Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx??(I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position ? or ?; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

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: This invention is in the fields of cancer therapy. More particularly it concerns compounds which are useful agents for treating cell proliferative disorders, especially those disorders characterized by over activity and/or inappropriate activity of a EGFR, including EGFR-related cancers, particularly for expanding the efficacy of drugs previously developed for this purpose, and for methods of treatments using the compounds for this purpose.

Abstract: Topically administering a propellant-free formulation as a spray in the form of aqueous suspension of drug particles, wherein said formulation consists essentially of: micronized particles of beclometasone dipropionate (BDP) suspended in an aqueous phase, said aqueous phase comprising: an emulsifying agent selected from the class of polysorbates in an amount of 0.1 to 0.2% w/v, based on the total volume of the formulation; a sugar or a sugar alcohol in an amount of 5.0 to 5.2% w/v, based on the total volume of the formulation; a mixture of microcrystalline cellulose and carboxymethylcellulose sodium in an amount of 0.5 to 1.0% w/v, based on the total volume of the formulation; one or more preservatives; and water up to 100%, is effective for the prophylaxis and/or treatment of a dermatological disease such as atopic dermatitis, acne and psoriasis.

Abstract: The present invention relates to a particular class of biodegradable linkers, ensuring transiently stable conjugation of building blocks and/or bioactive compounds into drug delivery systems (DDS), such as DDS based on polymeric micelles or hydrogels. In addition, the present invention relates to compounds, comprising said linkers, such compounds preferably being prodrugs. Further, the invention is directed to the use of said linkers, and especially said biodegradable linkers, in a drug delivery system. Moreover, the invention relates to controlled release system comprising a polymer matrix, capable of releasing an active ingredient, wherein the active ingredient is covalently linked to the polymer molecules of the polymer matrix through said linkers, as well as to a method of synthesising these linkers and preparing such controlled release systems.

Abstract: The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.

Abstract: The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.

Abstract: A dpi formulation comprises a solvate of beclomethasone with a non-cyclic, straight or branched C5-C7 hydrocarbon. The solvate particles are of size 0.5 to 10 microns and are obtained by crystallization of the steroid in the presence of ultrasound.

Abstract: Methods and formulations for the improvement of recovery following bone-impacting injury or surgery. The formulations of the present invention preferably include platelet-rich plasma with a pharmaceutical agent. The pharmaceutical agent may be a glucocorticoid hormone or other organic pharmaceutical agent. Particularly preferred pharmaceutical agents include dexamethasone, melatonin, purmorphamine, 17?-estradiol, vitamin K2 (menaquinone-4, MK4), bisphosphonates, derivatives thereof, and combinations thereof. The formulations of the present invention may be directly administered to a surgical or injury site where improved bone growth is desired. The formulations may also be applied to or otherwise incorporated into scaffolding structural components commonly employed in the medical field to promote bone structure and growth. The pharmaceutical agent may be employed in an immediate release form or a sustained release form.

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 invention relates to novel 9- and/or 10-substituted anthracenes, to their use in liquid crystal, light-emitting or semiconducting materials and devices, in anisotropic polymers, optical, electrooptical, decorative, security, cosmetic, diagnostic, electric, electronic, charge transport, semiconductor, optical recording, electroluminescent, photoconductor or electrophotographic applications, and to liquid crystal, light-emitting and semiconducting materials, polymers and devices comprising them.

Abstract: The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof The compounds are useful for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.

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: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.

Abstract: The invention relates to nitrooxyderivative of corticosteriods of general formula (I) and pharmaceutical acceptable salts or stereoisomers thereof wherein R is the corticosteriod residue of formulas (II): The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological disease and ocular diseases.

Abstract: A method for producing a 6?-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6?-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R1 may be, for example, acetate or propionate, The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®.

Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R-(Z)a-Rx??(I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2—CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position ? or ?; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.

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: Compounds of the formula and use of the compounds as medicaments.

Abstract: The invention relates to compositions and methods for a one-step synthetic technique for making cationic steroid pharmaceutical compositions for use in treating inflammation and other diseases and disorders.

Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

Abstract: Compounds of the formula and use of the compounds as medicaments.

Abstract: Steroidal compounds or their salts having general formula: A—B—C—NO2 are described, wherein: A=R—, wherein R is a steroidal drug radical; B=—TB—X2—TBI—, wherein TB is (CO), TBI is O, S, NH, and X2 is a bivalent bridging group; and C is a bivalent radical.

Abstract: A method for producing a 6?-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6?-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R1 may be, for example, acetate or propionate. The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®.

Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I: are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II: in which R(5) is OH, with an activated carboxylic acid of the formula III:  R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1)  III. They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.

Abstract: Compounds are disclosed of the formula 1

Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.

Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH 2 O—, RCH 2 NH—, —COOCH 2 R, —CONHCH 2 R and —SCH 2 R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.

Abstract: The present invention is directed to novel lipid soluble steroid prodrugs compositions comprising steroid prodrugs, and uses of the same.

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: A process for the preparation of a compound of the formula ##STR1##

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: 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: The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that is directly attached to, an first amine; and (c) contains, is directly attached to, or is attached to an atom that is directly attached to a phosphate, a second amine, or a cationic sulfur. In a preferred embodiment, the structure consists of at least a nonaromatic cyclic portion or substituted derivative thereof. In a specific embodiment, the structure is a nonaromatic cyclic compound. In another embodiment, the molecule is a steroid. In yet another particular aspect, the structure is an aromatic compound. In another embodiment, the structure can bind to a nucleic acid sequence in a nonintercalative manner.

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 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: Steroid derivatives represented by formula (I) are disclosed. ##STR1## wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group --OCOR.sub.1, wherein R.sub.1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.

Abstract: A 21-alkoxysteroid compound represented by the formula ##STR1## wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms or a methylthiomethyl group, R.sup.2 is an alkanoyl group having 2 to 7 carbon atoms, and a wavy line indicates the .alpha.- or .beta.-configuration has anti-inflammatory activity.

Abstract: C.sub.16 -unsaturated corticoids are readily transformed to the corresponding 16.alpha.-methyl-17.alpha.-hydroxy corticoids by use of a .DELTA..sup.17 (.sup.20)-20-silyl ether.

Abstract: This invention concerns a method of substituting a chlorine atom for a predetermined hydrogen atom located within an organic compound which comprises contacting the organic compound containing the predetermined hydrogen atom with an esterifying agent comprising a pyridine ring or a substituted or fused ring derivative of a pyridine ring so as to produce an ester and treating the ester with a chlorinating agent so as to substitute the chlorine atom for the predetermined hydrogen atom. The ester comprises the pyridine ring or the substituted or fused ring derivative of the pyridine ring so positioned within the ester with respect to the predetermined hydrogen atom that a chlorine atom attached to the nitrogen atom of the pyridine ring or substituted or fused ring derivative of the pyridine ring reacts with the predetermined hydrogen atom.

Abstract: Preparation of novel solvates of beclomethasone 17,21-dipropionate, by dissolution of beclomethasone 17,21-dipropionate in an ethereal or halogenated hydrocarbon solvent and precipitation by the addition of di-isopropyl ether. These new solvates are bulk stable, in both the micronized and non-micronized forms. The micronized form is especially suitable for the preparation of stable aerosol.

Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.