Abstract: The present invention relates to compositions and uses of novel high penetration compositions or high penetration prodrugs (HPP), in particular HPPs for 4-aminophenol derivatives, which are capable of crossing biological barriers with high penetration efficiency. The HPPs herein are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, due to the ability of penetrating biological barriers, the HPPs herein are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs herein can be administered to a subject through various administration routes.

Abstract: The present invention relates to a combination of a 5-HT4 receptor agonist and a cholinesterase inhibitor and pharmaceutical compositions and formulations containing the combination. The pharmaceutical combination may be employed for the treatment of altered gastrointestinal motility, sensitivity, secretion or abdominal disorders. The dosage is preferably oral. The preferred 5-HT4 receptor agonist is tegaserod.

Abstract: The present invention relates to a method of treating schizophrenia prodrome in human subjects using a NMDA glycine site agonist, a glycine transporter-1 inhibitor or mixtures thereof, optionally in combination with a pharmaceutically acceptable additive, carrier or excipient.

Abstract: The invention relates to novel compounds having an amphiphilic character (cationic, anionic, amphoteric and non-ionic), derivatives of n acyloxypropyl-type lysine amino acid according to general formula (I), which are intended to be used in the food, pharmaceutical and cosmetic industries as surface-active agents having a self-aggregating capacity and antimicrobial properties. Variations in activity are a function of the ionic nature of the final molecule, the number of fatty chains and the length thereof. The aforementioned products are prepared using a chemical synthesis method. The intermediate and final products are purified by means of liquid/liquid and liquid/solid extractions, crystallisations, cationic exchange chromatography and normal phase chromatography.

Abstract: A method of providing a fragrant odour to an application, comprising the addition thereto of at least one compound of the formula (I) wherein X and Y are independently selected from the group consisting of —CR1R2R3, —NR4R5 and —OR6, wherein R1 to R5 are selected from H and essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom, and R6 is selected from essentially hydrocarbon moieties that optionally comprise at least one oxygen, nitrogen or silicon atom; and A is an essentially hydrocarbon moiety that optionally comprises at least one oxygen, sulphur, nitrogen or silicon atom, with the proviso that the compound A-CHO is a fragrant aldehyde. The use of these compounds in laundry, household and personal care products confers a long-lasting freshness.

Abstract: Acyloxyalkyl carbamate prodrugs of ?-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of ?-amino acids and methods of using acyloxyalkyl carbamate prodrugs of ?-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of ?-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

Abstract: The invention provides compounds for use in photochemotherapy or diagnosis, said compounds being branched alkyl esters or substituted alkyl esters of 5-aminolevulinic acid, or derivatives or pharmaceutically acceptable salts thereof. In particular, the invention provides compounds of formula (I): R22N—CH2COCH2CH2CO—OR1 (wherein R1 represents an optionally substituted branched alkyl (e.g.

Abstract: The present invention relates to a preparation suitable for the prevention and/or treatment of vascular disorders, comprising the following fractions: fraction a) consisting of long chain polyunsaturated fatty acids; fraction b) consisting of phospholipids, which fraction contains at least two different phospholipids selected from the group consisting of phosphatidylserine, phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine. fraction c) consisting of compounds which are a factor in methionine metabolism, which fraction contains at least one member selected from the group consisting of folic acid, vitamin B12, vitamin B6, magnesium and zinc.

Abstract: Compounds or their salts of general formula (I): A-B—N(O)s wherein: s is an integer equal to 1 or 2; A=R-T1-, wherein R is the drug radical and T1=(CO)t or (X)t?, wherein X=O, S, NR1c, R1c is H or a linear or branched alkyl or a free valence, t and t? are integers and equal to zero or 1, with the proviso that t=1 when t?=0; t=0 when t?=1; B=-TB-X2—O— wherein TB=(CO) when t=0, TB=X when t?=0, X being as above defined; X2 is equal to R1B—X—R2B radical wherein X is as above defined, R1B and R2B, equal to or different from each other, are linear or branched C1-C6 alkylenes, or X2 is a radical wherein two alkylene chains C1-C4 are linked to nonadjacent positions of a central ring having 4 or 6 atoms, said ring being an unsaturated cycloaliphatic ring, or a saturated or aromatic heterocylic ring, containing one or two heteroatoms, equal or different, selected from O, S, N; wherein the unsaturated cycloaliphatic ring does not have aromatic character according to Huckel's rule.

Abstract: The invention relates to methods for the treatment of tumors and/or for immune suppression and/or sepsis by modulating the association of the glycolysis enzyme complex/M2-PK and/or by inhibition of transaminases and/or separation of the binding of the malate dehydrogenase to p36 comprising administering a pharmaceutical composition comprising a substance selected from the group consisting of amino acids, amino acid analogs, sugar phosphates, sugar phosphate analogs, and mixtures of said substances.

