Patents by Inventor Karl Bernauer
Karl Bernauer 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: 5705703Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: January 21, 1997Date of Patent: January 6, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5633371Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5476875Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Type: GrantFiled: October 21, 1994Date of Patent: December 19, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5389653Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1993Date of Patent: February 14, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5236952Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1991Date of Patent: August 17, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
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Patent number: 4820734Abstract: The novel phenethylamine derivatives of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each signify hydrogen, halogen, trifluoromethyl, lower alkoxy, lower alkyl, hydroxy or nitro, with the proviso that at least one of R.sup.1 and R.sup.2 is different from hydrogen, R.sup.3 and R.sup.4 each signify lower alkyl, n signifies the number 1, 2, 3 or 4 and B signifies the group --CO-- or --CHOH--, and their pharmaceutically acceptable acid addition salts have interesting analgesic and antidepressant properties. These substances can be manufactured according to various methods which are known per se and can be used as medicaments in the form of pharmaceutical preparation.Type: GrantFiled: November 4, 1987Date of Patent: April 11, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Hans Bruderer
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Patent number: 4482739Abstract: Imidazolidine derivatives of the formula ##STR1## wherein X is oxygen or imino and R is one of the groups ##STR2## their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.Type: GrantFiled: May 12, 1983Date of Patent: November 13, 1984Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Helmut Link, Harro Stohler
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Patent number: 4407814Abstract: Imidazolidine derivatives of the formula ##STR1## wherein X is oxygen or imino and R is one of the groups ##STR2## their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.Type: GrantFiled: December 14, 1981Date of Patent: October 4, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Helmut Link, Harro Stohler
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Patent number: 4360530Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are hydrogen, halogen or lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; R.sup.8 is hydrogen, lower alkyl or formyl; R.sup.9 and R.sup.10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R.sup.7 and R.sup.8 are lower alkyl, n is 0 (zero) or 1, prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.Type: GrantFiled: November 12, 1981Date of Patent: November 23, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Karlheinz Pfoertner
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Patent number: 4317914Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2, independently, are hydrogen, halogen or lower alkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, independently, are hydrogen or C.sub.1-3 alkyl; R.sup.8 is hydrogen, lower alkyl or formyl; R.sup.9 and R.sup.10, independently, are methyl or trifluoromethyl; and n is 0 (zero) or, when both R.sup.7 and R.sup.8 are lower alkyl, n is 0 (zero) or 1,prepared, inter alia, from p-aminobenzaldehydes which may be N-alkyl substituted, are described. The compounds of formula I are orally active antidiabetic agents.Type: GrantFiled: December 12, 1980Date of Patent: March 2, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Karlheinz Pfoertner
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Patent number: 4234736Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.Type: GrantFiled: October 24, 1978Date of Patent: November 18, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Helmut Link, Harro Stohler
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Patent number: 4230623Abstract: Pyrrolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter described, prepared inter alia from the corresponding pyrrolines, are described. The compounds are useful as analgesic agents.Type: GrantFiled: November 13, 1978Date of Patent: October 28, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Karlheinz Pfoertner, Fernand Schneider, Hans Schmid, deceased, by Mary Margrith Baumann-Schmid, heir, by Maria Albertine Schmid-Suter, heir, by Jeannette Martha Wawrla-Schmid, heir, by Ernst Georges Schmid-Gautschi, heir
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Patent number: 3991197Abstract: Compounds represented by the formula ##SPC1##Wherein R.sup.1 is a pyridyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is hydrogen, lower alkyl or benzyl and R.sup.4 is phenyl or phenyl substituted at one or more carbon atoms with one or more of halogen, lower alkyl, lower alkoxy, nitro or aminoand pharmaceutically acceptable acid addition salts thereof, having analgesic activity are disclosed.Type: GrantFiled: February 12, 1976Date of Patent: November 9, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Karlheinz Pfoertner, Fernand Schneider, Hans Schmid
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Patent number: 3988362Abstract: The present disclosure relates to intermediates 2,2,3-endo-trimethyl-7-anti-amino-norbornanes and N-substituted analogs thereof. In particular the aforesaid compounds have a conventional protective group on the amino moiety and also hydroxymethyl or p-toluenesulfonyl oxymethyl groups in the 3-position.Type: GrantFiled: February 28, 1975Date of Patent: October 26, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Marc Montavon, Hermann Bretschneider, Kraft Hohenlohe-Oehringen, Gunter Weis
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Patent number: 3935246Abstract: Compounds represented by the formula ##SPC1##WhereinR is a cyclopentyl or cycloheptyl andR.sub.1 is a hydrogen, halogen or lower alkoxy,Processes for their production and novel intermediates as well as therapeutic preparations containing the compounds as the active ingredient for amoebicidal or bacteriostatic treatment are disclosed.Type: GrantFiled: December 18, 1974Date of Patent: January 27, 1976Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Erika Bohni, Janos Borgulya