Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

Abstract: Anticonvulsant derivatives useful in treating autism.

Abstract: The naphthyloxyacetic acid derivatives of the formula (I) 1

Abstract: The invention concerns tye use of a inhibitor of retinoic acid as sole ingredient in a pharmaceutical or cosmetic composition comprising administering effective amount of the composition to treat sensitive skin or skin damage induced by UV radiation.

Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.

Abstract: The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I.The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

Abstract: A method of treating leukemia which includes administering an effective amount of composition comprising suramin and a biological response modifier, wherein the suramin and the biological response modifier show synergistic or additive anti-leukemic activity. A pharmaceutical composition is also disclosed.

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

Abstract: The use of a combination of an alpha RAR receptor-specific agonist ligand and a gamma RAR receptor-specific antagonist ligand to reduce the rate of apoptosis is disclosed.

Abstract: Tricyclic compounds are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, cancer metastasis, tumor angiogenesis, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes.

Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.

Abstract: Substituted triols are prepared by reducing appropriately substituted carboxylic esters. The substituted triols can be used as active substances in medicaments.

Abstract: This invention relates to a new and improved pharmaceutical composition and method for delivery of therapeutic or bioactive agents. The methods and composition of the invention can be used with several therapeutic or bioactive agents and can achieve site-specific delivery of a therapeutic or biologically-active substance. This can allow for lower doses and for improved efficacy with drugs, particularly agents such as oligonucleotides which are plagued with problems in achieving therapeutic levels at targeted sites.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Novel medicinally-useful compounds are provided herein. These compounds include isomeric cyclic tetramers of formaldehyde and 1-naphthol, and the derivatives or analogues of such cyclic tetramers, and linear oligomers of chromotropic acid, or its derivatives or analogues with naphthalene.

Abstract: Application of a compound having at least one sulfonic acid functional group which is at least partially non-neutralized, in a cosmetic or dermatological composition, to the skin is useful for treating intrinsic ageing of the skin.

Abstract: Compositions for improved topical delivery of lactic acid comprising lactic acid and an amphoteric or pseudoamphoteric agent.

Abstract: The invention is directed to a method of killing or inhibiting the growth of the malaria-causing pathogen Plasmodium falciparum by exposing the pathogen to an effective amount of a preparation comprising a compound selected from the group consisting of:a) a compound of formula I: ##STR1## where ##STR2## b) a compound of formula II; ##STR3## where each R' is --H or each R' is --OH; and c) a compound of formula III; ##STR4## where R" is --NH.sub.2, --H, or --SO.sub.3 M, and where M is H, Na, or K.

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

Abstract: Disclosed is a method of inhibiting hepatitis B infection by administering a therapeutically effective amount of a compound having the formula (Formula 1): ##STR1## wherein R1 is selected from the group consisting of H, lower alkanoyl, lower arylalkylacyl, arylacyl, and C-1-linked saccharide, and R2 is separately selected from the group consisting of H, lower alkyl, lower arylalkyl, aryl, and C-1-linked saccharide. The compounds may also be used to treat other conditions, such as inflammatory bowel disease, autoimmune diseases, transplant rejection, septic shock, and for protection against irradiation damage. Novel celastrol derivatives are also disclosed.

Abstract: This invention relates to an ocular hypotensive agent which comprises a compound represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon residue that may be bound via a hetero atom; R.sup.2 represents hydrogen or a hydrocarbon residue that may have a substituent; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X is a covalent bond between the 2 benzene rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n represents 1 or 2; ring A is a benzene ring having 1 or 2 optional substituents in addition to the group represented by COOR.sup.2, or a pharmaceutically acceptable salt thereof.

Abstract: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.

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: There are disclosed novel hydroquinone derivatives of the formula: ##STR1## The derivatives of the formula (I) have various pharmacological activities such as antioxidation in living bodies and are useful as medicaments.

Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.

Abstract: The invention describes the synthesis and use of photoactivated (or caged) fluorescent dyes. Upon illumination at less than about 400 nm the caged dyes release highly fluorescent, water soluble hydroxypyrenesulfonic acid dyes according to the following equation: ##STR1## X, Y, and Z are independently sulfonic acid, a sulfonic acid salt, a hydroxyl group, or hydrogen, with at least one of X, Y, and Z being a sulfonic acid or sulfonic acid salt. LINK is either an ether linkage or a carbonate linkage. BLOCK is a caging group whose photolysis results in liberation of a free hydroxypyrenesulfonic acid dye.The caged fluorescent dyes are useful for application in aqueous solutions, including fluids of biological origin. The caged dyes of the present invention are especially useful for flow tagging velocimetry.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: A is a bond or --OCH.sub.2 --, where the oxygen is linked to R.sup.1 ;B is --CH.sub.2 -- or when R.sup.3 is hydrogen, B may be --CH.sub.2 O-- where the oxygen is linked to the phenyl ring;R.sup.1 is an aryl group;R.sup.2 is hydrogen or lower alkyl;R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 together form the group --CH.sub.2 CH.sub.2 --; andR.sup.4 is --SO.sub.3 H, --P(O.sub.2 H)R.sup.5, --P(O.sub.2 R.sup.5')R.sup.5, --PO.sub.3 H.sub.2, --PO.sub.3 HR.sup.5' or --PO.sub.3 (R.sup.5').sub.2 where R.sup.5 and R.sup.5' are independently lower alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, for example, in the treatment of diabetes, obesity, achalasia, and gastrointestinal diseases.

