Abstract: A method of preparing a thioic acid intermediate of fluticasone propionate includes: treating a 17?-[(N,N-dimethyl carbamoyl)thio]carbonyl compound in a solution including an alcohol and an alkali metal hydroxide, an alkaline-earth metal hydroxide, or a mixture thereof to cleave an amide from the 17?-[(N,N-dimethyl carbamoyl)thio]carbonyl compound; treating the solution to separate an aqueous portion; and adding an acid to the aqueous portion to obtain the thioic acid intermediate of fluticasone propionate. A method of preparing fluticasone propionate includes preparing the thioic acid intermediate of fluticasone propionate, and alkylating the thioic acid intermediate of fluticasone propionate to prepare the fluticasone propionate.

Abstract: Method for preparing fluticasone furoate (6?,9?-difluoro-11?-hydroxy-16?-methyl-17?-[(2-furoyl)oxy]-3-oxo-androsta-1,4-diene-17?-carbothioic acid S-fluoromethyl ester) by directly subjecting a compound of Formula III and a complex of a fluoromethylating reagent in presence of an organic base to a replacement reaction to obtain the target compound. Generation of impurities in a process via Compound IV is avoided; the method is simple with mild reaction conditions, suitable for industrial production, and yields products with purity of 98% by HPLC.

Abstract: Provided are functional segregated telodendrimers having, for example, two or three functional segments. The telodendrimers can have one or more crosslinking groups (e.g., reversible photocrosslinking groups). The telodendrimers can aggregate to form nanocarriers. Cargo such as drugs, imaging probes, and other materials may be sequestered in the core of the aggregates via non-covalent or covalent interactions with the telodendrimers. Such nanocarriers may be used in drug delivery applications and imaging applications.

Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.

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: Described herein are processes for the preparation of monofluoromethylated organic biologically active compounds, starting from protected intermediates and/or reagents to obtain compounds such as fluticasone propionate and fluticasone furoate, in presence of decarboxylating reagents XeF2 and BrF3, or using FCH2SH as a reagent.

Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.

Abstract: The present invention relates to a cyclization process of forming a multiple ring compound from an isoprenoid compound. The cyclization process involves reacting the isoprenoid compound with an acetal initiator under conditions sufficient to form the multiple ring compound. The isoprenoid compound is contacted with an initiator and optionally with a catalyst. Cyclization occurs by reaction of the initiator with the isoprenoid compound. Cyclic acetal compounds wherein the acetal forms part of 6-membered unsaturated ring are also defined.

Abstract: A prodrug according to formula (I) wherein R2 is a residue of a drug, said drug having a hydroxyl group by which the COOR2 group is formed; Z is O or NH; m is 0 or 1; and R3 is an organic moiety comprising a lipophilic group or a residue of a polymer, provided that Z is 0 if the polymer is carboxymethyl dextran. A system includes a plurality of magnetic nanoparticles including a prodrug as described above, a stent and a source of uniform magnetic field capable of producing temporary magnetization of the stent and/or the magnetic nanoparticles. A method of treating a medical condition with a drug includes administering to a patient in need of the drug a prodrug as described above, the prodrug being capable of releasing the drug in the patient after the administration step.

Abstract: The invention provides electrophilic monohalomethylating reagents, methods for their preparation and methods for preparation of monohalomethylated biologically active compounds using such reagents. Typical monohalomethyl groups transferred are FH2C—, CIH2C— and others. The reagents used for transferal of the groups are described by Formulae A-D: wherein: X?F, CI, Br, I, sulfonate esters, phosphate esters or another leaving group; R11=tetrafluoroborates, inflates, halogen, perchlorate, sulfates, phosphates or carbonates The other variables are as defined in the claims.

Abstract: Method for preparing fluticasone furoate (6?,9?-difluoro-11?-hydroxy-16?-methyl-17?-[(2-furoyl)oxy]-3-oxo-androsta-1,4-diene-17?-carbothioic acid S-fluoromethyl ester) by directly subjecting a compound of Formula III and a complex of a fluoromethylating reagent in presence of an organic base to a replacement reaction to obtain the target compound. Generation of impurities in a process via Compound IV is avoided; the method is simple with mild reaction conditions, suitable for industrial production, and yields products with purity of 98% by HPLC.

Abstract: Processes for preparing lanostane triterpenes from the medicinal mushroom Ganoderma lucidum, and related compounds are described. Compounds, compositions, and methods for treating cancer are also described.

Abstract: The present invention relates to novel 4-pregenen-11?-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.

