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7417140 |
7α-Hydroxyacetyl and 7α-Hydroperoxyacetyl-substituted steroid compounds
The present invention involves intermediates, including a 7α-substituted steroid (II),
and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
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7414127 |
7 α-Enedione-substituted steroid compounds
The present invention involves intermediates, including a 7α-substituted steroid (II),
and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
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7411062 |
7α-biscarbonyl-substituted steroid compounds
The present invention involves intermediates, including a 7α-substituted steroid (II),
and processes which are used to prepare eplerenone, a useful pharmaceutical agent.
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7112670 |
Crystal form
The present invention involves a novel crystal form of 17β-hydroxy-7α-(5′-methyl-2′-furyl)-pregna-4,9(11)-die
n-3-one-21-carboxylic acid, γ-lactone, having the formula
which is an...
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6953851 |
Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I
wherein: —A—A—,...
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6586591 |
Process for preparation of 9,11-epoxy steroids and intermediates useful therein
A process for the formation of compounds of Formula VI: comprising hydrolyzing a compound corresponding to Formula VII: wherein —A—A—, —B—B—, R 3 , R 8 and R 9 are as defined in...
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6541463 |
Inhibitors of type 5 and type 3 17β-hydroxysteroid dehydrogenase and methods for their use
Novel methods of medical treatment and/or inhibition of development of diseases are disclosed for diseases that are sensitive to androgenic or estrogenic activity. The treatments utilize inhibitors...
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6177416 |
Oxyiminopregnancarbolactones
3-Oxyiminopregnane-21-carbolactones of formula I, ##STR1## wherein R is as defined by the specification, their production and use as pharmaceutical agents are described.
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5843933 |
11β-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents
Compounds of formula I ##STR1## wherein X, R 1 , R 2 , R 3 and R 4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical...
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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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5426179 |
Steroid compounds active on the cardiovascular system
Steroid compounds active on the cardiovascular system of formula ##STR1## wherein X, n, R, R 1 and R 2 have the meanings mentioned in the description are described.
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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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5273971 |
13-alkyl-11β-phenylgonanes
There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH; R 2 is alpha- or beta-position methyl or ethyl; R 1 is selected from heteroaryl...
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5244886 |
11β-phenyl-14βH steroids
New 11β-phenyl-14βH-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom...
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5001119 |
16-substituted androstanes and 16-substituted androstenes
Compounds of the formula: ##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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4987128 |
Novel 10β-alkynyl-steroids
Novel 10β-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally...
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4978657 |
Novel 11β-substituted-19-nor-steroids
Novel 19-nor-steroids of the formula ##STR1## wherein R 1 is an organic group of 1 to 18 carbon atoms optionally containing at leat one heteroatom with the atom immediately adjacent the 11-carbon...
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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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4904462 |
Multiply-tritiated steroidal-20,17-spirolactones and their use as tracer compounds
Novel, multiple-tritiated steroid-20,17-spirolactones of general Formula I ##STR1## wherein --A--B-- is --CH 2 --CH 2 --, --CHCH-- or ##STR2## and --C--D-- is ##STR3## R is hydrogen or tritium...
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4891365 |
17-Substituted estradienes and estratrienes
17-Substituted estradienes and estratrienes of Formula I ##STR1## wherein ##STR2## R is alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR3## R is hydrogen, alkyl, alkenyl or cycloalkyl...
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4808710 |
18-Phenyloestrane derivatives
A novel class of steroids having pregnancy-terminating and/or pregnancy-preventing activity and a very low antiglucocorticoid activity have been found. The compounds have the general formula:...
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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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4536401 |
11β-aryl estradienes, processes for their production and pharmaceutical preparations containing them
Compounds of the formula I ##STR1## wherein R 1 is ##STR2## wherein R I and R II each independently is alkyl of 1-4 carbon atoms, or R I and R II together with the connecting N-atom form a 5-...
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4507238 |
Process for the preparation of 3-(Δ.sup.4 -3-ketosteroid-17α-yl)propionic acid lactones
A simple process for preparing 3-(Δ 4 -3-keto-steroid-17α-yl)propionic acid lactones of the androstane series represented by the general partial formula ##STR1## wherein ABCD represents an...
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4502989 |
Aldosterone-antagonistic steroids
Novel spironolactone derivatives characterized by the C 11 -C 12 double bond which have a potent aldosterone-antagonistic activity without causing potassium loss, used alone in diagnosis and...
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4501695 |
Spironalactone process
The present invention relates to processes for the conversion of a 3-protected steroidal 17-ketone to a 17-spiro-γ-lactone having the appropriate 17-stereochemistry for spironolactone. Novel...
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4495102 |
Aminoalkyl steroids
Compounds of Formula I and II are useful as potent antiarrythmic agents without significant effect on cardiac output and blood pressure.
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4440684 |
Process for the preparation of 6-methyl-Δ.sup.4,6 -3-keto steroids
A process for preparing 6-methyl-Δ 4 ,6 -3-keto steroids of the formula ##STR1## comprises reacting a corresponding Δ 4 -3-keto steroid with methoxymethyl acetate (CH 3 --O--CH 2 --OAc) in an...
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4396614 |
Novel steroids
Novel steroids of the formula ##STR1## wherein R is selected from the group consisting of R 1 and R 2 , R 1 is selected from the group consisting of alkyl of 1 to 8 carbon atoms and alkenyl and...
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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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4267106 |
New process for the preparation 17β-hydroxy-3-oxo-17α-pregnene and pregnadiene-21-carboxylic acid γ-lactones
A process is disclosed for the preparation of 17β-hydroxy-3-oxo-l7α-pregn-4-ene-21-carboxylic acid γ-lactone and 17β-hydroxy-3-oxo-17α-pregna-4,6-diene-21-carboxylic acid γ-lactone of the...
