Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4696930
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is --alkylene'-13 NH.sub.2 or --alkylene'--A'; R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or methyl; A and A' are, independently, unsubstituted or lower alkyl or aryl substituted pyridinyl, imidazolyl, or pyrimidinyl; and when, an asymmetric carbon is present, enantiomers thereof, or racemic mixtures thereof; or pharmaceutically acceptable salts thereof, are described. These compounds are useful as antiarrhythmic agents.
    Type: Grant
    Filed: April 12, 1985
    Date of Patent: September 29, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John G. Mullin, Jr., Keiji Nakamura, Jefferson W. Tilley, Hiroshi Watanabe
  • Patent number: 4694084
    Abstract: Compounds of the general formula ##STR1## wherein two of the residues R.sup.1, R.sup.2 and R.sup.3 represent C.sub.10-30 -alkyl residues with at least 8 C-atoms in a straight chain, at least one of these residues being substituted by at least 2 C.sub.1-3 -alkyl residues and the sum of the C-atoms in the two residues being greater than 20; and the third residue is a residue --P(O)(O.sup.-)OR.sup.4 in which R.sup.4 represents a lower-alkyl or C.sub.5-7 -cycloalkyl residue which is substituted by a quaternary ammonium group or a C.sub.5-7 -cycloalkyl residue which contains a di-(lower-alkyl)-substituted nitrogen atom,are useful for the manufacture of colloidal solution systems. The compounds of formula I can be prepared starting from glycerol derivatives as described in more detail in the specification.
    Type: Grant
    Filed: March 8, 1985
    Date of Patent: September 15, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Manfred Breuninger, Dieter Schmidt
  • Patent number: 4692438
    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: August 12, 1985
    Date of Patent: September 8, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cedric H. Hassall, Geoffrey Lawton, Sally Redshaw
  • 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: 4691040
    Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.
    Type: Grant
    Filed: February 5, 1985
    Date of Patent: September 1, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Aschwanden, Quirico Branca, Emilio Kyburz, Rudolf Pfister
  • Patent number: 4691032
    Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha.,24,25-trihydroxycholecalciferol.
    Type: Grant
    Filed: November 1, 1985
    Date of Patent: September 1, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4689227
    Abstract: The antibacterially-active substance composition consisting of mecillinam and (2S,3S)-3-((Z)-2-(2-amino-4-thiazolyl)-2-((carboxymethoxy)imino)acetamido) -2-((carbamoyloxy)methyl-4-oxo-1-azetidinesulphonic acid (compound A), or pro-drugs and/or pharmaceutically usable salts thereof, has a pronounced synergism against Enterobacter strains which are resistant to mecillinam and which are only moderately sensitive to compound A.
    Type: Grant
    Filed: July 24, 1986
    Date of Patent: August 25, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Peter Angehrn
  • Patent number: 4687859
    Abstract: A novel process for the manufacture of the optically active lactone of the formula ##STR1## is described.
    Type: Grant
    Filed: May 15, 1985
    Date of Patent: August 18, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Horst Pauling, Christof Wehrli
  • Patent number: 4684731
    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 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: March 11, 1983
    Date of Patent: August 4, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Imhof, Emilio Kyburz
  • Patent number: 4681092
    Abstract: An apparatus for wrapping a balloon catheter such as an intra-aortic balloon catheter is disclosed. The wrapping apparatus comprises a housing having a channel which receives the balloon membrane of the intra-aortic balloon. The wrapping apparatus also includes a clutching means located in the channel for exerting a predetermined pressure on the balloon membrane to enable the balloon membrane to be wrapped as the wrapping apparatus is rotated relative to the balloon catheter. The clutching means also permits relatively free rotation of the balloon membrane within the wrapping apparatus after the balloon membrane has been wrapped.The clutching means can include a shoe and a biasing means for biasing the shoe towards the balloon membrane with a predetermined pressure while the balloon membrane is being wrapped, yet enable the balloon membrane to rotate relatively freely within the wrapping apparatus after the balloon membrane has been wrapped to a predetermined degree.
    Type: Grant
    Filed: May 21, 1985
    Date of Patent: July 21, 1987
    Assignee: Kontron Inc.
    Inventors: George E. S. Cho, Stephen B. Kessler
  • Patent number: 4680290
    Abstract: Steroids of the formula ##STR1## wherein n represents the number 2, 3 or 4; R.sup.1 represents hydrogen, lower-alkyl or lower-alkylidene; R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or lower-alkyl and the dotted C--C bonds in the 5(6)-, 7(8)-, 22(23)-, 24(28)- and 25(26)-position are optional, whereby the B-ring can contain only one double bond and the side-chain is either saturated or is mono-unsaturated or is di-unsaturated in the 22(23), 25(26)-position; and whereby R.sup.1 is lower-alkyl or lower-alkylidene when a 5(6)-double bond is present, n is 2 and R.sup.2, R.sup.3 and R.sup.4 are methyl,and pharmaceutically acceptable salts of these steroids have activity inhibiting the intestinal resorption of cholesterol. They can be manufactured from steroids which are otherwise substituted in the 3.beta.-position.
