Abstract: Process for synthesizing the lactone, (dl) 3,3a beta-4,5-6,6a beta-hexahydro-4beta(3-hydroxyl-1-trans-octenyl)-5alpha-hydroxy-2-oxo-2H-c yclopenta[b]furan, a known intermediate for producing prostaglandin E.sub.2 and F.sub.2.alpha. and a process for preparing 11-desoxy and 11-alkyl prostaglandins from dihydroresorcyclic acid.
Abstract: A new antibiotic, designated as antibiotic 1745A/X, is produced by the fermentation of the known microorganism Streptomyces antibioticus, ATCC 11891, using the novel compound erythronolide A oxime as the substrate. This new antibiotic is useful as an antibacterial agent.
Type:
Grant
Filed:
February 28, 1977
Date of Patent:
January 24, 1978
Assignee:
Hoffmann-La Roche, Inc.
Inventors:
Ronald A. LeMahieu, Richard W. Kierstead, David L. Pruess
Abstract: New hapten compositions useful in preparing antigens which may be employed in eliciting antibodies useful in immunoassay, particularly radioimmunoassay for propranolol. Utilizing an enantiomer in formation of the hapten allows preparation of an antibody which is able to discriminate between enantiomers selectively.
Abstract: An improved method and apparatus for reducing the echoes from reflectors disposed outside the focal line in an echo-sounding process using an ultrasonic field focusing in a focal line. A pulsed ultrasonic wave is transmitted having a cross-sectional area corresponding to one or more annularly arranged transducer segments having a total azimuth angle of less than 360.degree.. Echoes of the transmitted wave are received from the spatial region corresponding to at least a part of other annular transducer segments, which complement the annular segments of the cross-sectional area of the transmitted ultrasonic pulse to form a complete ring. The radiation or receiving surfaces of the transducer segments forming the transducer ring are inclined toward the axis of the ring.
Type:
Grant
Filed:
April 7, 1976
Date of Patent:
January 17, 1978
Assignee:
Hoffmann-La Roche, Inc.
Inventors:
Christoph Benedikt Burckhardt, Pierre-Andre Grandchamp, Heinz Hoffmann
Abstract: This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C-R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl groupAnd acid addition salts thereof.
Type:
Grant
Filed:
November 11, 1976
Date of Patent:
January 17, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Cedric Herbert Hassall, William Henry Johnson, Antonin Krohn, Carey Ernest Smithen, William Anthony Thomas
Abstract: Pharmaceutical dosage forms comprising an edible web having deposited thereon or at least partially thereon a particulate medicament, the webs being thereafter fabricated and finished to pharmaceutically elegant solid dosage forms having no medicament exposed on an exterior surface. The dosage forms have a consistency of release of medicament which can be controlled to exacting specifications. The disclosed solid dosage forms are prepared by high speed automated equipment and the process by which they are made is characterized by non-destructive quality control analysis and performance evaluation both conducted on-line and integrated into the manufacturing operation. Included in the scope of the disclosed invention are certain apparatus and methods of manufacture.
Type:
Grant
Filed:
April 4, 1977
Date of Patent:
January 17, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur Roman Mlodozeniec, Lawrence Samuel White
Abstract: Pharmaceutical dosage forms comprising an edible web having deposited thereon or at least partially thereon a particulate medicament, the webs being thereafter fabricated and finished to pharmaceutically elegant solid dosage forms having no medicament exposed on an exterior surface. The dosage forms have a consistency of release of medicament which can be controlled to exacting specifications. The disclosed solid dosage forms are prepared by high speed automated equipment and the process by which they are made is characterized by non-destructive quality control analysis and performance evaluation both conducted on-line and integrated into the manufacturing operation. Included in the scope of the disclosed invention are certain apparatus and methods of manufacture.
Abstract: There is disclosed a highly accurate counting and handling arrangement particularly adaptable to large-volume, high-speed multiple-output apparatus producing discrete, solid particular objects, such as tablets. Sensing means, preferably retroreflective optical sensors, fluidic sensors or strain-gauge sensing arrangements, are employed in associated with existing apparatus to detect each object at the point where the objects are substantially completely formed. The signals generated by the individual sensors are received by a control counter arrangement which provides a continuous separate displayed counting for each sensor employed. The control counter arrangement has provision for separately presetting the maximum desired count of sensed objects for each sensor employed.
Type:
Grant
Filed:
October 16, 1975
Date of Patent:
January 10, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jim Mills Adams, Edward Francis DEZabala
Abstract: An improved process for the preparation of 6,6-alkylenedioxyalkan-2-ones starting from alkyl vinyl ketones and alkyl acetoacetates is disclosed. The 6,6-alkylenedioxyalkan-2-ones are useful as intermediates in the total synthesis of therapeutically valuable steroids.
