Patents by Inventor Leo Henryk Sternbach
Leo Henryk Sternbach 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: 4111934Abstract: Novel 1,5-benzodiazepin-4-one derivatives, bearing between the 1,2-positions a triazolo ring, as disclosed. These 1,2-triazolo-1,5-benzodiazepin-4-ones are useful as muscle-relaxant, anti-convulsant and sedative agents.Type: GrantFiled: December 15, 1977Date of Patent: September 5, 1978Assignee: Hoffmann-La Roche Inc.Inventors: Rodney Ian Fryer, Leo Henryk Sternbach, Armin Walser
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Patent number: 4049667Abstract: 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: GrantFiled: April 12, 1976Date of Patent: September 20, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 4049666Abstract: 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: GrantFiled: April 12, 1976Date of Patent: September 20, 1977Assignee: Hoffman-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 4044016Abstract: Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anticonvulsants, muscle relaxants and sedative agents.Type: GrantFiled: May 7, 1976Date of Patent: August 23, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Leo Henryk Sternbach, Armin Walser
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Patent number: 4018765Abstract: Novel 2[2-(1,3-diazacycloalk-2-enyl)]benzophenone compounds and novel 1,3-diazacycloalkenyl[2,1-a]isoindole compounds having useful analgesic and psychostimulant properties are prepared inter alia by condensation of o-benzoylbenzaldehydes with aliphatic diamines.Type: GrantFiled: October 2, 1975Date of Patent: April 19, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Werner Metlesics, Leo Henryk Sternbach
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Patent number: 4017532Abstract: 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: GrantFiled: April 12, 1976Date of Patent: April 12, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 4017531Abstract: 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: GrantFiled: April 12, 1976Date of Patent: April 12, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 4014883Abstract: Derivatives of 7H-indolo[2,3-c]quinolin-6(5H)-one and 7H-indolo[2,3-c]quinoline, prepared, inter alia, from the corresponding 3-azido-4-phenylcarbostyrils or corresponding N-(lower alkylamino)-3-(2-fluorophenyl)-indole-2-carboxamides, are described. The end products of the invention are useful as anti-tumor agents, i.e., they inhibit the growth of transplantable tumors.Type: GrantFiled: July 16, 1975Date of Patent: March 29, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Rodney Ian Fryer, Robert Ye-Fong Ning, Leo Henryk Sternbach, Armin Walser
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Patent number: 4014916Abstract: 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: GrantFiled: April 12, 1976Date of Patent: March 29, 1977Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 3997591Abstract: 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: GrantFiled: April 12, 1976Date of Patent: December 14, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 3970664Abstract: Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anticonvulsants, muscle relaxants and sedative agents.Type: GrantFiled: January 13, 1975Date of Patent: July 20, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Leo Henryk Sternbach, Armin Walser
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Patent number: 3965151Abstract: 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: GrantFiled: March 11, 1975Date of Patent: June 22, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Michael Edward Derieg, James Valentine Earley, Rodney Ian Fryer, Leo Henryk Sternbach
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Patent number: 3954728Abstract: Novel preparations of triazolobenzodiazepines are disclosed. Novel 6-pyridyl-4H-triazolo[4,3-a]-1,4-benzodiazepines and novel intermediates are also disclosed which are useful as anti-convulsants, muscle relaxants and sedative agents.Type: GrantFiled: January 13, 1975Date of Patent: May 4, 1976Assignee: Hoffman-La Roche Inc.Inventors: Leo Henryk Sternbach, Armin Walser
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Patent number: 3954753Abstract: Novel pyrazino-1,4-diazepines are disclosed together with processes for their preparation and novel intermediates used in these processes. These novel diazepines are useful as sedatives, muscle-relaxants and anti-convulsants.Type: GrantFiled: February 13, 1975Date of Patent: May 4, 1976Assignee: Hoffmann-La Roche Inc.Inventors: George Francis Field, Leo Henryk Sternbach, Armin Walser
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Patent number: 3931217Abstract: Novel 2[2-(1,3-diazacycloalk-2-enyl)]benzophenone compounds and novel 1,3-diazacycloalkenyl[2,1-a]isoindole compounds having useful analgesic and psychostimulant properties are prepared inter alia by condensation of o-benzoylbenzaldehydes with aliphatic diamines.Type: GrantFiled: May 6, 1974Date of Patent: January 6, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Werner Metlesics, Leo Henryk Sternbach