Abstract: This invention is in the field of chemical restructuring of pharmaceutical agents known to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the anthracyclines, doxorubicin and daunorubicin, that are found to reduce levels of the pharmaceutical agent in noncancerous tissues. There orotate derivatives are equally efficacious in inhibiting the SCCAKI-1 kidney tumor in animals and the reduction in the heart tissue of doxorubicin compared with doxorubicin HCl suggests a reduction in toxicity induced by free radical generation by the anthrracyclines.

Abstract: The instant invention provides preparations comprising an oxidizing antimicrobial agent such as chlorine dioxide and a heterocyclic compound that improves the antibacterial effect of the oxidizing antimicrobial agent preparation. The invention has particular use as an eye care preparation such as an eye drop. The invention further provides methods for reducing bacterial colonization and treating infection.

Abstract: A composition protects against, minimizes the effects of, and hastens recovery from the typical symptoms associated with an alcohol induced hangover. The composition includes superoxide dismutase (SOD), and prickly pear cactus (OFI). In addition, sesamin and alpha-lipoic acid work with the SOD and OFI for enhanced antioxidant and therapeutic effects. Other ingredients can be added to the composition for additional treatment of symptoms.

Abstract: A delivery system for ingestible components is described. The delivery system comprises at least one orally soluble film but often comprises more than one orally soluble film. The orally soluble films within the delivery system comprise a different biologically active component or mixture of biologically active components so that a consumer can ingest more than one active at a single time. Often, the biologically active components are agents isolated from tea.

Abstract: A delivery system for ingestible components is described. The delivery system comprises at least one orally soluble film but often comprises more than one orally soluble film. The orally soluble films within the delivery system comprise a different biologically active component or mixture of biologically active components so that a consumer can ingest more than one active at a single time. Often, the biologically active components are agents isolated from tea.

Abstract: The invention relates to methods and compounds for treating chemotherapy-induced anemia. In particular, methods for treating chemotherapy-induced anemia in subjects refractory to treatment with recombinant human erythropoietin are encompassed herein.

Abstract: This invention relates to the use of prodrug for the manufacture of a medicament useful for treating an ocular disease affecting the posterior segment of the eye, in a subject in need thereof, wherein the prodrug is a composition injected into the vitreous body, and the frequency of injections does not exceed one injection per month.

Abstract: The present invention provides pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of acyclovir (ACV) to at least one target tissue. The present invention also provides methods of treating viral infection in at least one target tissue of a patient by iontophoretically delivering a formulation of the invention to the infected target tissues of the patient.

Abstract: The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula (I) are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods. wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene.

Abstract: Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS. 2 and 4, respectively, and are represented by the formula: Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

Abstract: A tablet for oral administration of nutritional indium comprises about 10–50 mg indium sulfate, about 4–20 mg caffeine, about 2–10% by weight cocoa powder, and about 5–10% by weight ethyl cellulose, in combination with about 50–150 ?g of each of zinc oxide, copper (II) oxide, magnesium oxide, potassium iodide, selenium amino acid chelate, chromium amino acid chelate and manganese amino acid chelate.

Abstract: A composition that will substantially reduce the deleterious effects of alcohol on the body and substantially reduce the side effects associated with hangovers (i.e. headaches, dizziness, nausea, dry mouth, etc) when taken as recommended. The composition includes an effective amount of (I)-glycine, (I)-glutathione, thiamine, magnesium, selenium, molybdenum. Other vitamins, mineral compounds, flavoring, coloring, and solubility agents may also be added.

Abstract: A composition for the topical treatment of sores, lesions, ulcers, and other disorders of the skin, said composition includes a combination of a bee product and caffeine. The bee product may comprise bee pollen, bee propolis, honey, or royal jelly. Variations of the composition may also contain a tannin. The composition may be in the form of an ointment or cream that is applied topically to an affected area of the body. The composition may also be used in other forms, such as a spray, shampoo, soap, lipstick, or adhesive bandage. The invention may also be useful as a health beverage.

Abstract: Methods of treating migrainous headaches and their associated symptoms are provided by administering a composition comprising parthenolide or feverfew transdermally to a patient in need thereof. Treatments are surprisingly effective with low total administered amounts of parthenolide or feverfew. Compositions and transdermal administration patches are also described.

