Abstract: The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: that includes preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof:

Abstract: A composition of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of the compound, and a diagnostically acceptable carrier. A method for detecting malignant tumors, by administering a tumor detecting effective amount to a host in need of tumor detection of a compound or derivative thereof in which at least one carbon atom of 5-aminolevulinic acid is a carbon isotope and/or a nitrogen atom in its amino group is a nitrogen isotope, and where said derivative is an ester, amide, salt, hydrate or solvate of said compound and detecting the malignant tumors using NMR.

Abstract: An antitumor combination comprising a stilbene derivative and an anticancer compound selected from the group consisting of taxanes, alkylating agents, antimetabolites, vinca alkaloids, platinum compounds, epidophylloptoxins, and antibiotics as the active ingredients is provided. Methods of using these pharmaceutical preparations for the treatment of solid carcinomas and the like are also provided.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: The invention to a pharmaceutical composition comprising as active principle a compound of general formula (I), in which R1, R2, R3, and A are as defined in claim 1. These compositions can be used in the treatment of pathologies associated with insulin resistance syndrome.

Abstract: With an agent for preparing a medication for treating the symptoms of Parkinson's disease, one obtains more effective treatment of the symptoms of said disease compared to classical treatment by a combination of effective substances comprising a substance increasing dopamine concentration in the synaptic cleft of the neurons of the brain along with a local anesthetic of the anilide group.

Abstract: Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).

Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.

Abstract: The present invention provides a virucide composition and/or sporicide composition having a high virucidal effect and sporicidal effect and being excellent in safety and workability. That is, the present invention provides a virucide composition and/or sporicide composition comprising (a) an inorganic peroxide, (b) tetraacetylethylenediamine and (c) at least one selected from a salt of an alkaline metal salt with an inorganic acid and a salt of an alkaline earth metal with an inorganic acid in a specific ratio.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: An antitumor combination containing a stilbene derivative and an anticancer compound chosen from taxanes, alkylating agents, antimetabolites, vinca alkaloids, epidophylloptoxins, and antibiotics as the active ingredients is provided. There are also provided methods of using these pharmaceutical preparations for the treatment of solid carcinomas and the like.

Abstract: Disclosed is a method of selecting analgesic agents based on their selective ability to block tetrodotoxin-insensitive sodium channels, particularly in comparison to blocking tetrodotoxin-sensitive sodium channels. Also disclosed is a novel class of compounds that is selective for blocking tetrodotoxin-insensitive sodium channels.

Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.

Abstract: The present invention thus provides compounds of Formula I: 1

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

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates beta-amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.

Abstract: The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

Abstract: A method of treating cells that carry at least one APOE4 allele comprises increasing nitric oxide levels in the cells (e.g., by administering an exogenous source of nitric oxide to the cells) by an amount sufficient to combat the decrease of nitric oxide level associated with the presence of the APOE4 allele. Also disclosed is a method of increasing nitric oxide levels in cells in need thereof which comprises administering APOE to the cells in an amount sufficient to increase nitric oxide levels in the cells.

Abstract: A local anesthetic for external use is prepared by blending a) an active ingredient selected from lidocaine, prilocaine, and pharmaceutically acceptable salts thereof; b) a percutaneous absorption accelerator, c) ethanol and/or isopropyl alcohol, and d) water, such that the blending ratio of ethanol and/or isopropyl alcohol to water is 0.5 to 1.2 by weight, and the pH is 6.0 to 8.5.

Abstract: The use of HETE derivatives in intraocular surgery (e.g., cataract surgery) is disclosed. The HETE derivatives protect and maintain the corneal endothelium.

Abstract: A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general surgical, therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents, including at least one local anesthetic agent, and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents.

Abstract: The use of HETE derivatives to treat dry eye conditions associated with refractive surgery is disclosed.

Abstract: The invention provides methods which are useful for treating diseases (e.g., cancer) where PKC&dgr; is implicated, and modulation (e.g, inhibition) of its activity is desired.

Abstract: A method for the treatment or prevention of pain and/or a headache disorder using a derivative of a valproic acid amide or a 2-valproenic acid amide, as well as pharmaceutical compositions comprising these derivatives or compounds.

Abstract: This invention relates to methods of using neurotrophic compounds having an affinity for FKBP-type immunophilins to stimulate or promote neuronal growth or regeneration and to prevent neuronal degeneration.

