Abstract: The invention features methods of treating a proliferative disorder characterized by elevated Pin1 marker levels and/or reduced Pin1 Ser71 phosphorylation in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating proliferative disorders (e.g., proliferative disorders characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with another anti-proliferative compound. Finally, the invention also features methods including high-throughput screens for discovering and validating Pin1 inhibitors.

Abstract: The present invention relates to recombinant cells, particularly recombinant plant cells, which are capable of producing dihydrosterculic acid and/or derivatives thereof. The present invention also relates to methods of producing oil comprising dihydrosterculic acid and/or derivatives thereof.

Abstract: The present disclosure relates to esters of 8-[2-(2-pentyl-cyclopropylmethyl)cyclopropyl]-octanoic acid (“DCPLA”). The disclosure further relates to compositions, kits, and methods for treatment using the esters.

Abstract: The present disclosure relates to PKC activators and combinations thereof. The disclosure further relates to compositions, kits, uses, and methods thereof.

Abstract: The present invention relates to enantiomeric forms of hepoxilin analogs of Formula I-VIII, pharmaceutical compositions thereof, a method for the separation of said enantiomeric forms of hepoxilin analogs comprising applying said hepoxilin to a chiral phase HPLC column and eluting said hepoxilin with an alkane and alcohol solvent mixture. Said enantiomeric forms of hepoxilin analogs of Formula I-VIII were found to be useful in controlling the biological effects of PPAR mediated transcriptional control for the treatment of diseases such as cancer, thromboxane-mediated diseases and for modulating intracellular calcium concentration.

Abstract: A process for the preparation of a composition comprising the cis9, trans11 and trans10, cis12 isomers of conjugated linoleic acid (CLA) comprises: providing a mixture comprising cis9, trans11 and trans10, cis12 isomers of conjugated linoleic acid (CLA) in which one of the cis9, trans11 and trans10, cis12 isomers is present in a first weight ratio X of at least 1.3:1 with respect to the other isomer; and subjecting the mixture to crystallization to form a composition comprising the cis9, trans11 and trans10, cis12 isomers in which one of the cis9, trans11 and trans10, cis12 isomers is present at a second weight ratio Y with respect to the other isomer, wherein Y is greater than X.

Abstract: Described herein are methods for making retinoids. Also described herein are retinoids and methods of use thereof.

Abstract: An oral pharmaceutical composition of isotretinoin containing at least two lipidic excipients, one of them being hydrophilic (i.e.

Abstract: The use of sterculic acid, and the pharmaceutically acceptable salt forms thereof, described for the treatment of inflammation, in particular, 7-ketocholesterol induced inflammation, 7-keto-cholesterol toxicity, and unregulated angiogenesis.

Abstract: The present invention discloses a method of producing triglycerides rich in XOX fat and/or XLX fat, which comprises the steps of heating and dissolving triglycerides (XOX fat and/or XLX fat) which comprise 20 to 60 mass % of a triglyceride having a saturated fatty acid residue on each of the first and third position and an oleoyl group and/or a linoleoyl group on the second position in total triglycerides in the presence of 1 to 30 mass % of a fatty acid lower alkyl ester; and then cooling the mixture to precipitate crystals and conducting solid-liquid separation. This method is a more efficient and industrially suitable fractionation and production method of fats and oils which are rich in a triglyceride (XOX fat and/or XLX fat) having a saturated fatty acid residue on each of the first and third position and an oleoyl group and/or a linoleoyl group on the second position.

Abstract: Compositions and methods of using compositions that induce UBE1L or a ubiquitin-like protein ISG15, or inhibit a deconjugase UBP43 to degrade oncogenic proteins and enhance apoptosis of cancer (neoplastic) or pre-cancerous (pre-neoplastic) cells are provided. Methods for the prevention or treatment of cancer via administration of these compositions are also provided.

Abstract: A method for stabilizing retinoic acid is provided. The method includes a step of mixing retinoic acid with a hydrophobic polymer/hydrophilic polymer adduct in the presence of an oxygen containing atmosphere to form a retinoic acid containing composition. The hydrophobic polymer/hydrophilic polymer adduct comprises a poly(vinylpyrrolidone/alkylene) polymer and a polymer comprising repeating carboxylic acid groups, hydroxyl groups, or a mixture of carboxylic acid groups and hydroxyl groups. A retinoic acid containing composition and a method of using a retinoic acid containing composition are provided.

Abstract: The invention relates to trans carotenoid salt compounds, methods for making them, methods for solubilizing them and uses thereof. These compounds are useful in improving diffusivity of oxygen between red blood cells and body tissues in mammals including humans.

