Patents by Inventor Armin Walser

Armin Walser has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4260772
    Abstract: There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogen and the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.
    Type: Grant
    Filed: July 30, 1980
    Date of Patent: April 7, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
  • Patent number: 4259241
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is a disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: February 21, 1980
    Date of Patent: March 31, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4259503
    Abstract: There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogenand the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.
    Type: Grant
    Filed: July 30, 1980
    Date of Patent: March 31, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
  • Patent number: 4257946
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: February 21, 1980
    Date of Patent: March 24, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4250095
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and aryl.Also presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: April 11, 1980
    Date of Patent: February 10, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4247463
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and arylAlso presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: April 11, 1980
    Date of Patent: January 27, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4244867
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is a disubstituted amineAlso presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: February 21, 1980
    Date of Patent: January 13, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4244868
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is a disubstituted amineAlso presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: February 21, 1980
    Date of Patent: January 13, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4243589
    Abstract: There is presented triazolobenzazepines of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl and X and Y are hydrogen or halogenand the pharmaceutically acceptable salts thereof.Also disclosed are novel processes and intermediates leading to the triazolobenzazepines.The triazolobenzazepines are useful compounds having anxiolytic, sedative, muscle relaxant and anticonvulsant activity.
    Type: Grant
    Filed: November 30, 1979
    Date of Patent: January 6, 1981
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
  • Patent number: 4240962
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl, Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl and R.sub.1 is selected from the group consisting of hydrogen, lower alkyl and arylAlso presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: April 11, 1980
    Date of Patent: December 23, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4226771
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl,Y is selected from the group consisting of hydrogen, halogen and trifluoromethyl andR.sub.1 is selected from the group consisting of hydrogen, lower alkyl and arylAlso presented are novel intermediates utilized in the process.The end products are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: July 25, 1979
    Date of Patent: October 7, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4226768
    Abstract: A multistep process is presented for the preparation of imidazobenzodiazepines of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl; Y is selected from the group consisting of hydrogen, halogen or trifluoromethyl; R.sub.1 is hydrogen or lower alkyl and R.sub.2 is a disubstituted amine.Also presented are novel intermediates utilized in the process.The end products and intermediates are useful as sedatives, anxiolytics, muscle relaxants and anticonvulsants.The end products are especially useful in intravenous compositions for use in preoperative anesthesia.
    Type: Grant
    Filed: May 29, 1979
    Date of Patent: October 7, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Armin Walser
  • Patent number: 4166185
    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: July 27, 1978
    Date of Patent: August 28, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
  • Patent number: 4147875
    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 lowe 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 hydrogenAnd 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: July 27, 1978
    Date of Patent: April 3, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
  • Patent number: 4146722
    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: July 27, 1978
    Date of Patent: March 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
  • Patent number: 4146537
    Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be different,And the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
    Type: Grant
    Filed: February 1, 1978
    Date of Patent: March 27, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer
  • Patent number: 4137229
    Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.4 is lower alkyl or hydrogen and may be different and the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
    Type: Grant
    Filed: February 1, 1978
    Date of Patent: January 30, 1979
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney I. Fryer
  • 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: 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: 4111931
    Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.2 is lower alkyl or hydrogen and may be differentand the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.
    Type: Grant
    Filed: February 1, 1978
    Date of Patent: September 5, 1978
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Armin Walser, Rodney Ian Fryer