Patents Represented by Attorney Samuel L. Welt
  • Patent number: 4226865
    Abstract: Thiobenzamides of the formula ##STR1## wherein X' is bromine, fluorine, iodine, trifluoromethyl or C.sub.3-4 alkyl prepared from N-(2-aminoethyl)-morpholine and a compound of the formula ##STR2## wherein X' is as hereinbefore set forth and;Y is methoxy or ethoxy are described. The end products, including p-chloro-N-(2-morpholinoethyl)-thiobenzamide, are useful in the treatment of depressive conditions, that is, are useful as antidepressants.
    Type: Grant
    Filed: May 19, 1978
    Date of Patent: October 7, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Willy Burkard, Pierre-Charles Wyss
  • Patent number: 4131655
    Abstract: D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.
    Type: Grant
    Filed: April 20, 1978
    Date of Patent: December 26, 1978
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Andor Furst, Marcel Muller, Ulrich Kerb, Rudolf Wiechert
  • Patent number: 4127736
    Abstract: An asymmetric synthesis of optically active prostaglandin F.sub.2.alpha. from cyclopentadiene including intermediates in this synthesis.
    Type: Grant
    Filed: September 19, 1977
    Date of Patent: November 28, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Naresh K. Chadha, John J. Partridge, Jr., Milan R. Uskokovic
  • Patent number: 4126503
    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 29, 1977
    Date of Patent: November 21, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: William E. Gardner
  • Patent number: 4126502
    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 29, 1977
    Date of Patent: November 21, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dennis J. Dabal, Joseph J. Williams
  • Patent number: 4125726
    Abstract: Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is selected from the group consisting of lower alkylthio together with the sulfoxide and sulfone thereof, halo, lower alkylamino or lower alkoxy; Y is oxo or thio; R.sub.3 is selected from the group consisting of hydrogen, --COOR.sub.4 wherein R.sub.4 is hydrogen or lower alkyl, --CONR.sub.6 R.sub.5 wherein R.sub.5 and R.sub.6 are hydrogen or lower alkyl; X is hydrogen or halogen; and R.sub.7 is lower alkyl or hydrogen and the pharmaceutically acceptable salts and N-oxides thereof.Also presented are processes to produce the above compounds and intermediates therefor and derivatives thereof.
    Type: Grant
    Filed: March 11, 1977
    Date of Patent: November 14, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
  • Patent number: 4124598
    Abstract: New psoralen compounds have been synthesized. The compounds all include the addition of substituent groups at the 4' position on the basic trioxsalen structure. Specifically, the compounds have the structure: ##STR1## wherein X may be any desired substituent such as halogenated alkyls, alcohols, ethers, aminoalkyls, etc. The new substituted psoralens exhibit high solubility in aqueous solution and low dissociation constants from deoxyribonucleic acid (DNA), as well as a reactivity with ribonucleic acids (RNA). Such psoralen compounds find use in the study of secondary structures of nucleic acids; as inhibitors of RNA replication; in the inactivation of viruses; and in the photo chemotherapy of psoriasis.
    Type: Grant
    Filed: October 20, 1976
    Date of Patent: November 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John E. Hearst, Henry Rapoport, Stephen Isaacs, Che-Kun J. Shen
  • Patent number: 4124757
    Abstract: 2,2'-Anhydro-1.beta.-D-arabinofuranosyl-5-fluorocytosine (hereafter AAFC) and its acid addition salts are known compounds. AAFC may now be conveniently prepared in extremely high yield by selective acid catalyzed hydrolysis of the corresponding 3'-O-acyl analogs of AAFC which unexpectedly hydrolyzes at the acyl group while the 2,2'-anhydro linkage remains intact.
    Type: Grant
    Filed: January 11, 1973
    Date of Patent: November 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Max Hoffer
  • Patent number: 4124595
    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: September 26, 1977
    Date of Patent: November 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pasquale N. Confalone, Elizabeth D. Lollar, Giacomo Pizzolato, Milan R. Uskokovic
  • Patent number: 4124619
    Abstract: Preparation of carboxylic acid esters of .gamma.-hydroxy-tiglic-aldehyde from bismonocarboxylic acid esters of but-2-en-1,4-diol via 1,4-diacetoxy-2-formyl butane including intermediates in this synthesis.
