Patents Assigned to Roche Colorado Corporation
  • Patent number: 7696311
    Abstract: The invention provides methods of obtaining a peptide that include steps of synthesizing a peptide intermediate having one or more side chain protecting groups; providing a solvent to the peptide intermediate to form a peptide intermediate composition; and providing a precipitating agent in an amount sufficient to precipitate the peptide intermediate from the peptide intermediate composition, wherein the precipitating agent is an alcohol having three or more carbon atoms. Also provided are methods for precipitating peptides, methods for concentration peptides, and methods for filtering peptides.
    Type: Grant
    Filed: December 23, 2004
    Date of Patent: April 13, 2010
    Assignee: Roche Colorado Corporation
    Inventors: Yeun-Kwei Han, Hiralal N. Khatri, Robert J. Topping
  • Patent number: 7544665
    Abstract: Methods for the solid phase synthesis of T-1249 peptides and peptide intermediates, in particular methods involving synthesizing T-1249 peptide intermediates at low loading factors to produce products having excellent purity and yield.
    Type: Grant
    Filed: December 30, 2005
    Date of Patent: June 9, 2009
    Assignee: Roche Colorado Corporation
    Inventors: Hiralal N. Khatri, Yeun-Kwei Han, David A. Johnston, L. Mark Hodges
  • Patent number: 7384939
    Abstract: The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: June 10, 2008
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, David A. Johnston, L. Mark Hodges
  • Patent number: 7365188
    Abstract: The present invention provides a process for producing a N4-acyl-5?-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: April 29, 2008
    Assignee: Roche Colorado Corporation
    Inventors: Christopher R. Roberts, Jim-wah Wong
  • Patent number: 7122684
    Abstract: The invention provides a multi-step process for preparing 1,2-diamino compounds of formula wherein R1, R1?, R2, R2?, R3 and R4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxides of formula wherein R1, R1?, R2 and R2? have the meaning given in the specification.
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: October 17, 2006
    Assignee: Roche Colorado Corporation
    Inventors: Jack D. Brown, Peter J. Harrington, Robert C. Hughes
  • Publication number: 20060014959
    Abstract: The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein.
    Type: Application
    Filed: July 5, 2005
    Publication date: January 19, 2006
    Applicants: Roche Colorado Corporation
    Inventors: Peter Harrington, David Johnston, L. Hodges
  • Publication number: 20050137392
    Abstract: The present invention provides a process for producing a N4-acyl-5?-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy.
    Type: Application
    Filed: December 22, 2004
    Publication date: June 23, 2005
    Applicant: Roche Colorado Corporation
    Inventors: Christopher Roberts, Jim-wah Wong
  • Patent number: 6858749
    Abstract: The present invention relates to a novel process for producing a ?-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-?-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: February 22, 2005
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Patent number: 6818789
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: November 16, 2004
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Patent number: 6765109
    Abstract: The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: July 20, 2004
    Assignee: Roche Colorado Corporation
    Inventors: Jack D. Brown, Hiralal N. Khatri, Peter J. Harrington, Dave A. Johnston, Robert J. Topping, Richard R. Dauer, Gary K. Rowe
  • Patent number: 6743927
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: June 1, 2004
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Publication number: 20030171602
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: September 11, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Rober J. Topping
  • Publication number: 20030158422
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: August 21, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Mitcheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Publication number: 20030158423
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1
    Type: Application
    Filed: February 10, 2003
    Publication date: August 21, 2003
    Applicant: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Patent number: 6552204
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein. In particular, the present invention relates to a process for enantioselectively producing the &dgr;-lactone and novel intermediates disclosed herein.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: April 22, 2003
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, Lewis M. Hodges, Kurt Puentener, Michelangelo Scalone
  • Patent number: 6545165
    Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: April 8, 2003
    Assignee: Roche Colorado Corporation
    Inventors: Michael P. Fleming, Yeun-Kwei Han, Lewis M. Hodges, David A. Johnston, Roger P. Micheli, Kurt Puentener, Chris R. Roberts, Michelangelo Scalone, Mark A. Schwindt, Robert J. Topping
  • Patent number: 6507284
    Abstract: The present invention provides an enclosure sign apparatus for unavoidable viewing of a sign before manipulation of an entryway opening device. The enclosure sign apparatus includes at least one side surface extending out as least as far as the entryway opening device, a back surface interconnected to the side surface, wherein the back surface comprises an opening to accommodate the entryway opening device therethrough, and a front surface having a sign. The front surface is capable of preventing access to the entryway opening device and is interconnected to the side surface. When in use, access is obtained to an entryway opening device by physically removing the enclosure sign apparatus so that there is unavoidable viewing of a sign before manipulation of the entryway opening device.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: January 14, 2003
    Assignee: Roche Colorado Corporation
    Inventor: Marc Thomas Rothney
  • Patent number: 6475080
    Abstract: An apparatus for reducing the amount of fumes escaping into the surrounding atmosphere from an open container and from a chemical dispenser, and a method of use thereof comprising a bung slot ventilation apparatus and a chemical dispenser holder apparatus and a method of use thereof. The bung slot ventilation apparatus includes an inlet passageway comprising a fume exhaust port and a bunghole adapter, and a fume exhaust system adapter. And the chemical dispenser holder apparatus includes a holder comprising an inlet and a fume exhaust system adapter.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: November 5, 2002
    Assignee: Roche Colorado Corporation
    Inventor: Marc T. Rothney
  • Patent number: 6136971
    Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: October 24, 2000
    Assignee: Roche Colorado Corporation
    Inventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
  • Patent number: 5892055
    Abstract: A method of preparing 2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopro pyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting 6-fluoro-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the dianion of N-?3-(1H-benzimidazol-2-yl)propyl!-N-methylacetamide to form N-?3-(1H-benzirnidazol-2-yl) propyl!-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-y l)-N-methylacetamide, reducing this to 2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopro pyl-1,2,3,4-tetrahydronaphthalen-2-ol, and treating the 2-?2-{?3-(1H-benzirnidazol-2-yl)propyl!methylarnino}ethyl!-6-fluoro-1-isop ropyl-1, 2,3,4-tetrahydronaphthalen-2-ol with methoxyacetic acid or an activated derivative of methoxyacetic acid. The invention is particularly applicable to the preparation of mibefradil, (1S,2S)-2-?2-{?3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro- 1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-yl methoxyacetate, and its dihydrochloride salt.
    Type: Grant
    Filed: June 26, 1998
    Date of Patent: April 6, 1999
    Assignee: Roche Colorado Corporation
    Inventor: Peter J. Harrington