Patents Assigned to Medivir AB
  • Patent number: 9828408
    Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: November 28, 2017
    Assignee: MEDIVIR AB
    Inventors: Genadiy Kalayanov, Staffan Torssell, Horst Wahling
  • Patent number: 9708332
    Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.
    Type: Grant
    Filed: October 29, 2013
    Date of Patent: July 18, 2017
    Assignee: MEDIVIR AB
    Inventors: Claudio Sturino, Teddy Halmos, Anne Decor, Martin Duplessis, Patrick Deroy, Araz Jakalian, Louis Morency, Cyrille Kuhn, Chantal Grand-Maitre, Martin Tremblay, Christian Brochu
  • Patent number: 9650388
    Abstract: There is provided Form 2 crystalline polymorph consisting of N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]-benzamide monohydrochloride and N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]benzamide hydrate monohydrochloride, its use as a medicament and methods for its preparation.
    Type: Grant
    Filed: August 13, 2014
    Date of Patent: May 16, 2017
    Assignee: MEDIVIR AB
    Inventors: Urszula Grabowska, Lourdes Salvador Oden, Victor M. Diaz Perez, Andrew Carr
  • Patent number: 9623022
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrog
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: April 18, 2017
    Assignees: Janssen Sciences Ireland UC, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
  • Patent number: 9540411
    Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
    Type: Grant
    Filed: July 14, 2016
    Date of Patent: January 10, 2017
    Assignee: MEDIVIR AB
    Inventors: Genadiy Kalayanov, Staffan Torssell, Horst Wahling
  • Patent number: 9481703
    Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: November 1, 2016
    Assignee: MEDIVIR AB
    Inventors: Genadiy Kalayanov, Staffan Torssell, Horst Wahling
  • Patent number: 9428517
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: August 30, 2016
    Assignee: MEDIVIR AB
    Inventors: Lourdes Salvador Oden, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
  • Publication number: 20160194334
    Abstract: There is provided Form 2 crystalline polymorph consisting of N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]-benzamide monohydrochloride and N-[1-6-(ethynyl-3-oxo-hexahydro-furo[3,2-b]pyrrole-4-carbonyl)-3-methyl-butyl]-4-[5-fluoro-2-(4-methyl-piperazin-1-yl)thiazol-4-yl]benzamide hydrate monohydrochloride, its use as a medicament and methods for its preparation.
    Type: Application
    Filed: August 13, 2014
    Publication date: July 7, 2016
    Applicant: MEDIVIR AB
    Inventors: Urszula GRABOWSKA, Lourdes Salvador ODEN, Victor M. DIAZ PEREZ, Andrew CARR
  • Patent number: 9353103
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrog
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: May 31, 2016
    Assignees: Janssen Sciences Ireland UC, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
  • Patent number: 9200006
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Grant
    Filed: April 9, 2014
    Date of Patent: December 1, 2015
    Assignee: MEDIVIR AB
    Inventors: Lourdes Salvador Oden, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
  • Patent number: 9040562
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: May 26, 2015
    Assignees: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist
  • Patent number: 9023808
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: May 5, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Agustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Milsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alverez, Bjorn Olaf Classon, Hans Kristian Wallberg
  • Patent number: 9012428
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 21, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Patent number: 9006209
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 14, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Patent number: 8937080
    Abstract: Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: January 20, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Pierre Jean-Marie Bernard Raboisson, Anna Karin Gertrud Linnea Belfrage, Björn Olof Classon, Karin Charlotta Lindquist, Karl Magnus Nilsson, Åsa Annica Kristina Rosenquist, Bertil Bengt Samuelsson, Horst Jürgen Wähling
  • Patent number: 8933052
    Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: January 13, 2015
    Assignees: Janssen Products, LP, Medivir, AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20140255347
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge
    Type: Application
    Filed: May 23, 2014
    Publication date: September 11, 2014
    Applicants: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
  • Publication number: 20140221654
    Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4 alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as oste
    Type: Application
    Filed: April 9, 2014
    Publication date: August 7, 2014
    Applicant: MEDIVIR AB
    Inventors: Lourdes Salvador ODEN, Magnus NILSSON, Pia KAHNBERG, Bertil SAMUELSSON, Urszula GRABOWSKA
  • Patent number: 8754105
    Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and whe
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: June 17, 2014
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov
  • Patent number: 8754106
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrog
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: June 17, 2014
    Assignees: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville