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).
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Patent number: 4260772Abstract: 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: GrantFiled: July 30, 1980Date of Patent: April 7, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
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Patent number: 4259241Abstract: 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: GrantFiled: February 21, 1980Date of Patent: March 31, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4259503Abstract: 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: GrantFiled: July 30, 1980Date of Patent: March 31, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
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Patent number: 4257946Abstract: 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: GrantFiled: February 21, 1980Date of Patent: March 24, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4250095Abstract: 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: GrantFiled: April 11, 1980Date of Patent: February 10, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4247463Abstract: 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: GrantFiled: April 11, 1980Date of Patent: January 27, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4244867Abstract: 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: GrantFiled: February 21, 1980Date of Patent: January 13, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4244868Abstract: 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: GrantFiled: February 21, 1980Date of Patent: January 13, 1981Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4243589Abstract: 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: GrantFiled: November 30, 1979Date of Patent: January 6, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rodney I. Fryer, Eugene J. Trybulski, Armin Walser
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Patent number: 4240962Abstract: 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: GrantFiled: April 11, 1980Date of Patent: December 23, 1980Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4226771Abstract: 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: GrantFiled: July 25, 1979Date of Patent: October 7, 1980Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4226768Abstract: 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: GrantFiled: May 29, 1979Date of Patent: October 7, 1980Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4166185Abstract: 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: GrantFiled: July 27, 1978Date of Patent: August 28, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
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Patent number: 4147875Abstract: 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: GrantFiled: July 27, 1978Date of Patent: April 3, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
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Patent number: 4146722Abstract: 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: GrantFiled: July 27, 1978Date of Patent: March 27, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
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Patent number: 4146537Abstract: 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: GrantFiled: February 1, 1978Date of Patent: March 27, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer
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Patent number: 4137229Abstract: 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: GrantFiled: February 1, 1978Date of Patent: January 30, 1979Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer
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Patent number: 4125726Abstract: 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: GrantFiled: March 11, 1977Date of Patent: November 14, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney I. Fryer, Louis Benjamin
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Patent number: 4118386Abstract: 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: GrantFiled: April 4, 1977Date of Patent: October 3, 1978Assignee: Hoffmann-La Roche Inc.Inventor: Armin Walser
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Patent number: 4111931Abstract: 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: GrantFiled: February 1, 1978Date of Patent: September 5, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Armin Walser, Rodney Ian Fryer