Abstract: The invention concerns anti-tumor agents of formula (I), wherein each of R1, R2 and R3 has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4C)alkynyl and (1-4C)alkoxyl; each of R4 and R5 is (1-4C) alkyl; each of R6 and R7 is hydrogen or (1-4C)alkyl; X is N-(1-4C)alkylimino, N-(3-4C)alkenylimino, or (3-4C)alkynylimino; m is 1 or 2 and each R8 is as defined in the specification; each Y′ and Y2 is halogen, (1-4C)alkanesulphonyloxy, benzensulphonyloxy or phenyl-(1-4C)alkanesulfonyloxy; or a pharmaceutical acceptable salt thereof; provided that at least one of R1, R2 and R3 is other than hydrogen; a process for their preparation, pharmaceutical composition containing them and their use for producing an anti-proliferative effect in a warm-blooded animal.

Abstract: 15-fluoro substituted analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

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

Abstract: Disclosed are novel thickened organic fluid/surfactant compositions that are uniform, flowable and dispersible in water. Also disclosed are novel pesticidal compositions comprising a pesticide and the novel thickened organic fluid/surfactant composition.

Abstract: A composition, comprising panthenol or a derivative thereof, chitosan or a derivative thereof, and a carrier, wherein the composition forms a barrier that enhances the removal of an object having an adhesive-containing surface from a another surface to which the composition is applied without substantially interfering with the ability of the adhesive to adhere to the other surface.

Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: Disclosed herein are simple and unique methods of methods of preparing liposomal compositions of N-(4-hydroxyphenyl) retinamide (4HPR) and/or other retinoids. Also disclosed are liposomal 4HPR compositions prepared by such methods, and use of such compositions in the treatment of diseases, such as breast cancer. This invention further provides methods for improving the efficacy of N-(4-hydroxyphenyl) retinamide (4HPR) as a chemopreventive agent in the presence of agents that potentiates its ability increase the expression of inducible nitric oxide synthase (iNOS, and NO production in cells.

Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for combating phytopathogenic fungi.

Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.

Abstract: A method of treatment of disorders of neurological origin and drug formulations for use in the method are disclosed. These conditions comprise fatigue and associated syndromes of pain, weakness and depressed mood which are associated with chronic fatigue syndrome, brain injury and stroke, stress, fibromyalgia, and irritable bowel syndrome. The treatment comprises administering to a patient in need thereof a selective inhibitor of noradrenaline reuptake combined with either phenylalanine or tyrosine in the same dosage form or the same pack.# The noradrenergic drug may be selected from lofepramine, desipramine or reboxetine. The selective inhibitor may be a combined inhibitor of both noradrenaline and serotonin reuptake such as venlafaxine, duloxetine or milnacipran, or an inhibitor of both noradrenaline and dopamine reuptake such as bupropion.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: Embodiments relate to reduced VOC hair spray compositions. One composition includes a concentrate and propellant. The concentrate includes 25-45 weight percent alcohol, 30-50 weight percent methyl acetate, 5-15 weight percent resin, 0.2-1.3 weight percent neutralizer, and 5-25 weight percent water. The propellant comprises dimethyl ether. The composition includes 50 to 90 weight percent concentrate and 10 to 50 weight percent propellant.

Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

Abstract: The present invention provides methods and compositions for preventing or treating virus infections in mammals that utilize microtubule dynamics within mammalian cells. The compositions are applied to mammals via parenteral, oral, anal, aural, ocular, nasal, and topical routes of administration until clinical signs are resolved.

Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ dysfunction, in which oxidants are overproduced.

Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: A method for increasing the effectiveness of a biocide is described. In the method, at least one biocide and at least one diethanolamide are applied to a substrate or aqueous system subject to the growth of microorganisms. The diethanolamide is applied in an amount effective to increase the biocidal activity of the biocide. Biocidal compositions are described where the biocide and the diethanolamide are present in a combined amount effective to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms on various substrates and in various aqueous systems are also described. The combination of the biocide and the diethanolamide is particularly useful as a biocide in the leather industry, the lumber industry, the papermaking industry, the textile industry, the agricultural industry, and the coating industry, as well as in industrial process waters.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: Compounds represented by formula (I), and pharmaceutically acceptacle salts thereof; and their method of preparation are provided. Compounds of the above formula are influenza virus neuraminidase inhibitors and can be used in treating patients infected with influenza virus.

Abstract: The present invention provides methods for treating disease conditions associated with abnormal cellular proliferation, inflammation and viral infection or proliferation by the administration of ceramic analogs. The ceramic analogs appear to be specific for modulation of the enzyme PKC&zgr;.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: Compounds of Formula 1, where the symbols are as defined in the specification, are useful as ocular hypotensive agents but do not exert their activity through the FP prostaglandin receptor. In particular the compound PGF2&agr; 1-ethanolamide, having the formula was discovered to be present in mammalian tissue as a naturally occurring substance, was synthesized in a substantially pure form and was found to be effective for lowering intraocular pressure in the mammalian eye, but not acting through the FP receptor through which many ocular hypotensive prostaglandins act.

Abstract: A composition comprising panthenol or a derivative thereof, chitosan or a derivative thereof, and a carrier, wherein the composition forms a barrier that enhances the removal of an object having an adhesive-containing surface from a another surface to which the composition is applied without substantially interfering with the ability of the adhesive to adhere to the other surface.

