Patents by Inventor Susana Ayesa
Susana Ayesa 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).
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Publication number: 20190002436Abstract: Compounds of Formula (I): (Formula I), wherein Z1 is NR1A, CHR1A, CR1BR1B; one of Z2 and Z3 is CH or CR1A?, the other is N, CH or CR1A?; n is 0, 1 or 2; q is 0, 1 or 2; R1A, R1A?, R1B, R2, and R3 are as defined herein, their use as inhibitors of RSV and related aspects.Type: ApplicationFiled: July 28, 2016Publication date: January 3, 2019Inventors: Susana AYESA, Karolina ERSMARK, Gennadiy KALAYANOV, Marie LEIJONMARCK, Lourdes Salvador ODEN, Hans WESTERLIND, Horst WAHLING, Megan BERTRAND, Christian BROCHU, Elise GHIRO, Cyrille KUHN, Claudio STURINO, Johan BYLUND, Fernando SEHGELMEBLE, Stina LUNDGREN
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Patent number: 9023808Abstract: 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: GrantFiled: January 16, 2008Date of Patent: May 5, 2015Assignees: Medivir AB, Janssen R&D IrelandInventors: 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
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Publication number: 20150025250Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of catType: ApplicationFiled: October 2, 2014Publication date: January 22, 2015Inventors: Susana AYESA, Urszula GRABOWSKA, Ellen HEWITT, Daniel JONSSON, Bjorn KLASSON, Pia KAHNBERG, Stina LUNDGREN, Jan TEJBRANT, Daniel WIKTELIUS
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Patent number: 8859505Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of caType: GrantFiled: June 16, 2011Date of Patent: October 14, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Bjorn Klasson, Pia Kahnberg, Stina Lundgren, Jan Tejbrant, Daniel Wiktelius
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Patent number: 8859605Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: GrantFiled: December 10, 2010Date of Patent: October 14, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Pia Kahnberg, Bjorn Klasson, Peter Lind, Lourdes Oden, Kevin Parkes, Daniel Wiktelius
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Patent number: 8853281Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.Type: GrantFiled: December 18, 2009Date of Patent: October 7, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Patent number: 8815809Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterized by inappropriate expression or activation of cathepsin S.Type: GrantFiled: December 10, 2010Date of Patent: August 26, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Stina Lundgren, Lourdes Odèn, Kevin Parkes, Daniel Wiktelius
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Publication number: 20130172232Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathType: ApplicationFiled: June 16, 2011Publication date: July 4, 2013Applicant: MEDIVIR UK LTDInventors: Susana Ayesa, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Bjorn Klasson, Pia Kahnberg, Stina Lundgren, Jan Tejbrant, Daniel Wiktelius
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Patent number: 8383584Abstract: 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: GrantFiled: February 8, 2008Date of Patent: February 26, 2013Assignees: Medivir AB, Janssen R&D IrelandInventors: Dmitry Antonov, Susana Ayesa Alvarez, Anna Karin Gertrud Linnea Belfrage, Carl Erik Daniel Jönsson, David Craig McGowan, Karl Magnus Nilsson, Pierre Jean-Marie Bernard Raboisson, Åsa Annica Kristina Rosenquist, Bengt Bertil Samuelsson
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Publication number: 20120309673Abstract: Compounds of Formula II wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4? is C1-C6alkyl, C1-C6haloalkyl or oxetany-3-yl. for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: ApplicationFiled: December 10, 2010Publication date: December 6, 2012Applicant: Medivir UK LtdInventors: Susana Ayesa, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Stina Lundgren, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
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Publication number: 20120283305Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: ApplicationFiled: December 10, 2010Publication date: November 8, 2012Applicant: Medivir UK LTDInventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
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Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Patent number: 7666834Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers 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 —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 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 or naphthyl, each optioType: GrantFiled: July 28, 2006Date of Patent: February 23, 2010Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Carl Erik Daniel Jönsson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Dmitry Antonov, Lourdes Salvador Odén, Susana Ayesa Alvarez, Björn Olof Classon
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Publication number: 20100041728Abstract: Compounds of the formula 1: 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: ApplicationFiled: February 8, 2008Publication date: February 18, 2010Inventors: Dmitry Antonov, Susana Ayesa Alvarez, Anna Karin Gertrud Linnea Belfrage, Carl Erik Daniel Jönsson, David Craig Mc Gowan, Karl Magnus Nilsson, Pierre Jean-Marie Bernard Raboisson, Åsa Annica Kristina Rosenquist, Bengt Bertil Samuelsson
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Publication number: 20100003216Abstract: Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus sych as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.Type: ApplicationFiled: September 11, 2009Publication date: January 7, 2010Applicant: Medivir ABInventors: Asa Rosenquist, Fredrik Thorstensson, Per-Ola Johansson, Ingemar Kvarnstrom, Susana Ayesa, Bjorn Classon, Laszlo Rakos, Bertil Samuelsson
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Patent number: 7608590Abstract: Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.Type: GrantFiled: January 28, 2005Date of Patent: October 27, 2009Assignee: Medivir ABInventors: Asa Rosenquist, Fredrik Thorstensson, Per-Ola Johansson, Ingemar Kvarnstrom, Susana Ayesa, Bjorn Classon, Laszlo Rakos, Bertil Samuelsson
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Publication number: 20090247512Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, 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 —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 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 or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturaType: ApplicationFiled: January 16, 2008Publication date: October 1, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alvarez, Bjorn Olof Classon, Hans Kristian Wallberg
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Publication number: 20090105302Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers 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 —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 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 or naphthyl, each optioType: ApplicationFiled: July 28, 2006Publication date: April 23, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Carl Erik Daniel Jonsson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov, Lourdes Salvador Oden, Susana Ayesa Alvarez, Bjorn Olof Classon
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Publication number: 20070161574Abstract: Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.Type: ApplicationFiled: January 28, 2005Publication date: July 12, 2007Inventors: Asa Rosenquist, Fredrik Thorstensson, Per-Ola Johansson, Ingemar Kvarnstrom, Susana Ayesa, Bjorn Classon, Laszlo Rakos, Bertil Samuelsson