Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C6 alkenyloxy, amino, C1-C6 alkylamino, or di-(C1-C6 alkylamino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.

Abstract: Disclosed are once-a-day antibiotic products for treating Methicillin-Resistant Staphylococcus aureus, or “MRSA,” the products comprising: a combination of at least two different antibiotics, wherein one of the at least two different antibiotics is selected from the group consisting of RNA-Polymerase Inhibiting antibiotics and wherein one of the at least two different antibiotics is selected from the group consisting of Elongation Factor G (EF-G) Inhibiting antibiotics (alternatively any or all of the aforementioned RNA-Polymerase Inhibiting antibiotics and Elongation Factor G (EF-G) Inhibiting antibiotics may be in the form of analogues, derivatives, polymorphs, metabolites, pro-drugs, salts, and/or hydrates of any of the foregoing); optionally in further combination with a resistance inhibitor, preferably a LexA protease cleavage inhibitor.

Abstract: A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,

Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl-naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.

Abstract: 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.

Abstract: Anti-infective articles capable of preventing infection associated with implantation of medical devices include low levels of anti-infective agents, may cover only a fraction of the portion of the medical device and be effective, or may rapidly elute anti-infective agent, without sustained elution, and still be effective.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.

Abstract: The invention relates to a compound having general formula (I): Wherein m, R1 and R2 are as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.

Abstract: The present invention is directed to linear, biodegradable polyesteramide (PEA) polymers synthesized with repeating units derived from aminophenol esters and diacids. These PEAs have a monomer repeat represented by as well as a variety of uses to coat, form or comprise medical devices, combination medical devices and pharmaceutical compositions, including sustained release formulations.

Abstract: The present invention provides novel methylenedioxy phenolic compounds and their derivatives, methods of making them and methods of using them to treat or prevent cardiovascular disease, vascular disease and/or inflammatory disease, as well as Type I and Type II Diabetes and Dyslipidemia patients at risk for hypertension, stroke, cardiovascular and renal disease.

Abstract: Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: wherein ? and R1-R8 are described herein, or a compound having the structure: wherein Y, Z, and R21, R24, R25, and R31-R33 are described herein.

Abstract: The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders.

Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.

Abstract: Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress N—CoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death.

Abstract: The present invention is directed to novel 3-(substituted ethyl) rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.

Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

Abstract: The invention relates to methods of treating neurological disorders in a subject, by activating a DISC1 pathway. Methods of promoting neurogenesis in adult neural progenitor cells, enhancing nerve generation and treating GSK3 disorders as well as related compositions are also provided.

Abstract: Disclosed are once-a-day antibiotic products for treating Methicillin-Resistant Staphylococcus aureus, or “MRSA,” the products comprising: a combination of at least three different antibiotics, wherein one of the at least three different antibiotics is selected from the group consisting of RNA-Polymerase Inhibiting antibiotics or Phenazine antibiotics, wherein one of the at least three different antibiotics is selected from the group consisting of Dihydropteroate Synthase Inhibiting antibiotics, and wherein one of the at least three different antibiotics is selected from the group consisting of Dihydrofolate Reductase Inhibiting antibiotics (alternatively any or all of the aforementioned RNA-Polymerase Inhibiting antibiotics, Dihydropteroate Synthase Inhibiting antibiotics, and Dihydrofolate Reductase Inhibiting antibiotics may be in the form of analogues, derivatives, polymorphs, metabolites, pro-drugs, salts, and/or hydrates of any of the foregoing); optionally in further combination with a resistance inhib

Abstract: Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.

Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.

Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a): X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.

Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.

Abstract: Methods for treating neurological or mental disorders in humans and the symptoms associated therewith are provided by administering eltoprazine and/or related compounds. In some embodiments, specific symptoms are treated by administering eltoprazine and/or a related compound in an effective amount to ameliorate the symptoms. Of particular significance are symptoms that are associated with cognitive dysfunction where eltoprazine will improve the symptoms and the disorder associated with that symptom. Of particular interest are non-ADHD-associated inattention, hyperactivity and impulsiveness. The methods provided herein are especially useful for improving functional recovery after CNS injury such as stroke where improved cognitive function will facilitate the acquisition of learning and memory of rehabilitative tasks.

Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.

Abstract: The present invention relates to a method for alleviation, prevention, and treatment of attention deficit disorder, anxiety, depression, sexual dysfunction, aggressive behavior, alcohol dependency, psychoses, and related conditions by administering adatanserin and/or metabolites of adatanserin. The present invention also relates to a method of weight loss by administering adatanserin and/or metabolites of adatanserin.

Abstract: Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin reuptake inhibitor.

Abstract: The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R2 represents general formula (A) or the like, wherein R3 represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.

Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.

Abstract: An in vitro method is provided for identifying nuclear receptors abnormally expressed by brain tumor stem cells and a corresponding ligand which, if administered to brain tumor stem cells (BTSC's), is capable of inhibiting cell proliferation. Once the nuclear receptor/ligand combination has been identified, it can be utilized in vitro and in vivo to inhibit the proliferation and survival of the cancerous stem cells and ultimately affect proliferation and survival of tumors. The method can be utilized alone or in combination with other treatment methods. The method can also be utilized with regard to other forms of cancer which have cancerous stem cells associated therewith and which abnormally express one or more nuclear receptors.

Abstract: This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders incl. schizophrenia.

Abstract: 3-cyanonaphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors, pharmaceutical compositions containing such compounds, methods of using such compounds for the treatment and/or inhibition of various diseases and disorders, processes for preparing such piperazine compounds, and intermediate products of these processes.

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: A method for preventing or reducing boar taint, a method of screening pigs to determine those more likely to have reduced boar taint and a method for screening substances that enhance skatole metabolism or androstenone in a pig, are disclosed These methods involve the use of the nuclear receptors constitutive androstane receptor, pregnane X receptor and farnesoid X receptor, which have been found to modulate the activity of the enzymes involved in skatole and/or androsterone metabolism

Abstract: An isoxazole derivative is provided. The isoxazole derivative has following formula: wherein R1, R2, R3, R4 and R5, independently, include hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis and cancer including an isoxazole derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: An isoflavone derivative is provided. The isoxazole derivative has following formula: wherein R1 and R2, independently, include C1-C12 alkyl optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy, and R3 includes hydrogen, hydroxy or C1-C12 alkoxy optionally substituted with oxirane, thiirane, aziridine, amino, cycloamino, aminohydroxy or cycloaminohydroxy. The invention also provides a pharmaceutical composition for treatment of osteoporosis including an isoflavone derivative or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Abstract: The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.

Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.

Abstract: The present invention relates to a method of forming shape-retentive and shape-conforming aggregate wound dressings and biomaterials composed of gel nanoparticles and wound or bodily fluid in which the aggregates are held together by non-covalent bond physical forces such as, without limitation, hydrophobic-hydrophilic interactions and hydrogen bonds. The method comprises introducing a dry powder of gel nanoparticles to a wound site in which the nanoparticles absorb some of the blood or wound exudate and coalesce in situ into the claimed shape-retentive aggregate dressing. The method also comprises introducing the dry nanoparticle powder in or on a wet bodily tissue in vivo to form the claimed shape-retentive biomaterial. In addition, the method also comprises incorporating biomedical agents to produce medicated aggregate dressings or biomaterials for a variety of medical applications. This invention also relates to uses of the method of formation of the shape-retentive aggregates of gel nanoparticles.

Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.

Abstract: The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject having, or predisposed to, one or more of the conditions, a therapeutically effective amount of a compound of the present invention and a pharmaceutically acceptable carrier.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.

Abstract: A therapeutic agent for administration to a bacterium or to the environment thereof which agent comprises synergistically effective amounts of (i) an RNA polymerase inhibitor and (ii) an ALS enzyme inhibitor.

Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.

Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.

Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.

Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.