Abstract: Therapeutic compounds have the formula:(X)j--(core moiety),J being an integer from one to three, the core moiety having at least one, five- to seven-membered ring and X being a racemic mixture, R or S enantiomer, slovate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.

Abstract: The present invention features pharmaceutical formulations containing a lipophilic compound that is solubilized in a solution containing ethanol 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) and D5W 1/2 N saline, to form a pharmaceutical formulation suitable for patient administration. The formulation is preferably used for parenteral administration.

Abstract: A composition for topical therapy for symptoms of back pain, muscle tension or myofascial pain or a combination thereof, which comprises a topical carrier system for intact skin of the back or outer synovial membranes or both, which comprises a therapeutic dose of a local anesthetic, and which applies the local anesthetic to a region of skin lying beneath the topical carrier system.

Abstract: A method of inhibiting tumor growth includes the steps of depleting intracellular iron levels of tumor cells to increase expression of cellular transferrin receptors in tumor cells and then exposing the tumor cells to monoclonal IgG anti-transferrin receptor antibodies.

Abstract: The invention relates to new derivatives of glycylanilides having general formula (I), wherein, particularly, R.sub.1, R.sub.3, R.sub.4, R.sub.8, R.sub.9 represent CH.sub.3 ; R.sub.2, R.sub.5, R.sub.6, R.sub.7 represent H; R.sub.10 represents C.sub.12 H.sub.25 and A is a sulfur atom. It also relates to the preparation process and the pharmaceutical compositions comprising as active principle at least one of said compounds, as well as the utilization of said derivatives for the fabrication of drugs intended to the treatment of hypercholesterolemy or atherosclerosis.

Abstract: 2-Amino-N-(1,2-diphenyl-1-methylethyl) acetamide (remacemide), or a pharmaceutically acceptable salt thereof, for use in the treatment of Parkinson's disease is disclosed.

Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.

Abstract: Novel substituted fluorene compunds of Formula I are active as melatonergic agents: ##STR1## wherein: X=H, halogen, OH or OZ;Z=C.sub.1-6 alkyl; --(CH.sub.2).sub.m --CF.sub.3 (m=0-2); CD.sub.3 ; or ##STR2## n=1 or 2; and R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, halogen substituted C.sub.1-6 alkyl, or C.sub.1-6 alkoxy substituted C.sub.1-6 alkyl.

Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which A, R.sub.1, R'.sub.1, R.sub.2, R.sub.3 and n are as defined in the description, and medicinal product containing the same useful for treating a mammal afflicted with a disorder of the melatoninergic system.

Abstract: The use of compound 1 and/or 2 of the formulae ##STR1## and of physiologically tolerable salts of compound 2 for the treatment of rejection reactions of the organ recipient to the transplanted organ is described.

Abstract: Compositions and methods are provided for increasing the serum half-life of a pharmacologically active agent. The novel compositions are covalent conjugates of the selected pharmacologically active agent and a transthyretin-binding ligand such as tetraiiodothyroacetic acid, 2,4,6-triiodophenol, flufenamic acid, or the like.

Abstract: 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: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Abstract: The present invention provides compositions comprising lidocaine and emu oil. The compositions are useful in a method of anesthetizing cornified skin comprising topically administering the subject compositions. The present compositions and methods permit rapid and effective anesthesia of cornified skin, such that various surgeries and interventions can be performed without the need for subcutaneous injections of local anesthetics. The present invention further provides a compartmentalized kit having a first container providing emu oil and a second container providing an aqueous solution of lidocaine.

Abstract: Topical Preparations for the treatment of acne and acneiform dermatitis containing as active principle therapeutically active quantities of N,N'bis (2-hydroxyethyl) nonandiamide together with dermatansulfate lithium salt, having molecular weight ranging from 2000 to 7000, combined with suitable excipients and/or diluents.

