Abstract: Novel compositions of a combination of nicotinic, opioid, serotonergic and/or adrenergic antagonists in combination with nicotinic and opioid agonists, anti-depressants, stimulants, non-steroidal anti-inflammatory drugs, and local anesthetics, such combinations being useful in the treatment of excitable system disorders, pain and psychiatric disorders, and methods of use thereof.
Type:
Grant
Filed:
June 23, 1998
Date of Patent:
November 28, 2000
Assignee:
The University of Kentucky Research Foundation
Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.
Abstract: Nicotine-responsive neuropsychiatric disorders can be treated by administering a nicotine antagonist, particularly mecamylamine. Combination therapy of mecamylamine with a neuroleptic drug also is disclosed. The neuropsychiatric disorders include Tourette's syndrome, schizophrenia, depression, bipolar disorder, tremors, attention deficit hyperactivity disorder, obsessive-compulsive disorder, hemidystonia, rage outbursts and tardive dyskinesia.
Type:
Grant
Filed:
November 23, 1998
Date of Patent:
March 7, 2000
Assignee:
University of South Florida
Inventors:
Paul R. Sanberg, Roland D. Shytle, Archie A. Silver
Abstract: The migraine-treating effectiveness of an antimigraine drug is significantly enhanced by administering a selective 5-HT.sub.1 agonist together with dextromethorphan or dextrorphan.
Abstract: This invention provides liposomic composition, containing as active ingredient (-)-N-.alpha.-dimethyl-N-(2-propynylphenylethylamine) (selegilin) and/or salt thereof. This composition contains: 0.1-40% by weight of selegilin and/or a salt thereof, 2 to 40% by weight of lipids, preferably phospholipids, 0 to 10% by weight of cholesterol, 0 to 20% by weight of an alcohol, 0 to 25% by weight of a glycol, 0 to 3% by weight of an antioxidant, 0 to 3% by weight of a preserving agent, 0 to 2% by weight of a viscosity influencing agent, 0 to 50% by weight of cyclodextrin or a cyclodextrin derivative and 30 to 90% by weight of water. This invention relates to pharmaceutical composition, containing the liposomic composition described and if desired, usual filling and diluting agents and other auxiliaries, preferably in oral, parenteral or transdermal form. This invention provides the process for the preparation of liposomic compositions containing selegilin and/or salt thereof.
Type:
Grant
Filed:
August 5, 1997
Date of Patent:
March 30, 1999
Assignee:
Chinoin Ltd.
Inventors:
Michael Mezei, Jozsef Gaal, Gabor Szekacs, Gyula Szebeni, Katalin Marmarosi, Kalman Magyar, Jozsef Lengyel, Istvan Szatmari, Agnes Turi
Abstract: The invention comprises inhibiting expression of TNF-.alpha. by administering an effective amount of a stabilized activated oxygen in a matrix of chlorite ions. Preferably, a pharmaceutically acceptable formulation of tetrachlorodecaoxide is used, and more preferably, WF-10. An effective amount of WF-10 comprises up to about 0.5 ml/kg. Another embodiment of the invention is a method of treating AIDS-associated dementia comprising the step of administering to a human an amount of a stabilized activated oxygen in a matrix of chlorite ions sufficient to inhibit production of TNF-.alpha..
Type:
Grant
Filed:
July 19, 1996
Date of Patent:
March 2, 1999
Assignee:
The Regents of the University of California
Abstract: A composition and method of inhibiting tumor growth and treating malignant melanoma without toxic side effects are disclosed. Betulinic acid or a betulinic acid derivative is the active compound of the composition, which is topically applied to the situs of tumor. Betulinic acid is obtained by the steps of preparing an extract from the stem bark of Ziziphus mauritiana to mediate selective cytotoxic profile against human melanoma in the subject panel of human cancer cell lines, conducting a bioassay-directed fractionation based on the profile of biological activity using cultured human melanoma cells as the monitor, and obtaining betulinic acid.
Type:
Grant
Filed:
March 21, 1995
Date of Patent:
August 19, 1997
Assignee:
Board of Trustees of the University of Illinois
Abstract: The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.
Type:
Grant
Filed:
June 17, 1996
Date of Patent:
July 29, 1997
Assignee:
Egis Gyogyszergyar RT
Inventors:
Zoltan Budai, Istvan Gacsalyi, Gabor Szenasi, Tibor Mezei, Aniko Kovacs, Gabor Blasko, Katalin Szemeredi, Gyula Simig, Lujza Petocz, Klara Reiter nee Esses
Abstract: A method of inhibiting viruses in which a virus is contacted with diamondoid alcohol, ketone, ketone derivative, adamantyl amino acid, quaternary salt or combinations thereof which have antiviral properties. These diamondoid derivatives are shown to have antiviral activity against HIV.
Abstract: Damage to CNS neurons of a human patient infected with a human immunodeficiency virus is reduced by administering an antagonist of the NMDA receptor complex.
Type:
Grant
Filed:
January 21, 1993
Date of Patent:
April 9, 1996
Assignee:
The Children's Medical Center Corporation
Abstract: A single-phase, either isotropic or anisotropic formulation is disclosed, which contains perfluorinated oil and one or more surfactant(s), is useful as an excipient for cosmetic and dermatologic formulations and is characterized in that at least one surfactant is selected from those having the following general formula: ##STR1## wherein: R.sub.F is an F--(CF.sub.2 --CF.sub.2).sub.i -- group;X is a group selected from: ##STR2## --(CH.sub.2 --O).sub.K --; and --(CH.sub.2 --S).sub.K --; wherein R.sup.I is a (C.sub.1 -C.sub.4)-alkyl;Y is a group selected from: NH.sub.2 (R.sup.II).sub.2 and N(R.sup.II).sub.4 ; wherein R.sup.II is a hydrogen atom, or a group selected from --CH.sub.2 --CH.sub.2 --OH and (C.sub.1 -C.sub.4)-alkyl;i is an integer comprised within the range of from 3 to 8;i is zero or 1;K is 2.l;l is an integer comprised within the range of from 1 to 10;m is 1 or 2.Such composition is spontaneously formed when the components are simply placed into contact with one another.
Abstract: Fluorinated triethylenediamine compounds such as perfluorotriethylenediamine and the novel compounds undecafluorotriethylenediamine and decafluorotriethylenediamine, prepared by indirect fluorination of triethylenediamine by passing triethylenediamine over, e.g., cobalt trifluoride (CoF.sub.3), are useful as a material capable of carrying oxygen in an aqueous emulsion for lifesaving a patient suffering from massive hemorrhage and for preserving internal organs in transplantation. The compounds undergo rapid biological elimination due to their low molecular weight.
Abstract: The invention is directed to compositions for topical application made up of active pharmaceutical permeants capable of existing in both free base and acid addition salt form. The permeants are present as a combination of both free base and acid addition salt forms. These combined forms provide skin penetration rates which are greater than the penetration rate of either the free base or acid addition salt forms utilized separately. The combined free base-acid addition salt permeants are formulated in a carrier vehicle which preferably also possesses skin penetration enhancement activity.
Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].
Abstract: A mixture of an extract from a plant belonging to the Zygophyllaceae family containing phenolic compositions and a nonalkali metal salt is useful as a pharmaceutical agent, for example, in the treatment of cancer, nonmalignant tumors, osteomyelitis, psoriasis and warts.