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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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7468433 |
Process for the production of 16,17-[(cyclohexylmethylen)bis(oxy)]-11,21-dihydroxy-pregna-1,4-dien-3,20-dion or its 21-isobutyrat by transketalisation
The invention relates to a process for the preparation of 16,17-[(cyclohexylmethylene)bis(oxy)]-11,21-dihydroxypregna-
1,4-diene-3,20-dione[11β,16α(R)] and similar compounds, by reaction of an...
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6787533 |
Process for R-epimer enrichment of 16,17-acetal derivatives of 21-acyloxy pregna,4-dien-11β, 16α, 17α-triol-3,20-dione derivatives
R-epimer enrichment of 16,17-acetal derivatives of 21-acyloxy pregna-1,4-dien-11beta,16alpha,17alpha-triol-3,20-dione derivatives is effected by fractional crystallization.
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6392036 |
Dry heat sterilization of a glucocorticosteroid
The invention provides a process for the sterilization of a powdered form of a glucocorticosteroid, sterile glucocorticosteroids, sterile formulations containing glucocorticosteroids and use...
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6369218 |
Isomerisation of 6β-fluorosteroids into the corresponding 6α-fluoro derivatives
Described herein is the isomerisation process of 6β-fluorosteroids into the corresponding pharmacologically active 6α-fluoro derivatives, comprising the reaction of 6β-fluorosteroids, or 6α/6β...
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6239120 |
Method and means for treating glomerulonephritis
The invention provides the use of a glucocorticoid having a first pass metabolism in the liver of at least 90% as active substance, for the manufacturing of a medicament for oral or rectal...
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6197762 |
Nitrosated and nitrosylated steroids compositions, and methods for treating respiratory disorders
Disclosed are (i) compounds of a steroid, a β-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO 2 group or a...
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6169178 |
Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position
Described herein is a process for the preparation of an acetal of formula (I) in which R 1 is an alkyl, R 2 is H or an acyl, X is β-OH and Y is H, comprising the acetalization with control of...
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5837698 |
Steroid nitrite and nitrate ester derivatives useful as anti-inflammatory drugs
The present invention relates to a pharmaceutical composition or preparation which comprises hydroxyl containing steroidal hormones and organic nitrite/nitrate or other nitric oxide donating agents.
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5792758 |
Steroid nitrite ester derivatives useful as anti-inflammatory drugs
The present invention discloses novel steroid nitrite ester derivatives, and to their use treating inflammatory diseases.
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5733901 |
Prednisolone derivatives
Epimers of the compound having the formula (I) are disclosed, both in their pure form and mixed in any desire mix ratio. ##STR1##
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5670676 |
Process for preparation of 9α -chloro-11β formyloxypregna-3.20-diones
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...
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5616573 |
Glucocorticoids
Glucocorticoids of general formula I R--Val--O--GC (II), are described, in which O-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action, Val represents a valine radical...
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5602248 |
Process for preparation of 9α-chloro-11β-formyloxypregna-3,20-diones
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...
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5556964 |
Process for the manufacture of budesonide
The present invention relates to a novel process for the manufacture of (22 R,S)-16α, 17α-butylidenedioxy-11β, 21-dihydroxypregna-1,4-diene-3,20 dione (I) by reacting 11β, 16α, 17α...
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5482934 |
Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
The present invention relates to compounds of the formula: ##STR1## in which X 1 and X 2 correspond to H or F without distinction; R 1 represents the following radicals: ##STR2## and R 2 ...
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5434258 |
δ.sup.1,4 -pregnadiene-3,20-diones
A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and...
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5310896 |
Process for preparing Δ.sup.1,4 -pregnadiene-3,20-diones
A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and...
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5200518 |
Anti-inflammatory carboxycyclic acetal pregnane derivatives
Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH 3 and Y is ##STR2## wherein R 1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl; R 2 is COOR 6 , R 5 COOR 6 , or R 5 ...
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5053404 |
Novel steroid derivatives, pharmaceutical compositions containing them and process for preparing same
The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen or hydroxyl group; X stands for hydrogen or halogen with the proviso that if A is...
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4950659 |
16,17-acetalsubstituted androstane-17β-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor
The invention refers to compounds having anti-inflamatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula the 1,2-position is saturated or is...
