Abstract: 17.alpha.-Acyloxy-5.beta.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
Abstract: 17.alpha.-Hydroxy-6,16-dimethylenepregn-4-ene-3,20-dione simultaneously isomerized and acylated to 17.alpha.-hydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dione 17-acetate.
Abstract: Estrogenic cyclopropyl analogs, when administered to a female subject, function as anti-fertility agents to prevent pregnancy in the subject. Further, the estrogenic cyclopropyl analogs may be used as estrogenic agents to produce an estrogenic response in a female subject. The estrogenic cyclopropyl analogs useful as estrogenic agents have the general structure: ##STR1## wherein: X is a halogen or hydrogen atom:R.sub.1 is a hydrogen atom, an alkyl group containing from 1 to about 3 carbon atoms, a monocyclic group, a hydroxy substituted monocyclic group, or an alkoxy substituted monocyclic group in which the alkyl substitutent contains from 1 to about 3 carbon atoms;R.sub.2 is a hydrogen atom, an acetate group, a hydroxyl group, an alkoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-dialkylaminoethoxy group in which the alkyl substituent contains from 1 to about 3 carbon atoms, a beta-monoaminoheterocycloethoxy group, or pharmaceutically acceptable salts thereof;R.sub.
Type:
Grant
Filed:
July 26, 1982
Date of Patent:
April 10, 1984
Assignee:
The Board of Regents for the University of Oklahoma
Abstract: Complexes of albumin combined with organic dibasic acid half esters, such as those of succinic acid and phthalic acid, of 7-hydroxycholesterol are soluble in water and have excellent immunosuppressive and anti-inflammatory action.
Abstract: Pharmaceutical composition in dosage unit form, comprising a therapeutically effective amount of 24,25-dihydroxycholecalciferol and a pharmaceutically acceptable carrier. The compound of 24,25-dihydroxycholecalciferol has anti-hypercalcemic activity, anti-ulcer activity, activity of preventing reduction of immunity, activity of controlling magnesium-metabolism, anti-hyperphosphatemic activity, activity of controlling blood sugar level and anti-tumor activity.
Abstract: Acyclic amines are used to transform 9.alpha.-substituted-11.beta.-hydroxy 21-acyloxy steroids to the corresponding 9.beta.,11.beta.-epoxy 21-acyloxy steroids without removal of the C.sub.17 or C.sub.21 ester. The acyclic amines are cheaper and easier to prepare than previously disclosed dehydrohalogenating agents which do not produce cleavage of the C.sub.21 ester.
Abstract: 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.
Abstract: A process for preparing 6-methyl-.DELTA..sup.4,6 -3-keto steroids of the formula ##STR1## comprises reacting a corresponding .DELTA..sup.4 -3-keto steroid with methoxymethyl acetate (CH.sub.3 --O--CH.sub.2 --OAc) in an inert solvent at temperatures above room temperature in the presence of an alkali metal acetate.
Type:
Grant
Filed:
February 4, 1983
Date of Patent:
April 3, 1984
Assignee:
Schering Aktiengesellschaft
Inventors:
Klaus Annen, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
Abstract: Novel compounds which are 7-acylderivatives of ursodeoxycholic acid are described of formula ##STR1## in which R-CO is the residue from a linear, saturated or unsaturated, carboxylic acid of 2-18 carbon atoms or the residue from a cycloalkanecarboxylic acid of 3-7 carbon atoms in the cycloalkane ring. The novel compounds are useful in the therapy of biliary calculosis, biliary diskinesia and hypertriglyceridemia.
Type:
Grant
Filed:
June 28, 1982
Date of Patent:
April 3, 1984
Inventors:
Carlo Scolastico, Cesare Sirtori, David Kritchevsky
Abstract: Water-soluble esters of steroid-oxazole derivatives of formula I ##STR1## wherein R is O or a H, (.beta.-OH) group, R.sub.1 is hydrogen, lower alkyl or phenyl, X is hydrogen, fluorine or chlorine, A stands for a direct carbon-carbon bond or a hydrocarbon chain containing from 1 to 4 carbon atoms, and M is hydrogen or a pharmaceutically acceptable cation are described as well as pharmaceutical compositions containing them particularly suitable for parenteral administration.
