Abstract: The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same.

Abstract: The invention relates to insecticide mixtures comprising thiodicarb and at least one other known active ingredient from the category of chloronicotinyls, as well as the use of these mixtures to control animal pests.

Abstract: The invention is dietary supplements, nutraceutical compositions, medical foods, and animal feeds that have cytoprotective (cell and tissue protection) and health promoting effects. The compositions contain a high dose range of agmatine and nutraceutical acceptable salts thereof as dietary fortification for providing effective long-term cytoprotection and affording for soft stool. The compositions may contain agmatine alone or in combination with other dietary ingredients having health promoting effects. The compositions can be prepared with dietary accepted excipients and compatible forms of carriers, including but not limited to, powders, tablets, capsules, controlled release carriers, lozenges and chewable preparations, liquid suspensions, suspensions in an edible supporting matrix or foodstuff and oral rehydration solutions, to enable consumption of said compositions.

Abstract: The present invention relates to the use, as active ingredient, of a 1-N-(halo-3-pyridylmethyl)-N-methylamino-1-alkylamino-2-nitroethylene derivative for preparing a veterinary pharmaceutical composition for topical use in the treatment of external parasites, in particular fleas, in domestic animals, in particular in dogs and cats, intended to be applied at least every 2 weeks.

Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.

Abstract: Methods are provided herein for treatment of myotonic dystrophy and other toxic RNA diseases in a subject. In some examples, the method comprises administration of a compound that binds a nucleotide repeat expansion in a ribonucleic acid molecule, thereby treating the disease. In additional examples, the method comprises administration of a compound that disrupts binding of muscleblind-like proteins to an RNA nucleotide repeat expansion. Compounds for use in the disclosed method include pentamidine or heptamidine or derivatives thereof. Representative compounds are described herein.

Abstract: This invention relates to new chemical compounds, application of these compounds as anticoagulants, pharmaceutical compositions, and plasma-substituting solutions on their basis, and can be used for treating thromboembolic complications of diseases such as myocardial infarction, stroke, and thrombosis of deep veins or a pulmonary artery; and for preventing hypercoagulation conditions in consequence of injuries, surgeries, sepsis, various obstetric pathologies, in disaster medicine, resuscitation, and so on.

Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to fluoroalkylphenylamidines of the general formula (I), to a process for their preparation, to the use of the amidines according to the invention for controlling unwanted microorganisms and also to a composition for this purpose, comprising the phenoxyamidines according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms by applying the compounds according to the invention to the microorganisms and/or their habitat.

Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.

Abstract: The invention concerns the use of guanabenz and its derivatives for making drugs for treating cystic fibrosis and diseases related to a protein addressing deficiency in the cells, said derivatives corresponding to formula (I), wherein: R?H or C1 and the phenyl group comprises two substituents, or a pharmaceutically acceptable salt of said derivatives.

Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.

Abstract: The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.

Abstract: This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prophylaxis and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isoproply-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1 as a pharmaceutical composition for the prophylaxis and treatment of osteoporosis.

Abstract: A method of treating osteoporosis comprising administering to a subject a composition comprising a compound, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or a salt thereof, is described. A method of inhibiting osteoclast activity and stimulating osteoblast activity in a subject also is described.

Abstract: Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).

Abstract: The present invention relates, in part, to methods of treatment, prevention, and inhibition of viral disorders. In one aspect, the present invention relates to inhibition of the M2 proton channel of influenza viruses (e.g. influenza A virus) and other similar viroporins (e.g., VP24 of Ebola and Marburg viruses; and NS3 protein of Bluetongue). The present invention further relates, inter alia, to compounds which have been shown to possess antiviral activity, in particular, inhibiting the M2 proton channel of influenza viruses.

Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g.

Abstract: The present invention relates to methods for treating uterine hypercontractility disorders. In particular, the present invention relates to methods for treating abnormal uterine bleeding and dysmenorrhea comprising administering to women suffering from such disorders a pharmaceutical composition comprising an S-alkylisothiouronium derivative.

Abstract: A remote treatment delivery system comprising a substantially non-skin piercing dosage projectile containing a biologically active agent and a transdermal carrier.

Abstract: There is a topical composition having carnitine creatinate and a cosmetically acceptable vehicle. There is also provided a method for improving the aesthetic appearance of skin. There is also provided a method for inhibiting the induced lipid synthesis in skin. There is also provided a method for inhibiting the formation of cellulite in skin.

