Abstract: A method for treating mammals suffering from conditions associated with excess phospholipase A.sub.2 activity and/or production comprising administering to the mammal an effective amount of a non-antimicrobial tetracycline sufficient to inhibit excess phospholipase A.sub.2 activity and/or production is disclosed. A pharmaceutical composition is also disclosed.

Abstract: The invention is a method of enhancing endogenous interleukin-10 production in mammalian cells and tissues, which includes administering an effective amount of a tetracycline derivative. The method also includes enhancing interleukin-10 production by administering an effective amount of the tetracycline derivative to a mammal. Preferred tetracycline compounds are tetracycline compounds which have been modified to reduce or eliminate their antimicrobial activity. The method can be used to treat medical conditions in mammals characterized by excessive IL-1 and TNF .alpha. production.

Abstract: A method is provided for the treatment of age-related macular degeneration by administering various antibiotics, such as tetracycline and its derivatives, rifamycin and its derivatives, macrolides, and metronidazole, to a patient in a therapeutically effective amount.

Abstract: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams.

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: The invention provides a medicament for topically treating aphthous ulcers in the oral mucosa, and methods of use. The medicament comprises a troche or powder comprising a dry dosage of one or more antibiotics and, preferably, one or more polyvalent metal compounds. The troche or powder is directly applied to the aphthous ulcer and dissolves in saliva, within about 5 to about 15 minutes, thereby directly delivering a supratherapeutic dosage of the antibiotic to the ulcerated oral tissue. Further, in a preferred embodiment the troche/powder directly delivers a therapeutically high concentration of a polyvalent metal compound in suspension to the aphthous ulcer, thereby forming a protective barrier over the ulcerated oral tissue.

Abstract: The invention discloses a novel method for preventing acute lung injury in a mammal following trauma. The method includes treating the mammal with an effective amount of a tetracycline prior to intrapulmonary accumulation of neutrophils.

Abstract: Mammalian hair growth is reduced by inhibiting the activity of a matrix metalloproteinase in the skin.

Abstract: The invention relates to the use ofa) a compound or several compounds from the group consisting of flavonoidsb) of the antioxidants orc) of the endogenous energy metabolism metabolites ord) of the endogenous enzymatic antioxidant systems and synthetic derivatives thereof (mimics) ore) of the antimicrobial action systems orf) of the antiviral action systems org) active compounds of the known, conventional treatment formsin each case for the treatment or prophylactic treatment of hyperreactive skin predisposed to dermatitis or deficient, hypoactive skin or dermatoses.

Abstract: An immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative, which is safe for the human, animals or the like, an immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative and (1) proline and/or glutamine, (2) an antibiotic, or (3) a water-soluble polymer or lecithin, which is safe for the human, animals or the like, and a process for the production thereof.

Abstract: A method for treating diabetes in a mammal by moderately controlling blood glucose concentration in the mammal together with administering to the mammal an amount of a tetracycline compound effective to reduce complications associated with diabetic hyperglycemia. The method enables long term management of diabetes by avoiding the problems associated with tight control of blood glucose concentrations, i.e., hypoglycemia tolerance and seizures, while simultaneously avoiding the problems associated with conventional moderate control of blood glucose concentrations, i.e., pathological complications associated with hyperglycemia, such as nephropathy, retinopathy, etc. Blood glucose concentration can be controlled by moderate administration (e.g.

Abstract: The invention is a method of inhibiting the production of nitric oxide (NO) in an in vivo, in vitro, or ex vivo biological system. The method employs a tetracycline compound to inhibit the production of NO and/or to inhibit the expression or activity of an inducible isoform of nitric oxide synthase (iNOS). Preferably, the tetracycline compound has inhibitory activity for metalloproteinases. Also it is preferred that the tetracycline compound is provided to the biological system in an amount which has little or no antibacterial activity in the system. Accordingly, preferred tetracycline compounds are tetracycline compounds which have be modified to reduce or eliminate their antimicrobial activity. The method can be used to treat medical conditions in mammals characterized by NO production mediated by iNOS, including, for example, inflammatory conditions.

Abstract: A method for the treatment of acne is provided which results in the reduction of vestibular side effects following administration of oral tetracycline antibiotics.

Abstract: The present invention relates pharmaceutical compositions comprising a conjugate of an active substance, a linker and a carrier for the treatment and/or diagnosis of inflammatory diseases. The present invention further relates to methods using such pharmaceutical compositions for treating and diagnosing inflammatory diseases including, but not limited to, infectious diseases, autoimmune diseases, skin diseases, and inflammatory neovascularization.

Abstract: Methods for screening for compounds which potentiate the activity of antibacterial agents against bacteria resistant to the antibacterial agent alone, pharmaceutical compositions including such potentiators, and methods of treating bacterial infections using a combination of a potentiator and a potentiated antibacterial agent, which are useful for overcoming the resistance of a bacterial strain for an antibacterial agent.

Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of 7-?substituted amino!-9-?(substituted glycyl)amido!-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein R, R.sub.2, R.sub.3, and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.

Abstract: Complexes of bismuth, e.g. bismuth salts, and polyacrylate, e.g. carbomer, are discloses which may be incorporated into pharmaceutical compositions for oral, oral delayed-release, and rectal administration. The complexes may be combined with an antibiotic, such as tetracycline, and an antiprotozoal agent, e.g. Metronidazole, for use in the treatment of Helicobacter pylori infection. The treatment of inflammatory bowel disease using bismuth/polyacrylate complexes, or other bismuth preparations, is also described.

Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 7-?substituted amino!-9-?(substituted glycyl)amido!-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein R, R.sub.2, R.sub.3, and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.

Abstract: The invention is a method of inhibiting cancer growth, including cellular proliferation, invasiveness, or metastasis in mammals. The method employs 6-demethyl-6-deoxy-4-dedimethylaminotetracycline (CMT-3) and other functionally related chemically modified, preferably non-antibacterial, tetracycline compounds to inhibit cancer growth. The method is particularly effective to inhibit the establishment, growth, and metastasis of solid tumors, such as tumors derived from colon cancer cells, breast cancer cells, melanoma cells, prostatic carcinoma cells, or lung cancer cells.

Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.

Abstract: A method for inhibiting the formation and progression of abnormal vascular dilatation and/or aneurysms. The method includes administering a tetracycline compound to a mammal in an amount which is effective against the formation or progression of aneurysm, or which is effective to induce regression of an established abnormal dilatation or aneurysm. The method is of particular advantage in the treatment of mammals having an abdominal aortic aneurysm, a relatively common, and life-threatening, condition. Further, there is provided a method for inhibiting elastolytic activity in vascular tissue, to diminish excessive proteolytic degradation of vascular elastic tissues, wherein such degradation is associated with abnormal vascular dilatation or aneurysm. Also provided is an apparatus for treating mammals suffering from an abnormal vascular dilatation and/or aneurysm.

Abstract: A method for improving the healing response of epithelialized tissue (e.g., skin, mucosae) to acute traumatic injury is disclosed. The method includes employing a tetracycline compound, having substantially no antibacterial activity, to improve the capacity of the epithelialized tissue to heal acute wounds. Specifically, the method involves increasing the rate of collagen accumulation of the healing epithelialized tissue above that associated with wound healing in the individual. The method decreases proteolytic activity in the epithelialized tissue by means of the tetracycline compound, most commonly decreasing collagenolytic activity and/or decreasing gelatinolytic activity. Collagenase and gelatinase activity have been shown to be decreased by the method of the invention. Preferably, the method is employed to improve the wound healing capacity of human or animal subjects in whom such capacity is impaired. Also, the non-antibiotic tetracycline is preferably administered topically at the site of the wound.