Type:
Grant
Filed:
April 27, 1981
Date of Patent:
April 3, 1984
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Giangiacomo Nathansohn, Giorgio Winters
Abstract: Disclosed is an improved process for the synthesis of 6-bromo-17,21-dihydroxy-3,11,20-trioxo-1,4,-pregnadienes 17,21-diesters. In particular, this invention relates to the conversion of 17,21-dihydroxy-3,11,20-trioxo-1,4-pregnadienes 17,21-diesters to 6-borom-17,21-dihyroxy-3,11,20-trioxo-1,4-pregnadienes-17-21-diesters via bromination under ionic conditions, e.g. bromine in acetic acid.
Type:
Grant
Filed:
December 27, 1982
Date of Patent:
April 3, 1984
Assignee:
Schering Corporation
Inventors:
Elliot L. Shapiro, Lawrence E. Finkenor
Abstract: This invention relates to the composition of a biologically compatible high concentration solution of progesterone, which is stable and non-toxic, and which can be used transdermally, orally, and in suppository and pessary form for the correction of progesterone deficiency states and other diseases.
Abstract: Novel compounds are described, which are 7-acyl-chenodeoxycholic acid of formula (I) ##STR1## in which R-CO is the residue from a linear, saturated or unsaturated carboxylic acid of 3-18 carbon atoms or the residue from a cycloalkanecarboxylic acid of 3-7 carbon atoms in the cycloalkane ring. The compounds are prepared by selective hydrolysis of the 3,7-diacyl derivatives of chenodeoxycholic acid. The compounds are valuable against biliary calculosis, diskinesia and hypertriglyceridemia.
Type:
Grant
Filed:
June 28, 1982
Date of Patent:
March 27, 1984
Inventors:
Carlo Scolastico, Cesare Sirtori, David Kritchevsky
Abstract: New steroidal chiral phosphines of formula ##STR1## wherein R represents a phosphorated group selected between ##STR2## methods for their preparation; catalytic systems comprising metal complexes and the above steroidal chiral phosphines; asymmetrical catalytic processes like hydrogenation, hydroformylation and hydrocarbalkoxylation of prochiral compounds which employ said catalytic systems.
Type:
Grant
Filed:
November 18, 1982
Date of Patent:
March 20, 1984
Assignee:
Consiglio Nazionale Delle Ricerche
Inventors:
Carlo Botteghi, Serafino G. Gladiali, Mauro Marchetti, Giovanni A. Faedda
Abstract: An agent for treating diseases in circulatory organs which comprises a piperazine compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are as defined hereunder, or a salt thereof and a pharmaceutically acceptable carrier.
Abstract: Loss of potency of estradiol cream compositions found to be due to unexpected oxidation of estradiol. Improved cream composition comprises 1% or less 17.beta.-estradiol in the presence of stabilizing members selected from phenolic-type antioxidants, metal chelating agents, and suspending agents.
Type:
Grant
Filed:
March 15, 1982
Date of Patent:
March 13, 1984
Assignee:
Mead Johnson & Company
Inventors:
Robert J. Bequette, Linda G. Hobbs, Joseph A. Scott
Abstract: A process for the preparation of 3.beta.,7.beta.,15.alpha.-trihydroxy-5-androsten-17-one and the 3,15-dipivalate thereof comprises epimerizing 3.beta.,7.alpha.,15.alpha.-trihydroxy-5-androsten-17-one in the presence of a ketone with or without a solvent, with dilute mineral acid and subsequent treatment with an organic base, and optionally subsequently esterifying the 3.beta.- and 15.alpha.-positions of the resultant 3.beta.,7.beta.,15.alpha.-triol with a reactive derivative of pivalic acid.
Type:
Grant
Filed:
September 21, 1982
Date of Patent:
March 6, 1984
Assignee:
Schering, Aktiengesellschaft
Inventors:
Karl Petzoldt, Henry Laurent, Rudolf Wiechert
Abstract: Androstenes having the formula ##STR1## wherein R.sub.1 hydrogen and R.sub.2 is alkyl, cycloalkyl, aryl, arylalkyl, alkylthioalkyl, alkoxyalkyl, alkanoyloxyalkyl, aroyloxyalkyl, alkoxycarobnylalkyl, carboxyalkyl, or arylalkyl, or R.sub.1 is alkanoyl or aroyl and R.sub.2 is alkyl;R.sub.3 is hydrogen, hydroxy, alkoxy, aryloxy, oxo, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or halogen;R.sub.4 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.5 is hydrogen or halogen; and R.sub.6 is hydrogen, methyl, hydroxy, alkanoyl or halogen are useful intermediates for the preparation of steroids having antiinflammatory activity.