Patents by Inventor Werner Aschwanden
Werner Aschwanden 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: 5034402Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups,enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.Type: GrantFiled: April 12, 1990Date of Patent: July 23, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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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
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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
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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
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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
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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
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Patent number: 4691040Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.Type: GrantFiled: February 5, 1985Date of Patent: September 1, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Quirico Branca, Emilio Kyburz, Rudolf Pfister
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Patent number: 4650878Abstract: 2-(2-Oxo-1-pyrrolidinyl)acetic acids of the formula ##STR1## wherein R.sup.2 is hydrogen or lower alkyl and R.sup.11 is hydrogen, lower alkanoyl or another group readily cleavable by means of ammonia, are described. The compounds of formula III of the invention are useful to prepare the compound of formula I of the invention which are useful as medicaments, for example, in the form of pharmaceutical preparations.Type: GrantFiled: June 25, 1984Date of Patent: March 17, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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Patent number: 4513002Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions, such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.Type: GrantFiled: December 14, 1981Date of Patent: April 23, 1985Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Quirico Branca, Emilio Kyburz, Rudolf Pfister
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Patent number: 4476308Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkanoyl, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl or a group of the formula --(CH.sub.2).sub.n --NR.sup.4 R.sup.5, wherein n is a whole number of 2 to 4 and R.sup.4 and R.sup.5 each, independently, are hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the nitrogen atom are a pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl group which is optionally substituted by one or two lower alkyl groups, enantiomers thereof, and acid addition salts of compounds of formula I and their enantiomers which are basic, are useful in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. The compounds of formula I of the invention can be prepared starting from starting materials hereinafter described, and are useful as medicaments, for example, in the form of pharmaceutical preparations.Type: GrantFiled: June 20, 1983Date of Patent: October 9, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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Patent number: 4461906Abstract: 1-Substituted-2-pyrrolidinones of the formula ##STR1## wherein one of R.sup.1, R.sup.2 and R.sup.3 represents hydroxy and the remaining substituents represent hydrogen,are capable of counteracting cerebral insufficiency produced experimentally in animal tests. They can be used therapeutically in the control or prevention of cerebral insufficiency or in the improvement of intellectual capacity. They can be manufactured from novel intermediates and can be processed to provide medicaments.Type: GrantFiled: July 28, 1980Date of Patent: July 24, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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Patent number: 4452807Abstract: 1-(3-Hydroxy-4-methoxybenzoyl)-3-hydroxy-2-pyrrolidinone of the formula ##STR1## suitable for the control or prevention of cerebral insufficiency is described. The compound contains an asymmetric carbon atom. Therefore, the two optically active enantiomeric forms as well as the racemate are described. The compound of formula I can be prepared by cleaving the protecting group(s) from a corresponding compound in which at least one of the two hydroxy groups is protected.Type: GrantFiled: January 20, 1982Date of Patent: June 5, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwanden, Emilio Kyburz
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Patent number: 4369139Abstract: 1-(p-methoxybenzoyl)-2-pyrrolidinone and intermediates useful in its preparation are described. The 1-(p-methoxybenzoyl)-2-pyrrolidinone is useful in the prevention of cerebral insufficiency.Type: GrantFiled: July 14, 1980Date of Patent: January 18, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Emilio Kyburz, Werner Aschwanden
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Patent number: 4349562Abstract: 1-substituted 2-pyrrolidinones and pharmaceutical compositions containing same are described. The pharmaceutical compositions are useful in counteracting cerebral insufficiency or improving intellectual capacity.Type: GrantFiled: February 19, 1980Date of Patent: September 14, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Emilio Kyburz, Werner Aschwanden
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Patent number: 4239770Abstract: 1-Substituted 2-pyrrolidinones and pharmaceutical compositions containing same are described. The pharmaceutical compositions are useful in counteracting cerebral insufficiency or improving intellectual capacity.Type: GrantFiled: February 2, 1979Date of Patent: December 16, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Emilio Kyburz, Werner Aschwanden