Abstract: A novel sordarin derivative was isolated from fungal cultures. The compound is useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops. Two novel cultures of fungi, ATCC No. PTA-3862 and ATCC No. PTA-3861 can be used to ferment and produce the present compound.

Abstract: Methods of treating, preventing and/or managing myclodysplastic syndromes are disclosed. Specific methods encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active ingredient, and/or the transplantation of blood or cells. Specific second active ingredients are capable of affecting or blood cell production. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: The present invention is directed to methods and pharmaceutical compositions for treating a mammal suffering from malaria or the sequelae of malarial infection, or for preventing a malarial infection, or for ameliorating the symptoms associated with a malarial infection using a therapeutically effective amount of an agent that down regulates G protein mediated functions. Also contemplated are methods for screening for novel compounds that down regulate G protein receptors, and the use of these compounds for treating mammals having malaria.

Abstract: A pain relief lollipop comprises a candy matrix comprising (a) an opioid agonist, (b) an N-methyl-D-aspartate receptor antagonist different from the opioid agonist, and, optionally, a muscle relaxant, sedative, anxiolytic, and/or antidepressant. A patient can self-administer small amounts of the pain relief drug as needed by simply licking or sucking on the lollipop in response to his subjective experience of pain.

Abstract: The present invention provides a method for treating cancer by promoting apoptosis and reducing clonogenic survival of cancer cells. The method encompasses co-administering 1) a cell cycle checkpoint abrogation agent (for example, UCN-01 or caffeine) and 2) an inhibitor of a compensatory cytoprotective pathway, such as an agent that inhibits the MEK 1/2 pathway (e.g. PD98059, U0126, or PD184352) or an agent that inhibits the PI 3 pathway (e.g. LIY294002 or wortmanin). In addition, because the co-administration step also radiosensitizes cancer cells, the method additionally encompasses the administration of radiation to further reduce clonogenic survival of cancer cells. The method promotes apoptosis and reduces clonogenic survival in many types of cancer cells, including leukemia cells, prostate cancer cells, breast cancer cells, myeloma cells, and lymphoma cells.

Abstract: This invention relates to the administration of ingredients which reduce the appetite, promote weight loss and increase energy using rapidly dissolving films or strips. The benefits of the invention may be achieved through a variety of different mechanisms including addition of active ingredients, including ingredients which alter taste, promote satiety and boost energy, to the rapidly dissolving strips.

Abstract: The present invention provides methods of treating proliferative disease in a patient (e.g., a mammal such as a human) in need of such treatment, said treatment comprising administering, concurrently or sequentially, an effective amount of (1) an anti-platelet or anti-clotting agent and (2) an anti-neoplastic agent and/or radiation therapy. A second method of treatment comprises administering Plavix, also known as clopidogrel, or SR 25909 to a patient in need of such treatment. An additional method comprises administering an anti-platelet or anti-clotting agent to an individual at risk for developing proliferative disease. The methods of the present invention are particularly useful for the treatment or prevention of various cancers, especially epithelial cancers, e.g., prostate cancer, lung cancer, breast cancer, colorectal cancer, and pancreatic cancer.

Abstract: Compositions with synergistic anti-inflammatory effects in inflammatory diseases resulting from activation and consequent degranulation of mast cells and followed by secretion of inflammatory biomolecules from the activated mast cells, composed of a heavily sulfated, non-bovine proteoglycan such as shark cartilage chondroitin sulfate C, an unrefined olive kernel oil/extract that increases absorption of these compositions in various routes of administration, and one or more of a hexosamine sulfate such as D-glucosamine sulfate, a flavone such as quercetin, S-adenosylmethionine, a histamine-1 receptor antagonist, a histamine-3 receptor agonist, an antagonist of the actions of CRH, caffeine, and a polyamine.

Abstract: Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.

Abstract: The present invention provides a medicinal composition comprising (1) a pharmacologically active substance, (2) a drug absorbefacient and (3) a taurine compound or a polyamine. A taurine compound has an efect of suppressing or preventing damage of the intestinal mucous membrane, and therefore adding the taurine compound to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to suppress or prevent damage of the intestinal mucosa. A polyamine improves the absorbability of pharmacologically active substances, and therefore adding the polyamine to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to decrease the dose of the drug absorbefacient, thereby suppressing or preventing damage of the intestinal mucosa.

