Abstract: Cosmetic and/or pharmaceutical preparations comprising (a) a carbonate of the formula (I): wherein R1 is a linear alkyl and/or alkenyl group having from 6 to 22 carbon atoms, a 2-ethylhexyl, isotridecyl or isostearyl group or a group derived from a polyol having from 2 to 15 carbon atoms and at least two hydroxyl groups; R2 has the same meaning as R1 or is an alkyl group having from 1 to 5 carbon atoms and each of n and m independently has a value of from 0 to 100; and (b) a propellant can be used as aerosols.

Abstract: Formulations in water suspension of microcapsules based on 3-iodo-2-propynyl butyl carbamate (IPBC) comprising (parts by weight): (a) 10-60 parts of polymeric microcapsules comprising inside them IPBC and a synergizing agent formed of one or more alkylbenzenes having a number of carbon atoms from 9 to 20: (2) 1-5 parts of one or more dispersants; (3) 1-20 parts of one or more excipients selected from thickeners, antifoam, antifreeze, in can preservative agents; (4) water to 100.

Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, acne, alopecia, hirsutism, a wound, prostate cancer, bladder cancer, liver cancer, breast cancer and Kennedy's disease.

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: The present application relates to a cosmetic composition comprising at least one carbonic acid ester corresponding to formula (I) below: R1—O—CO—O—R2 ??(I) in which R1 and R2 are identical or different and represent a linear or branched hydrocarbon-based radical, with the proviso that: when R1 and R2 are linear, they each contain from 1 to 6 carbon atoms, with 6?R1+R2?7; and when R1 and/or R2 are branched, they each contain from 1 to 8 carbon atoms, with 6?R1+R2?9. This composition can be used as a product for caring for and/or making up keratin materials, in particular the skin, the lips and/or the integuments.

Abstract: The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, 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 the active compound in question.

Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.

Abstract: Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.

Abstract: Methods of using compounds having certain inhibitory effect to treat cancer are disclosed. More specifically, methods of using myosin light chain kinase inhibitor (MLCK) to treat cancer are disclosed. MLCK inhibitors may cause reduction in MLC-P and induce apoptosis in neoplastic cells and prevent and or inhibit the tumor growth.

Abstract: Pharmaceutical compositions comprising an anti-emetic compound and a highly orally bioavailable form of propofol, oral dosage forms comprising an anti-emetic compound and a highly orally bioavailable form of propofol and methods of treating emesis in a patient comprising orally administering a therapeutically effective amount of an anti-emetic compound and a highly orally bioavailable form of propofol are disclosed.

Abstract: The present invention relates to hormone coating layers having desirable hormone delivery characteristics and product lifetime. In one embodiment, the invention is a hormone composition including a substrate having an external surface, and a coating layer disposed on the external surface. The coating layer preferably includes a polymer web, a UV protectant material, and from about 1 wppm to about 100,000 wppm of a hormone dispersed throughout the polymer web. The invention also relates to methods for making hormone coating materials of the present invention. The coating compositions of the present invention preferably are implemented in human and animal food packaging materials in order to safely and efficiently protect the foodstuffs contained therein from insect infestation.

Abstract: The present invention provides propofol prodrugs, methods of making propofol prodrugs, pharmaceutical compositions of propofol prodrugs and methods of using propofol prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as migraine headache pain and post-chemotherapy or post-operative surgery nausea and vomiting.

Abstract: Novel fenicol compounds having useful properties as antibiotic prodrugs, are provided, together with methods of making and using these new compounds.

Abstract: The present invention relates to hormone coating layers having desirable hormone delivery characteristics and product lifetime. In one embodiment, the invention is a hormone composition including a substrate having an external surface, and a coating layer disposed on the external surface. The coating layer preferably includes a polymer web, a UV protectant material, and from about 1 wppm to about 100,000 wppm of a hormone dispersed throughout the polymer web. The invention also relates to methods for making hormone coating materials of the present invention. The coating compositions of the present invention preferably are implemented in human and animal food packaging materials in order to safely and efficiently protect the foodstuffs contained therein from insect infestation.

Abstract: This invention relates to a method for the treatment of acne that comprises applying a fluid comprising a polyalkylene carbonate over the area affected by acne and penetrating pores within the area. Forming a polyalkylene carbonate film covering the affected area, and thereafter removing the film. The polyalkylene carbonate film can also contain medications useful in the treatment of acne.

Abstract: Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing the same as well as a method for treatment of parasitic disorders, wherein said compounds are administered. The present compounds are especially well suited for treatment of coccidiosis, particularly in poultry, and they have general formula (I): where Y is S or O and R is as defined in the specification.

