Abstract: This invention provides a method for repelling biting insects such as mosquitoes, ticks, and biting flies by topically applying to the skin of a subject emu oil, fractions of emu oil obtained by flash chromatography or a composition comprising emu oil or active fractions thereof and at least one other insect repellent such as citronella, DEET or saponin. Also provided are compositions for repelling biting insects comprising diluted fractions of emu oil, and compositions comprising emu oil or active fractions thereof and at least one other insect repellent such as citronella, DEET or saponin.

Abstract: Disclosed are antitumor compositions comprising taxol, taxotere or their derivatives in combination with an anthracycline antibiotic, the combination having a pharmacologic activity greater than the expected additive effect of its individual components.

Abstract: The present invention related to compounds represented by the following formula (I) and salts thereof, ##STR1## wherein R.sup.1 and R.sup.4 each represents a carboxyl or a carboxyl which is converted into an ester, an amide or hydroxamic acid; R.sup.2 represents a lower alkyl or a phenyl-lower alkyl; R.sup.3 represents a hydrogen atom, a lower alkyl, an amino-lower alkyl, a lower alkylamino-lower alkyl, a hydroxy-lower alkyl, a mercapto-lower alkyl, a carboxy-lower alkyl, a lower alkoxycarbonyl-lower alkyl, an imidazolyl-lower alkyl, an indolyl-lower alkyl, a (substituted) phenyl group, a (substituted) phenyl-lower alkyl group, a (substituted) naphthyl group, or a (substituted) naphtyl-lower group. The compounds of the present invention have inhibitory effects on endopeptidase 24.

Abstract: The present invention relates to novel colchicine derivatives of formula (1), where Y is a --CH.sub.2 --CH--NH--R.sub.3 group or a --CH--CH.sub.2 OR.sub.3 group and the other variables are as defined in claim 1, having antiproliferative, antitumoral and anti-inflammatory activities. The novel compounds have a cytotoxicity on human tumoral cell lines comparable with colchicine, but, in comparison with the latter, they are less toxic and more selective, particularly on cells resistant to the usual medicaments. Some compounds have a marked activity on TNF and interleukine 2, and therefore are very potent anti-inflammatory agents. They can be included in pharmaceutical formulations useful for the parenteral, oral and topical administrations.

Abstract: Methods of introducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a genetic vaccine facilitator and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produce a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.

Abstract: This invention relates to a naphthoquinone derivatives, to processes and to intermediates for preparing these derivatives, to pharmaceutical composition and to the use of these derivatives as antitumor agents in mammals.

Abstract: An external preparation for skin comprising at least one member selected from the group consisting of escinol and its salts represented by the following constitutional formula (1): ##STR1## (wherein R.sup.1 is hydrogen atom or hydroxyl group and R.sup.2 is pyranose residue.)Due to the effect of escinol which characterizes the present invention, the external preparation in accordance with the present invention is excellent in whitening effect and has a high safety.

Abstract: The invention relates to the use of Medicago saponins for the preparation of cosmetic or pharmaceutical compositions. The invention provides for the incorporation of 0.01% to 5% by weight of a saponin or a corresponding sapogenin, or a plant extract in which it is present, originating in particular from lucerne leaves or roots. The invention makes it possible to promote renewal of the epidermis, stimulate hair regrowth or delay hair loss, or else to combat the effects of ageing on the state of the skin and scalp, as is evident from the FIGURE.

Abstract: Administration of argininosuccinate synthetase activity reducing agents, e.g., argininosuccinate synthetase induction blocking agents (e.g., antibiotics that bind to DNA sequences present in the upstream regulatory region of the argininosuccinate synthetase gene, such as mithramycin) and argininosuccinate synthetase inhibitors (e.g., L-citrulline antagonists such as methyl citrulline and L-aspartate antagonists such as D-aspartate) is useful to prevent or treat sepsis or cytokine-induced systemic hypotension, is useful in the treatment of sepsis or cytokine-induced systemic hypotension to restore vascular sensitivity to the effects of .alpha..sub.1 -adrenergic agonists, and is useful to suppress an immune response, e.g., in treating inflammation. In one embodiment, certain argininosuccinate synthetase activity reducing agents are used together with arginine antagonists to treat sepsis or cytokine induced hypotension.

Abstract: The present invention relates to new antifungal compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, methyl, or hydroxymethyl; R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen and C.sub.1-5 alkyl; and R.sup.4 is selected from the group consisting of .beta.-L-xylosyl, .beta.-D-ribosyl, .alpha.-L-arabinosyl, .beta.-D-chinovosyl, .beta.-D-fucosyl, and .beta.-D-glucosyl; with the proviso that when R.sup.1 is methyl or hydroxymethyl, and one of R.sup.2 or R.sup.3 is methyl, R.sup.4 is not .beta.-D-glucosyl; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed herein are modified saponins or fractions thereof obtainable by modification of a crude Quillaja saponaria extract or by modification of purified saponins obtainable from a crude Quillaja saponaria extract useful in pharmaceutical compositions for enhancing the transport of pharmacologically active substances across mucous membranes of an animal. Also disclosed are modified saponins having reduced irritability wherein the aldehyde group is reduced and the fatty acid moiety may be removed by hydrolysis. Also disclosed are pharmaceutical compositions comprising the modified saponins of the invention.

Abstract: The present invention relates to a method of treating a patient suffering from a neoplastic disease state comprising administering to said patient an effective antineoplastic amount of N,N'-bis[3-(ethylamino)propyl]-1,7-heptanediamine in conjunctive therapy with an effective antineoplastic amount of a cytotoxic agent selected from the group consisting of an antineoplastic vinca alkaloid, an antineoplastic antibiotic, an antineoplastic antimetabolite and an antineoplastic platinum coordination complex, wherein a synergistic antineoplastic effect results.

Abstract: Hayumicin compounds, obtainable by cultivation of a strain of Actinomadura sp. designated ATCC 55432, and analogs of these compounds. The novel compounds have antitumor as well as antibiotic, particularly antibacterial, activity.

Abstract: Methods for treating mammals to reduce pain and/or reduce inflammation are described based on administering to the mammals synthetic ether derivatives of pseudopterosin having the formula: ##STR1## wherein A is an alkyl, aryl or amide group having from 2 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 are hydrogen or an acyl residue (--COR) having from 1 to 6 carbon atoms, R.sub.4 is hydrogen or --CH.sub.2 OH and R.sub.5 is a hydrocarbon having from 1 to 10 carbon atoms. Also disclosed are synthetic compositions having the above general formula which are useful in the described method.

Abstract: This invention relates to an etoposide preparation containing an etoposide composition comprising an etoposide, polyvinylpyrrolidone, and water-soluble cellulose ether derivative wherein the proportion of the respective components is about 0.25 to 2 parts by weight for polyvinylpyrrolidone and about 0.0028 to 0.2 parts by weight for the water-soluble cellulose ether derivative per 1 part by weight of the etoposide, and about 10 to 20% (w/w) for the etoposide in the whole amount of the composition.

Abstract: Methods of promoting wound healing and the growth and proliferation of keratinocytes, fibroblasts and endothelial cells are disclosed. These methods comprise contacting a wound with an effective wound healing amount of a composition comprising a pseudopterosin or pseudopterosin derivative.

Abstract: The use of active gibberellins for the preparation of a pharmaceutical composition for the treatment of prostatitis. The method results in a decrease in prostate mass.

Abstract: A production stimulator of nerve growth factor contains a new cyathane derivative of the form ##STR1## where R is either CHO or CH.sub.2 OH.

Abstract: Administration of argininosuccinate synthetase activity reducing agents, e.g., argininosuccinate synthetase induction blocking agents (e.g., antibiotics that bind to DNA sequences present in the upstream regulatory region of the argininosuccinate synthetase gene, such as mithramycin) and argininosuccinate synthetase inhibitors (e.g., L-citrulline antagonists such as methyl citrulline and L-aspartate antagonists such as D-aspartate) is useful to prevent or treat sepsis or cytokine-induced systemic hypotension, is useful in the treatment of sepsis or cytokine-induced systemic hypotension to restore vascular sensitivity to the effects of .alpha..sub.1 -adrenergic agonists, and is useful to suppress an immune response, e.g., in treating inflammation. In one embodiment, certain argininosuccinate synthetase activity reducing agents are used together with arginine antagonists to treat sepsis or cytokine induced hypotension.

Abstract: The present invention provides N- and O-substituted aminophenol derivatives of the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, G and L are as hereinbefore defined. The present invention also provides intermediates for the preparation of these aminophenol derivatives of general formula (I), as well as the use of the aminophenol derivatives of general formula (I) for the determination of hydrolases, as well as for the preparation of agents for carrying out determinations of hydrolysis.

