Abstract: The present invention provides methods and compositions for promoting healing of damaged tissue that result in an increased level of nitric oxide in the vicinity of the damaged tissue. Also provided are methods and compositions for inhibiting unwanted wound healing by inhibiting the activity of nitric oxide in the tissue.

Abstract: This invention relates to the stabilization of o/w microemulsions containing an active aza biocide by addition of an alkaline, water soluble buffering agent in an amount sufficient to adjust the pH to between 6 and 14 and to the use of said o/w microemulsions to control infestations and/or infections when topically applied to livestock or domestic animals.

Abstract: Methods for treating, preventing or inhibiting leishmaniasis in a subject comprising administering to the subject a therapeutically effective amount of at least one compound having the structural formula wherein Y is a heteroatom; R1 and R2 are independently H or an alkyl, cycloalkyl, heterocycloalkyl, aryl, amino or heteroaryl group; and X1, X2, and X3 are independently H or an alkyl, alkoxy, halo, amino, alkylamino, dialkylamino, acylamino, alkylthio, sulfonyl, cyano, carboxy, alkoxycarbonyl, or carbamoyl group are disclosed.

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 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: The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) a benzimidazole or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.

Abstract: Pentamidine, an anti-protozoa drug, is described herein as a potent PTPase inhibitor with anti-cancer activity. Pentamidine at its therapeutic doses inhibits recombinant PRL phosphatases and inactivates intracellular PRLs in NIH3T3 transfectants. Pentamidine treatment at a nontoxic dose markedly inhibits the growth of WM9 human melanoma tumors in nude mice coincident with tumor cell necrosis and is capable of inactivating an ectopically expressed PRL-2 in the cancer cells. The drug has growth inhibitory activity against different human cancer cell lines that express the PRLs, and therefore has broad anti-cancer activity based on inactivating the oncogenic phosphatases.

Abstract: Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer soluble in the liquefied hydrofluoroalkane which is selected from polymers including recurring amide containing structural units, copolymers of amide containing units and carboxylic acid ester units, polyvinylacetate and acrylic acid/methacrylic acid ester copolymers.

Abstract: Desoxypeganine and its pharmaceutically acceptable acid addition salts can be used in the treatment of alcoholism. Said substances are administered preferably in a continuos and controlled manner. The pharmaceutical administration form enables controlled release, e.g. for oral, transdermal or another route of parenteral administration.

Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.

Abstract: Desoxypeganine and its pharmaceutically acceptable acid addition salts can be used in the treatment of drug addiction or drug dependence. Said substances are administered preferably in a continuos and controlled manner. The pharmaceutical administration form enables controlled release, e.g. for oral transdermal or another route of parenteral administration.

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 multiple doses of 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 multiple doses of at least one inhibitor (one or more) of NO, such as an inhibitor of NOS.

Abstract: The present invention contains halogenated 2-amino-3,4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

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 relates to a method of inhibiting carcinoma progression wherein matriptase plays a role in a subject in need of such inhibition including administering to a subject an effective amount of a compound comprising two positively charged groups, which are the same or different. The groups are linked by a chemical group having a length of between 5 and 30 A, and preferably between 15 and 24 A. Diagnostic methods based on matriptase action and therapeutic methods involving inhibition of matriptase activity are provided.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention is directed to the use of compounds of Formula (I), as active principals for treating skin conditions and compositions containing these compounds wherein R4 is (CR5R6-CR7R81-X1)n-CR9R10R11; n is an integer from 1 to 18; R1, R2, R3, R5, R6, R7, R8, R9, R10 and R11, are independently, herein defined and X, X1, Y and Z are independently, 0, NH or S.

Abstract: The invention provides compounds that inhibit epoxide hydrolase in therapeutic applications for treating hypertension. A preferred class of compounds for practicing the invention have the structure shown by Formula I wherein Z is oxygen or sulfur, W is carbon phosphorous or sulfur, X and Y is each independently nitrogen, oxygen, or sulfur, and X can further be carbon, at least one of R1-R4 is hydrogen, R2 is hydrogen when X is nitrogen but is not present when X is sulfur or oxygen, R4 is hydrogen when Y is nitrogen but is not present when Y is sulfur or oxygen, R1 and R3 is each independently C1-C20 substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, or heterocyclic.

Abstract: The present invention provides a composition comprising synergistic amounts of a compound of the formula (I) 1

Abstract: Cosmetic composition for use in personal care applications comprising a carrier and a polymeric biguanide, characterised in that the polymeric biguanide is in the form of its salt with an organic acid containing from 4 to 30 carbon atoms.

Abstract: Compounds of 1-(adamantyl) amidine and their use in the treatment of conditions generally associated with abnormalities in glutamatergic transmittion.

Abstract: Terminally-branched polymeric prodrug platforms capable of high degrees of loading are disclosed. In preferred aspects of the invention, the prodrug platform releases multiple parent compounds after each branch holding the active agent undergoes a benzyl elimination reaction. Methods of preparing the prodrugs and using the same in the treatment of mammals are also disclosed.

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 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: The invention provides fungicidal compounds of formula I and salts thereof: 1

Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: The invention relates to a device and method for the treatment of Alzheimer's dementia with desoxypeganine and/or a pharmaceutically acceptable acid addition salt of desoxypeganine.

