Patents Represented by Attorney Samuel L. Welt

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  • Intermediates for steroid total synthesis process utilizing asymmetric induction
    Patent number: 4092483
    Abstract: A multi-step, stereospecific total synthesis of steroids is disclosed. The starting materials for this process are the relatively inexpensive and readily available m-alkoxy acetophenones. The process is suitable for the preparation of racemic or optically active, medicinally valuable steroids, particularly A-ring aromatic steroids. This process features an early optical resolution and a unique asymmetric induction which insures the correct stereochemistry of the final steroidal product.
    Type: Grant
    Filed: September 24, 1975
    Date of Patent: May 30, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Gabriel Saucy
  • Cephalosporins
    Patent number: 4091211
    Abstract: Cephalosporins represented by the formulaX-S-Ywherein X is a deacetoxycephalosporinyl group and Y is a 6-membered heterocyclic group containing 1-3 nitrogens at least one of which is substituted and at least one of which is adjacent to a carbonyl group, said heterocyclic group containing one or more ring substituents and being characterized by being non-aromatic and not enolizable to an aromatic form.
    Type: Grant
    Filed: June 13, 1975
    Date of Patent: May 23, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Marc Montavon, Roland Reiner
  • Dibenz[b,f]oxepin derivatives
    Patent number: 4091023
    Abstract: Dibenz[b,f]oxepins of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as hereinafter described, are described. The foregoing compounds exhibit strong central depressant and neuroleptic properties, and are useful, for example, in the treatment of acute or chronic schizophrenia and also as tranquilizers.
    Type: Grant
    Filed: March 18, 1977
    Date of Patent: May 23, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Max Gerecke, Emilio Kyburz, Jean-Pierre Kaplan
  • Isoindole derivatives
    Patent number: 4090027
    Abstract: Isoindole derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.6, A and Z are as hereinafter described. The isoindole derivatives are useful as appetite suppressants.
    Type: Grant
    Filed: August 25, 1976
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Synthesis of cyclopentanol
    Patent number: 4089889
    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.
    Type: Grant
    Filed: September 15, 1975
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Frank Kienzle, Perry Rosen
  • Stable solutions of ipronidazole
    Patent number: 4089968
    Abstract: Solutions of ipronidazole are disclosed which have excellent stability and physiological acceptance and thereby are amenable to parenteral administration. The subject preparations utilize as the solvent for ipronidazole a mixture of water and glycerinformal.
    Type: Grant
    Filed: March 22, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Heinrich Klaui
  • Thienothiazine derivatives
    Patent number: 4090020
    Abstract: Thienothiazine derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl; R.sub.2 is an unsubstituted aromatic heterocyclic radical which contains from 1 to 4 hetero atoms or one which is substituted by one or two lower alkyl groups, or is an unsubstituted phenyl radical or one substituted by halogen, hydroxy, lower alkyl, nitro, trifluoromethyl or lower alkoxy; and R.sub.3 and R.sub.4, independently, are hydrogen or lower alkyl,Prepared inter alia, from novel intermediates, are described. The end products are useful as anti-inflammatory, analgesic and anti-rheumatic agents.
    Type: Grant
    Filed: February 9, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dieter Binder, Otto Hromatka, Rudolf Pfister, Paul Zeller
  • (+)-(S)-Enantiomer of 3-{2-[4-(8-fluoro-10,11-dihydro-2-methyl-dibenzo[b,f]thiepin-10-yl)-1-pi perazinyl]-ethyl}-2-oxazolidinone
    Patent number: 4089861
    Abstract: (+)-(S)-enantiomer of 3-{2-[4-(8-fluoro-10,11-dihydro-2-methyldibenzo[b,f]thiepin-10-yl)-1-piper azinyl]-ethyl} -2-oxazolidinone, active as a neuroleptic agent, is described.
    Type: Grant
    Filed: May 26, 1976
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Emilio Kyburz
  • Antibacterial compositions
    Patent number: 4089950
    Abstract: Compositions comprising N-sulfanilyl-1-ethylcytosine and a sulfonamide potentiator, which are useful as antibacterial agents, are described.
    Type: Grant
    Filed: May 6, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erika Bohni, Marc Montavon
  • Process and intermediates for isoindole derivatives
    Patent number: 4089875
    Abstract: A process for the preparation of isoindole derivatives which comprises heating a compound of the formula ##STR1## wherein R,R.sub.1,R.sub.2,R.sub.3,R.sub.4 and R.sub.5 are hereinafter set forth, in the presence of a suitable imidazole, is described.
    Type: Grant
    Filed: July 7, 1977
    Date of Patent: May 16, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Jaunin
  • Optically active amides and process for producing the same
    Patent number: 4088662
    Abstract: A synthesis of Vitamin E in racemic or optically active forms from 6-methyl-2-hepten-4-ol; 6,10-dimethyl-2-undecen-4-ol or 6-benzyloxy-2,5,7,8-tetramethyl-chroman-2-acetaldehyde including intermediates in this synthesis.
