Abstract: There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin .alpha. and preventing nuclear importation and integration of the HIV viral genome into the host cell DNA, thereby preventing viral infection.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.

Abstract: Cancer cells are blocked from entering differentiation pathways because of abnormal methylation enzymes, which are responsible for keeping cancer cells in cycling state. Effective differentiation inducers are those capable of acting directly or indirectly to convert abnormal methylation enzymes into normal enzymes, thereby enabling cancer cells to undergo terminal differentiation. Differentiation employing inducer alone often can not reach completion because of the damage created by the inducer. Such damage can be prevented if differentiation is induced in the presence of helper inducers, which are basically inhibitors of the component enzymes of methylation. Thus, differentiation induced in the presence of helper inducers is more likely to reach completion. Therefore, helper inducers are essential components of differentiation therapy, not just merely to potentiate the activity of differentiation inducers.

Abstract: Compounds of formula I, ##STR1## wherein the substituents R.sub.1 -R.sub.4 and a have the given meanings and show an activity against inflammatory conditions.

Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.

Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.

Abstract: Pharmaceutical compositions having antiviral, antiinflammatory and other activities are disclosed. The compositions are of compounds derived from diterpene phorboids.

Abstract: An insect repellent including a liquid system containing DEET and a fragrance oil which acts as a carrier for dispersing DEET vapor into the atmosphere upon evaporation of the fragrance oil. In one embodiment of the invention, the liquid system is contained within a solid thermoplastic system which can be formed as pellets for fabricating utilitarian products, e.g., wristbands and tablecloths. In another embodiment of the invention, the liquid system is contained within the wax of a candle which can be burned to emit DEET vapor into the atmosphere. In a third embodiment, the liquid system can be mixed with alcohol, with or without water, and dispersed by an air-wick to repel insects. In a fourth embodiment, towelettes can be soaked in the liquid system for later use as applicators of the liquid system to areas of the skin from which Deet vapor can be released into the atmosphere for effectively repelling insects from around the entire body.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: A method and composition is provided for treating skin conditions including those arising from dermatologic disorders, chronoaging and environmental abuse. Non-ring esterified C.sub.11 -C.sub.30 alkyl or alkenyl esters of salicylic acid in combination with a retinol C.sub.18 -C.sub.30 fatty acid ester used as the active components are applied to the skin in a pharmaceutically acceptable carrier. Most preferred as the salicylate ester is tridecyl salicylate and as the retinol fatty acid ester is retinyl linoleate.

Abstract: Compositions for controlling the growth of microorganisms in or on a product, material or medium comprising synergistically effective amounts of halogenated acetophenones, such as 2-bromo-4-hydroxyacetophenone, and at least one organic acid, its salt or ester are disclosed. Methods to control the growth of microorganisms and prevent spoilage caused by microorganisms with the use of the compositions of the present invention are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a residue of the formula ##STR2## and R.sup.2 -R.sup.10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.

Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.

Abstract: A hazard-free method for controlling insects using a non-toxic composition. The invention includes a process for making the composition in the form of a fragrance and crystalline particles which puncture directly through the exoskeleton of an insect. In operation, the particles work themselves between the insect's protective body plates and then puncture the exoskeleton permitting entry of the fragrance into the body of the insect. Once inside, the particles absorb up to four times their weight of the vital body fluids of the insect and the fragrance has a neural effect on the insect.

Abstract: Topical compositions for the treatment of corns and calluses comprising a 4 carbon .alpha.-keto acid and a pharmaceutically acceptable carrier, are described.

Abstract: Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.

Abstract: Various hydroxy benzaldehyde derivatives including Vanillin, a natural product derived from the vanilla bean that is commonly used as a flavoring agent, is administered by injection (i.v., i.m., s.c., and the like) or intravenous infusion in an effective dose amount to a patient in need of calming or sedation.

Abstract: A Saishin N derivative represented by the following general formula: ##STR1## wherein X represents a carbonyl group or a >CH--ORx group, or X bonds to a carbon atom in Y or Z to represent a >C(ORx)--O-- group; Y and Z may be the same or different and each represents a carbonyl group or a >CH--ORy group, or each bonds to an oxygen atom in X to represent a >CH-- group; the broken line represents an optional bond; and Rx and Ry may be the same or different and each represents a hydrogen atom or an alkyl, alkenyl, aralkenyl, aralkyl, heterocyclic-alkyl or acyl group, is provided which is therapeutically usable as an antiulcer agent.