Abstract: Synthetic mammalian matrix metalloprotease inhibitors are useful in controlling angiogenesis. These compounds are thus useful in controlling the growth of tumors and in controlling neovascular glaucomas.

Abstract: The subject invention pertains to methods of using 4-guanidinobutyramide, or a physiologically-acceptable salt thereof, in a mammal or human to improve blood circulation.

Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

Abstract: The composition of the present invention combines the local anaesthetic lidocaine in free base form and the non-CFC aerosol propellant HFC-134a (1,1,1,2-tetrafluoroethane; CF.sub.3 CH.sub.2 F) or HFC-227 (1,1,1,2,3,3,3-Heptafluoropropane; (CF.sub.3 CHFCF.sub.3), or a combination thereof, thus incorporating previously-unattainable amounts of the lidocaine free base in solution in a non-CFC aerosol propellant. This particular form of relatively-concentrated cosolvent-free anaesthetic permits improved inhalation delivery to the airway and lung, and topical airway local anaesthesia is thus readily provided. A method in accordance with the invention provides for release of the anaesthetic in aerosolized form of selected dosage from a canister containing the pressurized local anaesthetic composition into a patient's respiratory system directly or by way of an airway.

Abstract: Stilbene compounds of the following formula (I) or their pharmaceutically acceptable salts are effective as carcinostatics and of low toxicity: ##STR1## wherein X represents a hydrogen atom or a nitrile group, and Y represents an amino acid acyl group.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: D-.beta.-Lysylmethanediamine represented by the formula (I) ##STR1## or a salt or a hydrate thereof has now been found to have an activity of inhibiting the infection with AIDS virus (a virus causative of acquired human immunodeficiency syndrome), mamely HIV. A pharmaceutical composition comprising the above compound or a salt or hydrate thereof as active ingredient is provided and expectable as one of remedial agents for treating AIDS which is now thought to be difficult to cure.

Abstract: 2-amino-N-(1,2-diphenyl-1-methylethyl) acetamide (remacemide) or a phamaceutically acceptable salt thereof, and L-dopa, are useful in conjunction with one another in the treatment of Parkinson's disease. Pharmaceutical products and formulations comprising these active agents are provided.

Abstract: .beta.-alethine is identified as an anti-tumor agent.

Abstract: The present invention relates, by way of novel industrial products, to compounds which are structurally related to 15-deoxyspergualin and which have the formula ##STR1## in which: A is a single bond, a group --CH.sub.2 --, a group --CH.sub.2 O--, a group --CH.sub.2 NH--, a group --CH(OH)--, a group --CHF-- or a group --CH(OCH.sub.3)--, andn is equal to 6 or 8,and their addition salts.These novel compounds are useful especially as immunosuppressants. The invention further relates to the method of preparing said compounds.

Abstract: A therapeutic method is provided to treat eosinophil-associated hypersensitivity diseases, such as bronchial asthma, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.

Abstract: Stick formulations for topical delivery of water soluble and/or water insoluble agents are disclosed. The stick formulations may contain steroids, antibiotics, antifungals, antihistamines anti inflammatories or local anesthetics. The vehicles comprise a combination of waxes and oils and a surfactant in embodiments involving water soluble agents. Methods for preparing the various stick formulations are also disclosed.

Abstract: A compound of the formula (I): ##STR1## wherein R.sup.1 is an unsubstituted or substituted amino group, a protected amino group, or a nitro group; R.sup.2 is an unsubstituted or substituted amino group, a protected amino group, an unsubstituted or substituted hydroxy group or a protected hydroxy group; R.sup.3 is an unsubstituted or substituted amino group, m is 0 to 2; n is 0 to 6; with the proviso that when m is 0, then n is an integer from 2 to 6, and pharmaceutically acceptable salts thereof. Compounds of formula (I) except those wherein R.sup.1 is a nitro group have activity in promoting the production of nerve growth factor.

