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6620801 |
17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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6489081 |
Organosilyl radical generators and their applications
Compounds of formula I wherein R 1 , R 2 , and R 3 independently of one another are hydrogen; C 1 -C 20 alkyl which is unsubstituted or substituted by OH, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio,...
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6133280 |
Androgen synthesis inhibitors
This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of...
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5808059 |
Matrix-supported sapphyrins
The invention relates to the field of polymer- and other matrix-supported sapphyrins. Disclosed are silica gel, glass, resin and other polymer- and matrix-supported sapphyrins and...
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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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5756722 |
Intermediates for the preparation of Δ.sup.4,9(11),17(20) -pregnatriene-3-ones
The novel intermediates of the formula ##STR1## wherein L, K and M are as defined in the specification which are useful intermediates for the preparation of Δ 4 ,9(11),16 -pregnatriene-3-ones.
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5741795 |
16-substituted-6-aza-androsten-4-ene-3-ones as 5-α-reductase inhibitors
Compounds of the formula I ##STR1## are inhibitors of 5α-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern...
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5641767 |
Modified bile acids process for their preparation and their use
The invention relates to linker-modified bile acid derivatives of the formula I: ##STR1## wherein the radicals X 1 , X 2 , X 3 and Y and n are as defined in the claims, and to a process for their...
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5401864 |
Process for preparing 21 acyloxy-Δ4,9(11),16 pregnatrienes 3-20-dione
A process for the preparation of a compound of the formula ##STR1## wherein R 1 is acyl of 1 to 8 carbon atoms, by reducing an intermediary to form an alcohol, oxidizing the alcohol to form an...
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5359055 |
Pregnane derivatives and processes for production thereof
There are provided pregnane derivatives represented by formula ##STR1## wherein A 1 represents a hydrogen atom or a hydroxyl group, A 2 represents a substituent such as a hydroxyl group when A 1 ...
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5359054 |
Initial compounds for the production of 10β-H-steroids and a process for the production of these initial compounds
The invention includes compounds of the following formula ##STR1## where A and B either A and B form an additional double bond and D is a hydrogen atom or B and D form an additional double bond and...
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5352781 |
Process for precursors to calcitriol and related compounds
The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula...
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5336686 |
17 Methylene lactones of steroids
A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application having antiglucocorticoid and antiprogestomimetic...
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5232915 |
9α-hydroxy-19,11β-bridged steroids, their production and pharmaceutical preparations containing these steroids
9α-Hydroxy-19,11β-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R 1 , R 2 , G, Z, R 4 --Y and R 4 ' --Y' follows from the description. The...
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5218109 |
Steroid compounds
Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R 1 and R 2 each is a hydrogen atom or a hydroxyl-protecting group, R is a...
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5187273 |
Δ.sup.4,9(11),17(20) -pregnatriene-3-ones
A compound of the formula ##STR1## wherein Hal is chlorine or bromine, R is selected from the group consisting of alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 carbon atoms and a silylated...
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5182381 |
Intermediates for 3-keto-19-nor-Δ.sup.4,9 -steroids
Novel 3-keto-19-nor-Δ 4 ,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.
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5144032 |
Preparation of tertiary amine borane adducts
An improved curing agent for use in coatings, laminates, moldings, castings and adhesives comprising the use of an amine-boron adduct component along with anhydride and epoxy component mixtures....
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5010202 |
Novel silicon-organic compounds, containing an oxazolidine group
Novel silicon-organic compounds containing an oxazolidine group are defined by the general formula (I): ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, n and y have the meanings reported in the...
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4977291 |
Process of producing a silanic or siloxanic compound containing at least one cycloalkyl ring
A process of producing a silanic or siloxanic compound containing at least one cycloalkyl ring by the hydrogenation of a corresponding compound containing at least one aromatic ring, in the...
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4977255 |
Steroidal 17α-silyl ethers and process to corticoids and progesterones
17β-Cyano-17α-hydroxy steroids (I) are transformed to 17α-halo silyl ethers (II) which are intermediates useful in the production of progesterones (V), 17-hydroxyprogesterones (VI), corticoids...
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4975536 |
Conversion of a delta16-steroid to a delta17(20)-20-silyl ether
The present invention is a process for conversion of Δ 16 -steroids (I) ##STR1## to the corresponding Δ 17 (20) -20-silyl ether (III) ##STR2## by reaction with (1) a preformed copper hydride or...
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4954414 |
Photosensitive composition containing a transition metal coordination complex cation and a borate anion and photosensitive materials employing the same
A composition including a cationic transition metal coordination complex and a borate anion, wherein said composition is capable of absorbing actinic radiation and producing free radicals which can...
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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).
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4912097 |
Novel 11 β-alkynylphenyl-10-nor-steroids
Novel 11β-alkynylphenyl-19-nor-steroids of the formula ##STR1## wherein R 1 is alkynyl of 2 to 8 carbon atoms optionally substituted with at least one member of the group consisting of --OH...
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4898694 |
17-Hydroxy-steroids
Compounds of the formulae: ##STR1## are useful as anti-cancer, anti-obesity, anti-diabetic, anti-coronary agents, anti-aging agents, anti-hypolipidemic agents and anti-autoimmune agents.
