Patents Represented by Attorney Jon S. Saxe
  • 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: 4696915
    Abstract: Parathymyosin alpha is a novel peptide isolated from mammalian thymus and contains approximately 105 amino acid residues. It bears a high degree of homology to prothymosin alpha both in sequence and amino acid composition. Parathymosin alpha acts as a blocker or modulator or prothymosin alpha activity.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: September 29, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Bernard L. Horecker
  • 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: 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: 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: 4689350
    Abstract: 1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(alpha-methylstyryl)naphthalene possesses antikeratinizing, antiinflammatory and immunomodulatory properties and can be used in the treatment or prevention of dermatoses which are accompanied by a pathological cornification as well as inflammatory, autoimmune, rheumatic and allergic illnesses.
    Type: Grant
    Filed: June 16, 1986
    Date of Patent: August 25, 1987
    Assignee: Hoffman-La Roche Inc.
    Inventor: Werner Bollag
  • 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: 4689427
    Abstract: The present invention is directed to novel hydroquinone derivatives which are useful as intermediates for the manufacture of (R,R,R)-.alpha.-tocopherol (natural vitamin E) as well as of racemic .alpha.-tocopherol. The invention is also directed to a process for the preparation of the hydroquinone derivatives of the invention.
    Type: Grant
    Filed: November 15, 1985
    Date of Patent: August 25, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Marquard Imfeld
  • Patent number: 4687849
    Abstract: The oxime ester compound [(isopropylideneamino)oxy]-ethyl-2-[[(6-chloroquinoxalinyl)oxy]phenoxy]pro pionate, processes for the preparation thereof, herbicidal compositions containing said compound and methods of use of the composition.
    Type: Grant
    Filed: October 4, 1985
    Date of Patent: August 18, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Frater, Milos Suchy, Jean Wenger, Paul Winternitz
  • 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: 4683197
    Abstract: A method for the detection of occult human blood in human stool samples by immunologically determining after performing the known peroxidase procedure, a human component abnormally present in the stool.
    Type: Grant
    Filed: May 6, 1985
    Date of Patent: July 28, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Harald Gallati
  • Patent number: 4681962
    Abstract: 7-fluoro-16-substituted 15-hydroxy PGI.sub.2 compounds which have saturated bond of the 13 position and which are useful as blood platelet anti-aggregating agents.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: July 21, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George W. Holland, Hans Maag, Perry Rosen
  • Patent number: 4681930
    Abstract: An intact human immune interferon protein and a method for the extraction and purification of intact recombinant human immune interferon is disclosed. This method permits the purification to homogenity of intact recombinant human immune interferon.
    Type: Grant
    Filed: August 10, 1984
    Date of Patent: July 21, 1987
    Assignees: Hoffmann-La Roche Inc., Takeda Chemical Industries Ltd.
    Inventors: Hsiang-Fu Kung, Hiromu Sugino, Susumu Honda
  • Patent number: 4681756
    Abstract: The effect of a controlled release, hydrodynamically balanced dosage formulation containing both an aqueous phase N-nitroso compound blocking agent and a lipid phase N-nitroso compound blocking agent in preventing the formation of nitrosamines and nitrosamides in the stomach is disclosed.
    Type: Grant
    Filed: June 26, 1986
    Date of Patent: July 21, 1987
    Assignee: Hoffman-La Roche Inc.
    Inventors: William J. Mergens, Harold L. Newmark, Prabhakar R. Sheth, Jacques L. Tossounian
  • 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: 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: 4680415
    Abstract: 7-fluoro-16-substituted 15-hydroxy PGI.sub.2 compounds which have saturated bond of the 13 position and which are useful as blood platelet anti-aggregating agents.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: July 14, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George W. Holland, Hans Maag, Perry Rosen