Abstract: Derivatives of C-076 are described in which the C-076 molecule, a series of macrolides in which one of the substituents is a 4-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrose has one or both of the carbohydrate moieties removed therefrom. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such use are also disclosed.
Type:
Grant
Filed:
April 17, 1978
Date of Patent:
June 3, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Helmut H. Mrozik, George Albers-Schonberg
Abstract: Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term "linear backbone" is meant that the polymer has only acyclic groups, i.e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from "branching" when it has no repeating monomer units extending from the polymer backbone; and it is free from "cross-linking" when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.
Type:
Grant
Filed:
April 11, 1979
Date of Patent:
June 3, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Nathaniel Grier, Tsung-Ying Shen
Abstract: Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term "linear backbone" is meant that the polymer has only acyclic groups, i. e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from "branching" when it has no repeating monomer units extending from the polymer backbone; and it is free from "cross-linking" when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.
Type:
Grant
Filed:
April 11, 1979
Date of Patent:
May 27, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Arthur F. Wagner, Nathaniel Grier, Tsung-Ting Shen
Abstract: Derivatives of C-076, a series of macrolides, are described in which the substituents are sugar or saccharide groups. The sugar groups are substituted on any of the available hydroxy groups of the C-076 molecule. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed.
Abstract: Certain novel acyl cyanoguanidines, their preparation, pharmaceutical compositions and novel methods of treating inflammation and autoimmune diseases such as rheumatoid arthritis are disclosed.
Abstract: Derivatives of C-076, a series of macrolides, are described in which the substituents are acyl groups. The acyl substituents may be aromatic of non-aromatic. The acyl derivatives are prepared by various procedures depending upon the particular C-076 compound being substituted. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed.
Type:
Grant
Filed:
April 17, 1978
Date of Patent:
May 6, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Helmut H. Mrozik, Michael H. Fisher, Peter Kulsa
Abstract: Derivatives of C-076, a series of macrolides are described, in which the substituents are hydrocarbon groups. The hydrocarbon groups generally are alkyl groups which may be straight or branched and may optionally be substituted with phenyl. The substituted C-076 compounds are prepared by various procedures depending upon the position of the reaction site, and the particular C-076 compound being substituted. The compounds have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed.
Type:
Grant
Filed:
August 4, 1978
Date of Patent:
April 29, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Michael H. Fisher, Aino Lusi, Richard L. Tolman
Abstract: Derivatives of C-076 are described in which the C-076 molecule, as series of macrolides, has a specific unsaturation, at the 22,23-position, catalytically reduced. Further reaction of the reduced C-076 compounds are also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.
Abstract: The invention provides an improved process for the growth of lymphoblastoid cells in a medium supplemented with human albumin. The invention further provides for the production of interferon by viral infection of these lymphoblastoid cells in a medium also supplemented with human albumin. This invention eliminates the necessity for adding animal proteins.
Type:
Grant
Filed:
March 30, 1979
Date of Patent:
April 15, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Alfred A. Tytell, Edgar Scattergood, Arthur K. Field
Abstract: Triazoles substituted at the 3 and 5 positions having an optional substituent in the 1 position are provided. Methods of preparing the novel substituted triazoles are described. The substituted triazoles are useful as anti-gout and anti-hyperuricemic agents. Compositions useful in the treatment of gout and hyperuricemia containing a substituted triazole as the active ingredient are also provided.
Abstract: Certain novel acyl saccharins and acyl 3-oxo-1,2-benzisothiazolines, their preparation, pharmaceutical compositions and novel methods of inhibiting elatase and treating emphysema are disclosed.
Type:
Grant
Filed:
August 20, 1975
Date of Patent:
March 25, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Dennis Mulvey, Howard Jones, Morris Zimmerman
Abstract: Synthetic novel cyclic hexapeptide having the structure: ##STR1## and the dipeptide ##STR2## are prepared. Oral administration of these peptides improves the digestive efficiency of certain herbivorous animals.
Abstract: Bicyclic somatostatin analogs and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by a combination of the solid phase method and the solution method. These analogs have the property of inhibiting the release of insulin, glucagon and growth hormone in humans and animals. The compounds are particularly useful in the treatment of diabetes. Due to the bicyclic structure, these analogs are resistant to enzymatic metabolism and have a longer duration of activity.
Abstract: Peptides having the structural formula: ##STR1## wherein A is D-Thr, D-Val;B is D-Phe, D-Tyr;C is D-Phe, D-Tyr, O-Me-D-Tyr;wherein the ring formed by the peptide backbone contains 26 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting release of insulin, inhibiting growth hormone release and inhibiting glucagon release in humans and animals without materially affecting gastric secretion. They have a longer duration of action than somatostatin.
Abstract: A novel salt of amiloride particularly amiloride citrate has been discovered. Because of its inherent insolubility and less bitter taste, it would lend itself to be more easily formulated into oral liquids, sustained release formulations and chewable tablets than would amiloride hydrochloride.
Abstract: 2,3-Dihydro-6,7-disubstituted-5-thienylmethyl or furylmethyl benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
Type:
Grant
Filed:
February 16, 1978
Date of Patent:
February 19, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., William F. Hoffman, Otto W. Woltersdorf, Jr.
Abstract: N-Alkyl and N-cycloalkyloxamic acid derivatives are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate urolithiasis (kidney and bladder stone disease).
Type:
Grant
Filed:
October 11, 1978
Date of Patent:
February 5, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Frederick C. Novello, Walfred S. Saari
Abstract: The invention disclosed herein relates to novel non-adhesive, free-flowing, pharmacologically acceptable compositions comprising ionene quaternary polymers effective as bile acid sequestrants, such as poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], adsorbed on a pulverulent, solid aggregate of large surface to mass ratio, such as fumed silicas and silica aerogels. It also relates to the novel process for preparing such adsorbate compositions which comprises forming a substantially, uniform suspension of the finely-divided solid aggregate in an aqueous solution of poly-[{methyl-(3-trimethylammoniopropyl)iminio}trimethylene dichloride], evaporatively removing the water from the suspension, and drying the adsorbate thus produced.