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4265816 |
Process for preparing steroid-carboxylates
An alkali metal salt of a 3-(17β-hydroxyandrosten-3-one 3-acetal-17α-yl)propiolic acid which is useful as an intermediate in the preparation of...
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4258039 |
Novel 7-alkyl-steroids
Novel 7-alkyl-Δ 4 -17α-pregnene-3-ones of the formula ##STR1## wherein R is selected from the group consisting of saturated and unsaturated alkyl of 2 to 8 carbon atoms, cycloalkyl alkyl of 4 to...
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4211701 |
Spironolactone process
Spironolactone (VIII) is produced from ethisterone (I) by formation of the lactone (IV), a halo lactone (VI) and a Δ4,6-lactone (VII).
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4192802 |
Process for the manufacture of steroid carboxylic acid lactones
An advantageous method for the manufacture of steroidal lactones of the spironolactone and canrenone type involves the following reaction sequence: bromination of a 3β ,17-dihydroxy-17α...
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4150127 |
Novel steroid compounds having an oxygen function in the 19-position
Novel 19-oxygenated steroids of the 20-spiroxane series of the formula ##STR1## in which R 3 is a lower alkyl radical carrying an oxygen-containing functional group and R 4 is two hydrogen atoms...
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4119627 |
Process for the manufacture of 6β,7-methylene-3-oxo-4-ene steroids
The invention provides a novel general process for the manufacture of 6β,7-methylene-3-oxo-4-ene-steroids by successively (a) reacting a 3ξ,5β-dihydroxy-6-ene-steroid which is optionally...
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4108851 |
3β,17-Dihydroxy-5α,17α-pregn-20-ene-21-carboxylic acid γ-lactone and esters thereof
Preparation of 3β,17-dihydroxy-5α,17α-pregn-20-ene-21-carboxylic acid γ-lactone and esters thereof, the analgesic utility of the esters, and the utility of the diol both as an intermediate and...
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4079054 |
7α-Halogeno-3-oxo-1,4-pregnadiene-21,17β-carbolactones and related compounds
Described are 3-oxo-7α-halogeno-17α-1,4-pregnadiene-21,17β-carbolactone
s and compounds related thereto, i.e. 2',3'α-tetrahydrofuran-2'-spiro-17(7α-halogeno-1,4-androst
adie ne-3-ones) and...
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4076708 |
Process for the preparation of 7α-halogeno-3-oxo-4-dehydro steroids and novel 7α-halogeno derivatives produced thereby
3-Oxo-6-unsubstituted-7α-halogeno-4-dehydro steroids, wherein said halogen is chlorine, bromine or iodine, are prepared by reaction of a 3-oxo-6,7-di-unsubstituted-4,6-bis-dehydro steroid with at...
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4058522 |
Steroids effective against heavy-metal poisoning
A compound of the following formula: ##STR1## wherein X 1 is hydrogen or mercapto; X 2 is mercapto or acetylthio; X 3 is hydrogen or acetylthio; and X 4 is hydrogen, acetylthio or X 3 ...
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4057543 |
Process for the preparation of 17β-hydroxy-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone
A new process utilizing certain novel intermediates for the preparation of 17β-hydroxy-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone is described herein. The procedure utilizes readily...
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3968132 |
(17R)-Spiro-[androstane-17,1'-cyclobutan]-2'-ones, methods for their manufacture and intermediates useful therein
(17R)-Spiro-[androstane-17,1'-cyclobutan]-2'-ones are prepared by the reaction of a 17-oxo androstane, wherein all other ketones are blocked, with a cyclopropylarylsulfide or with a...
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3966714 |
Process for the preparation of a Δ.sup.4 -3-keto steroid 17-propiolactone
4-Androstene-3,17-dione and 1,4-androstadiene-3,17-dione are converted to 3-(17β-hydroxy-4-androsten-3-on-17α-yl)-propionic acid lactone in three steps by reaction with propargyl alcohol in the...
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3959322 |
Synthesis of 13-alkyl-gon-4-ones
The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are...
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3920635 |
(6S)-17'-hydroxy-3'-oxospiro[oxirane-2,6'-[17α]pregn[4]ene]-21'-car boxylic acid γ-lactone, the Δ1,4 analog, and intermediates
Preparation and the desoxycorticosterone acetate-blocking, antiestrogenic, and progestational properties of (6S)-17'-hydroxy-3'-oxospiro[oxirane-2,6'-[17α]pregn-[4]ene
]-21'-car boxylic acid...
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3919198 |
Dienic derivatives of the androstane series and process
The present invention relates to a dienic derivative of the androstane series having the formula ##SPC1## Wherein R is a member selected from the group consisting of hydrogen, alkyl having 1 to 4...
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3886146 |
17-Hydroxy-3-oxo-17α-pregna-4,7-diene-21-carboxylic acid-lactone, 4',5'-dihydrospiro[androsta-4,7-diene-17,2'(3'H)-furan]-3-one, and intermediates thereto
Preparation of DCA-blocking 17-hydroxy-3-oxo-17α-pregna-4,7-diene-21-carboxylic acid γ-lactone and 4',5'-dihydrospiro[androsta-4,7-diene-17,2'(3'H)-furan]-3-on
e from estrogenic intermediates is...
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3607889 |
10β-METHYL-13β-POLYCARBONALKYLGON-4-EN-3-ONES
13-Aklyl-10-methylgon-4-en-3-ones possessing androgenic, anabolic, progestational activity are prepared from the correspondingly substituted 13-alkyl-10-methylgonan-4-ones wherein groups labile to...
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3547909 |
SYNTHESIS OF GONA-2,5(10)-DIENES
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