung injury and acute respiratory distress syndrome, which optionally may be associated with a malaria infection.
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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 23 May 2014)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 23 May 2014)
The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a Plasmodium parasite.
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Sphingosine analogs, compositions, and methods related thereto (Fri, 23 May 2014)
The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of, or diagnosed with a malaria infection.
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Amphoteric polyamidoamines in the treatment of malaria (Thu, 22 May 2014)
The present invention relates to the use of amphoteric polyamidoamines with MW of 10-100 kDa as antimalarial agents or carriers of antimalarial drugs and to formulations thereof.
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HDAC inhibitors and therapeutic methods using the same (Fri, 09 May 2014)
<p id="p-0001" num="0000">Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.</p>
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ARTEMISININ DERIVATIVES, METHODS FOR THEIR PREPARATION AND THEIR USE AS ANTIMALARIAL AGENTS (Fri, 09 May 2014)
Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in pharmaceutical compositions intended for the treatment of parasitic infections are provided. Methods are provided for the production of artemisinin derivatives via functionalization of positions C7 and C6a, and optionally, in conjunction with modifications at positions C10 and C9, via chemoenzymatic methods. Recombinant cytochrome P450 polypeptides are also provided for use in the methods. The artemisinin derivatives can be used for the treatment of malaria and other parasitic infections, alone or in combination with other antiparasitic drugs.
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COMPOUNDS FOR USE IN THE TREATMENT OF PARASITIC DISEASES (Fri, 09 May 2014)
The present invention relates to compounds useful for treating parasitic diseases, which are infectious diseases caused or transmitted by a parasite. Compounds of the invention are particularly active against the causative pathogens in malaria. Such compounds are selective inhibitors of parasitic histone deacetylase (PfHDAC) and suppress the growth of parasites, such as Plasmodium falciparum, at a lower concentration than the concentration required for the inhibition of the growth of mammalian cells.
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Novel means and methods for treating malaria and other parasitic disorders (Thu, 08 May 2014)
The present invention relates to a compound of formula (I) wherein X is NH or O; Y is OH; A is H or COOH; B is H, CH 2 OH or CH 2 NH 2 ; (a) ZR 1 R 2 is isoquinolin-1-yl, said isoquinolin-1-yl being partially or fully hydrated in the N-containing ring; or given by formula (II) or (b) Z is O or N; R 1 is (i) C 1 to C 6 alkyl, preferably CH 3 ; C 2 to C 6 alkenyl; or C 2 to C 6 alkynyl; or (ii) arylalkyl, preferably phenylalkyl, alkyl in said arylalkyl being C 1 to C 4 alkyl, phenylalkyl preferably being CH 2 C 6 H 5 ; R 2 is (iii)absent in case of Z being O; or (iv) H in case of Z being N.
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ENZYME INHIBITING COMPOUNDS AND METHODS (Fri, 11 Apr 2014)
<p id="p-0001" num="0000">The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe<sub>4</sub>S<sub>4 </sub>cluster of an isoprenoid biosynthesis enzyme.</p>
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Natural product derivatives with antiprotozoal activity (Fri, 11 Apr 2014)
<p id="p-0001" num="0000">The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria.</p>
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Plasmodial surface anion channel inhibitors for the treatment or prevention of malaria (Fri, 21 Mar 2014)
<p id="p-0001" num="0000">The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y—R<sup>1</sup>—R2 (I), wherein Q, Y, R<sup>1</sup>, and R<sup>2 </sup>are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.</p>
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NOVEL BISAMINOQUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS PREPARED THEREFROM AND THEIR USE (Fri, 21 Feb 2014)
<p id="p-0001" num="0000">The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.</p>
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Novel bisaminoquinoline compounds, pharmaceutical compositions prepared therefrom and their use (Fri, 21 Feb 2014)
The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.
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Compounds having antiparasitic or anti-infectious activity (Fri, 14 Feb 2014)
<p id="p-0001" num="0000">Compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.89mm" wi="33.10mm" file="US09206131-20151208-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> or formula II: </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.89mm" wi="32.43mm" file="US09206131-20151208-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">or a pharmaceutically acceptable salt of formula I or formula II, wherein:</li> <li id="ul0002-0002" num="0000">R<sup>1 </sup>is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl;</li> <li id="ul0002-0003" num="0000">R<sup>2 </sup>is methyl or haloalkyl;</li> <li id="ul0002-0004" num="0000">R<sup>4 </sup>is hydroxyl, carbonyloxy, or carbonyldioxy; and</li> <li id="ul0002-0005" num="0000">R<sup>3 </sup>is aliphatic, aryl, aralkyl, or alkylaryl; and</li> <li id="ul0002-0006" num="0000">R<sup>5</sup>, R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO<sub>2</sub>R<sup>10</sup>, wherein R<sup>10 </sup>is H, alkyl, amino or haloalkyl;</li> <li id="ul0002-0007" num="0000">provided that in formula I, R<sup>5 </sup>and R<sup>7 </sup>are not both H or R<sup>6 </sup>is not H or methoxy; and in formula II that if R<sup>4 </sup>is carbonyldioxy then R<sup>7 </sup>is not methoxy.</li> </ul> </li> </ul> </p>
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Pentamidine amidoxime acid esters as prodrugs and use thereof as drugs (Fri, 14 Feb 2014)
The invention relates to prodrug derivatives of pentamidine, to the use thereof for the treatment and/or prophylaxis of diseases, in particular tumours, leishmaniasis, trypanosomiasis, Pneumocystis carinii pneumonia (PcP), and malaria.
