AU2015340305B2 - Diheteroaryl histone deacetylase inhibitors and their use in therapy - Google Patents

Diheteroaryl histone deacetylase inhibitors and their use in therapy Download PDF

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Publication number
AU2015340305B2
AU2015340305B2 AU2015340305A AU2015340305A AU2015340305B2 AU 2015340305 B2 AU2015340305 B2 AU 2015340305B2 AU 2015340305 A AU2015340305 A AU 2015340305A AU 2015340305 A AU2015340305 A AU 2015340305A AU 2015340305 B2 AU2015340305 B2 AU 2015340305B2
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alkyl
amino
pyrazin
compound according
heteroaryl
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AU2015340305A1 (en
Inventor
Alexander Richard Liam Cecil
Somhairle Maccormick
William John NODES
Stephen Joseph Shuttleworth
Franck Alexandre Silva
Cyrille Davy Tomassi
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Karus Therapeutics Ltd
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Karus Therapeutics Ltd
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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AU2015340305A 2014-10-29 2015-10-29 Diheteroaryl histone deacetylase inhibitors and their use in therapy Ceased AU2015340305B2 (en)

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GBGB1419228.0A GB201419228D0 (en) 2014-10-29 2014-10-29 Compounds
GB1419228.0 2014-10-29
PCT/GB2015/053260 WO2016067040A1 (en) 2014-10-29 2015-10-29 Diheteroaryl histone deacetylase inhibitors and their use in therapy

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AU2015340305B2 true AU2015340305B2 (en) 2018-12-06

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US (1) US10407435B2 (enExample)
EP (1) EP3212625A1 (enExample)
JP (1) JP2017532357A (enExample)
KR (1) KR20170081194A (enExample)
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AU (1) AU2015340305B2 (enExample)
BR (1) BR112017008794A2 (enExample)
CA (1) CA2966072A1 (enExample)
GB (1) GB201419228D0 (enExample)
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US9676765B2 (en) * 2012-11-07 2017-06-13 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
NZ714283A (en) 2013-05-10 2020-04-24 Karus Therapeutics Ltd Novel histone deacetylase inhibitors
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
WO2016094307A1 (en) 2014-12-08 2016-06-16 The Research Foundation For The State University Of New York Anti-fungals targeting the synthesis of fungal shingolipids
EP3638649A4 (en) 2017-06-16 2021-03-17 The Research Foundation for The State University of New York Anti-fungals compounds targeting the synthesis of fungal sphingolipids
CA3144985A1 (en) 2019-06-27 2020-12-30 The George Washington University, A Congressionally Chartered Not-For-Profit Corporation Hdac6-activated macrophages, compositions, and uses thereof
US11850233B2 (en) 2019-10-28 2023-12-26 Matibur Rahaman Zamadar Reduced adaptive microbial resistance treatment for flesh eating disease (necrotizing fasciitis)
CN112237994B (zh) * 2020-09-21 2022-09-13 昆明冶金研究院有限公司 一种多金属硫化矿硫化锌抑制剂及其制备方法与应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0556396A1 (en) * 1990-11-09 1993-08-25 Nissan Chemical Industries, Limited Substituted pyrazole derivative and agrohorticultural bactericide
WO2007085540A1 (en) * 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
WO2009063240A1 (en) * 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
WO2010086646A1 (en) * 2009-01-28 2010-08-05 Karus Therapeutics Limited Scriptaid isosteres and their use in therapy

