Abstract: Novel biotransformation compounds I, II, III and IV are prepared by fermenting 3-[(2'-tetrazol-5-yl-biphenyl-4-yl) methyl]-7-methyl-2-propyl-3H-imidzao [4,5-b]pyridine in a culture of Streptomyces sp., Accession Number ATCC 55041. ##STR1## These novel compounds are Angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure and other indications known to respond to A II antagonists.
Abstract: The invention presented is a composition for the treatment of individuals addicted to narcotics or individuals having age-related conditions such as tinnitus and Alzheimer's disease, comprising a protected complex of procaine and a complexing agent for procaine in an amount effective to reduce the withdrawal symptoms of individuals addicted to narcotics or the symptoms of tinnitus and Alzheimer's disease.
Abstract: Methods and compositions are provided for treating drug-dependent individuals so as to effect withdrawal from the drug of abuse, e.g., natural and synthetic narcotics, or stimulant-type drugs such as cocaine, amphetamines, nicotine, or the like. The method involves substitution therapy wherein a serotonin antagonist such as ergotamine or a derivative thereof and a CNS stimulant such as caffeine are substituted for the drug of abuse.
Abstract: A moisture stable solid valproic acid formulation is provided. The formulation comprises:55 to 65 weight percent valproic acid,10 to 25 weight percent fillers,10 to 20 weight percent disintegrants,3 to 6 weight percent binders, and0.5 to 1.2 weight percent lubricantsA preferred formulation is:60 weight percent of valproic acid,20 weight percent of magnesium oxide,15 weight percent corn or potato starch,3 weight percent polyvinylpyrrolidone,1 weight percent sodium carboxymethylcellulose,0.8 weight percent magnesium stearate.The formulations are manufactured by mxing an alcohol solution of valproic acid with the fillers, drying and then milling the mixture, adding the disintegrants and wet granulating with at least a portion of the binder. The wet granulate is dried, sized and to it is added the lubricant and any remaining binder.The lubricated granulate can be compressed into tablets without a protective coating.
Abstract: A pharmaceutical composition and process for administering non-steroidal anti-inflammatory drugs which are protected against injury to gastrointestinal tract by beta adrenergic agonists.
Abstract: A compound and method are disclosed for reducing the effects of epilepsy, especially temporal lobe epilepsy. The treatment disclosed by the subject invention is provided by administering an aryl-cycloalkyl-alkanolamine substance having the general formula: ##STR1## The compounds procyclidine, biperiden, and trihexyphenidyl fall within this class of compounds. Although not previously recognized to be effective against epilepsy, all three representative compounds were tested against soman and pilocarpine, two cholinergic neurotoxins used in animal research on epilepsy. All three of those compounds were shown to be highly effective in providing protection against the seizures and neurological damage caused by cholinergic neurotoxins, even when administered only after the onset of convulsions.
Abstract: A pharmaceutical composition comprising a local anaesthetic adapted to inhibit relaxation of the lower oesophageal sphincter and a carrier therefor comprising a material adapted to float on gastrointestinal fluids contained in the stomach whereby to be more proximate to the gastric mucosa below said sphincter, than said fluids.
Abstract: Free fatty acids from fish oils, DHA and EPA, are useful in treating diabetes mellitus. The free fatty acids were an order of magnitude more effective in treating diabetes than unhydrolyzed fatty acids derived from fish oil.
Abstract: A mouthwash is disclosed and claimed which comprises silver acetate, ammonium nitrate, and nitric acid which, when present as a residue in the oral cavity, will cause an adverse taste when the user smokes a tobacco product. The bitter taste experience causes the development of an aversion to smoking. The use of other non-toxic silver compounds is also disclosed.
Abstract: A new combination of drugs is provided which is formed of an angiotensin converting enzyme inhibitor such as ceranapril or captopril, and a dopaminergic receptor blocker which is preferably pimozide and a method for treating obsessive-compulsive disorder and also motor and phonic tics in Tourettes' syndrome using such combinations.
Abstract: Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1 C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.
Type:
Grant
Filed:
May 21, 1990
Date of Patent:
June 25, 1991
Assignee:
Hovione Inter Ltd.
Inventors:
Ivan Villax, William Heggie, Philip R. Page
Abstract: The present invention relates to the art of organic chemistry. The novel compounds - ethyl-3-(2-ethyl-2,2-dimethylhydrazinium)-propionate salts have the general formula: ##STR1## wherein X is Cl, Br, I. The compounds of the present invention possess an antiarrhythmic effect.
Type:
Grant
Filed:
October 30, 1989
Date of Patent:
May 21, 1991
Inventors:
Gunar A. Bremanis, Felix Z. Meerson, Ivars Y. Kalvinsh, Nurlan Abdikaliev, Petr T. Trapentsier, Ma/Ya G. Pshennikova, Irene B. Antsena, Edmund Y. Lukevits, Boris Z. Simkhovich
Abstract: This invention provides a method of selectively antagonizing the 5-HT.sub.1A receptor in mammals by administering aryloxypropanolamines. Novel aryloxypropanolamines are also claimed.
Type:
Grant
Filed:
November 8, 1989
Date of Patent:
May 7, 1991
Assignee:
Eli Lilly and Company
Inventors:
Edward E. Beedle, David W. Robertson, David T. Wong
Abstract: The invention relates to methods for the treatment or prevention of neuronal loss in ischemia, hypoxia, hypoglycemia, brain and spinal cord trauma as well as for treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's Syndrome by administering a pharmaceutical composition comprising an effective amount of 10,5-(iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene (IDDC) or derivatives thereof to an animal.
Type:
Grant
Filed:
April 14, 1989
Date of Patent:
April 30, 1991
Assignee:
State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
Inventors:
Eckard Weber, John F. W. Keana, Peter Barmettler