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Dispiro 1,2,4-trioxolane antimalarials (Fri, 17 Jan 2014)
A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4 trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structuraiy simple, easy to synthesize, non-toxic, and potent against malarial Parasites. The compounds of tile invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
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ISOLATION OF AN ANTI-FALLIPHARUM DRUG CANDIDATE FROM THE LEAUES OF INDIAN ETHOS -MEDICINAL PLANT BAN-NARINGA OR SUREGADA MULTIFLORA (SYNOSMY; GELONIUM MULTIFLOROM) (Sat, 11 Jan 2014)
Leaves extract from Indian folk medicinal plant, ban-naringa effective against pali-azar or malaria, was shown to have anti-malarial activities against Plasmodiumfalcipharum in vitro. A 25% aquous-ethanolic crude extract (KS) inhibited 59% of theparasite growth in human RBC cells at 1 % concentration. Concentrated Fraction Y orTLC purified phyto-chemicals or most purified bioactive compound, KS-2000completely killed the parasites in vitro at a concentration 5-10μg/ml. Cytocidalactivities were assayed by both 3H-Hypoxanthine incorporation and Flurometricassays using Artimisinin and Chloroquine as standard. Crude extract or partially purephytochemical did not inhibit bacterium Escherichia, coli DH5∞, human HeLa cells ormolly fishes but significantly active against other protozoan parasites of the genusLeishmania and Trypanosoma at 20ug/ml and 50ug/ml respectively. The resultdemonstrated for the first time that ban-naringa plant (Scientific name: Suregadamultiflora and Synosym: Gelonium multiflorum) may be used as a potential source todevelop broad spectrum anti-protozoal drug to cure Bengal"s pali-azar and kala-azaror new world"s sleeping-sickness. The HPLC, MS, NMR, UV spectra(s) of KS-2000were initiated for identity the novel active principle, different from known activeprinciples. Mosquito-driven malaria disease is now spreading worldwide due tounavailability of vaccine and chloroquine resistance. Further investigation on KS-2000 may provide a lead to develop a better toxic drug against human blood borneprotozoa.
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Quinoline derivatives and uses thereof (Fri, 22 Nov 2013)
<p id="p-0001" num="0000">This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQ<sup>R </sup>and CQ<sup>S </sup>malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQ<sup>R </sup>reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQ<sup>R </sup>or CQ<sup>S </sup><i>Plasmodium </i>sp. (such as <i>P. falciparum</i>).</p>
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Plasmodial surface anion channel inhibitors for the treatment or prevention of malaria (Fri, 01 Nov 2013)
The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y-R<sp>1</sp>-R2 (I), wherein Q, Y, R<sp>1</sp>, and R<sp>2</sp> are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
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HDAC inhibitors and therapeutic methods of using same (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.</p>
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Compounds and compositions for the treatment of parasitic diseases (Fri, 25 Oct 2013)
<p id="p-0001" num="0000">The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.</p>
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ANTI-MALARIAL AGENTS (Fri, 18 Oct 2013)
The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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ANTI-MALARIAL AGENTS (Fri, 18 Oct 2013)
<br/><br/>The present invention relates to a novel class of quinolone-4-carboxamide <br/>P.function.3D7 inhibitors of general formula (I) <br/>(Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined <br/>herein, to their use in medicine, and in the treatment of <br/>malaria in particular, to compositions containing them, to processes for their <br/>preparation and to intermediates used in such processes.<br/></p>
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Therapeutic Compounds for Protozoal and Microbial Infections and Cancer (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and <i>trypanosoma </i>infections, bacterial infections such as <i>S. aureus </i>and <i>C. albicans</i>, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.</p>
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Anti-malaria compositions and methods (Fri, 04 Oct 2013)
<p id="p-0001" num="0000">Multilayer films comprise polypeptide epitopes from <i>Plasmodium falciparum</i>, specifically a circumsporozoite T1, B or T* epitope. The multilayer films are capable of eliciting an immune response in a host upon administration to the host. The multilayer films can include at least one designed peptide that includes one or more polypeptide epitopes from a <i>Plasmodium </i>protozoan.</p>
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MICROPARTICLE VACCINE AGAINST MALARIA (Fri, 04 Oct 2013)
Multilayer films comprise polypeptide epitopes from Plasmodium falciparum, specifically a circumsporozoite T1, B or T* epitope. The multilayer films are capable of eliciting an immune response in a host upon administration to the host. The multilayer films can include at least one designed peptide that includes one or more polypeptide epitopes from a Plasmodium protozoan.
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Cysteine protease inhibitors for the treatment of parasitic diseases (Fri, 20 Sep 2013)
<p id="p-0001" num="0000">Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, <i>ascariasis</i>, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.</p>
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HDAC inhibitors and therapeutic methods using the same (Fri, 13 Sep 2013)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
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TRIOXANE THIOACETAL MONOMERS AND DIMERS AND METHODS OF USE THEREOF (Sat, 07 Sep 2013)
Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.
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ANTI -MALARIAL AGENTS (Fri, 23 Aug 2013)
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.
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COMPOUNDS, COMPOSITIONS AND ASSOCIATED METHODS COMPRISING 3-ARYL QUINOLINES (Fri, 19 Jul 2013)
Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.
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HALOFUGINOL DERIVATIVES AND THEIR USE IN COSMETIC AND PHARMACEUTICAL COMPOSITIONS (Fri, 19 Jul 2013)
The present invention provides halofuginol, and derivatives and salts thereof, including diasteromerically enriched compositions thereof. The invention also provides pharmaceutical and cosmetic compositions thereof as well as methods for using halofuginol and derivatives thereof in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, malaria, ischemic damage, transplant rejection, neurodegenerative diseases, T-cell neoplasms, and cosmetic conditions.
