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7629334 |
Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT)
The use of mesoprogestins as pharmaceutical components for the manufacture of a medicament for hormone replacement therapy (HRT) and as components for the combined use together with an estrogen for...
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7579335 |
Androstane 17α-carbonate derivatives for use in the treatment of allergic and inflammatory conditions
The present invention is directed to compounds of formula (I):
wherein
R 1 represents C 4 -C 7 branched alkyl group, a bicycloalkyl group, or a C 5 -C 6 cycloalkyl which optionally may be...
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7498321 |
17β-carbothioate 17α-arylcarbonyloxyloxy androstane derivative as anti-inflammatory agents
There are provided according to the invention compounds of formula (I) wherein R 1 represents C 1-6 alkyl or C 1-6 haloalkyl; R 2 represents —C(═O)-aryl or —C(═O)-heteroaryl; R 3 ...
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7427610 |
2-substituted estra-1,3,5(10)-triene-3-yl sulfamate with an anti-tumour action
Disclosed are compounds of formula I
and use thereof in a method of treating a tumor disease that can be influenced positively by the inhibition of tubulin polymerization.
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7371741 |
Estradiol derivatives and pharmaceutical compositions using same
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula:
wherein the variables are defined in the...
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7291609 |
Specific glucocorticosteroid compound having anti-inflammatory activity
A compound of formula (I):
or a physiologically acceptable solvate thereof.
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7291608 |
Anti-inflammatory 17.β.-carbothioate ester derivatives of androstane with a cyclic ester group in position 17.α
There are provided compounds of formula (I)
wherein the variables are as defined by the present specification; and solvates thereof, processes for preparing them and their use in therapy.
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7208613 |
Synthesis of s-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-3-oxoandrosta-1,4-diene-17β-carbothioate
The present invention provides a convenient process for the preparation of S-fluoromethyl 6α,9α-difluoro-11β-hydroxy-16α-methyl-17α-propionyloxy-
3-oxoandrosta-1,4-diene-17β-carbothioate, a...
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7009063 |
Process for the production of oxandrolone
The present invention relates to a process for the synthesis of oxandrolone from mestanolone. The process comprises the steps of: (a) oxidizing mestanolone to form...
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6921757 |
Organic compounds
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
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6706701 |
6, 7-oxygenated steroids and uses related thereto
Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of...
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6689768 |
Pharmaceutical preparations for treating side effects during and/or after GnRHa therapy
The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of...
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6610866 |
Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral...
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6610675 |
Inactive metabolite approach to soft drug design
The invention provides novel soft steroidal anti-inflammatory agents, pharmaceutical compositions containing said agents, and methods of administering same to mammals in the treatment of...
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6596885 |
19-Nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, their use as medicaments and compositions
Novel compounds having a formula selected from the group consisting of wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds...
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6492536 |
Steroids, their use as medicaments, their preparation process, the intermediates of this process and the compositions containing them
The subject of the invention is the products of formula (I): in which either R 1 represents halogen, hydroxyl, (C 1 -C 8 ) alkyloxy or (C 1 -C 12 ) acyloxy, and R 2 represents halogen or...
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6468981 |
Compositions and methods for targeting pharmaceutically active materials to cells containing androgen receptors
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...
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6436917 |
Non-estrogenic estradiol derivative compounds with anti-oxidative activity
New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds...
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6388109 |
14,15-cyclopropano steroids of the 19-norandrostane series, method for the production thereof and pharmaceutical preparations containing said compounds
Described are new 14,15-cyclopropano steroids of the 19-norandrostane series of general formula (I) and their pharmaceutically acceptable salts, a process for their production and pharmaceutical...
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6365582 |
S-substitute 11β-benzaldoxime-estra-4, 9-diene-carbonic acid thiolesters, method for the production thereof and pharmaceutical preparations containing these compounds
Thiol esters of S-substituted 11β-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula I their pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical...
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6080735 |
Estra-1,3,5(10)-trien derivatives, processes for their preparation and pharmaceutical compositions containing these compounds
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5977096 |
Steroids with radical-attracting aromatic substituents, process for the production thereof and pharmaceutical compounds containing the said substances
Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment...
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5972922 |
Steroids which inhibit angiogenesis
Novel angiostatic Δ 4 ,9(11) -steroids (I), ##STR1## C 21 -oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a...
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5859266 |
"N-T-butyl-androst-3-5-diene-17 β-carboxamide-3-carboxylic" acid polymorph A
Polymorph "A" a novel polymorphic form of N-t-butyl-androst-3,5-diene-17β-carboxamide-3-carboxylic acid. Novel processes for preparing polymorph "A" are also disclosed.
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5760025 |
Steroid derivatives for the treatment of prostatic hypertrophy, their preparation and uses
Compounds of formula (I): ##STR1## wherein: R 1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R 2 is: aryl-substituted alkyl, aromatic...
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5717088 |
Method of making steroid derivatives for the treatment of prostatic hypertrophy
Compounds of formula (I): ##STR1## wherein: R 1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R 2 is: aryl-substituted alkyl, aromatic...
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5698720 |
Steroid derivatives
The invented compound ##STR1## is useful for the production of steroidal-17-amides that have 5α-reductase inhibitory activity.
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5693629 |
Progesterone compound and use thereof
A progesterone compound represented by the following formula (1): ##STR1## wherein R 1 represents a C1-C23 hydrocarbon group!, and a neovascularization inhibitor containing the same as the active...
