Malaria

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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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="US20140155367A1-20140605-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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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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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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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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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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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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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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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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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="US20140045888A1-20140213-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">or formula II:</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.89mm" wi="32.43mm" file="US20140045888A1-20140213-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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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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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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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-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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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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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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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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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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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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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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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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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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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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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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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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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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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="US20120302586A1-20121129-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003" num="0000">and a triazolopyrimidine class of compounds that conform to Formula IX:</p> <p id="p-0004" num="0000"><chemistry id="CHEM-US-00002" num="00002"> <img id="EMI-C00002" he="24.38mm" wi="59.10mm" file="US20120302586A1-20121129-C00002.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0005" num="0000">and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.</p>
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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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NEW 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 formulation 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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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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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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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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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="US20120232063A1-20120913-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, 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 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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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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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 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 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 [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 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 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 [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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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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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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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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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.</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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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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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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ANTIMALARIAL AGENTS THAT ARE INHIBITORS OF DIHYDROOROTATE DEHYDROGENASE (Fri, 08 Apr 2011)
Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound: and a triazolopyrimidine class of compounds that conform to Formula (IX): and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.
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ANTIMALARIAL AGENTS THAT ARE INHIBITORS OF DIHYDROOROTATE DEHYDROGENASE (Fri, 08 Apr 2011)
Inhibitors of parasitic dihydroorotate dehydrogenase enzyme (DHOD) are candidate therapeutics for treating malaria. Illustrative of such therapeutic agents include the compound: and a triazolopyrimidine class of compounds that conform to Formula (IX): and their solvates, stereoisomers, tautomers and pharmaceutically acceptable salts.</p>
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NOVEL ANTIMALARIAL 3-AZABICYCLO[3.2.2]NONANE DERIVATIVES (Fri, 01 Apr 2011)
The present invention relates to novel 3-azabicyclo[3.2.2]nonane derivatives of the general formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification. The novel 3-azabicyclo[3.2.2]nonane derivatives are particularly useful for treatment and prevention of malaria and trypanosomiasis.
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Novel antimalarial 3-azabicyclo[3.2.2]nonane derivatives (Thu, 31 Mar 2011)
The present invention relates to novel 3-azabicyclo[3.2.2]nonane derivatives of the general formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are as defined in the specification. The novel 3-azabicyclo[3.2.2]nonane derivatives are particularly useful for treatment and prevention of malaria and trypanosomiasis.
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Tetracycline compounds having target therapeutic activities (Thu, 31 Mar 2011)
Methods and compounds for treating osteomyelitis, bronchiectasis, cystic fibrosis, malaria or periodontitis, with a tetracycline compound of formula I: wherein: the substituents R 2 -R 12 have the values defined in the claims.
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Compounds and compositions useful for the treatment of parasitic diseases (Fri, 11 Mar 2011)
<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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O2-substituted 1- (2-carboxylato)pyrrolidin-1-yl diazen-1-ium-1,2-diolates (Thu, 10 Mar 2011)
O 2 -Substituted 1-[(2-carboxylato)pyrrolidin-1-yl] diazeniumdiolates are stable in aqueous solution and, in many cases, they can be activated for NO release by enzymatic action. Furthermore, if an N-nitroso derivative is formed by net formal cleavage of the N-N double bond of the 1-[(2-carboxylato)pyrrolin-1-yl]diazen-1-ium-1,2-diolate, the N-nitroso compound is noncarcinogenic. Such compounds are believed to be particularly useful in the treatment of fulminant liver failure, malaria, respiratory problems, impotence, and a variety of cardiovascular/hematologic disorders.
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Antimalarial Quinolines and Methods of Use Thereof (Fri, 25 Feb 2011)
<p id="p-0001" num="0000">One aspect of the invention relates to substitute quinolines with antimalarial activity, and compositions and kits comprising at least one of them. Another aspect of the invention relates to methods for the treatment or prevention or both of malaria comprising administering to a subject a therapeutically effective amount of such a compound. Importantly, a number of the compounds show excellent potency against both chloroquine-sensitive and chloroquine-resistant strains.</p>
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Dutpase inhibitors (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">Deoxyuridine derivatives of the formula</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="30.23mm" wi="76.03mm" file="US08017620-20110913-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> <br/> where <ul id="ul0001" list-style="none"> <li id="ul0001-0001" num="0000">R<sup>1 </sup>is H or various substituents;</li> <li id="ul0001-0002" num="0000">D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C≡C—, —NR<sup>5</sup>—;</li> <li id="ul0001-0003" num="0000">R<sup>4 </sup>is hydrogen or various substituents;</li> <li id="ul0001-0004" num="0000">R<sup>5 </sup>is H, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>alkanoyl;</li> <li id="ul0001-0005" num="0000">E is Si or C;</li> <li id="ul0001-0006" num="0000">R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are independently selected from C<sub>1</sub>-C<sub>8 </sub>alkyl, C<sub>2</sub>-C<sub>8 </sub>alkenyl, C<sub>2</sub>-C<sub>8 </sub>alkynyl or a stable monocyclic, bicyclic or tricyclic ring system;</li> <li id="ul0001-0007" num="0000">G is —O—, —S—, —CHR<sup>10</sup>—, —C(═O)—;</li> <li id="ul0001-0008" num="0000">J is —CH<sub>2</sub>—, or when G is CHR<sup>10 </sup>may also be —O— or —NH—;</li> <li id="ul0001-0009" num="0000">R<sup>10 </sup>is H, F, —CH<sub>3</sub>, —CH<sub>2</sub>NH<sub>2</sub>, —CH<sub>2</sub>OH, —OH;</li> <li id="ul0001-0010" num="0000">R<sup>11 </sup>is H, F, —CH<sub>3</sub>, —CH<sub>2</sub>NH<sub>2</sub>, —CH<sub>2</sub>OH, CH(OH)CH<sub>3</sub>, CH(NH<sub>2</sub>)CH<sub>3</sub>; or</li> <li id="ul0001-0011" num="0000">R<sup>10 </sup>and R<sup>11 </sup>together define an olefinic bond, or together form a —CH<sub>2</sub>-group, thereby defining a cis or trans cyclopropyl group; <br/> have utility in the prophylaxis or treatment of protozoal diseases such as malaria. </li> </ul> </p>
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Medicinal composition containing benzo[a]phenoxazine compound as the active ingredient for prevention or treatment of protozoal disease (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">Provided is a medicinal composition, in particular, a medicinal composition for treatment and/or prevention which has a high therapeutic effect on infection with a parasitic protozoa and a selective toxicity thereto and exhibits a life-prolonging effect and so on. A medicinal composition which contains as the active ingredient a benzo[a]phenoxazine compound represented by General formula (1) or a salt compound of the same, in particular, an agent for treating and/or preventing infection with a protozoa such as malaria, leishmaniasis, African trypanosomiasis, Chagas disease, toxoplasmosis, lymphatic filariasis, babesiosis or coccidium disease; and a novel compound which is contained therein as the active ingredient.</p>
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INDAZOLECARBOXAMIDE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF MALARIA (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.</p>
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Compounds and methods for their production (Fri, 28 Jan 2011)
<p id="p-0001" num="0000">The present invention relates to ansamycin 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 or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.</p>
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HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 28 Jan 2011)
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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HDAC INHIBITORS AND THERAPEUTIC METHODS USING THE SAME (Fri, 28 Jan 2011)
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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Substituted tetracycline compounds for the treatment of malaria (Thu, 27 Jan 2011)
This invention provides a method for treating or preventing malaria in a subject. The method includes administering to the subject an effective amount of a substituted tetracycline compound, such that malaria is treated or prevented. In one aspect, the invention relates to pharmaceutical compositions which include an effective amount of a tetracycline compound to treat malaria in a subject and a pharmaceutically acceptable carrier. The substituted tetracycline compounds of the invention can be used to in combination with one or more anti-malarial compounds or can be used to treat or prevent malaria which is resistant to one or more other anti-malarial compounds.
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FUSED IMIDAZOLES AND COMPOSITIONS COMPRISING THEM FOR THE TREATMENT OF PARASITIC DISEASES, SUCH AS E.G. MALARIA (Fri, 14 Jan 2011)
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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COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 14 Jan 2011)
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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Tumor necrosis factor-gamma (Fri, 07 Jan 2011)
<p id="p-0001" num="0000">Human TNF-gamma-alpha and TNF-gamma-beta polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing such polypeptides to inhibit cellular growth, for example in a tumor or cancer, for facilitating wound-healing, to provide resistance against infection, induce inflammatory activities, and stimulating the growth of certain cell types to treat diseases, for example restenosis. Also disclosed are diagnostic methods for detecting a mutation in the TNF-gamma-alpha and TNF-gamma-beta nucleic acid sequences or overexpression of the TNF-gamma-alpha and/or TNF-gamma-beta polypeptides. Antagonists against such polypeptides and their use as a therapeutic to treat cachexia, septic shock, cerebral malaria, inflammation, arthritis and graft-rejection are also disclosed.</p>
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MEDICINAL COMPOSITION CONTAINING BENZO[A]PHENOXANTHIN COMPOUND AS THE ACTIVE INGREDIENT FOR PREVENTING OR TREATING PROTOZOAL DISEASE (Thu, 06 Jan 2011)
Provided is a medicinal composition, in particular, a medicinal composition for treatment and/or prevention which has a high therapeutic effect on infection with a parasitic protozoa and a selective toxicity thereto and exhibits a life-prolonging effect and so on. A medicinal composition which contains as the active ingredient a benzo[a]phenoxazine compound represented by General formula (1) or a salt compound of the same, in particular, an agent for treating and/or preventing infection with a protozoa such as malaria, leishmaniasis, African trypanosomiasis, Chagas disease, toxoplasmosis, lymphatic filariasis, babesiosis or coccidium disease; and a novel compound which is contained therein as the active ingredient.
