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Class 552/639 - 17 alpha-position substituted (e.g., 17 alpha-alkynylandrosta-4, 6-diene 3,17-diols, etc.)


Subclass of Class 552 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which a substituent is bonded directly at the
No. of patents: 62
Last issue date: 03/27/2007


1    
NumberTitleIssue Date
7196074Methods of making, using and pharmaceutical formulations comprising 7α, 11β-dimethyl-17β-hydroxyestra-4, 14-dien-3-one and 17 esters thereof
Methods of using 7α,11β-dimethyl-17β-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their ...
03/27/2007
6780854Orally active androgens
Novel, orally active androgens are 7α-substituted Δ14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1...
08/24/2004
6756366Orally active androgens
Orally Active androgens are derivative of 7α-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the gro...
06/29/2004
6541465Orally active androgens
Novel, orally active androgens are 7଱-substituted Ɗ14 -nandrolone derivatives. The compounds satisfy the general formula: ##STR1## wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C...
04/01/2003
6406718Orthorhombic crystalline form of fluticasone propionate and pharmaceutical compositions thereof
The invention relates to a new polymorphic crystalline form of S-fluoromethyl 6଱,9଱-difluoro-11ଲ-hydroxy-16଱-methyl-3-oxo-17.alph a.-propionyloxyandrosta-1,4-diene-17ଲ-carbothiate (fluticasone propionate). The new polymor...
06/18/2002
5977096Steroids 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 of diseases due to radical-mediated cell damage. The novel...
11/02/1999
5952319Androgenic steroid compounds and a method of making and using the same
An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R1, R2, R3, R5 and R6 are as defined herein....
09/14/1999
5925630Neuroactive steroids of the androstane and pregnane series
The invention relates to 3଱-hydroxy, 17-(un)substituted derivatives of the androstane series and 3଱-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, t...
07/20/1999
58665586-alkynyl steroids
Compounds of formula I: ##STR1## wherein R, R1, R2, R3, and R4 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of aromatase, and are useful f...
02/02/1999
5723455Antiandrogenic agents and related pharmaceutical compositions and methods of use
Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R1 through R10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compo...
03/03/1998
5438134Process for the production of unsaturated 17 ଱-cyanomethyl-17 ଲ- h
The unsaturated 17଱-cyanomethyl-17ଲ-hydroxy steroids of the formula I, ##STR1## in which R1 =Me, Eth; R2 =H, Me; R3 =H, OH, an acetoxy or alkoxy group; R4 =H, R5 =OH, an acetoxy, alko...
08/01/1995
5081113Novel 3-keto-steroids
A compound selected from the group consisting of a compound of the formula ##STR1## wherein R6 is selected from the group consisting of halogen, --CH3, fluorine and chlorine, R9 and R11 together form a seco...
01/14/1992
5068368Stabilized lithium acetylide and reactions therewith
A process for the preparation of ethynyl carbinols of the formula: ##STR1## wherein R" is hydrogen, a substituted or unsubstituted aliphatic or aromatic hydrocarbon, R'" is a substituted or unsubstituted aliphatic or aromatic hydrocarbon or R" and R'...
11/26/1991
4945064Estrane 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 methylene, Z represents two hydrogen atoms, oxo or alkylenediox...
07/31/1990
4885117Process for the preparation of (Z)-17଱-halovinyl steroids
(Z)-17଱-halovinyl steroids of general Formula I ##STR1## wherein . . . . is a single bond or a double bond, V is a carbon-to-carbon bond or a methylene group, R1 is a hydrogen atom or a methyl group, X is a chlorine atom, a bromine atom or an ...
12/05/1989
470882317 ଱-chloroethynyl pregnane derivatives
Known pregnane derivatives are prepared by esterificiation of known androstane derivatives to give new ester of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond, n is 1 or 2, R1 is hydrogen or methyl, R
11/24/1987
4618456Ethynylation of 16-methyl-17-keto steroids
The process of the present invention transforms 16଱- or 16ଲ-methyl-17-keto steroids (I) to the corresponding 17଱-ethynyl-17ଲ-hydroxy-16଱- or 16ଲ-methyl steroids (II) without epimerization and loss of stereochemistry of ...
10/21/1986
4600538Corticosteroids from 17-keto steroids via 20-cyano-Ɗ17 (20)-pregnanes
The process of the present invention transforms 17-keto steroids (I) to the corresponding corticoids (IV) in three steps....
07/15/1986
4587235Novel androstane derivatives, process for their production, and pharmaceutical preparations containing them
Androstane derivatives of Formula I ##STR1## wherein is a single bond or a double bond, R1 is methyl or ethyl, R2 is hydrogen or alkyl of 1-8 carbon atoms, --X-- is --(CH2)n --, --CH.dbd.CH(CH2)m
05/06/1986
458559117ଲ-ethynylsteroids and process for preparing same
This is disclosed novel intermediates, i.e. 17ଲ-ethynylsteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for preparing the same....
04/29/1986
4567002Process for the preparation of 17-haloethynyl steroids, and novel 17-haloethynyl steroids
17-haloethynyl steroids of the partial formula ##STR1## wherein R1 is hydrogen or methyl, R2 is alkyl of 1-4 carbon atoms, acyl of 1-7 carbon atoms, trimethylsilyl, 2-tetrahydropyranyl, or nitrate, X is bromine or iodine, and V is me...
