Patents Represented by Attorney, Agent or Law Firm John P. Parise
  • Patent number: 6133309
    Abstract: Retinoids with retinoid receptor antagonistic activity, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found efficacious in treating T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: October 17, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Werner Bollag, Michael Klaus, Paola Panina-Bordignon, Francesco Sinigaglia
  • Patent number: 6121447
    Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 each independently represent hydrogen, C.sub.1-7 -alkyl, or C.sub.1-7 -alkoxy,A signifies--CN,a carbanionic R.sup.4 -alkynyl residue, in which R.sup.4 is hydrogen or C.sub.1-7 -alkyl, ora carbanionic residue of the malonic acid derivative of formula III ##STR2## in which B and B' independently represent --CN, --COOR.sup.5, or --C(O)R.sup.5, wherein R.sup.5 is alkyl or aryl.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: September 19, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Wolfgang Gohring
  • Patent number: 6103910
    Abstract: New compounds have the formula: ##STR1## wherein R, R.sup.1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: August 15, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
  • Patent number: 6103902
    Abstract: The present invention is concerned with a novel process for the carbamoylation of substituted pyridines, especially with a process for the preparation of compounds of formula I ##STR1## wherein R.sup.4 to R.sup.8 represent hydrogen, lower-alkoxy or halogen; or optionally salts thereof.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: August 15, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Uwe Klinkhammer
  • Patent number: 6100282
    Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell--cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: August 8, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
  • Patent number: 6087119
    Abstract: A method for the determination of factor IXa in a sample solution using a measurable factor IXa substrate and a water-miscible alcohol and measuring the cleavage of the factor IXa substrate as a measure for factor IXa activity is suitable for the direct determination of factor IXa.
    Type: Grant
    Filed: April 30, 1999
    Date of Patent: July 11, 2000
    Assignee: Roche Diagnostics GmbH
    Inventor: Jorg Sturzebecher
  • Patent number: 6083971
    Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is lower-alkyl, cycloalkyl or phenyl,R.sup.2 is H, OH or C(O)O-A, wherein A is lower-alkyl, cycloalkyl or phenyl, andR.sup.3, R.sup.4 and R.sup.5 are either methyl or R.sup.3 is H and R.sup.4 and R.sup.5 taken together are trimethyleneas well as hydrates or solvates and physiologically usable salts thereof can be used for the production of medicaments for the treatment or prophylaxis of illnesses which are caused by thrombin-induced platelet aggregation or fibrinogen clotting in blood plasma.
    Type: Grant
    Filed: December 15, 1998
    Date of Patent: July 4, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fran.cedilla.ois Diederich, Ulrike Obst, Lutz Weber
  • Patent number: 6051712
    Abstract: Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: April 18, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Binggeli, Volker Breu, Daniel Bur, Walter Fischli, Rolf Guller, Georges Hirth, Hans-Peter Marki, Marcel Muller, Christian Oefner, Heinz Stadler, Eric Vieira, Maurice Wilhelm, Wolfgang Wostl
  • Patent number: 6034275
    Abstract: Tertiary amines of the formula ##STR1## wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, L, M, p, T, and Q are as defined herein, have antimycotic and cholesterol-lowering activity.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: March 7, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Henrietta Dehmlow, Jacques Himber, Synese Jolidon, Hans Lengsfeld, Olivier Morand, Gerard Schmid, Ku-Hua Ji
  • Patent number: 6031103
    Abstract: A process manufactures of a compound of formula: ##STR1## and unique intermediates.
    Type: Grant
    Filed: April 22, 1999
    Date of Patent: February 29, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Anthony Brown, Hans Hilpert
  • Patent number: 6004965
    Abstract: Compounds of the formula: ##STR1## where A, B, R.sup.1 -R.sup.8 are as described herein are endothelin inhibitors that can be used in treating diseases associated with endothelin, such as high blood pressure. Chemical synthesis of these compounds and pharmaceutical compositions containing these compounds are also useful.
    Type: Grant
    Filed: August 15, 1997
    Date of Patent: December 21, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 6004996
    Abstract: Product containing tetrahydrolipstatin as the active ingredient and pharmaceutically acceptable excipients, characterized in that it is in the form of particles with a diameter of 0.25 to 2 mm; and pharmaceutical preparation s or compositions for oral administration containing the product.
    Type: Grant
    Filed: January 6, 1998
    Date of Patent: December 21, 1999
    Assignee: Hoffman-La Roche Inc.
    Inventors: Navnit Hargovindas Shah, Max Zeller
  • Patent number: 6001855
    Abstract: Compounds of formula I ##STR1## as well as pharmaceutically usable salts and esters thereof, wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in claim 1, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasing, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, kidney failure as well as infections caused by viruses, bacteria or fungi.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: December 14, 1999
    Assignee: Hoffman-La Roche Inc.
    Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
  • Patent number: 5977388
    Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.
    Type: Grant
    Filed: July 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5973188
    Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell--cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitrites.
    Type: Grant
    Filed: November 3, 1997
    Date of Patent: October 26, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Leo Alig, Paul Hadvary, Marianne Hurzeler Muller, Marcel Muller, Beat Steiner, Thomas Weller
  • Patent number: 5965733
    Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.
    Type: Grant
    Filed: November 16, 1998
    Date of Patent: October 12, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5962682
    Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5962686
    Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antiftngal properties.
    Type: Grant
    Filed: January 8, 1999
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda
  • Patent number: 5931814
    Abstract: An improved injection device has a casing containing an active substance reservoir, a cannula communicating with the reservoir, a device for inserting the cannula, and pump means for discharging the reservoir contents through the cannula. The cannula 11 is fixed relative to the casing and projects beyond the underside of the casing to the depth required for injection. The cannula is surrounded by a protective element which is moved by a spring drive from a first end position in which the protective device projects beyond the underside of the casing and beyond the cannula to a second end position in which the protective device does not project beyond the underside of the casing.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: August 3, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rainer Alex, Paul Hadvary, Hansjorg Tschirky
  • Patent number: 5900486
    Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antifungal properties.
    Type: Grant
    Filed: September 9, 1997
    Date of Patent: May 4, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shigeyasu Ichihara, Chikako Murasaki, Noriko Ohga, Jun Ohwada, Daisuke Sawada, Nobuo Shimma, Michio Shirai, Isao Umeda