Abstract: The invention relates to compounds of formula (I): wherein R is —C(O)CH2OCH2CH2OCH3 or —C(O)CH2N(CH3)2. The invention also relates to pharmaceutical compositions comprising a compound formula (I) and methods of treating or preventing a condition in an animal comprising administering to an animal in need thereof a compound of formula (I).

Abstract: The present invention provides a creatine ester anti-inflammatory compound which may be received by animals and then metabolized into a biologically active form of creatine. The biologically active creatine inhibits the production of chemical mediators, released during an inflammatory response, which are important components in the inflammatory response and the inflammation and pain resulting from physical or chemical trauma to cells and tissue.

Abstract: A composition for removing a radioactive element or compound such as systemic transuranic compounds, from mammals comprises a pharmaceutical carrier and a decorporation agent comprising ester and amide derivatives of DTPA. A method of treating a mammal to remove systemic compounds utilizing the DTPA derivatives is also disclosed.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2-CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: Provided herein are methods and compositions for treating or preventing mood disorders and certain other mental disorders.

Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.

Abstract: The subject invention relates to novel compositions containing a diffusion enhancing compound and their use in treating a variety of disorders.

Abstract: Pharmaceutical compositions having a pharmaceutically acceptable copper antagonist(s) or a pharmaceutically acceptable salts or prodrugs thereof, including copper (II) antagonists, and a pharmaceutically acceptable antihypertensive agent or a pharmaceutically acceptable salt or prodrug thereof, articles and kits and delivery devices containing compositions, tablets and capsules and formulations containing such compositions, and methods of use for treatment of subjects, including humans, who have or are at risk for various diseases, disorders, and conditions.

Abstract: Method of using immunomodulatory compounds for treating diseases related to an overproduction of inflammatory cytokines, including diseases selected from asthma, atopic dermatitis, allergic rhinitis, prostatitis, inflammatory bowel disease, diabetes, and rhumatoid arthritis, the compounds being of general formula (I): wherein: m and n, independently from each other, are an integer ranging from 1 to 4, X and Y represent —COOH, —O—P(O)(OH)2, —O—SO2(OH), —NH2, —OH, —CONH(CH2)n1—NH2, —CO—NH—CH(COOH)—(CH2)n1—COOH, —CO—NH—CH(COOH)—(CH2)n1—NH2, —O—CO—(CH2)n1—NH2, —O—CO—(CH2)n1—CHOH—CH2OH, —O—CO—(CH2)n1—OH, O—CO—(CH2)n1—COOH, —O—CO—(CH2)n1—CHO, —O—CO—(CH2)n1—NH—CO—(CH2)n2—COOH, R1 and R2 each designate an acyl group derived from a saturated or unsaturated, straight- or branched-chain carboxylic acid having from 2 to 18 carbon atoms, which is unsubstituted or bears one to three substituents selected among hydroxyl, dihydroxyphosphoryloxy, alkyl of 2 to 10 carbon atoms, alkoxy of 2 to 10 carbon atoms, acyloxy of

Abstract: The present invention concerns a method of administering at least one active pharmaceutical agent to a patient in need thereof, which method comprises the intranasal administration of a composition comprising a therapeutically effective amount of this agent, phospholipids, one or more C2-C4 alcohols and water, wherein the concentrations of the phospholipids and the one or more alcohols in the composition are in the ranges of 0.2 to 10% and 12 to 30% by weight, respectively, with the water content of said composition being not less than 30% by weight, the phospholipids forming vesicles in said composition. Further are disclosed pharmaceutical compositions and combinations suitable for intranasal delivery.

Abstract: The present invention relates to heparin-binding calixarene compounds of general Formula (I) in which R, R1, L and n have the meanings indicated in the description and their use in the biomedical field.

Abstract: A method of repelling wasps, which method comprises using a preparation comprising (a) one or more of ethyl 3-(N-n-butyl-N-acetylamino)propionate, dihydronepetalactone, and extract of catmint, and (b) at least one compound selected from certain perfume ingredients. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.

Abstract: Ester compounds of the formula I-a wherein R1 is selected from OH, NH2 and NH3+X?, wherein X is an inorganic anion, wherein R2 is a singly-branched saturated or unsaturated aliphatic hydrocarbon moiety selected from C7-C15, wherein R5 is selected from H, and a linear saturated or unsaturated aliphatic hydrocarbon moiety selected from C6-C14, and wherein R2 and R5 together have a total of 7 to 15 carbon atoms; that are useful as antibacterial or antifungal compounds in consumer products.

