Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, having a low incidence of the development of tolerance and having increased duration of action.

Abstract: In a method for treating lung diseases, a drug formulation is prepared by combining micronized crystalline beclomethasone dipropionate and lactose. The drug formulation is placed into a dry powder inhaler which provides inhalable drug particles having a mass median diameter of about 0.5-5.8 microns. The inhaler is preferably largely flow rate independent. Drug and lactose particles are separated in the inhaler during inhalation, most desirably via a spinning element. Due to deep deposition, the drug particles persist in the lungs for a surprisingly long duration, increasing the therapeutic effect of each dose. The patient inhales the drug particles with an inspiratory flow rate of about 10-60 liters/minute, to produce a deep lung deposition of inhaled particles.

Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6.alpha. and 7.beta. oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6.alpha. and 7.beta. oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and .delta.-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: A dry powder composition comprising one or more potent pharmaceutically active substances and a carrier substance, all of which are in finely divided form, wherein the formulation has a poured bulk density of from 0.28 to 0.38 g/ml is useful in the treatment of respiratory disorders.

Abstract: Compounds of Formula I: ##STR1## wherein: X.sub.1, and X.sub.2 are each independently either O.sup.- or S.sup.- ;X.sub.3 and X.sub.4 are each independently either --H or --OH, with the proviso that X.sub.3 and X.sub.4 are not simultaneously --H;R.sub.1 is selected from the group consisting of O, imido, methylene and dihalomethylene;R.sub.2 is selected from the group consisting of H, halo, alkyl, substituted alkyl, alkoxyl, nitro and azido;R.sub.3 is selected from the group consisting of H, alkyl, acyl, aryl, and arylalkyl; andR.sub.4 is selected from the group consisting of --OR', --SR', --NR', and --NR'R", wherein R' and R" are independently selected from the group consisting of H, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, alkoxyl, and aryloxyl, with the proviso that R' is absent when R.sub.

Abstract: Substances comprising disaccharides and substances comprising carboxylated and/or sulfated oligosaccharides in substantially purified form, and methods of using same, are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of active Tumor Necrosis Factor Alpha (TNF-.alpha.) can be either inhibited or augmented selectively by administration to the host of an effective amount of a substance of the invention. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF-.alpha.. The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be administered daily, at very low effective doses, typically below 0.

Abstract: This invention provides novel indenone derivatives, their pharmaceutical formulations and their use for the inhibition of leukocyte adherence to cells.

Abstract: Secretion of gastric acid and development of ulcers can be inhibited by administering to a patient in need thereof an effective amount of a hot water extract of the cultivated mycelia of Cordyceps sinensis.

Abstract: A medical gas mixture which comprises from 20 to 70% oxygen, from 1 to 10% carbon dioxide and the balance, except for incidental constituents not adversely affecting the basic properties of the gas mixture, being helium. The subject mixtures are useful in the treatment of asthma and in enhancing magnetic resonance imaging.

Abstract: Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.

Abstract: A combination preparation comprising a compound which has a phosphodiesterase-inhibiting action, and a compound which reduces the biologically effective intracellular Ca.sup.2+ content, is suitable for the treatment of immunological diseases.

Abstract: A method to increase cellular MnSOD production in an animal to treat oxidative damage by administering a protein having a thioredoxin active-site in reduced state. A composition and a method to protect an animal from lung disease are provided.

Abstract: The present invention relates to methods and pharmaceutical compositions for decreasing the production of interferon-gamma inducing factor (IGIF). The invention also relates to methods and pharmaceutical compositions for decreasing the production of interferon-gamma (IFN-.gamma.). The compositions comprise a therapeutically effective amount of a compound which inhibits interleukin-1.beta. converting enzyme (ICE) and a pharmaceutically acceptable carrier. The methods comprise the step of administering the above compositions to a subject. The present invention also relates to methods for treating or reducing the advancement, severity or effects of an IGIF- or IFN-.gamma.-mediated inflammatory, infectious or autoimmune condition.