Abstract: The present invention provides a class of chemical compounds useful in the treatment of sickle cell disease, diseases characterized by unwanted or abnormal cell proliferation and for the treatment of ocular disorders such as glaucoma. The active compounds are tri-(aryl or heteroaryl) methane compounds or analogues thereof which further comprise an imine moiety and where the tertiary carbon atom can be replaced with a different atom such as Si, Ge, N or P. The compounds enhance resistance to degradation in a biological medium, inhibit potassium flux in a cell, reduce mammalian cell proliferation, reduce the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Abstract: A new class of fluorinated or polyhalogenated triazapentadienes are disclosed. The synthesized triazapentadienes are thermally stable, soluble in typical solvents and have several metal binding sites for complexation with metal ions. The compounds are prepared as colorless crystalline solids. Synthesis takes advantage of a reaction with triethylamine. Synthesized triazapentadienes (with and without complexed metals) inhibit bacterial growth of both Gram positive and Gram-negative bacteria.

Abstract: This invention relates to a pharmaceutical composition containing 4-[(4-thiazolyl)phenoxyl]alkoxy-benzamidine derivatives expressed by the following formula 1 for the prevention and treatment of osteoporosis and more particularly, to the use of 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine or N-hydroxy-4-{5-[4-(5-iso-propyl-2-methyl-1,3-thiazol-4-yl)phenoxyl]pentoxy}-benzamidine expressed by the following formula 1, which is known as an antagonist of leukotriene-B4 receptor, as a pharmaceutical composition for the prevention and treatment of osteoporosis. [Formula 1], wherein, R is a hydrogen atom or a hydroxy group.

Abstract: The instant invention is directed towards compounds, including diamidines, that inhibit Tdp1 and are useful in the treatment and/or prevention of cancer and parasitic disease.

Abstract: An antimicrobial composition suitable for cleaning inanimate surfaces and human skin comprises two or more cationic biocides and two or more biocides which are slower acting than the cationic biocides, wherein each cationic biocide is independently either: (i) a quaternary ammonium compound at a concentration of at least 0.1% w/v; or (ii) a biguanide compound.

Abstract: The present invention relates to the use of S-alkylisothiouronium derivatives, including S-ethylisothiouronium diethylphosphate, for stabilizing blood pressure in hemodialysis patients. The compositions of the invention are effective in preventing hypotension in hemodialysis patients.

Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.

Abstract: The present invention relates to nitric oxide-releasing amidine diazeniundiolates, compositions comprising same, methods of using same, and a method for preparing same from imidate diazeniumdiolates and primary or secondary amines.

Abstract: Methods of detaching microorganisms (e.g., bacteria) from, or of inhibiting microbial (e.g., bacterial) attachment to, animal or poultry carcasses or seafood or parts thereof, wherein the method involves contacting animal or poultry carcasses or seafood or parts thereof at least once with at least one of the following: (i) a polysulfated polysaccharide, (ii) carboxymethyl cellulose, or (iii) guanidine or arginine, optionally together with sodium chloride and at least one non-ionic surfactant, or (iv) mixtures thereof, in an amount effective to detach microorganisms (e.g., bacteria) from, or inhibit microbial (e.g., bacterial) attachment to, animal or poultry carcasses or seafood or parts thereof.

Abstract: A compound of formula (I): namely (2S)-2-amino-4-{[2-(ethanimidoylamino)ethyl]thio}butanoic acid, compound with phosphoric acid, or a solvate or physiologically functional derivative thereof, is useful as a relatively non-hygroscopic selective inhibitor of inducible nitric oxide synthase.

Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer's disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.

Abstract: A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.

Abstract: Personal care composition, comprising a first ingredient selected from the group consisting of ?-phenyl butyl nitrone (PBN), PBN doxylcyclohexane radicals, 5,5-dimethyl pyrroline N-oxide (DMPO), ?-(4-pyridyl 1-oxide)-N-tert-butylnitrone (POBN), 2,2,6,6-tetramethylpiperidine 1-oxide, 4-hydroxytetramethylpiperidine 1-oxide, and the salts of N-(1-oxido-2,2,6,6-tetramethyl-4-piperidyl)-N,N-dimethyl-N-hydroxyethylammonium, 3,5-dibromo-4-nitrosobenzenesulfonic acid, 2-methyl-2-nitrosopropane, nitrosodisulfonic acid, ?-(4-pyridyl-1-oxide)-N-t-butylnitrone, 3,3,5,5-tetramethylpyrroline N-oxide, and 2,4,6-tri-t-butylnitrosobenzene, spin-trapping derivatives thereof, and mixtures thereof, a second ingredient selected from the group consisting of particulate materials, panthenol, pantothenic acid derivatives, tanning actives, and mixtures thereof; and a dermatologically acceptable carrier.

