JP6243918B2 - Pkm2調節因子およびそれらの使用方法 - Google Patents

Pkm2調節因子およびそれらの使用方法 Download PDF

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JP6243918B2
JP6243918B2 JP2015537799A JP2015537799A JP6243918B2 JP 6243918 B2 JP6243918 B2 JP 6243918B2 JP 2015537799 A JP2015537799 A JP 2015537799A JP 2015537799 A JP2015537799 A JP 2015537799A JP 6243918 B2 JP6243918 B2 JP 6243918B2
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pharmaceutically acceptable
stereoisomer
tautomer
acceptable salt
compound
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JP2015536325A (ja
JP2015536325A5 (OSRAM
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コク−カン ホ,
コク−カン ホ,
ヨン シュー,
ヨン シュー,
マイケル デイビッド サンダース,
マイケル デイビッド サンダース,
シャオフイ リウ,
シャオフイ リウ,
スコット アルバート ピーアス,
スコット アルバート ピーアス,
ケビン ブレット ライト,
ケビン ブレット ライト,
ジェイソン マーク フォークス,
ジェイソン マーク フォークス,
ケネス マーク パーネル,
ケネス マーク パーネル,
スティーブン ブライアン カナー,
スティーブン ブライアン カナー,
デイビッド リー ボルマー,
デイビッド リー ボルマー,
ジーフア リウ,
ジーフア リウ,
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トレロ ファーマシューティカルズ, インコーポレイテッド
トレロ ファーマシューティカルズ, インコーポレイテッド
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    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/65031Five-membered rings having the nitrogen atoms in the positions 1 and 2

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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JP2015537799A 2012-10-16 2013-10-16 Pkm2調節因子およびそれらの使用方法 Active JP6243918B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261714659P 2012-10-16 2012-10-16
US61/714,659 2012-10-16
US201361875855P 2013-09-10 2013-09-10
US61/875,855 2013-09-10
PCT/US2013/065296 WO2014062838A2 (en) 2012-10-16 2013-10-16 Pkm2 modulators and methods for their use

Related Child Applications (1)

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JP2017203963A Division JP6526767B2 (ja) 2012-10-16 2017-10-20 Pkm2調節因子およびそれらの使用方法

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JP2015536325A JP2015536325A (ja) 2015-12-21
JP2015536325A5 JP2015536325A5 (OSRAM) 2016-12-01
JP6243918B2 true JP6243918B2 (ja) 2017-12-06

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JP2015537799A Active JP6243918B2 (ja) 2012-10-16 2013-10-16 Pkm2調節因子およびそれらの使用方法
JP2017203963A Active JP6526767B2 (ja) 2012-10-16 2017-10-20 Pkm2調節因子およびそれらの使用方法
JP2018186629A Withdrawn JP2019023209A (ja) 2012-10-16 2018-10-01 Pkm2調節因子およびそれらの使用方法
JP2020035657A Withdrawn JP2020097631A (ja) 2012-10-16 2020-03-03 Pkm2調節因子およびそれらの使用方法
JP2020035656A Withdrawn JP2020105190A (ja) 2012-10-16 2020-03-03 Pkm2調節因子およびそれらの使用方法
JP2021120679A Active JP7128331B2 (ja) 2012-10-16 2021-07-21 Pkm2調節因子およびそれらの使用方法
JP2021129580A Pending JP2021181467A (ja) 2012-10-16 2021-08-06 Pkm2調節因子およびそれらの使用方法

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JP2017203963A Active JP6526767B2 (ja) 2012-10-16 2017-10-20 Pkm2調節因子およびそれらの使用方法
JP2018186629A Withdrawn JP2019023209A (ja) 2012-10-16 2018-10-01 Pkm2調節因子およびそれらの使用方法
JP2020035657A Withdrawn JP2020097631A (ja) 2012-10-16 2020-03-03 Pkm2調節因子およびそれらの使用方法
JP2020035656A Withdrawn JP2020105190A (ja) 2012-10-16 2020-03-03 Pkm2調節因子およびそれらの使用方法
JP2021120679A Active JP7128331B2 (ja) 2012-10-16 2021-07-21 Pkm2調節因子およびそれらの使用方法
JP2021129580A Pending JP2021181467A (ja) 2012-10-16 2021-08-06 Pkm2調節因子およびそれらの使用方法

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US (5) US9394257B2 (OSRAM)
EP (1) EP2909181B1 (OSRAM)
JP (7) JP6243918B2 (OSRAM)
DK (1) DK2909181T3 (OSRAM)
ES (1) ES2644758T3 (OSRAM)
WO (1) WO2014062838A2 (OSRAM)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2909181T3 (da) * 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
TN2019000290A1 (en) 2017-03-20 2021-05-07 Forma Therapeutics Inc Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
BR112021005188A2 (pt) 2018-09-19 2021-06-08 Forma Therapeutics, Inc. tratamento de anemia falciforme com um composto de ativação de piruvato cinase r
JP7450610B2 (ja) 2018-09-19 2024-03-15 ノヴォ・ノルディスク・ヘルス・ケア・アーゲー ピルビン酸キナーゼrの活性化
WO2020198067A1 (en) * 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Pkm2 modulators and methods for their use
AU2020245437A1 (en) 2019-03-22 2021-09-30 Sumitomo Pharma Oncology, Inc. Compositions comprising PKM2 modulators and methods of treatment using the same
PE20221009A1 (es) 2019-08-06 2022-06-15 Biocryst Pharm Inc Sintesis de un inhibidor de calicreina plasmatica a escala de proceso
BR112022004715A2 (pt) 2019-09-19 2022-06-14 Forma Therapeutics Inc Composições de ativação de piruvato quinase r (pkr)
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2779780A (en) 1955-03-01 1957-01-29 Du Pont 1, 4-diamino-2, 3-dicyano-1, 4-bis (substituted mercapto) butadienes and their preparation
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2861087B2 (ja) * 1989-08-08 1999-02-24 三菱化学株式会社 N―アシル‐5‐ピラゾールカルボキサミド類およびこれを有効成分とする殺虫、殺ダニ剤
FI941572A7 (fi) 1991-10-07 1994-05-27 Oncologix Inc Anti-erbB-2-monoklonaalisten vasta-aineiden yhdistelmä ja käyttömenete lmä
JPH08500962A (ja) 1992-02-06 1996-02-06 クリエイティブ バイオモレキュルズ,インコーポレイテッド 癌マーカー用生物合成結合蛋白質
IT1255527B (it) * 1992-09-29 1995-11-09 Mini Ricerca Scient Tecnolog Pirazolcarbossammidi ad attivita' insetticida ed acaricida
US6177401B1 (en) 1992-11-13 2001-01-23 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften Use of organic compounds for the inhibition of Flk-1 mediated vasculogenesis and angiogenesis
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
GB9520822D0 (en) 1995-10-11 1995-12-13 Wellcome Found Therapeutically active compounds
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
DE19600097C1 (de) 1996-01-03 1997-07-31 Siemens Ag Verfahren und Vorrichtung zur Bestimmung einer Flüssigkeitshöhe mit Hilfe von Ultraschallimpulsen
EP0885198B1 (en) 1996-03-05 2001-12-19 AstraZeneca AB 4-anilinoquinazoline derivatives
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
WO1998002437A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
WO1998002434A1 (en) 1996-07-13 1998-01-22 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
YU1899A (sh) 1996-07-18 2000-03-21 Pfizer Inc. Inhibitori matričnih metaloproteaza na bazi fosfinata
EA199900139A1 (ru) 1996-08-23 1999-08-26 Пфайзер, Инк. Производные арилсульфониламиногидроксамовой кислоты
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
AU5131998A (en) 1997-01-06 1998-08-03 Pfizer Inc. Cyclic sulfone derivatives
US6303636B1 (en) 1997-02-03 2001-10-16 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
AU5493598A (en) 1997-02-07 1998-08-26 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
CN1247531A (zh) 1997-02-11 2000-03-15 辉瑞大药厂 芳基磺酰基异羟肟酸衍生物
EP0984930B1 (en) 1997-05-07 2005-04-06 Sugen, Inc. 2-indolinone derivatives as modulators of protein kinase activity
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
PL338633A1 (en) 1997-08-08 2000-11-06 Pfizer Prod Inc Derivatives of aryloxyarylsuphonylamino hydroxamic acid
US6294532B1 (en) 1997-08-22 2001-09-25 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
JP2001518470A (ja) 1997-09-26 2001-10-16 メルク エンド カムパニー インコーポレーテッド 新規な血管形成阻害剤
JP2001522853A (ja) 1997-11-11 2001-11-20 ファイザー・プロダクツ・インク 抗癌剤として有用なチエノピリミジンおよびチエノピリジン誘導体
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
DK2020408T3 (da) 1998-05-29 2013-09-30 Sugen Inc Pyrrol-substitueret 2-indolinon som proteinkinaseinhibitor
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
ATE260255T1 (de) 1998-11-05 2004-03-15 Pfizer Prod Inc 5-oxo-pyrrolidine-2-carbonsäure- hydroxamidderivate
EP1143957A3 (en) 1998-12-16 2002-02-27 Warner-Lambert Company Treatment of arthritis with mek inhibitors
