Abstract: A process prepares a polymer-coated hard shell capsule, suitable as container for pharmaceutical or nutraceutical biologically active ingredients. The hard shell capsule can include a body and a cap. In the closed state, the cap overlaps the body either in a pre-locked state or in a final-locked state. The hard shell capsule can be provided in the pre-locked state and spray-coated with a coating solution, suspension, or dispersion that includes a polymer or a mixture of polymers to create a coating layer which covers the outer surface of the hard shell capsule in the pre-locked state.

Abstract: A system, method and corresponding software product are presented, the method comprising: providing a training data set comprising one or more spectrogram data pieces obtained from a plurality of individuals and respective data on a selected set of blood biomarkers of said individuals; selecting one or more groups of biomarkers selected from said selected set of biomarkers, wherein each group includes two or more (three or more) biomarkers; training one or more prediction models based on said training data, said one or more prediction model comprising one or more prediction routes for prediction of said one or more groups of biomarkers respectively. Accordingly, the prediction model comprises a selected number of prediction routes, each trained for predicting biomarkers concentrations of a respective groups of biomarkers.

Abstract: This invention relates to xanthine derivative compounds that are inhibitors of BET bromodomains proteins, the method of preparation thereof and applications thereof.

Abstract: The invention relates to pharmaceutical compositions comprising 6-thioguanidine (6-TG) wherein the composition is formulated for release of 6-TG in the distal intestine. Methods for treating a disease or condition of the distal ileum that responds to 6-TG wherein the 6-TG is released in the distal intestine are also disclosed.

Abstract: The present invention relates to solid dispersion of Naloxegol oxalate. Further, the present invention relates to an improved process for Naloxegol oxalate and intermediates thereof.

Abstract: Methods and kits for improving tear production are described, along with topical pharmaceutical compositions. In certain instances the composition comprises pentoxifylline and a pharmaceutically acceptable carrier. The compositions also may further comprise another active agent, such as an anti-bacterial agent, antiviral agent, antifungal agent, or immunosuppressant agent, and combinations thereof.

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Abstract: The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

Abstract: A silicone gel (“silogel”) composition used to deliver pharmaceutical products transdermally as well as a method for producing the silogel composition, which may contain up to 80% additive ingredients. Preferred embodiments of the invention may include silogel compositions which provide high viscosity/no separation due to API. They are not temperature-sensitive, have no shear stress from the ointment mill/EMP, have no gumming up/stickiness, and no hardening.

Abstract: This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: wherein the values of R1, R2, R3, R4, R5, Y1 and Y2 are described herein.

Abstract: The present invention relates, in general, to fibroproliferative disorders, and, in particular, to methods and compositions for treating fibroproliferative disorders by administering to a mammal in need of treatment pharmacologically effective doses of a phosphodiesterase inhibitor, such as pentoxifylline, and an anti-oxidant which is a precursor of glutathione, such as N-acetyl-cysteine, or their derivatives or metabolites.

Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for treating or preventing inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia, improves blood flow through peripheral blood vessels and therefore helps with blood circulation in the arms and legs (e.g.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of chronic diseases and inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Abstract: The present invention is directed to methods and compositions employing 9-(4-hydroxy-2-(hydroxymethyl)butyl)guanine (“H2G”) or derivatives or analogs thereof for the treatment of viral diseases, as well as for the treatment of other conditions, including, but not limited to, cancer, chronic fatigue syndrome, Alzheimer's disease, multiple sclerosis and Graves' disease. The H2G or derivative or analog thereof can be administered in a pharmaceutical composition and can be administered with an additional antiviral therapeutic agent or another agent for the treatment of other conditions.

Abstract: The present invention relates to pharmaceutical formulations comprising xanthine or xanthine derivatives, kits thereof, and methods for treating fibrotic diseases by local administration.

Abstract: The present invention in one embodiment relates to a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein: each of R1 and R2 is independently selected from —CH3 and —CD3; R3 is hydrogen or deuterium; each of Z1, Z2 and Z3 is independently selected from hydrogen and deuterium; each Z4 is hydrogen or deuterium; each Z5 is hydrogen or deuterium; and each Z6 is hydrogen or deuterium.

Abstract: The invention provides compositions and methods for determining GLP-1 analog and/or DPPIV inhibitor response in a subject. In one embodiment, the composition comprises a solid support comprising probes for measuring a biomarker panel comprising, for example, adiponectin, C-peptide, hsCRP, insulin, proinsulin. The simultaneous use of multiple biomarkers with independent classification power will increase the performance of the biomarker panel in characterizing GLP-1 analog and DPPIV inhibitor response. The invention also provides methods of treating a subject (e.g. one experiencing cardiodiabetes) and determining the efficacy of a therapy through assaying the various biomarkers of a biomarker panel disclosed herein.

