Abstract: A corticoid-containing pharmaceutical preparation adapted for topical application, comprising 0.005-2% by weight of a corticoid having antiinflammatory activity, a fatty phase, an aqueous phase, an emulsifier, a preservative, and, optionally, a fragrant substance, or an additional hydrophilic or lipophilic cosmetically active ingredients, wherein the fatty phase, and the aqueous phase are present in the form of a dispersed mixture of an oil/water emulsifier and a preservative, and a water/oil emulsion containing a water/oil emulsifier, the particle size of the inner phase of the emulsions being 2-50 .mu.m.
Type:
Grant
Filed:
October 17, 1988
Date of Patent:
April 17, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Wolfgang Stindl, Ingfried Zimmerman, Renate Reckers, Hans Wendt, Rainold Arndt
Abstract: In place of gelatin conventionally used as a material for shaping hard medicinal capsules, the invention proposes a hard capsule for medicinal use shaped of a polymer blend of a water-soluble cellulose ether, e.g., alkyl cellulose, hydroxyalkyl cellulose and alkyl hydroxyalkyl cellulose, and a polyvinyl alcohol in a weight ratio of 70:30 to 98:2. The inventive hard medicinal capsules have remarkably low permeability to oxygen and moisture with little influences on the medicament contained therein along with sufficiently high mechanical strengths and are much more stable than conventional gelatin-made capsules against the influences of the ambient conditions, such as, the crack formation unavoidable in a gelatin-made hard capsule when it is kept under an extremely low humidity.
Abstract: A synergistic fungicidal composition comprising a fungicidally effective amount of(a) 1-(4-phenyl-phenoxy)-1-(1,2,4-triazol-1-yl)-3,3-dimethyl-butan-2-ol of the formula ##STR1## (b) plus another fungicidally active derivative of 1,2,4-triazole of the formula ##STR2## in which A is the keto group of the CH(OH) group.
Type:
Grant
Filed:
August 23, 1988
Date of Patent:
April 3, 1990
Assignee:
Bayer Aktiengesellschaft
Inventors:
Wilhelm Brandes, Helmut Kaspers, Paul Reinecke, Hans Scheinpflug, Wolfgang Kramer
Abstract: Preparation of novel solvates of beclomethasone 17,21-dipropionate, by dissolution of beclomethasone 17,21-dipropionate in an ethereal or halogenated hydrocarbon solvent and precipitation by the addition of di-isopropyl ether. These new solvates are bulk stable, in both the micronized and non-micronized forms. The micronized form is especially suitable for the preparation of stable aerosol.
Abstract: An in-situ biocide having improved characteristics comprises polyoxymethylene polymers having an inherent viscosity of at least 0.1 as measured in para-chlorophenol at 60.degree. C. Such polymers provide continuous release of formaldehyde biocide in hydrocarbon production, transportation, ans storage systems by long term decomposition of the polyoxymethylene. The polyoxymethylenes used are water-insoluble materials, wherein decomposition rate can be controlled through the use of pH, temperature, and certain decomposition catalysts.
Abstract: Alcohol/aqueous solutions of certain relatively insoluble imidazole derivatives, particularly micronazole and miconazole nitrate, are prepared to concentrations of at least 1.0 percent by weight active agent. The solutions are pharmacologically acceptable for topical application as the treatment of fungal skin infections and are readily applied by means of a pump sprayer.
Abstract: A skin care composition having improved effectiveness in preventing and treating acute inflammatory skin conditions comprising miconazole nitrate and zinc oxide.
Type:
Grant
Filed:
February 11, 1985
Date of Patent:
March 27, 1990
Assignee:
Johnson and Johnson Consumer Products, Inc.
Abstract: Introduction of a C-12 substituent and especially a .beta. C-12 substituent into glucocorticoids improves their usefulness as topical antiinflammatories by increasing their topical activity relative to their systemic activity, thus reducing systemic side effects such as adrenal suppression.
Type:
Grant
Filed:
December 4, 1987
Date of Patent:
March 20, 1990
Assignee:
SRI International
Inventors:
Mitchell A. Avery, Masato Tanabe, Dennis Yasuda, George Detre
Abstract: 19-Substituted progesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pathways which will vary according to the nature of the specific 19-substituted progesterone or related compound desired.
Abstract: In a process for hydrating a nitrile compound by the action of a microorganism having nitrilase activity to convert the nitrile compound into the corresponding amide compound, the performances such as yield and reaction velocity are markedly enhanced by irradiation of the microorganism with light. The process of the present invention is characterized in that (a) the microorganism having nitrilase activity is a positive gram-staining microorganism, (b) the microbial cells are allowed to accept light energy of at least about 1.times.10.sup.-2 .mu.E/g microbial cells second before termination of the hydration reaction, and (c) the hydration reaction is carried out in a vessel composed at least partly of a non-light transmitting material.
Abstract: 26,26,26-Trifluoro-1.alpha.,25-dihydroxy-cholecalciferol, and the 25R or 25S epimer thereof, are described, as well as processes and intermediates utilized to prepare the same, as well as pharmaceutical compositions containing the same. 26,26,26-trifluoro 1.alpha.,25-dihydroxycholecalciferol and the 25R or 25S epimer thereof are useful agents in the treatment of disease states such as osteoporosis, osteodystrophy and leukemia.
