Patents by Inventor Hans Bruderer

Hans Bruderer 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: 5574055
    Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R is H or alkyl;Y.sup.1 is --CH.dbd. or --N.dbd.; andY.sup.2 --CH.dbd., --C(OH).dbd., --C(NO.sub.2).dbd., --C(NH.sub.2).dbd., --C(Hal).dbd., --N.dbd.;X is cycloalkenyl; bicyclo[2.2.1]hept-2-yl, optionally substituted by phenyl-2-oxo-5 -methoxymethyl-oxazolidinyl; bicyclo[2.2.1]-hept-5 -en-2-yl; adamantyl; or cycloalkyl or piperidinyl, optionally substituted by amino, alkyl, --CN, oxo hydroxyimino, ethylenedioxyor by --OR.sup.1,R.sup.1 is --CH(C.sub.6 H.sub.5).sub.2, --(CH.sub.2).sub.n C.sub.6 H.sub.5, alkyl, H, --(CH.sub.2).sub.n NHCOCH.sub.3, --(CH.sub.2).sub.n NH.sub.2, --(CH.sub.2).sub.n CN, --(CH.sub.2).sub.n SCH.sub.3 --(CH.sub.2).sub.n SO.sub.2 CH.sub.3, --CO-lower-alkyl, --COC.sub.6 H.sub.5, optionally substituted by oxazolidine;or by .dbd.CR.sup.2 R.sup.3,R.sup.2 is alkylR.sup.3 is H, --CN, alkyl, phenyl or COO-alkyl;or by --(CH.sub.2).sub.n R.sup.4R.sup.4 is --CN, amino, --NHCOCH.sub.3, --COC.sub.6 H.sub.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: November 12, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Janos Borgulya, Hans Bruderer, Roland Jakob-Roetne, Stephan R over
  • 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: 5318967
    Abstract: 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: Grant
    Filed: September 3, 1993
    Date of Patent: June 7, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
  • Patent number: 5318966
    Abstract: 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: Grant
    Filed: July 16, 1993
    Date of Patent: June 7, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Thierry Godel, Rene Imhof, Roland Jakob-Roetne
  • 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: 4833245
    Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position of X, and their acid addition salts, processes for their manufacture, pest control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of pests. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: May 23, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Renee Zurfluh
  • 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: 4766115
    Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position to X, and their acid addition salts, processes for their manufacture, insect control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of insects. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: August 23, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Rene Zurfluh
  • Patent number: 4559403
    Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is a lower alkoxy, n is the integer zero or 1, andA is ##STR2## wherein R.sub.1 is phenyl halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: December 17, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Richard W. Kierstead, John G. Mullin, Jr., Keiji Nakamura, Mitsuru Tateishi, Sidney Teitel, Jay P. O'Brien
  • Patent number: 4544657
    Abstract: Substituted isoquinolines of the formula ##STR1## wherein R is lower alkoxy, n is the integer zero or 1, and A is ##STR2## wherein R.sub.1 is phenyl, halophenyl, lower-alkylphenyl or lower-alkoxyphenyl, and pharmaceutically acceptable acid addition salts thereof, are described. The compounds of formula I are useful in the treatment of cerebral and cardiac ischemias.
    Type: Grant
    Filed: May 19, 1983
    Date of Patent: October 1, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Richard W. Kierstead, John G. Mullin, Jr., Keiji Nakamura, Mitsuru Tateishi, Teitel Sidney, Jay P. O'Brien
  • Patent number: 4448991
    Abstract: Cyclohexenes of the formula ##STR1## wherein R.sup.1 is hydroxy or lower alkoxy; n is 1 or 2; R.sup.2 is lower alkyl; and R.sup.3 is hydrogen, lower alkyl, lower alkenyl or lower cycloalkylmethyl,and their pharmaceutically acceptable acid addition salts are disclosed. The compounds of formula I have analgesic activity and are useful for the control of pains.
    Type: Grant
    Filed: March 24, 1982
    Date of Patent: May 15, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Albert E. Fischli, Rudolf Pfister
  • Patent number: 4336268
    Abstract: Cyclohexenes of the formula ##STR1## wherein R.sup.1 is hydroxy or lower alkoxy; n is 1 or 2; R.sup.2 is lower alkyl; and R.sup.3 is hydrogen, lower alkyl, lower alkenyl or lower cycloalkylmethyl, and their pharmaceutically acceptable acid addition salts are disclosed. The compounds of formula I have analgesic activity and are useful for the control of pains.
    Type: Grant
    Filed: January 27, 1981
    Date of Patent: June 22, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Bruderer, Albert E. Fischli, Rudolf Pfister