Patents Represented by Attorney Jon S. Saxe
  • Patent number: 4789750
    Abstract: 6-Etherified hydroxy -2-(4',8',12'-trimethyl-5'-tridecenyl)-2,5,7,8-tetramethylchromans with an oxo or hydroxy substituent at the 2' position which may be substituted with an arylsulfonyl or a carboxyalkyl at the 3' position and containing a single or double bond at the 11 position, said chromans being intermediates for producing natural vitamin E.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: December 6, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: David L. Coffen, Rudolf Schmid, Mark J. Sebastian
  • Patent number: 4788214
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl;enatiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: November 29, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Noal Cohen, Giuseppe F. Weber
  • 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: 4788213
    Abstract: Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.
    Type: Grant
    Filed: May 5, 1983
    Date of Patent: November 29, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger
  • Patent number: 4788210
    Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, and their acid addition salts, processes for the preparation of these compounds, pest control compositions which contain these compounds as the active substance, as well as the methods of use of such compounds or compositions for the control of pests.
    Type: Grant
    Filed: December 16, 1985
    Date of Patent: November 29, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christoph Luthy, Rene Zurfluh
  • 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: 4785017
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2 is hydrogen or halogen; R.sup.3, R.sup.4 and R.sup.5 are hydrogen, acyl or lower alkyl; R.sup.6 and R.sup.7, independently, are hydrogen or lower alkyl; X is alkylene.sub.3-7 ; and n is an integer of zero to four; provided that only one of R.sup.3, R.sup.4 or R.sup.5 can be acyl;enantiomers thereof, and, when R.sup.7 is hydrogen, salts thereof with pharmaceutically acceptable bases.The compounds of formulas I and II are useful as agents for the treatment of allergic conditions.
    Type: Grant
    Filed: May 29, 1984
    Date of Patent: November 15, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Noal Cohen, Giuseppe F. Weber
  • 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: 4783280
    Abstract: There is described a liquid crystalline mixture for electro-optical devices which are operated according to the two-frequency matrix addressing procedure. The mixture consists of three components A, B and C, each of which contains one or more compounds. Component A has a viscosity of at most about 40 cp, a clearing point of at least about 40.degree. C. and a dielectric anisotropy between about -2 and about +1. Component B has a dielectric anisotropy below about -2 both above and below the cross-over frequency of the total mixture and component C has a dielectric anisotropy above about +10, a clearing point of at least about 100.degree. C. and there is a cross-over frequency in the total mixture of at most about 15 kHz at 20.degree. C. Novel compounds for such mixtures and their manufacture and use are also described. The novel mixtures make possible especially high multiplex rates and short response times.
    Type: Grant
    Filed: May 20, 1987
    Date of Patent: November 8, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Martin Schadt, Alois Villiger
  • Patent number: 4782149
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently represent hydrogen, C.sub.1 -C.sub.10 -alkyl, adamantyl-(C.sub.1 -C.sub.4 -alkyl) or (C.sub.2 -C.sub.6 -alkanoyloxy)-(C.sub.1 -C.sub.4 -alkyl), and pharmaceutically acceptable salts thereof possess antihypertensive activity and can be used as theraputic or prophylactic agents in pharmaceutical preparations. Intermediates for the production of such compounds are also provided.
    Type: Grant
    Filed: March 17, 1988
    Date of Patent: November 1, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: 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: 4780251
    Abstract: The compounds 9-phenyl-3,7-dimethyl-2,4,6,8-nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: October 25, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Edward R. Aig, John W. Coffey, Allen J. Lovey, Michael Rosenberger
  • Patent number: 4777169
    Abstract: Benzodiazepine derivatives useful in immunoassays for benzodiazepines.
    Type: Grant
    Filed: November 6, 1987
    Date of Patent: October 11, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: James V. Earley, Norman W. Gilman
  • 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: 4774253
    Abstract: Oxazole and isoxazole derivatives of the formula ##STR1## wherein A is C.sub.1-6 -alkylene, Het is a 2-R-oxazol-5-yl, 5-R-oxazol-2-yl, 4-R-oxazol-2-yl, 2-R-oxazol-4-yl, 3-R-isoxazol-5-yl or 5-R-isoxazol-3-yl group which is optionally substituted on the heterocyclic ring by a C.sub.1-6 -alkyl group, R is phenyl or thienyl monosubstituted or disubstituted by halogen, trifluoromethyl or C.sub.1-6 -alkylthio, R.sup.1 and R.sup.2 each is a C.sub.1-6 -alkyl group and R.sup.3 is a hydroxy or C.sub.1-6 -alkoxy group or a group of the formula --NR.sup.4 R.sup.5 in which R.sup.4 and R.sup.5 each is a hydrogen atom or a C.sub.1-6 -alkyl group or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached is a 5-membered or 6-membered saturated heteromonocyclic ring which may contain an oxygen or sulphur atom or an additional nitrogen atom, and pharmaceutically acceptable salts of the compounds of formula I in which R.sup.3 is a hydroxy group with bases, have anti-arthritic activity.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Peter J. Machin, John M. Osbond, Christopher R. Self, Carey E. Smithen, Brian P. Tong
  • Patent number: 4774249
    Abstract: The pyrimidine derivatives of formula I ##STR1## wherein R.sup.1 is naphthyl, substituted naphthyl or substituted phenyl; R.sup.2 is hydrogen or lower alkoxy; and A is an optionally present ethylene or 1,3-propylene, and wherein the diaminopyridine group has the exo-configuration when A is present, are described. These compounds are useful as antibacterial agents, antimalarial agents and antitumor agents, and can be used in combination with sulfonamides in the control of bacterial infections.
    Type: Grant
    Filed: October 23, 1987
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Rita Locher, Hans Maag
  • Patent number: 4774330
    Abstract: There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: September 27, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Roland Reiner
  • Patent number: 4772254
    Abstract: A centrifuge having an interchangeable rotor provided with an information support means for machine-readable information, and a reader comprising detectors for scanning the information support means and an electronic circuit for processing the received information, the information support means comprising an array of permanent magnet pins distributed over the rotor and having in some cases their north poles and in other cases their south poles facing the detectors.
    Type: Grant
    Filed: December 3, 1986
    Date of Patent: September 20, 1988
    Assignee: Kontron Holding A.G.
    Inventors: Alfred Grassl, Erhard Knorr
  • Patent number: 4772547
    Abstract: The present disclosure relates to synthetic peptides derived from the conserved region of the HTLVIII envelope proteins. These peptides are useful as reagents for immunoassays for detection of AIDS antibodies, as components of immunogenic compositions useful as vaccines, and for the production of anti-bodies selective to said envelope protein and methods for detecting the presence of AIDS antibodies in biological fluid samples.
    Type: Grant
    Filed: February 3, 1986
    Date of Patent: September 20, 1988
    Assignees: Hoffmann-La Roche Inc., United States of America
    Inventors: Edgar P. Heimer, Premkumar E. Reddy, Robert C. Gallo, Flossie Wong-Staal