Abstract: Intermediate compounds which can be used in the preparation of phytone and Vitamin E, a process for the preparation thereof, and a process for the preparation of phytone and Vitamin E from these intermediate compounds.

Abstract: Disclosed is a prodrug of the formula: where A is a sulfur or a selenium, and R is derived from a mono- di- or oligo- saccharide. Also disclosed is a prodrug of the formula: where A is sulfur or selenium, R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O, and the R? groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine. Also disclosed is a prodrug of the formula; where A is sulfur or selenium, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is also be an alkyl or aryl group, or R? is ?O, and R‡ is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula: where R is COOH or H, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH,where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: Combinatorial libraries are disclosed which are represented by Formula I: (T′—L)q—Ŝ—C(O)—L′—II′  I wherein: Ŝ is a solid support; T′—L— is an identifier residue; and —L′—II′ is a ligand/linker residue. These libraries contain dihydrobenzopyrans of the formula: which interact (i.e., as agonists or antagonists) with &agr; adrenergic receptors, dopamine receptors, &dgr;-opiate receptors, and K+ channels and are inhibitors of carbonic anhydrase isozymes. They are useful in the treatement of ocular diseases such as glaucoma.

Abstract: A process is described for continuously preparing chromanol ester derivatives, in particular for continuously preparing carboxylic esters of tocopherols and tocotrienols by continuous acylation with carboxylic acids or carboxylic anhydrides.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.

Abstract: The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula —COOR, or —PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for rheumatic diseases.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.

Abstract: The present invention provides an antiproliferative compound having a structural formula where X and Y independently are oxygen, nitrogen o r sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers or nitriles; R2 and R3 are hydrogen or R4; R4 is methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide or amine; and R5 is alkenyl; where when Y is nitrogen, said nitrogen is substituted with R6, wherein R6 is hydrogen or methyl. Also provided are methods for treating a cell proliferative disease and for inducing apoptosis in a cell comprising administering this compound is also provided.

Abstract: Disclosed are methods for treating obstructive and ischemic bladder diseases which include administering a compound which includes a cyclic or acyclic disulfide covalently bonded to a lipid-soluble antioxidant or which include administering a reduced sulfhydryl derivative thereof. Also disclosed are compounds that include a benzopyran moiety which is directly or indirectly covalently bonded to a cyclic or acyclic disulfide, as well as reduced sulfhydryl derivatives of such compounds. Methods for making such compounds and reduced sulfhydryl derivatives using tocopherol and lipoic acid starting materials are also disclosed, as are methods for inhibiting oxidative and/or free radical damage in a subject's cells, nerve membranes, sarcoplasmic reticula, mitochondrial membranes, and/or muscle plasma membranes and methods for treating and/or preventing obstructive and ischemic bladder diseases, conditions involving hypoxia, ischemia, and/or reoxygenation injury.

Abstract: Novel intermediate compounds which can be used in the preparation of phytone and Vitamin E and a process for the preparation thereof. A process for the preparation of phytone and Vitamin E from these compounds is also claimed.

Abstract: Tocopherol derivatives are provided. In one embodiment, the tocopherol derivative includes a tocopherol moiety covalently coupled to branched hydrophilic moiety. In another embodiment, the tocopherol derivative includes a first tocopherol moiety covalently coupled to a second tocopherol moiety through a hydrophilic moiety. In other embodiments, the derivative includes three or more tocopherol moieties.

Abstract: The object of the present invention is to provide a tocotrienol derivative which is highly water-soluble and shows high bioavailability in the living body and &ggr;-CEHC delivering agent. (A tocotrienolcarboxylic acid ester derivative represented by the general formula (I). (wherein R2 means a carboxylic acid residue having a nitrogen substituent, and R1 and R3 mean a hydrogen atom or a methyl group.

Abstract: The present invention relates to benzopyrans and benzoxepines of formula (I), wherein X, A, R1, R2 and (R)p have the meanings as given in claim 1, which can be used in the treatment of dislipidaemias, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to processes allowing the preparation of these compounds.

Abstract: Orthomolecular Vitamin E derivative compounds, compositions, and their uses for effecting aging and longevity, nerve activity, hematopoiesis and maintenance of blood cells, hepatic activity, nephritic activity, heart and cardiovascular function, pulmonary function, muscular function, cartilage, bone, and joint health, gastrointestinal function, reproductive system function, vision, immune function, cell membrane integrity, and pain and inflammation; preventing or treating diseases or conditions; treating cancers or obesity; and reducing the risk of Sudden Infant Death Syndrome in an animal.