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CATHEPSIN CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF VARIOUS DISEASES (Thu, 30 Dec 2010)
The present invention relates to compounds capable of inhibiting and/or decreasing the activity of one or more cathepsins, thereby treating and/or preventing various disease states associated with one or more cysteine proteases including, but not limited to, cathepsins and papain-like cysteine proteases. Disease states treated and/or prevented by the compounds of the invention include, but are not limited to, mammalian parasitic diseases in which the parasite utilizes a critical cysteine protease from the papain family. Examples of parasitic diseases to be treated or prevented by the compounds of the invention include, but are not limited to, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, coccidiosis, giardiosis, cryptosporidiosis or schistosomiasis.
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PHENYLPYRIDYLPYRIDONES FOR USE AS ANTIMALARIAL AGENTS (Fri, 17 Dec 2010)
4-Pyridone derivatives of Formula (I) wherein R1, R2, X and n are as defined in the description and pharmaceutically acceptable salts thereof, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASE (Fri, 03 Dec 2010)
<p id="p-0001-en" 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, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. Compounds of formula I of the invention are capable of treating and/or preventing the above-identified diseases:</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="19.47mm" wi="56.73mm" file="US20100305056A1-20101202-C00001.TIF" img-content="photograph" img-format="png"/> </chemistry> </p>
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NOVEL POLYSPIRANE COMPOUNDS, APPLICATION THEREOF IN THE TREATMENT OF MALARIA OR TOXOPLASMOSIS AND METHOD FOR PREPARING SAME (Fri, 26 Nov 2010)
<p id="p-0001-en" num="0000">Novel polyspirane compounds used in the treatment of diseases involving parasites that belong to the phylum of apicomplexae, and a method for preparing the same.</p>
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TRIOXANE MONOMERS AND DIMERS (Fri, 26 Nov 2010)
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.
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Small molecules with antiprotozoal activity (Fri, 19 Nov 2010)
<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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4(1H)-pyridinone derivatives and their use as antimalaria agents (Thu, 04 Nov 2010)
4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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Desferrioxamine conjugates, derivatives and analogues (Fri, 29 Oct 2010)
<p id="p-0001" num="0000">The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.</p>
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MODIFICATIONS OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 22 Oct 2010)
<p id="p-0001-en" 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 cells.</p>
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Dicationic compounds which selectively recognize G-quadruplex DNA (Fri, 01 Oct 2010)
<p id="p-0001-en" num="0000">Dicationic compounds that are highly selective for binding G-quadruplex DNA are described. Several compounds exhibit groove binding toward G-quadruplex DNA and in vitro and in vivo activity versus <i>Trypanosoma brucei rhodesiense. </i>The compounds represent novel drugs for the treatment of cancer, malaria, leishmania, and trypanosomiasis.</p>
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MANNICH BASE TETRAOXANES (MANNOXANES) AND PHENOL SUBSTITUTED ANALOGUES (Fri, 01 Oct 2010)
The present invention relates to dispiro tetraoxane compounds of formula (VII) which may find application in the treatment of malaria.
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DISPIRO TETRAOXANE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MALARIA AND/OR CANCER (Thu, 30 Sep 2010)
A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=-C(O)NR 1 R 2 , -NR 1 R 2 or -S(O) 2 R 4 , where R 1 , R 2 and R 4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R 1 and R 2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring; or X=N and Y=-S(O) 2 R 3 or -C(O)R 3 , where R 3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.
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NEW METHOD FOR DETECTING ANTIMALARIAL DRUGS (Fri, 17 Sep 2010)
A method for screening a candidate substance as a potential drug for the treatment of malaria by assessing the formation of adducts substance:heme by mass spectrometry.
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Furo[3. 2-B] pyrrol derivatives (Fri, 27 Aug 2010)
<p id="p-0001" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R<sup>3 </sup>is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R<sup>4 </sup>is optionally substituted C<sub>1-8 </sub>alkyl or optionally substituted C<sub>3-8 </sub>cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="33.27mm" wi="73.07mm" file="US08053437-20111108-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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MODIFICATIONS OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 27 Aug 2010)
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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PYRIDOCARBAZOLE TYPE COMPOUNDS AND APPLICATIONS THEREOF (Fri, 27 Aug 2010)
The present invention relates to the use of pyridocarbazole-type compounds corresponding to the general formula (I) below: (I) as a medicament, and more particularly to the application thereof in anticancer chemotherapy. Another subject of the present invention is specific compounds of formula (I), and also pharmaceutical compositions comprising the compounds of formula (I) of the invention. Finally, the present invention relates to the use of the compounds of formula (I) for the preparation of a medicament intended for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, for the preparation of a medicament intended for preventing and/or treating parasitoses, such as malaria, or for the preparation of a medicament intended for preventing and/or treating glaucomas.
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PHOSPHATE ESTER OF A 4-PYRIDONE DERIVATIVE AND ITS USE IN THE CHEMOTHERAPY OF PARASITIC INFECTIONS (Fri, 27 Aug 2010)
A 4-pyridone (4-pyridinone) derivative of Formula I and pharmaceutically acceptable salts thereof, crystalline forms of said 4-pyridone derivative and salts thereof, pharmaceutical compositions comprising such 4-pyridone derivative and salts thereof and the use of the pharmaceutical compostitions in the chemotherapy of certain parasitic infections such as malaria, and in particular infection by Plasmodium falciparum.
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PYRIDOCARBAZOLE TYPE COMPOUNDS AND APPLICATIONS THEREOF (Fri, 27 Aug 2010)
The present invention relates to the use of pyridocarbazole-type compounds corresponding to the general formula (I) below: (I) as a medicament, and more particularly to the application thereof in anticancer chemotherapy. Another subject of the present invention is specific compounds of formula (I), and also pharmaceutical compositions comprising the compounds of for-mula (I) of the invention. Finally, the present invention relates to the use of the compounds of formula (I) for the preparation of a medicament intended for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, for the preparation of a medicament intended for preventing and/or treating parasitoses, such as malaria, or for the preparation of a medicament intended for preventing and/or treating glaucomas. </p>
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MODIFICATIONS OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 27 Aug 2010)
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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DESFERRIOXAMINE CONJUGATES, DERIVATIVES AND ANALOGUES (Thu, 12 Aug 2010)
The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.
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Sulfamoyl-phenyl-ureido compounds and their use as medicament (Fri, 06 Aug 2010)
<p id="p-0001" num="0000">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.</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="24.55mm" wi="69.85mm" file="US08343963-20130101-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Anti-malarial compound isolated from <i>Gomphostema niveum </i> (Fri, 06 Aug 2010)
<p id="p-0001" num="0000">The present invention provides an antimalarial compound 3-[2-(2-Hydroxymethyl-1,4a,5-trimethyl-7-oxo-1,2,3,4,4a,7 8,8a-octahydronaphthalen-1-yl)-ethyl]-5H-furan-2-one of the formula 1 given below</p> <p id="p-0002" num="0000"><chemistry id="CHEM-US-00001" num="00001"> <img id="EMI-C00001" he="40.72mm" wi="37.76mm" file="US08188303-20120529-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 derivatives thereof, isolated from <i>Gomphostema niveum </i>and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound.</li> </ul> </li> </ul> </p>
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Isoform selective HDAC inhibitors (Fri, 06 Aug 2010)
<p id="p-0001" num="0000">One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising an HDAC inhibitor of the invention.</p>
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SULFAMOYL- PHENYL-UREIDO BENZAMIDINE-DERIVATIVES AS ANTIMALARIAL AGENTS (Fri, 06 Aug 2010)
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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SULFAMOYL-PHENYL-UREIDO BENZAMIDINE-DERIVATIVES AS ANTIMALARIAL AGENTS (Fri, 06 Aug 2010)
The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologi-cally acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular un-complicated or severe malaria caused by plasmodia. </p>
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4 ( 1H) -PYRIDINONE DERIVATIVES AND THEIR USE AS ANTIMALARIA AGENTS (Fri, 23 Jul 2010)
4-pyridone (4-pyridinone) derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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MOLECULAR ASSAY FOR DIAGNOSIS OF MALARIA (Fri, 16 Jul 2010)
The invention is directed to compositions, methods and kits for diagnosing malaria using primers that amplify target sequences in Plasmodium falciparum, P. malariae, P. vivax, and P. ovale. The amplified target sequences are then analyzed by any number of mass spectrometric techniques, which data are queried against a database of base composition signatures of Plasmodia sp.
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DISPIRO 1,2,4-TRIOXOLANE ANTIMALARIALS (Thu, 08 Jul 2010)
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 structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the 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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Bisbenzimidazoles as antimalarial agents (Fri, 25 Jun 2010)
<p id="p-0001-en" num="0000">The present invention relates to antimalarial agents. In particular, the present invention relates to the use of bisbenzimidazoles of Formula I for the prevention and/or treatment of malaria,</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">wherein n is an integer selected from 0 to 10, and <ul id="ul0001-en" list-style="none"><li>R<sup>1 </sup>and R<sup>2 </sup>are each independently selected from hydrogen, halogen, hydroxyl, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, alkylcarbonyloxy, formyl, alkylcarbonyl, alkyloxycarbonyl, halocarbonyl, haloalkyl, haloalkoxy, carbamoyl, cyano, nitro, sulfo, or a carboxyl group.</li></ul></p>
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BISBENZIMIDAZOLES AS ANTIMALARIAL AGENTS (Thu, 17 Jun 2010)
The present invention relates to antimalarial agents. In particular, the present invention relates to the use of bisbenzimidazoles of Formula (I) for the prevention and/or treatment of malaria, wherein n is an integer selected from 0 to 10, and R<sp>1</sp> and R<sp>2</sp> are each independently selected from hydrogen, halogen, hydroxyl, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, alkylcarbonyloxy, formyl, alkylcarbonyl, alkyloxycarbonyl, halocarbonyl, haloalkyl, haloalkoxy, carbamoyl, cyano, nitro, sulfo, or a carboxyl group.
