Abstract: The present invention provides pharmaceutical compositions for the treatment of tumor cells in a subject of for the treating of undesirable symptoms associated with the presence of free radicals. The compositions comprising a complex compound having the structure: ##STR1## wherein R.sub.1 and R.sub.1, are the same or different and each is an alkyl group, a phenyl group or a substituted derivative of a phenyl group;wherein R.sub.2 and R.sub.2, are the same or different and each is hydrogen, an unbranched alkyl group, a halide or a group having the structure ##STR2## wherein R is hydrogen, an alkoxide group, an alkyl group, or OH; wherein R.sub.3 and R.sub.3, are the same or different and each is hydrogen or an alkyl group;wherein X and X' are the same or different and each is a water soluble group having weak to intermediate ligand field strength; andQ is a soluble, pharmaceutically acceptable negative ion and a pharmaceutically acceptable carrier.

Abstract: A method of treating rheumatoid arthritis which includes first, taking a blood test to determine a rate of erythrocyte sedimentation and a rheumatoid factor, and then fasting for a 12-hour period prior to orally administering a 500 milligram dosage of tetracycline achromycin, and observing any change in the symptoms of the rheumatoid arthritis including reduction of swelling and pain in the affected sites. This process is repeated over 24-hour cycles until the rheumatoid factor has decreased by at least 50% from the first determined level prior to treatment and erythrocyte sedimentation decreased, at which point the 24-hour cycles are continued, reducing the dosage of tetracycline achromycin to 250 milligrams until the symptoms of the rheumatoid arthritis condition disappear.

Abstract: A composition comprising approximately equal proportions by volume of wintergreen oil, olive oil and/or oil of Eucalyptus and alcohol has an analgesic effect in treating aches and pains when rubbed or massaged on skin covering tissue from which such aches or pains emanate.

Abstract: Inbred Lewis (LEW/N) female rats develop an arthritis in response to Group A streptococcal cell wall peptidoglycanpolysaccharide (SCW) which mimics human rheumatoid arthritis. Histocompatible Fischer (F344/N) rats, on the other hand, do not develop arthritis in response to the same SCW stimulus. To evaluate this difference in inflammatory reactivity between the two strains, the function of the hypothalamic-pituitary-adrenal axis and its ability to modulate the development of the inflammatory response was studied. It has been found that, in contrast to F344/N rats, LEW/N rats had markedly impaired plasma ACTH and corticosterone responses to SCW, recombinant human Interleukin-1 alpha (IL-1 alpha), the serotonin agonist, quipazine, and synthetic rat corticotropin-releasing hormone (CRH). In addition, LEW/N rats compared to F344/N rats had smaller adrenal glands and larger thymuses. Treatment of LEW/N rats with replacement doses of dexamethasone decreased the severity of their SCW-induced arthritis.

Abstract: Heparanase activity in a patient may be inhibited by administering an effective heparanase-inhibiting amount of heparin or an effective chemically modified derivative of heparin which inhibits heparanase activity. Such derivatives are preferably N-desulfated, N-acetylated heparin or O-desulfated, N-acetylated heparin. By means of this invention, allograft rejection may be prevented or delayed and autoimmune diseases such as arthritis may be alleviated and treated.

Abstract: A preparation method of sodium diclofenac enteric-coated microcapsules by spray drying technique comprising the steps of(a) dissolving sodium diclofenac in an appropriate amount of distilled water;(b) adding an effective amount of excipients to the above solution to form a suspension;(c) adding methacrylic acid-ethyl acrylate copolymers (Eudragit L 30D) and polyethyleneglycol 6000 (PEG 6000) as the enteric-coating material to form a slurry;(d) atomizing the slurry to form spray-dried powder;(e) mixing the spray-dried powder with a mixture of microcrystalline cellulose (neocel) and pregelatinized starch (flo-starch); and(f) compressing the powder mixture into a microdispersed enteric tablet.The spray drying technique could be easily performed to prepare the enteric-coated microcapsules with aqueous latex polymer dispersion such as Eudragit L 30D as an enteric-coating polymer.

Abstract: A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branch alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract: The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.

Abstract: A method of inhibiting phospholipase A2 in the control of inflammation, wherein delta-6,9,12,15-octadecatetraenoic acid (stearidonic acid) and/or delta-8,11,14,17-eicosatetraenoic acid is administered alone or in a pharmaceutically acceptable diluent or carrier.

Abstract: A topical medicament comprising a dilute aqueous solution of sodium bicarbonate and a transdermal carrier, preferably containing approximately equal proportions by weight of a 3 percent aqueous solution of sodium bicarbonate, and propylene glycol, the resultant solution comrpising about 1.5 weight percent sodium bicarbonate.

