Abstract: Provided is a method for producing cerebral cortex neurons from pluripotent stem cells. Provided is a method for producing cerebral cortex neurons from pluripotent stem cells, comprising (i) a step of performing a suspension culture of pluripotent stem cells in a culture medium containing a TGF? inhibitor, bFGF, a Wnt inhibitor, and a BMP inhibitor, (ii) a step of performing a suspension culture of the cells obtained in the step (i) in a culture medium containing a Wnt inhibitor and a BMP inhibitor, and (iii) a step of further culturing the cells obtained in the step (ii).

Abstract: There is provided a novel compound having neurite-outgrowing activity that is useful for the prevention or the treatment of a neurodegenerative disease. A compound of Formula (I) [where X is OR or NR1R2, Y is OH, NR3R4, —NHC(?NH)NHR5, or —NHC(?NH)R5, and Z is a hydrogen atom, a linear or branched C1-5 alkyl group, or a 5- or 6-membered ring aryl group optionally having 1 or 2 nitrogen atom(s), sulfur atom(s), or oxygen atom(s)], or a pharmaceutically or veterinary-medically acceptable salt of the compound.

Abstract: The invention provides 11?-hydroxyandrosta-4-ene-3-one compounds of Formula I, or physiologically acceptable salts or solvates thereof: wherein R4 represents a moiety selected from a group consisting of (A), (B) and (C), with a proviso that when R4 represents moiety (C), Z is S:

Abstract: The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer.

Abstract: There is provided a novel compound having neurite-outgrowing activity that is useful for the prevention or the treatment of a neurodegenerative disease. A compound of Formula (I) [where X is OR or NR1R2, Y is OH, NR3R4, —NHC(?NH)NHR5, or —NHC(?NH)R5, and Z is a hydrogen atom, a linear or branched C1-5 alkyl group, or a 5- or 6-membered ring aryl group optionally having 1 or 2 nitrogen atom(s), sulfur atom(s), or oxygen atom(s)], or a pharmaceutically or veterinary-medically acceptable salt of the compound.

Abstract: This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.

Abstract: A composition for treating cancer cells and a preparation method therefore is provided. The composition includes novel withanolide compounds derived from a Solanaceae plant, which the novel withanolide compounds have the cytotoxicity to the cancer cells.

Abstract: There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof; process for preparing them, compositions containing them and their use in therapy.

Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6&agr; and 7&bgr; oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6&agr; and 7&bgr; oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and &dgr;-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6&agr; and 7&bgr; oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6&agr; and 7&bgr; oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and &dgr;-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.

Abstract: The present invention relates to novel compounds comprising a steroid hormone linked to a DNA-interacting molecule that target nucleic acids to the cell nucleus. Further, the invention relates to a method for introducing nucleic acids into the nucleus of cells with the help of such compounds. Pharmaceutical preparations containing such compounds and the use of such compounds for gene therapy are also provided.

Abstract: The present invention relates (a) to new compounds represented by Formula I: 1

Abstract: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.

Abstract: The present invention provides novel derivatives comprising compounds in the androstane and androstene series, coupled with ascorbic acid, including salts thereof, and represented by one or more of the general formulae: 1

Abstract: According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and {overscore (-----)} represents a single or a double bond; and salts and solvates thereof together with a long-acting &bgr;2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract over a period of 24 hours or more.

Abstract: Anthraquinone chiral ligands (AQN) are used in asymmetric aminohydroxylation addition reactions of cinnamate based olefins for synthesizing aryl serines. The anthraquinones impart a reverse regioselectivity as compared to the commonly employed phalazine chiral ligands (PHAL). Carbamates are employed as the oxidant nitrogen source. The yields and enantiomeric efficiencies are Excellent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxycarbamate.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.

Abstract: Disclosed are steroid nitrite/nitrate ester derivatives of formula I: ##STR1## wherein, the substituents are as defined in the specification and their use in the treatment of inflammatory diseases.

Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.

Abstract: A compound having the formulae selected from the group consisting of ##STR1## wherein R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy, the dotted line in 9(11) position indicates an optional double bond and the dotted line in position 16(17) indicates an optional double bond ##STR2## is a 3-keto-.DELTA..sup.4 -system or 3-keto-.DELTA..sup.1,4 -system or 3-OR.sub.4 -.DELTA..sup.5 -system, R.sub.4 is hydrogen or a protector group of hydroxy, R is --CH.sub.3, --CH.sub.2 OH or --CH.sub.2 --OR', R' is a hydroxy protector group and R'.sub.1 is selected from the group consisting of methyl, a branched alkyl of 5 to 8 carbon atoms not possessing hydrogen in the .beta.-position, aryl of up to 10 carbon atoms and benzyl, hetroaryl of up to 10 carbon atoms and at least one heteroatom selected from the group consisting of nitrogen, sulfur and oxygen, with the exception of the compounds of formula Vc in which R is methyl, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 and R.sub.

Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethyl formamide; at a temperature within the range of about -78.degree. to about 0.degree. C., under anhydrous conditions under an inert atmosphere.

Abstract: Topically administrable C-21 thioether glucocorticoid steroid derivatives are disclosed as effective anti-inflammatory agents for the treatment of ophthalmic inflammatory disorders. These C-21 thioether derivatives do not cause a significant increase in intraocular pressure as a side effect.

Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 - .DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which is useful for the preparation of compounds of formula A.

Abstract: The present invention relates to novel sweet compounds derived from the leaves of the subtropical weed Abrus precatorius, and their use as sweeteners. In particular, the present invention contemplates four novel sweet compounds isolated from A. precatorius or A. fruticulosus, and particularly, Abrusosides A, B, C and D and related compounds. The present invention also contemplates the use of these abrusosides and related compounds as sugar substitutes. The present invention contemplates the use of Abrusosides A-D as individual components or in mixtures, in a method for sweetening comestibles, foodstuffs, beverages and medicinal agents.