Abstract: This invention relates to a pharmaceutical laxative composition in unit dosage form, for peroral administration of sennosides to a human or other animal subject, comprising a safe and effective amount of sennosides in a rapidly dissolving matrix; and a proximal colonic delivery carrier which effects release of said sennosides substantially near the junction between the small intestine and the colon or within the colon of said subject. This invention also involves methods for providing laxation for humans and other animals in need thereof by peroral administration of such compositions.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkoxy;R.sup.3 istetrazolyl, orand R.sup.4 and R.sup.5 are each hydrogen, hydroxy, acyloxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, optionally substituted phenyl, --SO.sub.3 H or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl;provided that when R.sup.3 is --CR'R".CHR'"CO.sub.2 H or tetrazolyl, R.sup.1 and R.sup.2 are each hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl C.sub.1-4 alkoxy; andor a pharmaceutically acceptable salt or ester thereof.

Abstract: Indole compounds substituted at the 3-position by a 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]thiazole, 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]oxazole, or 7-carbonyl(pyridin-3-yl)pyrrolo[1,2-c]pyrrole group are potent antagionists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointesinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.

Abstract: Disclosed herein are modified saponins or fractions thereof obtainable by modification of a crude Quillaja saponaria extract or by modification of purified saponins obtainable from a crude Quillaja saponaria extract useful in pharmaceutical compositions for enhancing the transport of pharmacologically active substances across mucous membranes of an animal. Also disclosed are modified saponins having reduced irritability wherein the aldehyde group is reduced and the fatty acid moiety may be removed by hydrolysis. Also disclosed are pharmaceutical compositions comprising the modified saponins of the invention.

Abstract: New cyathane derivatives shown by Formula (1) or (2) given below have the effect of stimulating production of nerve growth factors and antimicrobial effects: ##STR1## where R is either CHO or CH.sub.2 OH.

Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are piperazinyl benzyl compounds such as 1-[.alpha.-(4-Chlorophenyl)-3-methoxybenzyl]-4-allylpiperazine dihydrochloride.

Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are acrivastine esters and the pharmaceutically acceptable salts thereof.

Abstract: Disclosed are novel pradimicin compounds which possess antifungal activity and, preferably, improved water solubility. The compounds of the invention are prepared by modifying the 4'-amino or 4'-alkylamino moieties of known pradimicin compounds.

Abstract: The present invention relates to a freeze-dried preparation comprising (1) about 5 to about 50 W/W% of a non-volatile acid and/or a salt thereof, (2) about 10 to about 95 W/W% of 4-O-(2-deoxy-2-dimethylamino-4,6-O-ethylidene-.beta.-D-glucopyranosyl)-4'- demethyl-4-epipodophyllotoxin hydrochloride and (3) 0 to about 85 W/W% of at least one sugar as a stabilizer.

Abstract: Methods for enhancing the transport of pharmacologically active substances across mucous membranes of an animal by administration of pharmaceutical compositions comprising modified saponins or fractions thereof obtainable by modification of a crude Quillaja saponaria extract or by modification of purified saponins obtainable from a crude Quillaja saponaria extract. Also disclosed are modified saponins having reduced irritability wherein the fatty acid moiety is removed by hydrolysis or the aldehyde group is reduced. Also disclosed are pharmaceutical compositions comprising the modified saponins of the invention.

Abstract: The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.

Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are 2-(aminoethylamino) pyridines such as (E)-3-(6-(N-(2-Dimethylaminoethyl)-4-methoxybenzylamino)-2-pyridyl)acrylic acid.

Abstract: The present invention relates to a fermentation process for producing BMY-28960 and desxylosyl BMY-28960, and to a novel BMY-28960-producing organism belonging to the genus Actinomadura and designated as strain AB 1236 (ATCC 55208).

Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are acrivastine esters and the pharmaceutically acceptable salts thereof.

Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.

Abstract: Complexes of saponins from Centella asiatica, terminalia sp. and Terminalia sericea and relevant aglycons with phospholipids are described. The saponins may be asiaticoside, madecassicoside and sericoside. The molar ratio of phospholipids to saponins is from 0.5 to 2. The phospholipids are selected from the group consisting of soy lecithins, phospholipids from bovine or swine brain or cutis, phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine in which the acyl groups can be the same or different and are mostly derived from palmitic, stearic, oleic, linoleic, linolenic acids. Pharmaceutical compositions and the method of treatment are also described.

Abstract: Pharmaceutical compositions containing at least one of benanomicins A and B and their salts are now provided, which are useful to inhibit the infection of human T-cells with HIV, namely a virus causative of acquired human immunodeficiency syndrome (AIDS). Thus, benanomicins A and B as well as their salts are useful as antiviral agent against HIV.