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4017500A (en) 1973-07-16 1977-04-12 Schering Corporation Certain 8-amino-1,7-naphthyridines
DE2908324A1 (de) * 1979-03-03 1980-09-18 Hoechst Ag Triazolsubstituierte hydratopasaeurederivate, verfahren zu ihrer herstellung und ihre verwendung als pflanzenschutzmittel
US4792562A (en) 1985-12-04 1988-12-20 Hoechst-Roussel Pharmaceuticals, Inc. N-(pyrrol-1-yl)pyridinamines having memory enhancing activity
US5214038A (en) 1991-04-15 1993-05-25 Hoechst-Roussel Pharmaceuticals Inc. 1-(pyrido[3,4-b]-1,4-oxazinyl-4-yl)-1H-indoles and intermediates for the preparation thereof
DE4120107A1 (de) * 1991-06-14 1992-12-17 Schering Ag Bicyclisch substituierte vinylimidazole, -triazole und -tetrazole
TW343965B (en) * 1994-03-30 1998-11-01 Hoffmann La Roche Novel mono- and bicyclic DNA gyrase inhibitors
JP2000511883A (ja) 1996-04-19 2000-09-12 ノボ ノルディスク アクティーゼルスカブ ホスホチロシン認識ユニットを有する分子のモジュレーター
EP0887348A1 (en) 1997-06-25 1998-12-30 Boehringer Mannheim Italia S.p.A. Bis-Indole derivatives having antimetastatic activity, a process for their preparation and pharmaceutical compositions containing them
JP3712529B2 (ja) 1998-04-24 2005-11-02 大鵬薬品工業株式会社 ３，３−ジピリジルアクリル酸アミド誘導体又はその薬学的に許容される塩
JP5278983B2 (ja) 1999-11-17 2013-09-04 塩野義製薬株式会社 アミド化合物の新規用途
GB9929988D0 (en) 1999-12-17 2000-02-09 Celltech Therapeutics Ltd Chemical compounds
US6608053B2 (en) 2000-04-27 2003-08-19 Yamanouchi Pharmaceutical Co., Ltd. Fused heteroaryl derivatives
CN1186324C (zh) 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
AU2001270260A1 (en) 2000-06-30 2002-01-14 Sugen, Inc. 4-heteroaryl-3-heteroarylidenyl-2-indolinones and their use as protein kinase inhibitors
JP2002255964A (ja) 2000-10-24 2002-09-11 Sankyo Co Ltd イミダゾピリジン誘導体
WO2002034748A1 (fr) 2000-10-24 2002-05-02 Sankyo Company, Limited Derives d'imidazopyridine
US6905669B2 (en) 2001-04-24 2005-06-14 Supergen, Inc. Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase
US7429593B2 (en) 2001-09-14 2008-09-30 Shionogi & Co., Ltd. Utilities of amide compounds
ES2322950T3 (es) 2002-03-13 2009-07-02 Janssen Pharmaceutica Nv Derivados de aminocarbonilo como nuevos inhibidores de histona-desacetilasa.
JP2003313126A (ja) 2002-04-23 2003-11-06 Sankyo Co Ltd イミダゾピリジン誘導体を有効成分とする医薬
JP2004002826A (ja) 2002-04-24 2004-01-08 Sankyo Co Ltd 高分子イミダゾピリジン誘導体
JP4235726B2 (ja) 2002-11-19 2009-03-11 国立大学法人 奈良先端科学技術大学院大学 大きな二光子吸収特性を示すアセチレン結合により連結されたビス（イミダゾリルポルフィリン金属錯体）を構成単位とするポルフィリン連鎖体及びその製造方法
AU2003900608A0 (en) 2003-02-11 2003-02-27 Fujisawa Pharmaceutical Co., Ltd. Hdac inhibitor
EP1724267B1 (en) 2004-02-26 2013-11-06 ASKA Pharmaceutical Co., Ltd. Pyrimidine derivative
MXPA06014018A (es) 2004-06-01 2007-02-08 Hoffmann La Roche 3-amino-1-arilpropil-indoles como inhibidores de reabsorcion de monoaminas.
US20090110720A1 (en) 2004-10-06 2009-04-30 Anders Nykjaer Use of compounds for the prevention of drug-induced cell toxicity
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
JP2008530136A (ja) 2005-02-14 2008-08-07 ミイカナ セラピューティクス インコーポレイテッド ヒストンデアセチラーゼの阻害剤として有用な縮合複素環化合物