Abstract: The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor

Abstract: Disclosed are compounds that inhibit the microbial NAD synthetase enzyme. For example, disclosed are compounds of the formula Ar1—X—Ar2—Y—L—Z—Q, wherein Q is Q1Ar3 or Ar3Q1; Ar1, Ar2, and Ar3 are independently aryl or heteroaryl, optionally substituted with one or more substituents; X, Y, and Z are independently selected from the group consisting of a covalent bond or groups containing one or more of C, H, N, O, S atoms; L is a linker and Q1 is an alkylenyl, alkylenyl carbonyloxy alkyl, or alkylenyl carbonylamino alkyl group, optionally having a substituent; a covalent bond; a group containing amidine or guanidine function wherein the amidine or guanidine may be optionally N-substituted with an alkyl; or a zwitterion; or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.

Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1. The invention provides recombinant serine protease domains and methods of using peptides comprising a recombinant serine protease domain to screen for compounds that inhibit serine protease activity of matriptase or MTSP1.

Abstract: The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

Abstract: Applicant has discovered an in situ method of preparing quaternary ammonium methocarbonate salts and quaternary ammonium alkylcarbonate salts in high yield from tertiary amines, methanol, and at least one of a cyclic carbonate, an aliphatic polyester (such as a polycarbonate), or an ester (such as a carbonate ester), and their subsequent conversion to quaternary ammonium bicarbonates, quaternary ammonium carbonates or both in a one-pot reaction. According to one embodiment of the invention, the method includes reacting an amine and methanol with at least one of a cyclic carbonate and an aliphatic polyester to yield a quaternary ammonium methocarbonate. This method does not produce or require the handling of corrosive quaternary ammonium hydroxides. Another embodiment is a method of preparing quaternary ammonium alkylcarbonate salts by reacting tertiary amines, methanol, and an ester.

Abstract: The invention relates to anhydrous, pharmaceutical formulations of xanthogenates, to the production thereof and to agents containing said formulations for the treatment of virus, tumor or autoimmune diseases. The pharmaceutical preparations contain a xanthogenate of formula (I), wherein R1 represents an optionally substituted aryl or alkyl radical and R2 represents a metal atom, an optionally substituted alkyl, alkoxy, amino or ammonium group or halogen. Said preparations also contain an emulsifying agent that reduces the irritating effect of the xanthogenate and optionally an adjuvant enhancing the activity of the xanthogenate.

Abstract: Polysubstituted indan-1-ol compounds of formula I, its physiologically acceptable salts and physiologically functional derivatives are disclosed 1

Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: Provided are compounds of formula (I) 1

Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

Abstract: A compound of Formula I, providing tetrapartate prodrugs is provided wherein: L1 is a bifunctional linking moiety; D is a moiety that is a leaving group, or a residue of a compound to be delivered into a cell; Z is covalently linked to [D]y, wherein Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof, Y1, Y2, Y3 and Y4 are each independently O, S, or NR12; R11 is a mono- or divalent polymer residue; R1, R4, R9, R10 and R12 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; R2, R3, R5 and R6 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C1-6 alkoxy, phenoxy, C1-8 heteroalkyls, C1-8 heteroalkoxy, substituted C1-6 alkyls, C3-8 cycloalkyls, C

Abstract: The present invention provides compounds of Formula (I): 1

Abstract: Compounds are described which modulate the tzrosine kinase activity of p56lck and signal transduction pathways in which this enzyme is involved. The invention also relates to compounds which have immunomodulatory activity, e.g., which have immunosuppressant or immunostimulatory activity, and/or which have an antineoplastic effect. The invention further relates to compositions comprising these compounds, and methods of using them.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The present invention relates to novel prodrugs of gabapentin and to pharmaceutical formulations and sustained release formulations containing the prodrugs.

Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-Dmyo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor 5 agents which effectively inhibit the growth of mammalian cells.

Abstract: The present invention relates to the use of NAD(P)H oxidase inhibitors to increase cellular uptake of glucose and in the treatment and/or prevention of diseases caused by insulin resistance or diseases related thereto, such as type II diabetes. Specifically, the invention relates to a method for identifying an agent useful for the treatment or prophylaxis of a medical condition associated with elevated levels of blood glucose, the method comprising (i) contacting a candidate agent with a mammalian NAD(P)H oxidase or NAD(P)H oxidase complex; and (ii) determining whether said candidate agent inhibits the biological activities of the NAD(P)H oxidase or NAD(P)H oxidase complex.

Abstract: Ophthalmic compositions containing Lipoxin A4 and its analogs and methods of their use for treating dry eve are disclosed.