Abstract: Vasoactive compounds are described for the treatment of erectile dysfunction and impotence. The compounds are reaction products of an anionic or negatively charged vasoactive or erection-inducing component (such as alprostadil) and a cationic or positively charged vasoactive or erection-inducing component (such as prazosin) or a local anesthetic (such as lidocaine). These components are combined as acids and bases to form an organic salt or ionically bonded compound. The compounds have advantageous solubility characteristics and efficacy. A compound of the invention is combined with a pharmaceutical vehicle to form a composition which preferably includes an emulsifier. A local anesthetic and/or androgenic steroids may also be included. Compositions of the invention may also include more than one vasoactive organic salt compound. The composition can be advantageously formulated and administered to allow self-adjusted dosing, while minimizing or preventing overdosing.

Abstract: This invention provides novel quinazolinone compounds and pharmaceutically acceptable salts thereof, which are useful as local anesthetics. This invention also provides pharmaceutical compositions containing such compounds; methods for producing local anesthesia in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a &agr;v&bgr;3, &agr;v&bgr;6, &agr;5&bgr;1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: 1

Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q  (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent s

Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: The present invention relates to novel substituted diamine derivatives for the formula 1

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waster or inedible, such as the leaves, peel and immature, unripe fruit. The materials contain as least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methylamine. Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: The present invention features pharmaceutical formulations containing a lipophilic compound such as leflunomide. The lipophilic compound is solubilized in solution containing alcohol and a surfactant. The solubilized compound can then be further dissolved in a pharmaceutically acceptable aqueous solution, such as WFI (water for injection), D5W (5% dextrose in water) or D5W ½ N saline, to form a pharmaceutical formulation suitable for patient administration. The formulation is preferably used for parenteral administration.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

Abstract: A method for inhibiting angiogenesis comprising administering to a patient (mammal, such as a human) in need thereof, a pharmaceutically effective amount of an angiogenesis inhibitor containing a compound of formula (I) or a pharmaceutically acceptable salt thereof, either alone or in combination with a pharmaceutically acceptable carrier. The method of treatment may be used to treat diseases in which the angiogenesis participates, particularly retinal diseases such as diabetic retinopathy, macular degeneration, retinal vein occlusion and retinal artery occlusion, neovascular glaucoma and tumors such as hemangioma.

Abstract: The present invention relates to a novel aqueous composition based on a compound modulating the reactivity of nerve fibers. It relates more particularly to a pharmaceutical composition for topical use on a human or animal body and intended to anesthetize the skin or the mucous membranes or to treat pruritus.

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

Abstract: The present invention relates to new lipopolyamines (including salts thereof) characterised by a symmetrical, highly flexible lipophilic moiety having buffering capacity at physiological pH, and to the use thereof for the in vivo or in vitro introduction of biologically active materials, such as, for example, DNA, RNA, ribozymes, antisense DNA, PNA, peptides and proteins, into eukaryotic cells.

Abstract: The present invention relates to a method of treating migraine in a mammal, including a human, by administering to the mammal a 5HT1 receptor agonist, and particularly eletriptan, in combination with metoclopramide. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT1 receptor agonist and metoclopramide.

Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).

Abstract: A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

Abstract: The present invention intends to provide a derivative of sphingosine analogue that is able to regulate the functions of sphigolipid, and its pharmaceutical compositions. The present invention is the derivatives of sphingosine analogues represented by the general formula (I) described below. In the formula, R1 and R2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 carbon atoms, or acyl groups having 2-5 carbon atoms. R3 and R4, which are the same or different each other, are hydrogen or hydroxyl groups; or R3 and R4 make up a covalent bond. X1 is —(CH2)n—CO—NH—CH(R5)—R6 or —(CH2)m—O—CO—CH(R7)—R8.

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as for improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waste or inedible, such as the leaves, peel, and immature, unripe fruit. The materials contain at least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methyltyramine (1). Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: The invention relates to the use of certain pharmaceutical compounds as anti-inflammatory agents.

Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.

Abstract: The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same in the field of general health care, for example, to improve resistance to stress, improve production of desired characteristics or useful products in animals, to increase weight gain, and to decrease feed efficiency. The invention has applications in the field of animal husbandry. It also relates to administering beta-alethine to improve feed efficiency in an animal, comprising administering to animal an amount of .beta.-alethine sufficient to reduce the amount of food required to increase a unit of weight in the animal.

Abstract: The invention relates to methods of producing analgesia, particularly in the treatment-of-acute and persistent pain and neuropathic pain. The compound 2(ethylamino)-N-(3-hydroxy-2,6-dimethylphenyl) acetamide, or 3-hydroxymonoethylglycinexylidide (3-hydroxy MEGX), is shown to provide analgesia in settings of acute, persistent and neuropathic pain.