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7323454 Etonogestrel esters  
The subject invention provides new progestogen esters and uses thereof.
6855836 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds  
The invention relates to 17-methylene steroids, process for their production and pharmaceutical compositions that contain these compounds. The compounds according to the invention have a...
6737417 Compounds with hydroxycarbonyl-halogenoalkyl side chain  
The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral...
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...
6579864 3-methylene steroid derivatives  
The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R 1 is H or together with R 3 forms a β-epoxide or R 1 is absent if there is a 5-10 or 4-5 double...
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...
6177417 Cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives, process for preparation and use thereof  
The present invention relates to a cholanic acid ring based 4-(trifluoroacetyl)phenyl derivatives of the following formula 1, process for preparation and use thereof. The cholanic acid ring based...
5521169 Ascosteroside and analogs thereof useful in antifungal compositions for methods of treating infections and inhibition of fungal growth  
Ascosteroside, obtainable by cultivation of a strain of Ascotricha amphitricha A.T.C.C. No. 74237, analogs thereof and salts and prodrugs of these compounds. The compounds have antifungal activity...
5443758 Non-linear optical material containing steroidal ketone compound  
A steroidal ketone compound having a substituted or unsubstituted aromatic group or heterocyclic aromatic group is useful as a non-linear optical material in a non-linear optical device.
5252565 Haloethyl-substituted steroid enzyme inhibitors  
The present invention is directed to a group of compounds which are haloethyl substituted steroidal enzyme inhibitors. These compounds are useful as aromatase, 19-hydroxylase, and aldosterone...
5236913 11-methylene-oestr-15-enes, processes for their preparation, and pharmaceutical compositions  
The present invention is concerned with novel 11-methylene-oestr-15-enes of the formula: ##STR1## wherein R 1 =H or acyl with 1-18 C-atoms, preferably H, R 2 =ethinyl, vinyl, chloroethinyl,...
5162312 11β-substituted 16α, 17α-methylene-estra-4,9-dien-3-ones  
11β-substituted-16α, 17α-methylene-estra-4,9-dien-3-ones of formula I ##STR1## wherein R 1 is a methyl or ethyl group; R 2 is H; a C 1 -6 -alkyl, -alkoxymethyl, -alkanoyl or -alkoxcarbonyl...
5086047 Novel steroids  
A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon...
4990635 Synthesis of 6-methylene derivatives of androsta-1,4-diene-3,17-dione  
The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula (I) ##STR1## wherein each of R 1 and R 3 , independently, is hydrogen or C 1 -C 6...
4945064 Estrane and androstane derivatives, process for producing them and preparations containing these compounds  
Estrane and androstane derivatives of formula I ##STR1## wherein X is bromine, iodine, triphenyltin or trialkyltin of 1 to 6 carbon atoms per alkyl radical, Y represents two hydrogen atoms or...
4925834 3-methylene-4-androsten-17-ones, process for their production and pharmaceutical preparations containing them  
A 3-methylene-4-androsten-17-one of formula I ##STR1## wherein R a represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical...
4921638 17β-cyano-9α,17α-dihydroxyandrost-4-en-3-one  
The invention is the compound 17β-cyano-9α, 17α-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17α-halo silyl ethers (II).
4920114 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors  
19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein....
4876045 Process for the preparation of methylene derivatives of androsta-1,4-diene-3,17-dione  
The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R 1 and R 3 , independently, is hydrogen or C 1 -C 6 ...
4873233 17-Substituted androsta-1,4-dien-3-one derivatives  
The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R 3 , independently, is hydrogen or C 1 -C 6 alkyl; R 1 is...
4870069 11β-alkynyl-estrenes and -estradienes, their production and pharmaceutical preparations containing them  
11β-substituted steroids of the formula ##STR1## wherein A and B together represent a second bond between the 6-position and 7-position carbon atoms, or, respectively, are each H; X is O, two H...
4865767 Novel radioactive steroids  
Novel radioactive steroids labelled with tritium of the formula ##STR1## wherein 3 H is tritium and R and R 1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6...
4861763 17 α-(substituted-methyl)-17β-hydroxy/esterified hydroxy steroids and their progestational use  
Steroids of the formula: ##STR1## which are characterized by a 17α-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17β-hydroxy/esterified hydroxy...
4824830 6- or 7-methylenandrosta-1,4-diene-3,17-dione derivatives and process for their preparation  
The invention relates to new 6- or 7-methylenandrosta-1,4-diene-3,17-diones of the following formula ##STR1## wherein R is hydrogen or fluorine; R 1 is hydrogen or C 1 -C 6 alkyl; R 2 is...
4822528 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and process for their preparation  
The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R 1 , R 2 and R 3 is, independently, hydrogen or C 1 -C 6 ...
4808578 6-Alkylidene 10 β-alkynylestrene derivatives and pharmaceutical methods for their use  
The invention relates to 6-substituted 10β-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs. The...
4808616 6-substituted androsta-1,4-diene-3,17-diones  
The invention relates to 6-alkylidenandrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R 2 , independently, is hydrogen or C 1 -C 6 ...
