Abstract: The present invention relates to a method of preventing milk fever which comprises administering to a preparturient female ruminant an effective amount of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol.
Type:
Grant
Filed:
May 17, 1982
Date of Patent:
July 8, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alfred Boris, John J. Partridge, Milan R. Uskokovic
Abstract: Aqueous solutions of antibacterially active sulfonamides and sulfonamide potentiators, which are suitable for parenteral administration and which contain no organic solvent, are prepared by reacting a sulfonamide RH with an aldehyde R.sup.1 CHO to give a compound of the formula R.sup.1 CH(R).sub.2 and dissolving said compound in water together with the sulfonamide potentiator.
Abstract: A compound of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, alkaline earth metal or alkali metal; or magnesium halide salts thereof, useful as intermediates for unsaturated eicosanoic acids and derivatives thereof which inhibit the synthesis of SRS-A.
Type:
Grant
Filed:
October 31, 1984
Date of Patent:
July 8, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Ka-Kong Chan, George W. Holland, Perry Rosen
Abstract: Novel compounds of the formula ##STR1## wherein A signifies the group ##STR2## or --(CH.sub.2).sub.5 --, which inhibit pancreas lipase and can be used for the control or prevention of obesity and hyperlipaemia, are disclosed. The inventive compounds can be produced by the cultivation of microorganism Streptomyces toxytricini, identified as NRRL 15443.
Type:
Grant
Filed:
June 18, 1984
Date of Patent:
July 1, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Paul Hadvary, Erich Hochuli, Ernst Kupfer, Hans Lengsfeld, Ernst K. Weibel
Abstract: A catalytic synthesis of chromans in racemic or optically active forms, including intermediates thereto; the synthesis employs an asymmetric palladium (II) catalyzed oxidative cyclization of a 2-homoallylphenol and provides intermediates useful in making chromans, especially vitamin E in racemic or optically active forms.
Abstract: A novel process for the manufacture of the furanone of the formula ##STR1## is described. In this process, a diol is firstly reacted with thionyl chloride, then the sulphite formed, optionally after oxidation to the corresponding sulphate, is treated with sodium cyanide and the resulting hydroxynitrile is hydrolyzed.The furanone of formula I can be used as a starting material for the manufacture of R-(-)-pantolactone.
Abstract: Compounds of the formula ##STR1## wherein B is --C.tbd.C-- or --CH.sub.2 CH.sub.2 --, R.sup.1 is straight-chain C.sub.1 -C.sub.12 -alkyl and R.sup.2 is straight-chain C.sub.1 -C.sub.12 -alkyl or straight-chain C.sub.1 -C.sub.12 -alkoxy, their manufacture and use in liquid crystalline mixtures are described.
Abstract: A method of treating inflammation which comprises topically administering to the affected area a compound of the formula ##STR1## or a pharmaceutically acceptable addition salt thereof, is described.
Type:
Grant
Filed:
February 9, 1984
Date of Patent:
June 17, 1986
Assignee:
Hoffmann-LaRoche Inc.
Inventors:
Alfred Boris, Robert W. Guthrie, Richard W. Kierstead
Abstract: Apparatus for sample transfer and analysis by centrifugation, comprising a rotor having rotary joints at its periphery, to which cuvette carriers are connected so as to be able to perform a tipping movement through an angle of 90.degree., a locking device for locking the cuvette carriers in an inclined position, and cuvette assemblies for use in the cuvette carriers, the rotor preferably being in the form of a rotary beam at the two ends of which two cuvette carriers are disposed, and the cuvette carrier is in the form of a comb so that the teeth engage between the cuvette rows of the cuvette assembly. This apparatus enables samples to be transferred without mixing the cuvette contents.
Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,25-dihydroxyergocalciferol as well as substantially pure and crystalline 1.alpha.,25-dihydroxyergocolciferol. The end-product 1.alpha.,25-dihydroxyergocalciferol is useful in the treatment of disease states which are characterized by insufficient amounts of 1.alpha., 25-dihydroxycholecalciferol.
Type:
Grant
Filed:
December 17, 1984
Date of Patent:
June 17, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Enrico G. Baggiolini, Andrew D. Batcho, Alfred Boris, Milan R. Uskokovic
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, X is hydrogen or halogen, and A is the group ##STR2## wherein R.sub.1 is hydrogen, acyl or lower alkyl, R.sub.2 is hydrogen or lower alkyl, m is an integer from 2 to 4, n is an integer from 1 to 3, and t is an integer from 1 to 5, provided that R.sub.1 is adjacent to --(CH.sub.2).sub.m --O(CH.sub.2).sub.m ].sub.n O--, and, when R.sub.2 is hydrogen, salts thereof with pharmaceutically acceptable bases, are described. The compounds of formula I are useful as agents for the treatment of allergic conditions.
Abstract: Compositions containing the antibiotic having the designation X-537A, useful for the treatment and prevention of coccidiosis in poultry feed compositions containing the antibiotic and methods of treating coccidiosis are disclosed.
Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol. The end-products, 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol, are useful for the treatment of disease states which are characterized by insufficient amounts of 1,25 dihydroxycholecalciferol.
Type:
Grant
Filed:
December 27, 1983
Date of Patent:
June 10, 1986
Assignee:
Hoffman-La Roche Inc.
Inventors:
Enrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
Abstract: The syntheses of 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol and 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol and the epimeric mixture which are useful as differentiation inducing agent and anti-proliferation agents are described. 25,26-dehydro-1.alpha.,24R-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,24S-dihydroxycholecalciferol, and the epimeric mixture are useful in treating osteoporosis, tumors and leukemia.
Type:
Grant
Filed:
November 29, 1984
Date of Patent:
June 10, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
John J. Partridge, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --,and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
Abstract: The invention relates to compounds of the formula ##STR1## wherein R is lower alkyl or a carboxy group or a group of the formula--(CH.sub.2).sub.n --OY ain which n stands for 1 or 2 and Y is hydrogen or alkyl and R.sup.Y and R.sup.z each are hydrogen or one of R.sup.Y and R.sup.z is hydrogen and the other is hydroxy,and pharmaceutically acceptable acid addition salts thereof.These compounds and salts possess antibiotic and antitumor activity and can be used as medicaments in the form of pharmaceutical preparations.
Type:
Grant
Filed:
December 17, 1984
Date of Patent:
May 27, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael J. Broadhurst, Cedric H. Hassall, Gareth J. Thomas
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:
December 12, 1984
Date of Patent:
May 27, 1986
Assignee:
Hoffmann-La Roche Inc.
Inventors:
James G. Hamilton, Ann C. Sullivan, Lawrence D. Tobias, Joseph Triscari
Abstract: The present invention relates to a novel polyether ionophore antibiotic of the formula ##STR1## and its pharmaceutically acceptable salts. The compound of formula I and its salts exhibit activity as an antibacterial agent and as an anticoccidial agent.
Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present,are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.
Abstract: This invention is directed to methods for and compositions useful in reducing sebum secretion utilizing 1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-[.alpha.-methylstyryl]naphthalene as an active ingredient.