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INDOLE DERIVATIVES INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) (Fri, 28 Jun 2013)
The present invention encompasses compounds having general formula (I) able to inhibit the lactate production (lactic acid) involved in the angiogenesis of tumoral tissues, in the glycolytic metabolic process of tumoral cells, of immune system cells in asthmatic diseases, in vascular cells in the pulmonary hypertension, in the treatment of chronic back pain or hyperoxaluria, and in the process by which the parasites protozoan causing malaria obtain most of the necessary energy
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METHOD OF SYNTHESIZING THE COMPLEX [ZN(NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM (Fri, 21 Jun 2013)
<p id="p-0001" num="0000">Metal complex of Zinc(II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 172.4. This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="81.79mm" wi="39.37mm" file="US20130158267A1-20130620-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Use of inhibitors of the activity or function of PI3K (Fri, 21 Jun 2013)
The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.
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METHOD OF SYNTHESIZING THE COMPLEX [NI (NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 14 Jun 2013)
<p id="p-0001" num="0000">Metal complex of Nickel (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (1.4). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand.</p>
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NOVEL COMPOUNDS AND THEIR USE IN THERAPY (Fri, 14 Jun 2013)
The invention provides compounds which inhibit N-myristoyltransferase and are selective for protozoal N-myristoyltransferase and, consequently suitable to treat microbial infections, including viral and fungal infections, and protozoan infections such as malaria, leishmaniasis and sleeping sickness.
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Dispiro 1,2,4-trioxolane antimalarials (Thu, 06 Jun 2013)
Dispiro 1,2,4-trioxolane, pharmaceutical formulation thereof, means and method for treating malaria, schistosomiasis, and cancer using a dispiro 1,2,4-trioxolane.
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METHOD OF SYNTHESIZING A COMPLEX [MN (NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 31 May 2013)
<p id="p-0001" num="0000">Metal complex of Manganese(II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite <i>Plasmodium falciparum</i>. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 132.2 This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl)ethylidene]hydrazinecarbodithioate ligand (FIG. <b>1</b>).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="43.18mm" wi="37.76mm" file="US20130137871A1-20130530-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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METHOD OF SYNTHESIZING A COMPLEX [CU(NNS)CL] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 31 May 2013)
<p id="p-0001" num="0000">Metal complex of Copper (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the copper complex has been analyzeThis paper describes the synthesis and characterization of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene]hydrazinecarbodithioate ligand (FIG. <b>1</b>).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.38mm" wi="69.85mm" file="US20130137872A1-20130530-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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DISUBSTITUTED TRIAZINE DIMERS FOR TREATMENT AND/OR PREVENTION OF INFECTIOUS DISEASES (Fri, 17 May 2013)
The present invention relates to novel compounds (I) containing two disubstituted triazine rings covalently linked by an organic linker, thereby creating dimers. These compounds show activity against the causative infective agents of infectious diseases such as African trypanosomiasis, Chagas disease, Leishmaniasis, Malaria and HIV. The invention further relates to the prevention and/or treatment of these diseases.
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SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS (Fri, 03 May 2013)
In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase. The method includes providing a first model comprising Aldolase or residues of the amino acid sequence corresponding to SEQ ID NO: 1 said residues being at amino acid positions selected from the group consisting of 10-13, 26, 27, 29, 30, 31, 32, 33, 37, 39, 40, 41, 43, 44, 47, 48, 51, 52, 60, 63, 66, 79, 84, 85, 92, 93, 103, 106-109, 112-117, 138, 142, 146, 148, 151, 153, 179, 182, 183, 185, 186, 194, 196, 197, 198, 199, 208, 226-228, 231- 269, 270, 272, 277-283, 285-289, 294, 295, 297-299, 301-304, 306-310, 312, 313, 316, 317, 319, 321, 323, 326, 330, 344, 345, and 347, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for modifying the activity of Aldolase. The present invention also discloses compounds and compositions which modify the activity of Aldolase, or a complex between Aldolase and TRAP. Methods of treating or preventing malaria, or an infection by apicomplexan organisms are also disclosed.
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Method of Synthesizing the Complex [FE(NNS)2] Active Against the Malaria Parasite Plasmodium Falciparum (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">Metal complex of Iron (U) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-ER spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite <i>Plasmodium falciparum</i>. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (FIG. <b>1</b>).</p>
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METHOD OF SYNTHESIZING A COMPLEX [CO (NNS) 2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM (Fri, 19 Apr 2013)
<p id="p-0001" num="0000">Metal complex of Cobalt (11) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing the deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (FIG. <b>1</b>).</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="39.29mm" wi="39.37mm" file="US20130096307A1-20130418-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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ORAL BIOAVAILABLE PENTAMIDIN PRODRUGS FOR TREATMENT OF DISEASES (Fri, 05 Apr 2013)
<p id="p-0001" num="0000">The present invention relates to prodrug derivatives of pentamidine, their use in the treatment and/or prophylaxis of diseases such as tumor diseases, as well as leishmaniasis, trypanosomiasis, pneumocystis carinii pneumonia (PcP), and malaria.</p>
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SPHINGOSINE ANALOGS, COMPOSITIONS, AND METHODS RELATED THERETO (Fri, 05 Apr 2013)
The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of, or diagnosed with a malaria infection.
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Novel artmisinin derivatives (Thu, 28 Mar 2013)
Compound of general formula 1 wherein n=1-5 are disclosed, as well as composition, such as pharmaceutical compositions, comprising such compounds, and use thereof in treatment of diseases such as malaria. Also methods for producing such compounds are disclosed.
