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Class 552/632 - 19-position substituted (e.g., 19-methylene-androstanes, 10-cyanoestranes, 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: 38
Last issue date: 03/27/2007


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
6437158Testosterone derivative
The invention is drawn to (7a, 17b)-7-methyl-17-(1-oxoundecyl)oxy-estr-4-en-3-one, (MENT undecanoate), their pharmaceutical formulation and method of use is described. Unexpected results of the said compound compared with testosterone undecanoate is ...
08/20/2002
6433200Intermediates for preparation of 16-ene-vitamin D derivatives
Intermediates for the preparation of a vitamin D derivative have the following formulas: ##STR1## wherein R9 and R10 may be the same or different and each represents a hydrogen atom or a protecting group, and in Formula (5) the ...
08/13/2002
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
632650316-ENE-vitamin D derivatives
A compound having the formula (4): wherein ##STR1## X is oxygen or sulfur, R9 and R10 are each a hydrogen or a protecting group, and R11 is an aliphatic hydrocarbon, a --COR12 group where R12 is alkyl...
12/04/2001
5981517Androstene derivatives
The invention provides new androstene derivatives having anti-inflammatory activity, pharmaceutical compositions containing them, and methods of administering them to warm-blooded animals in the treatment of inflammation. The active compounds are alkyl ...
11/09/1999
5969168Androstanes for inducing hypothalamic effects
The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypo...
10/19/1999
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
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
5516922Process for the preparation of 10(2-propynyl)estr-4-ene-3,17-dione
This invention relates to a process for the preparation of 10-(2-propynyl)-estr-4-ene-3,17-dione, whereby this compound is synthesized utilizing ketals prepared from the addition of 2,2-dimethyl-1,3-propanediol to the starting compound, 19-norandrost...
05/14/1996
5252565Haloethyl-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 biosynthesis inhibitors and they are prepared from the correspo...
10/12/1993
5086047Novel 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 atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, option...
02/04/1992
5081114Steroids
A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, ##STR2## alkyl and alkoxy of 1 to 12 carbon atoms, aryl and aryloxy of 6 to 12 carbon atoms and aralkyl and aralkoxy of 7 to 12 carbon atoms, R1...
01/14/1992
5030627Ɗ4 -19-sulfur substituted-androstene derivatives having aromatase-inhibiting activity
The invention relates to Ɗ4 -androstene derivatives with aromatase-inhibiting activity having the formula: ##STR1## wherein R1 =O, (଱R5,ଲH) or N--O--R6 ; R2 =H, (1-12C)hydrocarbon radical...
07/09/1991
49258343-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 Ra represents a hydrogen atom or a saturated or unsaturated straight-chain or branched-chain, optionally substituted alkyl radical with 1-6 carbon atoms, in which Ra...
05/15/1990
48085786-Alkylidene 10 ଲ-alkynylestrene derivatives and pharmaceutical methods for their use
The invention relates to 6-substituted 10ଲ-alkynylestrene derivatives wherein the 6 substituent is amino, azido, halogen or an alkylidene group and to corresponding 6,7-dihalo analogs. The invention provides also a process for the preparation of the abov...
02/28/1989
4753932Novel 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 bond or --S-- and R is optionally substituted carbocyc...
06/28/1988
4745109Suicide inhibitors of aromatase
Thiol-substituted synthetic steriod hormones or androgens having a testosterone ring system backbone are used to inhibit aromatase's catalyzed conversion of C19 androgens having a A4,3-ketone group to estrogens in the treatment of es...
05/17/1988
4701449Novel 10-substituted steroids and their use in the induction of aldosterone antagonistic activity
Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atom...
10/20/1987
4634694Novel Ɗ4 - and Ɗ5 -androstene derivatives and pharmaceutical compositions containing these derivatives
The invention relates to novel steroids having the formula: ##STR1## wherein X=CH2 --S--R3 or S--S--R4 ; R1 =O or H (ଲR5); R2 =O or H (ଲR6); R3 =H, acyl (1-18C)...
01/06/1987
4495102Aminoalkyl steroids
Compounds of Formula I and II are useful as potent antiarrythmic agents without significant effect on cardiac output and blood pressure....
01/22/1985
447356419-Thio-androstane derivatives
The invention relates to novel 19-thio-androstane derivatives having the general formula: ##STR1## and the 4,5-dihydro analogues thereof, wherein R1 =H, hydrocarbyl(1-4C), aralkyl(7-9C), aryl(6-9C) or acyl derived from an organic carb...
09/25/1984
432241610-Alkynyl steroids
Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C1-4 alkyl; R1 is methyl or ethyl; R2 is (H) (OR8) or .dbd.O; R3 is ...
03/30/1982
428976210-(1,2-Propadienyl) steroids as irreversible aromatase inhibitors
Irreversible aromatase inhibitors are provided having the formulae ##STR1## wherein represents a single or a double bond; R1 is CH3 or C2 H5 ; R2 is (H) (OR8) or O; R3 is H or ...
09/15/1981
4239681Androst-4-en-19-ols
Derivatives of androst-4-en-19-ol are useful for enhancing libido and related psychic attitudes....
12/16/1980
4197286Testosterone derivatives and assay method
An anti-testosterone serum is provided which is highly selective to the measurement of testosterone using radioimmunossay techniques in both male and female plasma without resorting to chromatography even though the plasma may have a high 5଱-dihydro...
04/08/1980
4150127Novel 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 R3 is a lower alkyl radical carrying an oxygen-containing functional group and R4 is two hydrogen atoms or an oxo group, and which carry a ...
04/17/1979
413961719-Oxygenated-androst-5-enes for the enhancement of libido
The present invention concerns derivatives of 19-oxygenated-androst-5-enes which are useful in the enhancement of libido and related psychic attitudes....
02/13/1979
409614214,19-Dioxygenated steroid compounds and their 14-dehydro analogs and process for the preparation thereof
There are provided novel 14,19-dioxygenated steroid compounds and their 14-dehydro analogs, as well as processes for preparing such compounds. The above compounds are useful as intermediates in the preparation of other steroids, which in turn, may be conv...
06/20/1978
407162519-Oxygenated-5଱-androstanes for the enhancement of libido
Derivatives of 19-oxygenated-5଱-androstanes are described which are useful in enhancing the libido and related psychic attitudes in mammals....
01/31/1978
4071624Androst-4-en-19-ones for the enhancement of libido
The present invention concerns androst-4-en-19-ones which are useful in the enhancement of libido and related pyschic attitudes....
01/31/1978
40585394,6,8(14)-Triene steroids
There are provided novel 4,6,8(14)-triene-steroids as well as processes for preparing such compounds. The above compounds are useful as intermediates in the preparation of other steroids, which in turn, may be converted into valuable pharmaceutical agents...
11/15/1977
4054651Method of contraception
A method of contraception which comprises administering a compound of the following general formula: ##STR1## wherein R is --CHO or --CH2 OR1 ; each of R1 and R2 is hydrogen, alkylcarbonyl wherein the alkyl...
10/18/1977
405242113-Ethinyl-steroids and processes for their manufacture
A new class of 13-ethinyl-steroids is prepared by a novel process comprising Wittig reaction of a 13-formyl steroid with a chloro- or bromomethylenephosphorane and dehydrohalogenation of the intermediate 13-(2-halogenovinyl)steroid with an extremely stron...
10/04/1977
4022769Androst-4-en-19-ones
The present invention concerns derivatives of androst-4-en-19-one which are useful in the enhancement of libido and related psychic attitudes....
05/10/1977
 
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