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MODIFIED CHLOROQUINES WITH SINGLE RING MOIETY OR FUSED RING MOIETY (Fri, 11 Jun 2010)
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 (CQR) and chloroquine-sensitive (CQS) malaria parasites and other CQ-susceptible microorganisms, and processes and intermediates useful for preparing such compounds.
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MODIFIED CHLOROQUINES WITH BRANCHED MOIETY (Fri, 11 Jun 2010)
The disclosure provides modified chloroquine compounds having branched 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 (CQR) and chloroquine-sensitive (CQS) malaria parasites and other CQ-susceptible microorganisms, and processes and intermediates useful for preparing such compounds
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COMPOUNDS HAVING ANTIPARASITIC OR ANTI-INFECTIOUS ACTIVITY (Fri, 11 Jun 2010)
Compounds 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 or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and 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; provided that in formula (I), R5 and R7 are not both H or R6 is not H or methoxy; and in formula (II) that if R4 is carbonyldioxy then R7 is not methoxy. </p>
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DISPIRO TETRAOXANE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MALARIA AND/OR CANCER (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR<sup>1</sup>R<sup>2</sup>, —NR<sup>1</sup>R<sup>2 </sup>or —S(O)<sub>2</sub>R<sup>4</sup>, where R<sup>1</sup>, R<sup>2 </sup>and R<sup>4 </sup>are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R<sup>1 </sup>and R<sup>2 </sup>are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=—S(O)<sub>2</sub>R<sup>3 </sup>or —C(O)R<sup>3</sup>, where R<sup>3 </sup>is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="16.17mm" wi="60.28mm" file="US20100113436A1-20100506-C00001.TIF" img-content="chem" img-format="tif"/> </chemistry> </p>
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S1P LYASE INHIBITORS FOR THE TREATMENT OF CEREBRAL MALARIA (Fri, 07 May 2010)
<p id="p-0001-en" num="0000">Methods and compositions for treating, managing, and/or preventing cerebral malaria are disclosed.</p>
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S1P LYASE INHIBITORS FOR THE TREATMENT OF CEREBRAL MALARIA (Fri, 07 May 2010)
Methods and compositions for treating, managing, and/or preventing cerebral malaria are disclosed.
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NEW IMIDAZOLIDINEDIONE DERIVATIVES AS ANTIMALARIAL AGENTS, PREPARATION THEREOF, AND METHODS OF USE (Fri, 07 May 2010)
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.
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S1P LYASE INHIBITORS FOR THE TREATMENT OF CEREBRAL MALARIA (Fri, 07 May 2010)
Methods and compositions for treating, managing, and/or preventing cerebral malaria are disclosed. </p>
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New analogs of polysphorin and uses thereof for treating or preventing malaria (Thu, 22 Apr 2010)
The present invention discloses new analogs of polysphorin and their uses as antimalarial drugs which are highly effective in the hepatic phase of the disease. The present invention further discloses a new method for preparing these compounds.
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NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS (Fri, 16 Apr 2010)
<p id="p-0001-en" num="0000">The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant <i>Plasmodium falciparum </i>strains and in vivo activity against <i>P. berghei. </i></p>
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NEW ANALOGS OF POLYSPHORIN AND USES THEREOF FOR TREATING OR PREVENTING MALARIA (Fri, 16 Apr 2010)
The present invention discloses new analogs of polysphorin and their uses as antimalarial drugs which are highly effective in the hepatic phase of the disease. The present invention further discloses a new method for preparing these compounds.
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Natural product derivatives with antimalarial activity (Fri, 09 Apr 2010)
<p id="p-0001-en" 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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USE OF BENZOXAZOLE COMPOUNDS IN THE TREATMENT OF MALARIA (Fri, 02 Apr 2010)
The present invention provides methods of preventing or treating malaria using benzoxazole compounds. The present invention further provides pharmaceutical compositions including an effective amount of the benzoxazole compounds for the prevention or treatment of malaria.
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DUTPASE INHIBITORS (Fri, 26 Mar 2010)
<p id="p-0001-en" num="0000">Deoxyuridine derivatives of the formula</p> <p id="p-0002-en" num="0000"> <ul id="ul0001-en" list-style="none"> <li> <ul id="ul0002-en" list-style="none"> <li>where</li> <li>A is O, S or CH<sub>2</sub>; B is O, S or CHR<sup>3</sup>;</li> <li>R<sup>1 </sup>is H, or various substituents;</li> <li>R<sup>2 </sup>is H, F;</li> <li>R<sup>3 </sup>is H, F, OH, NH<sub>2</sub>; or R<sup>2 </sup>and R<sup>3 </sup>together form a chemical bond;</li> <li>D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C<u>═</u>C—, —NR<sup>5</sup>—; R<sup>4 </sup>is hydrogen or various substituents;</li> <li>R<sup>5 </sup>is H, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>alkanoyl;</li> <li>E is Si or C;</li> <li>R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are independently selected from C<sub>1</sub>-C<sub>8 </sub>alkyl, C<sub>2</sub>-C<sub>8 </sub>alkenyl, C<sub>2</sub>-C<sub>8 </sub>alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system <br/> have utility in the prophylaxis o treatment of parasitic diseases such as malaria </li> </ul> </li> </ul> </p>
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PRODRUGS OF ARTEMISININ (Fri, 26 Mar 2010)
This invention relates to prodrugs based on artemisinin and to a method of manufacturing such prodrugs. The prodrugs of artemisinin according to the invention have the general structure A-B-M wherein A is a dihydroartemisinin moiety; B is a linking group; and M is a moiety selected from the group consisting of moieties derived from anti-malarial drugs other than artemisinin, in particular quinoline derivatives, and moieties derived from amine compounds. The invention further relates to the use of such prodrugs in the prevention and treatment of malaria and in the manufacture of a medicament for use in such treatment. This invention also relates to the oral and transdermal application of such prodrugs.
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17-Oxymacbecin Derivatives and Their Use in the Treatment of Cancer and/or B-Cell Malignancies (Fri, 19 Mar 2010)
<p id="p-0001-en" num="0000">The present invention relates to 17-oxymacbecin 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 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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PURINE COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS FOR THE TREATMENT OF PLASMODIUM RELATED DISEASES (Fri, 05 Mar 2010)
<p id="p-0001-en" num="0000">The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.</p>
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QUINOLINE COMPOUNDS CONTAINING A DIBEMETHIN GROUP (Fri, 19 Feb 2010)
4-Amino-7-chloroquinolines are described containing dibenzylmethylamine (dibemethin) side chains attached via a methylene bridge to the amino group of the quinoline showing strong antimalarial and resistance reversing activity. The compounds are of the general formula (I), wherein X1, X2, X3 and X4 are independently selected from the group consisting of H, alkoxy, amido, optionally substituted amino, cyano, halo, haloalkyl, hydroxyl, nitro, sulphonamide and trifluoromethyl; Y is CH or N; m, n, p, q, r and s are independently from 0 to 5; R1, R2, R3 and R4 are independently selected from the group consisting of H, optionally substituted alkyl, alkenyl, alkynyl cycloalkyl, aryl, heteroaryl and heterocyclyl, wherein R3 and R4 together with the carbon atoms to which they are joined optionally form a six membered ring; or pharmaceutically acceptable salts thereof. Pharmaceutical compositions containing at least one of these compounds are also described for treating or preventing malaria.
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TRIOXANE DIMER SULFUR COMPOUNDS (Fri, 22 Jan 2010)
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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Furo[3,2-B] pyrrol -3-one derivatives and their use as cysteinyl porteinase inhibitors (Fri, 15 Jan 2010)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (1), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R<sup>1 </sup>and R<sup>2 </sup>is H, and the other is selected from F and Cl, or R<sup>1 </sup>and R<sup>2 </sup>are both F; R<sup>3 </sup>is selected from cyclopentyl and cyclohexyl; R<sup>4 </sup>is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p> <p id="p-0002-en" num="0000"/>
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COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA (Fri, 18 Dec 2009)
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. (I)
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COMPOUNDS AND COMPOSITIONS USEFUL FOR THE TREATMENT OF MALARIA (Fri, 18 Dec 2009)
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. (I) </p>
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ANTIMALARIAL QUINOLINES AND METHODS OF USE THEREOF (Fri, 11 Dec 2009)
One aspect of the invention relates to substitute quinolines with antimalarial activity, and compositions and kits comprising at least one of them. Another aspect of the invention relates to methods for the treatment or prevention or both of malaria comprising administering to a subject a therapeutically effective amount of such a compound. Importantly, a number of the compounds show excellent potency against both chloroquine-sensitive and chloroquine-resistant strains.
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Novel Compounds and Methods for Their Production (Fri, 04 Dec 2009)
<p id="p-0001-en" num="0000">The present invention relates to 15-desmethoxymacbecin 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 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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TRIOXANE DIMERS HAVING HIGH ANTICANCER AND LONG-LASTING ANTIMALARIAL ACTIVITIES (Fri, 27 Nov 2009)
<p id="p-0001-en" num="0000">The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.</p> <p id="p-0002-en" num="0000"/>
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NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS (Thu, 26 Nov 2009)
The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant Plasmodium falciparum strains and in vivoactivity against P.berghei.