Abstract: An improved method for using a NNRTI in the treatment of HIV-1 infection, comprising administering to a human, needing treatment for HIV-1 infection, a therapeutically effective amount of said NNRTI or a pharmaceutically acceptable salt thereof, and an amount of an inhibitor of the cytochromes P450 that is sufficient to elevate, enhance, or extend plasma concentrations of said NNRTI.

Abstract: The invention provides the use of an optionally hydroxyl-protected 4-hydroxy or hydroperoxy-3,5-dioxopyrazolidine or an equivalent wherein a pyrazolidine ring attached oxygen is replaced by a sulphur, or a physiologically acceptable salt thereof, for the manufacture of a medicament for use in drug therapy or prophylaxis. Additionally, the invention provides a method of combating HIV infection which comprises administering to an HIV-infected patient a T-lymphocyte growth suppressing agent, preferably a pyrazolidinol, in an amount sufficient to suppress T-lymphocyte growth in said patient for a period sufficient to reduce the T-lymphocyte concentration in lymph nodes in said patient.

Abstract: Methods of treatment and pharmaceutical combinations are provided for the treatment of acute leukemia, such as acute myelogenous leukemia, and myelodysplastic syndrome. The methods of treatment and pharmaceutical combinations employ an anti-CD33 cytotoxic conjugate in combination with at least one compound selected from the group consisting of an anthracycline and a pyrimidine or purine nucleoside analog. Preferred methods of treatment and pharmaceutical combinations employ gemtuzumab ozogamicin, daunorubicin, and cytarabine.

Abstract: Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.

Abstract: The present invention is directed to anti-depressive activity of Crassulaceae special extracts, Carpediol, containing 2-(4-hydroxyphenyl)ethyl-&bgr;-d-glucopyranoside or 3-[6-o-(&agr;-l-arabinopyranosyl)-&bgr;-d-glucopyranosyl]-oxy-1-phenylpropene in mammals, to method of preparation and analysis of these extract, as well to safety of their usage in combination with other drugs.

Abstract: A method for lessening or preventing non-pulmonary ischemia-reperfusion injury or inflammation in a mammal by identifying a mammal which has ischemia-reperfusion or is at risk for developing ischemia-reperfusion in a non-pulmonary tissue; and causing the mammal to inhale a therapeutically effective amount of gaseous nitric oxide sufficient to diminish the ability of leukocytes or platelets to become activated in a manner that contributes to an inflammatory process at the site of the ischemia-reperfusion or inflammation in the non-pulmonary tissue, thereby lessening or preventing non-pulmonary ischemia-reperfusion injury in the mammal.

Abstract: Methods of treating, preventing and/or managing macular degeneration are disclosed. Specific embodiments encompass the administration of an immunomodulatory compound, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and/or surgery. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: Methods of treating, preventing and/or managing macular degeneration are disclosed. Specific embodiments encompass the administration of a selective cytokine inhibitory drug, or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, clathrate, or prodrug thereof, alone or in combination with a second active agent and/or surgery. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: Methods of treating migrainous headaches and their associated symptoms are provided by administering a composition comprising parthenolide or feverfew sublingually to a patient in need thereof. Treatments are surprisingly effective with low total administered amounts of parthenolide or feverfew. Compositions and unit dose systems are also described.

Abstract: The compounds of the invention are modified forms of therapeutic agents. A typical prodrug compound of the invention comprises a therapeutic agent, an oligopeptide, a stabilizing group and, optionally, a linker group. The prodrug is cleavable by the CD10 enzyme. Methods of treatment using the prodrug and methods of designing a prodrug are also disclosed.

Abstract: The invention is both a composition and a method for promoting weight loss in mammals, for promoting thermogenesis in mammals, for increasing metabolism and boosting energy levels in mammals, promoting appetite suppression in mammals, for promoting lean muscle mass in mammals and for a diet supplement. The primary mechanism of action for the invention is that it increases norepinephrine levels, which promotes a rise in metabolism, thus leading to more calories burned and more energy expended primarily through the burning or metabolism of adipose tissue (fat) through lipolysis, without the destruction or metabolism of muscle tissue.

Abstract: Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.

