Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4834534
    Abstract: A flow cell for high performance chromatography, in which the measuring chamber is formed by a bore (12) in a plate (11) and the supply and discharge ducts are formed by bores (13, 14) in the plate (11) communicating with grooves (16, 18) in the plate surfaces (15, 17), the grooves being covered by transparent plates (19, 20) bonded on the plate surfaces, and thus forming closed ducts.
    Type: Grant
    Filed: April 21, 1988
    Date of Patent: May 30, 1989
    Assignee: Kontron Holding A.G.
    Inventor: Peter Wiget
  • Patent number: 4830470
    Abstract: Compounds of the formula ##STR1## wherein m represents is the number 0 or 1; A is a single covalent bond, --CH.sub.2 --CH.sub.2 --, --OCH.sub.2 --, --COO-- or --OOC--; rings B, C and D are 1,4-phenylene optionally substituted with cyano, halogen or lower alkyl; Y.sup.1 and Y.sup.2 are hydrogen or one of them also is cyano; and R.sup.1 and R.sup.2 each represents C.sub.1 -C.sub.18 -alkyl or C.sub.2 -C.sub.18 alkenyl, either of which is optionally halogen-substituted, in which one CH.sub.2 group or two non-adjacent CH.sub.2 groups is/are optionally replaced by oxygen; with the provisos that at least one of R.sup.1 and R.sup.2 has a chiral carbon atom or a C--C double bond or both when A is --COO-- and at least one of R.sup.1 and R.sup.2 has a C--C double bond when A is a single covalent bond, their preparation, liquid crystalline mixtures containing these compounds and their use for electro-optical purposes are described.
    Type: Grant
    Filed: May 20, 1987
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Buchecker, Hans-Jurgen Fromm, Stephen Kelly, Martin Schadt
  • Patent number: 4831130
    Abstract: Compounds of the formula ##STR1## wherein A is one of the following: ##STR2## in which R.sub.1, is acyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxycarbonyl or aminocarbonyl, R.sub.3 is hydrogen or lower alkyl and R.sub.4 and R.sub.4 ' are hydrogen, lower alkyl, lower alkoxy, acyl or aralkyl, as well as pharmaceutically acceptable salts of such compounds, are useful as antibacterial agents.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: May 16, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Harry A. Albrecht, Frederick M. Konzelmann, Dennis D. Keith
  • 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: 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: 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: 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: 4816581
    Abstract: The novel compounds of the formula ##STR1## wherein R.sup.11 signifies hydrogen, acyl or tri(lower alkyl)silyl, R.sup.2 signifies a phenyl group which is substituted in the o- and/or the p-position by halogen, lower alkyl, lower alkylthio or lower alkoxy and n signifies the number 0 or 2, and mixtures thereof with the corresponding optical antipodes are valuable intermediates for the manufacture of antimicrobially active penems and carbapenems which have as a common structural element a (R)-1-hydroxyethyl group in the 6-position. They can be manufactured by reacting a compound of the formula ##STR2## wherein R.sup.12 signifies acyl, tri(lower alkyl)silyl or a group of the formula --BR.sup.3 R.sup.4 and R.sup.3 and R.sup.4 have the same significance and each signify a branched-open chain, cyclic or bicyclic hydrocarbon residue with 5-10 carbon atoms or together signify an open chain or cyclic hydrocarbon residue with 5-10 carbon atoms and two free valencies and R.sup.
    Type: Grant
    Filed: September 28, 1987
    Date of Patent: March 28, 1989
    Assignee: Hoffman-La Roche Inc.
    Inventor: Gerard Schmid
  • Patent number: 4816476
    Abstract: Heterocyclic compounds of the formula ##STR1## wherein X is --CH.dbd.CH--, --O-- or --S--; R.sup.1 is a group Ar--R.sup.2 or --CH.dbd.CH--C(CH.sub.3).dbd.CH--R.sup.21 ; Ar is phenyl, pyridyl, furyl or thienyl; R.sup.2 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3, lower-alkylsulphonyl or formyl; R.sup.21 is a group --CO.sub.2 R.sup.3, --C(O)R.sup.4, --CH.sub.2 OR.sup.3 or formyl; R.sup.3 is hydrogen or lower-alkyl and R.sup.4 is hydrogen, hydroxy, amino, lower alkylamino, di-(lower alkyl)amino or lower-alkyl; at least one ring of the molecule being heterocyclic, salts thereof, processes for their preparation, rodenticidal compositions containing these compounds as the active ingredient and methods of use of the rodenticidal compositions are disclosed.
    Type: Grant
    Filed: December 12, 1986
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger, Harald Weiser
  • Patent number: 4816582
    Abstract: Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula ##STR1## in which H.sub.2 N ##STR2## represents an amino-substituted thiazolyl group, R.sup.1 is lower alkyl which is substituted by carbamoyl, lower alkylsuphonyl, azido, piperidine-carbonyl, (hexahydro-1H-azepin-1-yl)carbonyl or lower alkynyl, and R.sup.2 is hydrogen or a lower organic group, typically, carbamoyloxymethyl.
    Type: Grant
    Filed: October 22, 1987
    Date of Patent: March 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • 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: 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: 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: 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: 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: 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: 4808630
    Abstract: This invention is directed towards methods for treating patients having a psychotic illness such as schizophrenia and/or inhibiting the occurrence of movement disorders in patients receiving or having received a neuroleptic medication by administering to the patients a pharmaceutically effective amount of a retinoid, such as retinoic acid, and particularly isotretinoin.
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: February 28, 1989
    Assignee: United States of America
    Inventor: Gregory M. Straw
  • 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: 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: 4805821
    Abstract: An ampule opener is provided for automatically opening ampules. The ampule opener is especially suitable for use in a robotic sterility test system and is provided with a pneumatic actuator means releasably connected to an ampule opener arm. The head of an ampule is positioned with its neck on a knife edge so that when the ampule opener arm is rotated by the actuator means, the arm applies a pressure on the head of the ampule and the ampule head drops away.
    Type: Grant
    Filed: August 14, 1987
    Date of Patent: February 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ludwik Kowalczyk, Gilbert C. Kaetzel