Patents Represented by Attorney William G. Isgro
  • Patent number: 4407754
    Abstract: The vitamin D.sub.3 derivative 1.alpha.,25,26-trihydroxycholecalciferol which is useful for regulating the calcium metabolism or calcium transport in the body, cholestene intermediates and a process for their preparation are described.
    Type: Grant
    Filed: March 12, 1982
    Date of Patent: October 4, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4399136
    Abstract: Compounds of the formula ##STR1## wherein A is methylene, ethylene or propylene which may be substituted by lower alkyl, B is carbonyl or methylene, R.sup.1 is halogen, carboxyl, lower alkoxycarbonyl, hydroxyaminocarbonyl, mercapto, lower alkanoylthio or aryl(lower alkylthio)--, R.sup.2 is hydroxy, lower alkoxy or amino, R.sup.3 is hydrogen, lower alkyl, aryl or aryl(lower alkyl)--, R.sup.4 is hydrogen, lower alkyl, aryl, aryl-(lower alkyl)-- or a group of the formula --A-R.sup.1 wherein A and R.sup.1 are as described above and the broken line denotes an optional carbon-carbon bond which can be present only when B is carbonyl,and salts of the acids of formula I with pharmaceutically acceptable bases, a process for the manufacture thereof and pharmaceutical preparations containing same, are described. The compounds of formula I and their salts are useful as antihypertensive agents.
    Type: Grant
    Filed: June 10, 1981
    Date of Patent: August 16, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Christopher J. Moody
  • Patent number: 4397847
    Abstract: The present invention relates to a method of treating osteoporosis by administering to a host suffering from osteoporosis an effective amount of 24,24-difluoro-1.alpha.,25-dihydroxycholecalciferol.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: August 9, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Boris, John J. Partridge, Milan R. Uskokovic
  • Patent number: 4395559
    Abstract: 2,3-Indoledione derivatives of the formula ##STR1## wherein R is isopropyl or tert.butyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is lower alkyl or lower aralkyl, and their pharmaceutically acceptable acid addition salts, prepared from a compound of the formula ##STR2## wherein R.sup.3 is hydroxy and R.sup.4 is chlorine or bromine or R.sup.3 and R.sup.4, taken together, are oxygen, and R.sup.1 and R.sup.2 are as previously set forth, are described. The compounds of formula I and their pharmaceutically acceptable addition salts are useful as .beta.-adrenergic blocking agents and antihypertensive agents.
    Type: Grant
    Filed: December 1, 1980
    Date of Patent: July 26, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Graham A. Fothergill, John M. Osbond
  • Patent number: 4395350
    Abstract: Liquid crystal mixtures containing a coloring substance which comprise about 5 to about 40 weight % of trans-p-[5-(4-alkylcyclohexyl)-2-pyrimidinyl]benzonitriles, about 10 to about 60 weight % of trans-4-alkylcyclohexane carboxylic acid phenyl esters and about 0.1 to about 15 weight % of one or more coloring substances of the formula ##STR1## wherein m stands for the number 1 and X is alkoxy and Y is nitro; or m stands for the number 1 or 2; and X is p-alkoxyphenyl and Y is nitro or dialkylamino, or X is alkoxy and Y is -p-nitrophenyl or -(dialkylamino)phenyl; or m stands for the number 2, and X is alkoxy and Y is alkoxy, nitro or dialkylamino, or both X and Y are dialkylamino; and wherein the alkoxy denotes a straight-chain group containing 1 to 12 carbon atoms and the alkyl groups in the dialkylamino each denote a straight-chain alkyl group containing 1 to 4 carbon atoms are described.
    Type: Grant
    Filed: July 1, 1981
    Date of Patent: July 26, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Alfred Germann, Martin Schadt, Alois Villiger
  • Patent number: 4391731
    Abstract: Compounds of the formula ##STR1## wherein ring A is saturated or aromatic and a saturated ring A which may be present is trans-linked with the second ring; R.sup.1 is a straight-chain alkyl or alkoxy group containing 1 to 11 carbon atoms; R.sup.2 is cyano, a straight-chain alkyl group containing 1 to 11 carbon atoms, an ester group of the formula ##STR2## or, when ring A is saturated, additionally a straight-chain alkoxy group containing 1 to 11 carbon atoms; in the ester group of formula II ring B is either aromatic and X is oxygen or sulfur and R.sup.3 is cyano or a straight-chain alkyl or alkoxy group containing 1 to 10 carbon atoms, or ring B is a trans-1,4-disubstituted cyclohexane ring and X is oxygen and R.sup.3 is cyano or a straight-chain alkyl group containing 1 to 10 carbon atoms; and the total number of carbon atoms in the alkyl and/or alkoxy groups amounts to at most 12, are described. The compounds of formula I are useful in liquid crystal mixtures.
    Type: Grant
    Filed: August 3, 1981
    Date of Patent: July 5, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Martin Schadt, Alois Villiger
  • Patent number: 4391978
    Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 is acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.
    Type: Grant
    Filed: April 9, 1981
    Date of Patent: July 5, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Patent number: 4390540
    Abstract: Imidazoquinazolines of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, halogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.2-5 -alkoxyalkyl; or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy; and R.sup.4 and R.sup.5 are hydrogen or C.sub.1-4 -alkyl,and their tautomers, as well as their physiologically compatible acid addition salts, are described.The compounds of formula I inhibit the aggregation of the blood platelets, as well as gastric acid secretion, and have activity on the circulatory system.
