Abstract: The invention relates to 11-aryl steroid derivatives, having the structure ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described in the specificationand to processes for their preparation and to pharmaceuticals comprising these compounds.These compounds exhibit a strong anti-progestinic activity and a weak or non-existent anti-glucocorticoid activity.
Abstract: The present invention relates to a drug for human use, having contraceptive and menstrual cycle controlling properties, characterized in that the drug comprises N-acetyl-5-methoxytryptamine or melatonin, in a dose of 100-200 mg per day, N-acetyl-2-bromo-5-methoxytryptamine or 2-bromomelatonin in a dose of 25-50 mg per day, N-acetyl-2-iodo-5-methoxytryptamine or 2-iodomelatonin, in a dose of 20-40 mgs per day, in association with a progestine compound. The administration is carried out for 23 days, by using an association of 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin and a progestinic compound, followed by 5 days in which only 2-iodomelatonin and/or melatonin and/or 2-bromomelatonin is administered; the drug having oncostatic preventive and therapeutic properties, in mammary tumours and melanomas, characterized by the use of 2-iodomelatonin, melatonin and 2-bromomelatonin respectively with doses of 20-40 mgs., 100-200 mgs.
Type:
Grant
Filed:
September 27, 1991
Date of Patent:
December 21, 1993
Inventors:
Franco Fraschini, Bojidar Stankov, Luigi Di Bella, Ermanno Duranti, Aldo Lagguzzi
Abstract: A method of inhibiting the metabolism of cholesterol, comprising administering to a subject a pharmaceutical composition comprising a dioxabicyclo[3.3.0]octane derivative represented by the following general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 together form a methylene group or an ethylene group, and n, m and l are 0 or 1.
Abstract: A pharmaceutical preparation which comprises stigmasta-4-en-3-one as the active ingredient. This active ingredient can be used for the treatment of androgen-dependent diseases, especially for the treatment of benign prostatic hyperplasia.
Abstract: Disclosed is a contraceptive regimen, and method of using the regimen, comprising 24 daily sequential dosage units of: a first phase comprising about 7 to 9 separate first dosage units containing a progestogen at a daily dosage equivalent in progestogenic activity to 100 desogestrel and an estrogen at a daily dosage equivalent in estrogenic activity to 25 .mu.g ethinyl estradiol ("EE"). A second phase of 7 to 9 second dosage units, each of the second dosage units containing a progestogen equivalent to 125 .mu.g desogestrel and an estrogen equivalent lent to 20 .mu.g EE. A third phase of 7 to 9 third dosage units, each unit containing a progestogen equivalent to 50 .mu.g desogestrel and an estrogen equivalent to 20 .mu.g EE. The kit generally has 28 daily dosage units wherein four of the daily dosage units contain no contraceptive steroid, or, alternatively, have only 24 dosage units with a four day "pill-free" period.
Abstract: The invention relates to a method for improving inner ear microcirculation, which comprises administering an effective amount of a dihydropyridine compound of the general formula: ##STR1## wherein R.sup.1 is a nitrophenyl group; and R.sup.2, R.sup.3 and R.sup.4 each is a lower alkyl group, or a pharmaceutically acceptable salt thereof to a human or animal.
Abstract: The invention relates to methods for enhancing wound healing; enhancing gastric, duodenal, esophageal, decubitus, genito urinary ulcer and ulcerative keratitis healing; inhibiting scar formation; and treating periodontal disease in an animal by the topical, oral parenteral, transdermal or ophthalmic administration of a vitamin D compound.
Abstract: This invention provides novel vitamin D-related compounds characterized by extended unsaturated side chain structures. Such compounds exhibit increased activity in arresting the proliferation and promoting the differentiation of malignant cells with only minimal calcemic activity and thus represents new therapeutic agents applicable and uniquely useful in differentiation therapy of malignant diseases. The activity characteristics of these compounds provide the basis of a method for the treatment of neoplastic diseases, specifically leukemoid diseases.
Type:
Grant
Filed:
February 14, 1990
Date of Patent:
October 5, 1993
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman
Abstract: A method of treatment of inflammatory diseases which comprises administering, to a subject in need of such treatment, an anti-inflammatory effective amount of a polyoxyethylenesorbitan mono-higher-fatty acid ester.
