Abstract: Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

Abstract: Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: The invention provides a novel class of compounds viz. generally lipopeptides like Pam3CSK4, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness a vaccine.

Abstract: A composition for reconstruction, replacement or repair of damaged or diseased biological tissue comprising an extracellular matrix (ECM) composition that includes an ECM scaffold component derived from a mammalian source and at least one additional bioactive component selected from the group consisting of a statin and a chitin derivative.

Abstract: Compositions and methods are provided for the treatment of IL-17-type inflammatory demyelinating diseases with inhibitors of granulocyte function, e.g. elastase inhibitors. Diseases of interest include multiple sclerosis, neuromyelitis optica, animal models of such diseases, etc. In some embodiments pharmaceutical formulations comprising an elastase inhibitor in an effective dose for treatment of IL-17-type inflammatory demyelinating disease and a pharmaceutically acceptable excipient are provided. Patients may be classified into subtypes prior to treatment, which subtypes are informative of the patient's need for therapy and responsiveness to a therapy of interest.

Abstract: The present invention provides stable non-crystalline aspirin that does not crystallize at room temperature during storage for prolonged periods of time and processes for obtaining the stable non-crystalline aspirin.

Abstract: Methods are provided for treating and preventing renal disease in a subject by administering a gamma secretase inhibitor or a Notch pathway inhibitor to the subject.

Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with cardiovascular diseases, particularly coronary heart disease (especially myocardial infarction) or hypertension. For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection.

Abstract: The invention provides novel compounds and formulations of turmeric oil, fish oil, aspirin and anti-cancer drugs (paclitaxel) having anti-inflammatory, analgesic and/or anti-cancer activity.

Abstract: The present invention relates to stilbene and quinine compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis- or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BBOC amino acid esters are formed with the phenolic hydroxyl at the 3 -position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior stilbenes.

Abstract: Here described are compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

Abstract: The present invention relates to novel carboxylic acid-substituted idebenone derivatives, skin treatment compositions containing these carboxylic acid-substituted idebenone derivatives, methods of treating skin changes by topical application of these carboxylic acid-substituted idebenone derivatives, and their methods of synthesis. The carboxylic acid-substituted idebenone derivatives of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the carboxylic acid-substituted idebenone derivatives of the present invention have an antioxidant effect that is useful in treating a skin change.

Abstract: This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.

Abstract: Compositions and methods for managing or treating chronic pain are provided. More particularly, methods are provided for managing or treating chronic pain by administering to a patient in need thereof an effective amount of propofol or a propofol derivative having limited anesthetic properties. Methods of modulating HCN channel gating are also provided. Pharmaceutically acceptable compositions for, e.g., modulating HCN channel gating are further provided.

Abstract: Disclosed are edible formulations, for example, edible films and gummi confectioneries, that mask the taste of semen. The films and confectioneries include a composition that upon activation in the oral cavity provides a lasting taste masking effect that endures for up to 20 minutes. The composition includes a film former or gelling agent, an effective amount of a protein masker, and an effective amount of a bitter masker. The composition may also include a flavoring agent, sweetening agents, and sensates.

Abstract: A method of preventing or inhibiting L-cystine crystallization is disclosed, using the compounds of formula I: R1a—[O]v-(-A-L-)m-A-[O]v—R1b??I wherein A, L, R1a, R1b, m, and v are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to L-cystine crystallization, such as comprising (but not limited to) kidney stones.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: This present invention provides methods and pharmaceutical compositions for the treatment or prophylaxis of diabetes and related disorders, comprising the administration of an effective amount of a monoester of probucol, particularly the monosuccinic acid ester, or a pharmaceutically acceptable salt or derivative thereof.

Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or a group of formula COR4, or R1 represents a group of formula (A): R2 represents a group of formula NR5R6, or R2 represents a nitrogen-containing heterocyclic group, an aryl group or a heteroaryl group, R3 represents a hydrogen atom or an alkyl group, m represents an integer between 1 and 6 inclusive, n represents 0, 1 or 2, their optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating and/or preventing thrombotic events.

Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.

Abstract: This invention provides a method of synthesizing new active compounds for pharmaceutical uses including cancer treatment, wherein the cancers comprise breast, leukocytic, liver, ovarian, bladder, prostatic, skin, bone, brain, leukemia, lung, colon, CNS, melanoma, renal, cervical, esophageal, testicular, spleenic, kidney, lymphatic, pancreatic, stomach and thyroid cancers. This invention is an anti adhesion therapy which uses the compound as a mediator or inhibitor of adhesion proteins and angiopoietins. It inhibits excess adhesion and inhibits cell attachment. It modulates angiogenesis. The compounds also use as mediator of cell adhesion receptor, cell circulating, cell moving and inflammatory diseases.

Abstract: Methods for preparing a poly(ether carbonates) of the formula HO—[(CH2CH2—O)n—CO2]m—(CH2CH2—O)n—H are provided. The method comprises polymerizing an activated oligomer of the formula of H—O—(CH2CH2—O)n—CO2—Z, where Z is reactive leaving group.

Abstract: Organosiloxanes containing ester derivatives of ascorbic acid are disclosed having the formula (RiSiO)11Ro-Ii)Si—X-A wherein R is an alkyl group containing 1 to 6 carbon atoms, n is 1 to 3 inclusive, X is a divalent organic linking group, A is an ester derivative of ascorbic acid. A method of making an organosiloxane containing ester derivatives of ascorbic acid and the products prepared according to the method arc also taught. The compounds and compositions of the present disclosure are useful to affect tissue lightening when applied topically to keratinaceous tissue.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.