Abstract: Described in the present invention are a dispersion which comprises, as a dispersoid, (a) 5 to 40 wt. % of an amphipatic lipid containing, in the molecule thereof, at least one hydroxy and amide group, and (b) 2 to 55 wt. % of a surfactant in an aqueous medium; a washing-away type cosmetic composition comprising the dispersion; and a washing-away type cosmetic composition comprising (A) 0.01 to 10 wt. % of an amphipatic lipid which contains, in the molecule thereof, at least one hydroxy and amide group and having a melting point not less than 30° C. and (B) 5 to 95 wt. % of a surfactant. The dispersion according to the present invention is useful as a component of a washing-away type cosmetic composition having both an emulsion-like or pearl-lustrous appearance and low skin irritation.

Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.

Abstract: The novel agricultural and horticultural fungicidal compositions containing as active ingredients a combination of A) 1,1′-iminiodi(octamethylene)diguanidine of the formula  (iminoctadine) or an acid addition salt thereof and B) 1,1′-iminiodi(octamethylene)diguanidine of the formula  (fenhexamid) are outstandingly active as fungicides.

Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors and/or 1-acylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.

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: wherein RF is a fluorinated radical, X is a linear or branched alkylene, R1 is H or CH3, R2 is a radical having at least one OH group, R3 is a radical derived from an amino acid or a peptide, 1≦n≦50 and 0≦m≦200 with 0.2≦n/n+m≦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: An acylamino acid for enhancing the bio-availability of substances in organisms by permeabilization of cell membranes, the acylamino acid having general formula (I) wherein R1 is hydrogen, a primary, secondary or tertiary alkyl or alkenyl group and R2 is hydrogen, a straight or branched chain alkyl group or a straight or branched chain substituted alkyl group, the substituted being selected from thio, thioether, hydroxy, carboxy, quarternary ammonium, amide, heterocyclic, benzyl, substituted benzyl, amino, substituted amino groups and difunctional alkyl groups linking to the nitrogen atom. A preferred acylamino acid for incorporating into an animal or fish feed is 2-palmitoylaminoproprionic acid.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: HETE derivatives and methods of their use for treating dry eye are disclosed.

Abstract: A method of treating a hyperproliferative disorder in a subject in need of such treatment, comprising administering to said subject, in combination, a treatment effective amount of: (a) a ceramide-generating retinoid such as fenretinide or a pharmaceutically acceptable salt thereof; and (b) at least one (and in certain embodiments at least two) ceramide degredation inhibitor, such as compounds selected from the group consisting of (i) glucosylceramide synthesis inhibitors, (ii) sphingosine-1-phosphate synthesis inhibitors, and (iii) protein kinase C inhibitors. A preferred glucosyl ceramide synthesis inhibitor is 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol. A preferred sphingosine-1-phosphate synthesis inhibitor is D-erythro-N,N-dimethylsphingosine. A preferred protein kinase C inhibitor is L-threo-dihydrosphingosine.

Abstract: The present invention relates to a cleansing composition comprising at least one compound selected from N-long chain acylamino acids represented by formula (I): (wherein n represents 1 or 2; and R represents a saturated or unsaturated hydrocarbon group having 5 to 23 carbon atoms), and salts thereof.

Abstract: Novel pharmaceutical therapeutic compositions and methods for using same for the treatment of pain experienced by an individual are provided. The compositions contain at least one member selected from among anandamide and palmitylethanolamide.

Abstract: The present invention relates to novel cycloalkylalkanecarboxamides of the formula I 1

Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.

Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.

Abstract: The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

Abstract: The present invention is directed to novel ketomethylene group-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: A composition formulated from a primary anionic surfactant; optionally a secondary surfactant and/or a resin; and a nitrogen-containing compound of the structural formula: wherein R is a saturated, linear, branched or cyclic alkyl or aryl group containing 12 to 22 carbon atoms, with the proviso that R contains at least 80% of a single chain length and R is not lanolin, wheat germ or other natural broad-based chain distribution oil, R1 is a saturated or unsaturated, linear, branched or cyclic alkyl or aryl group containing 1 to 6 carbon atoms and may contain one or more hydroxyl groups, R2 is selected from the group consisting of hydrogen, methyl, ethyl and benzyl; and A− is a monovalent anion.

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: The invention relates to novel biaromatic compounds having general formula I and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: The present invention provides a family of branched fatty acids and their derivatives, which improve and enable the penetration and absorption of active ingredients through biomembranes, such as blood brain barrier. The invention further provides pharmaceutical compositions comprising these branched fatty acids and methods of using these compositions to permeabilize biological membranes thereby improving the administration of bioactive or therapeutic substances to cells or organs. According to a more preferred embodiment of this invention the methods are particularly useful to treat certain kinds of CNS lesions and diseases including tumors, infections, abscesses and degenerative and behavioral disorders.

Abstract: The invention provides a drug-oligomer conjugate having the following general formula: wherein D is a therapeutic drug moiety; H and H′ are each a hydrophilic moiety, independently selected from the group consisting of straight or branched PEG polymers having from 2 to 130 PEG subunits, and sugars; L is a lipophilic moiety selected from the group consisting of alkyl groups having 2-26 carbon atoms, cholesterol, adamantane and fatty acids; o is a number from 1 to the maximum number of covalent bonding sites on H; m+n+p together have a value of at least one and not exceeding the total number of covalent bonding sites on D for the —H′, —L and —H—L substituents; the H—L bond(s) are hydrolyzable and the D—L′ bond(s), when present, are hydrolyzable; the conjugate being further characterized by one of the following: (i) m is 0 and p is at least 1; (ii) n is 0 and p is at least 1; (iii) m and n are each 0 and p is at least 1; (iv) p is

Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: Dietary supplement compositions designed to be responsive to specific blood types, and thus most beneficial for people with specific antigenic blood types.