Abstract: The present invention deals with the combination of several synergistic antioxidants including enzymatic co-factors as adjuncts to therapy of desquamating inflammatory disorders, such as psoriasis. These topical compositions are aimed to neutralize free radical species generated by such inflammatory conditions which are responsible for certain clinical signs and symptoms. As such, damage to skin causing destruction of elastin and collagen tissues is reduced. The present synergistic antioxidants may be combined with anti-inflammatories, including corticosteroids, anti-microbials, including zinc pyrithione, and other preparations useful in the therapy of desquamating disorders as psoriasis, seborrhoeic dermatitis and related skin and scalp conditions.
Abstract: The present invention provides novel methods of lowering serum cholesterol and inhibiting smoother muscle cell proliferation, particularly restenosis, in humans, and inhibiting uterine fibroid disease and endometriosis in women comprising administering to a human/woman in need of treatment an effective amount of a compound of formula I ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, or trifluoromethyl;R.sup.1 and R.sup.2 each are the same or different C.sub.1 -C.sub.6 alkyl group;n is an integer from 2 to 6; andR.sup.3 and R.sup.4 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form a substituent selected from the group consisting of pyrrolidino, morpholino, piperidino, piperazino, 4-(C.sub.1 -C.sub.6 alkyl)piperazino, and 4-phenyl-piperazino; or a pharmaceutically acceptable salt thereof.
Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.
Type:
Grant
Filed:
March 16, 1998
Date of Patent:
December 28, 1999
Assignee:
Pharmacopeia, Inc.
Inventors:
Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
Abstract: A method for estimation of change in bone mineral density or a method for diagnosis of osteoporosis, comprising the step of measuring change in a concentration of soluble interleukin-6 receptor in a blood sample, by for example, sandwich assay or competition assay; and a kit for carrying out said methods, comprising:(1) an anti-sIL-6R antibody immobilized to a solid carrier, and(2) an anti-sIL-6R antibody is bound to a detectable marker or capable of binding to a detectable marker.
Abstract: The present invention provides an elastase-inhibiting protein isolated ("Guamerin") from a Korean leech, Guameri (Hirudo nipponia) and a process for preparing the same. Guamerin is a protein of a molecular weight of 6,110 Da which is composed of 57 amino acid residues, whose active site is composed of 36-methionine and 37-isoleucine, which retains an inhibiting-activity highly specific to elastase, and which shows stability against heat as well as strong acids and alkalies. Guamerin of the present invention can be applied in the treatment of diseases associated with an excess level of elastase, such as rheumatoid arthritis, emphysema, and psoriasis.
Type:
Grant
Filed:
August 6, 1998
Date of Patent:
December 28, 1999
Assignee:
Korea Advanced Institute of Science and Technology
Inventors:
Ke-Won Kang, Hyo-Il Jung, Seok-Jin Hong, Dong-Ryoung Kim, Ju-Yun Lee
Abstract: Disclosed is a method of assaying, in assay apparatus, for at least the ligand intended to be used to assay analyte in a sample, with which analyte the ligand will specifically bind. The method provides a product in which a ligand is labeled with a detectable tag and is immobilized on an appropriate substrate. An assay is made to measure the immobilized, labeled ligand by detecting the tag labeling the latter. The product can then be used to assay for the analyte by contacting the latter so as to form a complex. The extent and rate of specific binding of the analyte in the complex is identifiable, either by competition assay or sandwich assay as a rate of change, so the relative proportions of analyte and ligand are readily determinable.
Abstract: Disclosed are pharmaceutical compositions that comprise gallium complexes of 3-hydroxy-4-pyrones. These compositions provide enhanced gallium bioavailability particularly when orally administered as compared to the gallium bioavailability achieved by use of pharmaceutical compositions containing gallium salts. Compositions included in this invention are useful in providing gallium to humans and other mammals for a wide variety of medical and veterinary applications, including the treatment, prevention, or diagnosis of hypercalcemia, certain cancers, certain disorders of calcium homeostasis, and certain bone diseases including osteoporosis, osteopenia, and Paget's disease.
Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.