    Type: Grant
    Filed: August 10, 1984
    Date of Patent: July 14, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jean-Marie Cassal
  • Patent number: 4680408
    Abstract: There are presented compounds of the formula ##STR1## wherein R.sup.1 is one of the 3-substituents usable in cephalosporin chemistry, R.sup.2 is hydrogen, lower alkyl or COOR.sup.3 -lower alkyl, wherein R.sup.3 is hydrogen, a cation of a base or a readily hydrolyzable ester group, and X is sulphur, oxygen or one of the groups --SO-- and --SO.sub.2 --, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, also presented are methods for the manufacture of these compounds as well as compounds used in their manufacture.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: July 14, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Reiner, Urs Weiss
  • 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: 4676604
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or straight-chain alkyl; R.sup.2 is --CN, --R, --COR, --COOR or when R.sup.2 is positioned on an aromatic ring R.sup.2 also can be --OR, --OOCR or --F; R is alkyl; A is a group with 1 to 4 six-membered rings, these rings being linked directly with one another and with ring B in each case via a single covalent bond or being linked at one or two positions also via --COO--, --OOC-- or --CH.sub.2 CH.sub.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: June 30, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Martin Petrzilka
  • 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: 4674514
    Abstract: A real-time method and appartus is disclosed for scanning large body areas to produce an ultrasound cross-sectional picture of the area in which at least two different and partially overlapping sector scans of the body are carried out in one scanning plane by the pulse-echo method utilizing an ultrasound transducer unit having a rigid transducer which is pivotable about an axis of oscillation perpendicular to the scanning plane, which performs an oscillatory movement about the axis of oscillation and between two end positions on each scan, and which is segmented into adjacent transducer elements. In performing the scans, at least two different transducer sets are used, each containing one or more transducer elements, each transducer set being used both for the emission of the ultrasound pulses and for the reception of echo waves. In all the scans the position of the axis of oscillation remains unchanged with respect to the body.
    Type: Grant
    Filed: September 23, 1985
    Date of Patent: June 23, 1987
    Assignee: Kontron Holding AG
    Inventors: John G. Abbott, Christoph B. Burckhardt, Pierre-Andre Grandchamp, Peter Krummenacher, Claude Schlaepfer
  • Patent number: 4672033
    Abstract: There is presented antibiotic compounds designated as Antibiotics X-14889 A, C and D of the formulas ##STR1## wherein (for X-14889A) R.sub.1 is methyl, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is hydrogen or (for X-14889C) R.sub.1 is hydrogen, R.sub.2 is methyl, R.sub.3 is hydrogen, R.sub.4 is methyl and R.sub.5 is CO.sub.2 H or ##STR2## and the pharmaceutically acceptable salts thereof. The compounds exhibit antimicrobial activity and one of the compounds X-14889C also exhibits activity against Treponema hyodysenteriae (in vitro), Plasmodium berghei and as food efficiency enhancers in ruminants.Also presented is a process to produce the above compounds and another known component Antibiotic X-14889B.
    Type: Grant
    Filed: May 23, 1985
    Date of Patent: June 9, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, John Westley
  • Patent number: 4672066
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, Y is alkylene; Z is alkylene, ##STR2## the asterisk herein denotes bonding to the substituted acetophenone; R.sub.2 is hydrogen or lower alkoxy; and n is an integer of 1 to 3; A is ##STR3## and HET is a 5-or 6- membered nitrogen containing heterocyclic group, and their acid addition salts. The compounds of formula I of the invention are useful for the treatment of allergic conditions, such as, asthma and cardiovascular diseases, such as, angina and arrhythmias.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: June 9, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
  • Patent number: 4663470
    Abstract: A novel process for the manufacture of quinone derivatives which are suitable as intermediates for the manufacture of (2RS,4'R,8'R)-tocopherol is described. In this process a quinone of the formula ##STR1## is reacted with a phytyl derivative of the formula ##STR2## If desired, the thus-obtained compound of the formula ##STR3## is subsequently converted into the compound of the formula ##STR4## and, if desired, this compound is converted into the compound of the formula ##STR5## The compound of formula V is known and can be converted into (2RS,4'R,8'R)-tocopherol in a known manner.
    Type: Grant
    Filed: October 16, 1986
    Date of Patent: May 5, 1987
    Assignee: Hoffman-La Roche Inc.
    Inventor: August Ruttimann
  • Patent number: 4663161
    Abstract: The present disclosure relates to novel liposome compositions and methods for their preparation. Utilization of the present invention provides an efficient reconstitution of membrane proteins into large (0.1 to 2 micron diameter) phospholipid vesicles with a large, internal aqueous space. The method has been exemplified with the use of glycoproteins of influenza (A/PR8/34) and Sendai (parainfluenza type I) viruses.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: May 5, 1987
    Inventors: Raphael J. Mannino, Susan G. Fogerite