Abstract: Steroid-N-(2-halogen ethyl)-N-nitroso-carbamoylamino acid or peptide esters of the general formula: ##STR1## where R.sub.1 and R.sub.2, which may be identical or different, mean the radical of an amino acid beyond the C atom in the beta position (if present), R.sub.3 means the radical of a steroid or a stilbene derivative pharmacologically similar in action, n is a number from 0-5 and Hal stands for chlorine or fluorine, as well as the method for preparing them by the conversion of an appropriate carbamoyl-amino acid or carbamoyl-peptide in a manner known per se with steroid alcohols or the conversion of steroid-amino acid or steroid-peptide esters with corresponding N-nitroso-carbamoylation or corresponding N-nitroso-carbamoyl-amino acids or peptides in a manner known per se.
Type:
Grant
Filed:
May 8, 1985
Date of Patent:
October 7, 1986
Assignee:
Stiftung Deutsches Krebsforschungs Zentrum
Abstract: A novel method of treating inflammation of the colon and rectum of warm-blooded animals comprising administering to the colon and rectum of warm-blooded animals an anti-inflammatorily effective amount of 9.alpha.,11.beta.-dichloro-16.alpha.-methyl-21-oxycarbonyldicyclohexylmeth oxy-.DELTA..sup.1,4 -pregnadiene-3,20-dione.
Type:
Grant
Filed:
April 1, 1985
Date of Patent:
September 30, 1986
Assignee:
Roussel Uclaf
Inventors:
Francoise Delevallee, Roger Deraedt, Simone Jouquey
Abstract: The process of the present invention transforms 16-methylene-17-keto steroids (I) to the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-16-methylene steroids (II).
Abstract: A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl, comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms, with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
Type:
Grant
Filed:
September 26, 1983
Date of Patent:
September 30, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Karl Petzoldt, Rudolf Wiechert, Henry Laurent, Klaus Nickisch, Dieter Bittler
Abstract: Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.
Type:
Grant
Filed:
November 16, 1984
Date of Patent:
September 23, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico Baggiolini, Giacomo Pizzolato, Milan Uskokovic, Gary Truitt
Abstract: The syntheses of 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol, and the epimeric mixture thereof which are useful as differentiation inducing agents and anti-proliferation agents are described, 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol and the epimeric mixture thereof are useful for treating tumors and leukemia, and osteoporosis.
Type:
Grant
Filed:
November 29, 1984
Date of Patent:
September 16, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
Abstract: The present invention relates to novel immunogens which can be employed in a method for eliminating the offensive odor associated with the preparation of meats derived from uncastrated male pigs. "Boar taint," as the characteristic odor has been termed, can be eliminated, or at least substantially reduced by the administration of novel immunogen compositions which are chemical conjugates formed of certain C.sub.19 .DELTA..sup.16 -steroids and their mixtures with a carrier protein. The immunogens can be administered in conventional forms including a vaccine.
Type:
Grant
Filed:
October 19, 1984
Date of Patent:
September 9, 1986
Assignee:
Research Corporation
Inventors:
Albert M. Pearson, Roger I. Brooks, Maynard G. Hogberg, James J. Pestka, J. Ian Gray
Abstract: Steroid-N-(2-halogen ethyl)-N-nitroso-carbamoyl-amino acid or peptide esters of the general formula: ##STR1## where R.sub.1 and R.sub.2, which may be identical or different, mean the radical of an amino acid beyond the C atom in the beta position (if present), R.sub.3 means the radical of a steroid or a stilbene derivative pharmacologically similar in action, n is a number from 0-5 and Hal stands for chlorine or fluorine, as well as the method for preparing them by the conversion of an appropriate carbamoyl-amino acid or carbamoyl-peptide in a manner known per se with steroid alcohols or the conversion of steroid-amino acid or steroid-peptide esters with corresponding N-nitroso-carbamoylation or corresponding N-nitroso-carbamoyl-amino acids or peptides in a manner known per se.
Abstract: A novel steroid compound of the formula ##STR1## wherein A is a lower alkylene group; ##STR2## is an acyl group; and is a single bond or a double bond, and methods of producing the compound (I) as follows: ##STR3## and a pharmaceutical composition containing the compound (I). The compound (I) exhibits excellent antiandrogenic activity on oral administration and can be used for the treatment of prostatic hypertrophy.
Abstract: 11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,R.sup.3 is a hydrogen atom or an acyl group,R.sup.1 and A-B have various meanings,which possess antigestagen and antimineralocorticoid activity.
Type:
Grant
Filed:
December 21, 1984
Date of Patent:
September 2, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Ralph Rohde, Klaus Annen, Gunter Neef, Rudolf Wiechert, Sybille Beier, Walter Elger, David Henderson
Abstract: Novel 17.beta.-methoxycarbonyl derivatives of the androstane series of the formula ##STR1## in which R represents alkyl having from 1 to 4 carbon atoms are distinguished by a high local anti-inflammatory activity without having any systemic side effects. The compounds are manufactured by conventional processes of steroid chemistry.
Abstract: The method of preparing a 2.alpha.-cyano-4.alpha.,5.alpha.-epoxy-3-oxo steroid or a steroid fused at the 2- and 3-positions with a heterocyclic ring of controlled particle size which comprises dissolving the steroid in an organic solvent, precipitating the steroid by mixing a non-solvent for the steroid with the resulting solution, and controlling the time of mixing and the degree of agitation during mixing.
Abstract: A composition for use for the treatment of burns, cuts, wounds, abrasions and the like, comprises a pharmaceutically acceptable glycol, preferably propylene glycol, and a cellulose derivative, which is heat sterilizable, preferably hydroxyethyl cellulose. The composition optionally contains an antiseptic, an antibiotic and/or a topical corticosteroid.
Abstract: 7.alpha.-acylthio-4-pregnene-3,20-diones, active as mineralocorticoid hormone antagonists, of the formula: ##STR1## in which R.sub.1 is hydrogen, hydroxyl or acyloxy --OR.sub.2, R.sub.2 is an acyl group derived from a straight or branched-chain alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl or heterocyclic carboxylic acid having up to 12 carbon atoms.
Abstract: Estrane derivatives of the general formula I ##STR1## wherein one of the substituents X or Z signifies a hydrogen atom and the other together with Y represents a carbon-carbon bond, or wherein the substituents X and Z represent hydrogen atoms and Y represents an .alpha.-position hydroxy group or a .beta.-position alkyl group with up to 6 carbon atoms, are valuable intermediates for preparation of pharmacologically effective substances.
Type:
Grant
Filed:
August 27, 1984
Date of Patent:
July 29, 1986
Assignee:
Schering Aktiengesellschaft
Inventors:
Gunter Neef, Karl Petzoldt, Gerhard Sauer, Helmut Hofmeister
Abstract: Synthetic sapogenin and sterol compounds, administered orally to warm-blooded animals, inhibit the absorption of cholesterol and are useful in the treatment of hypercholesterolemia. Particular compounds suitable for such purposes include glycosides with spirostane, spirostene, or cholesterol aglycones, and esters of spirostanes, spirostenes and cholesterol.
Abstract: A novel process for the preparation of prednisone derivatives of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms and R.sub.
Abstract: Novel corticoid 17.alpha.-alkoxycarbonyl carboxylate derivatives are disclosed. These derivatives have strong topical anti-inflammatory activity and extremely weak systemic adverse reactions and are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.