Abstract: Pharmaceutical formulations containing a lipophilic compound solubilized in ethanol and a surfactant are disclosed. The solubilized compound can then be further dissolved in a pharmaceutically acceptable aqueous solution to form a pharmaceutical formulation suitable for patient administration. Preferred lipophilic compounds are 5-methylisoxazole-4-carboxylic acid-(4-trifluoromethyl)-auilide and N-(4-triflouromethylphenyl)-2-cyano-3-hydroxycrotonamide.

Abstract: Obesity is treated by the administration to a subject of a compound having the general formula (I): R.sub.4 --(CH.sub.2).sub.n --CO--N(R.sub.1)--CH(R.sub.2)--CO(--R.sub.3), wherein R.sub.1 represents H or CH.sub.3 ; R.sub.2 represents a side chain of a naturally occurring amino acid; R.sub.3 represents OH, OCH.sub.2 CH.sub.3 and NH.sub.2 ; n is 6-18; and R.sub.4 represents CH.sub.3 or a group having the general formula (II): R.sub.3 --CO--CH(R.sub.2)--N(R.sub.1)--CO--, wherein R.sub.1, R.sub.2 and R.sub.3 have the above meanings. The compounds of formula (I) wherein R.sub.4 is a group of formula (II), are novel compounds.

Abstract: The composition of the present invention combines the local anaesthetic lidocaine in free base form and the non-CFC aerosol propellant HFC-134a(1,1,1,2-tetrafluoroethane; CF.sub.3 CH.sub.2 F) or HFC-227 (1,1,1,2,3,3,3-Heptafluoropropane; (CF.sub.3 CHFCF.sub.3), or a combination thereof, thus incorporating previously-unattainable amounts of the lidocaine free base in solution in a non-CFC aerosol propellant. This particular form of relatively-concentrated cosolvent-free anaesthetic permits improved inhalation delivery to the airway and lung, and topical airway local anaesthesia is thus readily provided. A method in accordance with the invention provides for release of the anaesthetic in aerosolized form of selected dosage from a canister containing the pressurized local anaesthetic composition into a patient's respiratory system directly or by way of an airway.

Abstract: A topical anesthetic includes about 1-10% by weight lidocaine hydrochloride, about 0.01-0.10% by weight adrenaline, and about 0.25-4% by weight tetracaine hydrochloride, preferably in an aqueous base with about 2% benzyl alcohol or in a gel including about 3% hydroxyethyl cellulose. The topical anesthetic has been found to be at least as effective as TAC (tetracaine hydrochloride, adrenaline, cocaine), but with fewer harmful side effects and at a greatly reduced cost (about 1/10 of the cost of TAC).

Abstract: This invention relates to a process for reducing the population of bacteria in aqueous systems which comprises co-treating said aqueous system with 2,2-dibromo-3-nitrilopropionamide and chlorine dioxide under the conditions specified herein. By co-treating an aqueous system with both 2,2-dibromo-3-nitrilopropionamide and chlorine dioxide, one can achieve a more effective biocidal effect with the same amount of biocide than if either the 2,2-dibromo-3-nitrilopropionamide or chlorine dioxide are used separately.

Abstract: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: A therapeutic method is provided to treat eosinophil-associated hypersensitivity diseases, such as bronchial asthma, by locally administering to a mammal in need of such treatment, an effective amount of a topical anesthetic, such as lidocaine, or a pharmaceutically acceptable salt thereof.

Abstract: The use of lidocaine or other Class I cardiac antiarrhythmic compound in the management of preterm labor and the stoppage of labor preparatory to cesarian delivery, is disclosed. The electrophysiological effects of lidocaine on the sodium, calcium and potassium channels of freshly dissociated myocytes from late-pregnant rat uteri with the tight-seal patch-clamp method are presented. Dose-response relations on the sodium and calcium currents, and effects on the availability relation for sodium current are also presented. Also disclosed are the effects of chronic administration of lidocaine on the duration of pregnancy.