Abstract: The present invention relates to leave on, oil-in-water, skin care compositions, comprising: (A) from about 0.05% to about 20% of an acidic active ingredient, preferably having a solubility parameter from about 6 to about 12; (B) from about 0.1% to about 25% of alkoxylated alcohols, alkoxylated polyols, and mixtures thereof; (C) from about 1% to about 20% of an acid stable, hydrophobic, structuring agent selected from the group consisting of saturated C.sub.16 to C.sub.30 fatty alcohols, saturated C.sub.16 to C.sub.30 fatty alcohols containing from about 1 to about 5 moles of ethylene oxide, saturated C.sub.16 to C.sub.30 diols, saturated C.sub.16 to C.sub.30 monoglycerol ethers, saturated C.sub.16 to C.sub.30 hydroxy fatty acids, and mixtures thereof, having a melting point of at least about 45.degree. C.; (D) from about 0.

Abstract: A method is disclosed for inhibiting endogenous production of nitric oxide (NO) in an in vivo, in vitro, or ex vivo mammalian system. The method employs a tetracycline compound to inhibit production of NO and/or to inhibit the expression or activity of an inducible isoform of nitric oxide synthase (iNOS). Preferably, the tetracycline compound has inhibitory activity for metalloproteinases. Also it is preferred that the tetracycline compound is provided to the mammalian system in an amount which has little or no antibacterial activity in the system. Accordingly, preferred tetracycline compounds are tetracycline compounds which have be modified to reduce or eliminate their antimicrobial activity. The method can be used to treat medical conditions in mammals characterized by NO production mediated by iNOS, including, for example, inflammatory conditions.

Abstract: The present invention relates to methods of treating gram-positive bacterial infections by administration of a BPI protein product alone, or in combination with an antibiotic. BPI protein product alone has a bactericidal or growth inhibitory effect on selected gram-positive organisms. BPI protein product also increases the susceptibility of gram-positive organisms to antibiotics and can even reverse resistance of gram-positive organisms to antibiotic.

Abstract: A method for inhibiting the activity of serine proteinase in biological systems includes administering to the system a serine proteinase inhibitory amount of a hydrophobic 4-de(dimethylamino)tetracycline. The method reduces tissue destruction during inflammation resulting from the activity of human leukocyte elastase. The method is used for pharmaceutical and cosmetic purposes.

Abstract: Methods of inhibiting root caries formation on mammalian tooth surfaces are disclosed. The methods include topically contacting the tooth root surfaces with an effective amount of a non-antibacterial tetracycline which is not systemically absorbed into the blood stream. In preferred embodiments, the tetracyclines are included in various oral hygiene products such as dentifrices, lozenges, chewing gums and the like to contact the tooth root surfaces.

Abstract: An injection solution for subcutaneous or intramuscular administration to an animal, and a method of producing same, are provided. The injection solution is substantially free of chloride ions and employs a basic amino acid as a pH-adjusting agent, characteristics that make the injection solution more physiologically tolerable upon injection. Preferably, the injection solution comprises 5 to 30 g of oxytetracycline per 100 ml of injection solution, where the oxytetracycline is provided in a magnesium complex; 0 to 25 g of polyvinylpyrrolidone per 100 ml of injection solution; a basic amino acid in an amount sufficient to adjust a pH of the injection solution to from 5.5 to 9.5; and an additive in an aqueous/organic solvent phase.

Abstract: The present invention provides the new use in the treatment of amyloidosis with the anthracyclinone of formula (A) wherein R1, R2, R3, R4, and R5, are appropriate substituents. Some compounds of formula (A) are novel. Processes for their preparation and pharmaceutical composition containing them are also described.

Abstract: A pharmaceutical composition comprising a compound represented by the following formula (I):X--Y--Z (I)?where Y is represented by the following formula (III): ##STR1## X is a monovalent group of a tetracycline type compound, and Z is a monovalent group of asteroid type compound such as estrogen!.The compound can concentrate on the bone tissue and has a bone resorption inhibition/ossification promotion functions.

Abstract: A method of administering a drug to an eye including the steps of: (a) admixing a pharmaceutically acceptable hydrocarbonaceous semi-solid or oil which contains the drug with water at a temperature above the melting point of the semi-solid or oil; and (b) nebulizing the admixture to form liquid drops; and (c) applying the liquid drops to the eye.

Abstract: .beta.-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals.