Abstract: Gaseous nitric oxide (NO) can be delivered to a mammal for prophylactic or therapeutic purposes using a composition capable of delivering NO, comprising a compound capable of forming a reversible bond or association with NO. Methods for the manufacture and use of said composition are disclosed.

Abstract: Renin inhibitors nitroderivatives of formula (I): A-(X0—ONO2)s ??(I) having wider pharmacological activity and enhanced tolerability. They can be employed for treating or preventing congestive heart failure, coronary diseases, cardiac insufficiency, left ventricular dysfunction and hypertrophy, cardiac fibrosis, myocardial ischemia, stroke, atherosclerosis, restenosis post angioplasty, renal insufficiency, renal ischemia, renal failure, renal fibrosis, glomerulonephritis, renal colic, ocular and pulmonary hypertension, glaucoma, hypertension, diabetic complications such as nephropathy, vasculopathy and neuropathy, peripheral vascular diseases, liver fibrosis, portal hypertension, metabolic syndrome, erectile dysfunction, complications after vascular or cardiac surgery, complications of treatment with immunosuppressive agents after organ transplantation, hyperaldosteronism, lung fibrosis, scleroderma, anxiety, cognitive disorders.

Abstract: Highly concentrated, water-based dispersions of certain lipophilic and/or hydrophobic antimicrobially active materials are stabilized to a surprising degree by a surfactant combination including a nonionic acrylic graft copolymer surfactant and a alkoxylated polyarylphenol phosphate ester surfactant. The active materials may be present in dispersion concentrates of the present invention singly or in useful combinations. The active materials are selected from the group of fungicides and bactericides consisting of 1,2-benzisothiazol-3(2H)-one; 2-octyl-2H-isothiazol-3-one; 5-chloro-2-methyl-2H-isothiazol-3 -one; 2-methyl-2H-isothiazol-3-one; pyrithione zinc; 3-iodo-2-propynyl butylcarbamate; 2-methylthio-4-ethylamino-6-tert-butylamino-s-triazine; and 3-(4-isopropylphenyl)-1,1-dimethylurea, and mixtures thereof. The dispersion concentrates may be efficiently shipped and stored, and subsequently diluted with water to produce less concentrated dispersions when desired.

Abstract: A process is described for strengthening the barrier function of undamaged skin in particular against allergens and/or for preventing or inhibiting an allergic reaction of undamaged skin on contact with an allergenic active ingredient, with the following step: Preparation of a mixture comprising: (c) a ceramide and/or a pseudoceramide and (d) an anti-irritant Application of an effective amount of the mixture to the undamaged skin.

Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Abstract: The invention relates to a compound having general formula I, wherein: X represents CH2, C?O, C?S or CHOH, X represents CH2, C?O, C?S or CHOH, R1 represents an amino acid which is optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0.1 or 2, or X represents CH2, C?O, C?S, CHOH, R1 represents a peptide containing two amino acids, each amino acid being optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0 or 1, or XR1 represent PO3H or SO3H and n=0.

Abstract: A method for interrogating the microcirculation of a subject for use in characterizing function in health and disease, monitor changes in microcirculation over time, and identify responses in microcirculation to potentially harmful or beneficial interventions. The method includes delivering a study agent to a study surface for trans-surface delivery to the microvasculature of the subject and monitoring the microvasculature of the subject in the area of the study surface. A system is also provided which includes a micro-patch for delivery of study agent to a study surface for trans-surface delivery to the microvasculature of the subject and a monitoring probe for monitoring the microvasculature of the subject in the area of the study surface.

Abstract: Compositions comprising trans-clomiphene may be used in treating benign prostate hypertrophy, prostate cancer, elevated triglyceride levels and hypogonadism.

Abstract: The present invention discloses certain novel prodrugs of florfenicol and/or of florfenicol analogs, including prodrugs of salts pharmaceutically acceptable salts of florfenicol and its analogs, including nitrogen-containing esters of the secondary alcohol group of florfenicol and of its analogs, and pharmaceutically acceptable salts thereof, compositions containing them, and methods of administering them to subjects. In particular embodiments the prodrugs are sufficiently water-soluble to serve the functions needed of a water-soluble prodrug of florfenicol or of a water-soluble prodrug of a florfenicol analog. A certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing florfenicol or the florfenicol analog in question.

Abstract: Sterile, stable pharmaceutical formulations of poorly water-soluble drugs dissolved in dimethyl isosorbide, a water-miscible solvent, as well as methods for their preparation and administration.

Abstract: The invention relates to insecticidal mixtures comprising methiocarb and at least one further known active compound from the group of the neonicotinoids, and to the use of these mixtures for controlling animal pests and for seed dressing.

Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.

