Patents by Inventor Vadim Makarov

Vadim Makarov 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: 20220298149
    Abstract: Isoxazole-3-carboxamide derivatives and their use in treating viral infections and diseases, such as diseases caused by viruses of the Picornaviridae family of viruses (e.g., rhinoviruses, enteroviruses, and coxsackieviruses) is described. The derivatives have good efficacy against a range of viruses, including pleconaril-resistant viral strains, and have low induction of cytochrome P4503A4 (CYP3A4).
    Type: Application
    Filed: September 25, 2020
    Publication date: September 22, 2022
    Inventors: Vadim Makarov, Michaela Schmidtke, Sean Ekins
  • Patent number: 9790225
    Abstract: The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula I or pharmaceutically acceptable salts or propharmacons thereof, wherein at least one hydrogen atom in at least one of the phenyl groups A and B is substituted by a substituent RH, which has a Hammett constant ?p greater than 0.23. The present invention also concerns the method of its manufacture. For corresponding compounds, surprisingly a particularly high activity against viruses, in particular rhinoviruses and picornaviruses was determined. Furthermore, the compounds are tolerated very well. For these reasons the compounds are suitable for the treatment of viral infections and as drugs.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: October 17, 2017
    Assignee: Scandion Oncology A/S
    Inventors: Peter Wutzler, Michaela Schmidtke, Vadim Makarov
  • Publication number: 20140296259
    Abstract: The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula I or pharmaceutically acceptable salts or propharmacons thereof, wherein at least one hydrogen atom in at least one of the phenyl groups A and B is substituted by a substituent RH, which has a Hammett constant ?p greater than 0.23. The present invention also concerns the method of its manufacture. For corresponding compounds, surprisingly a particuarly high activity against viruses, in particular rhinoviruses and picornaviruses was determined. Furthermore, the compounds are tolerated very well. For these reasons the compounds are suitable for the treatment of viral infections and as drugs.
    Type: Application
    Filed: October 15, 2012
    Publication date: October 2, 2014
    Inventors: Peter Wutzler, Michaela Schmidtke, Vadim Makarov
  • Patent number: 8796264
    Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: August 5, 2014
    Assignee: Ecole Polytechnique Federale de Lausanne (EPFL)
    Inventors: Vadim Makarov, Stewart Cole
  • Publication number: 20130245007
    Abstract: The present invention relates to new 2-piperazin-1-yl-4H-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections caused by bacteria, especially diseases like tuberculosis (TB), Buruli ulcer and leprosy that result from infection with closely related mycobacteria. (I).
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
    Inventors: Vadim Makarov, Stewart Cole
  • Patent number: 8440842
    Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R1, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
    Type: Grant
    Filed: June 25, 2008
    Date of Patent: May 14, 2013
    Assignee: Leibniz-Institut fuer Naturstoff-Forschung und Infektionsbiologie e.V. Hans-Knoell-Institut
    Inventors: Ute Moellmann, Vadim Makarov, Cole T. Stewart
  • Publication number: 20110160193
    Abstract: The present invention relates to novel benzothiazinone derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance. The solution of the present invention is a compound of formula I wherein R1 to R6 are as defined in the specification.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 30, 2011
    Applicant: Leibniz Institute for Natural Product Research and Infection Biology E.V.
    Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Möllmann
  • Patent number: 7863268
    Abstract: Disclosed are benzothiazin derivatives of formula (I), preparation methods therefore, and treatment methods employing such compounds as antibacterial agents in treating infectious diseases of mammals caused by bacteria, especially diseases like tuberculosis and leprosy caused by mycobacteria: wherein R1, R2, R3, R4, R5, and R6, and other variables enumerated under one or more of R1, R2, R3, R4, R5, and R6 are as defined.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: January 4, 2011
    Assignee: Alere International
    Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Moellmann
  • Publication number: 20100286130
    Abstract: The present invention relates to compounds of Formula (I) or salts thereof wherein R?, R2, R3, R4, R5, R6, and other variables enumerated under one or more of same are as defined herein. Compounds of Formula I have activity as antimicrobial agents. Also disclosed are pharmaceutical compositions and methods of treating and preventing microbial infections in mammals, for example, a tuberculosis or leprosy infection, which employ compounds of Formula (I) or salts thereof.
    Type: Application
    Filed: June 25, 2008
    Publication date: November 11, 2010
    Inventors: Ute Moellmann, Vadim Makarov, Cole T. Stewart
  • Publication number: 20100010018
    Abstract: 4-amino-3-arylamino-6-arylpyrazolo[3,4-d]pyrimidine derivatives of general formula (I), pharmaceutically acceptable salts thereof, method for preparation of the aforesaid compounds and their use as antiviral agents.
    Type: Application
    Filed: June 20, 2007
    Publication date: January 14, 2010
    Inventors: Vadim Makarov, Peter Wutzler, Michaela Schmidtke, Hans-Martin Dahse
  • Publication number: 20090239851
    Abstract: The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria. The present invention aims at the generation of new compounds with activity against mycobacteria as potential new tuberculosis drugs to overcome problems concerning resistance and drug intolerance.
    Type: Application
    Filed: May 24, 2006
    Publication date: September 24, 2009
    Inventors: A. Vadim Makarov, Stewart T. Cole, Ute Möllmann
  • Publication number: 20080255166
    Abstract: The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
    Type: Application
    Filed: June 6, 2008
    Publication date: October 16, 2008
    Applicant: NEED PHARMACEUTICALS S.r.I.
    Inventors: Ute Mollmann, Vadim Makarov
  • Publication number: 20050032822
    Abstract: The invention relates to the use of dithiocarbamate derivatives for the therapeutic or prophylactic treatment of infectious diseases in mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and lepra caused by mycobacteria and infectious diseases caused by staphylococci. The invention further relates to novel dithiocarbamate derivatives of the formula (I), wherein X is a bivalent residue selected from the group consisting of formulae having excellent antibacterial activities, and to pharmaceutical preparations containing the same.
    Type: Application
    Filed: November 18, 2002
    Publication date: February 10, 2005
    Inventors: Ute Mollmann, Vadim Makarov
  • Publication number: 20020182151
    Abstract: The design, synthesis and antiviral activity of certain antiviral compounds are disclosed examples of which are shown below. These compounds inhibit the reverse transcriptase enzymes of several retroviruses, including human immunodeficiency virus.
    Type: Application
    Filed: December 13, 2001
    Publication date: December 5, 2002
    Applicant: The Government of the U.S.A. as represented by the Secretary of the Dept. of Health & Human Services
    Inventors: William G. Rice, Mingjun Huang, Robert W. Buckheit, David G. Covell, Grzegorz Czerwinski, Christopher J. Michejda, Vadim Makarov