Abstract: A method is disclosed treating a tumor in a host by administering a nonemulsified ultrapurified polymerized hemoglobin solution to the host and also administering a chemotherapeutic agent to the host. In a particularly preferred embodiment, the hemoglobin is bovine hemoglobin.

Abstract: The use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders.Pharmaceutical compositions containing both (i) and (ii) and methods for the preparation of pharmaceutical compositions containing (i) and (ii) are also described.

Abstract: A topical medication for the treatment of skin pathology including acne is comprised of tetracycline, minocycline, clindamycin, erythromycin, or doxicycline and selenium sulfide or sulfur in a pharmaceutically acceptable carrier. The lotion, cream or ointment is applied to the lesions, left in place briefly and washed off. This is repeated twice daily. The lesions generally clear up within a week. Because the treatment is local, the serious side effects of systemic administration of drugs is avoided.

Abstract: The present invention provides a method to treat susceptible cancers in humans comprising administering a cancer-treating amount of a member of the tetracycline family or a pharmaceutically acceptable salt thereof. Doxycycline, minocycline and tetracycline are utilized in the preferred method. Preferred methods of the present invention treat osteo-, breast, lung, prostate or Kaposi's cancers. Other aspects of the invention are described in the full application.

Abstract: The present invention relates to an improved method for controlling coccidiosis in poultry which comprises administering to poultry on shuttle medication an additional medication prior to switching from the starter compound to the grower compound, and continuing the additional medication for a period after the switching.

Abstract: The present invention relates to novel compounds useful for the treatment and prophylaxis of degenerative bone disorders and to the preparation thereof. These compounds are particularly characterized by two active moieties, the first of which possesses "bone-seeking" affinity and the second which is an inhibition of the enzyme carbonic anhydrase and/or an inhibitor of bone resorption. The novel compounds of this invention can be administered as pharmaceutically acceptable compositions and in convenient dosage unit form in a method for the treatment and prophylaxis of degenerative bone disorders.

Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1, R.sup.2 and W are defined in the specification. These compounds are useful as antibiotic agents.

Abstract: .beta.-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals.

Abstract: An antibiotic formulation comprising gentamicin, and optionally tetracycline or oxytetracycline, for use in plants.

Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 7-halogen-9-[hydrogen or [(substituted glycyl)amido]]-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein X and W are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.

Abstract: The invention provides a method for prevention, treatment or control of bacterial infections in warm blooded animals by administering a pharmacologically effect amount of a compound of the formula: ##STR1## wherein R, R.sup.1 and W are defined in the specification.

Abstract: The invention relates to a method for inhibiting angiogenesis and proliferation of endothelial cells by administering an inhibitory amount of a 9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracycline of Formula I: ##STR1## wherein W, R.sub.2 and R.sub.3 are as defined in the specification. The invention also relates to a method for inhibiting proliferation of tumor cells and tumor growth by administering an inhibitory amount of a compound of Formula I in combination with a chemotherapeutic agent or radiation therapy. The invention also relates to compositions containing an effective inhibitory amount of a compound of Formula I in a pharmaceutically acceptable carrier.

Abstract: A method for treating mammals suffering from excessive extracellular protein glycosylation which is associated with diabetes, scleroderma and progeria by administering to the mammal a tetracycline which effectively inhibits excessive protein glycosylation.

Abstract: The disclosure is drawn to a method of using novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Abstract: A method for treating mammals suffering from conditions associated with excess phospholipase A.sub.2 activity and/or production comprising administering to the mammal an effective amount of a non-antimicrobial tetracycline sufficient to inhibit excess phospholipase A.sub.2 activity and/or production is disclosed.

Abstract: The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein product with an antibiotic in treatment of gram-negative bacterial infections improves the therapeutic effectiveness of the antibiotic, including increasing antibiotic susceptibility of gram-negative bacteria and reversing resistance of the bacteria to antibiotics.

Abstract: The invention provides compounds of formula ##STR1## wherein X, R and R.sup.1 are defined in the specification. These compounds are useful as antibiotic agents.

Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR1## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.