Patents Represented by Attorney, Agent or Law Firm Arthur D. Dawson
  • Patent number: 6514989
    Abstract: The invention is a compound of formula or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are as defined in the specification. A compound of formula I has a good affinity to the adenosine receptor and can therefore be used for the treatment or protection of diseases mediated by this receptor.
    Type: Grant
    Filed: May 29, 2002
    Date of Patent: February 4, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthias Heinrich Nettekoven, Bernd Puellmann
  • Patent number: 6509328
    Abstract: The present invention is a compound of formula wherein X is an ethynediyl group, R1, R2 and R3 are as defined in the specification.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: January 21, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6506772
    Abstract: Substituted [1,2,4]triazolo[1,5a]pyridine derivatives and pharmaceutically active salts thereof with activity as adenosine receptor ligands are disclosed. These compounds are useful for treatment of diseases responsive to modulation of the adenosine receptor.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: January 14, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Brodbeck, Matthias Heinrich Nettekoven
  • Patent number: 6489485
    Abstract: Para-alkyl, aryl, cycloheteroalkyl or heteroaryl [carbonyl or sulfonyl] amino substituted phenyl amides active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: December 3, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fred Thomas Bizzarro, Nancy-Ellen Haynes, Ramakanth Sarabu
  • Patent number: 6482829
    Abstract: The invention relates to compounds of the formula as described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.
    Type: Grant
    Filed: May 21, 2001
    Date of Patent: November 19, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Thierry Godel, Annick Goergler, Torsten Hoffmann, Sabine Kolczewski, Stephan Roever
  • Patent number: 6479483
    Abstract: Compounds of the present invention are 4-phenyl-pyridine derivatives with activity as NK-1 receptor antagonists.
    Type: Grant
    Filed: July 10, 2001
    Date of Patent: November 12, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Quirico Branca, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6462198
    Abstract: The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula  wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: October 8, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6452001
    Abstract: The invention relates to compounds of the formula wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl; R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2; R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl; R is hydrogen or lower alkyl;
    Type: Grant
    Filed: May 14, 2001
    Date of Patent: September 17, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Thierry Godel, Reinhard Heck
  • Patent number: 6451819
    Abstract: The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q, X, A, Y B are as defined in the specification.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: September 17, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Patent number: 6440995
    Abstract: Phenyl substituted quinolin 4-yl derivatives and pharmaceutical compositions with activity as NMDA-receptor subtype selective blockers. The compounds of the invention modulate neuronal activity and plasticity.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: August 27, 2002
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Serge Burner, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, René Wyler
  • Patent number: 6432985
    Abstract: The invention relates to a compound of the formula its R,R-, S,S-enantiomers and racemic mixtures thereof and to their pharmaceutically acceptable acid addition salts. The compound of formula I and its R,R- and S,S-enantiomers may be used as medicaments for the treatment of diseases, wherein the therapeutic indications include acute forms of neurodegeneration caused by stroke or brain trauma; chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease or ALS (amyotrophic lateral sclerosis); neurodegeneration associated with bacterial or viral infections, and, diseases such as schizophrenia, anxiety, depression and chronic/acute pain.
    Type: Grant
    Filed: March 19, 2001
    Date of Patent: August 13, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, Rene Wyler
  • Patent number: 6432087
    Abstract: A hypodermic syringe with a selectively retractable includes an elongate barrel having an open proximal end and a distal end that defines a receiver with an inwardly projecting shoulder. The syringe has a hollow elongate plunger with an open proximal end and a closed distal end. There is an elongate plug extending distally into the hollow plunger from the open proximal end forming an enclosed cavity within the plunger. The syringe has an elongate hub having a passageway therethrough, a distally extending stem, and a proximal flange with an engagement for engaging said barrel. The syringe has an elongate needle having a fluid path therethrough, a sharpened distal end and a proximal end. The needle is mounted in the passageway so that the sharpened distal end projects. The syringe has an elongate spring disposed about the stem of the hub that is compressed between the flange and the inwardly projecting shoulder of the receiver to provide a bias.
    Type: Grant
    Filed: July 31, 2000
    Date of Patent: August 13, 2002
    Assignee: Becton, Dickinson and Company
    Inventors: Roger Hoeck, Charles L. Bush, Jr.
  • Patent number: 6420394
    Abstract: The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.