Abstract: The use of a compound of the formula (I): ##STR1## wherein R is hydroxy or 2-methoxyethylamino or a pharmaceutically acceptable salt thereof, in stimulating the `atypical` .beta.-adrenoceptors in the gastrointestinal tract and thereby inhibiting gastrointestinal motility. These compounds may be used for treating medical conditions wherein inhibition of gastrointestinal motility is thought to be of value, such as in the treatment of inflammatory bowel disease, irritable bowel syndrome (IBS), non specific diarrhoea and dumping syndrome.
Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treThis invention was made in part with government support under Grant Number PHS AM 19655 awarded by the National Institutes of Health. The government has certain rights in the invention.
Type:
Grant
Filed:
December 10, 1991
Date of Patent:
August 24, 1993
Assignee:
The Rockefeller University
Inventors:
Anthony Cerami, Peter C. Ulrich, Michael Brownlee
Abstract: The invention relates to the prevention and therapy of proteinuria by administration of a combination of ACE inhibitor and calcium antagonist.
Abstract: A method for treatment of hyperlipemia which comprises administering, to a subject in need of such treatment, a 15-keto-prostaglandin compound in an amount, effective in decreasing lipid concentration in the blood.
Abstract: A method of treating a mammal comprises administering to a mammal an effective amount to provide a desired therapeutic effect in the mammal of a compound selected from the group consisting of those having the formula: ##STR1## ,pharmaceutically acceptable acid addition salts thereof and mixtures thereof, wherein R.sub.1 and R.sub.4 are independently selected from the group consisting of H and alkyl radicals having 1 to 4 carbon atoms; the R.sub.2 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the R.sub.3 s are independently selected from H or alkyl radicals having 1 to 4 carbon atoms or are, together, oxo; the 2-imidazolin-2-ylamino group may be in any of the 5-, 6, 7- or 8- positions of the quinoxaline nucleus; and R.sub.5, R.sub.6 and R.sub.7 each is located in one of the remaining 5-, 6-, 7- or 8- positions of the quinoxaline nucleus and is independently selected from the group consisting of Cl, Br, H and alkyl radicals having 1 to 3 carbon atoms.
Type:
Grant
Filed:
January 13, 1992
Date of Patent:
July 27, 1993
Assignee:
Allergan, Inc.
Inventors:
Charles Gluchowski, Michael E. Garst, James A. Burke, Larry A. Wheeler
Abstract: The present invention relates to a method of modifying serum cholesterol levels in a mammal by topically administering to the skin of the mammal an effective amount of at least one phospholipid. Atherosclerosis, and related complications, can be treated, or prevented, using the present method.
Abstract: Methods and compositions of a deuterium-containing compound are disclosed that are utilized in the treatment of hypertension. Compositions containing deuterium oxide, deuterated foods or deuterated antihypertensive drugs dissolved or dispersed in a physiologically tolerable diluent are administered to patients in need of treatment for hypertensive disorders. Methods for the lowering of elevated blood pressure and for decreasing the likelihood of the onset of hypertension in a patient are disclosed.
Abstract: A method for increasing the choroidal blood flow which comprises administering to a subject in need of such increasing a 13,14-dihydro-15-keto-20-ethyl-prostaglandin F, a pharmaceutically acceptable salt thereof or a lower alkyl ester thereof.
Abstract: The present invention relates to compositions and method for inhibiting nonenzymatic cross-linking (protein aging) which contain diaminopyridines and derivates thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
Type:
Grant
Filed:
January 17, 1992
Date of Patent:
June 22, 1993
Assignees:
The Rockefeller University, Alteon Inc.
Inventors:
Peter C. Ulrich, Anthony Cerami, Dilip R. Wagle
Abstract: A method to increase plasma high density lipoprotein levels for the treatment and prevention of coronary artery disease by administering a therapeutic amount of a retinoid of the general formula: ##STR1##
Type:
Grant
Filed:
March 31, 1992
Date of Patent:
June 15, 1993
Assignee:
American Cyanamid Company
Inventors:
Andrew S. Katocs, Jr., Elwood Largis, Sotirios K. Karathanasis