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MODIFICATION OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 20 Nov 2009)
<p id="p-0001-en" 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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Papain Family Cysteine Protease Inhibitors for the Treatment of Parasitic Diseases (Fri, 23 Oct 2009)
<p id="p-0001-en" num="0000">Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition of these proteases can be useful in the treatment of these parasitic diseases, including toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis or schistosomiasis.</p>
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18 ,21-Didesoxymacbecin Derivatives for the Treatment of Cancer (Fri, 09 Oct 2009)
<p id="p-0001-en" num="0000">The present invention relates to 18,21-didesoxymacbecin 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 and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.</p>
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Analogues of coformycin and their use for treating protozoan parasite infections (Fri, 11 Sep 2009)
<p id="p-0001" num="0000">This invention relates to compounds that are analogues of coformycin, pharmaceutical compositions containing the compounds, and methods of using the compounds for treating protozoan parasite infections, especially malaria.</p>
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ODCase inhibitors for the treatment of malaria (Fri, 04 Sep 2009)
<p id="p-0001" num="0000">The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.</p>
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Compositions and methods to concurrently treat or prevent multiple diseases with cupredoxins (Fri, 21 Aug 2009)
<p id="p-0001-en" 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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21-DEOXYMACBECIN ANALOGUES USEFUL AS ANTITUMOR AGENTS (Fri, 21 Aug 2009)
<p id="p-0001-en" num="0000">The present invention relates to 21-deoxymacbecin 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 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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15-O-Desmethylmacbecin Derivatives and Their Use in the Treatment of Cancer or B-Cell Malignancies (Fri, 21 Aug 2009)
<p id="p-0001-en" num="0000">The present invention relates to 15-O-desmethylmacbecin analogues according to the formula (IA) or (IB) herein, or a pharmaceutically acceptable salt thereof: wherein: R<sub>1 </sub>and R<sub>2 </sub>either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R<sub>3 </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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DIHYDROOROTATE DEHYDROGENASE INHIBITORS WITH SELECTIVE ANTI-MALARIAL ACTIVITY (Fri, 21 Aug 2009)
<p id="p-0001-en" num="0000">Compounds according to Formula I, Formula II, Formula III, Formula V, Formula VI, or to Formula VII,</p> <p id="p-0002-en" num="0000"/> <p id="p-0003-en" num="0000">and pharmaceutical compositions of compounds that conform to Formula IV or Formula VIII:</p> <p id="p-0004-en" num="0000"/> <p id="p-0005-en" num="0000">where R<sup>1 </sup>through R<sup>33 </sup>are prescribed, selectively inhibit <i>P. falciparum </i>dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.</p>
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Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors (Fri, 14 Aug 2009)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof,</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="42.93mm" wi="73.32mm" file="US07846935-20101207-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein: <br/> X is CH or N; and <br/> R<sup>4 </sup>is optionally substituted C<sub>3-8 </sub>alkyl or optionally substituted C<sub>3-8 </sub>cycloalkyl. </p> <p id="p-0003-en" num="0000">The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p>
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Tetrahydrofuro[3,2-B] pyrrol-3-ones as cathepsin K inhibitors (Fri, 07 Aug 2009)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof,</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="39.45mm" wi="73.32mm" file="US07803803-20100928-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein: <ul id="ul0001-en" list-style="none"><li>X is CH or N;</li><li>one of R<sup>1 </sup>and R<sup>2 </sup>is H, and the other is selected from OR<sup>6</sup>, SR<sup>6</sup>, NR<sup>6</sup>R<sup>7</sup>, N<sub>3</sub>, Me, Et, CF<sub>3</sub>, SOR<sup>8 </sup>and SO<sub>2</sub>R<sup>8</sup>;</li><li>R<sup>3 </sup>is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl;</li><li>R<sup>4 </sup>is optionally substituted C<sub>1-8 </sub>alkyl or optionally substituted C<sub>3-8 </sub>cycloalkyl;</li><li>R<sup>6 </sup>and R<sup>7 </sup>are each independently selected from H, C<sub>1-8</sub>-alkyl and C<sub>3-8</sub>-cycloalkyl, or R<sup>6 </sup>and R<sup>7 </sup>are linked to form a cyclic group together with the nitrogen to which they are attached; and</li><li>R<sup>8 </sup>is C<sub>1-8</sub>-alkyl or C<sub>3-8</sub>-cycloalkyl.</li></ul></p> <p id="p-0003-en" num="0000">The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p>
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Furo[3,2-B] pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors (Fri, 31 Jul 2009)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R<sup>3 </sup>is cyclopentyl or cyclohexyl; X is CH or N; and R<sup>4 </sup>is optionally substituted C<sub>1-8 </sub>alkyl or optionally substituted C<sub>3-8 </sub>cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="33.36mm" wi="73.32mm" file="US07846934-20101207-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Tetrahydrofuro(3,2-B) pyrrol-3-one derivatives as inhibitors of cysteine proteinases (Fri, 24 Jul 2009)
<p id="p-0001-en" num="0000">A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof,</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="28.36mm" wi="69.85mm" file="US07799791-20100921-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> wherein: one of R<sup>1 </sup>and R<sup>2 </sup>is H, and the other is selected from OR<sup>6</sup>, SR<sup>6</sup>, NR<sup>6</sup>R<sup>7</sup>, N<sub>3</sub>, Me, Et, CF<sub>3</sub>, SOR<sup>8 </sup>and SO<sub>2</sub>R<sup>8</sup>; or <ul id="ul0001-en" list-style="none"><li>R<sup>1 </sup>and R<sup>2 </sup>are both H;</li><li>one of R<sup>3 </sup>and R<sup>4 </sup>is H, and the other is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; or</li><li>R<sup>3 </sup>and R<sup>4 </sup>are joined together with the adjacent backbone carbon atom to form a spiro-C<sub>5</sub>-C<sub>6 </sub>cycloalkyl group;</li><li>R<sup>6 </sup>and R<sup>7 </sup>are each independently selected from H, C<sub>1-8</sub>-alkyl and C<sub>3-8</sub>-cycloalkyl; or</li><li>R<sup>6 </sup>and R<sup>7 </sup>are linked to form a cyclic group together with the nitrogen to which they are attached;</li><li>R<sup>8 </sup>is C<sub>1-8</sub>-alkyl or C<sub>3-8</sub>-cycloalkyl;</li><li>R<sup>9 </sup>is a para-substituted 6-membered monocyclic aryl or heteroaryl ring which includes up to five heteroatoms.</li></ul></p> <p id="p-0003-en" num="0000">The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p>
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Furo[3, 2-b] pyrrol derivatives (Fri, 24 Jul 2009)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R<sup>3 </sup>is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R<sup>4 </sup>is optionally substituted C<sub>1-8 </sub>alkyl or optionally substituted C<sub>3-8 </sub>cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="33.27mm" wi="73.32mm" file="US07737150-20100615-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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SPIRO AND DISPIRO 1,2,4-TRIOXOLANE ANTIMALARIALS (Fri, 24 Jul 2009)
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, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.
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TETRAHYDROFURO (3, 2-B) PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES (Thu, 16 Jul 2009)
Compounds of formula (I) and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget' s disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain. Compounds (I) are cysteine protease inhibitors.
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DIHYDROOROTATE DEHYDROGENASE INHIBITORS WITH SELECTIVE ANTI-MALARIAL ACTIVITY (Fri, 03 Jul 2009)
Compounds according to Formula (I), Formula (II), Formula (III), Formula (V), Formula (VI), or to Formula (VII), and pharmaceutical compositions of compounds that conform to Formula (IV) or (Formula VIII): where R1 through R33 are prescribed, selectively inhibit P. falciparum dihydroorotate dehydrogenase. Accordingly, a method for preventing and treating malaria attaches to such compounds, as well as to pharmaceutically acceptable salts, solvates, stereoisomers, tautomers, and prodrugs thereof.
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COMPOSITIONS AND METHODS TO CONCURRENTLY TREAT OR PREVENT MULTIPLE DISEASES WITH CUPREDOXINS (Fri, 26 Jun 2009)
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.
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CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 05 Jun 2009)
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, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. Compounds of formula I of the invention are capable of treating and/or preventing the above-identified diseases:
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CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 05 Jun 2009)
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, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis. Compounds of formula I of the invention are capable of treating and/or preventing the above-identified diseases: </p>
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KYNURENINE-AMINOTRANSFERASE INHIBITORS (Sat, 23 May 2009)
Compounds of formula (I) : prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3 -hydroxy kynurenine.
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Biologically active compounds (Fri, 22 May 2009)
<p id="p-0001-en" num="0000">The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilate degradation.</p>
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Novel Compounds and Methods for Their Production (Fri, 08 May 2009)
<p id="p-0001-en" num="0000">The present invention relates to 11-O-desmethylmacbecin 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 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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DESFERRIOXAMINE CONJUGATES, DERIVATIVES AND ANALOGUES (Fri, 08 May 2009)
The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.
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DISPIRO 1,2,4-TRIOXOLANE ANTIMALARIALS (Fri, 08 May 2009)
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 structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the 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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DISPIRO 1,2,4-TRIOXOLANE ANTIMALARIALS (Fri, 08 May 2009)
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 structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the 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. </p>
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9A-SUBSTITUTED AZALIDES FOR THE TREATMENT OF MALARIA (Fri, 24 Apr 2009)
<p id="p-0001-en" num="0000">The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity.</p>
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Antimalarial compounds with flexible side-chains (Fri, 17 Apr 2009)
<p id="p-0001" num="0000">The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of <i>Plasmodium falciparum</i>, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.</p>
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ANTIMALARIAL COMPOUNDS WITH FLEXIBLE SIDE-CHAINS (Fri, 17 Apr 2009)
The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions.
