Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, mono-, di- or trifluoroalkyl, ##STR2## aryl or alkylthioalkyl, wherein R.sub.6 is alkyl or aryl and m is 1, 2, 3 or 4;R.sub.2 is ##STR3## wherein R.sub.7, R.sub.8 and R.sub.9 are each independently hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl or fluorine; andn is 0, 1 or 2;with the proviso that if R.sub.1 is alkylthioalkyl, n is 0.
Abstract: A fluorine-containing 3-oxygenated-.DELTA..sup.3,5 -steroid is prepared in a good yield by fluorinating a steroid with a compound of the formula:RCOOFwherein R is a hydrocarbon group.
Abstract: Method and composition for enhancing protein anabolism in an hypercatabolic mammal. The method comprises parenterally administering to the mammal nutritionally sufficient sources for amino acids, carbohydrates and lipids, the lipids comprising a controlled triglyceride source which, on hydrolysis, yields both long chain fatty acids and medium chain fatty acids, preferably about 20 to 80% long chain fatty acids and about 80 to 20% medium chain fatty acids. In one embodiment, the composition has the additional benefit of being capable of providing more than 60% of the total caloric requirements of the mammal via the lipid source without immunological impairment of the reticuloendothelial system of the mammal.
Abstract: The process of the present invention uses an amine to prepare monolithium acetylide which is sufficiently stable at up to 0.degree. and yet is sufficiently reactive to react with 16-substituted-17-keto steroids producing the useful 17.alpha.-ethynyl-17.beta.-hydroxy-16-substituted steroids.
Abstract: A novel process for preparing a steroid of the following formula (to be referred to as compound .circle.13 ) is provided. ##STR1## This compound is known to have marked anti-inflammatory and anti-rheumatoid arthritic activity with very much reduced side effects on humans, such as weight loss, sodium retention, potassium loss and adrenal and pituitary inhibition which are observed in many steroids. The process is characterized in that starting from hydrocortisone, it can produce the desired compound .circle.13 at low cost and that it goes through the following two novel compounds (I) and (II) as intermediates. ##STR2## In the above formulae, >W--X represents >C.dbd.O or >CH--OH, >Y--Z-- represents >C.dbd.CH-- or ##STR3## Q represents a hydrogen or bromine atom, and OR.sup.1 and OR.sup.2 are identical or different and each represents an acyloxy group or a sulfuric or phosphoric acid ester residue.
Abstract: Ovarian follicular development and related hormonal secretions are totally suppressed for periods of several months or longer by a single intramuscular injection of anordrin administered during menstruation given preferably on the first day of menstrual bleeding. The amount of anordrin administered is in the range of 2 to 10 mg per kg of body weight, and is effective to produce the suppression without administration of additional anordrin by any route. Suppression of progesterone and estradiol secretions is of therapeutic value in the treatment of endometrosis, breast cancer, and other conditions aggravated by ovarian hormones.
Abstract: 2-Fluoro-17.beta.-estradiol is synthesized by mercurating a 17.beta.-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.
Abstract: A compound which is biologically active in maintaining calcium and phosphorous metabolism in animals, selected from the group consisting of formula (IA) and (IB): ##STR1## wherein the bond between carbons C-22 and C-23 is single or double; Y is hydrogen, F, --CH.sub.3 or --CH.sub.2 CH.sub.3 ; Z is F, H or X; Y' is H, --CH.sub.3 or --CH.sub.2 CH.sub.3 ; Z' is F or H; Q.sup.a is CF.sub.3 or CH.sub.2 X; Q.sup.b is CF.sub.3 or CH.sub.3 ; X is selected from the group consisting of hydrogen and --OR.sup.1, wherein R.sup.1 is hydrogen or an orthoester glycoside radical of the formula (II) ##STR2## where A represents a glucofuranosyl or glucopyranosyl ring; R.sup.2 is hydrogen, lower alkyl, aralkyl, or aryl; and R.sup.3 is hydrogen or a straight or branched chain glycosidic residue containing 1-100 glycosidic units per residue; with the proviso that at least one of the R.sup.1 is an orthoester glycoside moiety of formula (II).
Abstract: New .DELTA.1,4,9(11)-pregnatrien-3-one-2o-carboxlic acid compounds are described, corresponding to general formula I below: ##STR1## in which X represents halogen, particularly chlorine or bromine or NH.sub.2. There is also described the process for producing compounds corresponding to general formula I by dehydrating the corresponding saturated starting compounds hydroxylated in the 11-position to form the 9(11)-ene-bond, after which the product obtained is, if desired, subjected to chemical transformation into the end products corresponding to general formula I. In particular, it is possible to carry out formation of the 20-acid halides and dehydration in the 9(11)-position in a single process step.
Abstract: Diabetes is treated by orally administering a dehydroepiandrosterone (DHEA) compound selected from the group consisting of DHEA, DHEA sulfate and soluble DHEA compounds. The DHEA compound is preferably administered in finely dispersed form, powdered or solution, mixed with the food diet of the diabetic in a dosage range of up to 0.4% by weight of the food diet. The pharmacological activity and utility of DHEA as a potent anti-diabetic agent and anti-hyperglycemic agent over a variable range of genetic background is documented.
Type:
Grant
Filed:
July 19, 1983
Date of Patent:
May 21, 1985
Assignee:
The Jackson Laboratory
Inventors:
Douglas L. Coleman, Norman Applezweig, Edward H. Leiter
Abstract: There are disclosed 6,19-epidioxyvitamin D.sub.3 derivatives which are represented by the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen atom or a hydroxyl group; when R.sub.1 is a hydrogen atom, R.sub.2 represents a hydroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group; when both R.sub.1 and R.sub.2 represent a hydroxyl group, R.sub.3 is a hydrogen atom or a hydroxyl group; and when R.sub.1 is a hydroxyl group and R.sub.2 is a hydrogen atom, R.sub.3 represents a hydroxyl group. The compounds are highly capable of inducing differentiation of human myeloid leukemia cells with minimum effects on calcium metabolism and are useful as an agent to treat leukemia.