Abstract: The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the pharmaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activities, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.

Abstract: A method for the treatment of arthritis or a related autoimmune disease that exhibits immune complexes in serum or synovial fluid is provided which comprises exposure of the serum or synovial fluid to an oligosaccharide containing a structural component that inhibits or disrupts the degree of occupancy of the Fc carbohydrate binding site on IgG, e.g., sialyllactose.

Abstract: The present invention relates to a method of treating diseases associated with elevated levels of interleukin 1 (IL-1) including inflammatory diseases such as arthritis, skin hypersensitivity and endotoxemia. More specifically, the invention relates to a method for the treatment of such diseases in warm-blooded animals, such as humans, which comprises the administration of a therapeutically effective amount of an aromatic diamidine, sufficient to inhibit IL-1 release from IL-1 producing cells. The aromatic diamidine can also be used to block interleukin 6 (IL-6) and tumor necrosis factor from cells producing these cytokines.

Abstract: The invention relates to a method for potentiation of a therapeutic agent, the method comprising the steps of administering an effective dose of insulin to induce to hypoglycemia; administering a pre-determined dose of a therapeutic agent; and administering a pre-determined dose of glucose sufficient to substantially neutralize the hypoglycemia. As an adjuvant system, the instant invention constitutes the combination of a quantity of insulin in the range of one to four units per 10 kilograms of body weight; a pre-determined quantity of the therapeutic agent; and glucose in the form of a hypertonic solution between about 5% and about 50% glucose, the volume of the solution being in the range of about 10 cubic centimeters to about 100 cubic centimeters. The inventive method is known as Insulin Potentiation Therapy (IPT).

Abstract: Dihydrobenz[c]acridine carboxylic acid derivatives are provided which are useful for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, autoimmune diseases, psoriasis and chronic inflammatory diseases.

Abstract: The present invention relates to a useful antiinflammatory and/or antiallergic composition comprising a compound of the formula: ##STR1## (wherein the R's are same or different and each means a hydrogen atom or lower alkyl group) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: This invention relates to N-hydroxy-N-[3-(2-substituted phenyl)prop-2-enyl]ureas and thioureas, formulations containing those compounds, and methods of using such compounds as 5-lipoxygenase inhibiting agents.

Abstract: The invention is directed to methods and materials useful in treating autoimmune diseases. The therapeutic agents are of the formula X--MHC--peptide or MHC--peptide--X wherein X represents a functional moiety selected from a toxin and a labeling group; MHC is an effective portion of the MHC glycoprotein, said glycoprotein dissociated from the cell surface on which it normally resides; and "peptide" represents an antigenic peptide sequence associated with an autoantigen; -- represents a covalent bond or a linker bound to X and MHC or to X and peptide by covalent bonds; and -- represents a covalent bond, to noncovalent association, or a linker covalently bound to or associated with the MHC and peptide. These complexes can be used to target helper T-cells which are specifically immunoreactive with autoantigens.

Abstract: 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.

Abstract: The invention relates to benylalcohol phospholipase A.sub.2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A.sub.2 -mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylalcohol phospholipase A.sub.2 inhibitor.

Abstract: Novel saccharide derivatives of protocatechualdehyde represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a benzoyl group, and R.sup.2 represents an alkyl group.The method for preparing thereof and the use of the compound as antiinflammatory agents.

Abstract: Pharmaceutical preparations are provided for preventing or treating autoimmune diseases in which the active principle is activated T-lymphocyte cells, specific for the autoimmune disease to be treated, which cells have been treated by incubation with a photoactivatable psoralen cross-linking agent, such as 8-methoxypsoralen, and then photoactivated. The active principle may also be the membrane fraction of such cells. Such preparations may be formulated into pharmaceutical compositions and administered to prevent or treat autoimmune disesases.

Abstract: The present invention relates to vinylogous hydroxamic acids, processes for their manufacture, pharmaceutical preparations containing them, and their use in the treatment of various disorders.

Abstract: Novel cyclic vinylogous N-hydroxy-N-methylureas are useful in the treatment of leukotriene mediated conditions such as asthma and rheumatoid arthritis.

Abstract: Retinoic esters of D-desosamine have the formula ##STR1## wherein the ##STR2## radical is (all trans) retinoyl, (13 cis) retinoyl or etretinoyl, and R.sub.2 represents linear or branched alkyl having 1-24 carbon atoms; and the .alpha. and .beta. anomers, their mixtures and their salts.These esters are usefully employed in human and veterinary medicines and in cosmetic compositions.