Abstract: A method of alleviating pain such as neuropathic pain or acute inflammatory pain is provided which comprises administering to a mammal that is either exhibiting pain or is about to be subjected to a pain-causing event a pain alleviating/pain suppressing amount of at least one nontoxic antagonist for the N-methyl-D-aspartate receptor, e.g., dextrorphan, or metabolic precursor of such antagonist, e.g., dextromethorphan, or at least one nontoxic substance that blocks a major intracellular consequence of N-methyl-D-aspartate receptor activation, e.g., a phenothiazine such as trifluoperazine.

Abstract: The invention relates to an adhesive, biocompatible, biodegradable and non-toxic composition for surgical use, in particular for binding tissues, which composition is of the following general formula: ##STR1## in which: R is a hydrocarbon chain containing from 1 to 50 carbon atoms,R.sub.1 and R.sub.2 are identical or different and are chosen from the following groups: ##STR2## R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.

Abstract: Isoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.

Abstract: The oligomers of the present invention are polyureas or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone with a predictable anion spacing, and are pharmaceutically-acceptable. The oligomers are useful for inhibiting the proliferation of smooth muscle cell.

Abstract: Synergistic antimicrobial combinations of polyether polyamino methylene phosphonates and one or more members selected from the group consisting essentially of the following non-oxidizing biocides:didecyl dimethyl ammonium chloride;dodecylguanidine hydrochloride;methylene bisthiocyanate;2,2-dibromo-3-nitrilo-propionamide;2-(thiocyanomethylthio)benzothiazole glutaraldehyde;potassium dimethyldithiocarbamate;5-chloro-2-methyl-4-isothiazolin-3-one;2-methyl-4-isothiazolin-3-one;tetrahydro-3,5-dimethyl-2,H-1,3,5-thiadiazin-2-thione;1,2-dibromo-2,4-dicyanobutane;are useful for inhibiting microbial growth in a variety of aqueous systems.

Abstract: An aerosol-dispensable pharmaceutical composition consisting essentially of a combination of lidocaine free base, a pharmacologically-acceptable phenylephrine acid addition salt, and a pharmacologically-acceptable organic solvent, all dissolved in a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane of the formula CF.sub.3 CH.sub.2 F (HFC-134a) and 1,1,1,2,3,3,3-heptafluoropropane of the formula CF.sub.3 CHFCF.sub.3 (HFC-227) or a combination of the said propellants, suitable for dispensing by means of a metered-dosage valve canister in which it is contained under pressure, avoids the necessity of premixing individual solutions by the physician just prior to use. The phenylephrine salt is preferably the hydrochloride and the solvent is preferably ethanol although other pharmacologically-acceptable solvents and pharmacologically-acceptable acid addition salts of phenylephrine may be employed.

Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.

Abstract: Methods for regulating cation transport across cellular membranes possessing cation channels are provided. The cell membrane possessing a specific ion channel is exposed to a non-aromatic polyamine compound having a lysine- or arginine-based moiety (or a guanidine moiety) coupled to a straight chain polyamine.These polyamines as well as a method for regulating NMDA through a spermidine-like effect on NMDA receptors by exposing a cell membrane to selected polyamines are also provided.

Abstract: A method of treating a pathological condition of an internal organ in a patient which comprises topically applying capsaicin to the skin of the patient containing nerves which lead to the spinal cord segments corresponding to the internal organ without the need of systemic absorption of the capsaicin.

Abstract: There are described new 2-cyclohexan-1-yl-amine derivatives of formula (I) ##STR1## in which A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meaning given in the description, and processes for their preparation.The compounds of the formula (I) are used as anti-microbial agents.

Abstract: This invention relates to a vascular hypertrophy inhibitor containing a compound of the formula ##STR1## or its pharmaceutically acceptable salt as an active ingredient. This composition produces excellent effects as a vascular hypertrophy inhibitor.

Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.