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ANTIMALARIAL COMPOUNDS WITH FLEXIBLE SIDE-CHAINS (Fri, 17 Apr 2009)
The present invention relates to novel compounds that are inhibitors of wild type and mutant dihydrofolate reductase (DHFR) of Plasmodium falciparum, which are useful for the treatment of malaria. It also relates to processes of making and using such compounds. The antimalarial compounds of the present invention have low toxicity to a host infected with the malarial parasite, and are potent when administered in pharmaceutical compositions. </p>
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BISBENZIMIDAZOLES AS ANTIMALARIAL AGENTS (Fri, 10 Apr 2009)
The present invention relates to antimalarial agents. In particular, the present invention relates to the use of bisbenzimidazoles of Formula (I) for the prevention and/or treatment of malaria, wherein n is an integer selected from 0 to 10, and R1 and R2 are each independently selected from hydrogen, halogen, hydroxyl, alkyl, alkoxy, amino, alkylamino, alkylcarbonylamino, alkylcarbonyloxy, formyl, alkylcarbonyl, alkyloxycarbonyl, halocarbonyl, haloalkyl, haloalkoxy, carbamoyl, cyano, nitro, sulfo, or a carboxyl group.
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FURO [3, 2-B] PYRROL DERIVATIVES (Thu, 09 Apr 2009)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R<sp>3</sp> is <i>tert</i>-butylmethyl, <i>sec</i>-butyl or <i>tert</i>-butyl; X is CH or N; and R<sp>4</sp> is optionally substituted C<sb>1-8</sb> alkyl or optionally substituted C<sb>3-8</sb> cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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PHARMACEUTICAL COMPOSITION COMPRISING AZARHODACYANINE COMPOUND AS ACTIVE INGREDIENT (Fri, 20 Mar 2009)
<p id="p-0001-en" num="0000">The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, <i>leishmania, </i>African sleeping sickness, Chagas disease, toxoplasmosis lymphatic filariasis, babesiosis, and coccidiosis, and a novel compound contained therein.</p>
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Inhibitors of cysteine proteases and methods of use thereof (Fri, 20 Mar 2009)
<p id="p-0001" num="0000">The present invention relates to semicarbazone or thiosemicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.</p>
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9-DEOXO-9A-METHYL-9A-AZA-9A-HOMOERYTHROMYCIN A DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MALARIA (Fri, 06 Feb 2009)
The present invention relates to novel 2'-O-substituted 9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity. More particularly, the invention relates to 2'-O-substituted-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A and 2'-O-substituted-3-O-decladinosyl-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity, to the intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof having antimalarial activity.
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Organophosphoric derivatives useful as anti-parasitic agents (Fri, 19 Dec 2008)
<p id="p-0001-en" num="0000">The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C<sub>1-4 </sub>alkoxy, C<sub>1-4 </sub>alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R<sub>1 </sub>is selected from the group consisting of hydrogen, C<sub>1-7 </sub>alkyl, C<sub>3-10 </sub>cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R<sub>2 </sub>is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.</p>
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DUTPase inhibitors (Fri, 19 Dec 2008)
<p id="p-0001-en" num="0000">Deoxyuridine derivatives of the formula (I) where R<sup>1 </sup>is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(═O)—, —CH═CH, —C≡C—, —NR<sup>5</sup>—; R<sup>4 </sup>is hydrogen or various substituents; R<sup>5 </sup>is H, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>alkanoyl; E is Si or C; R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are independently selected from C<sub>1</sub>-C<sub>8 </sub>alkyl, C<sub>2</sub>-C<sub>8 </sub>alkenyl, C<sub>2</sub>-C<sub>8 </sub>alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR<sup>10</sup>—, —C(═O)—; J is —CH<sub>2</sub>—, or when G is CHR<sup>10 </sup>may also be —O— or —NH—; R<sup>10 </sup>is H, F, —CH<sub>3</sub>, —CH<sub>2</sub>NH<sub>2</sub>, —CH<sub>2</sub>OH; —OHR<sup>11 </sup>is H, F, —CH<sub>3</sub>, —CH<sub>2</sub>NH<sub>2</sub>, —CH<sub>2</sub>OH, —CH(OH)CH<sub>3</sub>, CH(NH<sub>3</sub>)CH<sub>3</sub>; or R<sup>10 </sup>and R<sup>11 </sup>together define an olefinic bond, or together form a —CH<sub>2</sub>-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001-en" he="29.13mm" wi="75.86mm" file="US07795270-20100914-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compound and Methods For the Treatment of Cancer and Malaria (Fri, 19 Dec 2008)
<p id="p-0001-en" num="0000">Formula (I): Where R<sup>1 </sup>is an optionally substituted C<sub>3</sub>-C<sub>12 </sub>hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O)<sub>y</sub>R′ group (preferably forming an optionally substituted C<sub>2</sub>-C<sub>5 </sub>acyl group), or a S(O)<sub>x</sub>R′ group, where y is 0 or 1 and x is 0, 1 or 2 and R′ is H or an optionally substituted C<sub>1</sub>-C<sub>12 </sub>alkyl group, or R′ is an optionally substituted C<sub>5</sub>-C<sub>12 </sub>cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R<sup>5</sup>, R<sup>6</sup>, R<sup>7</sup>, R<sup>8</sup>, R<sup>9 </sup>and R<sup>10 </sup>are each independently selected from H, an optionally substituted C<sub>1</sub>-C<sub>12 </sub>hydrocarbyl group, including a C<sub>5</sub>-C<sub>12 </sub>cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R<sup>5 </sup>and R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>or R<sup>9 </sup>and R<sup>10 </sup>together form a keto (C═O) group; R<sup>N </sup>is H, an optionally substituted C<sub>1</sub>-C<sub>12 </sub>hydrocarbyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group, or an optionally substituted heteroaromatic group; A is Formula (II): a Formula (III): group, or a Formula (IV) or Formula (V) group, where Z is N, O or S; R<sup>a </sup>is H, a C<sub>1</sub>-C<sub>12 </sub>optionally substituted hydrocarbyl group or an optionally substituted aromatic group; n is from 0 to 3; and pharmaceutically acceptable salts thereof. Compounds according to the invention are useful in one or more aspects to inhibit farnesyl transferase, or to treat malaria, neoplasia, a hyperproliferative disease state or arthritis, including rheumaroid arthritis or osteoarthritis.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="119.89mm" wi="73.15mm" file="us20080312287a1-20081218-c00001.tif" img-content="chem" img-format="tif"/> </chemistry> </p>
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Dutpase Inhibitors (Fri, 05 Dec 2008)
<p id="p-0001-en" num="0000">Deoxyuridine derivatives of Formula (I′); where A is O, S or CH<sub>2</sub>; B is O, S or CHR<sup>3</sup>; R<sup>1 </sup>is H, or various substituents; R<sup>2 </sup>is H, F; R<sup>3 </sup>is H, F, OH, NH<sub>2</sub>; or R<sup>2 </sup>and R<sup>3 </sup>together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C≡C—, —NR<sup>5</sup>—; R<sup>4 </sup>is hydrogen or various substituents; R<sup>5 </sup>is H, C<sub>1</sub>-C<sub>4 </sub>alkyl, C<sub>1</sub>-C<sub>4 </sub>alkanoyl; E is Si or C; R<sup>6</sup>, R<sup>7 </sup>and R<sup>8 </sup>are independently selected from C<sub>1</sub>-C<sub>8 </sub>alkyl, C<sub>2</sub>-C<sub>8 </sub>alkenyl, C<sub>2</sub>-C<sub>8 </sub>alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="39.88mm" wi="69.93mm" file="US07601702-20091013-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Compositions and methods for treating malaria with cupredoxin and cytochrome (Fri, 28 Nov 2008)
<p id="p-0001" num="0000">The present invention relates to cupredoxin and cytochrome and their use, separately or together, to inhibit the spread of parasitemia in mammalian red blood cells and other tissues infected by the malaria parasite, and in particular the parasitemia of human red blood cells by <i>P. falciparum</i>. The invention provides isolated peptides that are variants, derivatives or structural equivalents of cupredoxins or cytochrome c, and compositions comprising cupredoxins and/or cytochrome c, or variants, derivatives or structural equivalents thereof, that are useful for treating or preventing malaria infection in mammals. Further, the invention provides methods to treat mammalian patients to prevent or inhibit the growth of malarial infection in mammals. The invention also provides methods to prevent the growth of malaria infection in insect vectors.</p>
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Compositions and methods for treating malaria with cupredoxin and cytochrome (Fri, 21 Nov 2008)
<p id="p-0001-en" num="0000">The present invention relates to cupredoxin and cytochrome and their use, separately or together, to inhibit the spread of parasitemia in mammalian red blood cells and other tissues infected by the malaria parasite, and in particular the parasitemia of human red blood cells by <i>P. falciparum</i>. The invention provides isolated peptides that are variants, derivatives or structural equivalents of cupredoxins or cytochrome c, and compositions comprising cupredoxins and/or cytochrome c, or variants, derivatives or structural equivalents thereof, that are useful for treating or preventing malaria infection in mammals. Further, the invention provides methods to treat mammalian patients to prevent or inhibit the growth of malarial infection in mammals. The invention also provides methods to prevent the growth of malaria infection in insect vectors.</p>
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Derivatives of artemisinin, and their uses in the treatment of malaria (Fri, 21 Nov 2008)
<p id="p-0001-en" num="0000">A new artemisinin derivatives, of following general formula (I):</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="40.30mm" wi="40.56mm" file="US07696362-20100413-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p> <p id="p-0003-en" num="0000">In which: <ul id="ul0001-en" list-style="none"><li><ul id="ul0002-en" list-style="none"><li>a and b are a single or a double bond,</li><li>n1 and n2 are 0 or 1,</li><li>R<sub>1 </sub>is a fluoroalkyl group or a fluoroaryl group,</li><li>R<sub>2 </sub>is a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble,</li><li>R<sub>3 </sub>is a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble,</li><li>R<sub>4 </sub>is H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.</li></ul></li></ul></p>
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Pyridinone derivatives against malaria (Fri, 21 Nov 2008)
<p id="p-0001-en" num="0000">4-pyridone derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.</p>
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Anticancer and antiprotozoal dihydroartemisinene and dihydroartemisitene dimers with desirable chemical functionalities (Fri, 07 Nov 2008)
<p id="p-0001-en" num="0000">This invention comprises compositions containing dihydroartemisinin- and dihydroartemisitene-dimers with activity as anticancer or anticancer metastasis agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer or prevention of cancer metastasis, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor or anti-metastasis agents, one that has shown promising activity against solid tumors.</p>
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1, 3, 5-triazepin-2, 6-diones for the treatment of malaria (Thu, 11 Sep 2008)
The present invention relates to various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds, their pharmaceutically acceptable salt derivatives, and their methods of use. In one aspect the present invention relates to compositions and methods for the treatment and prevention of disease in a mammal comprising administering the compounds of the invention in a pharmaceutically acceptable form to a mammal. In particular, the invention relates to medicaments comprising various novel substituted dipeptide derived nitrogen- containing heterocyclic compounds and pharmaceutically acceptable salt derivatives and methods for administration to a mammal for the treatment and prevention of malarial diseases. The compounds of the invention may optionally be administered with at least one pharmaceutically acceptable excipient, another biologically active agent or a combination thereof.