Abstract: Diarylacetylenes of the formula I ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.2 and R.sup.3 are each hydrogen or, when R.sup.1 is hydrogen, together form a --C(CH.sub.3).sub.2 --B--C(CH.sub.3).sub.2 -- group (where B is --CH.sub.2 Ch.sub.2 -- or --CH(CH.sub.3)--) or --OC(Ch.sub.3) (Z)CH.sub.2 CH.sub.2 -- group (where Z is C.sub.1 -C.sub.2 -alkyl) or R.sup.2 is C.sub.1 -C.sub.3 -alkoxy and R.sup.3 is C.sub.1 -C.sub.10 -alkyl or, when R.sup.2 is hydrogen, R.sup.1 and R.sup.3 are each alkyl as defined above, R.sup.4 is C.sub.1 -C.sub.6 -alkyl and n is 0, 1 or 2, are prepared as described and used as active compounds in drugs and cosmetics.

Abstract: The invention relates to an aqueous oral pharmaceutical preparation of diclofenac which can be used for treating pain and inflammatory processes, and to the preparation of a preparation of this type.

Abstract: An analgesic composition useful in providing temporary relief from the symptoms of arthritis is disclosedng having the following components in approximately the stated weight-percentages ranges:______________________________________ Water (Deionized) 86.00-95.35% by weight; Carbopol 934 0.5-2.00% by weight; Methylparaben 0.1-0.40% by weight; Propylparaben 0.05-0.20% by weight; Hampene 100 0.05-0.20% by weight; Aloe Vera Gel 0.05-2.00% by weight; Benzyl Alcohol 0.30-1.20% by weight; Camphor (U.S.P.) 0.50-2.00% by weight; Menthol (U.S.P.) 1.00-4.00% by weight; Thymol 0.10-0.60% by weight; Eugenol 0.10-0.60% by weight; Witch Hazel 0.05-1.50% by weight; Isopropyl Alcohol 0.05-1.50% by weight; Eucalyptus Oil 0.50-2.00% by weight; Triethanolamine 0.50-2.00% by weight; and, Quaternium-15 0.10-0.40% by weight.

Abstract: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.

Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.

Abstract: This invention relates to novel 3-(1-substituted-pyrazoyl)-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthease, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-(1-substituted-pyrazoyl-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel compounds useful as intermediates in the preparation of the 3-(1-substituted-pyrazoyl-2-oxindole derivatives of this invention and to a process for the preparation of the 3-(1-substituted-pyrazoyl)-2-oxindole derivatives.

Abstract: A method of treating inflammations of body joints in humans by topical application of anti-inflammatory agents may be used to treat joints afflicted by arthritic conditions such as gouty arthritis. The steps of the method include dissolving a predetermined quantity of a known anti-inflammatory drug, applying the medium with dissolved anti-inflammatory drug directly onto the skin covering a body joint known to be inflamed and allowing the medium with dissolved anti-inflammatory drug to be absorbed into the skin. Possible non-steroidal, anti-inflammatory drugs which may be used with the method include indomethacin, phenylbutazone and colchicine. Steroidal non-inflammatory drugs may also be used.

Abstract: An aggregate suspension containing holmium-166 hydroxide and a carrier (such as a particulate ferric hydroxide) is injected into a patient's anesthetized joint (such as a knee joint or hip joint) for the treatment of inflamed synovial tissues such as present in arthritis, especially rheumatoid arthritis. The aggregate suspension is in a range of particle sizes from 1 to 40 microns. The holmium-166-containing suspension treats the synovial tissues, whereby radiation synovectomy takes place.

Abstract: A method of selectively suppressing the excess immune reaction produced iatrogenically or autochthonously by administering 0.1 to 100 mg of ciamexone per kg of body weight.

Abstract: The present invention describes a novel material which is extractable from plants of the order Malvales and which demonstrates anti-allergic activity.

Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.

Abstract: Improved hexamethylmelamine containing parenteral emulsions are prepared in the absence of organic solvents and containing low levels of biocompatible emulsifiers using ultrahigh energy Microfluidizer.RTM. processing equipment. The emulsions have oil phase droplets with average diameters of less than about 0.4 microns with size distributions of less than about +/-50%.

Abstract: A method of treating leukocyte mediated autoimmune and skin diseases using psoralen reagent composition comprising sterile aqueous solutions suitable for extracorporeal administration to blood from a subject being treated by ultraviolet-A photophoresis.

Abstract: Strains, sprains and sore skeletal muscles are treated with topical application of pharmaceutical composition containing a combination of shark liver oil and garlic oil in a cream or ointment base.

Abstract: A double blind clinical trial of 10-deazaaminopterin versus the antirheumatoid drug methotrexate (MTX) established that 10-deazaaminopterin, in addition to being at least equally effective as methotrexate in all respects in ameliorating rheumatoid arthritis in humans, it is superior to methotrexate in controlling pain and joint stiffness and in improving grip strength. In accordance with this invention 10-deazaaminopterin is claimed as a more effective disease modifying arthritis remittive drug for the treatment of rheumatoid arthritis in humans.