Type:
Grant
Filed:
January 22, 1986
Date of Patent:
March 6, 1990
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, Giacomo Pizzolato, Gary A. Truitt, Milan R. Uskovic
Abstract: The present invention relates to a pharmaceutical combination product for the induction of labor or for preventing the development of pregnancy, containing(A) one or more antigestagen(s)(B) one or more long-chain polyunsaturated fatty acid(s) or preparations thereof and, if necessary,(C) prostaglandins,where suitable as antigestagens are all compounds which have a strong affinity for the gestagen receptor but at the same time do not themselves have any considerable intrinsic gestagenic activity.The products are preferably administered intravaginally or (extra)amnially. In this connection, it is possible for the antigestagens and the fatty acids according to the invention to be administered either simultaneously or separately, for example consecutively.
Abstract: The invention relates to 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.
Type:
Grant
Filed:
July 26, 1988
Date of Patent:
February 27, 1990
Assignee:
Farmitalia Carlo Erba S.p.A.
Inventors:
Franco Buzzetti, Natale Barbugian, Paolo Lombardi, Enrico di Salle
Abstract: The present invention relates to novel insecticidal aqueous-based microemulsion compositions and methods for controlling insects with said aqueous-based microemulsions. The microemulsions of the present invention contain a synthetic pyrethroid or organophosphate insecticide, a certain surfactant blend, microemulsion adjuvants such as antifoamers, antifreezing agents, thickeners and preservatives and provide thermodynamically, stable compositions uniquely suited for ultra-low volume (ULV) applications in combatting insect pests.
Abstract: A method is provided for suppressing atherogenesis in which a cholesterol 20-hydroperoxide is administered, which is preferably one or both of the novel compounds: 20(R)-hydroperoxy-25-hydrocholesterol and 29(S)-hydroperoxy-25-hydrocholesterol.
Type:
Grant
Filed:
October 26, 1988
Date of Patent:
February 13, 1990
Assignee:
Iowa State University Research Foundation, Inc.
Abstract: Novel vitamin D.sub.3 derivatives of the following formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group. These compounds have an activity of inducing differentiation of tumor cells, and are useful for antitumor agents. On the other hand, the compounds have almost no vitamin D activity.
Abstract: A process for preparing 15-oxygenated sterols, such as 3.beta.-hydroxy-5.alpha.-cholest-8(14)-ene-15 one, comprising converting 7-dehydrocholesterol to 3.beta.-benzoyloxycholesta-5,7-diene, converting the 3.beta.-benzoyloxycholesta-5,7-diene to a 3.beta.-benzoyloxy-5-cholesta-7,14-diene, converting the 3.beta.-benzoyloxy-5-cholesta-7,14-diene to a 3.beta.-benzoyloxy-14.alpha., 15.alpha.-epoxy-5-cholest-7-ene and converting the 3.beta.-benzoyloxy-14.alpha., 15.alpha.-epoxy-5-cholest-7-ene to a 15-oxygenated sterol. Preferably, the 3.beta.-benzoyloxy-cholesta-5,7-diene is converted to a 3.beta.-benzoyloxy-5-cholesta-7,14-diene by (i) contacting 3.beta.-benzoyloxy-cholesta-5,7-diene, in a solvent at a temperature of at most about -55.degree. C., with HCl at a concentration of at least about 2.0 M for a time sufficient to convert the 3.beta.-benzoyloxycholesta-5,7-diene to a 3.beta.
Type:
Grant
Filed:
February 5, 1988
Date of Patent:
January 30, 1990
Assignee:
William Marsh Rice University
Inventors:
George J. Schroepfer, Jr., William K. Wilson, Ker-Shi Wang, Alemka Kisic
Abstract: A fertility drug is made from an effective component comprising ferulyl stanol derivative represented by the following formula (I) and/or phytosterol fatty acid ester represented by the following formula (II). Such an effective component may be extracted from Job's tears seed, preferably bran thereof. A synthetic method of producing ferulyl phytostanol derivative is also disclosed.
Abstract: Novel intermediates useful in the synthesis of chenodeoxycholic acid, the intermediates being of the formula: ##STR1## wherein --X is an electron withdrawing group, n is an integer equal to zero or one, and --Y is a halogen.A process for producing such novel intermediates from 5.beta.-cholanic acid-3.alpha., 7.alpha., 12.alpha.-triol methyl ester is carried out without using highly toxic and carcinogenic compounds such as dichromates and chromium trioxide.
Abstract: Compounds having the formula: ##STR1## wherein R.sub.1 is H or an optionally substituted acyl group having 1-12 carbon atoms,R.sub.2 is H or an acyl group having 1-12 carbon atoms andR.sub.3 is C, N--CH.sub.3 or a direct bond;and mono- or bisquaternary ammonium compounds thereof and acid addition salts of the non- or mono-quaternary ammonium compounds. Process for the preparation of these compounds. Compositions comprising at least one of the above compounds as the active ingredient. The compounds are favorable neuromuscular blocking agents.
Type:
Grant
Filed:
April 13, 1988
Date of Patent:
January 16, 1990
Assignee:
Akzo N.V.
Inventors:
Thomas Sleigh, David S. Savage, Ian C. Carlyle