Patents by Inventor Henri Ramuz

Henri Ramuz 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: 4994612
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: February 19, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • Patent number: 4981861
    Abstract: 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: Grant
    Filed: January 5, 1990
    Date of Patent: January 1, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente
  • Patent number: 4847273
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: June 5, 1986
    Date of Patent: July 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • Patent number: 4808605
    Abstract: Compounds of the formula ##STR1## wherein R is lower-alkyl, R.sup.1 is halogen, R.sup.2 is C.sub.1 -C.sub.12 -alkyl, R.sup.3 is hydroxy, lower-alkoxy, lower-alkyl-carbonyloxy, lower-alkoxy-lower-alkylcarbonoyloxy, lower-alkylaminocarbonyloxy, arylaminocarbonyloxy or aryl-lower alkylaminocarbonyloxy, X is C.sub.1 -C.sub.18 -alkylene which optionally can be interrupted by 1,4-phenylene or interrupted or lengthened by 1,4-cyclohexylene, A is di- or tri-substituted 2-imidazolyl attached via an ethylene group or a substituted or unsubstituted heterocycle selected from the group consisting of benzimidazolyl, benzimidazolonyl, imidazo[4,5-c]pyridinyl, imidazo[4,5-c]pyridinonyl, benzthiazolyl, benzodiazepine-2,5-dion-1-yl and pyrrolo[2,1-c]-[1,4]benzodiazepine-5,11-dion-10-yl and n is the number 0 or 1, in the form of racemates and optical antipodes, as well as N-oxides and pharmaceutically usable acid addition salts thereof.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Quirico Branca, Roland Jaunin, Hans P. Maki, Franzi Marti, Henri Ramuz
  • Patent number: 4742069
    Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols A, R and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein.Compounds of formula I have a pronounced calcium-antagonistic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: May 3, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jaunin, Henri Ramuz
  • Patent number: 4692450
    Abstract: Polycyclic salts of the formulaA.sup.- XN.sup.+ CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O);Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar--C.sub.1-4 -alkyl, ArO or Arc(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.
    Type: Grant
    Filed: January 10, 1986
    Date of Patent: September 8, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
  • Patent number: 4680310
    Abstract: Tetrahydronaphthalene derivatives of the formula ##STR1## wherein Y, m, n, R and R.sup.1 to R.sup.9 are as set forth herein, are described.These compounds have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias and high blood pressure. The compounds of formula I can be prepared by the amination of a compound of the formula ##STR2## with a corresponding N-methyl-phenylalkylamine and optional subsequent O-acylation. Compounds of formula II and IV are also described and are within the scope of the invention.
    Type: Grant
    Filed: October 10, 1985
    Date of Patent: July 14, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urs Hengartner, Henri Ramuz
  • Patent number: 4675328
    Abstract: Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.
    Type: Grant
    Filed: January 15, 1986
    Date of Patent: June 23, 1987
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
  • Patent number: 4634710
    Abstract: 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: Grant
    Filed: April 8, 1985
    Date of Patent: January 6, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Albert Fischli, Anna Krasso, Henri Ramuz, Andre Szente
  • Patent number: 4599347
    Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: July 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Henri Ramuz
  • Patent number: 4565869
    Abstract: Novel pyrimidinedicarbamates of the formula ##STR1## wherein R is lower alkyl or (lower alkyloxy)-(lower alkyl) and X is a leaving group,can be manufactured by carbamoylating the corresponding free diamines. They are valuable intermediates and can be used, for example, for the manufacture of corresponding oxadiazolopyrimidines of the formula ##STR2## and pharmaceutically acceptable salts thereof. The latter have valuable long-lasting vasodilating and/or bloodpressure lowering properties and are accordingly suitable especially for the treatment of vascular-conditioned hypertensions or as vasodilators in the case of peripheral blood supply disorders.
