Abstract: The disclosure features dexamethasone prodrug dimers of dexamethasone and pharmaceutical compositions thereof useful for, e.g., the extended release of a drug and for the treatment of a disease or condition.

Abstract: The disclosure features dexamethasone prodrug dimers of dexamethasone and pharmaceutical compositions thereof useful for, e.g., the extended release of a drug and for the treatment of a disease or condition.

Abstract: The disclosure features dexamethasone prodrug dimers of dexamethasone and pharmaceutical compositions thereof useful for, e.g., the extended release of a drug and for the treatment of a disease or condition.

Abstract: A thick cleaning composition, comprising a long-chain fatty acyl acidic amino acid ester; a fatty compound of fatty acid, fatty alcohol, fatty alcohol ether or polyol fatty acid ester; a surfactant; a solvent composed of water, lower alcohol, polyol and polyol ether; and further comprising a beautifying and cleaning adjuvant for skin, eyes, teeth and hair. The cleaning composition can achieve satisfactory thick appearance when used for cleaning skin and hair, and maintain stable viscosity at different temperatures. In use, the composition can be easily daubed, and foams quickly with good foaming quality.

Abstract: The invention relates to a drug conjugate including a drug and a plant steroid. The drug conjugate may target the drug for intestinal cell delivery, and thus may be used to treat diseases, including intestinal diseases, or to affect intestinal metabolism. The invention therefore also relates to treating intestinal diseases and affecting intestinal metabolism with the drug conjugate.

Abstract: A unified homeostatic system of cholesterol and steroid hormone pathways is described, in which the uses or modulations of function of the homeostatic system of cholesterol and steroid hormone pathways are linked by lipoproteins, and are used or modulated to achieve a therapeutic benefit, to diagnose a disease or medical condition in humans, or to develop suitable active agents or combinations of active agents. Pharmaceutical compositions, methods of treatment, methods of drug development, and assay methods that rely on the new understanding of the homeostatic system are described.

Abstract: The present invention relates to betulonic and betulinic acid derivatives and, in particular, to C-28 and C-3 derivatives. The present invention relates to betulonic acid esters, and dihydro-betulonic acid esters. Betulinic acid and derivatives thereof may be bound to a poly(alkylene glycol) (PAG) such as poly(ethylene glycol). Binding may be via a linker, such as a diamine, an amino acid, a peptide, an ester or a carbonate. The compounds of the present invention may be used for the treatment of cancer or a viral infection. The present invention also provides pharmaceutical compositions comprising the compounds of the present invention.

Abstract: The present disclosure provides modified neuroactive steroids. The modified neuroactive steroids may comprise, consist of, or consist essentially of a therapeutic agent and/or a modifying moiety. The modified neuroactive steroid can have modified characteristics as compared to native neuroactive steroids that do not include a modifying moiety and/or therapeutic agent. The modified neuroactive steroid may be, for example, modified pregnenolone, pregnenolone metabolites, allopregnanolone, and/or allopregnanolone metabolites. The modified neuroactive steroids can be used to treat, prevent and/or ameliorating a phenotypic state of interest in a subject.

Abstract: The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided.

Abstract: [Problem] The purpose of the present invention is to provide organic particles containing pharmaceutical particles of which the particles are small and the particle size distribution is narrow, and a manufacturing method for the same. [Solution] Provided are pharmaceutical multimeric particles of which the particles are small and the particle size distribution is narrow and which are characterized in being obtained by pouring into water a solution of a pharmaceutical multimer dissolved in a water-miscible organic solvent, and a manufacturing method for the pharmaceutical multimeric particles. Pharmaceutical dimeric particles thereof are characterized in being obtained by pouring into water a solution of a compound represented by general formula (I) dissolved in a water-miscible organic solvent.

Abstract: Disclosed are compounds capable of facilitating transport of biologically active agents or substances into cells having the general structure: wherein Q is selected from the group consisting of N, O and S; L is any bivalent organic radical capable of linking each Q, such as C, CH, (CH2)l, or {(CH2)i-Y—(CH2)j}k, wherein Y is selected from the group consisting of CH2, an ether, a polyether, an amide, a polyamide, an ester, a sulfide, a urea, a thiourea, a guanidyl, a carbamoyl, a carbonate, a phosphate, a sulfate, a sulfoxide, an imine, a carbonyl, and a secondary amino group and wherein Y is optionally substituted by —X1-L?-X2—Z or —Z; R1-R6, independently of one another, are selected from the group consisting of H, —(CH2)p-D-Z, an alkyl, an alkenyl, an aryl, and an alkyl or alkyl ether optionally substituted by one or more of an alcohol, an aminoalcohol, an amine, an amide, an ether, a polyether, a polyamide, an ester, a mercaptan, an alkylthio, a urea, a thiourea, a guanidyl, or a carbamoyl group, and

