Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: Novel compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro;R.sup.5 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;R.sup.6 is selected from hydrogen, C.sub.1 -C.sub.4 ally and hydroxy; orR.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;R.sup.7 is selected from hydrogen and hydroxy,R.sup.8 and R.sup.9 are each selected from hydrogen, C.sub.1 -C.sub.4 alkyl and cyclo(C.sub.3 or C.sub.4) alkyl or together with the nitrogen form a morpholino group; andX is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R.sup.5, R.sup.6 and R.sup.7 is other than hydrogen and is always a bond when R.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone.

Abstract: A delivery system for applying a formula containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin which involves the topical application of capsaicin by use of patches, use of second skin, use of sprays and includes a unique method for applying the formulation using laser on the epidermis.

Abstract: The invention is directed to a method of treating a T cell-mediated autoimmune disease in animals, including humans, by the oral administration of autoantigens, fragments of autoantigens, or analogs structurally related to those autoantigens, which are specific for the particular autoimmune disease. The method of the invention includes both prophylactic and therapeutic measures.

Abstract: Disclosed is a novel transdermal delivery system for dehydroepiandrosterone (DHEA). Using phospholipids as vehicles, DHEA can be administered into and through the skin when topically applied. Numerous advantages apply to this modality of therapy.

Abstract: Dendritic cells are of interest therapeutically as antigen-presenting cells. A process is disclosed in which peripheral blood cells are first isolated and the CD 34 antigen-expressing blood progenitor cells which they contain are then enriched. These enriched cells are expanded ex-vivo using a combination of haematopoietic growth factors and cytokines. Over a period of 10-20 days, they give rise, in particular to dendritic cells which, where appropriate, can be purified still further. These cells are functionally active with regard to the ability to present antigen.

Abstract: Compounds represented by formula I: ##STR1## are disclosed. .sup.AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom. A pharmaceutical composition is also included. Methods of treating cancer and cytokine mediated diseases are also included.

Abstract: The invention is directed to a method of treating a T cell-mediated autoimmune disease in animals, including humans, by the oral administration of autoantigens, fragments of autoantigens, or analogs structurally related to those autoantigens, which are specific for the particular autoimmune disease. The method of the invention includes both prophylactic and therapeutic measures.

Abstract: The progression of infection and other pathologies produced by a viral infection may be inhibited by administering an effective dosage of Ajoene. Additionally, Ajoene has anti-tumor, anti-shock, and anti-inflammation effects. In general, Ajoene may be used to treat any integrin-mediated disease or condition.

Abstract: A composition containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin can be used to treat many types of discomforts, including musculo-skeletal pain, neuralgia and neurpathies, without the discomfort normally associated with the topical application of capsaicin.

Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections, and autoimmune or other diseases in which activated macrophages are involved, such as septic shock, heumatoid arthritis and multiple sclerosis.

Abstract: A composition containing capsaicin together with another ingredient to neutralize the discomfort resulting from the application of capsaicin to the skin can be used to treat many types of discomforts, including arthritis pain, hemorrhoid pain and itching, and poison ivy itching, without the discomfort normally associated with the topical application of capsaicin.

Abstract: A collagen mimetic peptide having the nine amino acid sequence glycine-proline-hydroxyproline-glycine -proline-glutamine-glycine-methionine-glycine, and analogs thereof is described. The collagen mimetic peptide may be included within a pharmaceutical composition also containing a pharmaceutically acceptable carrier and/or animal tissue. The collagen mimetic peptide is used in a treatment of rheumatoid arthritis by orally administering the collagen mimetic in an amount effective to reduce or alleviate one or more symptoms associated with rheumatoid arthritis.

Abstract: A method and composition are provided for treatment of disorders involving immunological dysfunction. The invention comprises the administration of a low level of ribonucleotide polymerase protein or a derivative thereof to a human or animal with an immune dysfunction disorder.

Abstract: The present invention is directed to a method and pharmaceutical formulations for the treatment of autoimmune arthritis and animal models therefore in mammals, including humans, by the oral, enteral or by-inhalation administration of whole collagen protein or biologically active peptide fragments of collagen.

Abstract: A composition for use in immunosuppression therapy is disclosed. The composition includes an immunosuppressant drug, such as cyclosporin A, and an ethanol extract of the root xylem of Tripterygium wilfordii. The extract is effective alone, or in combination with such an immunosuppressant, in the treatment of transplantation rejection. Also disclosed is a method of immunosuppression that includes administering to a subject a pharmaceutically effective amount of an immunosuppressant drug and an extract of the type above, in an amount effective to potentiate the action of the drug.

