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Class 552/595 - Unsaturation between the 4- and 5-positions (e.g., 17-alpha-hydroxy progesterones, etc.)


Subclass of Class 552 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain a double bond between the 4- and
No. of patents: 97
Last issue date: 05/22/2012


1      
NumberTitleIssue Date
8183402Industrial method for the synthesis of 17-acetoxy-11β[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
The present invention relates to a process for the synthesis of the 17-acetoxy-11β-[4-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione of formula (I): from 3,3-[1,2-etandiyl-bis(oxy)]-oestr-5(10),9(11)-d...
05/22/2012
8044223Crystalline 19-norsteroids
The present invention are two crystalline salts, 17α-acetoxy-21-methoxy-11β-(4-,N,N-dimethylaminophenyl)-19 norpregna-4,9-diene-3,20-dione hydrochloride and 17α-acetoxy-21-methoxy-11β-(4-,N,N-dimethylaminophenyl)-19 norpregna-4,9-diene-3,20-dione hydrobromide, o...
10/25/2011
7235655Processes to prepare eplerenone
The present invention involves intermediates, including a 7α-substituted steroid (II), and processes which are used to prepare eplerenone, a useful pharmaceutical agent. ...
06/26/2007
708759121-substituted progesterone derivatives as new antiprogestational agents
A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —C...
08/08/2006
6900193Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)...
05/31/2005
686141521-substituted progesterone derivatives as new antiprogestational agents
A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, â€...
03/01/2005
6768014PROCESS FOR PREPARING 17α-ACETOXY-11β-[4-N,N(DIMETHYLAMINO)PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES USEFUL IN THE PROCESS , AND PROCESSES FOR PREPARING SUCH INTERMEDIATES
A compound having general formula (I) in which R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R
07/27/2004
6365582S-substitute 11ଲ-benzaldoxime-estra-4, 9-diene-carbonic acid thiolesters, method for the production thereof and pharmaceutical preparations containing these compounds
Thiol esters of S-substituted 11ଲ-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula I ##STR1## their pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical preparations containing these compounds are described. ...
04/02/2002
6037339C-11 substituted steroids for treating menopausal complaints
A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis....
03/14/2000
5723638Process for 20-oxo-17଱,21-diol steroids
The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R1 is hydrogen or alkyl of 1 to 4 carbon atoms, R2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at ...
03/03/1998
5710144C-11 substituted steroids for treating menopausal complaints
A C-11 substituted steroid and a method of use of a C-11 substituted steroid to treat osteoporosis....
01/20/1998
5710293Method of preparation of ester derivatives of steroids
The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17଱-hydroxy-19-norpregn-4-ene-3,20-dione....
01/20/1998
5616742Process for preparing ÆŠ9,11 and 21-chloro corticosteroids
Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl5, PCl3, POCl3 or either SO2 Cl2 and imidazole, or PPh3 and CCl4. The disclosed process ...
04/01/1997
5608093Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds
Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH3 ; R(1) is aryl or heta...
03/04/1997
5502222Process for preparing delta 9,11 and 21-chloro corticosteroids
Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl5, PCl3, POCl3 or either SO.sub. Cl2 and imidazole, or PPh3 and CCl4. The disclosed process selecti...
03/26/1996
544603613-alkyl-11beta-phenylgonanes
There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH; R2 is alpha- or beta-position methyl or ethyl; R1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl r...
08/29/1995
541209116-methyl-ÆŠ1,4-pregnadiene-3,20-dione
A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-ÆŠ4-system or a 3-keto -ÆŠ1,4-system or a 3-OR4 - ÆŠ5-system in which R4 is hydrogen or a protector group of hydroxy, R is methyl --CH2...
05/02/1995
5352808Process for steroid preparation
A process for the preparation of a compound of the formula ##STR1## wherein R1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl a...
10/04/1994
527397113-alkyl-11ଲ-phenylgonanes
There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH; R2 is alpha- or beta-position methyl or ethyl; R1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl r...
12/28/1993
4956482Process for the preparation of pregnane derivatives
Known pregnane derivatives are prepared by esterification of know androstane derivatives to give new esters 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, R2...
