Abstract: Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in pharmaceutical compositions intended for the treatment of parasitic infections are provided. Methods are provided for the production of artemisinin derivatives via functionalization of positions C7 and C6a, and optionally, in conjunction with modifications at positions C10 and C9, via chemoenzymatic methods. Recombinant cytochrome P450 polypeptides are also provided for use in the methods. The artemisinin derivatives can be used for the treatment of malaria and other parasitic infections, alone or in combination with other antiparasitic drugs.

Abstract: The present invention relates to naphthopyran compounds that include at least one compound represented by the following Formulas (I), (II), and (III): With reference to Formulas (I), (II), and (III), there is the proviso that: (i) at least one R1 is a group L; and/or (ii) B and/or B? is substituted with at least one group L. The group L can be described as a lengthening group. The present invention also relates to photochromic-dichroic naphthopyran compounds and photochromic-dichroic articles containing such compounds.

Abstract: Pest controlling compositions exhibiting enhanced pesticidal activity levels and methods for preparing the same are disclosed. In one embodiment, a method includes providing a liquid composition that includes at least one pesticide and at least one co-ingredient that enhances pesticidal activity of the composition compared to a composition dissimilar only in not having the at least one co-ingredient. The at least one co-ingredient may include at least one metal oxide, a combination of at least one transition metal salt and at least one proteinaceous material or a combination of at least one proteinaceous material and at least one polymeric material. The method further includes spray drying the liquid composition to provide a solid composition. In one aspect of this embodiment, the solid composition provided by the spray drying exhibits enhanced pesticidal activity compared to the liquid composition.

Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted

Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.

Abstract: The invention relates to a cosmetic, dermatological or pharmaceutical preparation, containing one, two or more compounds of formula (I) and/or a pharmaceutically acceptable salt of a compound of this type, (i) for use in a method for preventing, treating or reducing cellulite, and/or (ii) in an adequate quantity to reduce the lipid quantity contained in subcutaneous fat tissue, and/or to inhibit the differentiation of preadipocytes, and/or to inhibit the lipogenesis in adipocytes, wherein the radicals R1 to R8, independently of one another, signify hydrogen, hydroxy or C1-C4-alkoxy, and/or two adjacent radicals together form a methylenedioxy group.

Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.

Abstract: The present invention relates to novel pterocarpan compound or pharmaceutically acceptable salt thereof and a composition for the prevention or treatment of metabolic disease or complications thereof comprising the same as an active ingredient. The novel pterocarpan compound of the present invention isolated from soybean leaves inhibits ?-glucosidase activity and hACAT activity, and suppresses LDL-oxidation efficiently. Therefore, the compound of the present invention not only can be effectively used for the prevention or treatment of metabolic disease or complications thereof but also can be effectively used as an anti-oxidative composition owing to its excellent anti-oxidative activity.

Abstract: Methods for synthesizing glycinols, glyceollins I and II, and isoflavene and chromane compounds using a Wittig reaction, compositions made therewith, and uses thereof are described.

Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.

Abstract: The present invention relates to novel platensimycin derivatives, their intermediates and preparing methods of the same. Platensimycin is known as an effective antibiotic material having a broad antimicrobial spectrum and its derivatives are also expected to be effective antibiotic candidates. The present invention also relates to a novel preparing method of platensimycin. The intermediates used for the production of platensimycin and its derivatives of the present invention are tricyclo ketone derivatives and tetracyclo derivatives. Tetracyclo derivatives are prepared from tricyclo ketone derivatives prepared by carbonyl ylide [3+2] cycloaddition of dia-zoketone derivative.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: The present invention relates to xanthone compounds isolated from the plant Psorospermum molluscum Hochr. (Clusiaceae), a Madagascar plant, which are potent cytotoxic agents.

Abstract: Methods for synthesizing glycinols, glyceollins I and II, and isoflavene and chromane compounds using a Wittig reaction, compositions made therewith, and uses thereof are described.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: Provided are a sulfated C-glycoside which is a novel compound serving as a precursor of chafuroside and chafuroside analogs; a method for efficiently producing the sulfated C-glycoside; and a method for efficiently producing chafuroside and chafuroside analogs using said sulfated C-glycoside. A sulfated C-glycoside represented by general formula (A1) or (B1) [wherein R1, R2 and R3 independently represent each a hydrogen atom or an OH group] is obtained by extracting tea leaves or tea tannins with water, a lower alcohol solvent having 1 to 3 carbon atoms or a liquid mixture comprising the same. Alternatively, the sulfated C-glycoside is produced by reacting a flavone C-glycoside such as isovitexin or vitexin with a sulfate group-introducing agent to thereby sulfate the flavone C-glycoside. By heating the sulfated C-glycoside thus obtained, chafuroside and chafuroside analogs are efficiently produced.

Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted

Abstract: The invention relates to a fluorescent dye of general formula I or II wherein R1, R2, R3 and R4 are independently hydrogen or a branched or unbranched, saturated or unsaturated, aliphatic or aromatic, functionally substituted, or unsubstituted hydrocarbon radical, wherein at least one of the R1 or R2 radicals and one of the R3 or R4 radicals is not hydrogen and the R1 and R3 radicals and/or R2 and R4 radicals in formula I can be bridged to each other, and X and Y independently represent a substituted or unsubstituted C1 or C2 hydrocarbon radical wherein any one carbon unit can be replaced by an N or S heteroatom. The dye is remarkable for its high fluorescence intensity and large Stokes shift in combination with a long fluorescence lifetime.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The invention is related to the area of new 6-Oxa-8?-steroid estrogen analogues and the synthesis of these new biological active steroid estrogen analogues, namely, to the preparation of 6-oxa-8?-steroid estrogens and their use as estrogen receptor modulators. These new estrogen analogues are ligands for estrogen receptors and as such may be useful for the treatment and prevention of a variety of conditions related to estrogen functioning. These conditions include bone and cartilage disorders, increased levels of LDL cholesterol, cardiovascular diseases, impairment of cognitive function, cerebral degeneration disorders, endometriosis and other types of inflammation, the metabolic syndrome, and cancer, in particular of the breast, uterus and prostate.

Abstract: Two distinct methods are disclosed and claimed for synthesizing glyceollin I plus glyceollin II as a mixture and as their pure forms. Stereochemical isomers and various synthetic intermediates are also synthesized and claimed for their novel compositions of matter. All compounds and their mixtures are claimed for use in formulations that are useful to treat or prevent cancer, or that have utility as selective estrogen receptor modulators, such formulations including enhanced or medical foods, dietary supplements and ethical pharmaceutical agents.

Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.

Abstract: A method is provided for improving the shelf-life of a nuclear staining solution. In particular, the present invention provides a method of adding an antioxidant to a hematoxylin staining solution which maintains the performance of the stain over its shelf-life.

Abstract: The invention relates to a cosmetic, dermatological or pharmaceutical preparation, containing one, two or more compounds of formula (I) and/or a pharmaceutically acceptable salt of a compound of this type, (i) for use in a method for preventing, treating or reducing cellulite, and/or (ii) in an adequate quantity to reduce the lipid quantity contained in subcutaneous fat tissue, and/or to inhibit the differentiation of preadipocytes, and/or to inhibit the lipogenesis in adipocytes, wherein the radicals R1 to R8, independently of one another, signify hydrogen, hydroxy or C1-C4-alkoxy, and/or two adjacent radicals together form a methylenedioxy group.

Abstract: The present invention relates to novel platensimycin derivatives, their intermediates and preparing methods of the same. Platensimycin is known as an effective antibiotic material having a broad antimicrobial spectrum and its derivatives are also expected to be effective antibiotic candidates. The present invention also relates to a novel preparing method of platensimycin. The intermediates used for the production of platensimycin and its derivatives of the present invention are tricyclo ketone derivatives and tetracyclo derivatives. Tetracyclo derivatives are prepared from tricyclo ketone derivatives prepared by carbonyl ylide [3+2] cycloaddition of dia-zoketone derivative.

Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention relates to xanthone compounds isolated from the plant Psorospermum molluscum Hochr. (Clusiaceae), a Madagascar plant, which are potent cytotoxic agents.

Abstract: The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.

Abstract: The disclosure relates to methods for dyeing keratinous fibers by treatment of said fibers with i) at least one entity chosen from hematoxylin, hematein, brazilin, brazilein, and their derivatives, ii) at least one metal salt, iii) hydrogen peroxide or at least one system which generates hydrogen peroxide and iv) at least one (bi)carbonate. The disclosure also relates to multicompartment devices and compositions comprising the ingredients i), ii), iii) and iv).

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The present invention is directed to 7 oxa-estra-4,9-diene-3,17-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.

Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.

Abstract: Novel metabolites of wortmannin and wortmannin analogs and their use in inhibiting PI-3 kinase activity in mammals and the treatment and prevention of cancer or tumor formation in a subject are described herein.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.

Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.

Abstract: The invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and their uses.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.

Abstract: Methods of making chiral psorospermin or its analogues and/or intermediates thereof are provided.

Abstract: The use as fragrance ingredient of a compound of formula (I) wherein R1 and Y have the same meaning as given in the description, and fragrance applications comprising them.

Abstract: A method is provided for improving the shelf-life of a nuclear staining solution. In particular, the present invention provides a method of adding an antioxidant to a hematoxylin staining solution which maintains the performance of the stain over its shelf-life.

Abstract: The present invention relates to processes for the production of 2-oxa-3-one androstane derivatives. The processes comprise reacting a 3-one androstane derivative with ozone to form a 2-oxa-3-one androstane derivative.

Abstract: The present invention is directed to novel 7-oxa-estra-4,9-diene-3,17-dione derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by at least one progesterone or glucocorticoid receptor.