Patents Represented by Attorney Bernard S. Leon
  • Patent number: 4628738
    Abstract: An ultrasonic imaging apparatus for operation in either or both linear and sector scan modes is disclosed which employs a common array of transducers. Circuitry is provided for controlling the order and timing of pulse echo transmission and reception, which further include control circuitry to operate variable delay and switching circuitry to generate transmission signals to be applied to the transducers, and to direct echo signals received by the transducers for processing to provide the image of the structures being inspected. Suitable interconnection/switching circuitry is provided so as to minimize prior art requirements for use of different elements for the separate scanning modes, with concomitant expenses associated with the larger number of components being reduced.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: December 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph B. Burckhardt, Rainer Fehr, Peter Krummenacher
  • Patent number: 4629581
    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: June 26, 1985
    Date of Patent: December 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Martin Petrzilka, Martin Schadt
  • Patent number: 4628115
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl, Z is alkylene of 1 to 10 carbon atoms, --(C*H.sub.2).sub.3 --C.tbd.C--, --C*H.sub.2 --C.tbd.C--(CH.sub.2).sub.3 --, and --(CH.sub.2).sub.2 O].sub.n (CH.sub.2).sub.2 -- wherein n is an integer of 1 to 3, the carbon atom marked with an asterisk is linked to the phenoxy moiety,and salts thereof with pharmaceutically acceptable bases. The compounds of formula I are antagonists of slow reacting substance of anaphylaxis (SRS-A; leukotrienes C.sub.4, D.sub.4 and E.sub.4), which renders them useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: March 25, 1985
    Date of Patent: December 9, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ronald A. LeMahieu, William C. Nason
  • Patent number: 4621901
    Abstract: Liquid crystalline mixtures containing compounds of the formula ##STR1## wherein n stands for the number 0 or 1; X.sup.1 and X.sup.2 denote single covalent bonds or one of the symbols X.sup.1 and X.sup.2 also denotes --COO--, --OOC-- or --CH.sub.2 CH.sub.2 --; the rings A.sup.1, A.sup.2, and A.sup.3 represent 1,4-phenylene, 2-fluoro-1,4-phenylene or trans-1,4-cyclohexylene or one of these rings also represents a 2,5-disubstituted pyrimidine ring or a trans-2,5-disubstituted m-dioxane ring; R.sup.1 signifies 4-alkenyl or on a cyclohexyl ring also 2Z-alkenyl; and R.sup.2 denotes alkyl, alkoxy, --CN or --NCS,as well as the manufacture of these compounds and the use for electro-optical purposes are described.
    Type: Grant
    Filed: June 26, 1985
    Date of Patent: November 11, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt
  • Patent number: 4619787
    Abstract: The novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, a residue readily removable by reduction, lower 1-hydroxyalkyl or lower alkanoyl andR.sup.2 is hydrogen, or each of R.sup.1 and R.sup.2 is a residue readily removable by reduction;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or a readily removable protecting group; andA is lower alkylidene or (C.sub.5-7)-cycloalkylidene,are valuable intermediates for the manufacture of antimicrobially-active .beta.-lactams.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: October 28, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Erwin Gotschi, Christian Hubschwerlen
  • Patent number: 4620013
    Abstract: Novel chiral phosphines are disclosed which when complexed with rhodium provide catalyst compositions for asymmetric hydrogenations.
    Type: Grant
    Filed: June 14, 1985
    Date of Patent: October 28, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Emil A. Broger, Yvo Crameri
  • Patent number: 4617297
    Abstract: The present invention relates to the method of treating disease states characterized by higher than normal levels of endogenously produced 1.alpha.,25 dihydroxy-cholecalciferol or conditions where there is an increased sensitivity to 1.alpha., 25 dihydroxy-cholecalciferol by administering to an organism suffering from such a disease state a pharmaceutically effective amount of the R or S epimer of 1.alpha.,25,26 trihydroxy-cholecalciferol.
    Type: Grant
    Filed: April 3, 1984
    Date of Patent: October 14, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Boris, John J. Partridge, Milan R. Uskokovic
  • Patent number: 4617150
    Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: October 14, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian N. Hubschwerlen, Gerard Schmid
  • Patent number: 4616091
    Abstract: Naphthalenyloxy carboxylic acids of the formula ##STR1## wherein X, R, m and n are as hereinafter set forth, are 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: January 8, 1986
    Date of Patent: October 7, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Ronald A. LeMahieu
  • Patent number: 4616010
    Abstract: Compounds which are imidazodiazepine derivatives of the formula ##STR1## wherein A together with the carbon atoms denoted by .alpha. and .beta. signifies the group ##STR2## one of R.sup.1 and R.sup.2 signifies hydrogen and the other signifies hydrogen, halogen or trifluoromethyl, R.sup.3 and R.sup.4 each signify hydrogen or halogen and n signifies the number 2 or 3, the compounds having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma., and their pharmaceutically acceptable acid addition salts have been discovered which possess anxiolytic, anticonvulsant, muscle relaxant and sedative-hypnotic properties. They can be prepared into compositions, including pharmaceutically acceptable ones, using suitable inert carriers.