Abstract: The present invention is a method of making (all-rac)-&agr;-tocopherol in a reaction having the following steps: a) reacting trimethylhydroquinone and a phytol selected from the group consisting of isophytol and phytol in the presence of a bis(perfluorinated hydrocarbyl sulphonyl)imide catalyst or a metal salt thereof of formula I: [(R1SO2)2N]xR2  (I)  wherein each R1, independently, signifies a perfluoroalkyl group CnF2n+1 or a pentafluorophenyl, or both symbols R1 together signify a poly-difluoromethylene group—(CF2)m—, with the proviso that both symbols R1 cannot simultaneously signify trifluoromethyl, R2 signifies a proton or a cationic form of a metal selected from the group consisting of boron, magnesium, aluminum, silicon, scandium, titanium, vanadium, manganese, iron, cobalt, nickel, copper, zinc, yttrium, zirconium, rhodium, palladium, silver, tin, lanthanum, cerium, praseodymium, neodymium, europium, dysprosium, thulium, ytterbium, hafnium, platinum, an

Abstract: A method for the production of a vitamin-A containing cream comprising the following steps: a) a first mixture—consisting of a number of water-soluble substances such as glycerine and extracts of plants—is mixed together during heating and comminution until the mixture has a temperature of about some 80° C., preferably 83° C., b) a second mixture consisting of a number of oil-soluble substances, including emulsifiers, and squalane and vegetable oils such as avocado oil are mixed together during heating until the mixture has a temperature of about some 80° C., preferably 83° C., c) said first mixture is then gradually added to said second mixture during high-shear-mixing with decreasing number of revolutions—from about 5000 rpm to about 3300 rpm—until the temperature of the mixture slowly has decreased to about some 50° C., preferably 51° C.

Abstract: The present invention provides an antiproliferative compound having the structural formula 1

Abstract: A process for the manufacture of d,l-&agr;-tocopherol by the acid-catalyzed condensation of trimethylhydroquinone with isophytol or phytol in ethylene or propylene carbonate or a mixture of both carbonates, or in a mixture of one or both of the carbonates and a non-polar solvent, comprises carrying out the condensation in the presence of at most 0.4 weight percent based on the weight of isophytol or phytol of 12-tungstophosphoric acid, 12-molybdophosphoric acid or 12-tungstosilicic acid. The product of the process is the most active and industrially important member of the vitamin E group.

Abstract: A process for the production of &agr;-tocopherol acetate in a recirculating process by condensation of trimethylhydroquinone and isophytol in the presence of a catalyst system of a zinc halide and an aqueous protonic acid and, optionally, an elemental metal, in a polar solvent/water mixture extractable or miscible with water, and subsequent acylation of the resultant &agr;-tocopherol and recirculation of the catalyst system.

Abstract: The present invention provides an antiproliferative compound having a structural formula 1

Abstract: Processes for purifying compounds are disclosed which include reacting (i) a mixture of at least one tocopherol compound or sterol compound, and an alcohol having from about 10 to 30 carbons with (i) one or more boron-containing compounds to form a second mixture of orthoborate esters, wherein the mole ratio of tocopherol, sterol and alcohol to boron is at least about 2.5:1; heating the second mixture to form a residue containing the orthoborate esters; contacting the residue with a compound capable of solvolyzing the orthoborate esters to form a third mixture including the boron-containing compound(s), the alcohol and the tocopherol and/or sterol compound(s); and recovering the tocopherol and/or sterol compound(s).

Abstract: A method and composition for preserving or enhancing the beneficial effects of interleukin-2 (IL-2) while simultaneously mitigating the adverse effects of IL-2 on a subject is disclosed. The method involves administering an amount of a leukotriene B4 (LTB4) antagonist, preferably a LTB4 receptor antagonistic, to a subject exhibiting adverse pharmacological effects due to exogenous IL-2, where the amount administered to the subject is sufficient to decrease the IL-2 induces adverse effects. Also disclosed is an article of manufacturing comprising a composition of the leukotriene B4 antagonist in combination with labeling instructions for treatment. Also disclosed is a method for preparing a pharmaceutical composition. Generally the LTB4 antagonist will reduce the IL-2-induced adverse effects while preserving or enhancing the antitumor, antiviral, or immunostimulatory effects of IL-2, thereby improving the therapeutic index of IL-2.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; R1 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxylic acid, carboxylate, carboxamide, ester, thioamide, thiolacid, thiolester, saccharide, alkoxy-linked saccharide, amine, sulfonate, sulfate, phosphate, alcohol, ethers and nitriles; R2 is hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R3 is selected from the group consisting of hydrogen, methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; R4 is of methyl, benzyl carboxylic acid, benzyl carboxylate, benzyl carboxamide, benzylester, saccharide and amine; and R5 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, carboxyl, amide and ester. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.