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 a new application of phosphodiesterase inhibitors for couple infertility treatment which forms an effective alternative to the invasive assisted reproductive techniques such as conjugal artificial insemination and which consists of the transvaginal administration of a phosphodiesterase inhibitor immediately before and/or after coitus. It also relates to dosage forms suitable for the intravaginal administration of phosphodiesterase inhibitors.

Abstract: Provided herein are diagnostic markers and uses thereof for predicting if a subject is at risk of a major adverse event. In particular, one aspect provided herein relates to methods to determine if a subject is at risk of having a major adverse effect by measuring at least 2, or at least 3 of the biomarkers beta 2 microglobulin, c-reactive protein and cystatin C.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a severe pain in an individual using such pharmaceutical compositions.

Abstract: A composition comprising at least one physiologically tolerated film-forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I or a stereoisomeric form or a physiologically tolerated salt of any of the foregoing. The composition is suitable for treatment of androgenic alopecia or hirsutism, that is, for avoiding undesirable hair growth, and for treatment of seborrhea and acne, and can furthermore be employed in cosmetics.

Abstract: The invention discloses a gastric resistant pharmaceutical or nutraceutical composition, comprising a core, comprising a pharmaceutical or nutraceutical active ingredient and a gastric resistant coating layer onto the core, wherein the gastric resistant coating layer comprises at least 30% by weight of a (meth)acrylate copolymer comprising polymerized units of 10 to 40% by weight of acrylic or methacrylic acid, 10 to 80% by weight of a C4- to C18-alkyl ester of acrylic or methacrylic acid and optionally 0 to 60% by weight of another vinylic monomer, whereby the release of the pharmaceutical or nutraceutical active ingredient is not more than 10% under in-vitro conditions at pH 1.2 after 2 hours in medium according to USP with and without the addition of 20% (v/v) ethanol.

Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

Abstract: Provided are materials and methods for the prevention and treatment of Juvenile Neuronal Ceroid Lipofuscinosis comprising administration of an effective amount of at least one of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor. In some embodiments, the methods comprise administration of an effective amount of each of a hemi-channel inhibitor and a phosphodiesterase-4 inhibitor. Also provided are pharmaceutical compositions comprising a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor, as well as kits comprising at least one effective dose of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor or a combination of both.

Abstract: This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: wherein the values of R1, R2, R3, R4, R5, Y1 and Y2 are described herein.

Abstract: Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed.

Abstract: This invention relates generally to methods and agents for modulating adiposity-related conditions. More particularly, the present invention relates to the use of TRAIL death receptor agonists, including nucleic acids such as TRAIL polynucleotides, peptides and polypeptides including TRAIL polypeptides, TRAIL DR agonist antigen-binding molecules, TRAIL DR peptide agonists as well as small molecule TRAIL DR agonists in compositions and methods for treating or preventing adiposity-related conditions such as obesity, diabetes mellitus and metabolic syndrome.

Abstract: The invention relates to a coating composition suitable for the coating of pharmaceutical or nutraceutical dosage form, comprising a core comprising one or more pharmaceutical or nutraceutical active ingredients, wherein the coating composition is comprising at least 20% by weight of an enteric core/shell polymer composition derived from an emulsion polymerisation process, wherein the core of the core/shell polymer composition is formed by a water-insoluble, cross-linked polymer or copolymer and the shell of the core/shell polymer composition is formed by an anionic polymer or copolymer.

Abstract: The present invention provides individual crystalline polymorphs of (S)-1-(4,4,6, 6,6-pentadeutero-5-hydroxy-hexyl)-3,7-dimethyl-1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); and (e) thermo gravimetric analysis (TGA).

Abstract: An animal model has been developed based the understanding that a central mechanism in patients with CTRF is that chemotherapy and/or radiation initiates canonical pathways leading to the development of disrupted sleep architecture, resulting in disruption of REM sleep and fatigue and cognitive dysfunction. Drugs that restore the activity patterns and levels towards normal and/or decrease the pro-inflammatory cytokines associated with the disrupted sleep, should be effective in alleviating one or more symptoms of CTRF. Pentoxifylline was demonstrated to improve activity levels in animals treated with etoposide.

