Patents Represented by Attorney, Agent or Law Firm Matthew Boxer
  • Patent number: 4886785
    Abstract: Compounds of the formula ##STR1## wherein A is C.sub.1-8 -alkylene, R.sup.1 is halogen, C.sub.1-4 -alkyl or halo-(C.sub.1-4 -alkyl), R.sup.2 is hydrogen, hydroxy or acyloxy, R.sup.3 is hydrogen or C.sub.1-4 -alkyl, R.sup.4 is aryl or aryloxy and X is O or NH,and tautomers thereof are described. The compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the control and prevention of viral infections.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: December 12, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
  • Patent number: 4882316
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl or halo-(C.sub.1-4 - alkyl), R.sup.2 is hydrogen, hydroxy or acyloxy, R.sup.3 and R.sup.4 each are hydrogen or C.sub.1-4 -alkyl, R.sup.5 is aryl or aryloxy, X is O or NH and Y is --CO--CH.sub.2 --, --CH(OH)--CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --S--, --SO-- or --SO.sub.2 --,and tautomers thereof are described. Compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the control and prevention of viral infections.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: November 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
  • Patent number: 4871755
    Abstract: The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2.T signifies lower carbalkoxy.X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy.Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner.and the physiologically compatible salts thereof have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. They are manufactured starting from corresponding primary amines.
    Type: Grant
    Filed: February 5, 1988
    Date of Patent: October 3, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4869895
    Abstract: A compound of the formula: ##STR1## wherein T is tritium; is described as well as intermediates for its preparation. The compound of formula I is useful in vivo for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.
    Type: Grant
    Filed: August 5, 1988
    Date of Patent: September 26, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Burger, Arnold A. Liebman, Clark W. Berry
  • Patent number: 4864058
    Abstract: A process for preparing optically active naphtho[1,2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.
    Type: Grant
    Filed: May 10, 1988
    Date of Patent: September 5, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Erno Mohacsi
  • Patent number: 4859229
    Abstract: The invention is concerned with 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as described herein, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for weed control. The invention is also concerned with herbicidally-active starting materials and weed control compositions containing these.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: August 22, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4826773
    Abstract: A reagent for determining quantitatively the amount of phosphorous in bodily fluids which comprises a surface active agent, a strong acid, ammonium molybdate, a heavy metal chelating compound, and anti-oxidant, and deionized water is described. A method of using such a reagent is also described.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard A. Kaufman, Henry J. Rosenfeld, Denise Zaunczkowski
  • Patent number: 4820835
    Abstract: A compound of the formula: ##STR1## wherein T is tritium; is described as well as intermediates for its preparation. The compound of formula I is useful in an assay for detecting the presence of benzodiazepine receptor occupiers in a warmblooded animal.
    Type: Grant
    Filed: June 30, 1986
    Date of Patent: April 11, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Burger, Arnold A. Liebman, Clark W. Perry
  • Patent number: 4808713
    Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## , R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: February 28, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4808580
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of lower alkoxy and halogen; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## or ##STR3## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.
    Type: Grant
    Filed: December 17, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erno Mohacsi, Jay P. O'Brien
  • 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: 4804502
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is hydrogen or fluorine are described. The compounds of formula I are useful as agents in the treatment of disease states characterized by metabolic calcium deficiencies. Examplary of such disease states are osteoporosis and renal osteodystrophy.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: February 14, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, John J. Partridge, Shian-Jan Shiuey, Gary A. Truitt, Milan R. Uskokovic
  • Patent number: 4801704
    Abstract: There are presented compounds of the formula ##STR1## wherein R.sub.2, R.sub.3, R.sub.4 and m are as described herein.
    Type: Grant
    Filed: May 16, 1988
    Date of Patent: January 31, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Dennis D. Keith, Chung-Chen Wei, Manfred Weigele
  • Patent number: 4792557
    Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: December 20, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ivan Kompis, G/e/ rald Rey-Bellet, Guido Zanetti
  • Patent number: 4774249
    Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present, are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.
    Type: Grant
    Filed: October 23, 1987
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Rita Locher, Hans Maag
  • Patent number: 4774253
    Abstract: Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter J. Machin, John M. Osbond, Christopher R. Self, Carey E. Smithen, Brian P. Tong
  • Patent number: 4772701
    Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonyl-amino-alkly or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl carbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralykoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group; R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.
    Type: Grant
    Filed: November 28, 1986
    Date of Patent: September 20, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael R. Attwood, Cedric H. Hassall, Robert W. Lambert, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4766133
    Abstract: (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: Grant
    Filed: August 6, 1986
    Date of Patent: August 23, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Albert Fischli, Anna Krasso, Andre Szente
  • Patent number: 4764522
    Abstract: Compounds of the formula ##STR1## wherein R is an aromatic, 5- or 6-membered heterocyclic residue, as described herein, and their pharmaceutically usable acid addition salts are described. These compounds have interesting monoamine oxidase inhibiting properties with low toxicity and can accordingly be used for the treatment of depressive states and parkinsonism.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: August 16, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Patent number: 4749710
    Abstract: The invention relates to pharmaceutical compositions comprising at least one Vitamin D derivative and a method of using the pharmaceutical compositions in suppressing immune responses.
    Type: Grant
    Filed: May 1, 1985
    Date of Patent: June 7, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gary A. Truitt, William R. Benjamin, Bruce H. Devens, Maurice K. Gately