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
JP2001172261A (ja) * 1999-12-20 2001-06-26 Mitsubishi Chemicals Corp ピラゾールカルボン酸アミド類、およびこれを有効成分とする殺虫、殺ダニ剤
PT1255752E (pt) 2000-02-15 2007-10-17 Pharmacia & Upjohn Co Llc Inibidores de proteína quinases: 2-indolinonas substituídas com pirrolo
NZ524120A (en) 2000-07-19 2005-08-26 Warner Lambert Co Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002022605A1 (en) * 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
JP2002363164A (ja) * 2001-04-06 2002-12-18 Mitsubishi Chemicals Corp ピラゾールカルボキサミド類、その中間体およびこれを有効成分とする有害生物防除剤
EP1384714A1 (en) * 2001-04-06 2004-01-28 Nihon Nohyaku Co., Ltd. Pyrazolecarboxamide derivative, intermediate therefor, and pest control agent containing the same as active ingredient
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
CA2478065C (en) 2002-03-08 2013-01-08 Eisai Co. Ltd. Macrocyclic compounds useful as pharmaceuticals
PL401638A1 (pl) 2002-03-13 2013-05-27 Array Biopharma Inc. N3 alkilowane pochodne benzimidazolu jako inhibitory MEK
US20070060589A1 (en) * 2004-12-21 2007-03-15 Purandare Ashok V Inhibitors of protein arginine methyl transferases
EP1869019B1 (en) * 2005-04-08 2014-08-27 Pfizer Products Inc. Bicyclic [3.1.0] heteroaryl amides as type i glycine transport inhibitors
AU2006250354A1 (en) * 2005-05-23 2006-11-30 Japan Tobacco Inc. Pyrazole compound and therapeutic agent for diabetes comprising the same
ES2481402T3 (es) 2005-07-21 2014-07-30 Ardea Biosciences, Inc. Inhibidores de N-(arilamino)sulfonamida de MEK
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US8552050B2 (en) 2007-08-16 2013-10-08 Beth Israel Deaconess Medical Center Activators of pyruvate kinase M2 and methods of treating disease
WO2009028280A1 (ja) * 2007-08-29 2009-03-05 Mitsui Chemicals, Inc. ピラゾールカルボン酸誘導体及びその製造方法、並びに殺菌剤
EP2205242B1 (en) 2007-09-12 2015-04-15 Genentech, Inc. Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック, インコーポレイテッド チエノピリミジン化合物の製造方法
CA3041868C (en) 2008-10-09 2023-03-07 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Bis sulfonamide piperazinyl and piperidinyl activators of human pyruvatekinase
CA2743146A1 (en) 2008-11-17 2010-05-20 Boehringer Ingelheim International Gmbh Heteroaryl diamide compounds useful as mmp-13 inhibitors
WO2010083246A1 (en) 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
CN102448951B (zh) * 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
ES2619557T3 (es) 2009-05-04 2017-06-26 Agios Pharmaceuticals, Inc. Activadores de PKM2 para uso en el tratamiento del cáncer
US8349832B2 (en) 2009-09-02 2013-01-08 Canthera Therapeutics Compounds and compositions for treating cancer
WO2011069298A1 (en) 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag Novel cyclopropane indolinone derivatives
WO2012041256A1 (en) 2010-09-30 2012-04-05 Chi-Ying Huang Anti-cancer extract and compounds
US8692001B2 (en) 2010-10-27 2014-04-08 Dynamix Pharmaceuticals Ltd. Sulfonamides for the modulation of PKM2
EP2651898B1 (en) * 2010-12-17 2015-12-09 Agios Pharmaceuticals, Inc. Novel n-(4-(azetidine-1-carbonyl)phenyl)-(hetero-)arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
CA2822432C (en) 2010-12-21 2019-09-24 Agios Pharmaceuticals, Inc. Bicyclic pkm2 activators
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
EP2497775A1 (en) 2011-03-11 2012-09-12 Ruprecht-Karls-Universität Heidelberg Ferrocene-based compounds and their use as ROS regulating prodrugs
WO2012160447A1 (en) * 2011-05-25 2012-11-29 Dynamix Pharmaceuticals Ltd. 3, 5 -diphenyl- substituted pyrazolines for the treatment of cancer, proliferative, inflammatory or autoimmune diseases
WO2013005157A1 (en) 2011-07-05 2013-01-10 Lupin Limited Sulfone derivatives and their use as pkm2 modulators for the treatment of cancer
DK2909181T3 (da) * 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
EP2917207A1 (en) 2012-11-08 2015-09-16 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions and their use as pkm2 modulators
US9447054B2 (en) 2014-01-15 2016-09-20 Korea Institute Of Radiological & Medical Sciences Anticancer supplement agent including benzo[D]oxazol derivative as effective ingredient

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