Abstract: A method of treating a mammalian patient suffering from or prone to a condition characterized by late phase allergic reactions, airway hyperresponsiveness or inflammatory reactions, e.g., asthma, allergic rhinitis, allergic dermatitis, allergic conjunctivitis, inflammatory bowel disease or rheumatoid arthritis, comprising the administration to the patient of an oral, parenteral, intrabronchial, topical, intranasal or intraocular pharmaceutical composition containing in each dose about 0.005 to about 1.0 mg per kilogram of patient body weight of ultra-low molecular weight heparins (ULMWH) or other sulfated polysaccharides having average molecular weights of about 1,000-3,000 daltons. Suitable inhalant and other pharmaceutical compositions for use in the novel treatment method are also disclosed.

Abstract: An extract composition derived from the peel of a banana and the method for producing the extract composition. An aqueous solvent is combined with the peel of a banana. If the banana is unripe, a base is also added. The mixture is homogenized and allowed to react at least until a black supernatant appears. The entire slurry is filtered. The resulting extract is used alone or combined with a cream or ointment. Medicinal benefits of the extract include relief from pain, swelling, itching, bruising, wrinkles, and sunburn.

Abstract: Effective amounts of formoterol (and/or a physiologically acceptable salt and/or solvate thereof) and budesonide are used in combination for simultaneous, sequential or separate administration by inhalation in the treatment of respiratory disorder.

Abstract: The invention relates to use of steroids or steroid analogues in the treatment of chronic and acute inflammation of the airways, particularly asthmatic conditions. It also relates to compounds and compositions which modulate airway remodelling. In a preferred embodiment, the steroid is 2-methoxyoestradiol.

Abstract: Methods utilizing descarboethoxyloratadine ("DCL"), for the treatment of allergic disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. Also included are methods for the treatment of allergic asthma using DCL and either a decongestant or a leukotriene inhibitor, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. The invention also encompasses the administration of DCL in a nasal or oral spray.

Abstract: Methods for treating respiratory disease, including cystic fibrosis, emphysema, bronchitis, and sinusitis are presented. Methods comprise administering to a patient an effective amount of DNA in a manner so as not to be effect gene transfer and expression.

Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: A method for treating the disease state in mammals caused by mammalian cells involved in the inflammatory response is disclosed. Mammalian cells participating in the inflammatory response are contacted with an inflammatory response mediator which reduces the undesired inflammatory response and is an antioxidant. The inflammatory response mediator may further provide a cellular energy source and be a building block in the cellular synthesis of other cellular components. Composition, for reducing and treating undesired inflammatory response are also disclosed.

Abstract: The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists.

Abstract: This invention is a healthful composition comprising a hot-water extract of the cultivated mycelia of Cordyceps sinensis.The healthful composition of the invention is an oral healthful composition which is highly safe and has excellent cardiotonic, hypotensive, antitussive and anti-fatigue effects.

Abstract: A method of treating a patient suffering from allergic diseases, comprises administering to said patient an effective amount of a pharmaceutical composition in dosage unit form comprising a dry powder of guava leaves.

Abstract: The present invention relates to compositions and methods for the prevention and/or treatment of allergic, autoimmune, septic shock or infectious diseases using magnesium gluconate alone or in combination with one or more antioxidants or an antiinflammatory agent. The invention also relates to the inhibition of production of inappropriate levels of lipid mediators and cytokines.

Abstract: A combination of a mucosally administrable bystander antigen and an orally, enterally, or parenterally administrable methotrexate is employed to make a pharmaceutical formulation and to treat or prevent autoimmune disease.

Abstract: This disclosure is of a surfactant mixed with an aerosollizing agent, and deposited by such agent, as a treatment for airway obstruction. It has been extensively tested, and has proved successful. It has been hypothesized that the addition of a hypersmolor drug will help to minimize mucus in the airways.

