Abstract: 4-Hydroxy-2-methyl-3-(2-pyridylcarbamoyl)-6-trifluoromethyl-2H-thieno[2,3-e ]-1,2-thiazine 1,1-dioxide of the formula ##STR1## and its pharmaceutically acceptable salts which possess valuable pharmacodynamic properties are described. More particularly, the compound and its salts display antiinflammatory, analgesic and antirheumatic activities and they are readily accessible by reacting a corresponding alkyl ester with 2-aminopyridine and, if desired, subsequent salt formation.
Type:
Grant
Filed:
August 31, 1983
Date of Patent:
October 1, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rudolf Pfister, Paul Zeller, Dieter Binder, Otto Hromatka
Abstract: Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy,and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.
Type:
Grant
Filed:
November 15, 1983
Date of Patent:
October 1, 1985
Assignee:
Hoffman-La Roche Inc.
Inventors:
Urs Brombacher, Marc Montavon, Hermann Bretschneider, Joachim Schantl, Wolfgang Turk
Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
Type:
Grant
Filed:
June 30, 1981
Date of Patent:
May 7, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ivan Kompis, Gerald Rey-Bellet, Guido Zanetti
Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions, such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.
Type:
Grant
Filed:
December 14, 1981
Date of Patent:
April 23, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Aschwanden, Quirico Branca, Emilio Kyburz, Rudolf Pfister
Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.
Abstract: Phenoxycarboxylic acids of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Z and n are as hereinafter set forth, are as described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.
Type:
Grant
Filed:
January 24, 1983
Date of Patent:
March 26, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Matthew Carson, Ronald A. LeMahieu, William C. Nason
Abstract: Racemic carboxylic acids are resolved into their enantiomers using optically active enantiomers of four lactones as resolving agents. The four lactones are 2,3-isopropylidene-ribonic acid-1,4-lactone, 1,2-isopropylideneglucofuranurono-3,6-lactone, 2-hydroxy-3,3-dimethyl-1,4-butyrolactone and 3,4-isopropylidene-arabino-1,5-lactone. Novel diastereoisomeric esters of the acids with the lactones are disclosed.
Abstract: The present disclosure relates to the use of thromboxane synthase inhibitors as antiobesity agents and insulin lowering agents. Such compounds fall into a variety of classes among which are 1-substituted imidazoles, 4-substituted imidazoles, 3-substituted pyridines, 3-substituted indoles, 4-substituted pyrimidines, 5-substituted tetrazoles, pyrazolidines, quinazolines, and substituted xanthene carboxylic acids.
Type:
Grant
Filed:
June 11, 1982
Date of Patent:
February 19, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
James G. Hamilton, Ann C. Sullivan, Lawrence D. Tobias, Joseph Triscari
Abstract: Imidazole derivatives of the formula ##STR1## wherein X is hydrogen or C.sub.1-4 -alkyl, Y is sulfur, sulfinyl or sulfonyl and Z is thienyl, optionally substituted by methyl or fluorine, or a group of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, methyl, fluorine, hydroxy, methoxy, methylthio or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy or one of R.sup.1, R.sup.2 and R.sup.3 is mono- or di-(C.sub.1-4 -alkyl)-amino and the other two are hydrogen,and physiologically or pharmaceutically compatible or acceptable acid addition salts thereof, are described. The compounds of formula I inhibit the aggregation of the blood platelets and have antihyperglycemic activity.
Abstract: The present disclosure is directed to 5-oxo- or methylene 17.beta.-hydroxy saturated or unsaturated deA-steroids wherein the 17.alpha.-position contains a propionic acid or propanol substituent and derivatives thereof wherein the hydroxy group at the 17-position forms a lactone ring with the carboxy substituent when the substituent at position 21 is carboxy. The deA-steroids and derivatives of the present disclosure are useful as potassium-sparing diuretics or for flushing oedemas.
Type:
Grant
Filed:
October 4, 1982
Date of Patent:
January 8, 1985
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Andor Furst, Peter Keller, Marcel Muller
Abstract: The preparation of bicyclic diketones of the formula ##STR1## wherein R.sub.1 is lower alkyl or ar-lower alkyl, from compounds of the formula ##STR2## wherein R.sub.1 is as set forth above, is described.
Abstract: The invention is directed to substituted phosphinic and phosphonic acids, a process for the preparation thereof and the use thereof for the treatment of inflammatory conditions, degenerative joint diseases and Wilson's disease.
Abstract: A process for the Raney nickel desulfurization of penicillins is described. In the process of the invention, amino penicillanic acid or derivatives thereof are reacted with Raney nickel under controlled conditions of temperature and time to yield azetidinones which are useful as intermediates for the synthesis of monocyclic beta-lactam antibiotics.
Abstract: The present invention relates to chlorocitric acids of the formula ##STR1## and stereoisomers, optical antipodes and pharmaceutically acceptable salts thereof, to methods of preparation thereof, including intermediates involved therein, and to their use as anorectic agents for the treatment of obesity in mammals.
Type:
Grant
Filed:
August 7, 1981
Date of Patent:
April 17, 1984
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Robert W. Guthrie, Richard W. Kierstead, Francis A. Mennona, Ann C. Sullivan
Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.