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4933168 |
Stable, crystalline flunisolide
A unique crystalline polymorphic form of flunisolide is disclosed which is stable in aerosols such as Freon® mixtures and is valuable in the treatment of respiratory diseases, particularly...
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4925933 |
Method of controlling the epimeric distribution in the preparation of 16,17-acetals of pregnane derivatives
A method of controlling the epimeric distribution in the preparation of 16,17-acetals of pregnane derivatives characterized in reaction of a corresponding 16,17-acetonide with an aldehyde or ketone...
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4835145 |
16,17 acetals of pregnane derivatives and pharmaceutical compositions containing them
A compound exhibiting anti-inflammatory properties having the formula ##STR1## in which X is H, Hal or CH 3 COO--; R 1 is CH 3 (CH 2 ) 2 CH--; and R 2 and R 3 are separately H or Hal; and a...
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4695625 |
Process for the preparation of 16,17 acetals of pregnane derivatives
A process for the preparation of 16,17 acetals of pregnane derivatives by trans-ketalization of 16,17-acetonides is described. In the instance of the preparation of...
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4693999 |
Liposomes containing steroid esters
Pharmaceutical composition for administration primarily to the respiratory tract when treating and controlling anti-inflammatory conditions comprising liposomes in combination with a compound of...
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4613463 |
Process and intermediates for the preparation of 17 alphahydroxyprogesterones and corticoids from an enol steroid
This invention discloses an improved process for the production of corticoids from 17α-hydroxy steroids utilizing peroxymonosulfate.
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4456601 |
3-Chloro-pregnane derivatives and a process for the preparation thereof
New Δ 1 ,3,5 -3-chloro-pregnane derivatives of the general formula (I), ##STR1## wherein X is hydrogen atom, acetyl group or a chloroacetyl group, and Y and Z represent hydrogen atom or a...
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4432976 |
Cyclocarbonate esters of 16α,17α, dihydroxy anti-inflammatory steroids
Corticoids of Formula I ##STR1## wherein is a single bond or a double bond, X is hydrogen, fluorine, or chlorine, Y represents two hydrogen atoms or an oxygen atom, and Z is hydrogen or...
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4404200 |
4-Pregnene-derivatives, a process for their preparation, composition and method for the treatment of inflammatory conditions
The invention refers to compounds having anti-inflammatory activity, characterized by the formula ##STR1## in the form of a stereoisomeric mixture or an epimer of the R or S type regarding the...
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4404141 |
Δ.sup.9(11) - And Δ.sup.16 -21-chloro-20-keto steroids of the pregnane and D-homopregnane series, their preparation and use as intermediates for the synthesis of highly effective corticoids
Δ 16 - and Δ 17 -21-chloro-20-keto steroids of the formula ##STR1## wherein n is 1 or 2, C 1 C 2 and C 9 C 11 represent a CC-single or CC-double bond, R 1 is H or OH, R 2 is H...
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4383992 |
Water-soluble steroid compounds
Beta-cyclodextrin forms a water-soluble complex or inclusion compound with steroid compounds having a molecular structure smaller than the interior cavity in the doughnut-shaped molecular structure...
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4376767 |
Pyridylmethyl esters of selected bio-affecting carboxylic acids
Novel pharmaceutically useful derivatives of selected known bio-affecting carboxylic acids are disclosed, said derivatives having the structural formula ##STR1## wherein R 1 and R 2 , which can be...
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4322349 |
Process for preparing 6-methylene steroids
A process for preparing a 6-methylene-Δ 4 -3-keto steroid of the formula ##STR1## wherein R is hydrogen, alkoxy of up to 6 carbon atoms or acyloxy of up to 6 carbon atoms wherein the acyl group...
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4221787 |
Esteramide prodrugs of anti-inflammatory corticosteroids
Transient, C-21 and/or C-17 esteramide prodrugs of the anti-inflammatory corticosteroids, prepared by esterification of hydroxy steroids, are disclosed.
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4198403 |
17 Beta-thiocarboxylic acid esters of 4-halo-3-oxoandrost-4-enes
Certain 3-oxoandrost-4-ene and 3-oxoandrosta-1,4-diene 17 beta-thiocarboxylic acid esters substituted at the 4-position with a fluoro, chloro or bromo and optionally substituted at the six position...