Abstract: This invention provides a method of inhibiting proliferation of tumor cells in a subject by administering to the subject an effective amount of ester and thioester compounds containing an N-formyl hydroxylamine group.

Abstract: This invention relates to novel alkylxanthates of formulae 1 to 3 and use of alkylxanthates of formulae 1 to 6 in the integrated pest management, more specifically alkyl xanthates are used as insect growth regulators for pest management in agricultural fields no or less environmental impact.

Abstract: The invention relates to the use of 2-(3,4-dihydroxyphenyl)ethyl-substituted carbonic acid derivatives as antioxidants or free-radical scavengers, in particular to the use for protecting human cells and tissues from the harmful, aging-accelerating effects of free-radicals and reactive oxygen compounds.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: The invention is directed to novel pharmaceutical compositions comprising chemicals agents that are useful in the treatment and prevention of cystic fibrosis and the prevention of signs and symptoms of this disease. These pharmaceutical compositions are surprisingly successful in the treatment disorders related to cystic fibrosis including disorders of blood production. Many of these compositions of the invention are even more effective when administered to a patient in pulses. Pulse therapy is not a form of discontinuous administration of the same amount of a composition over time, but comprises administration of the same dose of the composition at a reduced frequency or administration of reduced doses.

Abstract: A class of biopolymer including sulfur in the form of a thioester in the polymer backbone or a thioether in the polymer side chains has been developed. These are preferably produced by fermentation of bacteria with appropriate sulfur containing substrates, which are incorporated by a broad spectrum polyhydroxyalkanoate (“PHA”) polymerase. The sulfur-containing PHAs allow various applications and uses in industry. Representative embodiments of the applications of the sulfur-containing PHAs include their uses in the packaging industry, medicine, pharmacy, agriculture or food industry, as active agents or as coatings, packaging, or carriers.

Abstract: The present invention includes 16-HETE analogs which are agonists and antagonists of 16-HETE. The compositions may be formulated in pharmaceutically acceptable formulations. The invention also includes methods and products for inhibiting neutrophil adhesion and neutrophil aggregation using the 16-HETE agonists. One method of the invention involves the administration of a 16-HETE agonist in combination with a thrombolytic agent to a patient suffering from thromboembolic stroke.

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof.

Abstract: A method is provided for preventing or reducing the risk of onset of a cardiovascular event by administering an HMG CoA reductase inhibitor such as pravastatin, to a patient which has one or more risk factors for a coronary and/or cerebrovascular event such as hypercholesterolemia.

Abstract: The present invention provides a composition, and a method of use thereof, that is pesticide-free and yet is capable of cleansing an individual of a pest infestation. The composition of the present invention consists essentially of an acid, an alcohol, an aqueous detergent and water. The composition is used in the removal of pests and their ova from infested individuals. Preferably, the composition of the present invention takes the form of a shampoo and is used to cleanse individuals of lice infestations. In use, the composition is applied to hair and allowed to remain in contact with the hair and scalp for a period of time, called the residence time. After the residence time, the composition is rinsed from the hair. Then, the hair is combed with a suitable nit comb. These treatment steps may be repeated as necessary and appropriate to effectuate the removal of the pest infestation.

Abstract: The present invention relates to a nanoemulsion, the oil globules of which have an average size of less than 100 nm, comprising (1) a surfactant which is solid at a temperature of less than or equal to 45° C., which surfactant is chosen from sorbitan fatty esters and oxyethylenated sorbitan fatty esters, (2) at least one oil having a molecular weight of greater than 400 and (3) at least one ionic amphiphilic lipid chosen from the group formed by the alkaline salts of dicetyl and dimyristyl phosphate, the alkaline salts of cholesterol sulphate, the alkaline salts of cholesterol phosphate, lipoamino acids, the sodium salts of phosphatidic acid, cationic amphiphilic lipids and alkylsulfonic derivatives, the ratio by weight of the amount of oily phase to the amount of surfactant ranging from 2 to 10. The surfactant used is, for example, chosen from sorbitan monostearate, sorbitan monopalmitate and sorbitan 20 EO tristearate. The emulsion obtained is transparent and stable on storage.

Abstract: This invention relates to treating pulmonary diseases such as chronic obstructive pulmonary disease or asthma by administering a phosphodiesterase 4 inhibitor in combination with beta adrenergic bronchodilator.

Abstract: The present invention relates to novel retinol derivatives having the formula (I): and to processes for preparing them. The invention also relates to the use of these compounds in or for the preparation of compositions intended for treating conditions of the skin or scalp, for example in preventing or combating acne and/or chronological or actinic ageing of the skin.