Abstract: The present invention relates to compounds of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention also relates to the use of compound of general formula I for the treatment of malignancy by inhibition of PI3-Akt pathway and or induction of NO. The present invention further relates to a method of treating malignancy by inhibition of PI3-Akt pathway and or induction of NO by administration of compound or said composition to a mammal in need thereof.

Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.

Abstract: The present invention relates to a xanthophyll composition containing (trans, meso)-zeaxanthin), (trans, R,R)-zeaxanthin and (trans, R,R)-lutein useful for nutrition and health care and a process for its preparation. More particularly, the invention relates to a xanthophylls composition containing at least 80% by weight of total xanthophylls, out of which the (trans,3R,3?S, meso)-zeaxanthin content is at least 80%, the remaining being (trans, R,R)-zeaxanthin, (trans, R,R)-lutein and trace amounts of other carotenoids. This invention further provides a xanthophyll composition containing at least 80% by weight of total xanthophylls, out of which at least 50% being (trans, R,R)-zeaxanthin, the remaining being (trans,3R,3?S, meso)-zeaxanthin, (trans, R,R)-lutein and trace amounts of other carotenoids.

Abstract: The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are hexafluoro-honokiol analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. Representative hexafluoro-honokiol analogs include hexafluoro-honokiol, analogs in which one or both hydroxy groups are replaced with dichloroacetate esters, and analogs with increased fluorination. The compounds are believed to function, at least, by inhibiting angiogenesis and/or inducing apoptosis. Thus, the compounds are novel therapeutic agents for a variety of cancers.

Abstract: A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having low content in impurities.

Abstract: The present invention relates to a pharmaceutical composition comprising: a) at least one iron uptake inhibitor, and b) at least one vitamin D and/or at least one analog thereof and/or at least one vitamin D receptor modulator, and optionally a pharmaceutically acceptable carrier.

Abstract: This disclosure concerns novel methods for preventing or treating neurological or neurodegenerative diseases or disorders by using kombo butter acid enriched extracts derived from the seeds of African nutmeg, the main active compounds isolated from the extracts, namely sargaquinoic acid, sargachromenol, and sargahydroquinoic acid, or synthetic analogs or derivatives thereof, as neuroprotective agents. The methods for preparing the kombo butter or kombo butter acid extracts and the methods for isolating and purifying the active compounds and for preparing their acetylated derivatives are also described.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: The present invention relates to novel carboxylic acid-substituted idebenone derivatives, skin treatment compositions containing these carboxylic acid-substituted idebenone derivatives, methods of treating skin changes by topical application of these carboxylic acid-substituted idebenone derivatives, and their methods of synthesis. The carboxylic acid-substituted idebenone derivatives of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the carboxylic acid-substituted idebenone derivatives of the present invention have an antioxidant effect that is useful in treating a skin change.

Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed therein. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustain release of the statin and facilitate bone formation and repair of the fracture site.

Abstract: Osteoconductive matrices and methods are provided that have one or more statins disposed in calcium phosphate particles. The matrices may be injected into a fracture site. The osteoconductive matrices provided allow for sustained release of the statin and facilitate bone formation and repair of the fracture site.

Abstract: Apocynin derivative compounds, active pharmaceutical ingredients, dosage forms, and methods of use thereof as neuroprotectants in the brain of mammals.

Abstract: The present invention provides oral pravastatin formulations comprising a physical mixture of pravastatin and at least one pharmaceutically-acceptable excipient, wherein the composition for at least 6 months after its preparation is stable and has a pH of greater than about 7 to less than 9, as well as methods for the preparation and use of these stable formulations.

Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.

Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.

Abstract: Disclosed herein are stabilized aqueous formulations comprising a ubiquinol ester/diester or resveratrol ester, and a micelle-forming surfactant, and methods for preparing the formulations. In one embodiment, the formulation remains substantially clear and stable when stored at or below room temperature for a period of at least 12 months.

Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.

Abstract: Methods for delivering a biologically active agent into the body of a mammal are provided, the method comprising administering a carbamate-containing conjugate to the mammal.

Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.

Abstract: [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.

Abstract: Compositions containing one or more derivatives of essential oil compounds for use in personal care compositions, such as compositions for oral, throat and skin care are disclosed. These derivatives include acetals of parent essential oil aldehydes and ketones; esters or ethers of parent essential oil alcohols and phenolics; and esters of parent essential oil acids. Examples of parent essential oil aldehydes and ketones include citral, cinnamic aldehyde, ?-anisaldehyde, vanillin, ethyl vanillin, heliotropin, carvone, and menthone. Examples of parent essential oil alcohols and phenolics include thymol, eugenol, isoeugenol, dihydroeugenol, carvacrol, carveol, geraniol, nerol, vanillyl alcohol, heliotropyl alcohol, ?-anisyl alcohol, cinnamyl alcohol and ?-ionol. Examples of parent essential oil acids include ?-anisic acid, cinnamic acid, vanillic acid and geranic acid.

Abstract: Compounds and pharmaceutical compositions containing such compounds having formula I are provided: where R1, R2a, R2b, R3, R4, and R5 are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including anxiety and mood disorders such as depression.