Abstract: Disclosed are pyrrolopyridazine compounds, methods of preparing such compounds, and their use for the treatment of proliferative, inflammatory, and other disorders.

Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.

Abstract: This invention describes a method and composition to enhance the synthesis and release of the neurotransmitters by the oral administration of neurotransmitter precursors, along with natural plant substances that stimulate uptake of the neurotransmitters precursors, while adding natural plant substances that activate adenylate cyclase in order to avoid attenuation and prevent pharmacologic tolerance. The invention describes compositions for a medical foods that are designed to improve cognitive function, induced sleep, a improve Parasympathetic function, improve autonomic balance, increase nitric oxide production, reduce blood pressure, increase blood flow, and treat virus infections. The compositions include amino acids such as choline, herbs such ginkgo biloba, and other foods such as coca.

Abstract: Compositions with synergistic anti-inflammatory effects in inflammatory diseases resulting from activation and consequent degranulation of mast cells and followed by secretion of inflammatory biomolecules from the activated mast cells, composed of a heavily sulfated, non-bovine proteoglycan such as shark cartilage chondroitin sulfate C, and one or more of a hexosamine sulfate such as D-glucosamine sulfate, a flavone such as quercetin, an unrefined kernel olive oil that increases absorption of these compositions in various routes of administration, S-adenosylmethionine, a histamine-1 receptor antagonist, a histamine-3 receptor agonist, an antagonist of the actions of CRH, caffeine, and a polyamine.

Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.

Abstract: The present invention relates to tolerogenic dendritic cells (DCs) and methods for enriching for these cells in tissue preparations and using the cells for preventing or minimizing transplant rejection or for treating or preventing an autoimmune disease.

Abstract: The present invention provides, as a composition that is highly safe and superior in preservative properties, comprising (a) a xanthine, (b) a buffer and (c) at least one member selected from sorbic acid, EDTA, and salts thereof. This composition has superior preservative properties so that it inhibits the generation and proliferation of microorganisms even when stored for a long period of time. Furthermore, the present invention provides a method for enhancing the preservative properties of sorbic acid, EDTA, and salts thereof, which are known to have preservative properties, and the preservative properties of compositions containing these ingredients, and provides a method for producing a composition with superior preservative effectiveness.

Abstract: Compositions and methods for islet neogenesis therapy comprising an EGF and a gastrin in combination with immune suppression, and for treating or preventing early stage diabetes with a gastrin/CCK receptor ligand and an immunosuppressant are provided.

Abstract: The present invention relates to compositions and methods for treating immune system diseases such as rheumatic disease, by administering to a subject soluble CTLA4 molecules that block endogenous B7 molecules from binding their ligands, alone, or in conjunction with other agents including Disease Modifying Anti-Rheumatic Drugs (DMARDs).

Abstract: The present invention relates to an apparatus and method for administering diagnostic and therapeutic agents into a breast duct. A thymidine kinase vector may be administered into a breast duct in conjunction with an acycloguanidine compound for enhanced imaging on PET scanning of the breast to detect breast lesions. The thymidine kinase phosphoraylates the acycloguanidine compound to enhance visibility of lesions on PET scan. An acyclic nucleoside compound may be administered into the breast duct to form phosphorylated adducts that phosphorylate DNA and kill thymidine kinase expressing cancer cells.

Abstract: The present invention relates to combined preparation containing as active substance the following individual components, in the form of a kit-of-parts:

Abstract: A nutritional composition for enhancing alertness comprising:

Abstract: The present invention provides a controlled release device for sustained or pulsatile delivery of pharmaceutically active substances for a predetermined period of time. This invention further provides such device in which sustained or pulsatile delivery is obtained by the unique blend and Inmate mixture of pharmaceutically active substances with a microbial polysaccharide and uncrosslinked linear polymer and optionally a crosslinked polymer and/or lipophillic polymer and/or saturated polyglycolyzed glyceride. The invention also provides a process for the manufacture of such devices and pharmaceutical compositions containing the same.

Abstract: The present invention relates to herbal compositions and methods for regulating body weight, especially for promoting body weight loss, for maintaining or controlling body weight, reducing blood levels of circulating chemical fuels (e.g., glucose, carbohydrates, fatty acids, and cholesterol), facilitating or promoting metabolism, treating diabetes, treating body weight disorders, and the like.