    Type: Grant
    Filed: March 23, 1977
    Date of Patent: November 7, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter Fitton, Harold Moffet
  • Patent number: 4123553
    Abstract: A method is disclosed for controlling liver fluke infections comprising orally administering to host animals an anthelmintically effective amount of a compound selected from a group of halogen-substituted-benzenesulfonanilides represented by the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently chlorine or bromine, R.sub.3 is hydrogen or chlorine and each of R.sub.4 through R.sub.7 is independently hydrogen, halogen or trifluoromethyl, with the proviso that at least 2 of R.sub.3 through R.sub.7 is other than hydrogen and X is hydrogen or lower alkanoyl.
    Type: Grant
    Filed: March 7, 1977
    Date of Patent: October 31, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Milan Mitrovic, Terence J. Hayes
  • Patent number: 4123464
    Abstract: A multi-step process for the preparation of alpha,beta-unsaturated aliphatic aldehydes such as citral by first reacting an allylic alcohol with a butadienyl ether, or a corresponding acrolein derivative or its acetal, including novel intermediates in this process.
    Type: Grant
    Filed: December 30, 1976
    Date of Patent: October 31, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Willy Leimgruber, Donald H. Valentine, Jr.
  • Patent number: 4123465
    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.
    Type: Grant
    Filed: August 10, 1977
    Date of Patent: October 31, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Donald H. Valentine, Jr.
  • Patent number: 4122252
    Abstract: The present invention relates to a process for the manufacture of esters. More particularly, the invention is concerned with a process for the manufacture of esters of 2,2'-anhydro-1.beta.-D-arabinofuranosyl-5-fluorocytosine.
    Type: Grant
    Filed: November 30, 1977
    Date of Patent: October 24, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard D'Souza, Pierre-Charles Wyss
  • Patent number: 4120870
    Abstract: Group IB and IIB metal phosphine complexes are disclosed. These complexes are reacted with rhodium complex precursors to form useful enantioselective hydrogenation catalysts. Also disclosed is a method of preparing useful compounds having optical activity such as natural products and compounds useful as flavors and fragrances.
    Type: Grant
    Filed: July 18, 1977
    Date of Patent: October 17, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John Melvin Townsend, Donald Herman Valentine, Jr.
  • Patent number: 4120974
    Abstract: There is disclosed herein a novel compound, 6,7-epoxy-1-(p-ethylphenoxy)-3,4,7-trimethyl-nonane, which synergizes the insect regulation activity of 6,7-epoxy-1-(p-ethylphenoxy)-3-ethyl-7-methyl-nonane.
    Type: Grant
    Filed: December 27, 1976
    Date of Patent: October 17, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Frater, Albert Pfiffner, Milos Suchy, Rene Zurfluh
  • Patent number: 4121289
    Abstract: There is disclosed a method for standardizing, in terms of a pre-established range of acceptable in vitro release and/or in vivo response, production of tabletted formulations which have a dependency on tablet hardness, through control of the maximum tabletting compression force developed by the tablet press employed, and for providing an individual momentary as well as permanent readout in digital form of the maximum compression force developed for each tabletting event. One or more tablets are compressed from a particular batch of formulation at selected different press compression force settings. These tablets are processed to derive data regarding in vitro release and/or in vivo response with a determination of an optimum value being made directly from or by interpolation of the resulting data. This optimum value is correlated to a press setting and the press is then set thereat for the tabletting of the bulk of the batch of formulation.
    Type: Grant
    Filed: December 14, 1976
    Date of Patent: October 17, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Donald Melvyn Stiel
  • Patent number: 4119647
    Abstract: 25-Hydroxycholecalciferol-23,24-.sup.3 H and process for the preparation thereof are disclosed. 25-Hydroxycholecalciferol-23,24-.sup.3 H is useful in radioimmunoassay for the detection of 25-hydroxycholecalciferol, a physiologically important metabolite of cholecalciferol (vitamin D.sub.3).
    Type: Grant
    Filed: April 11, 1977
    Date of Patent: October 10, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arnold Alvin Liebman, Richard Robert Muccino
  • Patent number: 4118386
    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.
    Type: Grant
    Filed: April 4, 1977
    Date of Patent: October 3, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: RE29842
    Abstract: An untriakontapeptide having significant opiate agonist activity has been isolated from camel pituitary glands. The structure of this peptide has been determined and this peptide was then synthesized utilizing solid phase peptide synthesis. Both natural and synthetic material show identical physical and biological properties.
    Type: Grant
    Filed: August 8, 1977
    Date of Patent: November 21, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Choh H. Li