    Type: Grant
    Filed: December 8, 1976
    Date of Patent: May 9, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel Saucy
  • O,O-Dialkylphosphoryloxy-2,3,5,8-tetrahydro-1H-s-triazolo[1 ,2a]pyridazine-1,3-diones
    Patent number: 4088645
    Abstract: Dienylphosphates of the formula ##STR1## wherein each of R.sub.1 and R.sub.1 ' is lower alkyl, aryl or benzyl and each of R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower alkyl, are useful as anthelmintic agents and as intermediates for enolphosphates having anthelmintic activity.
    Type: Grant
    Filed: February 7, 1977
    Date of Patent: May 9, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar F. Burri, Frank Kienzle, Perry Rosen
  • Cyclohexenone phosphonium salts
    Patent number: 4088689
    Abstract: Phosphonium salts of 5-(2,6,6-trimethyl-3-oxocyclohexen-1-yl)-3-methyl-substituted-2-penten-4-y n or 2,4-pentadiene which are intermediates for canthaxanthin.
    Type: Grant
    Filed: February 4, 1977
    Date of Patent: May 9, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michael Rosenberger
  • Methylation of de-A steroids
    Patent number: 4087436
    Abstract: Treatment of de-A steroids with a methylation agent at extremely low temperatures, i.e., below -50.degree. C. produces corresponding 10.beta.-methyl-.DELTA..sup.9(11) -deA steroids with a high 10.beta. to 10.alpha. isomer ratio. A number of the product 10.beta.-methyl-.DELTA..sup.9(11) -deA steroids are novel compounds. They are useful as intermediates in the synthesis of known medicinally valuable steroids.
    Type: Grant
    Filed: June 23, 1975
    Date of Patent: May 2, 1978
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Paul Buchschacher, Andor Furst, Ludwig Labler, Werner Meier, John William Scott
  • Cyano-4-(0,0-dialkylphosphoryloxy)-cyclohex-4-enes
    Patent number: 4087488
    Abstract: Dienylphosphates of the formula ##STR1## wherein each of R.sub.1 and R.sub.1 ' is lower alkyl, aryl or benzyl and each of R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower akyl,Are useful as anthelmintic agents and as intermediates for enolphosphates having anthelmintic activity.
    Type: Grant
    Filed: February 7, 1977
    Date of Patent: May 2, 1978
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kaspar F. Burri, Frank Kienzle, Perry Rosen
  • Field effect light shutter employing low temperature nematic liquid crystals
    Patent number: 4086002
    Abstract: A field effect liquid crystal light shutter employing low temperature nematic liquid crystals of the p-alkylphenyl-p'-akyl and alkoxy benzoate series.
    Type: Grant
    Filed: November 20, 1973
    Date of Patent: April 25, 1978
    Assignee: Haffmann-La Roche Inc.
    Inventor: Sardari L. Arora
  • Tetramethyl chromanyl pentane amide
    Patent number: 4086249
    Abstract: Amides of 5[2,5,7,8-tetramethyl-chromanyl]-pentenanoic acid which are intermediates for Vitamin E.
    Type: Grant
    Filed: December 8, 1976
    Date of Patent: April 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ka-Kong Chan, Gabriel Saucy
  • Carcinoembryonic antigens
    Patent number: 4086217
    Abstract: Antigens associated with carcinomas and adenocarcinomas as well as methods for isolating, identifying and detecting them are disclosed.
    Type: Grant
    Filed: February 18, 1977
    Date of Patent: April 25, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans John Hansen
  • Therapeutic agent for improving cardiovascular function
    Patent number: 4083968
    Abstract: Methods of and compositions for improving cardiovascular function utilizing as the active agent certain pharmaceutically acceptable salts, derivatives, isomers and homologs of lasalocid (formerly known as antibiotic X-537A) are disclosed.
    Type: Grant
    Filed: January 9, 1976
    Date of Patent: April 11, 1978
    Assignee: Hoffmann-La Roche
    Inventor: John Westley
  • Derivatives of antibiotic X-537A
    Patent number: RE29651
    Abstract: Compound of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, phenyl, or phenyl substituted by halogen, nitro or lower alkyl; R.sub.2 is hydrogen; lower alkyl; lower alkanoyl; benzoyl; benzoyl substituted by halogen, nitro or lower alkyl; or R.sub.3 is hydrogen, halogen; nitro, amino, loweralkylamido or lower alkylamino; R.sub.4 is --OH, =O or =NOH which compound is useful as a coccidiostatic agent and as an anti-bacterial agent.
    Type: Grant
    Filed: December 28, 1976
    Date of Patent: May 30, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Stempel, John Westley