Type:
Grant
Filed:
February 3, 1983
Date of Patent:
May 14, 1985
Assignee:
Chugai Seiyaku Kabushiki Kaisha
Inventors:
Hiroaki Takayama, Sachiko Yamada, Keiko Nakayama, Tatsuo Suda
Abstract: R.sup.3 is a C.sub.1-6 alkyl group or a C.sub.3-7 cycloalkyl group; andR.sup.4 is a group --OR.sup.5 or --OCOR.sup.6 whereR.sup.5 is an optionally substituted alkyl or alkenyl group which may contain up to 6 carbon atoms, an optionally substituted C.sub.3-7 cycloalkyl group, a phenyl group or a carbon-attached 5-7 membered heterocyclic ring in which the hetero-atom is selected from nitrogen, oxygen and sulphur, andR.sup.6 is a hydrogen atom or a group R.sup.5 as defined above;provided that when the compounds contain a 5.beta.-hydrogen atom, R.sup.2 is a hydrogen atom and salts thereof, which compounds have activity as antidysthythmic agents.
Type:
Grant
Filed:
June 30, 1983
Date of Patent:
May 7, 1985
Assignee:
Glaxo Group Limited
Inventors:
Gordon H. Phillipps, David C. Humber, George B. Ewan, Barry A. Coomber
Abstract: A pharmaceutical composition of matter useful as a topical medicament which comprises an E-type prostaglandin compound or other water unstable active ingredient in a quick-breaking foam formulation to be dispensed from a pressurized container through a metered valve.
Abstract: Novel 9.alpha.,11.beta.-dichloro-16.alpha.-methyl-.DELTA..sup.1,4 -pregnadiene 3,20-diones of the formula ##STR1## wherein R is selected from the group consisting of trimethylsilylphenyl, cyclododecyloxy, dicyclopentylmethoxy and cyclohexylmethoxy having a suprising "in loco" anti-inflammatory activity limited to place of inflammation without systemic effects and a process for their preparation.
Type:
Grant
Filed:
September 15, 1983
Date of Patent:
May 7, 1985
Assignee:
Roussel Uclaf
Inventors:
Jean G. Teutsch, Roger Deraedt, Josette Benzoni
Abstract: The present invention provides a preparation for conditioning and grooming the hair. The active ingredients are vegetable lecithins, as well as cytochromes, phosphatidyl inositols, phosphatides and phosphatidic acids. Apart from the vegetable lecithins the other active ingredients are obtained by aqueous or ethereal extraction from fresh animal hearts, more particularly bovine hearts.
Abstract: Derivatives of biliary acids having formula I ##STR1## wherein St has the meaning of the 17-etiocholanyl residue, having two or more hydroxyl groups both in the .alpha. and .beta. conformation, some of which being optionally replaced by keto groups, and their pharmaceutically acceptable salts with alkaline or alkali-earth metals, or with organic bases.
Type:
Grant
Filed:
July 22, 1983
Date of Patent:
April 30, 1985
Assignee:
Lehner AG
Inventors:
Virginio Castagnola, Giuliano E. Frigerio, Roberto Pellicciari
Abstract: Novel steroids having the formula ##STR1## wherein R.sup.1 is selected from the group consisting of methyl, ethyl, and propyl;R.sup.2 is selected from the group consisting of H and methyl;R.sup.3 is selected from the group consisting of OXO and H(OR.sup.5); ##STR2## wherein R.sub.4 is selected from the group consisting of H.sub.2, H(methyl), H(Cl), H(F), and .dbd.CH.sub.2 ; or ##STR3## wherein R is selected from the group consisting of H, methyl, Cl, and F. Q-S is selected from the group consisting of --CH.dbd.CH-- and --CH.sub.2 CH--.Also disclosed is a method for making and therapeutically using the steroids and for making the intermediates.
Abstract: This invention provides novel 1,23-dihydroxyvitamin D compounds, a process for preparing such compounds of novel intermediates in such process.As indicated by its binding affinity for the 1.alpha.,25-dihydroxyvitamin D.sub.3 receptor protein, the compounds of this invention would function as effective substitutes for vitamin D and certain vitamin D metabolites for the regulation of calcium and phosphorous metabolism and for treatment of bone-related diseases.
Type:
Grant
Filed:
September 14, 1983
Date of Patent:
April 23, 1985
Assignee:
Wisconsin Alumini Research Foundation
Inventors:
Hector F. DeLuca, Heinrich K. Schnoes, Seok-Ho Lee
Abstract: The invention concerns new pharmaceutical preparations for topical administration, such as creams, ointments, foams, pastes or gels, which contain the anti-inflammatorily active glucocorticoid 2-chloro-6.alpha.,9.alpha.-difluoro-16.alpha.-methyl-11.beta.,17.alpha.,21 -trihydroxy-pregna-1,4-diene-3,20-dione (2-chloroflumethasone, halometasone) and the antimicrobial agent 2,4,4'-trichloro-2'-hydroxy-diphenyl ether (triclosan). The new dermatics may contain, besides these two components, pharmaceutical carriers as usually present in formulations for topical administration. The new dermatics are especially suitable for the treatment of inflected forms of acute eczematous dermatoses of different origin, for the initial treatment of strongly inflamed dermatomycoses or strongly inflamed forms of pyodermias.