Abstract: There is provided a hemihydrate of (3?, 5?, 7?, 12?)-7,12-dihydroxy-3-{2-[{4-[17?-hydroxy-3-oxo-17?-prop-1-ynylestra-4,9-dien-11?-yl]phenyl}(methyl)amino]ethoxy}cholan-24-oic acid in a crystalline form which is characterised by an X-ray diffraction pattern having major peaks at 2?=6.58±0.2, 8.54+0.2, 12.28±0.2, and 19.68±0.2. This crystalline material is useful in the treatment of conditions associated with an excess of hepatic glucocorticoid response.

Abstract: The present invention provides compounds, compositions and methods that enhance the transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The compounds, compositions and methods are useful for introducing agents such as genes into individual cells, as well as cells that are present as a tissue or organ.

Abstract: The need for new class of antifungal drugs with high efficacy, low toxicity and novel mode of action is well established. Synthesis and antifungal activity of bile acid derived new steroidal dimers N1,N3-Diethylenetriamine bis [cholic acid amide] (1) and N1,N3-Diethylenetriamine bis [deoxycholic acid amide] (2) having novel amphiphile topology is described.

Abstract: This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in the regulation of metabolism, especially lowering serum glucose levels, insulin levels, or lipid levels, and/or decreasing body weight.

Abstract: A water soluble delivery system for nucleic acids to cells having androgen receptors, preferably prostate cells, is provided comprising a steroid moiety capable of binding to said receptors, said steroid moiety being covalently linked to a polycationic material. This molecule may be complexed with therapeutic or diagnostic nucleic acids. Methods of diagnosis and therapy using these compositions are also provided, including gene therapy treatments for prostate cancer.

Abstract: This invention provides methods and compositions for enhancing transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The methods and compositions are useful for introducing agents into individual cells, as well as cells that are present as a tissue or organ.

Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.

Abstract: New steroidal polyamines have the structure of formula I or formula II: ##STR1## wherein R.sub.1 and R.sub.2 are independently N(R').sub.3.sup.+ or H in the .alpha.- or .beta.- position except both R.sub.1 and R.sub.2 are not H;R.sub.3 is N(R').sub.3.sup.+ in the .alpha.- position or hydrogenR.sub.4 is OH, N(R').sub.3, or NHC(NH.sub.2)NH.sub.2.sup.+R' is hydrogen, alkyl of one to four carbons, aralkyl, or combinations thereof.

Abstract: nor-Bile acid derivatives, processes for their preparation and the use of these compounds as medicaments nor-Bile acid derivatives of the formula IG1--X--G2 Iin which G1, G2 and X have the meanings given, processes for the preparation of these compounds and medicaments are described. On the basis of their pharmacological action, they can be used as an antihyperlipidemic agent.

Abstract: Herein is disclosed a cosmetic or an external preparation containing, as an oleo-phase component, an oil-soluble N-long chained acyl acidic amino acid mono- or di-ester having at least one sterol ester in the molecule, which is a novel compound of excellent emulsifying and hydrating performances.

Abstract: Bile acid derivatives of the formula IZ(X--GS)nin which GS, X, Z and n have the meanings indicated in the specification, and a process for the preparation of these compounds are described. The compounds are pharmacologically active and can, therefore, be used as pharmaceuticals, in particular as a hypolipidemic.

Abstract: The invention relates to bile acid derivatives of the formula IG1--X--G2 (I)in whichG1 and G2 are bile acid radicals or modified bile acid radicals in the form of the free acids, the esters or amides, the salt forms and also the forms derivatized on the alcohol groups andX is a bridge group or a single covalent bond, it being possible for G1 and G2 to be optionally bonded via X.The compounds according to the invention have a high affinity for the specific bile acid transport system of the small intestine and inhibit bile acid absorption in a concentration-dependent and competitive manner.

Abstract: Herein are disclosed (1) an oil-soluble N-long chained acyl acidic amino acid mono- or di-ester having at least one sterol ester in the molecule, which is a novel compound of excellent emulsifying and hydrating performances, (2) an oily composition consisting of or comprising a mixture of such esters, and (3) perfuming cosmetics blended with such ester or such oily composition.