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Heterocyclic compounds (Thu, 11 Sep 2008)
4-pyridone derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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Malaria MSP-1 C-terminal enhanced subunit vaccine (Fri, 05 Sep 2008)
<p id="p-0001-en" num="0000">A vaccine or immunogenic composition is described that contains recombinantly produced, secreted, forms of malaria MSP-1 C-terminal subunit proteins from any of the <i>Plasmodium falciparum </i>strains as active ingredients combined with one or more adjuvants. The immunogenic compositions that result in a protective response are based on the use of a single adjuvant that forms an emulsion or use of such emulsion in combination with a second adjuvant that is an immunomodulating agent. Such a vaccine elicits a strong immune response characterized by antibodies that are capable of inhibiting parasite growth in vitro as well as antibodies that are incapable of inhibiting parasite growth in vitro, but are capable of enhancing the activity of the inhibitory antibodies. The disclosed vaccine formulations are capable of generating a protective response against malaria in vaccinated subjects.</p>
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NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS (Fri, 29 Aug 2008)
The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant Plasmodium falciparum strains and in vivoactivity against P.berghei.
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Quinoline derivatives and uses thereof (Fri, 08 Aug 2008)
<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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Pyridopyrimidinone compounds with antimalarial activity (Fri, 08 Aug 2008)
<p id="p-0001-en" num="0000">The present invention provides pyridopyrimidinone compounds with desirable biological activity and toxicity profiles for the enhanced treatment and prevention of malaria. The invention also relates to methods of making such molecules.</p>
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PURINE COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS FOR THE TREATMENT OF PLASMODIUM RELATED DISEASES (Fri, 08 Aug 2008)
The invention provides a class of purine derivates, pharmaceutical compositions comprising such compounds and the use of such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.
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COMPOUNDS AND COMPOSITIONS AS KINASE INHIBITORS (Fri, 08 Aug 2008)
The invention provides a class of purine derivates, pharmaceutical compositions comprising such compounds and the use of such compounds to treat or prevent diseases or disorders associated with kinase activity, particularly malaria.</p>
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ADENOVIRAL VECTOR-BASED MALARIA VACCINES (Fri, 18 Jul 2008)
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 P. falciparum circumsporozoite protein (CSP) operably linked to a human CMV promoter, and/or (b) a second adenoviral vector comprising a nucleic acid sequence encoding a P. falciparum apical membrane antigen 1 (AMA-1) antigen operably linked to a human CMV promoter.
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ANTI-MALARIAL COMPOUND ISOLATED FROM GOMPHOSTEMMA NIVEUM (Thu, 26 Jun 2008)
The present invention provides a novel antimalarial compound 3-&lsqb;2-(2-Hydroxymethyl- 1, 4a, 5-trimethyl-7-oxo-l,2,3,4,4a, 7 8, 8a-octahydronaphthalen-l-yl)-ethyl&rsqb;-5H-furan- 2-one of the formula (I) given below or pharmaceutically acceptable derivatives thereof, isolated from Gomphostema niveum and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound.
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ODCASE INHIBITORS FOR THE TREATMENT OF MALARIA (Thu, 19 Jun 2008)
The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.
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Dispiro 1,2,4-trioxolane antimalarials (Fri, 30 May 2008)
<p id="p-0001" num="0000">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 structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the 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.</p>
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SPIRO AND DISPIRO 1,2,4-TRIOXOLANE ANTIMALARIALS (Fri, 30 May 2008)
<p id="p-0001-en" num="0000">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, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.</p>
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NOVEL COMPOUNDS AND METHODS FOR THEIR PRODUCTION (Fri, 16 May 2008)
The present invention relates to ansamycin 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 or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.
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18, 21-DIDESOXYMACBECIN DERIVATIVES FOR THE TREATMENT OF CANCER (Fri, 16 May 2008)
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.
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18, 21-DIDESOXYMACBECIN DERIVATIVES FOR THE TREATMENT OF CANCER (Fri, 16 May 2008)
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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NOVEL COMPOUNDS AND METHODS FOR THEIR PRODUCTION (Fri, 16 May 2008)
The present invention relates to ansamycin 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 or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.</p>
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DISPIRO TETRAOXANE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MALARIA AND/OR CANCER (Fri, 04 Apr 2008)
A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=-C(O)NR1R2, -NR1R2 or -S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=-S(O)2R3 or -C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.
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MODIFICATIONS OF CUPREDOXIN DERIVED PEPTIDES AND METHODS OF USE THEREOF (Fri, 21 Mar 2008)
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 cells.
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PHARMACEUTICAL COMPOSITION COMPRISING AZARHODACYANINE COMPOUND AS ACTIVE INGREDIENT (Thu, 06 Mar 2008)
The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, leishmania, African sleeping sickness, Chagas disease, toxoplasmosis lymphatic filariasis, babesiosis, and coccidiosis, and a novel compound contained therein.
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Zinc finger ejectors and methods of use thereof (Fri, 15 Feb 2008)
<p id="p-0001-en" num="0000">Techniques for the chelation or ejection of Zn2+ from zinc finger peptides are disclosed, which can be useful in the treatment or control of viruses and viral diseases and malaria. The invention comprises contacting a zinc finger peptide with an effective amount of a bishydroxamic acid or salt thereof, either in vivo or in vitro. </p>
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ISOFORM-SELECTIVE HDAC INHIBITORS (Fri, 15 Feb 2008)
One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.
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ISOFORM-SELECTIVE HDAC INHIBITORS (Fri, 15 Feb 2008)
One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.</p>
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1,2,4-TRIOXOLANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME (Mon, 11 Feb 2008)

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Heterocyclic compounds (Fri, 25 Jan 2008)
<p id="p-0001-en" num="0000">4-pyridone (4-pyridinone) derivatives of Formula I</p> <p id="p-0002-en" num="0000"> <br/> and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided. </p>
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AIGIALOMYCIN D AND DERIVATIVES THEREOF AND THEIR USE IN TREATING CANCER OR MALARIA OR A MICROBIAL INFECTION (Fri, 25 Jan 2008)
The invention describes a process for making compound (2), comprising the step of cyclising diene (3). Compound (2) may be aigialomycin D or a derivative thereof or may be elaborated to make aigialomycin D or derivative thereof. Furthermore compound (2) or derivative thereof can be used in treating cancer or malaria or a microbial infection.
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TETRAHYDROFURO [3, 2-B] PYRR0L-3-ONES AS CATHEPSIN K INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from H, OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R4 is optionally substituted Ci-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R 6' and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; R8 is C1-8-alkyl or C3-g-cycloalkyl; and k is an integar chosen from 1 or 2. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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FURO[3,2-B]PYRROL-3-ONE DERIVATIVES AND THEIR USE AS CYSTEINYL PROTEINASE INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof: wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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TETRAHYDROFURO (3, 2-B) PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES (Fri, 18 Jan 2008)
Compounds of formula (I) and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget' s disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain. Compounds (I) are cysteine protease inhibitors.
