Abstract: Disclosed is an intraocular pressure reducing method and composition wherein 11-acyl prostaglandins are contained in a pharmaceutically acceptable excipient for topical application to the surface of the eye.

Abstract: The present invention relates to a method of inhibiting the protein kinase C-mediated biological response inflammation. The method comprises administering to a mammal a non-tumor promoting 12-deoxyphorbol ester. Phorbol esters suitable for use in the method include 12-deoxyphorbol 13-monoesters wherein the ester is a formate, acetate, propionate, butyrate, pentanoate, hexanote, benzoate or phenylacetate ester. The invention also relates to novel 12-deoxyphorbol 13-monoesters, wherein the ester can be a formate, propionate, butyrate or pentanoate ester, and to pharmaceutical compositions comprising same.

Abstract: Sensitizing tumoral cells to anticancerous drugs and/or inhibiting the tumoral cells resistance to antitumoral drugs employing as a modulator agent a vinca alkaloid dimer, analog to vinblastine or vincristine, with a low cytotoxicity or devoid of cytotoxicity, comprising at least one stereoisomerism different from that of vinblastine or vincristine in the C-14', C-16' or C-20' position. Notably, the modulator agent may have the R absolute configuration in the C-16' position.

Abstract: An emulsified composition having an average particle size of 0.010 to 0.070 .mu.m contains at least the following components (A), (B) and (C):(A) a lipid-soluble drug and a lipid;(B) glycerol and water;(C) a phospholipid and/or a water-soluble nonionic surfactant having a molecular weight of 1000 or more, with (A)/(C) being 0.5 to 5 (weight ratio).

Abstract: This invention relates to a composition comprising a tramadol material and acetaminophen, and its use. As used herein tramadol refers to various forms of tramadol. The compositions are pharmacologically useful in treating pain and tussive conditions. The compositions are also subject to less opioid side-effects such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, where the components of the compositions are within certain ratios the pharmacological effects of the compositions are superadditive (synergistic).

Abstract: A composition embraces an oil, for instance, a mineral oil, animal oil, or plant or vegetable oil, in combination with an acetal that can release aldehyde functionality on aqueous contact. It may be used in a method for kill or control of bacterium or virus for a suitable part of a human being or animal subject. For example, a 5% mineral oil and 2,2'-trimethylenebis(1,3-dioxolane) mixture can be used as a microbiocidal lubricant for drill bits in dentistry, or a suitably formulated composition may be used topically.

Abstract: The present invention relates to an anxiolytic drug comprising as an active ingredient a 1-amino-5-halogenouracil represented by formula [I]: ##STR1## wherein X represents a halogen atom, or pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents are amino acids and their derivatives which contain an active nitrogen-containing group. Particular agents comprise lysine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

Abstract: A method of targeting a diagnostic or therapeutic agent to a focus of infection comprises injecting a patient infected with a pathogen parenterally with an antibody conjugate which specifically binds to an accessible epitope of the pathogen or of a pathogen-associated antigen accreted at the focus of infection, the antibody conjugate further comprising a bound diagnostic or therapeutic agent for detecting, imaging or treating the infection. Polyspecific composite conjugates enhance the efficacy of the method, which is especially useful for treating infections that are refractory towards systemic chemotherapy.

Abstract: The specification discloses a method for enhancing the inhibiting action of drugs against multidrug resistant cells, representing various parasitic diseases, apparently by reversing the glycoprotein "pumps" associated with such cells.

Abstract: The present invention is a cyclization process utilizing the catalyst copper aluminum borate which process comprises the step of contacting (1) a compound having a fragment in which a carbon-containing chain of at least three atoms in sequence is bonded at one end thereof to a nitrogen, oxygen, or sulfur atom, and at the opposite end to a carbon, nitrogen, oxygen, or sulfur atom, where the latter are bonded to at least one hydrogen atom; with (2) a catalyst comprising at least one member selected from the group consisting of copper aluminum borate and zero valent copper on a support comprising aluminum borate, under conditions sufficient to effect ring closure between the ends of the fragment to obtain a compound comprising a heterocyclic ring.

Abstract: A nutritional supplement, functioning as a food for special dietary use, enhances diets and assists persons recovering from addiction to health damaging substances. Since cellular damage and deficiencies occur and continue to exist even after the person has stopped abusing the substances, use of the nutritional supplement, which contains a variety of minerals, vitamins, herbs, amino acids, and other substances and nutrients, should be continuous. The nutritional supplement consists of a mixture of nutrients which cooperate synergistically in enhancing cellular metabolic pathways and assists in normalization of cellular functions and optimization of cellular health.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamass) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: The present invention relates to a method and pharmaceutical composition for treating fever blisters or cold sores in mammals, and particularly in humans, by topically administering a pharmaceutical composition comprising ethyl alcohol in a concentration of at least 85% W/V and lidocaine in a concentration of 0.5-10% W/V at a periodicity of at least 10 to 12 times daily.

Abstract: The present invention provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells which comprises treating the cells so as to render them resistant to an antitumor agent and contacting the resulting resistant cells under suitable conditions with an amount of a compound effective to selectively induce terminal differentiation of such cells. The compound has a structure:[R-A ]-B-[A.sub.1 -B.sub.1 -].sub.a [A.sub.2 -B.sub.2 -].sub.b [A.sub.3 -R.sub.1 ].The invention also concerns a method of treating a patient having a tumor characterized by proliferation of neoplastic which comprises administering to the patient an amount of an antitumor agent to render the cells resistant to the antitumor agent and subsequently administering to the patient an amount of the compound effective to selectively induce terminal differentiation of such neoplastic cells and thereby inhibit their proliferation.

Abstract: The present invention relates to a method of inhibiting cell proliferation and lysyl hydroxylase expression. The method involves the use of minoxidil derivatives. The inhibitory activity of hydroxy derivatives of minoxidil is such that these compounds can be used as selective antifibrotic agents.

Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, composition is disclosed which comprises 1,2-disubstituted benzimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.

Abstract: A pesticidal organotin formulation is a water dispersible solid concentrate comprising at least one pesticidal organotin compound and polyvinylpyrrolidone. The formulation is prepared by dissolving the organotin compound and the polyvinylpyrrolidione in a solvent, followed by removal of the solvent, preferably by evaporation at a pressure below atmospheric pressure to yield the solid concentrate. The formulation may be dispersed in water, either with or without agitation, to yield an aqueous dispersion which may be applied to a locus to combat pests, especially acarids.

Abstract: Compounds that provide non-teratogenic effects and lack irritation to the skin are shown in the formula below where the partially drawn ring signifies an aromatic ring which may be carbocyclic or heteroaromatic, 6-membered or 5-membered, and may be condensed with another ring. R.sub.1 is lower alkyl, Cl, Br, or I, R.sub.2 is H, lower alkyl, Cl, Br, or I, and R.sub.3 is lower alkyl, Cl, Br, I, or is an ether, thioether, ester, thioester, amine or substituted amine group.

Abstract: The present invention relates to a quinolone carboxylic acid derivative represented by the following the formula (I), ##STR1## wherein R.sub.1 is a lower alkyl group, R.sub.2 is a hydrogen atom or a lower alkyl group, R.sub.3 is a hydrogen atom or a halogen atom, R.sub.4 and R.sub.5 together form a five- or six-membered ring which may contain hetero atoms or may have substituents, provided that a compound wherein R.sub.1 is a methyl group, R.sub.2 and R.sub.3 are hydrogen atom and ##STR2## is a piperazinyl group is excluded; or a salt thereof; to an antimicrobial agent comprising the same as an effective component; and to an intermediate for producing same.