Patents Represented by Attorney William G. Isgro
  • Patent number: 4861772
    Abstract: The known compound, t-butyl (S)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][ 1,4]benzodiazepine-1-carboxylate of the formula ##STR1## is effective in the prevention or interruption in a human being of panic states, accompanying phobias and the associated social consequences such as anticipatory anxiety and avoidance behavior. In particular, it is effective in the discontinuous, purely attack-based prevention or interruption of panic states.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: August 29, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Walter Merz
  • Patent number: 4859665
    Abstract: Compositions for treating hypertension comprising an effective amount of a dihydropyridine of the formula ##STR1## in which X is 1 or 2 identical or different substituents from the group consisting of nitro, chlorine and trifluoromethyl, or together with the phenyl ring, the group ##STR2## R.sup.1 is alkyl of 1 to 4 C atoms, which is optionally substituted by alkoxy of 1 to 4 C atoms,R.sup.2 is alkyl of 1 to 12 C atoms, which is optionally substituted by alkoxy of 1 to 3 C atoms, fluorine or N-methyl-N-benzylamino andR.sup.3 is alkyl of 1 to 4 C atoms, cyano or hydroxymethyl, and a pyridazodiazepine of the formula ##STR3## in which R.sup.4 is aralkyl,R.sup.5 is hydrogen or alkyl of 1 to 8 C atoms,R.sup.6 is hydrogen or alkyl of 1 to 8 C atoms andR.sup.7 and R.sup.8 are hydrogen, or together, an oxo group, are described.
    Type: Grant
    Filed: December 2, 1986
    Date of Patent: August 22, 1989
    Assignees: Hoffmann-LaRoche Inc., Bayer Akt.
    Inventors: Bernward Garthoff, Marcel Gerold, Fridolin Hefti, Stanislav Kazda, Andreas Knorr
  • Patent number: 4855297
    Abstract: The compounds of the formula ##STR1## wherein Ra,R.sub.b,R.sub.c R.sub.d are defined in the specification and pharmaceutically acceptable addition salts are disclosed.The compounds of formula I have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relevant, seditive-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, isomnia, anxiety states and/or convulsions.
    Type: Grant
    Filed: December 4, 1986
    Date of Patent: August 8, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Widmer Ulrich
  • Patent number: 4851519
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or , when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a)in which A is a C.sub.1-8 alkylene group which is optionally substituted by one or two phenyl groups,Z is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen,R.sup.4 is unsubstituted phenyl, R.sup.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: July 25, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Lambert, Joseph A. Martin, Gareth J. Thomas
  • 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: 4826980
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --N(R.sup.6)-- in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    Type: Grant
    Filed: July 12, 1988
    Date of Patent: May 2, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4814332
    Abstract: The imidazolium compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and their pharmaceutically acceptable acid addition salts, which possess valuable pharmacological properties are described. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties and are especially active against parasitic protozoa and worms. The compounds of formula I can be prepared according to known methods.
    Type: Grant
    Filed: May 4, 1987
    Date of Patent: March 21, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventors: Wilhelm Klotzer, Helmut Link, Renate Mussner, Werner Schiestl, Nicolas Singewald
  • Patent number: 4808727
    Abstract: The pharmaceutically acceptable salts corresponding to the imidazolium hydrogen carbonates of the formula ##STR1## wherein the symbol Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group or the group --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.
    Type: Grant
    Filed: September 29, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-LaRoche Inc.
    Inventor: Helmut Link
  • Patent number: 4808736
    Abstract: In this process of the invention a compound of the formula ##STR1## wherein R is a leaving group, is reacted with a compound of the formula ##STR2## wherein R.sup.1 is an ether protecting group, and, if desired a thus-obtained compound of the formula ##STR3## is converted in a known manner into d-.alpha.-tocopherol.
    Type: Grant
    Filed: August 10, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4808631
    Abstract: Use of compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, independently are hydrogen, alkyl, or C.sub.3-7 -cycloalkyl or two adjacent residues R.sup.1 to R.sup.5 taken together with adjacent carbons of the phenyl ring form a 5- to 7-membered ring optionally substituted by one or more lower alkyl groups; X is --NR.sup.7 --CO-- or --CO-NR.sup.7 --; R.sup.6 is hydroxy, lower-alkoxy or --NR.sup.8 R.sup.9 ; and R.sup.7, R.sup.8 and R.sup.9, independently, are hydrogen or lower-alkyl, and where R.sup.6 is hydroxy, their pharmaceutically usable salts, for the treatment of inflammatory and rheumatic diseases.
    Type: Grant
    Filed: October 14, 1987
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Michael Klaus
  • Patent number: 4806541
    Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: February 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
  • Patent number: 4800206
    Abstract: Pyridine-ethanolamines of the formula ##STR1## wherein n, X, Y, R.sup.1, R.sup.2 and R.sup.3 have the significances given in the description, their corresponding enantiomers, diastereomers, and racemates as well as the pysiologically compatible salts thereof are describe. The compounds of formula I have catabolic activity and can be used for the treatment of obesity and of diabetes mellitus or of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. The compounds of formula I can be prepared by alkylating the primary or secondary amines corresponding to the secondary or tertiary amines of formula I.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: January 24, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Marcel Muller
  • Patent number: 4788206
    Abstract: Compounds of the formula ##STR1## Y is O ir S, *A is paraphenylene or *----(CH.sub.2)n----(X).sub.m --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: November 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4786646
    Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: November 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4785093
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, alkanoyl or aroyl; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen or aryl; R.sup.4 and R.sup.5 each are hydrogen or R.sup.4 and R.sup.5 taken together are oxo; and Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --or--N(R.sup.6)--in which R.sup.6 is hydrogen, alkyl or aralkyl, as well as pharmaceutically acceptable salts thereof with bases when R.sup.2 is hydrogen and pharmaceutically acceptable salts thereof with acids when Y is --N(R.sup.6)--, which have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations, are described.The compounds of formula I contain at least one asymmetric carbon atom. Therefore, the invention comprises not only the optically uniform forms of these compounds, but also the various diastereoisomeric racemates and mixtures of different diastereoisomeric racemates.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: November 15, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • Patent number: 4782176
    Abstract: Phenoxycarboxylic acids of the formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 R.sub.5, Z and n are as hereinafter set forth, are as described. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A), which renders them useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: May 23, 1983
    Date of Patent: November 1, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ronald A. LeMahieu, William C. Nason
  • Patent number: 4775671
    Abstract: There is presented compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. signifies one of the groups ##STR2## and the dotted line signifies the double bond present in cases (1), (2) and (4) and wherein R.sup.1 signifies a 5- or 6-membered aromatic heterocyclic group or the group --C(R.sup.6).dbd.NOR.sup.7 (B), R.sup.2 signifies hydrogen and R.sup.3 signifies hydrogen or lower alkyl or R.sup.2 and R.sup.3 together signify dimethylene, trimethylene or propenylene, R.sup.4 and R.sup.5 each signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl, R.sup.6 signifies hydrogen or lower alkyl and R.sup.7 signifies lower alkyl, the compound of formula I having the (S) or (R,S) configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.
    Type: Grant
    Filed: November 18, 1987
    Date of Patent: October 4, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz
  • Patent number: 4775756
    Abstract: The invention relates to substituted phenylbarbituric acids of the formula ##STR1## wherein R.sup.1 and R.sup.3, independently, are lower-alkoxy or lower-alkylthio; R.sup.2 is lower-alkoxy, hydroxy or amino; and R.sup.4 is hydrogen; or R.sup.1 and R.sup.2 are lower-alkoxy, R.sup.3 is hydrogen and R.sup.4 is lower-alkyl,which are prepared from correspondingly substituted benzene derivatives and alloxan. The compounds of formula I can be converted into substituted benzaldehydes which in turn are known intermediates in the preparation of pharmaceutically valuable benzylpyrimidines.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: October 4, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Dieter Kagi
  • Patent number: 4735940
    Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: April 5, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
  • Patent number: 4732902
    Abstract: The invention relates to long-acting depot producing antipsychotic pyrroloisoquinolinyl-dimethyloxoalkyl alkanoates of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently, are hydrogen, alkyl of 1 to 4 carbon atoms, cycloalkyl or alkenyl, or taken together are alkylene of 3 to 6 carbon atoms; and R.sub.3 is hydrogen, alkyl, hydroxyalkyl, phenylhydroxyalkyl, halophenylhydroxyalkyl, alkylphenylhydroxyalkyl, alkoxyphenylhydroxyalkyl, alkoxyalkyl, aryloxyhydroxyalkyl, alkoxyhydroxyalkyl, acyloxyalkyl, arylcarbonylalkyl, alkoxycarbonylalkyl, aralkyl, alkenyl, alkylcycloalkyl, alkynyl, thienylalkyl, furylalkyl, arylcarboxamidoalkyl, acylalkyl, cyclic-alkyloxoalkyl, cyclic-alkylhydroxyalkyl, alkenyloxyalkyl, aralkenyl, aryloxyalkyl, or aryl-N-imidazolonylalkyl; R.sub.4 is alkyl; and n is the integer 2 or 3,their corresponding optical isomers, geometric isomers, and mixtures thereof, and the pharmaceutically acceptable acid additional salts.The compounds of formula I are useful as antipsychotic agents.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: March 22, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson