Abstract: The present invention is directed to a new class of excitatory amino acid antagonists. The compounds contain quinoline or thieno pyridine moieties.
Abstract: The 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 the use of esters of hexahydro-8-hydroxy-2,6-methano-2H-quinolizin-3(4H)-one and hexahydro-8-hydroxy-2,6-methano-2H-quinolizines in the manufacture of a medicament for the treatment of anxiety, psychosis, glaucoma and for the stimulation of gastric motility.
Type:
Grant
Filed:
May 16, 1990
Date of Patent:
April 30, 1991
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Maurice W. Gittos, Francis P. Miller, Stephen M. Sorensen, John R. Fozard, Paul Moser, Michael G. Palfreyman, Hsien Cheng
Abstract: The present invention is directed to a multi-layered tablet containing an ibuprofen layer, a piperidino-alkanol antihistamine layer, and a layer or layers containing conventional pharmaceutical excipients which is interspersed between the ibuprofen and piperidino-alkanol layer and serves to physically separate them. This tablet solves the problems associated with the physical and chemical incompatibilities between ibuprofen and the piperidinoalkanol antihistamines.
Type:
Grant
Filed:
April 27, 1989
Date of Patent:
March 12, 1991
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Herbert Schock, David F. Long, William R. Nadler
Abstract: This invention concerns the recovery of glycopeptidic antibiotics from aqueous solutions resulting from fermentation broths or process streams. Examples of glycopeptidicantibiotics to which the process of this invention may be applied are the following: vancomycin, actaplanin, ristocetin, avoparcin, actinoidin, LL-AM-374, A 477, OA 7653, A 35512 B, A 515668, AAD 216, A 41030, A 47934, A-40926 (European Pat. Appln. No. 85112406.5), the individual factors, derivatives and pseudo-aglycones and aglycones thereof, teicoplanin and teicoplanin-like compounds.
Abstract: The present invention is directed to the discovery of a new use for a group of known 2-carboxylic indole derivatives. The compounds are excitatory amino acid antagonists.
Type:
Grant
Filed:
April 24, 1989
Date of Patent:
October 2, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Francesco G. Salituro, Boyd L. Harrison, Bruce M. Baron
Abstract: The present invention is directed to a new class of piperidinyl benzimidazole antihistamines which can be described by the following formula: ##STR1## wherein Y is represented by CO or CHOH; m is an integer from 1 to 2; R is represented by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, hydroxy and hydrogen, X is represented by hydrogen, COOR.sub.2 in which R.sub.2 is represented by a C.sub.1-4 alkyl, or X is an alkylene phenyl radical of the formula: ##STR2## wherein T is represented by CHOH, CO, O, or a direct bond; R.sub.1 is represented by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, hydroxy, 2,2-dimethyl ethanoic acid and hydrogen; n is an integer from 1 to 5; or a pharmaceutically acceptable acid addition salt thereof.
Type:
Grant
Filed:
October 13, 1988
Date of Patent:
March 13, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Albert A. Carr, Hsien C. Cheng, John M. Kane
Abstract: The present invention is directed to a new antibiotic substance denominated antibiotic A 42867 pseudoaglycon, a pharmaceutically acceptable salt thereof, a process for its preparation from antibiotic A 42867 and pharmaceutical compositions containing the new substance of the invention.
Type:
Grant
Filed:
January 24, 1989
Date of Patent:
March 13, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Ernesto Riva, Maurizio Denaro, Pietro Ferrari, Giovanni Cassani
Abstract: The present invention pertains to the use of 1,4-disubstituted-piperidinyl compounds in the treatment of insomnia.Said compounds have the following general formula: ##STR1## wherein: each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is independently selected from the group consisting of hydrogen, a C.sub.1-6 alkyl group, halogen, trifluoromethyl, hydroxy, a C.sub.1-6 alkoxy group, or an amino group; n is 2, 3, or 4; and the pharmaceutically acceptable acid addition salts thereof.
Type:
Grant
Filed:
January 19, 1989
Date of Patent:
March 13, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Paul J. Schechter, John M. Orwin, Christian K. Hinze
Abstract: Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used to control the growth of tumor tissue and can be used as antigout agents.
Type:
Grant
Filed:
April 9, 1987
Date of Patent:
February 27, 1990
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Sai P. Sunkara, Michael L. Edwards, David M. Stemerick
Abstract: The present invention concerns new 2'-substituted-4-deoxy-thiazolo[5,4-c]rifamycin SV derivatives having antibacterial activity.These compounds are compounds obtained by chemical modification of thiazolo[5,4-c]rifamycin SV.
Type:
Grant
Filed:
August 24, 1988
Date of Patent:
November 14, 1989
Assignee:
Gruppo Lepetit S.P.A.
Inventors:
Bruno Cavalleri, Marco Turconi, Giovanni Tamborini
Abstract: The present invention relates to a method for relieving or alleviating the symptomatology associated with fibromyalgia comprising administering to a patient a compound as described by Formula I.
Abstract: The present invention concerns new antibiotic substances denominated antibiotic A 40926 N-acylaminoglucuronyl aglycon complex AB, antibiotic A 40926 N-acylaminoglucuronyl aglycon factor A, antibiotic A 40926 N-acylaminoglucuronyl aglycon factor B, antibiotic A 40926 N-acylaminoglucuronyl aglycon factor B.sub.0, antibiotic A 40926 N-acylaminoglucuronyl aglycon factor B.sub.1, antibiotic A 40926 aglycon and the addition salts thereof, a process for their preparation starting from antibiotic A 40926 complex or a factor thereof, and their use in the treatment of infectious diseases involving microorganisms susceptible to them.
Type:
Grant
Filed:
December 23, 1986
Date of Patent:
September 19, 1989
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Enrico Selva, Ernesto Riva, Giovanni Cassani, Francesco Parenti
Abstract: Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used as antigout agents. The chalcone derivatives are also reported to inhibit the destruction of the myelin sheath in the central nervous system of multiple sclerosis patients and are thus useful in controlling the progressive nature of the disease.
Type:
Grant
Filed:
December 14, 1988
Date of Patent:
September 5, 1989
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael L. Edwards, Sai P. Sunkara, David M. Stemerick
Abstract: 1,3-Dihydro-4-pyridoyl-2H-imidazol-2-ones are prepared in a three step process by(a) reducing 1-pyridyl-1,3-deketo-2-oximinoalkanes to produce 1-pyridyl-1-hydroxy-2-amine-3-ketoalkanes;(b) reacting the thus produced hydroxyaminoketone with cyanate ion to produce a 1,3-dihydro-4-hydroxy(pyridyl)methyl-2H-imidazol-2-one; and(c) oxidizing the thus produced hydroxymethyl compound to yield the desired product.
Type:
Grant
Filed:
October 7, 1986
Date of Patent:
February 7, 1989
Assignee:
Merrell Dow Pharmaceuticals, Inc.
Inventors:
Richard A. Schnettler, Chi-Hsin R. King
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 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