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BIPHENYL COMPOUNDS FOR USE IN TREATING MALARIA AND OTHER PARASITIC DISORDERS (Fri, 15 Mar 2013)
The present invention relates to a compound of formula (I), wherein R1 and R2 are independently selected from (a) C1 to C6 alkyl; C2 to C6 alkenyl; C2 to C6 alkynyl; substituted or unsubstituted heterocycloalkyl or cycloalkyl, substituents being C1 to C6 alkyloxycarbonyl; (b) arylalkyl, heteroarylalkyl, or alkoxyphenylalkyl, alkyl in said arylalkyl, heteroarylalkyl and alkoxyphenylalkyl being C1 to C4 alkyl, alkoxy in said alkoxyphenylalkyl being C1 to C4 alkoxy; R3 and R4 are defined as follows: (c) R3 and R4 are independently selected from OH, OCH3 and phenylalkyl; (d) one of R3 and R4 is OH and the other is COOH; or (e) R3 and R4 are together (i) CO-O to form a 6-membered lactone ring; (ii) O-C(A)(B)-O to form a 7-membered acetal or ketal ring; or (iii) O-CH(A)-CH(B)-O or O-(CH2)n-O to form a ring with two ether oxygens, n being 1, 2, 3 or 4; wherein A and B are independently selected from hydrogen and C1 to C4 alkyl or C1 to C4 alkenyl such as allyl, preferably one of A and B being methyl or ethyl, the other being hydrogen; X1-Y1-Z1 and X2-Y2-Z2 are independently selected from CH2-CO-O, NH-CNH-NH, CH2-CO-NH, CH2-CNH-O, CH2-CNH-NH and CH2-CO; and R5, R6, R7, R8, R9 and R10 are H, wherein, in case R3 and R4 are selected from OH and OCH3, at least one of R3 and R4 is OH, at least one of X1-Y1-Z1 and X2-Y2-Z2 is NH-CNH-NH, CH2-CNH-O, CH2-CNH-NH or CH2-CO and/or at least one of R1 and R2 is substituted or unsubstituted heterocycloalkyl or cycloalkyl as defined above, pyridinylalkyl or naphtylalkyl, alkyl in said pyridinylalkyl and/or naphtylalkyl being C1 and C4 alkyl.
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SMALL MOLECULE NAPHTHOQUINONE- AND PHTHALIMIDE-BASED LIPOCATIONS AS ANTI-PARASITIC AGENTS (Fri, 15 Mar 2013)
Small molecule naphthoquinone- and phthalimide-based lipocations are provided, as well as methods for their use in treating or preventing anti-parasitic diseases, such as malaria, Chagas disease, and African Sleeping Sickness.
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SUBSTITUTED 2-ALKYL-1-OXO-N-PHENYL-3-HETEROARYL-1,2,3,4- TETRAHYDROISOQUINOLINE-4-CARBOXAMIDES FOR ANTIMALARIAL THERAPIES (Fri, 01 Mar 2013)
In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl-,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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DERIVATIVES OF PHENYL (THIO) UREA DEOXYTHYMIDINE AND USE THEREOF AS ANTIMALARIALS (Fri, 01 Feb 2013)
Deoxythymidine derivatives according to formula (I) are disclosed. wherein: X may be O or S; and R1, R2, R3, R4 and R5 may each be independently selected from H, halo, C1-C6 alkyl, C1-C6 haloalkyl, nitro, phenyl, heteroaryl, substituted heteroaryl wherein the substituents may be C1-C6 alkyl or C1-C6 haloalkyl, benzyl, -CH2OAr, -OR6 and six-membered ring heterocyclic groups containing 1 or more O and/or N heteroatoms wherein any N heteroatom may be C1-C6 alkyl-substituted; and R6 may be selected from C1-C6 alkyl, phenyl, six-membered ring heterocyclic groups containing at least one O heteroatom, benzyl and substituted benzyl wherein the substituents may be halo, C1-C6 alkyl or C1-C6 alkoxy; R7 may be H or C1-C6 alkyl; and the stereochemistry of the bond depicted as 〰 is either α or β. Such derivatives have shown good inhibitory activity against malaria-causing parasites, e.g. Plasmodium falciparum, but have shown low levels of toxicity to human cells.
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Small molecules with antimalarial activity (Fri, 25 Jan 2013)
<p id="p-0001" num="0000">The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria.</p>
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RUTHENIUM CARBON MONOXIDE RELEASING MOLECULES AND USES THEREOF (Fri, 25 Jan 2013)
The present invention provides novel ruthenium compounds of Formula (I): or salts, isomers, hydrates, or solvates thereof, or combinations thereof; wherein E, R1, R2, R3, R4, R5, X1, and X2 are as defined herein, and pharmaceutical compositions thereof. Also provided are methods of use and treatment. Such compounds have been found useful in the treatment of malaria infection. Such compounds may also be useful in the treatment of inflammatory conditions, such as acute lung injury and acute respiratory distress syndrome, which optionally may be associated with a malaria infection.