    Type: Grant
    Filed: March 7, 1983
    Date of Patent: January 21, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Marquard Imfeld, Henri Ramuz, Peter Vogt, Jean-Claude Muller
  • Patent number: 4554280
    Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: November 19, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Henri Ramuz
  • Patent number: 4549019
    Abstract: 2,4-Disubstituted 6-[3,6-dihydro-1(2H)-pyridyl]pyrimidine-3-oxides of the formula ##STR1## wherein R.sup.1 is lower alkyl or lower alkoxy-lower alkyl, R.sup.2 is hydrogen or --COOR.sup.3 wherein R.sup.3 is lower alkyl or lower alkoxy-lower alkyl,which are important for the preparation of therapeutically valuable 1,2,5,6-tetrahydropyridyl-substituted 2-oxo-2H-[1,2,4]oxadiazolopyrimidinecarbamates, are described. The foregoing oxides of formula I can be prepared by reacting the corresponding arylsulfonyloxy- or alkylsulfonyl-substituted derivatives with 1,2,5,6-tetrahydropyridine.
    Type: Grant
    Filed: July 1, 1982
    Date of Patent: October 22, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz
  • Patent number: 4511720
    Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.
    Type: Grant
    Filed: August 5, 1982
    Date of Patent: April 16, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Henri Ramuz
  • Patent number: 4435406
    Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 or 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
    Type: Grant
    Filed: August 5, 1981
    Date of Patent: March 6, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Henri Ramuz
  • Patent number: 4410698
    Abstract: Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.
    Type: Grant
    Filed: August 13, 1982
    Date of Patent: October 18, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urs Hengartner, Jean-Claude Muller, Henri Ramuz
  • Patent number: 4366160
    Abstract: Imidazole derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3, independently, are hydrogen, halogen, trifluoromethyl, nitro, lower alkyl or lower alkylthio; one of R.sup.4 and R.sup.5 is hydrogen and the other is hydrogen, halogen, hydroxy or lower alkoxy; R.sup.6 is hydrogen or lower alkyl; R.sup.7 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and either R.sup.8 is hydrogen, lower alkyl, lower alkenyl, aryl(lower alkyl) or acyl and R.sup.9 taken together with R is an additional bond, or R.sup.9 is lower alkyl, lower alkenyl or aryl(lower alkyl) and R.sup.8 taken together with R is an additional bond; provided that R.sup.4 or R.sup.5 is not hydroxy when R.sup.7 is lower alkoxy and/or R.sup.8 is acyl, and that R.sup.7 is not hydroxy when R.sup.4 or R.sup.5 is lower alkoxy and/or R.sup.8 is acyl, and their pharmaceutically acceptable acid addition salts are described, the compounds of formula I have valuable therapeutic properties and are especially useful as analgesics.
    Type: Grant
    Filed: August 26, 1981
    Date of Patent: December 28, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Henri Ramuz
  • Patent number: 4360521
    Abstract: Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable, long-lasting vasodilating and/or blood pressure-lowering properties and are useful for the treatment of vascular-conditioned hypertensions or as vasodilators in peripheral blood supply disorders. The compounds are prepared, inter alia, by carbamoylating the corresponding derivative containing a free amino group and optional salt formation.
    Type: Grant
    Filed: December 4, 1982
    Date of Patent: November 23, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Urs Hengartner, Jean-Claude Muller, Henri Ramuz
  • Patent number: 4355033
    Abstract: 2-Imino-imidazolidine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.
    Type: Grant
    Filed: August 14, 1980
    Date of Patent: October 19, 1982
    Assignee: Hoffman-La Roche Inc.
    Inventor: Henri Ramuz
  • Patent number: 4336380
    Abstract: Oxadiazolotriazine derivatives of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, are described.A process for preparing compounds of formula I wherein R.sup.1 is hydrogen, R.sup.2 is a group of the formula --COOR.sup.5, wherein R.sup.5 is as hereinafter set forth, and R.sup.3 is as hereinafter set forth, by cyclizing an intermediate of the formula ##STR2## wherein R.sup.3 and R.sup.5 are as hereinafter set forth, is also described. The compounds of formula I are useful in the treatment of vascular-condition hypertension or also as vasodilators in the case of peripheral blood supply disorders.
    Type: Grant
    Filed: February 17, 1981
    Date of Patent: June 22, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Claude Muller, Henri Ramuz