09/11/1990
494853311a-hydroxy steroid diester
The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17଱-hydroxy-11଱-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs....
08/14/1990
493333211-desoxy-17-଱-hydroxycorticosterone derivatives
11-Desoxy-17଱-hydroxycorticosterone derivatives of the general formula: ##STR1## wherein R is --OC(CH2)n C6 H4 N(CH2 CH2 Cl)2, n=1,3....
06/12/1990
492939516଱-methylation process
C16 -unsaturated corticoids are readily transformed to the corresponding 16଱-methyl-17଱-hydroxy corticoids by use of a ÆŠ17 (20)-20-silyl ether....
05/29/1990
492163817ଲ-cyano-9଱,17଱-dihydroxyandrost-4-en-3-one
The invention is the compound 17ଲ-cyano-9଱, 17଱-dihydroxyandrost-4-en-3-one (I) which is particularly useful as an intermediate in the production of the 17଱-halo silyl ethers (II)....
05/01/1990
4920216Selective chlorination of steroids and other substrates directed by covalently linked pyridine derivatives acting as templates
This invention concerns a method of substituting a chlorine atom for a predetermined hydrogen atom located within an organic compound which comprises contacting the organic compound containing the predetermined hydrogen atom with an esterifying agent comp...
04/24/1990
4913852Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives
Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of ÆŠ-4-pregnene-3,20-dione or with derivatives of ÆŠ-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucoco...
04/03/1990
487006911ଲ-alkynyl-estrenes and -estradienes, their production and pharmaceutical preparations containing them
11ଲ-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 atoms or hydroximino; Z is the residue of a pentagonal ...
09/26/1989
483113111ଲ,17଱-Dihydroxy-17ଲ-cyano-androstanes
Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17଱-acyl progesterones....
05/16/1989
481070111-desoxy-17଱-hydroxycorticosterone derivatives
11-Desoxy-17଱-hydroxycorticosterone derivatives of the general formula: ##STR1## wherein R is --OC(CH2)n C6 H4 N(CH2 CH2 Cl)2, n=1,3....
03/07/1989
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
470445516଱-methylatedÆŠ17(20)-corticoids
C16 -unsaturated corticoids are readily transformed to the corresponding 16଱-methyl-17଱-hydroxy corticoids by use of a ÆŠ17 (20)-20-silyl ether....
11/03/1987
4655971Novel process for the preparation of steroidal esters
A process for the preparation of corticosteriod esters of the formula ##STR1## in which ---- signifies that a double bond can be present; X is hydrogen, chlorine or fluorine; R1 is hydrogen, fluorine, chlorine or methyl, which may be either &#x...
04/07/1987
4634695Steroid derivatives
Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the...
01/06/1987
4613463Process and intermediates for the preparation of 17 alphahydroxyprogesterones and corticoids from an enol steroid
This invention discloses an improved process for the production of corticoids from 17଱-hydroxy steroids utilizing peroxymonosulfate....
09/23/1986
4600538Corticosteroids from 17-keto steroids via 20-cyano-ÆŠ17 (20)-pregnanes
The process of the present invention transforms 17-keto steroids (I) to the corresponding corticoids (IV) in three steps....
07/15/1986
4588718Carboxy containing ester prodrugs of corticosteroids
A compound of the formula ##STR1## wherein St represents a corticosteroid moiety bonded to the carbonyl via the 21-hydroxy group of said corticosteroid; wherein Z is a bond or --O--; wherein n is an integer from 4 to 9; wherein Q is (1) Y--CH2 ...
05/13/1986
4588530Anti-inflammatory prednisolone steroids
Derivatives of prednisolone of the formula ##STR1## wherein CR1 is C.dbd.O, ଱-HCOH, ଲ-HCOH, or a mixture of ଱-HCOH and ଲ-HCOH CR2 is HC(OH) OR6 or HCO when CR1 is C.dbd.O; CR2
05/13/1986
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
4568492ÆŠ16-20-Keto steroid conversion to 17଱-hydroxy-20-keto steroids
ÆŠ16-20-keto steroids (I) are converted to 17଱-hydroxy-20-keto steroids (III) in 2 steps, hydrosilylation followed by peracid oxidation....
02/04/1986
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
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