Abstract: The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

Abstract: The present disclosure is generally directed to neuroactive substituted cyclopent[a]anthracenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The present disclosure is generally directed to neuroactive substituted cyclopenta[b]phenanthrenes as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: Compounds and methods that release 1-methylcyclopropene, 1-trifluoromethylcyclopropene, and other substituted cyclopropenes are disclosed. The compounds and methods overcome present limitations for storage, transportation, and application of the cyclopropene containing compounds by using light, including sunlight, and/or heat as the primary release trigger. Additional products released include innocuous gases and value added aryl-group compounds.

Abstract: This invention concerns product and process to convert a hydroxyl group (bold in R3C—OH) in a tigliane-type compound to a hydrogen (bold in R3C—H) to obtain deoxytigliane-type compounds or structural or functional analogs thereof. The process has wide application particularly to produce specific biologically active compounds in quantity for use as pharmaceuticals. In particular the process can be used to convert phorbol to a 12-deoxytigliane (prostratin), which is a therapeutic lead for the treatment of AIDS. New compositions of matter are also disclosed.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to methods of producing ingenol-3-angelate (I) from ingenol (II). Furthermore, the invention relates to intermediates useful for the synthesis of ingenol-3-angelate (I) from ingenol (II) and to methods of producing said intermediates.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gel formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: The present invention relates to an improved transdermal hydroalcoholic testosterone gen formulation that provides, among other things, a desirable pharmacokinetic hormone profile, and methods of use.

Abstract: [Problem to be Solved] An immunostimulant highly safe and administrable for a long period of time as well as a pharmaceutical composition containing the immunostimulant as an active ingredient and drink or food products for immunostimulation are developed and provided. [Solution] An immunostimulant containing a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient is provided. R1 is a hydrogen atom or a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms, R2 to R5 are independently a hydrogen atom, or a substituted or unsubstituted lower alkyl or lower acyl group, X is —(CH2)2—, —(CH2)3—, —(CH2)4—, —CO—CH2—, —CO—(CH2)2—, —CO—(CH2)3—, —CH2—CO—CH2—, —CO—O—CH2—, —CO—O—(CH2)2—, —O—CO—CH2—, —O—CO—(CH2)2—, —CH2—O—CH2—, —CH2—O—(CH2)2—, —O—CH2—, —O—(CH2)2—, —O—(CH2)3—, —NHY—CO—CH2—, —NHYCO—(CH2)2—, —CO—NHY—CH2— or —CO—NHY—(CH2)2—, Y herein is a hydrogen atom or a lower alkyl group.

Abstract: This invention concerns product and process to convert a hydroxyl group (bold in R3C—OH) in a tigliane-type compound to a hydrogen (bold in R3C—H) to obtain deoxytigliane-type compounds or structural or functional analogs thereof. The process has wide application particularly to produce specific biologically active compounds in quantity for use as pharmaceuticals. In particular the process can be used to convert phorbol to a 12-deoxytigliane (prostratin), which is a therapeutic lead for the treatment of AIDS. New compositions of matter are also disclosed.

Abstract: Compounds and methods that release 1-methylcyclopropene, 1-trifluoromethylcyclopropene, and other substituted cyclopropenes are disclosed. The compounds and methods overcome present limitations for storage, transportation, and application of the cyclopropene containing compounds by using light, including sunlight, and/or heat as the primary release trigger. Additional products released include innocuous gases and value added aryl-group compounds.

Abstract: Disclosed is a method for the screening of a compound having an activity to selectively modulate an androgen receptor. The method comprises the steps of: contacting a substance to be tested with a prostate cancer cell and measuring the level of expression of mRNA for a prostate-specific antigen or the level of production of the prostate-specific antigen in the prostate cancer cell; and contacting the substance with an adipocyte and measuring the level of expression of mRNA for uncoupling protein-1 or the level of production of uncoupling protein-1 in the adipocyte. Also disclosed is a selective androgen receptor modulator comprising a compound represented by any one formula selected from the structural formulae (I) to (III) as an active ingredient. Further disclosed is a composition for preventing or treating lifestyle-related diseases, which comprises the selective androgen receptor modulator.

Abstract: This invention concerns a process to convert a hydroxyl group (bold in R3C—OH) in a tigliane-type compound to a hydrogen (bold in R3C—H) to obtain deoxytigliane-type compounds or structural or functional analogs thereof. The process has wide application particularly to produce specific biologically active compounds in quantity for use as pharmaceuticals. In particular the process can be used to convert phorbol to a 12-deoxytigliane (prostrating which is a therapeutic lead for the treatment of AIDS. New compositions of matter are also disclosed.