EP2491926B1 (en) 2005-03-22 2018-05-09 President and Fellows of Harvard College Treatment of protein degradation disorders
JP2008545660A (ja) 2005-05-20 2008-12-18 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼ阻害剤として有用なピロロピリジン化合物
TW200716545A (en) 2005-06-10 2007-05-01 Sigma Tau Ind Farmaceuti Indole derivatives having anti-tumor activity
WO2007050348A2 (en) 2005-10-21 2007-05-03 Merck & Co., Inc. Potassium channel inhibitors
WO2007084667A2 (en) 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
JP5302186B2 (ja) 2006-04-26 2013-10-02 エフ．ホフマン−ラ ロシュ アーゲー Ｐｉ３ｋ阻害剤としてのピリミジン誘導体
CN101511840A (zh) 2006-04-26 2009-08-19 吉宁特有限公司 磷酸肌醇3-激酶抑制剂化合物及其使用方法
WO2008007780A1 (fr) 2006-07-13 2008-01-17 Kyowa Hakko Kirin Co., Ltd. Dérivé du pentadiènamide
CN101534831B (zh) 2006-09-11 2013-07-17 柯瑞斯公司 包含锌结合基团的取代的酪氨酸抑制剂
ES2532899T3 (es) 2006-10-28 2015-04-01 Methylgene Inc. Derivados de dibenzo[b,f][1,4]oxazepina como inhibidores de histona desacetilasa
JP5178731B2 (ja) 2006-11-22 2013-04-10 カルス セラピューティクス リミテッド デプシペプチドおよびその治療的使用
JP2010518014A (ja) 2007-01-31 2010-05-27 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用な２−アミノピリジン誘導体
CN101663276A (zh) 2007-01-31 2010-03-03 沃泰克斯药物股份有限公司 用作激酶抑制剂的2-氨基吡啶衍生物
WO2008122115A1 (en) * 2007-04-09 2008-10-16 Methylgene Inc. Inhibitors of histone deacetylase
WO2008139987A1 (ja) 2007-04-26 2008-11-20 Japan Science And Technology Agency Ｇタンパク質共役型レセプタ－作動剤
WO2008137270A1 (en) 2007-05-04 2008-11-13 H. Lundbeck A/S Methods of diagnosing and monitoring of npy y5 based disorders
EP2154965A4 (en) 2007-05-29 2011-08-17 Glaxosmithkline Llc NAPHTHYRIDINE DERIVATIVES AS P13 KINASE INHIBITORS
GB0710528D0 (en) 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
WO2009137462A2 (en) 2008-05-05 2009-11-12 Envivo Pharmaceuticals, Inc. Methods for treating cognitive disorders using inhibitors of histone deacetylase
JP2011529932A (ja) 2008-08-05 2011-12-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 置換ナフチリジン及び医薬としてのその使用
US20110257170A1 (en) 2008-10-03 2011-10-20 Merck Serono Sa 4-morpholino-pyrido[3,2-d]pyrimidines
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
BR112012003955A2 (pt) 2009-08-20 2017-09-26 Karus Therapeutics Ltd compostos heterocíclicos tricíclicos como inibidores da fosfoinositídeos 3-quinase
GB201007347D0 (en) 2010-04-30 2010-06-16 Karus Therapeutics Ltd Compounds
ES2647368T3 (es) 2010-10-08 2017-12-21 Vib Vzw Inhibidores de HDAC para tratar la enfermedad de Charcot-Marie-Tooth
AR084312A1 (es) 2010-12-16 2013-05-08 Genentech Inc Compuestos triciclicos inhibidores de la pi3k y composiciones farmaceuticas
CA2825599C (en) 2011-02-01 2021-07-13 The Board Of Trustees Of The University Of Illinois 4-methyl-n-hydroxybenzamide compounds as histone deacetylase (hdac) inhibitors
EP2508510A1 (en) 2011-04-06 2012-10-10 Ikerchem, S.L. Hydroxyphenyl pyrrole compounds containing an hydroxamic acid as hdac inhibitors and medicinal applications thereof
JP6169076B2 (ja) 2011-07-20 2017-07-26 ザ ジェネラル ホスピタル コーポレイション 骨疾患の処置のためのヒストン脱アセチル化酵素６選択的阻害剤