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SUBSTITUTED TETRACYCLINE COMPOUND FOR TREATMENT OF MALARIA (Fri, 18 Jan 2013)
<p>PROBLEM TO BE SOLVED: To provide a method for treatment or prevention of malaria in a subject.</p><p>SOLUTION: In one aspect, the invention relates to a method for treatment or prevention of malaria by administering an effective amount of substituted tetracycline compound. In another aspect, provided is a pharmaceutical composition that contains a pharmacologically acceptable carrier as well as an effective amount of tetracycline compound for the treatment of malaria in the subject. The substituted tetracycline compound can be used in combination with one or more anti-malarial compounds, and can be used for treatment or prevention of malaria resistant to one or more other antimalarial compounds.</p><p>COPYRIGHT: (C)2013,JPO&INPIT</p>
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COMPOUNDS INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS (Fri, 07 Dec 2012)
<p id="p-0001" num="0000">The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.</p>
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COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY (Fri, 07 Dec 2012)
Compound of formula I: or formula II, or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl, haloalkyl, or heteroaryl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or -SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; and R3 is
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Antimalarial agents that are inhibitors of dihydroorotate dehydrogenase (Fri, 30 Nov 2012)
<p id="p-0001" num="0000">Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="29.97mm" wi="45.38mm" file="US09238653-20160119-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and a triazolopyrimidine class of compounds that conform to Formula IX: </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.38mm" wi="59.10mm" file="US09238653-20160119-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts. </p>
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NEW ANTI-MALARIAL AGENTS (Thu, 29 Nov 2012)
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 formulation for the inhibition of malaria parasite proliferation.
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Method for treatment of malaria (Fri, 23 Nov 2012)
<p id="p-0001" num="0000">A method for treatment of malaria including administering to a patient in need thereof a flavonoid glycoside compound.</p>
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Anti-malarial agents (Fri, 23 Nov 2012)
<p id="p-0001" num="0000">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.</p>
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PHOSPHORIBOSYLTRANSFERASE INHIBITORS AND USES THEREOF (Fri, 09 Nov 2012)
The invention relates to compounds of formula (I) that are inhibitors of hypoxanthine and/or guanine purine phosphoribosyltransferases and to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit hypoxanthine and/or guanine purine phosphoribosyltransferases. Such diseases include malaria.
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GUANIDYLIMIDAZOLE AND GUANIDYLIMIDAZOLINE DERIVATIVES AS ANTIMALARIAL AGENTS, SYNTHESIS OF AND METHODS OF USE THEREOF (Fri, 02 Nov 2012)
The present invention relates to new guanidylimidazole derivatives and guanidylimidazoline derivatives, methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
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NOVEL BISAMINOQUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS PREPARED THEREFROM AND THEIR USE (Fri, 02 Nov 2012)
The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.
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2-GUANIDINO-4-OXO-IMIDAZOLINE DERIVATIVES AS ANTIMALARIAL AGENTS, SYNTHESIS AND METHODS OF USE THEREOF (Fri, 02 Nov 2012)
The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
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MACROLACTAM COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 19 Oct 2012)
The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by structural formula (l), wherein the values and preferred values of the variables are defined herein.
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PLASMODIAL SURFACE ANION CHANNEL INHIBITORS FOR THE TREATMENT OR PREVENTION OF MALARIA (Fri, 19 Oct 2012)
The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y-R1-R2 (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
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Anti-infective peptides comprising a C terminal amine group (Thu, 18 Oct 2012)
The invention relates to non-ribosomal peptides isolated from ontamopathogenic bacteria which have antibiotic activities against protozoan parasites wherein said peptides comprise a C terminal amine group. This group may be as a phenylethylamine, agmatine or tryptamne amino acid. Furthermore, the invention provides novel gene clusters which encode for the non-ribosomal peptide synthetases (NRPS) that mediate the biochemical synthesis of the inventive peptides. The peptides provided by the invention fall under the categories Xenortides, Rhabdopeptides and Mevalagmapeptides. Their use in medicine, specifically in the treatment of a disease caused by a protozoan parasite, such as malaria or sleeping sickness; and/or as insecticidals, for example in plant protection agents is disclosed. Furthermore provided are methods for the production of the peptides of the invention, and the enzymes and. nucleic acids useful for their synthesis in a host cell.
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HDAC inhibitors and therapeutic methods of using same (Fri, 05 Oct 2012)
<p id="p-0001" num="0000">Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.</p>
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2-aminoindole compounds and methods for the treatment of malaria (Fri, 14 Sep 2012)
<p id="p-0001" num="0000">The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="27.86mm" wi="56.64mm" file="US08980926-20150317-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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2-AMINOINDOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Thu, 06 Sep 2012)
The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)- The values and preferred values of the variables in Structural Formula I are defined herein.
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A METHOD OF SYNTHESIS OF COL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 18 Aug 2012)
Metal complex of Cobalt (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing the deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIS OF MNL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 18 Aug 2012)
Metal complex of Manganese(II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 132.2 This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIS OF NIL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 18 Aug 2012)
Metal complex of Nickel (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (1.4). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIS OF CDL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 18 Aug 2012)
Metal complex of Cadmium (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 172.4. This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIS OF FEL2 WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 18 Aug 2012)
Metal complex of Iron (II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 10 Aug 2012)
Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
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Enzyme inhibiting compounds and methods (Fri, 03 Aug 2012)
<p id="p-0001" num="0000">The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.</p>
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Isolation of Simalikalactone E and use thereof as a medicament, in the treatment of malaria (Fri, 15 Jun 2012)
<p id="p-0001" num="0000">The subject of the invention is a novel molecule, Simalikalactone E, which can be extracted from the plant <i>Quassia amara</i>, and also the use thereof as a medicament, in particular in the prevention and treatment of malaria.</p>
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ANTIMALARIAL COMPOUNDS (Fri, 01 Jun 2012)
The present invention relates to antimalarial compounds. More specifically, the present invention relates to novel substituted quinolone derivatives of formula (I) and related quinoline derivatives of formula (II) as defined herein that possess potent antimalarial activity. The present invention also relates to processes for the preparation of these quinolone and quinoline derivatives, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of malaria.
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Compounds inhibitors of enzyme lactate dehydrogenase (LDH) and pharmaceutical compositions containing these compounds (Fri, 01 Jun 2012)
The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.