Abstract: This invention relates to a process for the preparation of tocopherol concentrates from a material containing tocopherols and free fatty acids. The free fatty acids in the tocopherol-containing material are converted to the alkali metal salts thereof in a specific organic solvent that can not, practically, dissolve the alkali metal salts of fatty acids. The free fatty acids are removed as a precipitate of their alkali salts, and the tocopherols are recovered from the supernatant by removing the solvent. The said specific organic solvents include acetone, ethyl acetate, dimethylformamide, acetonitrile and their mixtures. The alkali salts are preferably sodium and potassium salts.

Abstract: The invention provides a method of producing &agr;-tocopherol and &agr;-tocopheryl esters. The method comprises using a biological system to produce farnesol or geranylgeraniol. Then, the farnesol or geranylgernaiol is chemically converted into &agr;-tocopherol or an &agr;-tocopheryl ester.

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: Disclosed is a method for preparing DL-&agr;-tocopherol with a high yield through the condensation of isophytol or phytol derivatives with trimethylhydroquinone (TMHQ) in the presence of a Zn—Al heterogeneous catalyst system. At 80 to 120° C., the condensation is carried out for 2 to 7 hours in the presence of a Zn(II) ion-coated alumina-silica catalyst in an n-heptane solvent. The synthetic Zn(II) ion-coated silica-alumina synthetic catalyst system can remarkably reduce side-reactions upon the condensation of isophytol or phytol derivatives and TMHQ, thus producing DL-&agr;-tocopherol with a high purity at a high yield. In addition, the catalyst system is greatly convenient to handle and therefore apply for continuous reactions for the preparation of DL-&agr;-tocopherol. With these advantages, the catalyst system can be effectively used in preparing highly pure DL-&agr;-tocopherol at a high yield on a commercial scale.

Abstract: Disclosed is a process for the oxidation of sulfonamides to sulfonyl imines using chromium (IV) dioxide as the oxidant.

Abstract: A method of making (all-rac.)-&agr;-tocopherol by the acid-catalyzed condensation of trimethylhydroquinone with isophytol or phytol wherein the condensation is carried out in the presence of a tris(perfluoroalkanesulphonyl or pentafluorobenzenesulphonyl)methane or a metal salt thereof as the catalyst in an organic solvent. In addition to the metal salt, a Bronsted acid, e.g. sulfuric acid, phosphoric acid or p-toluenesulphonic acid, may be used as a co-catalyst. The product of the method of making is the most active member of the vitamin E group.

Abstract: A process for the production of a Mannich reagent comprises reacting formaldehyde, especially paraformaldehyde, with a secondary amine in the complete or almost complete absence of a solvent. An alternative comprises reacting a diaminomethane produced from a secondary amine, formaldehyde, especially paraformaldehyde, as well as water with one another in about equimolar amounts. The invention is also concerned with a process for the aminomethylation of &dgr;-tocopherol or of tocopherol mixtures containing this and comprises using a Mannich reagent which has been produced in the above manner. After completion of this aminomethylation process excess Mannich reagent can be separated by distillation and can be reacted with water and formaldehyde, especially paraformaldehyde, in order to regenerate further Mannich reagent suitable for use in the aminomethylation, this regeneration representing a further aspect of the invention. Finally, the invention includes certain novel bis(aminomethyl)-&ggr;-tocopherols.

Abstract: Disclosed is polyoxypropylenepolyoxyethylene vitamin E, represented by formula (I). It is prepared by subjecting vitamin E to polyethoxylation and then, to polypropoxylation to a proper extent. The vitamin E is of superior anti-oxidation activity with water solubility. The bent chain of the polyoxypropylenepolyoxyethylene vitamin E increases the cross-sectional area of the whole molecule, making it difficult for the molecule to penetrate into the skin. It is very safe to apply to the skin. The polyoxypropylenepolyoxyethylene vitamin E has superb surface activity by forming close bilayer vesicle structures, like phospholipids or dialkyl surfactants, so it can be advantageously used in the cosmetic industry, the food industry and the medical industry. In said formula, R1 is —(OCH2CH2)m— wherein m is an integer of 0 to 150; R2 is (a) wherein n is an integer of 1 to 200; A is (b) or (c); B is —CH3 at the 5-, 7- or 8-position of vitamin E; and p is an integer of 1 or 3.

Abstract: A source of material known as a byproduct solution of Bixa orellana seed components, which is obtained as an oily material after the bulk of annatto color, is removed from either the aqueous extract or solvent extract of annatto seeds. Further, this byproduct contains a tocotrienol component and a geranylgeraniol component and can be used as a source for the recovery of a tocotrienol component and a geranylgeraniol component.

Abstract: 3-(Hydroxymethyl)chromen-4-ones of formula (I) are described and a process for preparing said compounds.