Abstract: Methods and compositions for treating or preventing inflammatory diseases such as psoriasis or multiple sclerosis are provided, comprising the step of delivering to the site of inflammation an anti-microtubule agent, or analogue or derivative thereof.

Abstract: This invention discloses the method of preparation of creatine ester-salts. Creatine is an extremely popular ergogenic aid, and is found most often in the form of creatine monohydrate. Creatine monohydrate is poorly soluble in water however and while esters gain solubility, there functionality is greatly decreased. The material can be administered in a variety of ways including capsules, tablets, powdered beverages, bars, gels, liquids, liposomes or drinks.

Abstract: Disclosed is crystalline ladostigil tartrate of a specified density, compositions, including pharmaceutical compositions comprising such ladostigil tartrate, and a process for the manufacture thereof.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2-CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2—CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.

Abstract: The present invention relates to a preparation suitable for the prevention and/or treatment of vascular disorders, comprising the following fractions: fraction a) consisting of long chain polyunsaturated fatty acids; fraction b) consisting of phospholipids, which fraction contains at least two different phospholipids selected from the group consisting of phosphatidylserine, phosphatidylinositol, phosphatidylcholine and phosphatidylethanolamine. fraction c) consisting of compounds which are a factor in methionine metabolism, which fraction contains at least one member selected from the group consisting of folic acid, vitamin B12, vitamin B6, magnesium and zinc.

Abstract: Antimicrobial system which comprises a cationic surfactant, derived from the condensation of fatty acids and esterified dibasic amino acids, according to the following formula (I), where: X is Br, Cl or HSO4R1: is linear alkyl chain from an saturated fatty acid, or hydroxyacid from 8 to 14 atoms of carbon bonded to the ?-amino acid group through amidic bond. R2 is a linear or branched alkyl chain from 1 to 18 carbon atoms or aromatic. R3: is Formula (II), where n can be from 0 to 4, and at least one antimicrobial agent characterised for its enhanced activity.

Abstract: Remedies for spinocerebellar degeneration or compositions for treating the same which contain as the active ingredient one or more members selected from among D-cycloserine, D-serine esters, D-serine and salts thereof. A method for treating spincerebellar degeneration which comprises administering to a patient with this disease in an efficacious dose of one or more members selected from among D-cycloserine, D-serine esters, D-serine and salts thereof.

Abstract: There is provided a topical composition that comprises (a) a substantially anhydrous insect repellent selected from the group consisting of ethyl 3-(N-butylacetylamino) propionate or a derivative thereof, p-menthane-3,8-diol, hydroxyethyl isobutyl piperidine carboxylate (1-piperidine carboxylic acid), and mixtures thereof, and (b) a non-volatile solvent. A second embodiment of the present composition includes the same insect repellent, and a volatile solvent, and, optionally, a film former. A third embodiment includes the same insect repellent, a non-volatile solvent, a volatile solvent, and, optionally, a film former.

Abstract: The present invention provides a compound of formula I; R22N—CH2COCH2—CH2CO—OR1??(I) wherein R1 represents (a) an optionally substituted branched C6-30 alkyl group, comprising a straight chain C4-29 alkyl group, branched by substitution with one or more C1-6 alkyl groups, wherein said site of substitution is at C2 or a higher C atom, (b) a non-heteroaromatic aryl substituted alkyl group, wherein said aryl group is substituted, or (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group, wherein in (a) and (b) said substituents are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo or fluoro groups, and said alkyl group is optionally interrupted or terminated by one or more —O—, NR3—, —S— or PR3— groups; R2, each of which may be the same or different, represents a hydrogen atom or a group R1, wherein R1 represents (a) an optionally substituted branched C5-30 alkyl group, comprising a

Abstract: Disclosed is an aerosol insect repellent composition. The composition has (a) an amount of an insect repellent effective to repel insects when applied to the skin and (b) a cosmetically-acceptable vehicle in which to disperse and deliver the insect repellent active. The vehicle has (i) a VOC component capable of volatilizing upon exposure to a reduction in pressure for delivering the composition in an aerosol form, and (ii) a non-VOC component. The aerosol composition has a VOC content of not greater than about 55 wt. % based upon the weight of the aerosol composition. Further disclosed is a method of repelling insects from skin wherein the aerosol composition is applied to or sprayed on the skin.

Abstract: An agent for diagnosing or photokinetically treating malignant tumors, comprising as an active ingredient a compound 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, or an ester, amide, salt, hydrate or solvate of the compound.

Abstract: A method for suppressing undesired viral growth in a host which comprises administering to the host an effective amount of a compound of the formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of HO—, CH3O— and CH3(C?O) O—. The method is exemplified by inhibiting Tat transactivation of a lentivirus and in suppressing Herpes simplex virus.