Abstract: Transport reagents and conjugates of therapeutic agents linked to transport reagents are described. In particular, the transport reagents have a plurality of guanidinium moieties that are either contiguous or spaced along a backbone, but are sufficiently removed from the backbone via tethers, to allow their interaction with a cell or tissue surface, leading to uptake of the therapeutic agent.

Abstract: The invention describes compounds represented by the general formula (I) given below: in which: n is an integer between 1 and 4; R1 and R2 are chosen independently from hydrogen and a methyl group; R3 is chosen independently from a linear, branched or cyclic alkyl group containing from 1 to 3 carbon atoms (R3a) and a simple amino group (R3b) or an amino group substituted with a nitro group (R3c) The compounds are useful for treating central nervous system diseases or peripheral neuropathies.

Abstract: A method of treating pain in a warm-blooded animal comprising administering to anwarm-blooded animal in need thereof an amount of a compound of the formula wherein the substituents are defined in accordance with the disclosure.

Abstract: The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), X= R3= Y= Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl. Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R?=H or O(?) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addition and obesity based thereon.

Abstract: This invention relates to a novel class of partial or full muscarinic receptor agonists intermediates for their preparation, and pharmaceutical compositions and methods of use for the treatment or prevention of diseases the treatment or prevention of which is mediated by muscarinic receptor agonism.

Abstract: The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.

Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.

Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis, differentiation and maturation in hematopoietic tissue, wherein the hematopoietic tissue is contacted with at least one inhibitor of NO, such as one or more inhibitors of nitric oxide synthase (NOS), thereby producing hematopoietic tissue having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis, differentiation and maturation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor (one or more) of NO, such as an inhibitor of NOS.

Abstract: Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: 1

Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells in bone marrow which are capable of undergoing normal hematopoiesis and differentiation, wherein the bone marrow is contacted with an inhibitor of NO, such as an inhibitor of nitric oxide synthase (NOS), thereby producing bone marrow having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis and differentiation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor of NO, such as an inhibitor of NOS. The invention also pertains to a method of regenerating tissue in an adult mammal comprising contacting a selected tissue (e.g.

Abstract: The invention relates to new derivatives of 2-(iminomethyl)amino-phenyl which are NO synthase inhibitors and can trap reactive oxygen species. These compounds can notably be used for the treatment of stroke, of neurodegenerative diseases and of ischemic or hemorragic cardiac or cerebral infarctions.

Abstract: Disclosed are compounds having the formula: where R1=H, C1-C6 alkyl, cycloalkyl, R2=H, C1-C6 alkyl, cycloalkyl W=CnH2n-m—NH (n=1-6, m=0, 2, or 4), Z=CONR8(CH2)n, CONR8(CH2)nCO, P(CH3)OCHR8OCOR9, SO2, SO2(CH2)n, SO2(CH2)nCO, SO2NR8(CH2)n, SO2NR8(CH2)nCO, n=1-4 R4=H, (CH2)nOH, (CH2)nOCOR10, (CH2)nNR10R11, (CH2)nCONR10R11, n=0-4 R5=H, (CH2)nNR12R13, n=0-4 R6=H, (CH2)nNR14R15, n=0-4 R7=H, C1-C6 alkyl, cycloalkyl; R8=H, C1-C6 alkyl, cycloalkyl; R9=H, C1-C6 alkyl, cycloalkyl; R10=H, C1-C6 alkyl, cycloalkyl; R11=H, C1-C6 alkyl, cycloalkyl; R12=H, C1-C6 alkyl, cycloalkyl; R13=H, C1-C6 alkyl, cycloalkyl; R14=H, C1-C6 alkyl, cycloalkyl; R15=H, C1-C6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH2)n, n=1-3, R′=H or O(═) as well as pharmaceuticals c

Abstract: This invention relates to a biocidal composition resistant to the formation of a gel and to the method for stabilizing a concentrate containing, in addition to the biocide, a carbodiimide, a lipophilic/hydrophilic emulsifier mixture having a HLB of 6 to 20 and optionally an oil and/or an alkoxylated ester of a polyhydroxylated compound, by adding to the concentrate an effective anti-gelling amount of an anti-gelling agent selected from the group of an inorganic oxide, a epoxidized naturally occurring or synthetic vegetable oil and an epoxylated ester of a saturated or unsaturated C6 to C18 aliphatic acid optionally containing hydroxy substitution and mixtures of the foregoing anti-gelling agents.

Abstract: The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.

Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.