Patents by Inventor Rene Imhof
Rene Imhof 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: 5318967Abstract: The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl,the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.Type: GrantFiled: September 3, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
-
Patent number: 5318966Abstract: The invention relates to cis-2,3,3a,4,5,9b-Hexahydro-1H-benzo[b]indole derivatives of the formula ##STR1## wherein R.sup.1 is a residue of the formula --O--CO--NR.sup.4 R.sup.5, R.sup.2 is lower alkyl, lower cycloalkyl or lower alkyl substituted by lower cycloalkyl, aryl, aroyl, aroylamino, amino or by a cyclic amino, amide or imide group, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is lower alkyl and R.sup.5 is hydrogen or lower alkyl,the corresponding trans isomers or cis-trans isomeric mixtures and pharmaceutically acceptable salts thereof. These compounds and salts are especially suitable for the treatment or prophylaxis of cognitive disorders and senile dementia particularly, Alzheimer's disease, and for the improvement of memory capacity.Type: GrantFiled: July 16, 1993Date of Patent: June 7, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
-
Patent number: 5204482Abstract: Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl, monohalophenyl, monolower-alkylphenyl, monolower-alkoxyphenyl, monotrifluoromethylphenyl, monocyanophenyl or monaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl,as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.Type: GrantFiled: February 4, 1991Date of Patent: April 20, 1993Assignee: Hoffman-LaRoche Inc.Inventors: Walter Gassner, Rene Imhof
-
Patent number: 5030636Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen; lower-alkyl, unsubstituted or substituted by hydroxy, lower-alkoxy, cyano, halogen, lower-alkoxycarbonyl, aminocarbonyl, substituted benzoyl or substituted .alpha.-hydroxybenzyl; lower-alkenyl; cycloalkyl; cycloalkyl-lower-alkyl; heteroaryl-lower-alkyl; or aryl-lower-alkyl, unsubstituted or substituted by hydroxy, lower-alkoxy, lower-alkyl or halogen, and R.sup.2 is hydrogen or lower-alkanoyl,in the form of the racemates and the optical antipodes as well as pharmaceutically acceptable acid addition salts thereof which are active as selective, presynaptically-acting dopamine receptor agonists and are accordingly suitable for the control or prevention of central nervous system illnesses, especially for the control or prevention of psychotic disorders such as chronic schizophrenia, are described. The compounds of formula I can be prepared according to various methods which are known.Type: GrantFiled: March 13, 1990Date of Patent: July 9, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Hans H. Keller
-
Patent number: 5017608Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxycarbonyl-(C.sub.2 -C.sub.5)-alkyl, piperidino-(C.sub.2 -C.sub.Type: GrantFiled: September 6, 1989Date of Patent: May 21, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
-
Patent number: 5011849Abstract: Ethylenediamine monoamides of the formulaR--CO--NH--CH.sub.2 --CH.sub.2 --NH.sub.2 Iwherein R is one of groups ##STR1## in which R.sup.1 is phenyl monohalophenyl, monolower-alkylphenyl, monolower-alkoxypheynl, monotrifluoromethylphenyl, monocyanophenyl or monoaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R.sup.2 is hydrogen, halogen or amino, R.sup.3, R.sup.5 and R.sup.7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R.sup.4 and R.sup.6 each are hydrogen or amino and R.sup.8 is hydrogen or lower-alkyl, as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders.Type: GrantFiled: July 21, 1989Date of Patent: April 30, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Walter Gassner, Rene Imhof, Emilio Kyburz
-
Patent number: 4957911Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: August 17, 1989Date of Patent: September 18, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
-
Patent number: 4883815Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.Type: GrantFiled: July 5, 1988Date of Patent: November 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
-
Patent number: 4876340Abstract: Benzazecinediones of the formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen, as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: February 11, 1988Date of Patent: October 24, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
-
Patent number: 4764522Abstract: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.Type: GrantFiled: August 16, 1985Date of Patent: August 16, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4749791Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen,as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: November 18, 1987Date of Patent: June 7, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
-
Patent number: 4732979Abstract: Benzazecinediones of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or chlorine, R.sup.3 is hydrogen, fluorine, chlorine, bromine or methoxy, R.sup.4 is hydrogen, chlorine or methoxy and R.sup.5 is hydrogen, acetyl, propionyl, benzoyl, chlorobenzoyl, methoxybenzoyl or phenylacetyl, with the proviso that 2 or 3 of the groups R.sup.1 to R.sup.4 are hydrogen.as well as many of the corresponding benzo[f]quinolines from which these benzazecinediones can be prepared by oxidation are suitable for the control or prevention of cerebral insufficiency or for the improvement of cognitive functions in mammals. They can be produced according to various processes and can be prepared into pharmaceutical compositions.Type: GrantFiled: January 21, 1987Date of Patent: March 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Rene Imhof, Roland Jakob, Emilio Kyburz
-
Patent number: 4684731Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.Type: GrantFiled: March 11, 1983Date of Patent: August 4, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4391978Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 is acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.Type: GrantFiled: April 9, 1981Date of Patent: July 5, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4338444Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X,Y,R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: December 18, 1980Date of Patent: July 6, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4329467Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: December 18, 1980Date of Patent: May 11, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4316030Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, and described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: December 18, 1980Date of Patent: February 16, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4306067Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: December 18, 1980Date of Patent: December 15, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rene' Imhof, Emilio Kyburz
-
Patent number: 4272627Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X,Y,R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: May 12, 1980Date of Patent: June 9, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz
-
Patent number: 4236010Abstract: Phenyl-quinolizidines of the formula ##STR1## wherein X, Y, R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The compounds of formula I are useful as antipsychotics, antiemetics and analgesics.Type: GrantFiled: October 15, 1979Date of Patent: November 25, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Rene Imhof, Emilio Kyburz