Abstract: The present invention comprehends a method for treating diarrhea comprising administering to an animal in need of anti-diarrheal treatment an effective antidiarrheal amount of a compound of the formula ##STR1## AND ACID ADDITION SALTS THEREOF WHEREIN Y is alkylene containing 1-4 carbon atoms; R.sub.2 and R.sub.3 together with N is a heterocyclic ring system comprising azamonocyclic ring of the formula ##STR2## wherein Z is phenylhydroxymethylmethylene, phenylhydroxymethylene, phenylcarboxymethylene, phenylcarbalkoxymethylene or azabicycloalkyl or phenyl or hydroxyl substituted azabicycloalkyl containing 6-9 carbon atoms and containing at least 5 atoms in each ring of the azabicycloalkyl or 4-azatricyclo[4.3.1.1.sup.3,8 ]undec-4-yl; Ar.sub.1 and Ar.sub.2 are phenyl, halo-substituted phenyl, (lower alkyl) substituted phenyl, pyridyl, thienyl or furyl, and Ar.sub.
Type:
Grant
Filed:
April 16, 1975
Date of Patent:
December 21, 1976
Assignee:
G. D. Searle & Co.
Inventors:
Gilbert W. Adelstein, Esam Z. Dajani, Chung Hwai Yen
Abstract: A new composition of matter, (+) 3-acetoxy- quinuclidine and its salts, ophthalmic compositions comprising this compound or any of its physiologically acceptable salts in a suitable carrier such as a phosphate buffer, and a process of preparation of the active ingredients, which comprises esterifying quinuclidinol so as to obtain racemic 3-lower-alkoxy quinuclidine, subjecting same to enzymatic hydrolysis by a cholinesterase so as to selectively hydrolyze the (-) isomer, separating the unchanged (+) lower-alkoxy quinuclidine, hydrolyzing the latter and esterifying it to the desired compound. Amongst various homolophes the preferred compound is (+)3-acetoxy quinuclidine as this is pharmaceutically the most potent one.
Abstract: The present invention relates to novel 1,5-dithia-2,4,6,8-tetra-aza-cyclooctane-1,1,5,5-tetraoxides of the formula: ##STR1## wherein R represents halogen or a (lower) alkylsulphonyl radical,R.sub.1 represents hydrogen or chlorine.The compounds according to the present invention exert valuable bacteriostatic, bactericidal, virostatic, cytostatic and immunosuppressive activities.
Type:
Grant
Filed:
November 14, 1975
Date of Patent:
December 7, 1976
Assignee:
Chem. Pharmaz. Fabrik Dr. Hermann Thiemann GmbH
Abstract: A photographic color coupler consisting of a phenolic compound having in the 2-position the radical ##STR1## wherein Y is an amide or a sulfonamide bridging radical and wherein R is aryl or alkyl.
Type:
Grant
Filed:
January 7, 1971
Date of Patent:
December 7, 1976
Assignee:
Minnesota Mining and Manufacturing Company
Abstract: A process for resolving racemic .alpha.-hydroxy-.beta.,.beta.-dimethyl-.gamma.-butyrolactone, referred to as D,L-pantolactone, into its optical antipodes, based on the separation of diastereomeric salts of D,L-pantoic acid (.alpha.,.gamma.-dihydroxy-.beta.,.beta.-dimethylbutyric acid), produced from D,L-pantolactone, by means of (-)-3-aminomethylpinane, (+)-3-aminomethylpinane or one of their acid addition salts, as a new resolving agent.
Type:
Grant
Filed:
January 24, 1975
Date of Patent:
December 7, 1976
Assignee:
BASF Aktiengesellschaft
Inventors:
Werner Hoffmann, Walter Himmele, Joachim Paust, Karl Von Fraunberg, Hardo Siegel, Sigberg Pfohl
Abstract: Ester and amide derivatives of three-hydroxycitric acid .gamma.-lactone inhibit fatty acid synthesis in biological systems and are useful in the treatment of obesity and in correcting conditions of lipid abnormalities.
Type:
Grant
Filed:
August 1, 1975
Date of Patent:
November 30, 1976
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Robert William Guthrie, Richard Wightman Kierstead
Abstract: Novel 4-(3,5-dialkyl-4-hydroxyphenyl)-1,2-dithiole-3-thiones are used as additives for organic materials. They are prepared by reacting a corresponding alkylated phenol with sulfur and if necessary reacting the resulting compound with sodium disulphide and then with a corresponding halide.
Type:
Grant
Filed:
June 18, 1974
Date of Patent:
November 30, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
John Grey Dingwall, Peter Miles, Donald Richard Randell
Abstract: A variety of substances are reported which alter host resistance to cocci and bacilli bacterial infections. Nevertheless, because of the extreme difficulty of total eradication, and the frequent reappearance of the same strains, even after their apparently successful elimination, there is a continuing need for drugs for the treatment of coccic infections. Certain guanidinoacylhistidines are effective in inducing resistance to infections due to cocci and bacilli.