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Compounds having antiparasitic or anti-infectious activity (Fri, 11 May 2012)
<p id="p-0001" num="0000">Compounds of formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.81mm" wi="33.10mm" file="US08598354-20131203-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000"> <ul id="ul0002" list-style="none"> <li id="ul0002-0001" num="0000">or formula II:</li> </ul> </li> </ul> </p> <p id="p-0003" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.81mm" wi="32.43mm" file="US08598354-20131203-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <ul id="ul0003" list-style="none"> <li id="ul0003-0001" num="0000"> <ul id="ul0004" list-style="none"> <li id="ul0004-0001" num="0000">or a pharmaceutically acceptable salt of formula I or formula II, wherein:</li> <li id="ul0004-0002" num="0000">R<sup>1 </sup>is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl;</li> <li id="ul0004-0003" num="0000">R<sup>2 </sup>is methyl or haloalkyl;</li> <li id="ul0004-0004" num="0000">R<sup>4 </sup>is hydroxyl, carbonyloxy, or carbonyldioxy; and</li> <li id="ul0004-0005" num="0000">R<sup>3 </sup>is aliphatic, aryl, aralkyl, or alkylaryl; and</li> <li id="ul0004-0006" num="0000">R<sup>5</sup>, R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO<sub>2</sub>R<sup>10</sup>, wherein R<sup>10 </sup>is H, alkyl, amino or haloalkyl;</li> <li id="ul0004-0007" num="0000">provided that in formula I, R<sup>5 </sup>and R<sup>7 </sup>are not both H or R<sup>6 </sup>is not H or methoxy; and in formula II that if R<sup>4 </sup>is carbonyldioxy then R<sup>7 </sup>is not methoxy.</li> </ul> </li> </ul> </p>
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Trioxane monomers and dimers (Fri, 04 May 2012)
<p id="p-0001" num="0000">Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.</p>
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METHODS OF TREATING CANCER AND OTHER DISEASES (Fri, 04 May 2012)
Disclosed are a method of treating cancer in a cell, a method of enhancing the chemotherapeutic treatment of a cancer treatment agent, a method of reducing resistance of a cancer cell to a chemotherapeutic agent, a method of reducing the amount or activity of an ABC-family mRNA and/or protein, a method of reducing the amount or activity of the ABCB1 mRNA and/or protein or the ABCC1 mRNA and/or protein in an animal cell undergoing cancer treatment, a method of reducing the amount or activity of glutathione and/or Bcl2 in the cancer cell, a method of treating other multidrug resistant diseases, and a method of treating a multidrug resistant cell such as a bacterial multidrug resistant Staphylococcus aureus (MRSA), tuberculosis, fungal infection, or MDR malaria, by administering a compound of the Formula (I): a diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein R1-R4 are as described herein. Also disclosed are pharmaceutical compositions comprising a compound of formula (I), a diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
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Pyridocarbazole type compounds and applications thereof (Fri, 17 Feb 2012)
<p id="p-0001" num="0000">Pyridocarbazole-type compounds of formula (I):</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="26.84mm" wi="45.21mm" file="US08604048-20131210-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> are provided as a medicament, and more particularly for application in anticancer chemotherapy. Also provided is a pharmaceutical composition with the compound and methods for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, parasitoses, such as malaria, or glaucomas. </p>
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Fused imidazoles and compositions comprising them for the treatment of parasitic diseases, such as e.g. malaria (Fri, 20 Jan 2012)
The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.
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A METHOD OF SYNTHESIS OF ZNL(LH)CL COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST THE CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Sat, 07 Jan 2012)
Metal complex of Zinc(II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 172.4. This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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AMINOALKYL SUBSTITUTED CHALCONES AND ANALOGUES AND DERIVATIVES THEREOF (Fri, 09 Dec 2011)
This invention relates to B-ring aminoalkyl substituted chalcones and analogues thereof. It also relates to processes for the synthesis of such compounds and to the use of such compounds as medicaments, in particular but not exclusively for the treatment of cancer and malaria.
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DERIVATIVES OF PANTOTHENIC ACID AND THEIR USE FOR THE TREATMENT OF MALARIA (Fri, 09 Dec 2011)
The present invention concerns novel pantothenone compounds having pantetheinase inhibitory activity as well as antiplasmodial activity. These compounds can suitably be used in therapeutic and or prophylactic treatment of malaria. Furthermore, the present invention provides combinations of pantothenone compounds and pantothenamides. Combining a pantothenone with a pantothenamide increases the antimalarial potency by an order of magnitude. It is hypothesized that inhibition of pantetheinase activity could protect pantothenamides against degradation by serum-derived pantetheinases, thereby revealing the hitherto unknown antimalaria activity of pantothenamides. The present invention thus, for the first time, makes available compounds and combinations of compounds for use in therapeutic and or prophylactic treatment of malaria infection in a human or animal subject in need thereof, relying on interference with host or pathogen-derived pantetheinase dependent pathways.
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A METHOD OF SYNTHESIZING THE COMPLEX [ZN(NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM (Fri, 28 Oct 2011)
Metal complex of Zinc(ll) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 172.4. This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand.