Abstract: Complexes formed between aescin, cholesterol or .beta.-sitosterol and phospholipids are described. The molar ratio of phospholipids to aescin/.beta.-sitosterol or cholesterol is from 0.5 to 2. The phospholipids are selected from the group of soy or egg lecithins, phospholipids from bovine or swine brain or cutis, phosphatidylcholine, phospatidylserine, phosphatidylethanolamine in which the acyl groups may be the same or different and are mostly derived from palmitic, stearic, oleic, linoleic, linolenic acids, for instance, pharmaceutical compositions and a method for producing an anti-inflammatory effect in an animal are also described.

Abstract: As a new compound is now provided N-acetylbenanomicin B which is useful as an antifungal agent and also as antiviral agent for inhibiting infection of human T-cell with HIV, namely a virus causative of acquired human immunodeficiency syndrome. N-acetylbenanomicin B may be prepared by acetylation of 4"-amino group of benanomicin B which is fermentatively produced by a new microorganism, MH193-16F4 strain of actinomycetes.

Abstract: As a new antifungal and antiviral antibiotic is provided benanomicin A 4"'-O-sulfate or a salt thereof having formula (I) ##STR1## wherein M.sup.1 denotes a mono-valent alkali metal atom or a di-valent alkaline earth metal atom or a hydrogen atom and A denotes an organic base; n is zero when M.sup.1 is an alkali metal atom or alkaline earth metal atom but n is 1 or zero when M.sup.1 is a hydrogen atom, and M.sup.2 denotes a hydrogen atom or an alkali metal atom or an alkaline earth metal atom. This new compound is useful as antifungal agent to treat fungal infections in mammals and as antiviral agent to inhibitingly treat HIV.

Abstract: The present invention provides antitumor 4'-Demethylepipodophyllotoxin glycosides characterized by the fact that the glycoside moiety is altrose.

Abstract: Substantially pure saponins are disclosed. The saponins of the present invention are useful as immune adjuvants. Disclosed as well are immune response-provoking compositions comprising an antigen in admixture with the substantially pure saponins.

Abstract: Disclosed herein are pradimicin amides which are active as antifungel agents.

Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.

Abstract: A composition for the treatment of skin injuries is described including an antiseptic, a sapogenine, a proteolytic enzyme and a suitable vehicle. The composition is directly applied on the injury, forming a film which isolates and protects same from infection and suppresses pain. The film is self-adherent and transparent, which allows inspection of the healing injury, without the need of removing the film, as with bandages. The composition is antiseptic and microbiocidal, helps cicatrization and produces a biochemical debridement. The film allows the natural motility of the injury zone and produces a compression which helps to decrease or prevent edema. The film also allows the passage of air, preventing the production of anaerobiosis, decreasing the output of liquids, and preventing, in large injuries, dehydration and loss of electrolytes. The film can be removed merely by wetting.

Abstract: The association of chitin or chitosan with soy saponins in an orally administered composition has appetite moderating and antigastritis activity. The objectionable side effects of the two active ingredients are also eliminated in the composition.

Abstract: Disclosed herein are antibiotic BU-3608 D and E isolated from Actinomadura hibisca. These compounds are active antifungal agents.

Abstract: A method of preparing a triterpenoids from Ilex pubescens which includes extracting the Ilex pubescens roots with organic solvent to an initial extract and converting the initial extract to the triterpenoids exhibiting antithrombotic activity on humans or mammals. Also, a pharmaceutical composition containing an effective antithrombotic amount of the triterpenoids from the Ilex pubescens.

Abstract: This invention relates to a novel method for the delivery of cytotoxic drugs to tumor cells by the administration of a tumor-specific antibody-enzyme conjugate that binds to the tumor cells, and the additional administration of a prodrug that is converted at the tumor site, in the presence of the antibody-bound enzyme, to an active cytotoxic drug. According to preferred embodiments of this invention, antibody-enzyme conjugates containing the enzyme, alkaline phosphatase ("AP"), have been used in conjunction with the novel prodrug, etoposide-4'-phosphate or 7-(2'-aminoethyl phosphate)mitomycin or a combination thereof, to effect killing of tumor cells. According to another embodiment of the invention, an antibody-enzyme conjugate containing the enzyme, penicillin V amidase ("PVA"), has been used in conjunction with a novel prodrug, N-(p-hydroxyphenoxyacetyl)adriamycin to effect killing of tumor cells.

Abstract: An aqueous solution comprises lysozyme hydrochloride, dipotassium glycyrrhizinate, at least one selected from the group consisting of sodium chloride, potassium chloride, calcium chloride, magnesium chloride, sodium phosphate, potassium phosphate, sodium citrate, potassium citrate, sodium carbonate and potassium carbonate and water, has a pH of 5 to 9 and is useful for eye drops.