Abstract: Compositions comprising a compound of formula I ##STR1## where R and R' are independently selected from hydrogen and alkyl of 1 to 4 carbon atoms, R" is a moiety selected from the group consisting of (a) hydrogen, (b) a halogen atom selected from the group consisting of F, Cl, Br, and I, and (c) a nitro group, or the hydrochloride salt of said compound; and at least one preservative are disclosed which are synergistically effective compared to the respective components alone in controlling and/or reducing the growth of microorganisms in or on a material or medium. Methods to control and/or reduce the growth of microorganisms and prevent spoilage caused by microorganisms with the use of the compositions of the present invention are also disclosed.

Abstract: Various .beta.,.gamma.-dihydropolyprenyl alcohol derivatives having the formula: ##STR1## wherein n is an integer of 5 to 7 and R is hydrogen, a lower alkyl group or an aliphatic or aromatic acyl group are effective at pritigating stress in animals.

Abstract: Compositions for oral administration for the treatment of gastric disorders comprising histamine H.sub.2 -receptor antagonist, and antacid, optimally buffered to promote local absorption of the H.sub.2 -receptor antagonist, wherein the quantity of H.sub.2 -receptor antagonist per unit dosage form is less than 25 mg.

Abstract: Compounds of the formula ##STR1## where W is (CH.sub.2).sub.n where n is 1 or 2, or n is 0 and W represents lower alkyl groups attached to each oxygen;m is an integer between 1 and 8;R.sub.1 is COOH or a pharmaceutically acceptable salt thereof, COOR.sub.4, CONR.sub.5 R.sub.6, CONR.sub.5 SO.sub.2 R.sub.7, CH.sub.2 OH, CH.sub.2 OR.sub.7, CH.sub.2 O--COR.sub.7, CH.sub.2 O--CONR.sub.5 R.sub.7, CH.sub.2 OCOOR.sub.7, CH.sub.2 NH.sub.2, CH.sub.2 NR.sub.5 R.sub.6, CH.sub.2 NR.sub.5 COR.sub.7, CHO, CH(OR.sub.8).sub.2, CH(OR.sub.9 O), --COR.sub.10, CR.sub.10 (OR.sub.8).sub.2, or CR.sub.10 OR.sub.9 O, where R.sub.4 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.4 is phenyl or lower alkylphenyl, R.sub.5 and R.sub.6 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.7 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.8 is lower alkyl, and R.sub.

Abstract: Methods for visibly reducing a skin wrinkle and for reversing the effect of aging on human facial skin involving comprising topically applying to the wrinkle and/or affected facial skin saccharic acid or saccharolactone.

Abstract: An improved dental root canal bacterialcidal lubricant for allowing the cleaning wires or files to move more freely when removing a nerve from a tooth. The composition reduces packing of tissue and dentin debris within the nerve cavity. This new formulation is also resistive to decomposition during cold weather shipping and includes cetyl alcohol, stearyl alcohol, sodium lauryl sulfate, stearic acid, propylene glycol, methyl paraben, propyl paraben, butyl, paraben all in a purified (spring) water solution.

Abstract: Dialkyl ethers lower Lp(a) and triglycerides, and elevate HDL-cholesterol, and are thereby useful for treating vascular diseases and noninsulin-dependent diabetes mellitus.

Abstract: The present invention provides methods for treating autoimmune disease in humans by administering to an afflicted host pharmaceutical compositions containing a therapeutically effective amount of a combination of ##STR1## in a weight ratio ranging from about 1:1 to about 1:10 (A:B); wherein R is OH, NH.sub.2, OW, or H;X is H, F, Cl, Br, I, OH, OW, NO.sub.2, or NH.sub.2 ;Y is H, F, Cl, Br, or I;W is ##STR2## or a C.sub.1 to C.sub.12 aliphatic group; Z is an aliphatic or aromatic group of C.sub.1 to C.sub.12 ;X and Y can both vary within the compound; or pharmaceutically acceptable salts thereof.Particularly disclosed herein is a composition comprising a 1 to 4 ratio of the sodium salts of phenylacetylglutamine and phenylacetic acid, formulated in both oral and parenteral forms clinically useful in the treatment of rheumatoid arthritis, lupus erythematosus, vasculitis, insulin dependent diabetes mellitus and multiple sclerosis.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes of the phorbol-, resiniferonol- and ingenol-classes.

