公开(公告)号：US20200071310A1

公开(公告)日：2020-03-05

申请号：US16467148

申请日：2017-12-11

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  ASTEX THERAPEUTICS LIMITED

Inventor： Brian W. BUDZIK ,  Peng LI ,  Joseph E. PERO ,  Charlotte Mary GRIFFITHS-JONES ,  Thomas Daniel HEIGHTMAN ,  David NORTON ,  Hendrika Maria Gerarda WILLEMS ,  Alison Jo-Anne WOOLFORD

IPC: C07D413/08 ,  C07D413/14 ,  C07D403/08 ,  C07D401/14 ,  C07D417/14 ,  C07D419/14 ,  A61P11/00

Abstract: The present invention relates to N-aryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators. In particular, the compounds of this invention include a compound of Formula (I):

公开(公告)号：US20190224212A1

公开(公告)日：2019-07-25

申请号：US16375047

申请日：2019-04-04

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics, Limited

Inventor： Jeffrey K. Kerns ,  James Francis Callahan ,  Hongxing Yan ,  Thomas Daniel Heightman ,  Jeffrey Charles Boehm ,  Alison Jo-Anne Woolford

IPC: A61K31/5513 ,  A61K31/421 ,  A61K31/403 ,  A61P11/00 ,  C07D519/00 ,  C07D403/06 ,  C07D267/14 ,  C07D413/10 ,  C07D413/06 ,  C07D498/04

Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.

公开(公告)号：US10351530B2

公开(公告)日：2019-07-16

申请号：US15765377

申请日：2016-10-06

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

Inventor： James Callahan ,  Jeffrey K. Kerns ,  Tindy Li ,  Brent W. McCleland ,  Hong Nie ,  Joseph E. Pero ,  Thomas Glanmor Davies ,  Charlotte Mary Griffiths-Jones ,  Thomas Daniel Heightman ,  Steven Howard ,  David Norton ,  Marinus Leendert Verdonk ,  Alison Jo-Anne Woolford

IPC: C07D231/14 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/10 ,  C07D403/14

Abstract: The present invention relates to arylcyclohexyl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

公开(公告)号：US10045982B2

公开(公告)日：2018-08-14

申请号：US15019563

申请日：2016-02-09

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Valerio Berdini ,  Gordon Saxty ,  Patrick Rene Angibaud ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet ,  Bruno Roux ,  Lieven Meerpoel

IPC: C07D471/04 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377

CPC classification number: A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/04

Abstract: The invention relates to new pyridopyrazine derivative compounds of formula (I-A) or formula (I-B): to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US20180179187A1

公开(公告)日：2018-06-28

申请号：US15736075

申请日：2016-06-15

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics, Limited

Inventor： Jeffrey K. KERNS ,  James CALLAHAN ,  Hongxing YAN ,  Thomas Daniel HEIGHTMAN ,  Charlotte Mary GRIFFITHS-JONES ,  Alison Jo-Anne WOOLFORD ,  Tindy LI ,  Ami Lakdawala SHAH ,  Roderick S. DAVIS ,  David NORTON ,  Jeffrey Charles BOEHM ,  Paris L. HAMILTON

IPC: C07D403/10 ,  C07D413/10 ,  C07D471/04 ,  C07D413/14 ,  C07D255/04 ,  C07D498/04 ,  C07D405/10 ,  C07D487/04 ,  C07D273/01 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D233/64 ,  C07D401/10

CPC classification number: C07D403/10 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P27/00 ,  A61P35/00 ,  A61P37/00 ,  C07D233/60 ,  C07D233/64 ,  C07D249/18 ,  C07D255/04 ,  C07D267/14 ,  C07D273/01 ,  C07D401/10 ,  C07D401/14 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D451/02 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D498/04

Abstract: Provided are aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.

公开(公告)号：US20180021332A1

公开(公告)日：2018-01-25

申请号：US15549881

申请日：2016-02-09

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Diego Fernando Domenico BROGGINI

IPC: A61K31/498 ,  A61K47/18

CPC classification number: A61K31/498 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/4858 ,  A61K47/18 ,  A61K47/26

Abstract: The invention relates to pharmaceutical compositions comprising N-(3,5-dimethoxyphenyl)-N′-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine, or a pharmaceutically acceptable salt thereof or a solvate thereof; to processes for the preparation of said compositions and to the use of said compositions for the manufacture of a medicament for the prophylaxis of or the treatment, in particular the treatment, of diseases, e.g. cancer

公开(公告)号：US20170334907A1

公开(公告)日：2017-11-23

申请号：US15585908

申请日：2017-05-03

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Alison Jo-Anne WOOLFORD ,  Steven HOWARD ,  Ildiko Maria BUCK ,  Gianni CHESSARI ,  Christopher Norbert JOHNSON ,  Emiliano TAMANINI ,  James Edward Harvey DAY ,  Elisabetta CHIARPARIN ,  Thomas Daniel HEIGHTMAN ,  Martyn FREDERICKSON ,  Charlotte Mary GRIFFITHS-JONES

IPC: C07D471/04 ,  C07D487/10 ,  C07D487/04 ,  C07D471/10 ,  C07D413/14 ,  C07D403/14 ,  A61K31/496 ,  C07D401/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/5025 ,  A61K31/501 ,  A61K31/497 ,  C07D403/06 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00

Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US20150239883A1

公开(公告)日：2015-08-27

申请号：US14404188

申请日：2013-05-30

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Patrick René Angibaud ,  Isabelle Noëlle Constance Pilatte ,  Olivier Alexis Georges Querolle

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/5025 ,  A61K31/4375

CPC classification number: A61K31/5377 ,  A61K31/4375 ,  A61K31/4985 ,  A61K31/5025 ,  A61K45/06 ,  C07D403/04 ,  C07D471/04

Abstract: The invention relates to new pyridopyrazine and naphthyridine derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的吡啶并吡嗪衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US20150051199A1

公开(公告)日：2015-02-19

申请号：US14355786

申请日：2012-10-31

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Andrew James Woodhead ,  Christopher Charles Frederick Hamlett ,  Gilbert Ebai Besong ,  Gianni Chessari ,  Maria Grazia Carr ,  Alessia Millemaggi ,  David Norton ,  Susanne Maria Saalau-Bethell ,  Hendrika Maria Gerarda Willems ,  Neil Thomas Thompson ,  Steven Douglas Hiscock

IPC: C07C225/16 ,  A61K31/44 ,  A61K45/06 ,  C07C221/00 ,  C07D213/50 ,  C07D241/20 ,  A61K31/4965 ,  A61K31/138 ,  C07C255/58 ,  A61K31/277 ,  C07D239/26 ,  A61K31/505 ,  C07D275/02 ,  A61K31/425 ,  C07D213/65 ,  C07D261/08 ,  A61K31/42 ,  C07D498/04 ,  A61K31/5383 ,  C07C253/30 ,  C07D213/73

CPC classification number: C07C225/16 ,  A61K9/0019 ,  A61K9/19 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/138 ,  A61K31/277 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/5383 ,  A61K45/06 ,  A61K47/10 ,  A61K47/26 ,  C07B2200/05 ,  C07C221/00 ,  C07C225/18 ,  C07C225/22 ,  C07C229/38 ,  C07C237/06 ,  C07C237/10 ,  C07C237/24 ,  C07C237/30 ,  C07C253/30 ,  C07C255/58 ,  C07C313/06 ,  C07C2601/02 ,  C07D213/50 ,  C07D213/64 ,  C07D213/65 ,  C07D213/73 ,  C07D213/74 ,  C07D213/79 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D231/12 ,  C07D239/26 ,  C07D239/38 ,  C07D241/20 ,  C07D261/08 ,  C07D275/02 ,  C07D277/28 ,  C07D401/04 ,  C07D498/04

Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): or a salt, N-oxide, tautomer or stereoisomer thereof, wherein A is CH or N; E is CH or N; R1 is selected from: an optionally substituted acyclic C1-8 hydrocarbon group wherein one carbon atom of the acyclic C1-8 hydrocarbon group may optionally be replaced by O, S, NRc, S(O) or SO2, or two adjacent carbon atoms of the acyclic C1-8 hydrocarbon group may optionally be replaced by CONRc, NRcCO, NRcSO2 or SO2NRc provided that in each case at least one carbon atom of the acyclic C1-8 hydrocarbon group remains; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is hydrogen or X—R8; X is a C1-8 alkanediyl group wherein one carbon atom of the C1-8 alkanediyl group may optionally be bonded to a —CH2—CH2— moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C1-8 alkanediyl group may optionally be bonded to a —(CH2)n moiety, where n is 1 to 5, to form a C3-7-cycloalkane-1,2-diyl group; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0-3 heteroatom ring members selected from N, O and S; R4 is hydrogen or R4a wherein R4a is halogen; cyano; C1-4 alkyl; fluoro-1-4 alkyl; C1-4 alkoxy; fluoro-C1-4 alkoxy; hydroxy-C1-4 alkyl; or C1-2 alkoxy-C1-4 alkyl; R5 is hydrogen or R5a wherein R5a is selected from C1-2 alkyl optionally substituted with fluorine; C1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R8 is hydroxy or C(═O)NR10R11; provided that when R8 is hydroxy, there are at least two carbon atoms in line between the hydroxy group and the nitrogen atom to which X is attached; R10 is hydrogen or C1-4 alkyl; and R11 is hydrogen; amino-C2-4 alkyl or hydroxy-C2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.

公开(公告)号：US20150031669A1

公开(公告)日：2015-01-29

申请号：US14354636

申请日：2012-10-26

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Steven John Woodhead ,  Christopher William Murray ,  Valerio Berdini ,  Gordon Saxty ,  Gilbert Ebai Besong ,  Lieven Meerpoel ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet

IPC: C07D471/04 ,  A61K31/4985 ,  C07D403/04 ,  C07D405/14 ,  A61K45/06 ,  C07D241/42 ,  C07D413/04 ,  A61K31/506 ,  C07D405/04 ,  C07D417/04 ,  C07D401/04 ,  C07D401/14

CPC classification number: A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D241/44 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D407/04 ,  C07D407/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04

Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract translation: 本发明涉及新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。 癌症。