Abstract: The present invention is directed to polymeric-prodrug transport forms of the formula: 1 2

Abstract: The current invention provide novel retinoid compounds and methods for their synthesis, methods of treating or preventing emphysema, cancer and dermatological disorders and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

Abstract: Pharmaceutical preparations containing of agmatine, congeners, analogs or derivatives thereof for use in preventing or treating epilepsy, seizures and other electroconvulsive disorders are provided. Embodiments include administering an effective amount of agmatine, an agmatine analog or a pharmaceutically acceptable salt thereof to a human subject in need of treatment or prevention of epilepsy, seizure or other electroconvulsive disorder to treat, reduce, or prevent the disorder in the subject.

Abstract: The present invention relates to compositions and methods for promoting tissue regeneration, preferably neural tissue regeneration. Compositions of the invention include (i) certain diphenyl sulfides, diphenyl sulfoxides, diphenyl sulfones, and sulfide, sulfoxide and sulfones of dibenzothiophene and thioxanthene, as well as various analogues and derivatives of these compounds; (ii) one or more cells harvested from an animal or organism subsequent to the administration of a composition comprising a compound of (i); or (iii) any combination of (i) and (ii). The invention can be useful in treating decreases in neuronal function, for example from injury or disease.

Abstract: Novel compounds of the formula I in which X, R1, R2, R3, R4 and R5 have the meaning indicated in Patent Claim 1, are inhibitors of the coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

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 the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated blood-coagulation factor X, and they are useful as agents for preventing or treating various diseases caused by thrombi or emboli.

Abstract: The present invention is directed to the use of compounds of Formula (I), as active principals for treating skin conditions and compositions containing these compounds; wherein R4 is (CR5R6—CR7R8—X1)n—CR9R10R11, n is an integer from 1 to 18; R1, R2, R3, R5, R6, R7, R8, R9, R10 and R11, are independently, hydrogen or non-hydrogen substituents; and X, X1, Y and Z are independently NH.

Abstract: Compounds represented by formula I: or a pharmaceutically acceptable salt or hydrate thereof, are disclosed. Pharmaceutical compositions and methods of treatment are also included.

Abstract: The present invention provides novel amidine compounds and novel pesticides containing these amidine compounds as active ingredients.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: 1

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing compounds, of formula (I), wherein wherein x is —NH—NH—CH2R1 and R1 denotes C8 to C20 alkyl.

Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the indexes have the meanings given in the specification, their salts, their preparation and their use.

Abstract: The compound of the above formula wherein R1-R5 are independently selected from hydrogen, alkyl and aryl and prodrugs thereof; and pharmaceutically acceptable salts thereof; and use of the compounds in therapy, particularly for treatment of a condition generally associated with abnormalities in glutamtergic transmission.

Abstract: This invention relates to a single phase emulsifiable concentrate composition comprising (a) between about 0.05 and about 25 wt. % of a biologically, fungicidally and/or herbicidally active aza compound; (b) between about 2 and about 40 wt. % of a lactam selected from the group of N-methyl pyrrolidone, N-methyl caprolactam, a C8 to C18 alkyl pyrrolidone, a C8 to C18 caprolactam and a mixture thereof; (c) between about 2 and about 20 wt. % of a moisture scavenging agent selected from the group consisting of a liquid molecularly hindered carbodiimide, a molecular sieve or a mixture thereof and (d) between about 10 and about 80 wt. % of a mixture of at least two non-ionic surfactants having an overall hydrophilic/lipophilic balance (HLB) above 7. The invention also relates to the stable oil-in-water (o/w) miniemulsions prepared from the above by dilution to between about 40 and about 99.99 wt. % water for a “pour on”, dip or spray solution useful in the treatment of animals or plants.

Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.

Abstract: A method for controlling ectoparasites systemically through host animal blood which comprises administering at least one neonocotinoid compound among those defined in the specification to the host animal.

Abstract: Provided is a pharmaceutical composition comprising a tablet or capsule containing a pharmacologically effective amount of a pharmaceutical compound, or a pharmaceutically acceptable salt thereof, having an amidine-based group and an optional ester group, a pharmaceutically acceptable solid carrier, and a pharmaceutically acceptable acid in an amount to modify the pH of the composition to substantially that of the compound at pH of maximum stability.Such a composition is prepared by adding water during formulation manufacture and contacting the compound during formulation manufacture with a pharmaceutically acceptable acid having a pH in a saturated aqueous solution substantially that of the compound at pH of maximum stability.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: The present invention relates to the use of creatine compounds including cyclocreatine and creatine phosphate for treating or preventing a metabolic disorder consisting of hyperglycemia, insulin dependent diabetes mellitus, impaired glucose tolerance, hyperinsulinemia, insulin insensitivity, diabetes related diseases in a patient experiencing said disorder. The creatine compounds which can be used in the present method include (1) analogues of creatine which can act as substrates or substrate analogues for the enzyme creatine kinase; (2) compounds which can act as activators or inhibitors of creatine kinase; (3) compounds which can modulate the creatine transporter (4) N-phosphocreatine analogues bearing transferable or non-transferable moieties which mimic the N-phosphoryl group. (5) compounds which modify the association of creatine kinase with other cellular components.

Abstract: The present application describes 6-membered aromatics of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein D may be CH.sub.2 NH.sub.2 or C(.dbd.NH)NH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or R