Abstract: Synergistic antimicrobial combinations comprising 1,2-dibromo-2,4-dicyanobutane and at least one ester of parahydroxybenzoic acid are disclosed. Methods for using these synergistic combinations to inhibit microbial growth are also disclosed.

Abstract: Compositions for oral administration for the treatment of gastric disorders comprising histamine H.sub.2 -receptor antagonist and antacid, optionally buffered to promote local absorption of the H.sub.2 -receptor antagonist, wherein the quantity of H.sub.2 -receptor antagonist per unit dosage form is less than 25 mg.

Abstract: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof.

Abstract: The present invention relates to a method of treating hyperproliferative epithelial lesions by topical administration. The method prevents growth and actively cross-links these aberrant cells, thereby killing the cells. The present invention is useful in control and prevention of hyperproliferative epithelial disorders, such as HPV-infected cell lesions, actinic keratosis, melanomas, and malignant and pre-malignant carcinomas.

Abstract: Disclosed are a novel class of antiandrogenic compounds including saturated and unsaturated fatty acids, catechin gallates, their derivatives, and synthetic analogs, their method of synthesis, and their use in treating disorders associated with androgenic activities. Also disclosed is the use of known compounds not previously known for their antiandrogenic activity in treating disorders related to androgenic activities and cancers.

Abstract: A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.

Abstract: A pharmaceutical or cosmetic composition comprising in combination, a retinoid and a sterol inhibits the biosynthesis of cholesterol, is disclosed wherein a synergistic effect, principally in the treatment of disorders of epidermic keratinization, disorders of epidermic or epithelial proliferation and/or disorders of sebaceous function, is exhibited.

Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.

Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--;wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole;wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation;wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons;wherein p and q are integers from 0 to 20;wherein n is 0 or 1; andwherein m is 0, 1, 2, or 3.

Abstract: This invention relates to methods for treating Adult Respiratory Distress Syndrome (ARDS) which involves the administration of 2,3-alkylcarbonyloxybenzoic acid and salts thereof wherein the alkyl group has 2-18 carbon atoms.

Abstract: A therapeutical use is provided for cornpounds selected from the group which consists of (a) phenols of formula (I): ##STR1## wherein R is a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C1-12 alkoxy group, a formyl group, a C2-12 alkanoyl group, a C1-12 hydroxyalkyl group, a primary, secondary or tertiary amide group, an OCH.sub.3 group, CH.sub.2 OH or a COOH group or an A--COOH group where A is a C1-11 aliphatic hydrocarbon residue; and (b) the corresponding salts and esters thereof when R is COOH or A--COOH; for obtaining an antiviral drug for use in the human or veterinary therapeutical treatment of viral diseases.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodobenzoic acid derivatives as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Abstract: A method for inducing the production of interleukin 2 in a warm blooded animal by administering an effective amount of a compound of the formula (I) ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.

Abstract: Compositions for controlling the growth of microorganisms in or on a product, material or medium comprising synergistically effective amounts of halogenated acetophenones, such as 2-bromo-4-hydroxyacetophenone, and at least one organic acid, its salt or ester are disclosed. Methods to control the growth of microorganisms and prevent spoilage caused by microorganisms with the use of the compositions of the present invention are also disclosed.

Abstract: Compositions for controlling the growth of microorganisms in on a product, material or medium comprising synergistically effective amounts of methylene-bis(thiocyanate) and at least one organic acid, its salt or ester are disclosed. Methods to control growth of microorganisms and prevent spoilage caused by microorganisms with the use of the compositions of the present invention are also disclosed.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.

Abstract: The present invention relates to new polycyclic aromatic derivatives, to processes for their preparation and to their use in therapeutic and cosmetic formulations.

Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.

Abstract: Compounds having the formula ##STR1## are useful as inhibitors of protein kinase C. Also disclosed are pharmaceutical compositions including such compounds and methods for using such compounds to inhibit protein kinase C in animals, including man.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p -- (CR.sub.3 =CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p -- C.dbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.

Abstract: Compound of the formula ##STR1## where R is CH.sub.3 (CH.sub.2).sub.m, A and B are hydrogen, a bond or --(CH.sub.2).sub.n,X is ##STR2## m is 0, 1 , 2 or 3, n is 1 , 2, or 3, R.sub.1 is hydrogen or lower alkyl, andY is --OH, --OR.sub.2 or --NR.sub.3 R.sub.4where R.sub.2, R.sub.3 and R.sub.4 are hydrogen or unsubstituted or substituted alkyl, aryl and aralkyl substituents.