Abstract: A novel process for preparing a compound of formula (I) which comprises converting a compound of formula (II) to a compound of formula (I) via a compound of formula (III), or a salt thereof, without isolating any intermediates.

Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.

Abstract: This invention relates to compositions (e.g., otic compositions) comprising an antibiotic (generally a quinolone or naphthyridinone), corticosteroid, and organic acid (generally a fatty acid). This invention also relates to treatment methods using such a composition, uses of such a composition to make medicaments, and therapeutic kits comprising such a composition.

Abstract: Steroid compounds possessing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: Steroid compounds processing a hydrogen donor in 3beta position, either in the form of a hydroxy- or a sulfate group, function as efficient blockers of the 3alpha-hydroxy-pregnan-steroid action and thus have utility as therapeutic substances for the prevention and/or treatment of steroid related CNS disorders. Treatment methods based on the administration of these substances are disclosed, and these substances either alone or in combination are also suggested for the manufacture of pharmaceuticals for the treatment of many specific steroid induced CNS disorders.

Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.

Abstract: It is an object of the present invention to provide a novel method for producing a steroid compound. The present invention provides a method for producing 5?-3,7-dioxocholanic acid or an ester derivative thereof, using, as a raw material, a sterol having double bonds at position 5 and at position 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, via the following 4 steps: (I) a step involving oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step involving the oxidative cleavage of a side chain to convert position 24 to a carboxyl group or an ester derivative thereof; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5? configuration by reductive saturation of a double bond at position 4.

Abstract: According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: There is provided a crystalline complex comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in that the crystalline complex is of space group P212121 having unit cell dimensions of about 12.5±1.0 §, 15±1.0 §, and 16.2±1.0 § when determined at either 120K or 150K.

Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.

Abstract: The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: —X1—(CH2)m-Q-(CH2)n—X2—??III D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to process and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

Abstract: This invention relates to a highly efficient artificial low-density lipoprotein (LDL) carrier system for the targeted delivery therapeutic agents across the blood-brain barrier (BBB). In particular, this invention relates to artificial LDL particles comprised of three lipid elements: phosphatidyl choline, fatty-acyl-cholesterol esters, and at least one apolipoprotein. The present invention further relates to compositions, methods and kits comprising artificial LDL particles for targeting drugs to and across the BBB for the prevention and treatment of brain diseases.

Abstract: There is provided a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I) or a solvate thereof.

Abstract: There are provided crystalline particles of unsolvated Form 1 polymorph of the compound of formula (I): characterised in that the particles are in the form of substantially triangular plates.

Abstract: The present application describes deuterium-enriched mometasone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: There are provided according to the invention compounds 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 ? 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. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

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: The present invention relates to, for example, a compound of formula (VIII) useful in the manufacture of anti-inflammatory androstane derivatives.

Abstract: The present invention relates to, for example, a compound of formula (X) useful in the manufacture of anti-inflammatory androstane derivatives.

Abstract: According to one aspect of the invention, there is provided a compound of formula (I) and solvates thereof. There are also provided compositions containing the compound, processes for preparing it, and its use in therapy.

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

Abstract: Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I): {wherein R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group or, etc.; R3 represents a hydrogen atom etc.; R4 represents a hydrogen atom etc.; R5 represents a hydrogen atom etc.; R6 represents a cyano group, an amino group, COR53 (wherein R53 represents a substituted lower alkyl group etc.), a substituted or unsubstituted aryl group, a substituted or unsubstituted heterocyclic group, etc}, or pharmaceutically acceptable salts thereof.

Abstract: Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals

Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.

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 ? 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 together with a long-acting ?2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of COPD over a period of 24 hours or more.

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) 1

Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P212121 having unit cell dimensions of about 12.1±0.6 Å, 14.9±0.7 Å, and 16.2±0.8 Å when determined at either 120K or 150K.

Abstract: There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212121 having unit cell dimensions of about 7.6±0.6 Å, 12.7±0.7 Å, and 33±3 Å when determined at 120K.

Abstract: The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.

Abstract: There is provided a pharmaceutical aerosol formulation comprising (i) a compound of formula (I) or a solvate thereof as medicament, (ii) a liquified hydrofluoroalkane (HFA) gas as propellant; and characterized in that the compound of formula (I) or a solvate thereof is completely dissolved in the formulation.

Abstract: An androgenic steroid compound of the formula: 1

Abstract: This invention relates to processes for the preparation of novel 7-carboxy substituted steroid compounds of Formula I, 1

Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.

Abstract: According to one aspect of the invention, there is provided a compound of formula (I) 1