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TETRAHYDROFURO [3, 2 -B] PYRR0L-3-ONES AS CATHEPSIN K INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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FURO [3, 2-B] PYRROL DERIVATIVES (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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FURO [3,2-B] PYRROL-3-ONE DERIVATIVES AND THEIR USE AS CYSTEINYL PROTEINASE INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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FURO [3,2-B] PYRROL-3-ONE DERIVATIVES AND THEIR USE AS CYSTEINYL PROTEINASE INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget' s disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
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TETRAHYDROFURO [3, 2 -B] PYRR0L-3-ONES AS CATHEPSIN K INHIBITORS (Fri, 18 Jan 2008)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is selected from from OR6, SR6, NR6R7, N3, Me, Et, CF3, SOR8 and SO2R8; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl and cyclohexyl; R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl; R6 and R7 are each independently selected from H, C1-8-alkyl and C3-8-cycloalkyl, or R6 and R7 are linked to form a cyclic group together with the nitrogen to which they are attached; and R8 is C1-8-alkyl or C3-8-cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.</p>
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Tumor necrosis factor-gamma (Fri, 28 Dec 2007)
<p id="p-0001-en" num="0000">Human TNF-gamma-alpha and TNF-gamma-beta polypeptides and DNA (RNA) encoding such polypeptides and a procedure for producing such polypeptides by recombinant techniques are disclosed. Also disclosed are methods for utilizing such polypeptides to inhibit cellular growth, for example in a tumor or cancer, for facilitating wound-healing, to provide resistance against infection, induce inflammatory activities, and stimulating the growth of certain cell types to treat diseases, for example restenosis. Also disclosed are diagnostic methods for detecting a mutation in the TNF-gamma-alpha and TNF-gamma-beta nucleic acid sequences or overexpression of the TNF-gamma-alpha and/or TNF-gamma-beta polypeptides. Antagonists against such polypeptides and their use as a therapeutic to treat cachexia, septic shock, cerebral malaria, inflammation, arthritis and graft-rejection are also disclosed.</p>
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Berberine as a selective lung cancer agent (Fri, 28 Dec 2007)
<p id="p-0001-en" 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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DIHYDROOROTATE DEHYDROGENASE INHIBITORS WITH SELECTIVE ANTI-MALARIAL ACTIVITY (Fri, 28 Dec 2007)
Pharmaceutical compositions comprising compounds of the formula (I) where R1, R2, and R3 are described here, have therapeutic utility in selectively inhibiting P. falciparum dihydroorotate dehydrogenase. Accordingly, such compositions have use in the treatment and prevention of malaria.
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Heterocyclic compounds (Fri, 07 Dec 2007)
<p id="p-0001-en" num="0000">3-Chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, having the following formula:</p> <p id="p-0002-en" num="0000"> <br/> is described along with its pharmaceutically acceptable salts, processes for its preparation, pharmaceutical formulations thereof and its uses in treatment of certain parasitic infections such as malaria. </p>
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NOVEL HETEROCYCLIC COMPOUNDS (Fri, 07 Dec 2007)
4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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NOVEL HETEROCYCLIC COMPOUNDS (Fri, 07 Dec 2007)
4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.</p>
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Novel heterocyclic compounds (Thu, 06 Dec 2007)
4-pyridone derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
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17-OXYMACBECIN DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND/OR B-CELL MALIGNANCIES (Fri, 16 Nov 2007)
The present invention relates to 17-oxymacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt thereof, wherein: R1 represents H, OH or OCH3; R2 represents H or CH3 R3 represents H or CONH2 R4 and R5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R6 represents H or OH; and R7 represents H or CH3. 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.
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18,21-DIDESOXYMACBECIN DERIVATIVES FOR THE TREATMENT OF CANCER (Fri, 16 Nov 2007)
The present invention relates to 18,21-didesoxymacbecin 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 and their use in medicine, in particular, in the treatment and/or prophylaxis of cancer or B-cell malignancies. Formula (I) wherein: R1 represents H, OH, OMe; R2 represents H or Me; R3 represents H or CONH2; R4 and R5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); R6 represents H or F; R7 represents H or F; and R8 represents H or F.
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NOVEL COMPOUNDS (Fri, 16 Nov 2007)
The present invention relates to 18,21-didesoxymacbecin 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 and their use in medicine, in particular, in the treatment and/or prophylaxis of cancer or B-cell malignancies. Formula (I) wherein: R1 represents H, OH, OMe; R2 represents H or Me; R3 represents H or CONH2; R4 and R5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); R6 represents H or F; R7 represents H or F; and R8 represents H or F.</p>
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17-OXYMACBECIN DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND/OR B-CELL MALIGNANCIES (Fri, 16 Nov 2007)
The present invention relates to 17-oxymacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt thereof, wherein: R1 represents H, OH or OCH3; R2 represents H or CH3 R3 represents H or CONH2 R4 and R5 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R6 represents H or OH; and R7 represents H or CH3. 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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9A-SUBSTITUTED AZALIDES FOR THE TRATMENT OF MALARIA (Fri, 09 Nov 2007)
The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity.
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Method of screening inhibitors of mevalonate-independent isoprenoid biosynthetic pathway (Wed, 24 Oct 2007)
<p id="p-0001-en" num="0000">The present invention provides the structure of the enzyme 4-diphosphocytidyl-2-C-methylerythritol (CDP-ME) synthase, a member of the cytidyltransferase family of enzymes from <i>Escherichia coli</i>. CDP-ME is a critical intermediate in the mevalonate-independent pathway for isoprenoid biosynthesis in a number of prokaryotic organisms, in algae, in the plastids of plants, and in the malaria parasite. Since vertebrates synthesize isoprenoid precursors using a mevalonate pathway, CDP-ME synthase and other enzymes of the mevalonate-independent pathway for isoprenoid production represent attractive targets for the structure-based design of selective antibacterial, herbicidal, and antimalarial drugs. Accordingly, the present invention provides methods for screening for compounds that inhibit enzymes of the mevalonate-independent pathway and pharmaceutical compositions and antibacterial formulations thereof. Further provided are methods of inhibiting the enzymes of the pathway and bacterial terpenoid synthesis and methods for treating a subject suffering from a bacterial infection.</p>
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15-DESMETHOXYMACBECIN DERIVATIVES FOR THE TREATMENT OF CANCER DISEASES (Fri, 12 Oct 2007)
The present invention relates to 15-desmethoxymacbecin 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 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.
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4, 5-DIHYDROMACBECIN DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER OR B-CELL MALIGNANCIES. (Fri, 12 Oct 2007)
The present invention relates to 4,5-dihydromacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt there of: wherein: R1 represents H or CONH2. 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.
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NOVEL COMPOUNDS AND METHODS FOR THEIR PRODUCTION (Fri, 12 Oct 2007)
The present invention relates to 11-O-desmethylmacbecin 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 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.
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15-O-DESMETHYLMACBECIN DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER OR B-CELL MALIGNANCIES (Fri, 12 Oct 2007)
The present invention relates to 15-0-desmethylmacbecin analogues according to the formula (IA) or (IB) below, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R3 represents H or CONH2 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.
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SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE (Fri, 12 Oct 2007)
The present invention relates to compounds having the general structure: (I) and pharmaceutically acceptable salts and hydrates thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
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SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE (Fri, 12 Oct 2007)
The present invention relates to compounds having the general structure: (I) and pharmaceutically acceptable salts and hydrates thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic ß cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.</p>
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Iron binding agents (Fri, 05 Oct 2007)
<p id="p-0001" num="0000">Composition, article of manufacture for and method of treating malaria in a human having an infestation of <i>Plasmodium </i>protozoans are described. The method comprises administering a therapeutically-effective amount of a compound of formula (I) or (IV), i.e. sufficient quantity to reduce the population of <i>Plasmodium</i>. The composition of the invention is a compound of formula (I) or (IV) with a pharmaceutical excipient. The article of manufacture is the composition in combination with labeling for treating malaria. The substituents are detailed in the specification.</p>
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QUINOLIN-4-YLHYDRAZINE DERIVATIVES AS ANTIMALARIAL AGENT (Fri, 21 Sep 2007)
Novel quinolyl and acridinylhydrazone compounds of formula (I), which present remarkable biological activity especially against the choloroquine-resistant Plasmodium falciparum strains, useful for the treatment and prevention of malaria infection are described herein.
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ANALOGUES OF COFORMYCIN AND THEIR USE FOR TREATING PROTOZOAN PARASITE INFECTIONS (Fri, 31 Aug 2007)
This invention relates to compounds that are analogues of coformycin, pharmaceutical compositions containing the compounds, and methods of using the compounds for treating protozoan parasite infections, especially malaria.
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Antimalarial and antiproliferative pharmacophore models, novel tryptanthrin compounds having increased solubility, and methods of making and using thereof (Wed, 22 Aug 2007)
<p id="p-0001-en" num="0000">Disclosed herein is a pharmacophore model for antimalarial activity and methods of making and using thereof. The pharmacophore comprises two hydrogen bond acceptor (lipid) functions and two hydrophobic (aromatic) functions. The pharmacophore model was made using a test set of tryptanthrin compounds which exhibit antimalarial activity. Also disclosed are tryptanthrin compounds having greater solubility and bioactivity as compared to prior art tryptanthrin compounds and methods of making and using thereof. Also disclosed are methods of treating malaria in a subject.</p>
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Antiparasitic artemisinin derivatives (endoperoxides) (Fri, 17 Aug 2007)
<p id="p-0001-en" num="0000">This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.</p> <p id="p-0002-en" num="0000"/>
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Indazolecarboxamide derivatives for the treatment and prevention of malaria (Fri, 10 Aug 2007)
<p id="p-0001-en" num="0000">The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.</p>
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AZA HETEROCYCLICS FOR THE TREATMENT OF MALARIA OR AIDS (Fri, 06 Jul 2007)
Methods for the synthesis of various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds (I) and their pharmaceutically acceptable salt derivatives are provided. The compounds of the invention are claimed and are useful as medicaments for the treatment or prevention of disease in a mammal, for example a human. In particular the compounds are useful as immuno therapeutics and anti -microbial drugs or vaccines. These heterocyclic derivatives can be used as an active agent in a pharmaceutical, as well as a diagnostic utility.
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21-DEOXYMACBECIN ANALOGUES USEFUL AS ANTITUMOR AGENTS (Fri, 06 Jul 2007)
The present invention relates to 21-deoxymacbecin 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 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.