Abstract: The invention relates to N-aryl-azetidinones, their preparation process and their use as active serine elastase inhibitors.The N-aryl-azetidinones are in accordance with formula: ##STR1## in which R.sup.1 and R.sup.2 can be a halogen atom or an organic radical, R.sup.3 represents a halogen atom or another good starting group and R.sup.4 represents H or an organic radical.The compounds with R.sup.3 .dbd.Cl or OSO.sub.2 CH.sub.3, R.sup.4 .dbd.H and R.sup.1 .dbd.R.sup.2 .dbd.F or R.sup.1 .dbd.F and R.sup.2 .dbd.Br are irreversible and selective elastase inhibitors.

Abstract: There are disclosed herein novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D.sub.3 providing excellent pharmacological effects, and a process for the preparation thereof. These novel compounds are represented by the general formula ##STR1## wherein R.sub.1 and R.sub.2 each denotes a hydrogen atom or a protecting group for the hydroxyl group; R.sub.3 and R.sub.4 each denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group and R.sub.4 ' and R.sub.5 ' each denotes a hydrogen atom, or alternatively R.sub.3 and R.sub.3 ' together or R.sub.4 and R.sub.4 ' together denote an oxo group; provided that R.sub.3, R.sub.3 ', R.sub.4 and R.sub.4 ' cannot denote hydrogen atoms simultaneously. The process for the preparation comprises subjecting a previtamin D.sub.3 derivative represented by the formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.3 ', R.sub.4 and R.sub.4 ' are as defined above, to thermal isomerization to give a vitamin D.sub.

Abstract: Hematopoietic cells are selectively eliminated by cytotoxic agents which rely upon light activation. The cytotoxic agents are joined to ligands, particularly sugars, specific for myeloid monocyte and lymphocytic lineages. Further specificity can be achieved by limiting the light target. The method and compositions find particular use in organ transplants and arthritis.

Abstract: A novel pyrazinoxide compound of NF-1616-904 having the formula (1), ##STR1## prepared by hydrolyzing the intermediate compound of NF-1616-902 which is separated from a culture broth of a microorganism belonging to the genus Thielavia.The pyazinoxide compound of NF-1616-904 possess biological and pharmacological activities, and is useful agent for preventing and treating diseases caused by superoxide radicals (O.sub.2.sup.-), and nephritis.

Abstract: The present invention pertains to an unpleasant taste masking composition which comprises a flavoring agent having a bitter taste or unpleasant off-note and a sufficient amount of a non-bitter intense sweetener to nullify the taste or off-note of the flavoring agent. The unpleasant taste masking composition may be used in ingestible products such as hard and soft confections, chewing gum compositions and the like. The present invention also pertains to a method for preparing the unpleasant taste masking compositions and the ingestible products in which they may be used.

Abstract: Derivatives of 1,2-O-isopropylidene-.alpha.,D-glucofuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as autoimmune deficiency syndrome, psoriasis, atopic dermatitus, rheumatoid arthritis, osteoarthritis, scleroderma and systemic lupus erythematosus.

Abstract: Inflammation, acute and/or chronic, is treated with a CIF (TGF-.beta.). The CIF may be administered locally or systemically, depending upon the indication, and does not require coadministration or activator or cofactor for efficacy.

Abstract: Inbred Lewis (LEW/N) female rats develop an arthritis in response to Group A streptococcal cell wall peptidoglycanpolysaccharide (SCW) which mimics human rheumatoid arthritis. Histocompatible Fischer (F344/N) rats, on the other hand, do not develop arthritis in response to the same SCW stimulus. To evaluate this difference in inflammatory reactivity between the two strains, the function of the hypothalamic-pituitary-adrenal axis and its ability to modulate the development of the inflammatory response was studied. It has been found that, in contrast to F344/N rats, LEW/N rats had markedly impaired plasma ACTH and corticosterone responses to SCW, recombinant human Interleukin-1 alpha (IL-1 alpha), the serotonin agonist, quipazine, and synthetic rat corticotropin-releasing hormone (CRH). In addition, LEW/N rats compared to F344/N rats had smaller adrenal glands and larger thymuses. Treatment of LEW/N rats with replacement doses of dexamethasone decreased the severity of their SCW-induced arthritis.

Abstract: There are disclosed novel pharmaceutical compositions which comprise diclofenac or a salt thereof, a penetration agent such as 1-n-dodecylazacycloheptan-2-one or dimethyllauroylamide and, as vehicle, a mineral oil. These compositions have excellent skin penetration properties and can therefore be used in transdermal therapeutic systems (TTS) as drug reservoir.