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5683995 |
17 substituted acyl-3-carboxy 3,5-diene steroidals as α-reductase inhibitors
Invented are 17α and 17β-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these...
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5641877 |
17-α and 17-β substituted acyl-3-carboxy-3, 5-dienes and use in inhibiting 5-α-reductase
Invented are 17α and 17β-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these...
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5641765 |
17-αand 17-βsubstituted acyl-3-carboxy-3,5-dienes and use in inhibiting 5-α-reductase
Invented are 17α and 17β-substituted acyl-3-carboxy-3,5-diene analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods for using these...
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5618806 |
17α and 17β-substituted estra-1,3,5(10)-triene-3-carbboxlic acid
Invented are 17α and 17β-substituted acyl-3-carboxy aromatic A ring analogues of steroidal synthetic compounds. Representative of such compounds include the following ##STR1## wherein Z is α or...
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5599806 |
Hydrazino and hydroxyamino-14-β-hydroxyandrostane derivatives active on the cardiovascular system processes for their preparation and pharmaceutical compositions containing same
The invention describes hydrazino and hydroxyamino-14β-hydroxyandrostane derivatives having general formula (I): ##STR1## wherein the symbol means α or β configuration and A, B, R 1 , R 2 , R 3...
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5596110 |
Process for the preparation of 3 β, 14 β-dihydroxyethianaldehyde
An improvement in a process for producing 3β,14β-dihydroxyethianaldehyde is disclosed wherein the oxidation of the lactone ring of digitoxigenin-3-acetate is conducted with an alkaline periodate...
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5596109 |
N-t-butyl-androst-3,5-diene-17β-carboxamide-3-carboxylic acid polymorph A
The invention describes a process for the preparation of the polymorph A form of a compound having the structure ##STR1## which involves triturating, crystallizing, or precipitating crude...
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5576310 |
11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds
This invention relates to new 11-benzaldoxime-estra-diene derivatives of the general formula I ##STR1## wherein Z is --CO--CH 3 , --CO--O--C 2 H 5 , --CO--NH-phenyl, --CO--NH--C 2 H 5 , --CO--C 2...
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5565588 |
9-alpha-hydroxy steroids, process for their preparation, process for the preparation of the corresponding 9(11)-dehydro derivatives and pharmaceutical preparations containing said steroids
New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione. The resulting compounds are useful intermediates in the...
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5561124 |
17-α-acyl steroids which inhibit 5-α-reductase
The invention relates to substituted 17α-acyl steroidal 5α-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for...
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5478957 |
Preparation of 6α, 9α-difluoro steroids
A process for the preparation of 6α,9α-difluoro steroids of the formula ##STR1## wherein R is hydrogen or an ester remainder.
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5444055 |
17-hydroxyiminomethyl-5-β, 14 β-androstane derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same
17-hydroxyiminomethyl-14β-hydroxy-5β androstane derivatives, active on the cardiovascular system, a process for their preparation and pharmaceutical compositions thereof having the general...
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5438134 |
Process for the production of unsaturated 17 α-cyanomethyl-17 β- h
The unsaturated 17α-cyanomethyl-17β-hydroxy steroids of the formula I, ##STR1## in which R 1 =Me, Eth; R 2 =H, Me; R 3 =H, OH, an acetoxy or alkoxy group; R 4 =H, R 5 =OH, an acetoxy, alkoxy...
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5436401 |
22-oxacholecalciferol derivative and process for preparing the same
A 22-oxacholecalciferol derivative represented by formula (I): ##STR1## wherein R 1 represents a hydrogen atom or a hydroxyl group; and R 2 and R 3 , which may be the same or different, each...
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5426102 |
14β-H-, 14-and 15-En-11β-aryl-4-oestrenes
Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which either Ia) R 11 represents a hydrogen atom in the...
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5407928 |
11β-aryl-gona-4,9-dien-3-ones
This invention relates to 11β-aryl-gona-4,9-dienes of the general formula I ##STR1## wherein the variables are defined in the specification. The compounds are progesterone antagonists and are...
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5399727 |
Preparation of Δ.sup.9(11) steroid
A process for the preparation of a compound of the formula ##STR1## comprising reacting a compound of the formula ##STR2## with chlorosulfonic in an organic solvent wherein the reaction is effected...
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5212166 |
Unsaturated 17β-subsituted 3-carboxy steroids
The present invention concerns steroidic 5α-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur; R is a group; a) --OR 4 , wherein R 4 is hydrogen...
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5196411 |
17β-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5α-reductase inhibitors
17β-acyl-3-carboxy-androsta-3,5-dienes as testosterone 5α-reductase inhibitors of the formula: ##STR1## wherein R is C 3 -C 8 cycloalkyl, which can be substituted with C 1 -C 4 alkoxy or C 6 ...
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5149696 |
19➝nor➝steroids
Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and...
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5140106 |
Process for the production of 3-deoxy-4-ene steroids
A process for the production of 3-deoxy-4-ene steroids of the general formula I ##STR1## is described, in which R 1 , R 2 and R 3 mean a hydrogen atom or a methyl group, R 4 represents a...
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5116830 |
Stereoisomerically pure 17α-ethynyl-estra-2-en-17β-ol and the 17β esters thereof, methods of preparation and uses
This invention relates to a stereoisomerically pure Δ 2 compound of the formula (I): ##STR1## wherein: R 1 is hydrogen or --(CO)--R 2 , wherein: R 2 is an organic substituent selected...
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