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4891426 |
16α-methyl-17α 20-epoxysteroid and process
C 16 -unsaturated corticoids are readily transformed to the corresponding 16α-methyl-17α-hydroxy corticoids by use of a Δ17(20)-20-silyl ether.
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4758383 |
Ergosta-1,5,7,22-tetraen-3β-ol and its use as an intermediate for 1α-hydroxy vitamin D.sub.2
New processes for preparing new steroid derivatives including ergosta-1,5,7,22-tetraen-3β-ol, 1α-hydroxyergosteryl diacetate, etc. which are useful intermediates in the synthesis of 1α-hydroxy...
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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...
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4614616 |
Process for preparing 3β7β-dihydroxy-Δ.sup.5 -steroids
A process for preparing a 3β,7β-dihydroxy-Δ 5 -steroid of the formula ##STR1## wherein Q is ##STR2## and R 1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl,...
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4599330 |
Method of treating milk fever
The present invention relates to a method of preventing milk fever which comprises administering to a preparturient female ruminant an effective amount of...
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4568492 |
Δ16-20-Keto steroid conversion to 17α-hydroxy-20-keto steroids
Δ16-20-keto steroids (I) are converted to 17α-hydroxy-20-keto steroids (III) in 2 steps, hydrosilylation followed by peracid oxidation.
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4550163 |
Ligand analog-irreversible enzyme inhibitor conjugates
The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding...
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4548748 |
Cyanohydrin process
Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17α-acyl progesterones.
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4519946 |
Steroids
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 carbons atoms containing at least one atom selected from the group consisting...
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4447424 |
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...
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4421690 |
Process for the preparation of 24,24-difluoro-1α,25-dihydroxy vitamin D.sub.3 and intermediates obtained therefrom
The present invention relates to a process and intermediates for the preparation of 24,24-difluoro-1α,25-dihydroxycholecalciferol from the readily-available 1α,3β-dihydroxyandrost-5-en-17-one...
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4407753 |
8α-Oestra-1,3,5(10)-triene derivatives, processes for their preparation and pharmaceutical compositions
The invention relates to new 8α-oestra-1,3,5(10)-triene derivatives having the formula: ##STR1## in which R 1 =H or a free, esterified or etherified hydroxy group; R 2 =H or a free,...
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4401596 |
Novel 17-oxazoline-steroids
Novel 17-oxazoline-steroids of the formula ##STR1## wherein R 1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted with a member of the group...
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4336193 |
Process for preparing vitamin D-lactones
The invention provides methods for preparing the various isomeric forms of 25-hydroxyvitamin D 3 -26,23-lactone utilizing cyanohydrin formation with readily prepared steroid materials followed by...
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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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4287129 |
Synthesis of 1α-hydroxy-7-dehydrosteroids
Enol acetylation is carried out on a variety of 1,4,6-trien-3-ones to form 1,3,5,7 tetraene structures from which 1α-hydroxy-7-dehydro steroids are obtained. The compounds are intermediates used...
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4272530 |
Δ.sup.1,3,5(10) -Estratrienes
Novel 11β -substituted-Δ 1 ,3,5(10) -estratrienes of the formula ##STR1## wherein R 1 is selected from the group consisting of optionally substituted unsaturated alkyl of 2 to 8 carbon atoms,...
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4243608 |
3-(4-Hydroxyphenyl)pentanedioic acid, monohydrazide, derivatives and analogs
Compounds having the formula ##STR1## and acid-addition salts thereof, wherein R is hydrogen or alkyl of 1 to 3 carbon atoms and n is 0,1,2,3 or 4 are useful reagents for derivatizing organic...
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4239681 |
Androst-4-en-19-ols
Derivatives of androst-4-en-19-ol are useful for enhancing libido and related psychic attitudes.
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4233296 |
11β-Substituted-Δ.sup.4,9 -estradienes
Novel steroids of the formula ##STR1## wherein R 1 is linear or branched alkyl of 1 to 12 carbon atoms, unsaturated alkyl of 2 to 8 carbon atoms optionally substituted, optionally substituted aryl...
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4222940 |
Cyclization substrates, cyclization process and related 11β-axially-substituted steroids
There are disclosed substrates of the formula: ##STR1## wherein: (a) R 1 is H or C 1 -C 4 alkyl; (b) R 2 is H or C 1 -C 4 alkyl with the proviso that R 1 is H when R 2 is alkyl, and with...
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4221713 |
Cyclization substrates and related 11α-equatorially-substituted steroids
Cyclisation substrates are disclosed of the formula: ##STR1## wherein: (a) R 1 is H or alkyl of one to four carbon atoms; (b) R 2 is H or alkyl of one to four carbon atoms, with the proviso...
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4216159 |
Synthesis of 16-unsaturated pregnanes from 17-keto steroids
17-Keto steroids (I) in their protected form (IIa or IIb) are reacted with a metalated olefin (VI) to give a 21-aldehyde (IV) which is readily transformed to a 16-unsaturated pregnane (V) which is...
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4191697 |
Novel steroids
Novel Δ 1 ,3,5(10),6 -estratetraenes of the formula ##STR1## R is selected from the group consisting of hydrogen, acyl of an alkanoic acid of 1 to 5 carbon atoms, optionally substituted benzoyl,...
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