Abstract: The present invention relates to novel peptides derived from the autoantigen HC gp-39, said peptides comprising at least one of the amino acid sequences FGRSFTILAS (SEQ ID No. 1), FTLASSETG (SEQ ID No. 2), YDDQESVKS (SEQ ID No. 3) and FSKIASNTQ (SEQ ID No. 4). The peptides resemble MHC Class II restricted T-cell epitopes present on the autoantigen HC gp-39 in articular cartilage. HC gp-39, proteins comprising an amino acid sequence which exhibits at least 50% homology with the amino acid sequence YKLVCYYTSWSQYREGDGSCFPDALDRFLCTHIIYSFANISND (SEQ ID No: 10) and said peptides can be used in antigen-specific treatment of articular cartilage destruction in autoimmune diseases in mammals to induce systemic tolerance of the immune system. The autoantigen HC gp-39, proteins comprising an amino acid sequence which exhibits at least 50% homology with the amino acid sequence YKLVCYYTSWSQYREGDGSCFPDALDRFLCTHIIYSFANISND (SEQ ID NO: 10) and said peptides are also suitable to induce arthritis in animals, preferably mice.

Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; A is selected from (a) optionally substituted alkylene, (b) optionally substituted cycloalkylene, (c) optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, (d) optionally substituted alkenylene and (e) ##STR2## X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from --OR.sup.4, --NR.sup.6 R.sup.7, and a pharmaceutically acceptable metabolically cleavable group, (c) --OR.sup.2, (d) tetrazolyl, (e) --CH(OR.sup.2)--CH.sub.2 OR.sup.8, (f) --CH(OR.sup.2)--CH.sub.2 --CH.sub.2 OR.sup.8, (g) --CH(OR.sup.2)--CH(OR.sup.8)--CH.sub.2 OR.sup.9, and (h).dbd.N--OR.sup.2 ; and R.sup.

Abstract: This invention is directed to a dietary regimen and a unique combination of nutritional supplements and a method. More specifically, this invention is directed to a unique combination of nutritional supplements which provides symptomatic relief from arthritis. The unique combination of nutritional supplements of this invention is believed to function by both increasing the available (effective blood level) of anti-inflammatory agents and promotion of the healing/regenerative process in the effected joints, thus producing unexpected and lasting symptomatic relief from the debilitating effects of both osteoarthritis and rheumatoid arthritis.

Abstract: A method of treating animals, particularly rhea and ostrich chicks with adipose depletion, by injection with an oil derived from rhea or ostrich adipose or by injection with an active component of the oil that increases anti-inflammatory capabilities and phospholipid formation.

Abstract: The analgesic effectiveness of an NSAID is significantly enhanced by administering the NSAID prior to, with or following the administration of an analgesia enhancer which is a nontoxic NMDA receptor blocker and/or a nontoxic substance that blocks at least one major intracellular consequence of NMDA receptor activation.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

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 and composition are provided for treatment of disorders involving immunological dysfunction. The invention comprises the administration of a low level of ribonucleotide polymerase protein or a derivative thereof to a human or animal with an immune dysfunction disorder.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

Abstract: A soluble protein having IL4 and/or IL13 antagonist or partial antagonist activity comprises an IL4 mutant or variant fused to least one human immunoglobulin constant domain or fragment thereof.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

Abstract: The present invention is directed to a method and pharmaceutical formulations for the treatment of autoimmune arthritis and animal models therefore in mammals, including humans, by the oral, enteral or by-inhalation administration of whole collagen protein or biologically active peptide fragments of collagen.

Abstract: An orally administrable therapeutic protein is provided by combining the therapeutic protein with a stabilizing agent in an aqueous solution. The solution is coated onto nonpareils and microencapsulated with a water emulsifiable enteric coating composition. The microcapsules are orally administered. The coating protects the protein as it passes through the stomach. Upon reaching the small intestines, the basic pH of the intestinal juices will dissolve the coating, allowing the protein to be released and induce antigen specific immune response which has the specificity of the native molecule. The stabilizing agent protects the therapeutic protein from denaturation during the encapsulation process.

Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.

Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.

Abstract: The present invention relates to adenosinedeaminase inhibitors containing at least one O-alkylated moiety derivative and the pharmaceutically acceptable salts thereof. The pharmaceutical compositions of the present invention include adenosinedeaminase inhibitors containing at least one of the compounds represented by Formula (I): ##STR1## wherein each of R.sub.1, R.sub.2, and R.sub.3 are the same or different and is hydrogen or alkyl;R is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkynyl, alkoxy, phenyl, hydroxy, amino, alkylamino, phenylamino or halogen;X is hydrogen, alkyl, alkynyl, allyl, methallyl, cycloalkyl, alkyl having one or more hydroxy groups, phenyl, substituted phenyl, alkyl having one or more phenyl groups, alkyl having one or more substituted phenyl groups, bicycloalkyl, naphthylalkyl, acenaphthylenylalkyl or a compound represented by Formula (II) or Formula (III) ##STR2## wherein Z is hydrogen, hydroxy or lower alkoxy;Q is hydrogen or hydroxy;A is --CH.sub.

Abstract: Methods are described for identifying the amino acid residues of an antibody variable domain which may be modified without diminishing the native affinity of the domain for antigen while reducing its immunogenicity with respect to a heterologous species and for preparing so modified antibody variable domains which are useful for administration to heterologous species. Antibody variable regions prepared by the methods of the invention are also described.