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4198336 |
Chemical process for preparing androsta-4-ene 17α-carboxylic acids
This invention is a process for preparing 3-keto-androst-4-ene 17α-carboxylic acids, androsta-1,4-diene 17α-carboxylic acids and their 17α-esters by reacting a corresponding...
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4086254 |
Photocleavable steroids
This invention relates to novel compounds of the formula: ##STR1## wherein X is H, methoxy, bromine or chloro; R 1 is hydrogen or hydroxy, acyloxy wherein acyl is 2 to 8 carbon atoms, R 2 is...
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4065452 |
21,21-Dihalo steroids
Novel, topically-active anti-inflammatory steroids are represented by the formula ##STR1## wherein X is fluoro, chloro or hydrogen; X 1 is fluoro, chloro, bromo, or hydrogen; X 2 is hydroxy or...
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4064240 |
21-Cyclic acetals of steroidal 21-aldehydes and methods of preparation
21-Cyclic acetals of steroids of the corticoid series are prepared from the corresponding 21-hydroxy steroids. The products have utility as anti-inflammatory agents.
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4049804 |
Novel pregnanoic acid derivatives
Pregnanoic acid derivatives of general formula ##STR1## wherein is a single bond or a double bond; X is hydrogen, fluorine or methyl; Y is hydrogen, fluorine or chlorine; Z is...
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4031075 |
Alkylated pregnanes and process for obtaining same
The invention relates to novel 21-alkylated steroids of the pregnane series having the formula: ##STR1## WHEREIN X = H or halogen; Y = h 2 , h(oh), h(oacyl), O or H(halogen); R 1 = an alkyl...
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4011315 |
21-Acetals and mixed acetals of steroidal 21-aldehydes, intermediates and methods of preparation
21-ACETALS AND MIXED ACETALS OF STEROIDS OF THE CORTICOID SERIES ARE PREPARED FROM THE CORRESPONDING 21-HYDROXY STEROIDS AND HAVE UTILITY AS ANTI-INFLAMMATORY AGENTS.
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3996359 |
Novel stereoisomeric component A of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steroid 21-acylates, compositions thereof, and method of treating therewith
A process for the resolution of stereoisomeric mixtures of certain steroids obtained by synthesis into its components, comprising subjecting the stereoisomeric mixture to gel filtration, the...
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3996358 |
21-Esters of steroidal-21-aldehyde hydrates and 21-aldehyde hemiacetals and methods of preparation
21-Esters of 21-aldehyde hydrates and 21-aldehyde hemiacetals of steroids of the corticoid series are prepared from the corresponding 21-hydroxy steroids and have utility as antiinflammatory agents.
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3992534 |
Compositions and method of treating with component B of stereoisomeric mixtures of 2'-unsymmetrical 16,17-methylenedioxy steriods
A process for the resolution of stereoisomeric mixtures of certain steroids obtained by synthesis into its components, comprising subjecting the stereoisomeric mixture to gel filtration, the...
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3984544 |
Retinoic acid esters of steroids of the pregnane series, their use in the treatment of acne and pharmaceutical formulations useful therefor
Novel retinoic acid esters of anti-inflammatory steroids of the pregnane series are described and their use in the treatment and control of acne vulgaris via the topical or intralesional route. A...
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3983233 |
Compositions and method of treating with stereoisomeric mixtures of 2-unsymmetrical 16,17-methylenedioxy steroids
Novel steroids having the general formula: ##SPC1## Wherein X and Y are independently selected from hydrogen and fluorine, X being selected from hydrogen and fluorine when Y is hydrogen and X being...
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3976637 |
3,20-Diketopregnenes having an 11β-acetal group
3,20-Diketopregnenes having in the 11β-position a group of the formula ##SPC1## Wherein R 1 is alkyl and R 2 is hydrogen, alkyl, alkoxy, or halogen, and having a cyclic 16,17-acetal or ketal...
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3975378 |
20-Cyano-20,21-epoxy steroids
Novel compounds useful as anti-inflammatories are represented by the formula ##SPC1## Wherein Z is a single or double bond; X and X 1 are independently H, F or Cl; and X 2 is OH or when X 1 is...
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