Abstract: A catalyst composition for a cross-coupling reaction comprising a nickel salt-amine complex of formula (1), and triphenylphosphine. where R1 thru R4 independently represent alkyl, aryl, heteroaryl or alkenyl; n is an integer of 1-6; and X independently represents halo, hydroxyl, nitrate or acetate group. Using the catalyst composition, a cross-coupling reaction is carried out between a boron-containing compound of formula (2) and a compound of formula (3). where R5 and R6 are the same as R1-R4 defined above; Y independently represents hydroxyl or alkoxy, Z is halo, methanesulfonate or trifluoromethanesulfonate.

Abstract: In part, the present invention is directed to coordination complexes comprising a therapeutic agent. In one aspect, the subject compositions comprise a platinum metal center and a covalently attached therapeutic agent.

Abstract: The present invention provides an additive for a photoresist composition for a resist flow process. A compound of following Formula 1 having low glass transition temperature is added to a photoresist composition containing a polymer which is not suitable for the resist flow process due to its high glass transition temperature, thus improving a flow property of the photoresist composition. As a result, the photoresist composition comprising an additive of Formula 1 can be used for the resist flow process. wherein, A, B, R and R′ are as defined in the specification of the invention.

Abstract: The disclosure concerns novel use of diterpene compound as a therapeutic agent of inlfammation, immune disease or cancer. More particularly, the present invention relates to novel use of diterpene compound that include kamebanin, kamebacetal A, kamebakaurin, and exisanin A, which would be effective for the treatnent inflammation, immune disease or cancer by inhibiting the production of nitric oxide, prostaglandin, and TNF-a, through the suppression of NF-k B activity.

Abstract: Newly-isolated and purified metabolites which are effective in regulating the development of at least one filamentous fungal microorganism species are disclosed. These compounds, which are referred to as conidiogenol and conidiogenone, may be used to induce conidiation in and/or to inhibit the growth of populations of such fungal species. The compounds are preferably produced by culture of the fungal species Penicillium cyclopium, and may be subsequently recovered from the culture medium and purified. Methods of using and methods of producing these compounds are also disclosed.

Abstract: The present invention is a novel process for the transformation of 17&agr;-hydroxy-6&agr;-methylpregn-4-ene-3,20-dione 17-acetate (I) 1

Abstract: A process is disclosed for the preparation of 21-bromo-4-pregnene-3,20-dione derivatives of general Formula I ##STR1## wherein R.sub.1 is a hydrogen atom, a hydroxy group or an alkanoyl group of up to 6 carbon atoms,R.sub.2 symbolizes a hydrogen atom or a methyl group, or whereinR.sub.1 and R.sub.2 jointly mean an isopropylidenedioxy group,whereinR.sub.3 is a hydrogen atom, a fluorine atom or a methyl group,V is a methylene group or ethylene group,X is a hydrogen atom, a fluorine atom or a chlorine atom, andY is a methylene group, a hydroxymethylene group or a carbonyl group.

Abstract: Compounds of the formula: ##STR1## useful as anti-cancer agents, anti-obesity agents, anti-hyperglycemic agents, anti-aging agents, anti-hyperglycemic agents and anti-autoimmune agents.

Abstract: Substituted anthrasteroid derivatives represented by the following formula: ##STR1## wherein R is hydrogen or lower alkyl; X is hydrogen, lower alkyl, halogen, hydroxy, hydroxymethyl, or halomethyl; Y is C.dbd.O, CH.about.OR', or OH C R", wherein R' is hydrogen, lower alkyl, cycloalkyl which may have an unsaturated bond or a substituent, or aliphatic lower acyl which may have carboxy or its lower alkyl ester at the terminal; R" is lower alkyl or lower alkynyl; the dotted line indicates the presence or absence of double bond; and the wavy line indicates .alpha. or .beta. configuration; or ketal derivatives thereof being effective against androgen-dependent diseases e.g., prostatic hypertrophy, prostatic cancer.

Abstract: Substituted 4-oxo-4H-benz-[d,e] anthracenes are fluorescent dyes which are useful in biomedical studies and analytical determinations. They are particularly useful in assays for living organisms, e.g. microorganisms, carried out at a pH of 9 or less. For these determinations, the fluorescent dyes can be attached to reducible compounds which will release the dye upon reduction. Alternatively, these dyes can be used in assays for hydrolytic enzymes or biological cells containing these enzymes. For these determinations, the dyes are attached to blocking groups.

Abstract: Described are substituted tricyclodecane derivatives having the generic structure: ##STR1## wherein Y is a moiety having a structure selected from the group consisting of: ##STR2## wherein one of the dashed lines represents a carbon-carbon single bond and the other of the dashed lines represents a carbon-carbon double bond; wherein R.sub.1 and R.sub.2 represent hydrogen or methyl with the proviso that one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is methyl; wherein R.sub.3 is hydrogen, C.sub.1 -C.sub.3 acyl, C.sub.3 or C.sub.4 alkyl or C.sub.3 or C.sub.4 alkenyl; wherein R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or methyl with the additional proviso that one of R.sub.4, R.sub.5 and R.sub.6 is methyl and the other two of R.sub.4, R.sub.5 and R.sub.6 is hydrogen.