Type:
Grant
Filed:
May 3, 1976
Date of Patent:
January 10, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Urs Oskar Hengartner, Pius Anton Wehrli
Abstract: Plant growth regulant compositions containing as the active ingredients copper (II) complexes of 2,3:4,6-di-O-(substituted)-alpha-L-xylo-2-hexulofuranosonic acid and, preferably, copper (II) 2,3:4,6-di-O-isopropylidene-alpha-L-xylo-2-hexulofuranosonate monohydrate and tripyridine copper (II) 2,3:4,6-di-O-isopropylidene-alpha-L-xylo-2-hexulofuranosonate, are described.
Abstract: A Tc-99m stannous sulfur colloid radiopharmaceutical having simplicity of formulation, improved stability and desirable small particle size as well as a method of preparation therefor are described. Also provided is a reagent suitable for the preparation of such radiopharmaceutical by the addition thereto of technetium-99m pertechnetate.
Abstract: Phenyl-pyrimidines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are as hereinafter set forth, are described. The end products are useful as liquid crystals.
Type:
Grant
Filed:
September 8, 1976
Date of Patent:
January 3, 1978
Assignee:
Hoffman-La Roche Inc.
Inventors:
Arthur Boller, Marco Cereghetti, Hanspeter Scherrer
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:
January 27, 1977
Date of Patent:
January 3, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Robert Cohen, Richard Wightman Kierstead, Jefferson Wright Tilley
Abstract: There is disclosed a highly accurate counting and handling arrangement particularly adaptable to large-volume, high-speed multiple-output apparatus producing discrete, solid particular objects, such as tablets. Sensing means, preferably retroreflective optical sensors, fluidic sensors or strain-gauge sensing arrangements, are employed in associated with existing apparatus to detect each object at the point where the objects are substantially completely formed. The signals generated by the individual sensors are received by a control counter arrangement which provides a continuous separate displayed counting for each sensor employed. The control counter arrangement has provision for separately presetting the maximum desired count of sensed objects for each sensor employed.
Type:
Grant
Filed:
November 17, 1975
Date of Patent:
January 3, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jim Mills Adams, Edward Francis DEZabala
Abstract: A process for the preparation of heterocyclic compounds containing one nitrogen atom and novel 2,3,4,5-tetrahydro-1H-3-benzazepines prepared by this process are disclosed. The resulting heterocyclic compounds, including the novel 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives, exhibit analgesic, appetite suppressant, and anti-edema activity.
Type:
Grant
Filed:
June 20, 1975
Date of Patent:
December 27, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arnold Brossi, Benjamin Pecherer, Robert Sunbury
Abstract: A process for the preparation of 9,10-seco-steroids of the formula ##STR1## WHEREIN R.sup.1 and R.sup.2 independently are hydrogen, amino, OR.sup.5, OCOR.sup.6 or NHCOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl and R.sup.6 is lower alkyl or phenyl; R.sup.3 is lower alkyl; R.sup.4 is oxo, ##STR2## wherein R.sup.13 is lower alkyl, lower alkoxy -- lower alkylene, tetrahydropyranyl or tetrahydrofuryl, R.sup.14 is lower alkyl or aryl and R.sup.15 and R.sup.16 are lower alkyl or taken together form lower alkylene or arylene, and n is 1 or 2 is disclosed. The 9,10-seco-steroids of this invention are useful intermediates for the preparation of steroids.
Type:
Grant
Filed:
January 23, 1976
Date of Patent:
December 20, 1977
Assignee:
Hoffmann-La Roche, Inc.
Inventors:
Jean-Marie Cassal, Andor Furst, Werner Meier
Abstract: A novel process for the preparation of biotin is disclosed wherein said process employs inexpensive starting materials and reagents resulting in the obtention of biotin devoid of the biologically inactive stereoisomers.
Type:
Grant
Filed:
February 23, 1977
Date of Patent:
December 13, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Pasquale Nicholas Confalone, Elizabeth Dianne Lollar, Giacomo Pizzolato, Milan Radoje Uskokovic
Abstract: Compounds of the formula ##STR1## wherein when X is nitrogen, Y and Z are --CH--; or when Y is nitrogen, X and Z are --CH--; or when Z is nitrogen, X and Y are --CH--; and one of R.sub.1 and R.sub.2 is cyano and the other is straight-chain alkyl of 1 to 7 carbon atoms, straight-chain alkoxy of 1 to 7 carbon atoms or straight-chain alkanoyloxy of 2 to 7 carbon atoms,Prepared by a variety of methods, are described. The compounds of the invention are useful as components of nematic mixtures.
Type:
Grant
Filed:
August 30, 1976
Date of Patent:
December 13, 1977
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Arthur Boller, Marco Cereghetti, Hanspeter Scherrer