01/28/1986
454212817଱-Pregn-4-ene-3-oxo-21-carboxylic acid esters, process for the preparation thereof, and use thereof as medicinal agents
17଱-Pregn-4-ene-3-oxo-21-carboxylic acid esters of Formula I ##STR1## wherein C1 C2 is a CC single or C.dbd.C double bond, --A--B--is ##STR2## --C--D--is ##STR3## and R is an alkyl or alkenyl residue of up t...
09/17/1985
4526720Process 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 steroids producing the useful 17଱-ethynyl-17ଲ-h...
07/02/1985
4507238Process for the preparation of 3-(Ɗ4 -3-ketosteroid-17଱-yl)propionic acid lactones
A simple process for preparing 3-(Ɗ4 -3-keto-steroid-17଱-yl)propionic acid lactones of the androstane series represented by the general partial formula ##STR1## wherein ABCD represents an optionally substituted cyclopentanophenanthr...
03/26/1985
4502989Aldosterone-antagonistic steroids
Novel spironolactone derivatives characterized by the C11 -C12 double bond which have a potent aldosterone-antagonistic activity without causing potassium loss, used alone in diagnosis and improvement of condition of primary aldoster...
03/05/1985
4482494Process for preparing 17଱-hydroxy-pregn-4-en-3,20-dione
The invention relates to a novel process for the preparations of pregnane derivatives of formula I, ##STR1## wherein R1 stands for a methyl or an ethyl group, R2 represents a hydrogen atom or a methyl group, and X is a hydrogen atom ...
11/13/1984
4474701Process for the separation of 4-androsten-3,17-dione and 1,4-androstadien-3,17-dione
A process is disclosed for the separation of 4-androsten-3,17-dione/1,4-androstadien-3,17-dione mixtures, which are produced, e.g., upon microbiological sterol-side chain decomposition, through conversion of said mixture into a mixture of 17ଲ-c...
10/02/1984
4457925Androstane derivatives, process for their production, and pharmaceutical preparations containing them
Androstane derivatives of Formula I ##STR1## wherein ---- is a single bond or a double bond, R1 is methyl or ethyl, R2 is hydrogen or alkyl of 1-8 carbon atoms, --X-- is --(CH2)n --, --CH.dbd.CH(CH2)m...
07/03/1984
4452994Process for isolating organic compounds and lithium salt complexes useful in said process
An improved process for isolating organic compounds from crude product or reaction mixtures by dissolving said crude product or reaction mixture in a suitable solvent, contacting the resulting solution with a lithium salt to form a solid metal salt comple...
06/05/1984
4440684Process for the preparation of 6-methyl-Ɗ4,6 -3-keto steroids
A process for preparing 6-methyl-Ɗ4,6 -3-keto steroids of the formula ##STR1## comprises reacting a corresponding Ɗ4 -3-keto steroid with methoxymethyl acetate (CH3 --O--CH2 --OAc) in an inert solvent ...
04/03/1984
4440689Acyloxysteroids and process for producing same
There is disclosed novel intermediates, i.e. acyloxysteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for producing the same....
04/03/1984
4383947Introduction of a fluorine atom
Perchloryl fluoride when reacted with the appropriately protected 9଱-hydroxyandrostenedione stereoselectively produces the corresponding 6ଲ-fluoro steroid....
05/17/1983
4368160Process for preparing 17଱-hydroxy-pregn-4-en-3,20-dione derivatives
The invention relates to a novel process for the preparation of pregnane derivatives of formula I, ##STR1## wherein R1 stands for a methyl or an ethyl group, R2 represents a hydrogen atom or a methyl group, and X is a hydrogen atom o...
01/11/1983
4360663Steroid hormone-antitumor derivatives
A process for producing a steroid hormone-antitumor derivative which selectively affects to tumor or cancer cells comprises reacting X group of a steroid hormone derivative having the formula ##STR1## wherein ST represents a steroid moiety having a c...
11/23/1982
4357279Preparation of corticoids from 17-keto steroids
A process for the preparation of corticoids (XI) which comprises reacting a protected 17-keto steroid (II) with a metallated 1,2-dihaloethene (III)....
11/02/1982
4346037Base 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 including hydroxy steroids....
08/24/1982
4342702Metallated halogenated acetylene corticoid synthesis
A process for the preparation of corticoids (IX) which comprises reacting a 17-keto steroid (I) with a metallated halogenated acetylene (II) followed by reaction with a sulfenylating agent (IV) and C17 side chain rearrangement....
08/03/1982
4323511Steroid derivatives and their use in radioimmunoassays
Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a 6-dehydro derivative of a 3-oxo-4,5-dehydro steroid intended for radioimmunoassay, said steroid being saturated in the 1,2-position; R is hydrogen or alkyl of 1 to 3 carbon ...
04/06/1982
4297350Male contraceptive steroids and methods of use
The steroids of the present invention have been found to be useful as male contraceptives when administered orally. Upon cessation of administration of the male contraceptive steroids of the present invention the male promptly regains normal fertility....
10/27/1981
4272445Process for preparing active compounds
A process for the preparation of a compound of the formula (A): ##STR1## wherein: R3 is a C1-5 alkyl group, a C3-6 alkenyl group, a C3-6 cycloalkyl group or an alkylphenyl group in which the alkyl moiety co...
06/09/1981
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