    Type: Grant
    Filed: August 12, 1981
    Date of Patent: June 28, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Madhukar S. Chodnekar, Ado Kaiser, Frank Kienzle
  • Patent number: 4389329
    Abstract: Pyrimidine derivatives of the formula ##STR1## wherein at least one of rings A and B is a trans-1,4-disubstituted cyclohexane ring and the other, optionally, may be aromatic and R is straight-chain alkyl or alkoxy of 1 to 10 carbon atoms or a branched-chain alkyl group of the formula C.sub.2 H.sub.5 --CH(CH.sub.3)--(CH.sub.2).sub.n -- wherein n is 1, 2 or 3, are described. Processes for the preparation of the compounds of formula I as well as their uses in liquid crystalline mixtures are also described.
    Type: Grant
    Filed: January 30, 1981
    Date of Patent: June 21, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Martin Schadt, Alois Villiger
  • Patent number: 4388467
    Abstract: Neuroleptically active cycloalka[4,5]pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein n, R.sub.1, R.sub.2 and X are as hereinafter set forth, and intermediates therefore are described.
    Type: Grant
    Filed: March 25, 1982
    Date of Patent: June 14, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson
  • Patent number: 4387100
    Abstract: Phenoxy-aminopropanol derivatives of the formula ##STR1## wherein R is lower alkyl, X is oxygen or sulfur, n is the integer zero or 1, Y is methylene, ethylene or propylene or, when n is zero, Y can also be a group of the formula--CH.dbd.CH--C*H.sub.2 -- (a), wherein the double-bond is trans and the carbon atom marked with an asterisk is linked to Z, and Z is a 5-membered aromatic heterocyclic ring which contains one or more nitrogen atoms as the sole hetero atom (s), said heterocyclic ring is linked to Y via a nitrogen atom, and may be substituted by halogen, lower alkyl, lower alkoxy, aryl, cyano or carboxamido, or on adjacent carbon atoms by a group of the formula ##STR2## and pharmaceutically acceptable acid addition salts thereof are described. A process for the preparation of the compound of formula I and pharmaceutical preparations containing them are also described. The aforementioned compounds and salts possess .beta.-adrenergic blocking activity and antihypertensive activity.
    Type: Grant
    Filed: February 24, 1981
    Date of Patent: June 7, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Peter J. Machin
  • Patent number: 4382945
    Abstract: Imidazole derivatives of the formula ##STR1## wherein X is hydrogen or C.sub.1-4 -alkyl, Y is sulfur, sulfinyl or sulfonyl and Z is thienyl, optionally substituted by methyl or fluorine, or a group of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are hydrogen, methyl, fluorine, hydroxy, methoxy, methylthio or two of R.sup.1, R.sup.2 and R.sup.3 on adjacent carbon atoms taken together are methylenedioxy or ethylenedioxy or one of R.sup.1, R.sup.2 and R.sup.3 is mono- or di-(C.sub.1-4 -alkyl)-amino and the other two are hydrogen,and physiologically or pharmaceutically compatible or acceptable acid addition salts thereof, are described. The compounds of formula I inhibit the aggregation of the blood platelets and have antihyperglycemic activity.
    Type: Grant
    Filed: April 16, 1981
    Date of Patent: May 10, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Romano Derungs
  • Patent number: 4376121
    Abstract: Antiallergically-active pyrimidine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, chlorine, bromine or C.sub.1-4 -alkyl, and R.sup.2 is hydrogen or methyl, prepared starting from corresponding 4-oxothieno-[3,2-d]pyrimidine derivatives, are described.
    Type: Grant
    Filed: June 19, 1981
    Date of Patent: March 8, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Frank Kienzle
  • Patent number: 4374139
    Abstract: Levorotatory N-substituted acylmorphinans of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl-lower alkyl, cyano-lower alkyl, aryl-lower alkyl, or 5- or 6-membered heterocyclic-lower alkyl, and one of R.sub.2 or R.sub.3 is hydrogen and the other of R.sub.2 or R.sub.3 is alkanoyl of 2 to 7 carbon atoms, aroyl, trifluoromethylcarbonyl or ##STR2## wherein R is hydrogen or lower alkyl and n is an integer of 0 to 6, and salts thereof with pharmaceutically acceptable acid addition salts, are described. The compounds of formula I are useful as analgesic agents.
    Type: Grant
    Filed: November 9, 1981
    Date of Patent: February 15, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ernest Mohacsi
  • Patent number: 4374261
    Abstract: 1-Ethyl-1,4-dihydro-6-(2-naphthyl)-4-oxonicotinic acid and C.sub.1-6 -alkyl esters thereof as well as their alkali metal, alkaline earth metal or ammonium salts are described. The foregoing compounds are useful as central nervous system stimulants. Also described are 1-ethyl-6-(2-naphthyl)-4-oxo-1,4,5,6-tetrahydronicotinic acid and C.sub.1-6 -alkyl esters thereof, which are useful as intermediates.
    Type: Grant
    Filed: October 28, 1981
    Date of Patent: February 15, 1983
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Alexander E. Wick
  • 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: 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: 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: 4349678
    Abstract: Neuroleptically active octahydro-1H-pyrrolo[2,3-g]isoquinolines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as hereinafter set forth, are described.
    Type: Grant
    Filed: December 12, 1980
    Date of Patent: September 14, 1982
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Berger, Gary L. Olson