Patents by Inventor Andre Szente
Andre Szente 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: 5466708Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: September 19, 1994Date of Patent: November 14, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 5376674Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: June 14, 1993Date of Patent: December 27, 1994Assignee: Hoffman-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 5260310Abstract: Novel compounds of the formula ##STR1## wherein Q, R.sup.1 and R.sup.2 are described herein, are disclosed along with pharmaceutical compositions, methods of use, and process for producing compounds of formula I which starts from the corresponding .beta.-hydroxycarboxylic acids.Type: GrantFiled: August 12, 1992Date of Patent: November 9, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Romano Derungs, Hans P. Marki, Henri Stalder, Andre Szente
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Patent number: 4981861Abstract: Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl land R.sup.8 is hydrogen nor lower alkyl,and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increaased gastric acid secretion.Type: GrantFiled: January 5, 1990Date of Patent: January 1, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente
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Patent number: 4950677Abstract: A compound of the formula ##STR1## wherein R.sup.1 -R.sup.19 are as described in the specification. The present invention is concerned with benzimidazole derivatives, particularly benzimidazole-2-yl pyridinium compounds of formula I which are pharmaceutically useful in treating or preventing gastric and duodenal ulcers. The invention includes the compounds I, pharmaceutical compositions containing such compounds and the use of such compounds in therapeutic treatment or prevention of gastric and duodenal ulcers.Type: GrantFiled: July 21, 1988Date of Patent: August 21, 1990Assignee: Hoffmann-La Roche Inc.Inventors: Albert Fischli, Anna Krasso, Andre Szente
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Patent number: 4766133Abstract: (Benzimidazol-2-yl)-pyridinium compounds of the formula ##STR1## wherein A is --SR.sup.9, --SO.sub.3.sup.- or --S--SO.sub.3.sup.- ; R.sup.1 and R.sup.3 each is hydrogen or (C.sub.1 -C.sub.7)-alkyl; R.sup.2 is hydrogen, (C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxy or a negatively charged oxygen atom; R.sup.4 is hydrogen or a negative charge; R.sup.5, R.sup.6, R.sup.7 and R.sup.8 each is hydrogen, (C.sub.1 -C.sub.7)-alkyl, aryl, halogen, cyano, nitro, formyl, (C.sub.2 -C.sub.7)-alkanoyl, arylcarbonyl, carboxy, carboxy-(C.sub.1 -C.sub.7)-alkyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl, aryloxycarbonyl, aryl-(C.sub.1 -C.sub.7)-alkoxycarbonyl, (C.sub.1 -C.sub.7)-alkoxycarbonyl-(C.sub.1 -C.sub.7)-alkyl, carbamoyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl, pyrrolidinocarbonyl, piperidinocarbonyl, carbamoyl-(C.sub.1 -C.sub.7)-alkyl, mono- or di-(C.sub.1 -C.sub.7)-alkylcarbamoyl-(C.sub.1 -C.sub.7)-alkyl, pyrrolidinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, piperdinocarbonyl-(C.sub.1 -C.sub.7)-alkyl, hydroxy, (C.sub.Type: GrantFiled: August 6, 1986Date of Patent: August 23, 1988Assignee: Hoffman-La Roche Inc.Inventors: Albert Fischli, Anna Krasso, Andre Szente
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Patent number: 4634710Abstract: Tricyclic imidazole derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.3 is lower alkyl and the other is hydrogen or lower alkyl, R.sup.2 is lower alkyl, n is the number 0 or 1, A is ##STR2## R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each is lower alkyl and R.sup.8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.Type: GrantFiled: April 8, 1985Date of Patent: January 6, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente
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Patent number: 4474777Abstract: There are presented novel pharmaceutically active substances which inhibit the intestinal resorption of cholesterol and which accordingly can be used in the control or prevention of atherosclerosis. These active substances are benzodiazepines of the formula ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen or methyl, R.sup.3 and R.sup.4 each are halogen and R.sup.5 is (C.sub.3 -C.sub.9)-alkylamino substituted by at least two hydroxy groups, (C.sub.3 -C.sub.6)-cycloalkylamino substituted by at least one hydroxy group, glucosamino, galactosamino, mannosamino, monohydroxy-1-azetidinyl, mono- or dihydroxy-1-pyrrolidinyl or mono-, di- or trihydroxy-1-piperidinyl,and the readily hydrolyzable esters and ethers thereof, as well as pharmaceutically acceptable salts of these compounds.Type: GrantFiled: December 17, 1982Date of Patent: October 2, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Marie Cassal, Albert E. Fischli, Andre Szente
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Patent number: 4472435Abstract: There is presented novel benzophenone derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen or aminoacetyl, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is hydrogen or halogen, R.sup.5 is hydrogen, amino, nitro or a group of the formula R.sup.3 --ON.dbd.C(R.sup.6)--and R.sup.6 is lower alkyl, with the proviso that R.sup.5 is a group of the formula H--ON.dbd.C(R.sup.6)--when R.sup.2 and R.sup.3 are both hydrogen, and their pharmaceutically acceptable acid addition salts.The compounds exhibit aldosterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.Type: GrantFiled: July 15, 1981Date of Patent: September 18, 1984Assignee: Hoffman-La Roche Inc.Inventors: Quirico Branca, Albert E. Fischli, Andre Szente
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Patent number: 4377522Abstract: There are presented novel benzodiazepine derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl, lower hydroxyalkyl or lower dialkylaminoalkyl, R.sup.2 and R.sup.3 each are lower alkyl, R.sup.4 is halogen, R.sup.5, R.sup.7 and R.sup.8 each are hydrogen or halogen and R.sup.6 is nitro, amino, lower alkylamino, lower dialkylamino or a group of the formula H.sub.2 N--C(CH.sub.3).sub.2 --CO--NH--, R.sup.9 R.sup.10 N--CO--NH-- or ##STR2## and either R.sup.9 is hydrogen or lower alkyl and R.sup.10 is lower alkyl or lower hydroxyalkyl or R.sup.9 and R.sup.10 together with the nitrogen atom are a 3- to 7-membered heterocycle which, provided it is at least 5-membered, can contain as a ring member an oxygen or sulfur atom or a group of the formula >N--R in which R is hydrogen or lower alkyl,and their pharmaceutically acceptable acid addition salts.Type: GrantFiled: July 6, 1981Date of Patent: March 22, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albert E. Fischli, Andre Szente
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Patent number: 4374773Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group, R.sup.2 and R.sup.3 each are a hydrogen atom or a lower alkyl group, R.sup.4 is a halogen atom and either R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 is a lower alkyl or lower hydroxyalkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached are a 3-membered to 7-membered heterocycle,and pharmaceutically acceptable acid addition salts thereof.The compounds and their salts are novel and possess valuable pharmacodynamic properties.Type: GrantFiled: January 16, 1981Date of Patent: February 22, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albert E. Fischli, Andre Szente
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Patent number: 4361511Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is a lower alkyl group, R.sup.2 is a hydrogen atom or a lower alkyl group, R.sup.3 is a hydrogen or halogen atom, R.sup.4 is a hydrogen atom or a group of the formula R.sup.5 --CO--,R.sup.6 R.sup.7 N--O--, ##STR2## A is a lower alkylene group, X is an oxygen or sulphur atom or a group of the formula >N--.sup.8 , R.sup.5 is a lower alkyl or lower haloalkyl group, R.sup.6 is a hydrogen atom or a lower alkyl group, R.sup.7 is a lower alkyl group and R.sup.8 is a hydrogen atom or a lower alkyl or lower hydroxyalkyl group, and their pharmaceutically acceptable acid addition salts.The compounds have aldosterone-antagonistic properties and are accordingly suitable for the control or prevention of heart failure, hepatic ascites, primary aldosteronism and idiopathic hypertension.Type: GrantFiled: January 16, 1981Date of Patent: November 30, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albert E. Fischli, Andre Szente
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Patent number: 4327026Abstract: There is presented benzodiazepine derivatives of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is lower alkyl, R.sup.2 and R.sup.3 each are hydrogen or lower alkyl, R.sup.4 is the group ##STR3## R.sup.5 is hydrogen or halogen, R.sup.8 is hydrogen or lower alkyl, R.sup.9 is lower alkyl or lower alkoxyalkyl, R.sup.10 is lower alkyl, R.sup.11 is hydrogen, lower alkyl or lower hydroxyalkyl, R.sup.12 is hydrogen or lower alkyl and R.sup.14 is lower alkyl or aryl, and either R.sup.6 is hydrogen or lower alkyl and R.sup.7 is lower alkyl or lower hydroxyalkyl or R.sup.6 and R.sup.7 together with the nitrogen atom are a 3- to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R.sup.13, in which R.sup.13 is hydrogen or lower alkyl, and either R.sup.6 ' is hydrogen or lower alkyl and R.sup.7 ' is lower alkyl or R.sup.6 ' and R.sup.Type: GrantFiled: July 16, 1981Date of Patent: April 27, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Albert E. Fischli, Andre' Szente
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Patent number: 4299767Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula ##STR2## in which R.sup.Type: GrantFiled: September 11, 1980Date of Patent: November 10, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4296031Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N--R.sup.7 in which R.sup.Type: GrantFiled: September 11, 1980Date of Patent: October 20, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4294758Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula ##STR2## in which R.sup.Type: GrantFiled: September 11, 1980Date of Patent: October 13, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4281188Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N--R.sup.7 in which R.sup.Type: GrantFiled: September 11, 1980Date of Patent: July 28, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4251443Abstract: This invention provides benzodiazepine derivatives of the general formula ##STR1## wherein R.sup.1 represents a lower alkyl group, R.sup.2 represents a hydrogen atom or a lower alkyl group, R.sup.3 represents a halogen atom and R.sup.4 represents a hydrogen or halogen atom and either R.sup.5 represents a hydrogen atom or a lower alkyl group and R.sup.6 represents a lower alkyl, lower hydroxyalkyl or lower acyloxyalkyl group or R.sup.5 represents a hydrogen atom and R.sup.6 represents an aryl or lower aralkyl group or R.sup.5 and R.sup.6 together with the nitrogen atom to which they are attached represent a 3-membered to 7-membered heterocycle which, when it is at least 5-membered, can contain as a ring member an oxygen or sulphur atom or a group of the formula >N-R.sup.7 in which R.sup.Type: GrantFiled: August 2, 1979Date of Patent: February 17, 1981Assignee: Hoffmann-La Roche Inc.Inventors: Albert E. Fischli, Andre Szente
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Patent number: 4046890Abstract: This invention is directed to pharmacologically active compounds of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or lower alkyl group and R.sub.2 represents a halogen atom.The compounds of formula I are optically active and have the absolute configuration S at the carbon atom in the 3-position. They exhibit anthelmintic, sedative, anticonvulsant and muscle relaxant activity.Also provided are methods for their preparation and formulations which incorporate the active compounds.Type: GrantFiled: June 23, 1975Date of Patent: September 6, 1977Assignee: Hoffmann-La Roche Inc.Inventor: Andre Szente
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Patent number: 4031078Abstract: This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group and R.sub.1 represents a hydrogen or halogen atom or a trifluoromethyl group which have the absolute configuration S at the 3-position carbon atom.Also presented is a process to produce the above benzodiazepine derivatives and pharmaceutical preparations therefor. The above benzodiazepine derivatives exhibit pronounced anthelmintic, especially schistosomicidal, activity and muscle relaxant, anticonvulsant and sedative activities.Type: GrantFiled: October 14, 1975Date of Patent: June 21, 1977Assignee: Hoffmann-La Roche Inc.Inventor: Andre Szente