Abstract: Provided herein are multiple solid forms of a defined steroid-like compound, and methods for the preparation and use thereof. In one aspect, there is provided a crystalline form of said steroid-like compound, and methods for the preparation and use thereof. In another aspect, there is provided a substantially amorphous form of said steroid-like compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like. In still another aspect of the present invention, there are provided kits containing compounds according to the present invention and/or compositions containing same.

Abstract: The present invention relates to pharmaceutical compositions comprising 4-pregenen-11?-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.

Abstract: The invention provides skin protecting and penetrating, easy-to-administer base and active agent-containing compositions, such as those including hydrocortisone, for treating the skin of mammals for different dermatologic disorders. This is effected by topically administering effective amounts of the compositions thereto in forms that address the skin and mucosa of the mouth and lips, and the rest of the body. Additionally, an optional flavoring addition to these products affords significantly better tasting, and less bitter, compositions, allowing a more pleasant experience and better compliance by patients. The compositions include a unique formulation of FANCOL VB, Natunola Castor 1023, Finsolv TN, bees wax and, optionally, one or a plurality of plant or plant seed oils, fatty alcohols, fats and flavorings, in desirable weight percents thereof, in various forms, and preferably in a form of a solid roll-on stick in a variety of sizes and of a jar or pot.

Abstract: The present invention relates to an improved method of administration of glucocorticoid based compositions in glucocorticoid replacement therapies enabling an objectively based regimen for administration enabling correct individual dosing of glucocorticoids resulting in an optimised individual replacement therapy and thus an improved long-term outcome for patients with temporary or chronic adrenal insufficiency.

Abstract: Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

Abstract: Provided herein are water-soluble, functionalized fullerenes, and processes for producing water-soluble, functionalized fullerenes. The process includes sulfonating a fullerene in an acidic solution comprising sulfuric acid to produce a sulfonated fullerene, isolating the sulfonated fullerene from the acidic solution without neutralizing the acidic solution, reacting the sulfonated fullerene with hydrogen peroxide to form a reaction product, and isolating a polyhydroxylated fullerene from the reaction product produced from reacting the sulfonated fullerene with the hydrogen peroxide. The process of producing water-soluble fullerenes further includes functionalizing a polyhydroxylated fullerene with one or more pendant functional groups by reacting the polyhydroxylated fullerene with one or more functional group precursors.

Abstract: Methods, devices and compositions for treatment of severe and uncontrolled asthma are provided by which high amounts of an inhaled corticosteroid are directed to the small airways of the lower lungs. The invention provides for a substantial decrease in the dose of concurrently administered oral corticosteroids. A particular advantage of the invention is the significant reduction in corticosteroid-related adverse effects.

Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are selected independently of each other and as defined herein. The present invention also provides compounds (and salts, solvates, esters, prodrugs, tautomers, and isomers) of Formulas II, III, IV, V, and VI, as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions.

Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.

Abstract: Corticosteroid receptors and/or mineralo-corticoid receptors are administered in combination with an addictive drug or the pharmacodynamic equivalent thereof for the therapy of an addictive disease triggered by said addictive drug or connected thereto.

Abstract: The present disclosure describes aerosol formulations that are particularly effective for pulmonary aerosol delivery. The aerosol formulations comprise an aqueous dispersion of active agent particles, said aqueous dispersion having an excess of a surface tension reducing agent. As a result of the reduced surface tension of the aqueous dispersion, the resulting aerosol droplets formed have a particle size less in one embodiment of than 10 microns in size or in an alternate embodiment of less than 6 microns in size. The present disclosure also provides for a method for forming an aerosol from said aerosol formulation, a method of treating a mammal in need of said treatment using said aerosol formulation, and a method of diagnosing a mammal in need of such diagnosis using said aerosol formulation.

Abstract: The invention is directed to a method for sterilizing a pharmaceutical formulation comprising a suspension of a water-insoluble pharmaceutical, comprising the steps of heat-sterilizing an aqueous solution of a viscosity enhancer, to result in a first sterile pre-mix. Next is sterile-filtering an aqueous solution of a mixture of a pharmaceutically-active compound, which results in a second sterile pre-mix. Next is heat-sterilizing a mixture of water, a water-insoluble pharmaceutical, and at least a partial amount of an electrolyte to provide a sub-saturated solution of the electrolyte, and adding under aseptic conditions an aqueous surfactant, to give a third sterile pre-mix. Finally, combining all three pre-mixes in sterile fashion to achieve a sterile suspended pharmaceutical formulation. Thus, for the third pre-mix, use of either Sodium chloride (in varying proportion) or Sodium acetate (in one proportion, but not limited to) is given as an example.

Abstract: The invention provides an improved process for the preparation of 17-esters of 9.alpha.,21 -dihalo-pregnane-11.beta.,17.alpha.-diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the following scheme: ##STR1## wherein RCO, R.sup.1, X, Y and the dotted line are as defined in the specification. The novel process is especially suitable for the preparation of Mometasone Furoate.

Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.

Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.

Abstract: The invention provides a modified human cytotoxic T cell line, which is characterized by dual activity in vitro and in vivo against malignant cells and virus-infected cells. Also provided are effective and safe methods for use of the modified cells in adoptive therapy of cancer and untreatable vital diseases in MHC-mismatched recipients, and in marrow purging to achieve complete eradication of residual tumor cells from marrows of patients with leukemia and other types of cancer. Also provided are effective and safe methods for use of the cytokine stimulated, irradiated TALL-104 cells in the manufacture of a veterinary composition for adoptive therapy of canine and feline malignancies.

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: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.

Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R and R' and the A and B are as defined in the specification. ##STR2## K is selected from the group consisting of ##STR3## n is 2 or 3 and the dotted lined is an optional bond.

Abstract: Oxidation of C--H bonds in organic chemical compounds to C--OH bonds is accomplished by utilizing, as a monooxygenase, a heme protein such as methemoglobin or metmyoglobin in the presence of sulfate ion, in an aqueous medium.

Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.

Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.

Abstract: A process for crystallizing a pharmaceutically active steroidal product, without mechanical procedure, to obtain a homogeneous granulometric class which may be prepared beforehand, wherein the product which is desired to be crystallized is dissolved in a ternary mixture made of a lipophilic solvent, a hydrophilic solvent and a surface active agent at a temperature close to the boiling point of the mixture of solvents and wherein the mixture of solvents is allowed to revert to a temperature where the crystallization initiates, then, the thus-formed crystals are recovered.

Abstract: An improved process for the preparation of hydrocortisone and novel intermediates which avoids an 11-hydroxylation step and results in improved yields.

Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.