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21-DEOXYMACBECIN ANALOGUES USEFUL AS ANTITUMOR AGENTS (Fri, 06 Jul 2007)
The present invention relates to 21-deoxymacbecin 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 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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USE OF 1,3,5-TRIAZEPIN-2,6-DIONES TO TREAT MALARIA (Fri, 06 Jul 2007)
The present invention relates to various novel substituted dipeptide derived nitrogen-containing heterocyclic compounds, their pharmaceutically acceptable salt derivatives, and their methods of use. In one aspect the present invention relates to compositions and methods for the treatment and prevention of disease in a mammal comprising administering the compounds of the invention in a pharmaceutically acceptable form to a mammal. In particular, the invention relates to medicaments comprising various novel substituted dipeptide derived nitrogen- containing heterocyclic compounds and pharmaceutically acceptable salt derivatives and methods for administration to a mammal for the treatment and prevention of malarial diseases. The compounds of the invention may optionally be administered with at least one pharmaceutically acceptable excipient, another biologically active agent or a combination thereof. </p>
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ORGANOPHOSPHORIC DERIVATIVES USEFUL AS ANTI-PARASITIC AGENTS (Fri, 29 Jun 2007)
The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1-4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents.
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ORGANOPHOSPHORIC DERIVATIVES USEFUL AS ANTI-PARASITIC AGENTS (Fri, 29 Jun 2007)
The present invention relates to novel phosphonic acid compounds having the structural formula (I): wherein: (a) R is a group of 1 to 5 substituents independently selected from the group consisting of fluoro, chloro, bromo, C1- 4 alkoxy, C1-4 alkyl, hydroxy, formyl, trifluoromethoxy, phenyl, heterocyclic, heterocyclic-substituted methyl, aminomethyl, hydroxy methyl, bromomethyl, sulfonyl chloride, acetyl chloride, nitroso and cyano, (b) R1 is selected from the group consisting of hydrogen, C1-7 alkyl, C3-10 cycloalkyl, aryl, arylalkyl and heterocyclic, and (c) R2 is selected from the group consisting of hydroxy and hydroxy-protecting groups, and stereoisomer, solvates and salts thereof. These compounds are useful as anti-infectious and anti-parasitic agents, in particular anti-malaria agents. </p>
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TRIOXANE DIMERS HAVING HIGH ANTICANCER AND LONG-LASTING ANTIMALARIAL ACTIVITIES (Fri, 15 Jun 2007)
The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions.
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TRIOXANE DIMERS HAVING HIGH ANTICANCER AND LONG-LASTING ANTIMALARIAL ACTIVITIES (Fri, 15 Jun 2007)
The invention provides novel trioxane dimers having formulae III, IV or V: methods for their preparation, pharmaceutical compositions containing these compounds, and methods for treating cancer and/or malaria using these compounds and compositions. </p>
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Dicationic compounds which selectively recognize G-quadruplex DNA (Thu, 07 Jun 2007)
Dicationic compounds that are highly selective for binding G-quadruplex DNA are described. Several compounds exhibit groove binding toward G-quadruplex DNA and in vitro and in vivo activity versus Trypanosoma brucei rhodesiense. The compounds represent novel drugs for the treatment of cancer, malaria, leishmania, and trypanosomiasis.
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ODCASE INHIBITORS FOR THE TREATMENT OF MALARIA (Fri, 13 Apr 2007)
The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.
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ANTI-MALARIAL COMPOUND ISOLATED FROM GOMPHOSTEMA NIVEUM (Fri, 13 Apr 2007)
The present invention provides a novel antimalarial compound 3-[2-(2-Hydroxymethyl- 1, 4a, 5-trimethyl-7-oxo-l,2,3,4,4a, 7 8, 8a-octahydronaphthalen-l-yl)-ethyl]-5H-furan- 2-one of the formula (I) given below or pharmaceutically acceptable derivatives thereof, isolated from Gomphostema niveum and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound.
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ANTI-MALARIAL COMPOUND ISOLATED FROM GOMPHOSTEMMA NIVEUM (Fri, 13 Apr 2007)
The present invention provides a novel antimalarial compound 3-[2-(2- Hydroxymethyl- 1, 4a, 5-trimethyl-7-oxo-l,2,3,4,4a, 7 8, 8a- octahydronaphthalen-l-yl)-ethyl]-5H-furan- 2-one of the formula (I) given below or pharmaceutically acceptable derivatives thereof, isolated from Gomphostema niveum and also provides a method for the extraction thereof as well as methods for the treatment of malaria using said compound. </p>
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ODCASE INHIBITORS FOR THE TREATMENT OF MALARIA (Fri, 13 Apr 2007)
The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The invention also includes new 6-substituted uridine derivatives for use as therapeutics, in particular to treat malaria.</p>
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ADENOVIRAL VECTOR-BASED MALARIA VACCINES (Fri, 09 Mar 2007)
The invention provides adenoviral vectors comprising an adenoviral genome comprising heterologous antigen-encoding nucleic acid sequences, such as Plasmodium nucleic acid sequences, operably linked to promoters. The invention further provides a method of inducing an immune response against malaria in a mammal comprising administering the adenoviral vectors to the mammal.
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BIOLOGICALLY ACTIVE COMPOUNDS (Fri, 02 Mar 2007)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease and diseases involving matrix or cartilage degradation.
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COMPOSITIONS AND METHODS FOR TREATING MALARIA (Fri, 02 Mar 2007)
Polyene macrolide compounds, analogues thereof and compositions containing polyene macrolides or analogues are described for use in treating malaria infections in humans and animals. Examples of polyene macrolide compounds are amphotericin B, nystatin A, natamycin (pimaricin), filipin, rimocidin, candidin and vacidin, and in particular, formulations similar to those described for amphotericin B, such as amphotericin B deoxycholate, amphotericin B colloidal dispersion, amphotericin B lipid complex and liposomal amphotericin B. The polyene macrolide may be produced by a microorganism, by chemically modifying a polyene macrolide or via de novo synthesis. The analogue may be chemically modified to improve solubility, bio-availability and/or bio-activity or limit toxicity. The polyene macrolide or analogue may be administered together with one or more other antimalarial compounds, such as chloroquine, quinine, quinidine, mefloquine, halofantrine, sulfonamides, tetracyclines, atovaquone, artemisinin compounds, rimaquine, proguanil or pyrimethamine, so as to increase the efficacy of the other antimalarial compound.
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Anticancer and antiprotozoal dihydroartemisinin and dihydroartemisitene dimers with desirable chemical functionalities (Thu, 22 Feb 2007)
This invention comprises compositions containing dihydroartemisinin- and dihydroartemisitene- dimers with activity as anticancer or anticancer metastasis agents and anti-protozal, including anti-malarial and anti-leishmanial properties. This invention also describes methods of preparation of these compositions and methods of use of such compositions for the treatment of cancer or prevention of cancer metastasis, and protozoal infections, including malaria, or leishmaniasis. The compounds of this invention represent a potential new class of anti-tumor or anti-metastasis agents, one that has shown promising activity against solid tumors.
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PAPAIN FAMILY CYSTEINE PROTEASE INHIBITORS FOR THE TREATMENT OF PARASITIC DISEASES (Fri, 02 Feb 2007)
The invention relates to the treatment of parasitic disease with inhibitors of the papain family cysteine proteases The parasitic diseases include toxoplasmosis, malaria, African trypanosomiasis, Changas disease, leishmanasis and schistosomiasis The invention also relate to the pharmaceutical compositions comprising a papain family cysteine protease inhibitor and another agent in the treatment for parasitic disease.
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Antiparasitic artemisinin derivatives (endoperoxides) (Fri, 26 Jan 2007)
<p id="p-0001-en" num="0000">This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.</p> <p id="p-0002-en" num="0000"/>
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Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof (Fri, 26 Jan 2007)
<p id="p-0001" num="0000">The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.</p>
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MALARIA MSP-1 C-TERMINAL ENHANCED SUBUNIT VACCINE (Fri, 12 Jan 2007)
A vaccine or immunogenic composition is described that contains recombinantly produced, secreted, forms of malaria MSP-I C-terminal subunit proteins from any of the Plasmodium falciparum strains as active ingredients combined with one or more adjuvants. The immunogenic compositions that result in a protective response are based on the use of a single adjuvant that forms an emulsion or use of such emulsion in combination with a second adjuvant that is an immunomodulating agent. Such a vaccine elicits a strong immune response characterized by antibodies that are capable of inhibiting parasite growth in vitro as well as antibodies that are incapable of inhibiting parasite growth in vitro, but are capable of enhancing the activity of the inhibitory antibodies. The disclosed vaccine formulations are capable of generating a protective response against malaria in vaccinated subjects.
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Antiprotozoal imidazopyridine compounds (Fri, 29 Dec 2006)
<p id="p-0001-en" num="0000">Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).</p> <p id="p-0002-en" num="0000"> <chemistry id="chem-us-00001-en" num="00001"> <img id="emi-c00001" he="87.63mm" wi="60.03mm" file="US07429590-20080930-C00001.TIF" alt="embedded image" img-content="chem" img-format="tif"/> </chemistry> </p>
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Antiparasitic artemisinin derivatives (endoperoxides) (Fri, 22 Dec 2006)
<p id="p-0001-en" num="0000"> This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis. </p>
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COMPOSITIONS AND METHODS FOR TREATING MALARIA WITH CUPREDOXIN AND CYTOCHROME (Fri, 01 Dec 2006)
The present invention relates to cupredoxin and cytochrome and their use, separately or together, to inhibit the spread of parasitemia in mammalian red blood cells and other tissues infected by the malaria parasite, and in particular the parasitemia of human red blood cells by P. falciparum. The invention provides isolated peptides that are variants, derivatives or structural equivalents of cupredoxins or cytochrome c, and compositions comprising cupredoxins and/or cytochrome c, or variants, derivatives or structural equivalents thereof, that are useful for treating or preventing malaria infection in mammals. Further, the invention provides methods to treat mammalian patients to prevent or inhibit the growth of malarial infection in mammals. The invention also provides methods to prevent the growth of malaria infection in insect vectors.
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