Abstract: Described herein are the use of peripheral blood derived germline stem cells and their progenitors, methods of isolation thereof, and methods of use thereof.

Abstract: The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids.

Abstract: A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.

Abstract: Some aspects of the invention provide for essential fatty acids which are substituted in specific positions to slow down oxidative damage by Reactive Oxygen Species (ROS), and to suppress the rate of consequent formation of reactive products, for the purpose of preventing or reducing the damage associated with oxidative stress associated diseases such as neurological diseases and age-related macular degeneration (AMD).

Abstract: The subject application provides an aqueous composition suitable for use as an artificial tear solution comprising one or more lipids produced by an enzyme of the diacylglycerol acyltransferase 2 (DGAT2) family and/or the acyl-CoA cholesterol acytransferase (ACAT) family. This invention also provides related methods.

Abstract: The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.

Abstract: The present invention relates to a photochromic material comprising a proteorhodopsin apoprotein and a retinal analog. In one embodiment, the retinal analog is an azulenic retinoid compound. In another embodiment, the retinal analog is a compound that is structurally similarly to all-trans-retinal. The proteorhodopsin apoprotein and the retinal analog form a photochromic material having different spectral properties from those of a corresponding photochromic material formed by the same proteorhodopsin apoprotein and all-trans-retinal. In one embodiment of the application, the retinal analog-containing proteorhodopsin has an absorbance spectrum that does not overlap significantly with that of all-trans-retinal-containing proteorhodopsin. In another embodiment of the application, the retinal analog-containing proteorhodopsin yields a red-shifted visual chromophore compared with the all-trans-retinal-containing proteorhodopsin chromophore.

Abstract: A novel composition and methods of its use and preparation of polybasic metal carboxylate complexes having the general formula: (A)2M.nD(OH)2.xH2O.m(B)2N wherein: A is an organic fatty acid and is selected from the group consisting of saturated C12-24 carboxylic acids, unsaturated C12-24 carboxylic acids, aromatic C12-24 carboxylic acids, alicyclic C12-24 carboxylic acids, polycarboxylic acid derivatives thereof, anhydride derivatives thereof and blends thereof, preferably stearate; M is a divalent metal cation, preferably calcium; n is a fractional or whole number from about 1 to about 10 inclusive; D is an alkali earth metal, preferably calcium; x is a fractional or whole number from about 0 to about 3 inclusive; N is a divalent metal cation other than calcium, preferably zinc; and m is a fractional or whole number from 0 to about 1.

Abstract: Compounds of formula (I); wherein R1 and R2 are the same or different and may be selected from the group consisting of a hydrogen atom, a hydroxy group, an alkyl group, a halogen atom, an alkoxy group, an acyloxy group, an acyl group, an alkenyl group, an alkynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, an alkylsulfinyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; and X represents a carboxylic acid group, a carboxylate group, or a carboxamide group; or any pharmaceutically acceptable salt, solvate, complex or pro-drug thereof, with the provisos that the compound of formula (I) is not (all-Z)-4,7,10,13,16,19-docosahexaenoic acid (DHA), alpha-methyl DHA, alpha-methyl DHA methyl ester, alpha-methyl DHA ethyl ester or alpha-hydroxy DHA ethyl ester, are disclosed. A fatty acid composition and a pharmaceutical composition comprising such compounds are also disclosed.

Abstract: The present invention aims to provide a novel agent for treating and/or preventing diabetes which agent can not only control a blood sugar level but also fundamentally treat a patient with type I diabetes suffering from destruction of ? cells and a patient with type II diabetes suffering from dysfunction in insulin secretion. The present invention provides an agent for treating and/or preventing diabetes, the agent containing retinoic acid as an active ingredient. Retinoic acid incorporated as an active ingredient may be all-trans retinoic acid, an isomer thereof, a derivative thereof, a salt thereof or a prodrug thereof. Retinoic acid may be incorporated singly. Alternatively, composite particles of retinoic acid and an appropriate inorganic or organic substance are prepared, and the retinoic acid composite particles may be incorporated.

Abstract: The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6; and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.

Abstract: C-4 substituted retinoic acid analogs, synthesis methods of C-4 substituted retinoic acid analogs and methods of using C-4 substituted retinoic acid analogs to treat various cancers and dermatological diseases and conditions. The C-4 substituted retinoic acid analogs include C-4 all-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-CRA) analogs. The C-4 substituted retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. The C-4 substituted retinoic acid analogs also have ATRA-mimetic activity. The preferred substitutions at C-4 are an azole group, a sulfur, oxygen, or nitrogen containing group, a pyridyl group, an ethinyl group, a cyclopropyl-amine group, an ester group, or a cyano group, or forms, together with the C-4 carbon atom, an oxime, an oxirane or aziridine group.