Abstract: A pharmaceutical formulation comprising (i) one or more particulate medicaments, and (ii) 1,1,1,2-tetrafluoroethane as propellant, which formulation contains less than 0.0001% w/w surfactant based upon the weight of medicament, particulate medicament being present in an amount from 0.005 to 5% w/w relative to the total weight of the formulation and having a particle size of less than 100 microns, with the proviso that said medicament is other than salmeterol, salbutamol, fluticasone propionate, beclomethasone dipropionate or a physiologically acceptable salt or solvate thereof and with the proviso that when said formulation consists of betamethasone, ergotamine tartrate or sodium cromoglycate and 1,1,1,2-tetrafluoroethane the weight to weight ratio of medicament to propellant is other than 69:7900 or 0.866% w/w.

Abstract: An agent for the prevention or alleviation of allergy symptoms contains as an effective component a dioxabycyclo?3.3.0!octane derivative represented by the following general formula (I): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently represent a hydrogen atom or alkyl group of 1-3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 together represent a methylene or ethylene group, and n, m and l represent 0 or 1.An agent for the prevention or alleviation of allergy symptoms also contains as an effective component an antioxidant in addition to the dioxabicyclo?3.3.0!octane derivative.

Abstract: There is provided novel substituted 4-aryl-3-hydroxyquinolin-2-one derivatives of the formula ##STR1## wherein R is hydrogen or methyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, bromo, chloro or trifluoromethyl, and when R.sup.1, R.sup.3 and R.sup.4 are hydrogen, R.sup.2 is nitro;R.sup.5 is hydrogen or methyl; andR.sup.6 is bromo or chloro;or a nontoxic pharmaceutically acceptable salt thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

Abstract: This invention concerns compositions and methods utilizing a compound of the formula: ##STR1## for reducing or controlling inflammation and treating pathological conditions mediated by intercellular adhesion. More particularly, the present invention concerns compositions and methods for blocking or modulating the function of the Beta.sub.2 Integrin family of cell adhesion molecules.

Abstract: The use of leukotrienes and other products of the 5-lipoxygenase pathway to enhance bacterial defense and treat infections is described. The products are especially useful when administered to the lungs for the treatment of pneumonia and other lower respiratory tract infections. The products may be administered for treatment or prophylactic purposes and may be administered concomitantly with antibiotics to combat infection.

Abstract: A C to T DNA variation at position 3365 in exon 5 of the human Asthma Associated Factor 1 (AAF1) produces the predicted amino acid substitution of a methionine for a threonine at codon 117 of AAF1. When this substitution occurs in both alleles in one individual, it is associated with less evidence of atopic allergy including asthma, fewer abnormal skin test responses, and a lower serum total IgE. Thus, applicant has identified the existence of a non-asthmatic, non-atopic phenotype characterized by methionine at codon 117 when it occurs in both AAF1 gene products in one individual.

Abstract: The present invention relates to a method to protect an animal from a disease involving inflammation by treating that animal with an effective amount of IL-12. The present invention also relates to a method for prescribing treatment for a respiratory disease involving an inflammatory response and a method for monitoring the success of a treatment for a respiratory disease involving an inflammatory response in an animal. Also included in the present invention is a formulation comprising IL-12 and a compound capable of enhancing the effectiveness of the IL-12 at protecting an animal from a disease involving inflammation.

Abstract: The present invention relates to a method to protect an animal from a disease involving inflammation by treating that animal with an effective amount of IL-12. The present invention also relates to a method for prescribing treatment for a respiratory disease involving an inflammatory response and a method for monitoring the success of a treatment for a respiratory disease involving an inflammatory response in an animal. Also included in the present invention is a formulation comprising IL-12 and a compound capable of enhancing the effectiveness of the IL-12 at protecting an animal from a disease involving inflammation.

Abstract: Methods utilizing descarboethoxyloratadine ("DCL"), for the treatment of allergic disorders, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. Also included are methods for the treatment of allergic asthma using DCL and either a decongestant or a leukotriene inhibitor, while avoiding the concomitant liability of adverse side-effects associated with other non-sedating antihistamines. The invention also encompasses the administration of DCL in a nasal or oral spray.

Abstract: Process for the preparation of (-)-pimara-9(11),15-diene-19-oic acid(acanthoic acid) and pharmaceutical compositions comprising acanthoic acid useful for the treatment of diseases caused by an excessive production of interleukin-1 or tumor necrosis factor-.alpha..

