Patents by Inventor Shai Rubnov

Shai Rubnov 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).

  • Publication number: 20190298675
    Abstract: The present invention relates to extended-release pharmaceutical compositions comprising pregabalin or a salt thereof, which are adapted to release the pregabalin active ingredient according to a dual release profile. The formulations comprise two components, the first (fast ER) providing extended-release of the active ingredient in a short controlled manner lasting from about 4 to about 6 hours, and the second (slow ER or maintenance) providing extended release of the active ingredient over a period of 24 hours. The proportion of each component in the formulation may be adjusted to achieve the desired AUC and therapeutic effect following oral administration to a subject. The invention further relates to methods of using the pharmaceutical compositions for treating conditions and disorders which are responsive to pregabalin treatment, such as neuropathic pain associated with diabetic peripheral neuropathy (DPN), post herpetic neuralgia (PHN), epilepsy, seizures and fibromyalgia.
    Type: Application
    Filed: July 16, 2017
    Publication date: October 3, 2019
    Applicants: MAPI PHARMA LTD., JIANGSU NHWA PHARMACEUTICAL CO., LTD.
    Inventors: Yoram SELA, Shai RUBNOV
  • Patent number: 10111867
    Abstract: The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: October 30, 2018
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 9994522
    Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.
    Type: Grant
    Filed: July 20, 2014
    Date of Patent: June 12, 2018
    Assignee: MAPI PHARMA LTD.
    Inventors: Shai Rubnov, Ehud Marom
  • Publication number: 20180008584
    Abstract: The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.
    Type: Application
    Filed: February 17, 2015
    Publication date: January 11, 2018
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud MAROM, Shai RUBNOV
  • Publication number: 20170174626
    Abstract: The present invention provides a new amorphous form of apremilast, pharmaceutical compositions comprising same, methods for preparation and use thereof in treating conditions mediated by inhibition of TNF-? production or inhibition of phosphodiesterase 4 (PDE4), e.g., psoriatic arthritis and other chronic inflammatory diseases.
    Type: Application
    Filed: July 20, 2014
    Publication date: June 22, 2017
    Applicant: MAPI PHARMA LTD.
    Inventors: Shai RUBNOV, Ehud MAROM
  • Patent number: 9617241
    Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: April 11, 2017
    Assignee: MAPI PHARMA LTD.
    Inventors: Anna Gopin, Shai Rubnov, Galina Zats, Ehud Marom
  • Publication number: 20160355500
    Abstract: The present invention relates to a process for the preparation of (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylene-1-piperidinyl)-1-(1H-1,2,4-triazol-1-yl)-2-butanol (Efinaconazole) and intermediates used in such process.
    Type: Application
    Filed: March 2, 2015
    Publication date: December 8, 2016
    Applicant: MAPI PHARMA LTD.
    Inventors: Anna GOPIN, Shai RUBNOV, Galina ZATS, Ehud MAROM
  • Patent number: 9206197
    Abstract: An amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
    Type: Grant
    Filed: September 2, 2012
    Date of Patent: December 8, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 9200114
    Abstract: The present invention relates to a synthetic polypeptide which is a random linear pentapolymer comprising alanine, glutamic acid, lysine, tyrosine and phenylalanine and use thereof in treating autoimmune diseases, in particular multiple sclerosis.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: December 1, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 9102592
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: August 11, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 9096574
    Abstract: The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.
    Type: Grant
    Filed: January 1, 2013
    Date of Patent: August 4, 2015
    Assignee: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 9006188
    Abstract: The present invention provides novel co-crystal forms of dapagliflozin, namely a dapagliflozin lactose co-crystal and a dapagliflozin asparagine co-crystal, to pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating type 2 diabetes.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: April 14, 2015
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Shai Rubnov
  • Patent number: 8981095
    Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
    Type: Grant
    Filed: June 13, 2012
    Date of Patent: March 17, 2015
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Susanna Tchilibon, Shai Rubnov
  • Patent number: 8975244
    Abstract: The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: March 10, 2015
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Shai Rubnov, Michael Mizhiritskii
  • Publication number: 20150051419
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Application
    Filed: August 28, 2014
    Publication date: February 19, 2015
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud MAROM, Michael MIZHIRITSKII, Shai RUBNOV
  • Publication number: 20140371273
    Abstract: The present invention provides novel crystalline forms of perampanel, pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating seizures and epilepsy.
    Type: Application
    Filed: January 1, 2013
    Publication date: December 18, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Publication number: 20140350004
    Abstract: The present invention provides an amorphous form of dolutegravir sodium, pharmaceutical compositions comprising same, methods for its preparation and use thereof as an antiretroviral agent.
    Type: Application
    Filed: September 2, 2012
    Publication date: November 27, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Shai Rubnov
  • Publication number: 20140343010
    Abstract: The present invention provides novel co-crystal forms of dapagliflozin, namely a dapagliflozin lactose co-crystal and a dapagliflozin asparagine co-crystal, to pharmaceutical compositions comprising same, methods for their preparation and uses thereof for treating type 2 diabetes.
    Type: Application
    Filed: May 23, 2014
    Publication date: November 20, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud MAROM, Shai RUBNOV
  • Patent number: 8865742
    Abstract: The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 8841447
    Abstract: The present invention is based on the discovery of a process for preparing pyrimidin-dione compounds, especially alogliptin and its derivatives, which comprises the reaction of a urea derivative of formula (VIII) with a malonic acid or its derivatives to form intermediates of formulae (VII) or (VII-A), which are subsequently converted to a compound of formula (II) upon introduction of a leaving group X. Compound (II) then reacts with an amine to form compound (I), which is optionally converted to its salts of formula (IV).
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: September 23, 2014
    Assignee: Mapi Pharma Ltd.
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov