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).

  • Patent number: 5705703
    Abstract: 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: Grant
    Filed: January 21, 1997
    Date of Patent: January 6, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5633371
    Abstract: 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: Grant
    Filed: September 15, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
  • Patent number: 5476875
    Abstract: 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: Grant
    Filed: October 21, 1994
    Date of Patent: December 19, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5389653
    Abstract: 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: Grant
    Filed: April 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5236952
    Abstract: 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: Grant
    Filed: April 16, 1991
    Date of Patent: August 17, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose DaPrada, Gerhard Zurcher
  • Patent number: 4820734
    Abstract: 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: Grant
    Filed: November 4, 1987
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Hans Bruderer
  • Patent number: 4482739
    Abstract: 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: Grant
    Filed: May 12, 1983
    Date of Patent: November 13, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Helmut Link, Harro Stohler
  • Patent number: 4407814
    Abstract: 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: Grant
    Filed: December 14, 1981
    Date of Patent: October 4, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Helmut Link, Harro Stohler
  • Patent number: 4360530
    Abstract: 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: Grant
    Filed: November 12, 1981
    Date of Patent: November 23, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Karlheinz Pfoertner
  • Patent number: 4317914
    Abstract: 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: Grant
    Filed: December 12, 1980
    Date of Patent: March 2, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Karlheinz Pfoertner
  • Patent number: 4234736
    Abstract: Imidazolidine derivatives, as well as processes for their preparation, which have antiandrogenic and schistosomicidal activity.
    Type: Grant
    Filed: October 24, 1978
    Date of Patent: November 18, 1980
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Helmut Link, Harro Stohler
  • Patent number: 4230623
    Abstract: 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: Grant
    Filed: November 13, 1978
    Date of Patent: October 28, 1980
    Assignee: 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
  • Patent number: 3991197
    Abstract: 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: Grant
    Filed: February 12, 1976
    Date of Patent: November 9, 1976
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Karlheinz Pfoertner, Fernand Schneider, Hans Schmid
  • Patent number: 3988362
    Abstract: 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: Grant
    Filed: February 28, 1975
    Date of Patent: October 26, 1976
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Marc Montavon, Hermann Bretschneider, Kraft Hohenlohe-Oehringen, Gunter Weis
  • Patent number: 3935246
    Abstract: 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: Grant
    Filed: December 18, 1974
    Date of Patent: January 27, 1976
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Erika Bohni, Janos Borgulya