CA2850757A1 (en) 2011-10-03 2013-04-11 The Trustees Of Columbia University In The City Of New York Novel molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1
PH12014500724A1 (en) 2011-10-04 2014-05-19 Institute For Hepatitis And Virus Res Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication
EP2790705B1 (en) 2011-12-15 2017-12-06 Novartis AG Use of inhibitors of the activity or function of pi3k
KR101415742B1 (ko) 2011-12-21 2014-07-04 영남대학교 산학협력단 6―아미노피리딘―3―올 유도체 또는 이의 약제학적 허용가능한 염 및 이를 유효성분으로 함유하는 혈관신생으로 인한 질환의 예방 또는 치료용 약학조성물
GB201204125D0 (en) 2012-03-08 2012-04-25 Karus Therapeutics Ltd Compounds
WO2014032019A2 (en) 2012-08-23 2014-02-27 Georgetown University Compounds and methods of use thereof for treating tumors
US9676765B2 (en) 2012-11-07 2017-06-13 Karus Therapeutics Limited Histone deacetylase inhibitors and their use in therapy
CA2889905A1 (en) 2012-11-08 2014-05-15 Rhizen Pharmaceuticals Sa Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor
US9169214B2 (en) 2012-12-21 2015-10-27 The Board Of Trustees Of The Leland Stanford Junior University Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions
US20160052926A1 (en) 2013-03-15 2016-02-25 Hutchison Medipharma Limited Novel pyrimidine and pyridine compounds and usage thereof
WO2014153280A1 (en) 2013-03-22 2014-09-25 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
NZ714283A (en) 2013-05-10 2020-04-24 Karus Therapeutics Ltd Novel histone deacetylase inhibitors
GB201402431D0 (en) 2014-02-12 2014-03-26 Karus Therapeutics Ltd Compounds
JP6556146B2 (ja) 2014-08-26 2019-08-07 武田薬品工業株式会社 複素環化合物
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201609786D0 (en) 2016-06-03 2016-07-20 Karus Therapeutics Ltd Compounds and method of use
WO2017222952A1 (en) 2016-06-23 2017-12-28 Merck Sharp & Dohme Corp. 3- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histone deacetylase 6 (hdac6) inhibitors
EP3475275B1 (en) 2016-06-23 2024-04-10 Merck Sharp & Dohme LLC 3-aryl and heteroaryl substituted 5-trifluoromethyl oxadiazoles as histone deacetylase 6 (hdac6) inhibitors
WO2017222950A1 (en) 2016-06-23 2017-12-28 Merck Sharp & Dohme Corp. 3-heterocyclyl substituted 5-trifluoromethyl oxadiazoles as histone deacetylase 6 (hdac6) inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0556396A1 (en) * 1990-11-09 1993-08-25 Nissan Chemical Industries, Limited Substituted pyrazole derivative and agrohorticultural bactericide
WO2007085540A1 (en) * 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
WO2009063240A1 (en) * 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
WO2010086646A1 (en) * 2009-01-28 2010-08-05 Karus Therapeutics Limited Scriptaid isosteres and their use in therapy

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CAS RN 1187969-17-0, STN Entry Date 13 Oct 2009 *
CAS RN 1257852-06-4, STN Entry Date 29 Dec 2010 *
Uno, S., et al, "N2-N1 Migration of s-Triazinyl Group in the Reaction of N1-Acetyl-N2-(s-triazinyl)alkylenediamines", Bulletin of the Chemical Society of Japan, 1973, 46(7), 2257-8 *

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