Patents by Inventor Roumen Nikolaev Radinov

Roumen Nikolaev Radinov has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Processes for the manufacture of propane-1-sulfonic acid (3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl)-amide
    Patent number: 9556172
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: January 31, 2017
    Assignee: Hoffman La-Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID (3-[5-(4-CHLORO-PHENYL)-1H-PYRROLO[2,3-b]PYRIDINE-3-CARBONYL]-2,4-DIFLUORO-PHENYL)-AMIDE
    Publication number: 20160083378
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: August 27, 2015
    Publication date: March 24, 2016
    Inventors: Corey James BRUMSTED, Hendrik MOORLAG, Roumen Nikolaev RADINOV, Yi REN, Pius WALDMEIER
  • Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
    Patent number: 9150594
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: October 6, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID -AMIDE
    Publication number: 20140288308
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Inventors: Corey James BRUMSTED, Hendrik MOORLAG, Roumen Nikolaev RADINOV, Yi REN, Pius WALDMEIER
  • Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
    Patent number: 8779150
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: July 15, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8741920
    Abstract: The present invention relates to a composition comprising the compound of formula (1), and the compound of formula (B),
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8530661
    Abstract: The present invention further relates to a process for the manufacture of compound (I), wherein X is —Br or —Cl.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 10, 2013
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS
    Publication number: 20130005761
    Abstract: The present invention relates to a composition comprising the compound of formula (1), and the compound of formula (B),
    Type: Application
    Filed: September 13, 2012
    Publication date: January 3, 2013
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS
    Publication number: 20130005978
    Abstract: The present invention further relates to a process for the manufacture of compound (I), wherein X is —Br or —Cl.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 3, 2013
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8329724
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Novel Processes for the manufacture of Propane-1-sulfonic acid -amide
    Publication number: 20120022258
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 26, 2012
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • PROCESS FOR THE MANUFACTURE OF PHARMACEUTICALLY ACTIVE COMPOUNDS
    Publication number: 20110028511
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: July 27, 2010
    Publication date: February 3, 2011
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • Biocatalytic asymmetric reduction in preparation of (S)-N-[5-(1,2-dihydroxy-ethyl)-pyrazinyl]-2,2-dimethyl-propionamide
    Patent number: 7727750
    Abstract: The present invention relates to biocatalytic asymmetric reduction for the preparation of 2-amino-[5-(1-hydroxy-2-hydroxy or halogen-ethyl)]-pyrazine derivatives of the formula wherein R is lower alkylcarbonyl or an amino protecting group and R1 is hydroxy or halogen. The compounds are key intermediates in the manufacture of a glucokinase activator.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: June 1, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Steven Paul Hanlon, Hans Iding, Ernst Kupfer, Roumen Nikolaev Radinov, Lianhe Shu, Ping Wang
  • BIOCATALYTIC ASYMMETRIC REDUCTION IN PREPARATION OF (S)-N-[5-(1,2-DIHYDROXY-ETHYL)-PYRAZINYL]-2,2-DIMETHYL-PROPIONAMIDE
    Publication number: 20080248537
    Abstract: The present invention relates to biocatalytic asymmetric reduction for the preparation of 2-amino-[5-(1-hydroxy-2-hydroxy or halogen-ethyl)]-pyrazine derivatives of the formula wherein R is lower alkylcarbonyl or an amino protecting group and R1 is hydroxy or halogen. The compounds are key intermediates in the manufacture of a glucokinase activator.
    Type: Application
    Filed: April 3, 2008
    Publication date: October 9, 2008
    Inventors: Steven Paul Hanlon, Hans Iding, Ernst Kupfer, Roumen Nikolaev Radinov, Lianhe Shu, Ping Wang
  • Crystalline solvate of glucokinase activator
    Publication number: 20070254895
    Abstract: Provided is a crystalline IPA solvate of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
    Type: Application
    Filed: April 11, 2007
    Publication date: November 1, 2007
    Inventors: Duk Soon Choi, Hitesh Parmendra Chokshi, Ahmad Waseem Malick, Roumen Nikolaev Radinov
  • Process for the preparation of an isopropanol solvate of a glucokinase activator
    Publication number: 20070244129
    Abstract: Provided is a process for the preparation of 2(R)-(3-Chloro-4-methanesulfonyl-phenyl)-3-((R)-3-oxo-cyclopentyl)-N-pyrazin-2-yl-propionamide and its isopropanol solvate as a glucokinase activator which increases insulin secretion in the treatment of, for example, type II diabetes.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 18, 2007
    Inventors: Andrzej Robert Daniewski, Wen Liu, Roumen Nikolaev Radinov
  • Process and intermediates useful to produce vitamin D analogs
    Patent number: 6353123
    Abstract: A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
    Type: Grant
    Filed: April 16, 2001
    Date of Patent: March 5, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andrzej Robert Daniewski, Marek Michal Kabat, Masami Okabe, Roumen Nikolaev Radinov
  • Process useful to produce vitamin D analogs
    Patent number: 6294688
    Abstract: A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: September 25, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrzej Robert Daniewski, Marek Michal Kabat, Masami Okabe, Roumen Nikolaev Radinov
  • Process and intermediates useful to produce vitamin D analogs
    Patent number: 6291694
    Abstract: A stereospecific method for accomplishing the below reaction: results in the compound of formula 2 having the same stereochemistry at both carbon 1 and carbon 3 as that in the compound of formula 1. Thus, if carbon 3 is in the R-configuration in the compound of formula 1, then carbon 3 will be in the R-configuration in the compound of resulting formula 2. In the above process, R1 is C1-C6 alkyl that can be straight-chain or branched. The process functions using a fluorinated alcohol having a pKa less than about 9, in the presence of a palladium catalyst. The compounds of formula 1, as well as novel intermediates in this process, are useful in manufacturing vitamin D analogs.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: September 18, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrzej Robert Daniewski, Marek Michal Kabat, Masami Okabe, Roumen Nikolaev Radinov
  • Process for preparing antiosteoporotic agents
    Patent number: 6255501
    Abstract: Methods for preparing antiosteoportic agents are disclosed. Compounds useful in the methods are also disclosed.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: July 3, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Andrzej Robert Daniewski, Roumen Nikolaev Radinov