Patents Assigned to Vernalis (R&D) Ltd
  • Patent number: 10556911
    Abstract: Compounds of formula (I) are A2B receptor antagonists: Wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated rin
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: February 11, 2020
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
  • Patent number: 10457689
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6 and Y are as defined in the description. Medicaments.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: October 29, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Attila Paczal, Zoltán Szlávik, András Kotschy, Maïa Chanrion, Ana Leticia Maragno, Olivier Geneste, Didier Demarles, Balázs Bálint, Szabolcs Sipos
  • Patent number: 10457687
    Abstract: Compounds of formula (I): wherein R1, R2, R5, R6, R7, R12, X, Y, A, E and n are as defined in the description. Medicinal products containing the same which are useful in treating a condition requiring a pro-apoptotic agent.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: October 29, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Zoltán Szlávik, Zoltán Szabó, Márton Csékei, Attila Paczal, András Kotschy, Alain Bruno, Olivier Geneste, I-Jen Chen, James Edward Paul Davidson, James Brooke Murray, Levente Ondi, Gábor Radics, Szabolcs Sipos, Ágnes Proszenyák, Françoise Perron-Sierra, Balázs Bálint
  • Patent number: 10414754
    Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: September 17, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jérôme-Benoît Starck, Jean-Michel Henlin, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen
  • Patent number: 10383871
    Abstract: Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: August 20, 2019
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Stephen Roughley, Steven Walls, Terance Hart, Rachel Parsons, Paul Brough, Christopher Graham, Alba Macias
  • Patent number: 10323041
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, W, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: June 18, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Balazs Balint, Márton Csékei, Zoltán Szabó, Zoltan Szlavik, András Kotschy, Maïa Chanrion, Olivier Geneste, I-Jen Chen, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Levente Ondi, Ágnes Proszenyák
  • Patent number: 10322131
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R14, A and n are as defined in the description.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: June 18, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Zoltan Szlavik, Attila Paczal, Balazs Balint, András Kotschy, Maïa Chanrion, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Ágnes Proszenyák
  • Patent number: 10278972
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: May 7, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: András Kotschy, Zoltán Szlávik, Márton Csékei, Attila Paczal, Zoltán Szabó, Szabolcs Sipos, Gábor Radics, Ágnes Proszenyák, Balázs Bálint, Alain Bruno, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Françoise Perron-Sierra
  • Patent number: 10258626
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: February 9, 2017
    Date of Patent: April 16, 2019
    Assignees: LES LABORATORIES SERVIER, VERNALIS (R&D) LTD
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Mikl{dot over (o)}s Nyerges, Guillaume De Nanteuil
  • Patent number: 10227358
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R13, Ra, Rb, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
    Type: Grant
    Filed: June 22, 2016
    Date of Patent: March 12, 2019
    Assignees: LES LABORATOIRES SERVIER, VERNALIS &R&D) LTD.
    Inventors: Zoltan Szlavik, András Kotschy, Maïa Chanrion, Didier Demarles, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Attila Paczal, Balazs Balint
  • Patent number: 9944620
    Abstract: Compounds of formula (I) wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: April 17, 2018
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jéròme-Benoît Starck, Jean-Michel Henlin, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen
  • Patent number: 9920066
    Abstract: Compounds of formula (I) are A2B receptor antagonists: Wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —N(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated rin
    Type: Grant
    Filed: February 20, 2017
    Date of Patent: March 20, 2018
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
  • Patent number: 9809574
    Abstract: Compounds of formula (I): wherein Het, R3, R4, R5, R7, R8, R9, T, p, p?, q, and q? are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: November 7, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Claire Walmsley, Mark Dodsworth, Johannes W. G. Meissner, Paul Brough, Imre Fejes, János Tatai, Miklós Nyerges, András Kotschy, Zoltán Szlávik, Olivier Geneste, Arnaud Le Tiran, Thierry Le Diguarher, Jean-Michel Henlin, Jérôme-Benoît Starck, Anne-Françoise Guillouzic, Guillaume De Nanteuil
  • Patent number: 9765056
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R3, R4, R5, A1, A2, T and W are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: September 19, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Patrick Casara, Thierry Le Diguarher, Jean-Michel Henlin, Jéröme-Benoit Starck, Arnaud Le Tiran, Guillaume De Nanteuil, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Claire Walmsley, Christopher John Graham, Stuart Ray, Daniel Maddox, Simon Bedford
  • Patent number: 9718793
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: August 1, 2017
    Assignees: Vernalis (R&D) Ltd., Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Patent number: 9670227
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R12, X, A and n are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: June 6, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: András Kotschy, Zoltán Szlávik, Márton Csékei, Attila Paczal, Zoltán Szabó, Szabolcs Sipos, Gábor Radics, Ágnes Proszenyák, Balázs Bálint, Alain Bruno, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Françoise Perron-Sierra
  • Patent number: 9610290
    Abstract: Compounds of formula (I) are A2B receptor antagonists: Wherein R1 is optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; R2 and R3 are independently selected from hydrogen, C1-C6 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkyl-(C1-C6)-alkyl, aryl-(C1-C6)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C1-C6 alkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or R2 and R3 taken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; R4 is C1-C3 alkyl, C2-C3 alkenyl, —(—R5)—R6, or optionally substituted heteroarylmethylamino; and R5 and R6 are independently selected from hydrogen or C1-C3 alkyl; or R5 and R6 taken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring
    Type: Grant
    Filed: July 20, 2015
    Date of Patent: April 4, 2017
    Assignee: Vernalis (R&D) Ltd.
    Inventors: Allan Jordan, Simon Bedford, Klenke Burkhard, Ian Yule, Karine Poullennec
  • Patent number: 9604975
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: March 28, 2017
    Assignee: Vernalis (R&D) Ltd
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Patent number: 9603854
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 15, 2015
    Date of Patent: March 28, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • Patent number: 9598427
    Abstract: Compounds of formula (I): wherein A1, A2, Ra, Rb, Rc, Rd, R3, R4, R5 and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Grant
    Filed: July 13, 2015
    Date of Patent: March 21, 2017
    Assignees: LES LABORATOIRES SERVIER, VERNALIS (R&D) LTD
    Inventors: Arnaud Le Tiran, Thierry Le Diguarher, Jérôme-Benoît Starck, Jean-Michel Henlin, Anne-Françoise Guillouzic, Guillaume De Nanteuil, Olivier Geneste, Imre Fejes, Janos Tatai, Miklos Nyerges, James Edward Paul Davidson, James Brooke Murray, I-Jen Chen, Didier Durand