    Type: Grant
    Filed: February 20, 1986
    Date of Patent: October 7, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Walter Hunkeler, Emilio Kyburz
  • Patent number: 4613208
    Abstract: A liquid crystalline mixture comprising(a) at least one compound of the formula: ##STR1## wherein R.sup.1 is alkyl, alkoxy, p-alkylphenyl, p-alkoxyphenyl, trans-4-alkylcyclohexyl, 4'-alkyl-4-biphenylyl, p-(trans-4-alkylcyclohexyl)phenyl, 2-(trans-4-alkylcyclohexyl)ethyl or p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl and R.sup.2 is trans-4-alkylcyclohexyl; or R.sup.1 is trans-4-alkylcyclohexyl and R.sup.2 is p-(trans-4-alkylcyclohexyl)phenyl, p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl or 4'-(trans-4-alkylcyclohexyl)-4-biphenylyl; or R.sup.1 is p-alkylphenyl and R.sup.2 is p-[2-(trans-4-alkylcyclohexyl)ethyl]phenyl; and the alkyl and alkoxy groups in the substituents R.sup.1 and R.sup.2 are straight-chain groups of 1 to 7 carbon atoms, and;(b) at least one dichroic coloring substance selected from the group of compounds consisting of: ##STR2## wherein R.sup.3 is straight-chain C.sub.1 -C.sub.12 -alkyl and R.sup.4 is straight-chain C.sub.1 -C.sub.4 -alkyl, Z.sup.1 is hydrogen or chlorine, one of the symbols Z.
    Type: Grant
    Filed: November 18, 1983
    Date of Patent: September 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Arthur Boller, Alfred Germann, Martin Petrzilka, Martin Schadt
  • Patent number: 4613594
    Abstract: Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: September 23, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico Baggiolini, Giacomo Pizzolato, Milan Uskokovic, Gary Truitt
  • Patent number: 4612324
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each individually is hydrogen, or lower alkyl and R.sup.4 is hydroxy, lower alkoxy, aryl-(lower alkoxy), amino, mono(lower alkyl)amino or di(lower alkyl) amino,and pharmaceutically acceptable salts thereof which are useful in the treatment of degenerative joint diseases and of Wilson's disease are described.
    Type: Grant
    Filed: February 1, 1984
    Date of Patent: September 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Colin H. Cashin, Noel A. Roberts, Brian P. Tong
  • Patent number: 4612308
    Abstract: The syntheses of 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol, 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol, and the epimeric mixture thereof which are useful as differentiation inducing agents and anti-proliferation agents are described, 25,26-dehydro-1.alpha.,23S-dihydroxycholecalciferol 25,26-dehydro-1.alpha.,23R-dihydroxycholecalciferol and the epimeric mixture thereof are useful for treating tumors and leukemia, and osteoporosis.
    Type: Grant
    Filed: November 29, 1984
    Date of Patent: September 16, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Gary A. Truitt, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4605744
    Abstract: 6-Amidinopenicillanic acid derivatives wherein one of the nitrogen atoms of the amidino group is part of a heterocyclic ring having on a side chain an unsubstituted heterocyclic ring containing 2 to 3 nitrogen atoms, and being useful as an antibiotic.
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chung-Chen Wei, Manfred Weigele
  • Patent number: 4605674
    Abstract: Antivirally active compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy;R.sup.2 represents lower alkoxy;R.sup.3 represents hydrogen or lower alkoxy; andR.sup.4 represents phenyl which may be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl which may be substituted by lower alkyl,pharmaceutical compositions containing them and a process for the preparation of those compounds of formula I which are novel.
    Type: Grant
    Filed: April 24, 1984
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Morio Fujiu, Yasuji Suhara, Hideo Ishitsuka
  • Patent number: 4603223
    Abstract: A novel process for the manufacture of quinone derivatives is described.In this process a compound of the formula ##STR1## is reacted with a compound of the formula ##STR2## and the resulting compound of the formula ##STR3## is subjected to a retro-Diels-Alder reaction. The substituents R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the significance given in the description.
    Type: Grant
    Filed: July 24, 1984
    Date of Patent: July 29, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: August Ruttimann, George H. Buchi
  • Patent number: 4601984
    Abstract: There are provided antibiotics X-14873 A, G and H of the formulas ##STR1## wherein for X-14873A, R.sub.1 is CO.sub.2 H and R.sub.2 is ##STR2## for X-14873G, R.sub.1 is hydrogen and R.sub.2 is ##STR3## and for X-14873H, R.sub.1 is hydrogen and R.sub.2 is ##STR4## The compounds exhibit antibiotic activity. Also disclosed is a process to produce the above compounds.
    Type: Grant
    Filed: June 30, 1983
    Date of Patent: July 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chao-Min Liu, Homer D. Tresner, John Westley
  • Patent number: 4602036
    Abstract: Aluminium panthenolate and zinc panthenolate, their manufacture and use as topical medicaments are described.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: July 22, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Hanck, Horst Pauling
  • Patent number: 4599347
    Abstract: Tricyclic imidazole derivatives of the formula ##STR1## wherein R.sup.1 is 2-pyridyl optionally substituted by lower alkyl or lower alkoxy, n is the integer 0 to 1, R.sup.2 is hydrogen or lower alkyl, R.sup.3 and R.sup.4, independently, are hydrogen or lower alkyl, A is a group of the formula ##STR2## m is the integer 2 or 3, R.sup.5, R.sup.6, R.sup.7 and R.sup.8, independently, are hydrogen or lower alkyl, and R.sup.9 is hydrogen and R.sup.10 is hydrogen or lower alkyl or R.sup.9 and R.sup.10 taken together are oxo, provided that at least one of R.sup.3 and R.sup.4 is lower alkyl when A is a group of the formula--CH.dbd.CH--CH.dbd.CH-- or --(CH.sub.2).sub.4 --,and their pharmaceutically acceptable acid addition salts. The compounds of formula I inhibit gastric acid secretion and prevent the formation of gastric ulcers.
    Type: Grant
    Filed: December 12, 1983
    Date of Patent: July 8, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Anna Krasso, Henri Ramuz