Abstract: The invention provides a novel process for the preparation of prostaglandins and analogues thereof, and new crystalline intermediates in the process.

Abstract: Disclosed is a process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.

Abstract: The invention relates to a process for conjugating two double bonds separated by a methylene bridge in a long-chain alkene, in which the long-chain alkene is isomerized with an a) imino base, or b) iminophosphorane base, as catalyst.

Abstract: A method of minimizing or reducing the toxicity of a retinoid having a free carboxyl group and the resulting modified retinoids are described. The method comprises the step of esterifying the carboxyl group of the retinoid with a highly sterically hindered compound, which is preferably a secondary or tertiary alcohol. The resulting retinoid esters are rendered much less toxic than the starting or parent retinoid. This process provides a retinoid ester analog of reduced toxicity so that it may be administered orally with minimal side effects and with a much greater therapeutic window. The modified retinoid compounds are useful in the treatment and prophylaxis of all diseases and disorders where retinoid compounds have been shown effective.

Abstract: Disclosed is a process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.

Abstract: The present invention deals with the certain novel esters derived from a specific 36 carbon diol and fatty acids, which unlike other esters are surprisingly stable to hydrolysis and consequently of interest in high and low pH applications.

Abstract: The invention relates to trans carotenoid salt compounds, methods for making them, methods for solubilizing them and uses thereof. These compounds are useful in improving diffusivity of oxygen between red blood cells and body tissues in mammals including humans.

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: C-4 substituted retinoic acid analogs, synthesis methods of C-4 substituted retinoic acid analogs and methods of using C-4 substituted retinoic acid analogs to treat various cancers and dermatological diseases and conditions. The C-4 substituted retinoic acid analogs include C-4 all-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-CRA) analogs. The C-4 substituted retinoic acid analogs inhibit all-trans retinoic acid (ATRA) 4-hydroxylase activity, thereby inhibiting the catabolism of ATRA. The C-4 substituted retinoic acid analogs also have ATRA-mimetic activity. The preferred substitutions at C-4 are an azole group, a sulfur, oxygen, or nitrogen containing group, a pyridyl group, an ethinyl group, a cyclopropyl-amine group, an ester group, or a cyano group, or forms, together with the C-4 carbon atom, an oxime, an oxirane or aziridine group.

Abstract: The present invention deals with the certain novel esters derived from a specific 36 carbon diol and guerbet acids, which unlike other esters are surprisingly stable to hydrolysis and consequently of interest in high and low pH applications.

Abstract: In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.

Abstract: Monoesters, diesters and polyesters are provided wherein both the acid-derived moiety and the alcohol-derived moiety of the esters are carotenoid compounds. The synthetic ester linkage between two or more carotenoids provides new compounds in which the similar and complementary properties of the individual carotenoids are combined. The new all-carotenoid esters may be useful as antioxidants, therapeutic agents, pigmenting ingredients in poultry feed or as coloring agents for fats. The polyesters have the potential to act as molecular wires with unique electrical conductance characteristics. The all-carotenoid esters may be prepared from the esterification of at least one hydroxy carotenoid with at least one carboxylic carotenoid, or via the reaction of the acid chloride of a carboxylic carotenoid with a hydroxy carotenoid. Preferred hydroxy carotenoids include lutein, zeaxanthin, cryptoxanthin, violaxanthin, carotene diol, hydroxy carotene, hydroxylycopene, alloxanthin and dehydrocryptoxanthin.

Abstract: Compositions and methods of using conjugated linoleic acid preparations enriched for the t10,c12 and c9,t11 isomers are disclosed. It is found that preparations of conjugated linoleic acid containing a ratio of t10,c12 to c9,t11 of about greater than 1.2:1 are desirable for a wide variety of nutritional, therapeutic and pharmacologic uses.

Abstract: There is disclosed a fuel lubricity additive, made by a two-step process wherein the first step is co-reacting an unsaturated base oil, predominantly from vegetable oil sources, and a compound having a diene structure and a carboxylic acid group, wherein the second step is esterifying or amidifying the free carboxylic acid group of anhydride group with a poly-hydroxy-containing compound or poly-amine compound to form the final fuel lubricity additive useful in diesel fuels. The inventive fuel lubricity additive also is useful as a dispersant.