Abstract: The invention is directed to monoclonal antibodies reactive with a member of the V.beta.3 family variable region of the beta chain of the TCR. More particularly, the invention provides for detection of the V.beta.3.1 subfamily. In a specific embodiment the invention provides for detection of V.beta.3.1, without cross-reacting with other V.beta.3 family variable regions. In a specific embodiment, the monoclonal antibodies of the invention do not react with V.beta.3.2. In particular, the invention provides monoclonal antibodies, termed 5E4 and 8F10, which react with the variable region of a member of the V.beta.3 family. In various embodiments of the invention, these antibodies, or fragments or derivatives thereof, can be used to bind with a member of the V.beta.3 family TCR variable region amino acid sequences, either as part of an intact TCR or peptide, or T cell-surface molecule, or a fragment thereof.

Abstract: An anti-inflammatory drug comprising as the effective component at least one compound selected from the group consisting of colominic acid, partial hydrolysis products of colominic acid and pharmaceutically acceptable salts, thereof. The drug is used as a drug for renal diseases, a drug for hepatitis, an immunomodulator and a drug for inhibiting the chemotaxis of neutrophil.

Abstract: An improved method for suppressing xenograft rejection in a host subject is disclosed. The method includes administering an immunosuppressant drug, where the drug or the amount of drug administered is, by itself, ineffective to suppress xenograft rejection. Effective xenograft suppression is achieved by also administering an ethanolic extract of Triterygium wilfordii or a purified triptolide component thereof.

Abstract: Compositions of finely divided powder of safflower seed or its extract, and methods for the treatment of rheumatoid-based arthritic diseases and menopause.

Abstract: This invention provides a method for alleviating the symptoms of arthritis in mammals which comprises orally administering a composition obtained by separating water-insoluble undenatured Type II collagen containing animal tissue from animal tissue not containing Type II collagen, subdividing and sterilizing said tissue under conditions which do not change the original structure of the Type II collagen, in an amount effective and for time effective to alleviate such symptoms.

Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.

Abstract: A formulation for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible nerve blockade when implanted or injected in a patient, and an amount of colchicine effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without colchicine.

Abstract: The present invention relates to a ketoprofen liposome gel and a process for its preparation which is distinguished by a simple method of preparation by spontaneous formation of liposomes from phospholipids and ketoprofen.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

Abstract: The invention is directed to a method of treating a T cell-mediated autoimmune disease in animals, including humans, by the oral administration of autoantigens, fragments of autoantigens, or analogs structurally related to those autoantigens, which are specific for the particular autoimmune disease. The method of the invention includes both prophylactic and therapeutic measures.

Abstract: Compounds and methods of making them having the following formula are described which bind to selectin receptors and thus modulate the course of inflammation, cancer and related diseases by modulating cell-cell adhesion events: ##STR1## wherein each R.sup.1 is independently H or lower alkyl (1-4C); R.sup.2 is H, OH or lower alkyl (1-4C), or a lipophilic group such as a higher alkyl group (5-15C), alkylaryl or one or more additional saccharide residues;R.sup.3 is a negatively charged moiety including SO.sub.4.sup.2-, PO.sub.4.sup.2-, or related group;Y is H or lower alkyl (1-4C); andX is H or --CHR.sup.4 (CHOR.sup.1).sub.2 CHR.sup.5 OR.sup.1 wherein R.sup.4 and R.sup.5 are each independently H, lower alkyl (1-4C), or taken together result in a five- or six-membered ring optionally containing a heteroatom selected from the group consisting of O, S, and NR.sup.1 ;said five- or six-membered ring optionally substituted with one substituent selected from the group consisting of R.sup.1, CH.sub.2 OR.sup.1, OR.sup.

Abstract: A method of treating rheumatoid arthritis is provided which involves administering an effective amount of allogeneic mononuclear cells or a molecule derived from these cells to an individual having rheumatoid arthritis. Also provided are compositions for the treatment of rheumatoid arthritis.

Abstract: The present invention is directed to a method and pharmaceutical formulations for the treatment of autoimmune arthritis and animal models therefore in mammals, including humans, by the oral, enteral or by-inhalation administration of whole collagen protein or biologically active peptide fragments of collagen.

Abstract: Arthritic conditions treated by oral administration of inorganic nickel compound(s), with or without bromide(s). In an especially preferred embodiment, the nickel compound used to treat these conditions is NiBr.sub.2.

Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.

Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.

Abstract: A therapeutic herbal composition including Trigonella foenum-graecum seed, Syzygium aromaticum fruit, Allilum sativum bulb, Cinnamonmum zyelanicum bark, Saussurea costus root and Euphorbia lathyris bud which includes an effective amount of sodium chloride to promote the digestibility and storage stability of the compositions, have been shown effective in reducing cholesterol, and triglycerides. This herbal composition has use in lowering cholesterol and treating arthritis, blood pressure and Alzheimer's disease. It is also effective as a bitters tonic.