Abstract: The present invention refers to new s-triazolo[3,4-a]phthalazine derivatives, to the process for their preparation and to the pharmaceutical compositions containing them.
Type:
Grant
Filed:
October 20, 1987
Date of Patent:
November 29, 1988
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Emilio Occelli, Domenico Barone, Giorgio Tarzia, Adele Giunta
Abstract: This invention relates to a new class of compounds having important biochemical and pharmacological properties. More particularly, this invention relates to N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5HT.sub.2 receptor site, and to the processes for their preparation and use.
Abstract: The present invention is directed to new 3,6-disubstituted-1,2,4-triazolo[3,4-a]phthalazine derivatives of formula I ##STR1## wherein R represents phenyl or substituted phenyl, n is 1 or 2, R.sup.1 is an amino group of formula NR.sup.4 R.sup.5, or an alkoxy of cycloalkoxy group of formula OR.sup.6, and R.sup.2 and R.sup.3 represent hydrogen, halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, to the process for their preparation and to the pharmaceutical compositions containing them. The compounds of the present invention are as active as anti-anxiety substances.
Abstract: The present invention concerns a new antibiotic substance denominated antibiotic A 40926 mannosyl aglycon and the addition salts thereof, a process for preparing it from antibiotic A 40926 complex or a factor thereof, and its use in the treatment of infectious disease involving microorganisms susceptible to it.
Type:
Grant
Filed:
December 23, 1986
Date of Patent:
November 1, 1988
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Enrico Selva, Beth P. Goldstein, Pietro Ferrari, Giovanni Cassani, Francesco Parenti
Abstract: This invention relates to an improvement in a process for making 2,6-di-tertiarybutyl-4-mercaptophenol and 4,4'-isopropylidenedithio-bis-(2,6-di-tertiarybutylphenol), which is effected by carrying out an electrocatalytic reduction of bis(3,5-di-tertiarybutyl-4-hydroxyphenol)polysulfide at a lead cathode in an acidic electrolyte medium.
Abstract: Novel 3-carboxy- and 3-carbalkoxy-5-benzoyl-2(1H)-pyridinones as well as the pharmaeutically acceptable salts thereof are cardiotonic agents useful in the treatment of heart failure.
Type:
Grant
Filed:
July 31, 1986
Date of Patent:
September 6, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Jr., Richard A. Dage, Richard A. Schnettler
Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.
Abstract: Polymorphically pure terfenadine, 1-(p-tert-butylphenyl)-4-[4'-(.alpha.-hydroxydiphenylmethyl)-1'-piperidiny l]-butanol, is prepared by carefully controlled recrystallization methods.
Type:
Grant
Filed:
June 30, 1987
Date of Patent:
May 3, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Timothy G. Fawcett, Christian T. Goralski, David W. Ziettlow
Abstract: This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.
Type:
Grant
Filed:
February 28, 1986
Date of Patent:
March 22, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard A. Schnettler, Richard C. Dage
Abstract: The present invention relates to an improved process for preparing sucrose encrusted methylcellulose particles which readily disperse in cold aqueous liquids. These encrusted particles are suitable for use in bulk laxative compositions. In the improved process, hot sucrose syrup is mixed with powdered methylcellulose, dried and milled.
Type:
Grant
Filed:
August 26, 1986
Date of Patent:
March 22, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Dhiren N. Shah, Gregory V. Hammer, Jack Domet
Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.
Type:
Grant
Filed:
May 27, 1986
Date of Patent:
March 15, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard A. Schnettler, Richard C. Dage
Abstract: Sparsomycin derivatives of the formula ##STR1## wherein X and y are each independently an oxo or an imino group; n is O or the integer 1 or 2; R.sub.1 is a hydrogen or 1 to 4 carbon alkyl group; R.sub.2 is a hydrogen, a 1 to 4 carbon alkyl, a 2 to 5 carbon acyl or a benzoyl group; and R is a 1 to 6 carbon alkyl, 3 to 8 carbon alkenyl, cyanomethyl carboxymethyl, carbalkoxymethyl wherein the alkoxy moiety is a 1 to 4 carbon alkoxy group, nitromethyl, alkylcarbonylmethyl wherein the alkyl moiety is a 1 to 4 carbon alkyl group, pyridyl, furanyl, or furfuryl group or a phenyl or benzyl group optionally substituted by a methylenedioxy or one to two halogen, 1 to 4 carbon alkyl, 1 to 4 carbon alkoxy, 1 to 4 carbon alkylthio, hydroxy, nitro or cyano groups or a pharmaceutically acceptable acid addition salt thereof. Also described are their use as antiprotozoals and antibacterials.
Abstract: This invention relates to amino acid, dipeptide and tripeptide derivatives of 2,6-diamino-3-haloheptanedioic acids, processes for preparing the same, and their use as antibacterial agents.
Type:
Grant
Filed:
January 27, 1986
Date of Patent:
March 8, 1988
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Ekkehard H. Bohme, Fritz Gerhart, William Higgins
Abstract: The present invention refers to a process for transforming teicoplanin factor A.sub.2 component 1 into teicoplanin factor A.sub.2 component 3 by means of a chemical reaction which includes the catalytical hydrogenation of the substrate.
Abstract: A method useful for alleviating cardiac arrhythmias such as tachycardias in animals by administering to arrhythmic animals an antiarrhythmic amount of 4,4'-(isopropylidenedithio)bis (2,6-di-t-butylphenol), probucol.
Abstract: The present invention is directed to pyridazino[4,3-c]isoquinolines of Formula I ##STR1## wherein R represents methyl, phenyl or substituted phenyl groups, R.sub.1 represents inter alia amino or substituted amino, alkoxy or cycloalkoxy groups, having pharmacological activity, to process for preparing them and to the pharmaceutical compositions containing them. The compounds of the invention possess anti-anxiety activity.