4794119 Aqueous crystalline suspension of steroid glycoesters  
An aqueous crystalline suspension of a 17-tertiary steroid glycoester contains a compound of Formula I ##STR1## wherein X is two hydrogen atoms or an oxygen atom, Y is two hydrogen atoms or a...
4777165 6α, 16β-dimethyl corticoids and their anti-inflammatory use  
6α,16β-Dimethyl corticoids of general Formula I ##STR1## wherein the bond - ------- is a single bond or a double bond, and X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine...
4753932 Novel 10-substituted steroids  
A novel steroid of the formula ##STR1## wherein X is methylene and R is an optionally substituted carbocyclic aryl or heterocyclic aryl or optionally substituted vinyl or ethynyl or X is a simple...
4670427 1α,2α-methylene-6-methylene- and 6α-methylpregnenes, their preparation and pharmaceutical use  
1α,2α-methylene-6-methylene- and 6α-methylpregnenes of Formula I ##STR1## wherein A is ##STR2## and R is a hydrogen atom, an acyl group, or an alkoxymethyl group are strong antiandrogens, and...
4634695 Steroid derivatives  
Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R 1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting...
4619922 6α, 16α-dimethyl corticoids  
6α,16α-Dimethyl corticoids of general Formula I ##STR1## wherein the bond is a single bond or a double bond, X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom, R...
4618456 Ethynylation of 16-methyl-17-keto steroids  
The process of the present invention transforms 16α- or 16β-methyl-17-keto steroids (I) to the corresponding 17α-ethynyl-17β-hydroxy-16α- or 16β-methyl steroids (II) without epimerization and...
4614621 Ethynylation of 16-methylene-17-keto steroids  
The process of the present invention transforms 16-methylene-17-keto steroids (I) to the corresponding 17α-ethynyl-17β-hydroxy-16-methylene steroids (II).
4582644 Epi-ethynylation process  
Ethynylation of 17-keto steroids (I) by standard means in the presence of a polar amine solvent produces the epi (17β-ethynyl-17α-hydroxy) configuration at C 17 . The epi-ethisterone compounds...
4567001 16-Methylene-17α-hydroxy-progesterones  
16-Methylene-17-keto steroids (III) are transformed to the corresponding 16-methylene-17α-hydroxyprogesterones (VII) which are intermediates useful in the production of betamethasone, diflorasone...
4567000 11-Difluoromethylene steroids  
11-Difluoromethylene steroids having progestational and anti-progestational properties, useful as anti-fertility agents, are disclosed as well as a process for making the 11-difluoromethylene...
4557867 11β-Difluoromethyl and (E)- and (Z)-11-fluoromethylene steriods  
Known reactions are arranged in a novel manner to produce 11β-difluoromethyl and (E)- and (Z)-11-fluoromethylene 19-norandrostenediones and 19-nor-13β-ethylandrostenediones which are useful as...
4555507 Novel 6, 16-dimethylcorticoids, their preparation and use  
Compounds of Formula I ##STR1## wherein the bond is a single bond or a double bond, X is hydrogen, flourine, chlorine, or bromine, R 1 is formyl, alkanoyl or alkoxyalkyl each of which...
4548748 Cyanohydrin process  
Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17α-acyl progesterones.
4546098 Estrogen synthesis inhibitors  
Invention relates to 3-methylene substituted androst-4-ene-17-oxygenated compounds substituted with various substituents at the 10β-position which are useful as inhibitors of estrogen biosynthesis.
4544555 3,20-Diketo, 6-methyl, 17-alpha-hydroxy 19-norpregna 4,6-diene, its esters and the uses thereof  
A novel 3,20-diketo, 6-methyl, 17-alpha hydroxy 19-norpregna-4,6-diene is disclosed, along with a method for its production from 17-alpha-hydroxy 19-nor-progesterone acetate. The 17-alpha acetic...
4526720 Process to prepare stabilized monolithium acetylide  
The process of the present invention uses an amine to prepare monolithium acetylide which is sufficiently stable at up to 0° and yet is sufficiently reactive to react with 16-substituted-17-keto...
4512986 Progrestationally active steroids  
Novel steroids having the formula ##STR1## wherein R 1 is selected from the group consisting of methyl, ethyl, and propyl; R 2 is selected from the group consisting of H and methyl; R 3 is...
4443377 Isomerization-acylation process  
17α-Hydroxy-6,16-dimethylenepregn-4-ene-3,20-dione simultaneously isomerized and acylated to 17α-hydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dion e 17-acetate.
4396615 Method of treating androgen-related disorders  
A method of treating androgen-related disorders in an animal which comprises administering to the animal dihydrotestosterone level decreasing amounts of a compound of formula (I): ##STR1## wherein...
4371529 11-Methylene-Δ.sup.15 -steroids, their preparation and use in pharmaceuticals  
11-Methylene-Δ 15 -steroids of Formula I ##STR1## wherein R 1 is hydrogen or acyl and R 2 is ethynyl, chloroethynyl or propynyl, are distinguished by a strong progestational activity and...
4346037 Base catalyzed acylation with enol esters  
This invention relates to processes for base catalyzed acylations using enol esters, for example, isopropenyl acetate. Particularly, the processes are useful for acylating acid sensitive alcohols...
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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