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Class 552/613 - Oxygen bonded directly at the 1-position


Subclass of Class 552 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein oxygen is bonded directly at the 1-position
No. of patents: 34
Last issue date: 11/27/2007


NumberTitleIssue Date
7300926Steroidal quinols and their use for estrogen replacement therapy
The present invention relates to novel estrogen-related steroidal quinols and their use as drugs for estrogen replacement therapy. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved distribution ...
11/27/2007
7026306Steroidal quinols and their use for antioxidant therapy
The present invention relates to novel estrogen-related steroidal quinols and their use as prodrugs for phenolic estrogens and estrogen analogs. The quinols of the present invention provide improved physicochemical properties, increased bioavailability, and improved...
04/11/2006
695832718 Norsteroids as selectively active estrogens
The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11′, R14, R15, R
10/25/2005
6689768Pharmaceutical preparations for treating side effects during and/or after GnRHa therapy
The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount ...
02/10/2004
6436917Non-estrogenic estradiol derivative compounds with anti-oxidative activity
New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, esp...
08/20/2002
5892069Estrogenic compounds as anti-mitotic agents
The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found belo...
04/06/1999
5633393Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting compositon containing the conjugate or estradiol derivative.
Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30° to 150° C. for 3 minutes to 48 hours and then reco...
05/27/1997
5621124Process for the alkylation of estrone derivatives
The invention relates to a process for the alkylation of estrone derivatives, which is characterized in that a suspension of the estrone derivatives in dimethylformamide is produced and carbonic acid diester and guanidine and/or alkyl guanidines are disso...
04/15/1997
5561125Estradiol derivative and growth inhibiting composition thereof
Estradiol derivatives of the formula: ##STR1## wherein R1 is C1-4 alky or C1-4 alkoxy; R2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as t...
10/01/1996
5491138Estradiol derivative alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting composition containing the conjugate or estradiol derivative
Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or ...
02/13/1996
5480878Method for treating prostatic hypertrophy with estradiol derivatives
Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or benzyl; ...
01/02/1996
5478818Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting composition containing the conjugate or estradiol derivative
Disclosed is an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of...
12/26/1995
5354745Estradiol derivative-chlorambucil conjugate process for preparing the same, and pharmaceutical composition
An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R2 is acyl, dansyl, or alkyl; R3, R4, and R5 independently are H, ...
10/11/1994
52507121ଲ,15଱-di hydroxy-1଱-methyl-5଱-androstane-3,17-dione, its production and use
The invention relates to the 1ଲ, 15଱-dihydroxy-1଱-methyl-5଱-androstane-3,17-dione of formula I ##STR1## and preparation thereof using microorganisms of the genera Glomerella or Fusarium. The invention also relates to furt...
10/05/1993
4954446Aromatic steroid 5-଱-reductase inhibitors
Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-଱-reductase including using these compounds to reduce prosta...
09/04/1990
489869417-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....
02/06/1990
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
4725426Estrogenic 17଱-halogen-vinylestranes
17଱-bromo-଱ and 17଱-iodo-vinyl-estrane derivatives of general formula I ##STR1## wherein X is a bromine or iodine atom in Z or E position, R1 is hydrogen, hydroxy or acyloxy with up to 3 C atoms, R2 is hydrogen, alk...
02/16/1988
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
4599330Method 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 24,24-difluoro-1଱,25-dihydroxycholecalciferol....
07/08/1986
4421690Process for the preparation of 24,24-difluoro-1଱,25-dihydroxy vitamin D3 and intermediates obtained therefrom
The present invention relates to a process and intermediates for the preparation of 24,24-difluoro-1଱,25-dihydroxycholecalciferol from the readily-available 1଱,3ଲ-dihydroxyandrost-5-en-17-one which is made by a known microbiological proc...
12/20/1983
44077538଱-Oestra-1,3,5(10)-triene derivatives, processes for their preparation and pharmaceutical compositions
The invention relates to new 8଱-oestra-1,3,5(10)-triene derivatives having the formula: ##STR1## in which R1 =H or a free, esterified or etherified hydroxy group; R2 =H or a free, esterified or etherified hydroxy group, with th...
10/04/1983
4397847Method of treatment
The present invention relates to a method of treating osteoporosis by administering to a host suffering from osteoporosis an effective amount of 24,24-difluoro-1଱,25-dihydroxycholecalciferol....
08/09/1983
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
43070881-Hydroxy steroids, a process for the production thereof, and pharmaceutical preparations containing them
1-Hydroxy steroids of formula I ##STR1## wherein R1 and R2 are independently hydrogen or alkanoyl of 1-8 carbon atoms are distinguished by strong progestational activity and only very minor androgenic side effects....
12/22/1981
4222940Cyclization substrates, cyclization process and related 11ଲ-axially-substituted steroids
There are disclosed substrates of the formula: ##STR1## wherein: (a) R1 is H or C1 -C4 alkyl; (b) R2 is H or C1 -C4 alkyl with the proviso that R1 is H when R2 is alky...
09/16/1980
4177197Cyclization substrates and 7଱-substituted 19-norsteroid derivatives
Novel cyclization substrates are disclosed of the formula ##STR1## wherein: (a) R1 is H or alkyl of one to four carbon atoms; (b) R2 is H or alkyl of one to four carbon atoms, with the proviso that R1 is H when R2
12/04/1979
4144334Novel ଱-hydroxy steroids
1଱-Oxysteroid of the formula ##STR1## wherein R1 is methyl or ethyl, R2 and R3 each are hydrogen or alkanoyl of 1-8 carbon atoms, and R4 is hydrogen or hydrocarbon of 1-4 carbon atoms, Are progestestionally act...
03/13/1979
40962531-Oxygenated steroids
1-Oxygenated steroids and a method of preparing same as described. The 1-oxygenated steroids are useful as antifertility agents....
06/20/1978
4066674Process for the preparation of 1,3-oxygenated 8଱-estratrienes and novel intermediates obtained therefrom
Novel 1,3-dialkoxy 8଱-estratriene compounds of the formula ##STR1## WHEREIN R1 is alkyl of 1-18 carbon atoms, R2 is alkyl of 1-5 carbon atoms and Ac is alkanoyl of 1-8 carbon atoms, are obtained by a three-step synthesis f...
01/03/1978
40641739,10-Seco-steroids
A process for the preparation of 9,10-seco-steroids of the formula ##STR1## WHEREIN R1 and R2 independently are hydrogen, amino, OR5, OCOR6 or NHCOR5 wherein R5 is hydrogen or lower alkyl a...
12/20/1977
40297791଱-Hydroxy steroids
1଱-Oxysteroid of the formula ##STR1## wherein R1 is methyl or ethyl, R2 and R3 each are hydrogen or alkanoyl of 1-8 carbon atoms, and R4 is hydrogen or hydrocarbon of 1-4 carbon atoms, Are progestestionally act...
06/14/1977
4002746Synthesis of gon-4-enes
1. A therapeutic composition having progestational activity comprising as active ingredient a 17-aliphatic carboxylic acid ester of 17଱-ethynyl-18-methyl-19-nortestosterone and a pharmaceutical carrier for said compound....
01/11/1977
39519581,3-Oxygenated-8଱-estratrienes
1,3-Dihydroxy-8଱-estratrienes of the formula ##SPC1## Wherein R is lower-alkyl and --A--B is ##SPC2## Wherein R' is a saturated or unsaturated hydrocarbon group and R" is lower-alkyl, aralkyl or phenyl, and the esters and ethers thereof, possess ...
04/20/1976
 
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