Abstract: The present invention relates to the preparation of poly(amino oxalate) (PAOX) using oxalyl chloride, 1,4-cyclohexanedimethanol, and piperazinediethanol, the preparation of biodegradable polymer particles using the PAOX, and the use of PAOX particles as a drug delivery vehicle. The PAOX according to the present invention is a polymer that has three characteristics of biodegradability, biocompatibility, and cationic properties at the same time with appropriate hydrophobicity and thus can be prepared as particles that allow rapid drug release. Moreover, the particles improve the delivery efficiency of a drug into cells and thus can be efficiently used as a drug delivery vehicle for the treatment of acute inflammatory diseases such as acute liver failure and acute lung injury.

Abstract: An animal model has been developed based the understanding that a central mechanism in patients with CTRF is that chemotherapy and/or radiation initiates canonical pathways leading to the development of disrupted sleep architecture, resulting in disruption of REM sleep and fatigue and cognitive dysfunction. Drugs that restore the activity patterns and levels towards normal and/or decrease the pro-inflammatory cytokines associated with the disrupted sleep, should be effective in alleviating one or more symptoms of CTRF. Pentoxifylline was demonstrated to improve activity levels in animals treated with etoposide.

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by one of the following structural formulas: wherein the values of R1, R2, Y1 and Y2 are described herein.

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.

Abstract: Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

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 invention is based upon the discovery that red blood cells contain phosphodiesterase 3B (PDE3B), and that inhibition of that phosphodiesterase allows for an enhanced accumulation of cAMP and subsequent release of ATP. It was further discovered that RBCS treated with insulin accumulate significantly less cAMP and release significantly less ATP than normal RBCS. Likewise, RBCS of patients suffering from type 2 diabetes (hyperinsulinemia) accumulate significantly less cAMP and release significantly less ATP than normal RBCS. It was further discovered that prostaglandin analogues synergistically work with phosphodiesterase 3B inhibitors to improve or increase cAMP accumulation and ATP release RBCS. Thus the invention is directed to compositions and methods for improving ATP release by RBCS, via administering PDE3B inhibitor or a combination of PDE3B inhibitor and prostaglandin analogue.

Abstract: Disclosed are methods and compositions related to the use of boswellic acids (such as acetyl-11-keto-?-boswellic acid, 11-keto-?-boswellic acid, ?-boswellic acid, acetyl-?-boswellic acid, 9,11-dehydro-?-boswellic acid, acetyl-9,11-dehydro-?-boswellic acid, ?-boswellic acid, acetyl-?-boswellic acid, 11-dehydro-?-boswellic acid, acetyl-9,11-dehydro-?-boswellic acid, lupeolic acid, acetyl lupeolic acid, 12-ursene-2-diketone, incensole, incensole acetate, a derivative, in particular an ester thereof, a pharmaceutically acceptable salt thereof, a combination thereof, or a preparation containing one or more of these compounds) for the human medical or veterinary prophylaxis and/or treatment of: a) damage to and/or inflammation of the islets of Langerhans and/or b) damage to the B-cells of the islets of Langerhans.

Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.

Abstract: The present invention relates to compositions and methods for promoting and enhancing the analgesic, anesthetic and anticonvulsant properties of epoxygenated fatty acids, in particular, epoxy-eicosatrienoic acids (“EETs”) and inhibitors of soluble epoxide hydrolase (“sEH”) in the presence of elevated levels of cyclic adenosine monophosphate (“cAMP”) by combining or co-administering the epoxygenated fatty acid, EET and/or inhibitor of sEH with an agent that increases intracellular levels of cAMP, e.g., a phosphodiesterase inhibitor.

Abstract: Provided is a method for determining whether an individual is likely to be susceptible to radiation pneumonitis from radiation therapy and for developing a treatment based on the determination of susceptibility. The method involves measuring SOD and GPX activity levels. A high SOD or low GPX activity, or a combination thereof, is indicative that the individual is likely to be susceptible to radiation pneumonitis.

Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.

Abstract: The invention relates to methods of treating or preventing pathological cardiac remodeling and/or preventing heart failure. These methods include the administration of a PDE1 inhibitor to a patient under conditions effective to treat or prevent pathological cardiac remodeling, and therefore heart failure that occurs as a result of such remodeling. Pharmaceutical compositions and delivery vehicles that can be used in the methods of the present invention are also disclosed herein.

Abstract: A pharmaceutical dermatological composition based on Pentoxifylline, to be applied on the skin in the form of a cream, gel, unguent, solution, in an emulsion, in liposomes and in microcapsules, being selective for the vascular disorders of rosacea and disorders with photosensitivity, reducing the blood vessels and the reactions of reddening of the skin, CHARACTERIZED in that said composition consists of: from 1% to 99% of Pentoxifylline, from 0.1% to 80% of base cream and from 0.1% to 75% of liposomes.

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.