    Type: Grant
    Filed: April 8, 1998
    Date of Patent: July 16, 2002
    Assignee: Roche Consumer Health (Worldwide) SA
    Inventor: Andreas Supersaxo
  • Patent number: 6413237
    Abstract: A hypodermic syringe with a selectively retractable needle includes an elongate barrel having an open proximal end, an open distal end and a hollow bore. The syringe includes an elongate plunger including a hollow outer housing having an open proximal end and an open distal end. The plunger has a hollow inner sleeve defining a cavity therein. The plunger has releasable engagement elements preventing relative axial movement between the outer housing and the inner sleeve, the elements allowing the relative axial movement when released and a distal stopper. There is an open cutter mounted at a proximal end of the inner sleeve to cut through the stopper to expose the cavity in the inner sleeve when the engagement elements are released and sufficient distal axial force is applied to the plunger. The syringe has a hub housing with an open proximal end having an inwardly projecting shoulder, a hub with a proximal flange and an axial stem, sized to fit within the hub housing.
    Type: Grant
    Filed: August 31, 2000
    Date of Patent: July 2, 2002
    Assignee: Becton, Dickinson and Company
    Inventors: Richard Caizza, Simon Cohn, Jonathan Gabel
  • Patent number: 6409701
    Abstract: A retractable needle syringe includes a barrel defining a receiver. There is a plunger having an inner rod extending distally from the proximal end. The plunger includes a hollow sleeve that is disposed over and extend beyond an inner rod. The plunger includes a hollow cutter extending from the inner rod and a stopper disposed over the end of the sleeve. The plunger has a displaceable collar to prevent movement of the inner rod with respect to the sleeve, that is by distal force to the plunger by engagement with the proximal end of the barrel allowing the cutting surface to cut through the stopper. There is a hub with a stem, a proximal flange and an engagement. A clip having a proximal foot with an opening therethrough and a distal grip is disposed on the stem of the hub. The proximal foot of the clip is disposed at the distal surface of the flange and the grip at the engagement on the stem.
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: June 25, 2002
    Assignee: Becton, Dickinson and Company
    Inventors: Simon Cohn, Roger Hoeck, Richard Caizza, Volker Niermann
  • Patent number: 6410037
    Abstract: The present invention relates to the use of pantothenic acid and/or its derivatives for treating dermatological disorders which involve mastocyte degranulation, such as atopic dermatitis, psoriasis, contact eczema, skin allergies, skin inflammation due to insect bites, skin allergies, senile pruritus, and to compositions comprising pantothenic acid and/or its derivatives, glycine and pharmaceutically and/or cosmetically acceptable additives which compositions are synergistic for the inhibition of mastocyte degranulation.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: June 25, 2002
    Assignee: Roche Consumer Health AG
    Inventors: Raymond De Bony, Eric Gooris
  • Patent number: 6407235
    Abstract: The invention is a compound of the formula wherein R is a) —C(O)(CH2)nC(O)OH, b)  wherein R1 is —N(R2)(R3), or is a five or six member aromatic or non-aromatic heterocyclic ring having one or more heteroatoms selected from nitrogen, oxygen or sulfur, unsubstituted or substituted by lower alkyl, c) —P(O)(OH)2, or is d) —C(O)(CH2)nNHC(O)(CH2)nN(R2)(R3); and R2/R3 are hydrogen or lower alkyl; n is 1, 2, 3 or 4; or a pharmaceutically acceptable acid addition salt thereof
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: June 18, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Alanine, Bernd Buettelmann, Holger Fischer, Marie-Paule Heitz Neidhart, Joerg Huwyler, Georg Jaeschke, Emmanuel Pinard, René Wyler
  • Patent number: 6407111
    Abstract: The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: June 18, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Guido Galley, Thierry Godel, Torsten Hoffmann, Walter Hunkeler, Patrick Schnider, Heinz Stadler
  • Patent number: 6407094
    Abstract: The present invention relates to compounds of with a base structure of formula 1 The compounds of formula I are shown to have activity as metabotropic glutamate receptor antagonists.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: June 18, 2002
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Geo Adam, Alexander Alanine, Erwin Goetschi, Vincent Mutel, Thomas Johannes Woltering
  • Patent number: 6399641
    Abstract: The present invention is a series of 2H-tetrazole-5-yl-amide derivatives showing activity as ligands of metabotropic glutamate receptors.
    Type: Grant
    Filed: June 27, 2001
    Date of Patent: June 4, 2002
    Assignee: Hoffmann-la Roche Inc.
    Inventors: Synese Jolidon, Vincent Mutel, Eric Vieira, Juergen Wichmann