Abstract: Aerosol formulations for oral inhalation containing flunisolide dispersed in HFC 134a and/or HFC 227 which are free of chlorofluorocarbons and surfactants, and contain little or no ethanol, are disclosed. Metered dose inhalers suitable for delivering such formulations are also disclosed.

Abstract: The present invention relates to intercellular adhesion molecules (ICAM-3) which is involved in the process through which lymphocytes recognize and migrate to sites of inflammation as well as attach to cellular substrates during inflammation. The invention is directed toward such molecules, screening assays for identifying such molecules and antibodies capable of binding such molecules. The invention also includes therapeutic and diagnostic uses for adhesion molecules and for the antibodies that are capable of binding them.

Abstract: Aerosol formulations for oral inhalation containing triamcinolone acetonide and HFC 134a and/or HFC 227 as a propellant which are free of chlorofluorocarbons and surfactants are disclosed.

Abstract: The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of upper and/or lower airway passages and/or lungs, e.g., allergic rhinitis and asthma is disclosed.

Abstract: This invention encompasses a substantially homogeneous lipid chemoattractant released from stressed mammalian tissue which is a neutral lipid which is acid labile and stable to base and is stable in boiling water. This lipid recruits macrophages but not neutrophils to stressed tissue. The invention also encompasses a method for detecting injured tissue by detecting the presence of the above described lipid chemoattractant in body fluids such as urine, serum and saliva. The invention also includes a method for reducing recruitment of macrophages to injured tissue by reducing the amount of the above lipid chemoattractant or by blocking the interaction of this lipid chemoattractant with its macrophage binding site. The addition of this lipid chemoattractant to injured skin tissue promotes healing.

Abstract: Methods and compositions for the treatment of the symptoms of a patient who has a pulmonary condition associated with an inhibition of surfactant secretion by type II alveolar cells are described. The method of treatment involves causing a patient to inhale an amount of a pH-raising buffer effective to raise the pH of the aqueous fluid in the microenvironment of the type II alveolar cell lumenal surface, thereby inducing an increase in the rate of surfactant secretion by type II alveolar cells.

Abstract: Fructose-1,6-diphosphate (FDP), a sugar-phosphate compound, can be useful in treating asthma, when administered as an inhalable drug, either by itself or as a component of a mixed formulation. On a cellular level, inhalable FDP appears to offer at least four beneficial effects for asthma sufferers: (1) it reduces histamine release by activated mast cells; (2) it suppresses production of oxygen free radicals by polymorphonuclear cells; (3) it helps suppress the activation and proliferation of T-lymphocytes; and, (4) it helps reduce the expression of interleukin compounds by T-lymphocytes. All four effects have been measured and shown to occur in animal and/or human tests, and these effects render FDP likely to help reduce and retard the progressive worsening of asthma that occurs in many sufferers. In addition, when tested in inhalable form on humans, FDP was shown to increase bronchial flow rates.

Abstract: A method of facilitating the clearance of retained pulmonary secretions in a subject using lantibiotics is disclosed. The method comprises administering to the lungs of the subject an effective amount of a lantibiotic. The lantibiotic is preferably administered by topically applying it to the respiratory epithelia, such as by generating an aerosol thereof which is then inhaled by the subject. A preferred lantibiotic for carrying out the present invention is duramycin. The method may be used in treating disorders such as cystic fibrosis, chronic bronchitis, and asthma. Also disclosed is a method of combatting tuberculosis comprising administering a lantibiotic to a subject in need of such treatment.

Abstract: The optically pure R(-) isomer of albuterol, which is substantially free of the S(+) isomer, is a potent bronchodilator for relieving the symptoms associated with asthma in individuals. A method is disclosed utilizing the optically pure R(-) isomer of albuterol for treating asthma while minimizing the side effects associated with albuterol.

Abstract: A therapeutic method is provided to treat an eosinophil-associated pathology, such as bronchial asthma, by administering to a mammal in need of such treatment, an effective amount of at least one topical anesthetic, such as lidocaine, with an effective amount of one or more glucocorticoids, or the pharmaceutically acceptable salts thereof.

Abstract: Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.