Abstract: There is described 1,8-naphthyridin-2(1H)-one compounds with bronchodilating and hypotensive properties prepared by reaction of 2,6-diaminopyridine with an appropriate .beta.-diketone providing a 2-aminonaphthyridine compound which upon treatment with nitrous acid is converted to the 2-oxo product. Alternatively, an appropriate .beta.-diketone can be reacted with an alkyl alkoxycarbonylacetimidate, the alkyl 2-aminonicotinate thus formed converted to the hydrazide, which upon treatment with a sulfonyl halide forms the N-sulfonyl hydrazide derivative. This intermediate is reacted with an alkali metal carbonate to provide the 2-aminonicotinaldehyde which upon reaction with an ester of a substituted aliphatic carboxylic acid provides the desired product. In some cases the aminonicotinaldehyde is generated in situ in the presence of the ester thereby giving the desired product in one step from the N-sulfonyl hydrazide derivative.
Type:
Grant
Filed:
February 20, 1975
Date of Patent:
November 23, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Clarence Stanley Rooney, Haydn Windsor Richard Williams, Burton Kendall Wasson
Abstract: In the synthesis of gamma butyrolactones by reaction of an olefin with acetic acid in the presence of a reducible metal ion M of higher-valent form, such as manganic ion Mn.sup.+.sup.+.sup.+, the lactone product is recovered and coincidently therewith the metal ion M, in reduced form, is regenerated to its higher-valent form and recycled.
Abstract: Process for synthesizing a prostaglandin from a hexahydro-4-(lower alkoxy)-2H-oxireno[3,4]cyclopenta[1,2-b]furan, utilizing as an intermediate in the process a hexahydro-5-hydroxy-2-lower alkoxy-2H-cyclopentab]furan-4-carboxaldehyde, and the novel cyclopenta(b)furan intermediates of the process.
Type:
Grant
Filed:
September 10, 1975
Date of Patent:
November 9, 1976
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hans Johann Mayer, Albert Eduard Fischli, Michael Josef Klaus, Alexander Eduard Wick
Abstract: Thianthrene in monochlorotoluene, is reacted with excess chlorine in the presence of a Lewis acid catalyst, to yield a mixture of chlorothianthrenes, the major component of which is 2,3,7,8-tetrachlorothianthrene. Recrystallization of the chlorothianthrene mixture from a suitable solvent, such as tetrahydrofuran yields 2,3,7,8-tetrachlorothianthrene of greater than 90 percent purity.
Type:
Grant
Filed:
August 1, 1975
Date of Patent:
November 2, 1976
Assignee:
Hooker Chemicals & Plastics Corporation
Inventors:
Harry E. Buckholtz, Arun C. Bose, John C. Graham
Abstract: A new class of organic chemical compounds [1]benzothieno[3,2-b]furans, are made by O-alkylation of 3-hydroxybenzo[b]thiophene-2-carboxylates with alkyl haloacetates, haloacetonitriles or .alpha.-halomethyl alkyl ketones, followed by cyclization of the intermediate products with alkali metals or alkali metal alkoxides. The compounds are antimicrobials.
Abstract: 7-Methoxy-6-thiatetracyclines of the formula ##SPC1##Wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are H or alkyl of 1 to 4 carbon atoms, and the physiologically acceptable acid addition salts thereof.
Type:
Grant
Filed:
July 30, 1975
Date of Patent:
October 26, 1976
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Werner Rogalski, Richard Kirchlechner, Juergen Seubert, Rudolf Gottschlich, Walter Hameister, Rolf Bergmann, Helmut Wahlig
Abstract: Dibenzo[b,e]thiepin derivatives of the formula ##SPC1##Wherein X is sulfur or sulfonyl and R is hydrogen or methyl, are described. The compounds of formula I are useful as diuretic agents.
Abstract: 6-Oxo-7,7-disubstituted-1,2,7,8-tetrahydro (and 7,8-dihydro)-6H-indeno-[5,4-b]furan (and thiophene)carboxylic acids, the salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
Type:
Grant
Filed:
February 24, 1975
Date of Patent:
October 5, 1976
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: Physiologically active substances ML-236 of the formula ##SPC1##Wherein R is hydrogen atom, hydroxy group or 2-methylbutyryloxy group having cholesterol- and lipid-lowering effects in blood and liver and thus utility as hypocholesteremic and hypolipemic medicaments. They are obtained by cultivation of an ML-236-producing microorganism belonging to the genus Penicillium in a culture medium and subsequent recovery thereof from a cultured broth.
Abstract: Chain extended polyurethanes are prepared, using certain 3-(hydroxyhydrocarbylsecondaryamino)thiophene 1,1-dioxides, some of which are new chemicals. E.g., 3-(2-hydroxypropylamino)tetrahydrothiophene 1,1-dioxide is especially useful as a chain extender for high resiliency, flexible polyurethane foams.