Abstract: A chemical synthesis apparatus (20) for building chemical compounds includes a head assembly (21) having an array of nozzles (22) with each nozzle or plurality of nozzles coupled to a reservoir (23) of liquid reagent (24), and a base assembly (25) having an array of reaction wells (26). A transport mechanism (27) aligns the reaction wells (26) and selected nozzles (22) in a longitudinal X-direction for deposition of liquid reagent (24) into selected reaction wells (26). A plurality of independently controllable sliders (100) move nozzle columns (41) in a lateral Y-direction for deposition of liquid reagent (24) into selected reaction wells (26). A first sliding seal (30) is positioned between the head assembly (21) and the base assembly (25) to form a common chamber (31) enclosing both the reaction well (26) and the nozzles (22) therein. A plurality of second sliding seals (120) is positioned between head assembly (21) and sliders (100).
Abstract: This invention relates to the use of the baculovirus glycoprotein, Interferon Stimulating Protein (ISP) (also known as gp67, gp64 EFP, or gp64), or the gene sequence encoding ISP, to stimulate production of interferon, such as for immunotherapy, anti-viral, anti-cancer, anti-bacterial, or anti-parasitic therapy. This invention also relates to novel mutant forms of ISP that show enhanced biological (i.e., anti-viral) activity, increased stability, higher yield or better solubility.
Type:
Grant
Filed:
June 26, 1998
Date of Patent:
December 14, 1999
Assignees:
Humn Genome Sciences, Inc., Washington University
Inventors:
David M. Hilbert, Daniel P. Bednarik, Bernadetta Nardelli, Marianne Murphy, David Parmelee, Ann Gronowski, Robert Schreiber
Abstract: The present invention provides a method for identifying a peptide which binds to an anti-double stranded DNA antibody. The present invention also provides a class of peptides identified by the method of the present invention which bind to anti-double stranded DNA antibodies and compositions containing these peptides. The present invention also provides methods for the diagnosis and treatment of systemic lupus erythematosus utilizing the peptides of the present invention.
Type:
Grant
Filed:
September 20, 1995
Date of Patent:
December 14, 1999
Assignee:
Albert Einstein College of Medicine of Yeshiva University
Inventors:
Bruce D. Gaynor, Betty A. Diamond, Matthew D. Scharff, Philippe Valadon
Abstract: This invention relates to a method for selecting PDE IV inhibitors which have a salutory therapeutic index, and to compounds having these properties.
Type:
Grant
Filed:
September 3, 1997
Date of Patent:
December 7, 1999
Assignee:
SmithKline Beecham Corporation
Inventors:
Mary S. Barnette, Theodore J. Torphy, Siegfried Benjamin Christensen, IV
Abstract: Disclosed are pharmaceutical compositions that comprise gallium complexes of 3-hydroxy-4-pyrones. These compositions provide enhanced gallium bioavailability particularly when orally administered as compared to the gallium bioavailability achieved by use of pharmaceutical compositions containing gallium salts. Compositions included in this invention are useful in providing gallium to humans and other mammals for a wide variety of medical and veterinary applications, including the treatment, prevention, or diagnosis of hypercalcemia, certain cancers, certain disorders of calcium homeostasis, and certain bone diseases including osteoporosis, osteopenia, and Paget's disease.
Abstract: Treatment of acne through topical administration is an aspect of the present invention. Specifically, muscarinic agents may be applied in any therapeutically acceptable carrier including gels, creams, lotions, and sprays. Therapeutic effects observed with the present invention include decrease in redness, swelling, and inflammation. Treatment of other inflammatory conditions is also disclosed. Treatment of suitable conditions in accordance with the present invention results in significant improvements in healing of those conditions.
Abstract: A method of reducing or inhibiting inflammation and inducing or promoting anti-pyresis comprises administering to a mammal in need of such treatment, an amount of a glutathione depleting agent effective to reduce or inhibit neutrophil sequestration at the inflammation site. The agent may be administered as a pharmaceutical composition including a carrier. Examples of the agent itself are diethylmaleate (DEM), phorone, buthionine-sulfoximine (BSO), glutathione depleting diethylmaleate (DEM) mimetics, glutathione depleting phorone mimetics and glutathione depleting buthionine sulfoximine (BSO) mimetics.