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A METHOD OF SYNTHEZISING THE COMPLEX [FE(NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 28 Oct 2011)
Metal complex of Iron (U) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-ER spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was foun to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIS OF CDL2 COMPLEX WITH HIGH BIOLOGICAL ACTIVITY AGAINST AT LEAST CHLOROQUINE RESISTANT STRAIN OF THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 28 Oct 2011)
Metal complex of Nickel (II) containing a dithio-based ligand have been synthesized and char¬ acterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (1.4). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[l-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIZING THE COMPLEX [NI (NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 28 Oct 2011)
Metal complex of Nickel (Π) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (1.4). This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIZING A COMPLEX [MN (NNS)2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 28 Oct 2011)
Metal complex of Manganese(II) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of 132.2 This paper describes the synthesis, characterization and biological results of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIZING A COMPLEX [CU(NNS)CL] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM FALCIPARUM (Fri, 28 Oct 2011)
Metal complex of Copper (II) containing a dithio- based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the copper complex has been analyzeThis paper describes the synthesis and characterization of the said metal complex containing deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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A METHOD OF SYNTHESIZING A COMPLEX [CO (NNS) 2] ACTIVE AGAINST THE MALARIA PARASITE PLASMODIUM (Fri, 28 Oct 2011)
Metal complex of Cobalt (11) containing a dithio-based ligand have been synthesized and characterized by elemental analysis, mass spectrometry, Proton NMR and FT-IR spectrometry. A single crystal X-ray structure of the cadmium complex has been analyzed. The metal complex was subjected to biological tests on falcipain-2 (FP-2) and falcipain-3 (FP-3) cysteine protease enzymes from the malaria parasite Plasmodium falciparum. They were further tested in vitro against chloroquine resistant strain (W2). Whereas the potency of the metal complexes was weaker than the control regarding the FP-2 and FP-3, the potency of metal complexes was found to be exceedingly greater than the control when tested against the chloroquine resistant strain (W2) with a strength ratio of (0.5). This paper describes the synthesis, characterization and biological results of the said metal complex containing the deprotonated 3-[1-(2-pyridyl) ethylidene] hydrazinecarbodithioate ligand (Fig. 1).
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Quinoline derivatives and uses thereof (Fri, 21 Oct 2011)
<p id="p-0001" num="0000">This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQ<sup>R </sup>and CQ<sup>S </sup>malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQ<sup>R </sup>reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQ<sup>R </sup>or CQ<sup>S </sup><i>Plasmodium </i>sp. (such as <i>P. falciparum</i>).</p>
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Modified chloroquines with single ring moiety or fused ring moiety (Fri, 14 Oct 2011)
<p id="p-0001" num="0000">The disclosure provides modified chloroquine compounds having single ring or fused ring moieties. Also provided are pharmaceutical compositions comprising such compounds, methods of using such compounds to inhibit or treat diseases or conditions caused by chloroquine-resistant (CQ<sup>R</sup>) and chloroquine-sensitive (Cq<sup>S</sup>) malaria parasites and other CQ-susceptible microorganisms, and processes and intermediates useful for preparing such compounds.</p>
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IMIDAZOLIDINEDIONE DERIVATIVES AS ANTIMALARIAL AGENTS, PREPARATION THEREOF, AND METHODS OF USE (Fri, 23 Sep 2011)
<p id="p-0001" num="0000">Embodiments disclosed herein relate to new imidazolidinedione derivatives, methods of making these compounds, and methods of using the same to prevent, treat, or inhibit malaria in a subject.</p>
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Modifications of cupredoxin derived peptides and methods of use thereof (Fri, 23 Sep 2011)
The present invention provides modified cupredoxin derived peptides with pharmacologic activity that have improved pharmacokinetic properties, and methods to use them to treat mammals suffering from various conditions related to the pharmacologic activities. Modifications of the cupredoxin derived peptides include amino acid sequence variants and structural derivations that increase the plasma half- life of the peptide, increase the specific activity of the pharmacologic activity, decrease immunogenicity, and decrease the biotransformation of the peptides. The modified cupredoxin derived peptides can be used in methods to treat mammals for cancer, conditions related to inappropriate angiogenesis, viral and bacterial infections, and specifically HIV and malaria, conditions related to ephrin signaling, and to deliver cargo compounds, including diagnostic compounds, to cancer cell.
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FUSED HETEROCYCLIC COMPOUNDS FOR USE IN THE TREATMENT OF MALARIA (Fri, 26 Aug 2011)
A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is -NR3R4 or -OR5; R2 is selected from aryl, heteroaryl, fused aryl- heterocycloalkyl and fused heteroaryl-heterocycloalkyl each of which may be optionally substituted by one or more R8 groups; R3 is H or alkyl; R4 is: (i) cycloalkyl optionally substituted by one or more -NR11R12, -NHCO2R11, -NHCOR11 and -NHSO2R11 groups; or (ii) -(CH2)n-heterocycloalkyl, wherein said heterocycloalkyl is a 4, 5 or 6-membered nitrogen-containing group optionally containing one or more CO groups, wherein said heterocycloalkyl is optionally substituted by one or more one or more (CH2)nR7 groups; (iii) -(CH2)n-heteroaryl, wherein said heteroaryl group is optionally substituted by one or more R7 groups; or (iv) alkyl substituted by one or more -NR11R12groups; or R3 and R4 are linked together with the nitrogen to which they are attached to form a 4, 5 or 6-membered heterocycloalkyl group optionally containing one or two further groups selected from CO, O, N and S, and which is optionally further substituted by one or more R7 groups; R5 is selected from alkyl, -(CH2)n-heteroaryl and -(CH2)n-heterocycloalkyl, wherein said heteroaryl and heterocycloalkyl groups are each optionally substituted by one or more R7 groups; each R11 and R12 is independently H or alkyl; and each n is independently an integer from O to 6; for use in treating or preventing a disorder associated with CDPK. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of PfCDPK1.
