Abstract: Novel 3-(butylamino) or (1-pyrrolidinyl)-4-phenoxy-5-sulfamylbenzoic acid derivatives where the butyl group contains either a double bond or a hydroxy, ketone, acid or ester functional group or groups, said compounds being useful as diuretics.
Abstract: A process to produce diazepine-3-carboxylates of the formula ##STR1## is selected from the group consisting of ##STR2## R.sub.6 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, and lower alkanoyl;R.sub.4 is lower alkyl; R.sub.3 is selected from the group consisting of phenyl, mono-substituted phenyl, disubstituted phenyl, pyridyl and mono-substituted pyridyl; and R.sub.2 is hydrogen or lower alkyl which comprises reacting a compound of the formula ##STR3## wherein R.sub.1 is of the formula ##STR4## AND R.sub.5 is lower alkyl with a compound of the formulaN.dbd.C-CH.sub.2 --COOR.sub.4in the presence of a base sufficiently strong to generate the anion of the isocyanoacetate.
Abstract: Analogs of human .beta.-endorphin having a phenylalanine at position 27 and glycine at position 31 are disclosed. The subject analogs exhibit potent analgesic activity.
Abstract: Thymosin .alpha..sub.1, was chemically synthesized by the fragment condensation of the protected amino terminal tetradecapeptide with the protected carboxyl terminal tetradecapeptide. Similarly prepared was the analog [Asn.sup.2 ]-thymosin .alpha..sub.1 utilizing the appropriately modified protected amino terminal tetradecapeptide. Both products are active as agents which affect regulation, differentiation and function of thymus dependent lymphocytes (T cells).
Abstract: A liquid chromatography system comprises the following major components in combination: gas pressurized buffer reservoirs, automatic buffer selection valve, mixer/debubbler chamber, pump means, automatic sample valve, chromatography column, detector and fraction collector.
Abstract: The increase of bile flow and the decrease of the levels of lipids such as cholesterol and triglyceride is obtained in biological systems by utilizing specific 3 .alpha.,12.alpha. dihydroxy cholane derivatives and the non-toxic salts of these derivatives.
Type:
Grant
Filed:
April 22, 1977
Date of Patent:
September 26, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Hugo Gallo-Torres, James Guthrie Hamilton, Ann Clare Sullivan
Abstract: Novel 9-substituted or unsubstituted thienyl-3,7-dimethyl-nona-2,4,6,8-tetraene derivatives, useful as antitumor agents as well as processes for their preparation and novel intermediates are disclosed.
Type:
Grant
Filed:
May 31, 1977
Date of Patent:
September 26, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Josef Klaus, Beverly Ann Pawson
Abstract: A self-centering rotatable closure retainer adapted for use with a conventional cylindrical primary container cap is disclosed. The retainer comprises a support to which three or more radially inwardly projecting flexible ribs are attached so that they tangentially engage the outer wall of the cap frictionally securing the retainer to the cap. The self-centering closure retainer can be readily rotated about and removed from the primary cap without disturbing the cap.
Abstract: 2,4-Diaminopyrimidines bearing a substituted benzyl group in position-1 are prepared from the correspondingly substituted .alpha.-alkoxymethylcinnamonitrile by treatment of the latter with an alkali metal alkoxide in mono-methyl ether of ethylene glycol and subsequently reacting the resulting reaction mixture with guanidine.
Abstract: Ribofuranoysl-imidazole derivatives of the formula ##STR1## wherein R, X, Y and Z have one of the meanings set forth hereinafter, are described. The ribofuranosyl-imidazole derivatives have cardiac and circulatory-dynamic properties and are useful in the treatment of angina pectoris.
Abstract: L-2-amino-4-(2-aminoethoxy)-butanoic acid, methods for its preparation and novel intermediates employed in these processes are disclosed. L-2-amino-4-(2-aminoethoxy)-butanoic acid enhances ethylene production in fruit and therefore has utility as a ripening agent and as an abscission agent.
Abstract: A method for the homogeneous catalytic enantioselective hydrogenation of alkyl and alkenyl substituted acrylic acids wherein these acids are selectively hydrogenated at the double bond alpha, beta to the acid function, said hydrogenations are catalyzed by rhodium complexes of chiral tertiary phosphines. This method provides a route to chiral dihydrogeranic acid and other intermediates useful in the synthesis of chiral vitamin E, citronellal, and menthol. Novel chiral tertiary phosphines are also disclosed.
Abstract: Antihypertensively active thiourea derivatives of the formulas ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and X are as hereinafter described, as well as a method of using a compound of the formula ##STR2## wherein R.sub.1 ', R.sub.2 ', R.sub.3 and X are as previously described, or a compound of formula II as an anti-hypertensive agent, is described.
Type:
Grant
Filed:
October 25, 1977
Date of Patent:
September 12, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Robert Cohen, Richard Wightman Kierstead, Jefferson Wright Tilley
Abstract: Levo-rotary 3-phenoxy N-substituted morphinans and derivatives thereof useful as analgesics and/or narcotic antagonists and their preparation form (-)-3-hydroxy-N-lower alkyl morphinan including intermediates in this preparation.
Abstract: Novel 1,5-benzodiazepin-4-one derivatives, bearing between the 1,2-positions a triazolo ring, as disclosed. These 1,2-triazolo-1,5-benzodiazepin-4-ones are useful as muscle-relaxant, anti-convulsant and sedative agents.
Type:
Grant
Filed:
December 15, 1977
Date of Patent:
September 5, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Rodney Ian Fryer, Leo Henryk Sternbach, Armin Walser
Abstract: A synthesis of 2,6,10-trimethyl-undecan-1-ol, an intermediate for producing vitamin E, from methacrolein, crotonaldehyde, .beta.-hydroxy-isobutyric acid including intermediates in this synthesis.
Abstract: Angiotensin I and iodinated angiotensin I solutions are stabilized against enzymatic degradation by the addition of phenylmethylsulfonyl fluoride (PMSK). Such solutions are used as standards and reagents in immunoassay kits for determinatin of plasma renin levels. Stabilized solutions prepared in accordance with this disclosure can be shipped at ambient temperature which represents a substantial advantage in convenience over previously available solutions of angiotensin I and radioiodinated angiotensin I.
Type:
Grant
Filed:
February 22, 1977
Date of Patent:
September 5, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Bruce Charles Farrenkopf, Magdalena Usategui Gomez