Abstract: A mixture of a pomegranate seed oil product and a pomegranate juice product and a pharmaceutical composition containing same. The mixture, which is a cancer chemopreventive, includes a pomegranate seed oil product and pomegranate juice product. The pharmaceutical composition includes physiologically active amounts of pomegranate seed oil product, a pomegranate juice product and a pharmaceutically acceptable carrier. According to some disclosed embodiments, a pomegranate peel product is further included. Further disclosed is a selective estrogen receptor modulator and other biologically active compounds derived from pomegranates as well as methods of use thereof.

Abstract: Disclosed are prodrugs as follows: (I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide; (II) a prodrug of the formula where A is sulfur or selenium, R′ is a sugar, or ═O, and the R″ groups are hydrogen, alkyl, alkoxy, carboxy; (III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine; (IV) a prodrug of the formula where A is sulfur or selenium, and R′ is a sugar, or an alkyl or aryl group, or ═O, and R‡ is an alkoxy, or an amine group; (V) a prodrug of the formula R is COOH or H, and R′ is a sugar or ═O.

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: A formulation for topical use in hydrophobic gel form comprising, in weight percentages on the total weight of the formulation: 20 to 70% of vitamin E acetate, 20 to 70% of a volatile silicone chosen from the group comprising pentamer cyclomethicone tetramer cyclomethicone, hexamer cyclomethicone, hexamethyldisiloxane and mixtures thereof to 13% of hydrogenated castor oil.

Abstract: The present invention provides an isolated and purified &agr;-tocopherol transport protein polypeptide. Human recombinant &agr;-tocopherol transport protein, polynucleotides encoding human &agr;-tocopherol transport protein and methods of using &agr;-tocopherol transport protein polypeptides and polynucleotides are also provided.

Abstract: The invention provides methods for producing tocopherol compounds of the Vitamin E family by reduction of various 4-chromanone trienol materials. In preferred embodiments the invention provides methods of preparing and hydrogenating 4-chromanone trienols to provide gamma-tocopherol.

Abstract: Process for the production of &agr;-tocopherol acetate in a recycling process by condensation of trimethylhydroquinone diesters and isophytol in the presence of a catalyst system consisting of a zinc halide and of an aqueous protonic acid and optionally of an elemental metal in a polar solvent/water mixture which is extractable or miscible with water and subsequent recycling of the catalyst system.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiathermogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: Nonalcoholic steatohepatitis (NASH) is a disease of the liver characterized by inflammation and damage to the liver cells. Typically, steatohepatitis involves inflammation of the liver related to fat accumulation, and mimics alcoholic hepatitis but is observed in patients who seldom or never consume alcohol. Nonalcoholic steatohepatitis can lead to serious liver damage, and ultimately cirrhosis. The present invention provides methods and compositions useful for the treatment or alleviation of nonalcoholic steatohepatitis and the pharmaceutical formulations for their administration to a human. Specifically, compositions comprised of lecithin, antioxidants and vitamin B complex are administered parenterally, most preferably by oral administration. Specific therapeutic formulations include admixtures of these compounds and specific dosage formulations include daily oral administrations of these compounds in tablet or powder forms.

Abstract: The invention provides processes for producing phytol, isophytol, and certain phytol derivatives by a method of oxidizing or epoxidizing geranylgeraniol or geranylgeraniol derivatives to form epoxygeranylgeraniol derivatives, reducing or hydrogenating the epoxygeranylgeraniol derivatives to produce epoxyphytol derivatives, and then deoxygenating the epoxyphytol derivatives to produce phytol, isophytol, phytene derivatives, isophytene derivatives, or mixtures thereof. The step of deoxygenating is carried out in the presence of deoxygenation catalysts, including rhenium trioxide compounds. The invention also provides methods for the synthesis of certain novel substituted epoxyphytyl compounds and substituted phytene compounds having removable protecting groups.

Abstract: Multiple micro-encapsulations of a high concentration oleophilic substance using heat to set the primary particle renders the composition suitable for the production of free-flowing powders or beadlets. Microencapsulation involves forming an emulsion out of the oleophilic substance and a polymer, and then use heat setting and/or cross-linking the polymer encapsulates the oleophilic composition. This process is then repeated with a second polymer or third polymer, and with or without cross-linked via the same or different mechanism to further protect the oleophilic substance.

Abstract: Compounds, methods and compositions are provided for inducing natriuresis in a mammal. Methods for isolating and synthesizing the natriuretic compounds are also provided. Therapeutic methods using the natriuretic compounds are also provided. The natriuretic compounds are capable of inducing sodium excretion in a mammal without inducing corresponding prolongated potassium excretion.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.