Abstract: Compositions and methods of using conjugated linoleic acid preparations enriched for the t10,c12 and c9,t11 isomers are disclosed. It is found that preparations of conjugated linoleic acid containing a ratio of t10,c12 to c9,t11 of about greater than 1.2:1 are desirable for a wide variety of nutritional, therapeutic and phatmacologic uses.

Abstract: An optically active bisoxazoline compound of the formula [I]: ##STR1## wherein R.sub.1 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted or alkoxy group and two geminal alkyl groups may be joined together to form a cyclic structure;R.sub.2 represents alkyl group, cycloalkyl group, aralkyl group, phenyl group which may be substituted;R.sub.3 represents hydrogen atom, (C2-C4)alkyl group or cycloalkyl group; andthe asterisk * represents an asymmetric carbon atom.

Abstract: This invention relates to the novel retinoyloxy(aryl-substituted)-alkylene butyrate compounds of Formula (I) and pharmaceutical compositions containing same, to methods of treating, preventing or ameliorating cancer and other proliferative diseases in a subject in need of such treatment comprising administering a compound of Formula (I) and pharmaceutically-acceptable salts and prodrugs thereof. ##STR1## The compounds of the invention are also useful in methods of inhibiting histone deacetylase, ameliorating wrinkles, treating or ameliorating dermatological disorders, inducing wound healing, treating cutaneous ulcers and treating gastrointestinal disorders.

Abstract: A method of inhibiting parasitic activity is disclosed in which the biosynthesis, structure and/or function of the glycosyl phosphatidylinositol (GPI) anchor of said parasite may be affected by incorporating into said GPI anchor selected analogs of myristic acid containing various heteroatoms, substituents and unsaturated bonds, including ester-containing analogs, ketocarbonyl-containing analogs, sulfur-containing analogs, double bond- and triple bond-containing analogs, aromatic moiety-containing analogs, nitrated analogs and halogenated analogs.

Abstract: This invention relates to the novel compounds of Formula (I) and pharmaceutical compositions containing same, to methods of treating, preventing or ameliorating cancer and other proliferative diseases in a subject in need of such treatment comprising administering a compound of Formula (I) and pharmaceutically-acceptable salts and prodrugs thereof. ##STR1## The compounds of the invention are also useful in methods of ameliorating wrinkles, inducing wound healing, treating cutaneous ulcers and treating gastrointestinal disorders.

Abstract: A dental material based on polymerizable monomers is described which contains at least one polymerizable monomer which has liquid crystalline properties. Compared with traditional materials, the dental material displays a lower decrease in volume upon polymerization and, because of its low viscosity, higher filler contents can be achieved.

Abstract: Esters and amides of 9-cis-retinoic acid are synthesized, formulated into pharmaceutically acceptable carriers and administered for the treatment of acne vulgaris, cystic acne, hyper-pigmentation, hypo-pigmentation, psoriasis, dermal and epidermal hypoplasia and kerotoses, the reduction of wrinkling of the skin as an incident of aging and actinic damage, normalization of the production of sebum, the reduction of enlarged pores, promoting the rate of wound healing, limiting of scar tissue formation during healing and the like. They are additionally useful for treatment or amelioration of the same additional classes of skin disorders as is retinoic acid itself and other retinoids. These disorders include ichthyoses (e.g., ichthyosis hystrix, epidermolytic hyperkeratosis, and lamellar ichthyosis), follicular disorders (e.g., pseudofolliculites, senile comedones, nevus comidonicas, and trichostatis spinulosa), benign epithelial tumors (e.g.

Abstract: Methods for stereospecific synthesis of 9-cis olefins and retinoids. In one particular aspect, a cis olefin is generated via a lactol ring opening with complete retention of double bond configuration.

Abstract: A method of synthesizing 9-cis-retinoic acid, all-trans-retinoic acid or 9-nor-retinoic acid is disclosed. The method comprises the steps of adding a Grignard reagent of ##STR1## to 2,2,6 trimethyl cyclohexanone is disclosed. R is a methyl group or H and the CH.sub.2 --OH group is in either the cis or trans orientation relative to the HC.tbd.C- group. The resulting product is converted into retinoic acid. In the preferable form of the present invention, a tritium-labelled retinoic acid is synthesized, wherein the labelling is at the C.sub.20 position. A preparation of tritium-labelled 9-cis-retinoic acid with a specific activity of greater than 65 Ci/mmol is also enclosed. In a most preferred embodiment, the specific activity is greater than 75 Ci/mmol.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and poiyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.