Abstract: Derivatives of prednisolone of the formula ##STR1## wherein CR.sub.1 is C.dbd.O, .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH CR.sub.2 is HC(OH) OR.sub.6 or HCO when CR.sub.1 is C.dbd.O;CR.sub.2 is COOR.sub.3 or CONHR.sub.4 when CR.sub.1 is .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH:R.sub.3 is alkyl of 1-5 carbon atoms;R.sub.4 is alkyl of 1-5 carbon atoms, benzyl, or phenethyl;R.sub.5 is hydrogen, acetyl, or benzoyl;R.sub.6 is alkyl of 1-5 carbon atoms;R.sub.7 is .alpha.- or .beta.-position of hydrogen, hydroxyl, methyl, acetate esters of 1-5 carbon atoms, or alkoxy of 1-5 carbon atoms; andX and Y are hydrogen, halogen or methyl;and process for preparing these compounds. The compounds are useful as anti-inflammatory agents which have reduced side effects.
Type:
Grant
Filed:
June 9, 1983
Date of Patent:
May 13, 1986
Assignee:
Florida Agricultural and Mechanical University
Abstract: Androstane derivatives of Formula I ##STR1## wherein is a single bond or a double bond,R.sub.1 is methyl or ethyl,R.sub.2 is hydrogen or alkyl of 1-8 carbon atoms,--X-- is --(CH.sub.2).sub.n --, --CH.dbd.CH(CH.sub.2).sub.m --, or --C.tbd.C--(CH.sub.2).sub.m -- wherein n is 2 to 6 and m is 1 to 4,--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CCl.dbd.CH--, ##STR2## --U--V< is --CH.sub.2 --CH<, --CH.dbd.C<, --C(OH).dbd.C<, or --CCl.dbd.C<, and--W--Y-- is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --C(CH.sub.3).sub.2 --, or ##STR3## with the proviso that the compound is not 17.alpha.-(3-acetoxypropyl)-17.beta.-hydroxy-4,6-androstadien-3-one, are pharmacologically efficacious compounds, e.g., are sebum suppressive.
Type:
Grant
Filed:
June 27, 1984
Date of Patent:
May 6, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Wiechert
Abstract: 6.alpha.-Methylprednisolone derivatives of Formula I ##STR1## wherein R.sub.1 is 1-oxoalkyl of 2-6 carbon atoms or benzoyl andR.sub.2 is 1-oxoalkyl of 2-6 carbon atoms, are pharmacologically efficacious compounds, e.g., as antiinflammatories.
Type:
Grant
Filed:
October 27, 1983
Date of Patent:
May 6, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Klaus Annen, Karl Petzoldt, Henry Laurent, Rudolf Wiechert, Helmut Hofmeister
Abstract: This is disclosed novel intermediates, i.e. 17.beta.-ethynylsteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for preparing the same.
Abstract: Novel 6-oxygenated corticoid 17.alpha.-carbonates are disclosed. These compounds have strong topical anti-inflammatory activity which are accompanied by extremely weak systemic adverse reaction. The present compounds are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.
Abstract: 17.beta.-Hydroxy-17.alpha.-methyl-5.alpha.-androstano[3,2-c]pyrazole 17-methyl ether is a very potent reversible male contraceptive which has a very low degree of androgenic side effects. Upon cessation of administration fertility promptly returns.
Abstract: An Estracyt compound having a carcinostatic bound thereto is obtained by reacting an Estracyt compound with a carcinostatic having one or more radicals selected from among COOH, Cl, NH.sub.2 and OH, either directly or after reaction with an amine to replace one or both Cl groups in the nitrogen mustard portion in the Estracyt compound with a NH.sub.2 group, in the presence or absence of a catalyst. The resulting compound is more effective in cancer control than the Estracyt compound associated substance.
Abstract: Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-position. Preferred starting materials include estrones or derivatives thereof. The estrones are preferably reduced after masking and amination to form the corresponding estradiols, which are then halogenated, deaminated and deprotected to provide the novel 1-haloestradiols.
Type:
Grant
Filed:
April 9, 1984
Date of Patent:
April 22, 1986
Assignee:
University of New Mexico
Inventors:
Mark D. Hylarides, Fred A. Mettler, Jr.
Abstract: 6,6-ethylene-15,16-methylene-3-oxo-17.alpha.-pregn-4-ene-21,17.alpha.-carbo lactones of general Formula I ##STR1## wherein ##STR2## is a CC-single of CC-double bond, R.sub.1 is a hydrogen atom or a methyl group,R.sub.2 is a methyl or ethyl group, and ##STR3## exhibit strong gestagen potency and an aldosterone-antagonistic activity.
Type:
Grant
Filed:
January 18, 1985
Date of Patent:
April 22, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Klaus Nickish, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Sybille Beier, Walter Elger
Abstract: Ethynylation of 17-keto steroids (I) by standard means in the presence of a polar amine solvent produces the epi (17.beta.-ethynyl-17.alpha.-hydroxy) configuration at C.sub.17. The epi-ethisterone compounds are useful intermediates in the production of 17.alpha.-hydroxyprogesterones.
Abstract: A method of treating thrombosis, which comprises administering to a living body a thrombosis preventive and curative preparation containing as an active ingredient a pharmaceutically effective amount of a plant sterol selected from the group consisting of sitosterol and fucosterol, or an ester thereof.
Abstract: Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.
Type:
Grant
Filed:
July 14, 1983
Date of Patent:
March 25, 1986
Assignee:
Glaxo Group Limited
Inventors:
Gordon H. Phillipps, Brian M. Bain, Stuart B. Laing
Abstract: Novel 6.alpha.-fluoro-9.alpha.-chloro-16.beta.-methyl-prednisolone 17, 21-diesters, and a method for their preparation, are described. The novel products are particularly valuable as anti-inflammatory agents.
Abstract: A composition for curing respiratory diseases which contains a medicine such as antibiotic, chemotherapeutic and anticancer drug for respiratory disease and lung surfactant.
Abstract: Sebum secretion accelerator composition comprising a cholesteryl ester of a branched fatty acid represented by the formula (I): ##STR1## in which R represents a saturated aliphatic hydrocarbon group having from 11 to 23 carbon atoms and at least one alkyl substituent at a position between the carboxyl bond and the center of the main chain. The cholesteryl ester should be contained not smaller than 25 wt % of the total composition.The composition according to the invention promotes sebum secretion, and is effective in keeping healthy and beautiful skin.The composition is further advantageous in that it can be readily formed into various types of cosmetics such as lotions, creams and ointments.
Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha., 24,25-trihydroxycholecalciferol.
Type:
Grant
Filed:
February 27, 1984
Date of Patent:
February 4, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Andor Furst, Ludwig Labler, Werner Meier
Abstract: A compound of the formula ##STR1## wherein Z is alkoxy of 1-4 carbon atoms or hydroxyalkoxy of 2-4 carbon atoms and Y is nitro, inhibiting the growth of murine ductal carcinoma (MXT mammary tumors).
Abstract: A composition containing spironolactone in an amount effective to suppress excess androgenic activity. The spironolactone-containing composition is applied directly to the skin site afflicted with excess androgens.