Abstract: A process for the treatment of anxiety and tension, which comprises administering to a patient in need therefor an anxiolytically effective amount of a compound of the formula ##STR1## wherein X is hydrogen, a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl residue, or halogen; R.sup.1 and R.sup.2 are independently of each other a C.sub.1-4 alkyl, cycloalkyl, C.sub.2-4 hydroxyalkyl, or heteroalkyl residue, or R.sup.1 and R.sup.2 together form a C.sub.2-6 alkylene residue in which one --CH.sub.2 -- group can be replaced by oxygen, nitrogen or sulfur; n is 0 or 1, and m is 0 or a cardinal number from 1-5, or a pharmaceutically acceptable salt of the compound.
Type:
Grant
Filed:
May 15, 1998
Date of Patent:
November 30, 1999
Assignee:
Arzneimittelwerk Dresden GmbH
Inventors:
Angelika Rostock, Rita Dost, Christine Tober, Reni Bartsch, Klaus Unverferth, Chris Rundfeldt
Abstract: Subject of the invention is a molecule characterized by the general structure as no. 1., where meaning of x: 1 or 2 valency metallic ion adequate from therapeutic point of view, value of n: 1 or 2, or the application of its metabolite being suitable for the treatment or prevention of embryonic retardation or discordance.
Type:
Grant
Filed:
November 13, 1998
Date of Patent:
November 30, 1999
Assignee:
Biogal Gyogyszergyar RT
Inventors:
Laszlo Vojcek, Tibor Bedo, Tibor Pok, Gabor Bartok, Zsolt Agni
Abstract: The levo-isomers of certain imidazole derivatives, particularly medetomidine, have been found to be inverse agonists of adrenergic .alpha.-2 receptors and are therefore useful in the prevention or treatment of conditions associated with overexpression or hypersensitization of the adrenergic .alpha.-2 receptors, such as obesity, a withdrawal symptom to an adrenergic .alpha.-2 receptor agonist, a neurological disorder, multiple system atrophy, diabetes mellitus, benign prostatic hyperplasia, and drug-induced sensitization of adrenergic .alpha.-2 receptors. The pharmaceutical composition is preferably transdermal.
Type:
Grant
Filed:
September 16, 1998
Date of Patent:
November 30, 1999
Assignee:
Orion Corporation
Inventors:
Karl E. O. .ANG.kerman, Christian Jansson, Jyrki Kukkonen, Juha-Matti Savola, Siegfried Wurster, Victor Cockcroft
Abstract: Fluorescent conjugates suitable for use in flow cytometry and other biological applications. The fluorescent conjugates comprise an antibody having a polymeric dye bound thereto. The polymeric dye is preferably enhanced by a hydrophobic and conformationally restrictive moiety either bound thereto or in close association therewith. The hydrophobic and conformationally restrictive moiety is preferably derived from a cyclodextrin. The polymeric dye comprises a polymeric entity having signal-generating groups, such as aminostyryl pyridinium dye residues attached thereto. The fluorescent conjugates exhibit exceptional stability characteristics and avoid many of the problems of energy transfer, bio-conjugability, and solubility.
Type:
Grant
Filed:
February 1, 1996
Date of Patent:
November 30, 1999
Assignee:
Abbott Laboratories
Inventors:
Christopher Bieniarz, Jeffrey B. Huff, Michael J. Cornwell, Seshagiri R. Tata Venkata
Abstract: Microelectronics wafer substrate surfaces are cleaned to remove metal contamination while maintaining wafer substrate surface smoothness by contacting the wafer substrate surfaces with an aqueous cleaning solution of an alkaline, metal ion-free base and a polyhydroxy compound containing from two to ten --OH groups and having the formula: ##STR1## wherein or in which --R--, --R.sup.1 --, --R.sup.2 -- and --R.sup.3 -- are alkylene radicals containing two to ten carbon atoms, x is a whole integer of from 1 to 4 and y is a whole integer of from 1 to 8, with the proviso that the number of carbon atoms in the polyhydroxy compound does not exceed ten, and wherein the water present in the aqueous cleaning solution is at least about 40% by weight of the cleaning composition.