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Compounds and compositions useful in the treatment of malaria (Fri, 05 Aug 2011)
<p id="p-0001" num="0000">Provided herein compounds, compositions and methods useful for the treatment of malaria for a subject in need thereof, including compounds of Formula (I), Formula (II), Formula (III), Formula (IV), and Formula (V).</p>
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NEW ANTI-MALARIAL AGENTS (Fri, 22 Jul 2011)
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 formulation for the inhibition of malaria parasite proliferation.
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AMINOPYRIDINE DERIVATIVES AS ANTI-MALARIAL AGENTS (Fri, 22 Jul 2011)
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 formulation for the inhibition of malaria parasite proliferation.</p>
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METHODS AND COMPOSITIONS FOR TREATING A MALARIA-RELATED COMPLICATION (Fri, 15 Jul 2011)
Malaria infection remains the world's foremost parasitic disease affecting the central nervous system. Hundreds of millions of individuals are infected each year, resulting in more than 1 million deaths with staggering medical, economic, and emotional burdens in developing countries. A significant consequence of malaria infection is cerebral malaria (CM). It is clear that there is an unmet medical need for treating CM and other consequence of malaria infection. To this end, novel methods and compositions for treating a malaria-related complication are described herein, including methods and compositions for treating CM.
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18,21-Didesoxymacbecin Derivatives for the Treatment of Cancer (Fri, 01 Jul 2011)
<p id="p-0001" num="0000">The present invention relates to macbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pre-treatment for cancer. The present invention also provides methods for the production of these compounds involving incorporation of non-natural starter units and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.</p>
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Sulfamoyl- phenyl-ureido compounds and their use as medicament (Fri, 24 Jun 2011)
The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
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COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA (Fri, 17 Jun 2011)
<p id="p-0001" num="0000">The invention provides a class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.65mm" wi="60.20mm" file="US20110144107A1-20110616-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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TRIOXANE DIMER SULFUR COMPOUNDS (Thu, 09 Jun 2011)
The disclosure provides novel trioxane sulfur dimers having Formula I: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions.
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Trioxane dimer sulfur compounds (Fri, 27 May 2011)
<p id="p-0001" num="0000">The disclosure provides novel trioxane sulfur dimers having Formula I:</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="53.68mm" wi="75.10mm" file="US08592611-20131126-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer, proliferative disorders, and/or malaria using these compounds and/or compositions. </p>
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AMINO ARYL ACETAMIDES AND THEIR USE IN THE TREATMENT OF MALARIA (Fri, 27 May 2011)
Amino phenyl acetamide compounds of Formula (I):and pharmaceutically acceptable salts thereof: wherein R1, R2, R3 and Ra are as defined in the description, use of such compounds in the chemotherapy of certain parasitic protozoal infections such as malaria, pharmaceutical compositions including such compounds and processes for the preparation of such compounds, are provided.
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COMPOUNDS INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS (Fri, 13 May 2011)
The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.
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COMPOUNDS INHIBITORS OF ENZYME LACTATE DEHYDROGENASE (LDH) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS (Fri, 13 May 2011)
The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.</p>
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2-AMINOINDOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 06 May 2011)
The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)- The values and preferred values of the variables in Structural Formula I are defined herein.
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2-AMINOINDOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA (Fri, 06 May 2011)
The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)- The values and preferred values of the variables in Structural Formula I are defined herein.</p>
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S1P lyase inhibitors for the treatment of cerebral malaria (Fri, 29 Apr 2011)
Methods and compositions for treating, managing, and/or preventing cerebral malaria are disclosed.
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4,5-Dihydromacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies (Fri, 22 Apr 2011)
<p id="p-0001" num="0000">The present invention relates to 4,5-dihydromacbecin analogues to the formula (IA) or (IB), or a pharmaceutically acceptable salt there of: wherein: R<sub>1 </sub>represents H or CONH<sub>2 </sub>that are useful, e.g. in the treatment of cancer, B-cell malignancies malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.</p>
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Berberine as a selective lung cancer agent and other compositions and methods (Fri, 15 Apr 2011)
<p id="p-0001" num="0000">Berberine or its salts or derivatives are identified as the active compound for selectively inhibiting lung cancer, potentially without toxic side effects. Berberine is preferably obtained by synthesis or partial synthesis, or is obtained from natural sources, such as <i>Coptis teeta</i>, or other berberine containing plants. Berberine and its derivatives are also active against HIV, and may be a safe new drug for the prevention of AIDS, alone or in combination with other antiviral agents. Composition and method of inhibiting tumor or viral infections and malaria without toxic side effects. A natural composition from the rhizome of <i>Coptis teeta </i>may be used as a safe new drug for the prevention of human breast cancer.</p>
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NEW DERIVATIVES OF THIENO[2,3-B]PYRIDINE AND 5,6,7,8-TETRAHYDROTHIENO[2,3-B]QUINOLINE IN PARTICULAR USEFUL IN THE TREATMENT OF MALARIA (Fri, 15 Apr 2011)
51 ABSTRACT New derivatives of thieno[2,3-b]pyridine and 5,6,7,8-tetrahydrothieno[2,3-b]quinoline in 5 particular useful in the treatment of malaria The present invention is related to compounds of formula (I) N S R1 R2 R4 R3Ar AA' (I)10 in particular useful for the treatment of malaria, and to pharmaceutical compositions containing them.
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ENZYME INHIBITING COMPOUNDS AND METHODS (Fri, 15 Apr 2011)
The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.
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New derivatives of thieno[2,3-b]pyridine and 5,6,7,8 tetrahydrothieno[2,3 b]quinoline in particular useful in the treatment of malaria (Thu, 14 Apr 2011)
The present invention is related to compounds of formula (I) in particular useful for the treatment of malaria, and to pharmaceutical compositions containing them.
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