Abstract: The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
Type:
Grant
Filed:
July 17, 1995
Date of Patent:
August 20, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Ian A. McDonald, Francesco G. Salituro, Robert Schwarcz
Abstract: The present invention is directed to new antibiotic substances denominated antibiotic GE 2270 factors A.sub.1, A.sub.2, A.sub.3 and H, the addition salts thereof, the pharmaceutical compositions thereof and their use as medicaments, particularly in the treatment of infectious diseases involving microorganisms susceptible to them.
Abstract: The invention is directed to a new class of antiarrhythmic agents of the formula: ##STR1## in which R is represented by hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, CF.sub.3, SR.sub.1, NHC(O)R.sub.2, NH.sub.2, or OH; R.sub.1 is hydrogen or C.sub.1-4 alkyl; R.sub.2 is C.sub.1-4 alkyl; X is represented by CO or CHOH; R.sub.3 and R.sub.4 are each independently represented by methyl, ethyl, n-propyl, or R.sub.3 and R.sub.4 together with the carbon atom to which they each are attached form a C.sub.5 or C.sub.6 cycloalkyl; and Alk is a C.sub.1-4 alkyl; or a pharmaceutically acceptable addition salt thereof.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
July 30, 1996
Assignee:
Merrell Pharmaceuticals, Inc.
Inventors:
Albert A. Carr, Richard C. Dage, David A. Hay, John E. Koerner, Tung Li
Abstract: The present invention is directed to a process for recovering the antibiotics produced by fermentation of Actinoplanes sp. ATCC 33076 or a producing mutant thereof, from a fermentation broth or a process stream, which comprises extraction of the antibiotics by a non-ionic surfactant or a cationic surfactant miscible with or dispersable in water and capable of dissolving the antibiotics, formation of two phases in the first of which the antibiotic and the surfactant are present together, and separation of the antibiotic from the surfactant by addition of suitable organic solvents.
Abstract: New naphthazarin derivatives obtained by introducing in the 7' position of Purpuromycin or .gamma.-Rubromycin an amino or a monosubstituted amino group.The compounds of the invention show antibiotic activity against Gram positive and Gram negative microorganisms, fungi and protozoa and are suitable for the treatment of vaginal infections.
Type:
Grant
Filed:
May 25, 1995
Date of Patent:
June 25, 1996
Assignee:
Gruppo Lepetit SpA
Inventors:
Aldo Trani, Clelia M. L. Dallanoce, Romeo Ciabatti
Abstract: The present invention is directed to an amide derivative of the glycopeptide, teicoplanin. This compound is an antibiotic that is active against gram positive bacteria. This compound is produced by subjecting teicoplanin to an amidation reaction.
Abstract: The present invention is directed to a new antibiotic substance denominated antibiotic GE 2270 factor C.sub.2a, the addition salts thereof, the pharmaceutical compositions thereof and its use as medicament, particularly in the treatment of infectious diseases involving microorganisms susceptible to it and its use as animal growth promoter.
Type:
Grant
Filed:
April 21, 1995
Date of Patent:
May 7, 1996
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Enrico Selva, Sergio Stella, Luigi Colombo, Maurizio Denaro
Abstract: The present invention is directed to a new neuroprotective agent. The agent is R-4-oxo-5-phosphononorvaline. This agent is useful in the treatment of ischemic and hypoxic conditions such as stroke.
Abstract: The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
March 19, 1996
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Adriano Malabarba, Pierfausto Seneci, Jurgen K. Kettenring, Romeo Ciabatti
Abstract: The invention concerns the aglycons of factors A1, A2, A3, A'1, A'2, A'3 of antibiotic A/16686, their corresponding tetrahydroderivatives and mixtures thereof. The aglycons are produced by the selective hydrolysis of antibiotic A/16686 factor A1, A2, A3, A'1, A'2 or A'3. The compounds have antibacterial activity against widely diffused gram positive bacteria and are particularly useful for topical treatment of wound infections and acne.
Abstract: The present invention relates to a method for extracting teicoplanin A.sub.2 from a whole culture fermentation broth by filtration of the mycelium in an alkaline medium and recovery by extraction of the filtered fermentation broth with organic solvents or mixtures thereof or by adsorption onto suitable matrixes.
Abstract: The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
Type:
Grant
Filed:
December 10, 1993
Date of Patent:
January 16, 1996
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Ian Alexander McDonald, Francesco G. Salituro, Robert Schwarcz
Abstract: The present invention concerns novel naphthazarin antibiotic derivatives having general formula I ##STR1## and the pharmaceutically acceptable addition salts thereof.
Type:
Grant
Filed:
May 26, 1994
Date of Patent:
December 12, 1995
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Aldo Trani, Clelia M. L. Dallanoce, Romeo Ciabatti
Abstract: The present invention is directed to a class of 4,6-disubstituted tryptophan derivatives, 4,6-disubstituted kynurenines, their use as NMDA antagonists and to pharmaceutical compositions containing these compounds.
Type:
Grant
Filed:
June 17, 1994
Date of Patent:
November 28, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Ian A. McDonald, Francesco G. Salituro, Robert Schwarcz, Bruce M. Baron