Abstract: Calixarene derivatives, their synthesis and use as chloride channel blockers are described. Preferred calixarene derivatives are of the formula: ##STR1## wherein R is an acidic group or salt thereof, such as SO.sub.3 X or R.sup.1 SO.sub.3 X where X is H or Na, and R.sup.1 is ##STR2## where m=1-2, and R.sup.3 and R.sup.4 the same or different is each H or a C.sub.1-4 alkyl, or a nitrogen-containing group of the formula ##STR3## or A, wherein R.sup.5 is a C.sub.1-4 alkyl, R.sup.6 is a C.sub.1-4 alkyl and A is ##STR4## where R.sup.7 and R.sup.8, the same or different each is H or a C.sub.1-4 alkyl, and R.sup.9 and R.sup.10, the same or different, each is H or a C.sub.1-4 alkyl; R' is H or a C.sub.1-4 alkyl; and n is an integer of 4-8, preferably 4, 6 or 8.

Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.

Abstract: The present invention relates to methods for treating cachexia in a patient and inhibiting IL-6 bioactivity. This is accomplished by administering to a patient an effective amount of a sulfate-containing compound, for example, suramin, a derivative of suramin, Pentosan polysulfate, or Dextran sulfate. The present invention is also effective in combating IL-6 related diseases.

Abstract: The narrow poly- or mono-dispersed oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a recurring unit of from 3 to 50. These oligomers are water-soluble, preferably have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The narrow poly- or mono-dispersed oligomers are useful for the treatment and/or diagnosis of AIDS and/or ARC or HSV.

Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a macrocyclic compound composed of aryl ring subunits connected one to another by ring-attached bridge linkages, and containing sulfonic acid-derived substituents carried on non-bridge atoms of the subunits.

Abstract: 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.

Abstract: A compound and method for inhibiting cell infection by an enveloped virus. The compound is a macrocyclic chromotropic acid derivative which can be substituted at a variety of naphthalene ring and bridge positions. The compound may be administered parenterally, orally, or topically for treating infection by enveloped viruses.

Abstract: A method of inhibiting cell infection by herpes simplex virus-1 or -2. The method includes contacting the virus with a macrocyclic chromotropic acid compound, in an amount effective to inhibit cell infectivity of the virus.

Abstract: A series of new azulene analogues are disclosed, which are represented by the following formula: ##STR1## wherein: R.sub.1 is --COOH, --COOR.sub.4 (R.sub.4 represents a lower alkyl), --CH.dbd.CH--COOH, --CH.sub.2 --COOH or --SO.sub.3 H;R.sub.2 is a hydrogen atom or lower-alkyl group;R.sub.3 is a hydrogen atom, a lower alkyl or benzyl group;A is --SO.sub.2 --, ##STR2## (R.sub.5 represents a lower alkyl); B is a phenyl, a lower alkylphenyl, a lower alkoxyphenyl, nitrophenyl, trifluoroalkylphenyl, mono-or di-halogenated-phenyl, naphthyl or tetrahydroaphthyl group;Y is an alkylene or alkenylene group.The compounds of the present invention are useful as thromboxane A.sub.2 and prostagrandin endoperoxide receptor antagonists.

Abstract: This invention concerns certain diethyl- or dipropylacetic acid salts of sodium valproate which have physiological properties similar to those of valproic acid or sodium valproate but show highly superior stability characteristics.

Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.

Abstract: External preparations consisting essentially of about 0.1% to about 5% of tocopherol acetate and/or about 0.05% to about 0.3% of glycyrrhetinic acid, about 1% to about 15% of a methacrylic acid-ethyl acrylate copolymer, and about 0.2% to about 3% of a thickening agent in an alcoholic solvent, wherein said copolymer is characterized by that the monomer ratio of ethyl acrylate to methacrylic acid is within a range from 75/25 to 95/5, with residual monomer being 50 ppm or less and with practically no surfactants.

Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.

Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of dermatological disorders.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is an anthracene or substituted anthracene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

Abstract: This invention relates to novel [(2-substituted 1,2-dihydro-1-oxo-1H-inden-5-yl)oxy]alkanesulfonic acids and salts thereof. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, the neurological problems caused by AIDS, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions, and elevated intracranial pressure.

Abstract: A method of stimulating the immune response of a patient which comprises administering to a patient in need thereof an immunostimulating effective amount of 8,8'-[carbonylbis]imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene) carbonylimino]]bis-1,3,5-naphthalenetrisulphonic acid hexasodium salt.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid additon salts thereof; wherein Ar is a perylene or substituted perylene ring system; R.sup.1 contains not more than eight carbon carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl; R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

Abstract: A method of treating diabetes mellitus using arylglyoxals which are known compounds.

Abstract: A method of inhibiting the complement system using multisulfonated naphthalene ureas.

Abstract: The invention relates to contraceptive vaginal tablets as well as to a process for preparing them. The tablets of the invention have the following composition:0.2 to 3 parts by weight of boric acid,10 to 20 parts by weight of tartaric acid,1 to 2 parts by weight of vitamin K.sub.3 -sodium bisulfite adduct,0.8 to 1.2 parts by weight of polyvinyl pyrrolidone,2 to 5 parts by weight of magnesium stearate,8 to 12 parts by weight of carboxymethyl cellulose,8 to 12 parts by weight of lactose and50 to 65 parts by weight of microcrystalline cellulose.The vaginal tablets contain preferably 5 to 10 mg of vitamin K.sub.3 -sodium bisulfite adduct and have a total weight of 500 mg.The tablets of the invention are prepared preferably in such way that the boric acid, the tartaric acid and the vitamin K.sub.