Patents Represented by Attorney Samuel L. Welt
  • Patent number: 4054589
    Abstract: Novel 9-substituted phenyl-3,7-dimethyl-nona-2,4,6,8-tetraene derivatives useful as anti-tumor agents.
    Type: Grant
    Filed: September 15, 1975
    Date of Patent: October 18, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
  • Patent number: 4053486
    Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is a carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl-halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: October 11, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Zoltan George Hajos
  • Patent number: 4053459
    Abstract: A sensitive radioimmunoassay for methaqualone and its major metabolites is described. Included within this disclosure is the preparation of novel methaqualone haptens, the preparation of antigens from such haptens by coupling to an immunogenic carrier material, the use of such antigens to elicit antibodies selective to methaqualone and its major metabolites and an improved radiolabelled derivative of a methaqualone analog used in the practice of said radioimmunoassay.
    Type: Grant
    Filed: September 24, 1975
    Date of Patent: October 11, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: James Gordon Christenson
  • Patent number: 4053431
    Abstract: Liquid crystalline compounds of the formula ##STR1## wherein R is as hereinafter set forth, WHICH ARE USEFUL AS DIELECTRICS IN ELECTRO-OPTICAL DEVICES, ARE DESCRIBED.
    Type: Grant
    Filed: December 22, 1975
    Date of Patent: October 11, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hanspeter Scherrer, Arthur Boller
  • Patent number: 4053487
    Abstract: 15-Oxasteroids of the androstane, pregnane, estrane, and 19-norpregnane series are useful as hormonal agents.
    Type: Grant
    Filed: July 2, 1976
    Date of Patent: October 11, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Perry Rosen
  • Patent number: 4052413
    Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: October 4, 1977
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Zoltan George Hajos
  • Patent number: 4052446
    Abstract: 11-Substituted prostaglandins E.sub.1, E.sub.2 and F.sub.2.alpha. useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy and a process for preparing these prostaglandins.
    Type: Grant
    Filed: June 18, 1974
    Date of Patent: October 4, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George William Holland, Jane Liu Jernow, Perry Rosen
  • Patent number: 4051153
    Abstract: A synthesis of vitamin E in racemic or optically active forms from methacryolein or beta-hydroxyisobutyric acid including intermediates in this synthesis.
    Type: Grant
    Filed: December 9, 1975
    Date of Patent: September 27, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Gabriel Saucy
  • Patent number: 4051186
    Abstract: Biologically active substances having labile aryl groups can be converted to the corresponding aryl amine derivatives. The biologically active substances are reacted with a diazonium compound which optionally can be linked to a solid, inorganic carrier such as porous glass beads for ease of purification. The diazo reaction product is then reductively cleaved with a chemical reducing agent such as with hydrosulfite to yield the desired amine derivative. A preferred class of biologically active substances used herein is the catecholamines.
    Type: Grant
    Filed: January 28, 1976
    Date of Patent: September 27, 1977
    Assignee: The Regents of the University of California
    Inventor: Nathan O. Kaplan
  • Patent number: 4051174
    Abstract: A process for isomerizing vitamin A and derivatives thereof utilizing either palladium or a palladium containing compound as a catalyst.
    Type: Grant
    Filed: August 16, 1974
    Date of Patent: September 27, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hansjorg Stoller, Hans Peter Wagner
  • Patent number: 4051319
    Abstract: Alkynyl, benzyl or phenyl, ethers and esters which are ring substituted with an oxy or a thio aliphatic chain. These ethers and esters are useful in killing and preventing the proliferation of insects by upsetting their hormonal balance.
    Type: Grant
    Filed: March 29, 1976
    Date of Patent: September 27, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Madhukar Subraya Chodnekar, Albert Pfiffner, Norbert Rigassi, Ulrich Schwieter, Milos Suchy
  • Patent number: 4049677
    Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxymethylene, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: September 20, 1977
    Assignee: Hoffman-La Roche Inc.
    Inventor: Zoltan George Hajos
  • Patent number: 4049667
    Abstract: Tricyclic benzodiazepine derivatives ("A") bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. "A" bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. "A" bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. "A" are useful as sedative, muscle relaxant and anti-convulsant agents.
    Type: Grant
    Filed: April 12, 1976
    Date of Patent: September 20, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
  • Patent number: 4049666
    Abstract: Tricyclic benzodiazepine derivatives (A) bearing a hydroxylower alkyl substituent in the 1-position and a heterocyclic ring joined between positions 4 and 5 of the benzodiazepine moiety are described. The heterocyclic ring will contain the nitrogen atom appearing at position 4 of the benzodiazepine ring as well as the hetero atom, which may be either oxygen or nitrogen, attached to the carbon atom at the 5-position of the benzodiazepine ring. A bearing an oxygen atom in the new heterocyclic ring may be formed from the corresponding 4,5-unsaturated benzodiazepines by treatment with an epoxide compound in the presence of an acid catalyst. A bearing either a nitrogen or an oxygen atom in the new heterocyclic ring may be prepared by cyclization of the corresponding open compound. A are useful as sedative, muscle relaxant and anti-convulsant agents.
    Type: Grant
    Filed: April 12, 1976
    Date of Patent: September 20, 1977
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
  • Patent number: 4048195
    Abstract: Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 TO 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen, R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.
    Type: Grant
    Filed: July 14, 1976
    Date of Patent: September 13, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Zoltan George Hajos
  • Patent number: 4046751
    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 group and acid addition salts thereof.
    Type: Grant
    Filed: November 11, 1976
    Date of Patent: September 6, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric Herbert Hassall, William Henry Johnson, Antonin Krohn, Carey Ernest Smithen, William Anthony Thomas
  • Patent number: 4046813
    Abstract: Process for producing ketoisophorone from .beta.-isophorone by oxidation utilizing a metal salt catalyst and an organic nitrogen base.
    Type: Grant
    Filed: March 28, 1975
    Date of Patent: September 6, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Wolf Brenner
  • Patent number: 4046890
    Abstract: This invention is directed to pharmacologically active compounds of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or lower alkyl group and R.sub.2 represents a halogen atom.The compounds of formula I are optically active and have the absolute configuration S at the carbon atom in the 3-position. They exhibit anthelmintic, sedative, anticonvulsant and muscle relaxant activity.Also provided are methods for their preparation and formulations which incorporate the active compounds.
    Type: Grant
    Filed: June 23, 1975
    Date of Patent: September 6, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Andre Szente
  • Patent number: 4045383
    Abstract: Improved temperature monitoring films formed from stable emulsions containing compounds capable of existing in the cholesteric liquid crystalline phase which are protected and stabilized against aging, and the atmosphere by the inclusion of an antioxidant are provided. The thus-formed film materials are used in thermography and/or thermometry.
    Type: Grant
    Filed: January 21, 1976
    Date of Patent: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Arnold Koff
  • Patent number: 4045490
    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: August 30, 1977
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Marie Cassal, Andor Furst, Werner Meier