JP6092118B2 - ニ環式ｐｋｍ２活性化剤 - Google Patents

ニ環式ｐｋｍ２活性化剤 Download PDF

Info

Publication number
JP6092118B2
JP6092118B2 JP2013546384A JP2013546384A JP6092118B2 JP 6092118 B2 JP6092118 B2 JP 6092118B2 JP 2013546384 A JP2013546384 A JP 2013546384A JP 2013546384 A JP2013546384 A JP 2013546384A JP 6092118 B2 JP6092118 B2 JP 6092118B2
Authority
JP
Japan
Prior art keywords
alkyl
formula
independently selected
heterocyclyl
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2013546384A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014500330A (ja
JP2014500330A5 (enExample
Inventor
フランセスコ ジー． サリトゥロ，
フランセスコ ジー． サリトゥロ，
ジェフリー オー． サウンダーズ，
ジェフリー オー． サウンダーズ，
Original Assignee
アジオス ファーマシューティカルズ， インコーポレイテッド
アジオス ファーマシューティカルズ， インコーポレイテッド
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by アジオス ファーマシューティカルズ， インコーポレイテッド, アジオス ファーマシューティカルズ， インコーポレイテッド filed Critical アジオス ファーマシューティカルズ， インコーポレイテッド
Publication of JP2014500330A publication Critical patent/JP2014500330A/ja
Publication of JP2014500330A5 publication Critical patent/JP2014500330A5/ja
Application granted granted Critical
Publication of JP6092118B2 publication Critical patent/JP6092118B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2013546384A 2010-12-21 2011-12-21 ニ環式ｐｋｍ２活性化剤 Expired - Fee Related JP6092118B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201061425513P 2010-12-21 2010-12-21
US201061425557P 2010-12-21 2010-12-21
US201061425528P 2010-12-21 2010-12-21
US201061425499P 2010-12-21 2010-12-21
US61/425,528 2010-12-21
US61/425,499 2010-12-21
US61/425,513 2010-12-21
US61/425,557 2010-12-21
PCT/US2011/066595 WO2012088314A1 (en) 2010-12-21 2011-12-21 Bicyclic pkm2 activators

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016066131A Division JP2016153418A (ja) 2010-12-21 2016-03-29 ニ環式ｐｋｍ２活性化剤

Publications (3)

Publication Number Publication Date
JP2014500330A JP2014500330A (ja) 2014-01-09
JP2014500330A5 JP2014500330A5 (enExample) 2015-02-12
JP6092118B2 true JP6092118B2 (ja) 2017-03-08

Family

ID=45509688

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2013546384A Expired - Fee Related JP6092118B2 (ja) 2010-12-21 2011-12-21 ニ環式ｐｋｍ２活性化剤
JP2016066131A Withdrawn JP2016153418A (ja) 2010-12-21 2016-03-29 ニ環式ｐｋｍ２活性化剤

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2016066131A Withdrawn JP2016153418A (ja) 2010-12-21 2016-03-29 ニ環式ｐｋｍ２活性化剤

Country Status (7)

Country Link
US (3) US9328077B2 (enExample)
EP (1) EP2655350B1 (enExample)
JP (2) JP6092118B2 (enExample)
CA (1) CA2822432C (enExample)
ES (1) ES2569712T3 (enExample)
MX (1) MX336022B (enExample)
WO (1) WO2012088314A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR077292A1 (es) 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas
US9328077B2 (en) * 2010-12-21 2016-05-03 Agios Pharmaceuticals, Inc Bicyclic PKM2 activators
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
CN105272904B (zh) * 2014-07-18 2019-04-09 中国科学院广州生物医药与健康研究院 N-苯基酰胺类化合物及其应用
DE102017005089A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substitulerte 3,4-Dihydrochinoxalin-2(1H)-one
DE102017005091A1 (de) 2016-05-30 2017-11-30 Bayer Pharma Aktiengesellschaft Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one
KR102007135B1 (ko) 2017-03-20 2019-08-02 포르마 세라퓨틱스 인크. 피루베이트 키나제 (pkr) 활성화제로서의 피롤로피롤 조성물
WO2019075367A1 (en) 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
US20200247815A1 (en) 2017-10-19 2020-08-06 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Pyrazolyl-containing tricyclic derivative, preparation method therefor and use thereof
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
EP3941463A1 (en) 2019-03-22 2022-01-26 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
US11566030B2 (en) 2021-02-08 2023-01-31 Global Blood Therapeutics, Inc. Substituted 2,6-dihydropyrrolo[3,4-c]pyrazoles as pyruvate kinase activators
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL80569C (enExample) 1949-07-23
GB935538A (en) 1959-04-06 1963-08-28 Stop Motion Devices Corp Stop-motion head for use on knitting machines
GB1274436A (en) 1970-06-09 1972-05-17 Wolfen Filmfab Veb Process for the sensitization of photographic silver chloride and silver chlorobromide emulsions that may contain colour couplers
US3998828A (en) 1975-01-31 1976-12-21 Pfizer Inc. 4-[2-(1,3-Dialkyl-1,2,3,4-tetra-hydropyrimidine-2,4-dione-5-carboxamido)ethyl]-1-piperidine sulfonamide
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
DE2948434A1 (de) 1979-12-01 1981-06-11 Hoechst Ag, 6000 Frankfurt 1-piperidinsulfonylharnstoffe und verfahren zu ihrer herstellung
US4474599A (en) 1982-07-14 1984-10-02 The Dow Chemical Company 1-(Pyridyl)-1H-1,2,3-triazole derivatives, and use as herbicidal agents
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
GB8325370D0 (en) 1983-09-22 1983-10-26 Fujisawa Pharmaceutical Co Benzoxazoline and benzothiazoline derivatives
US4593102A (en) 1984-04-10 1986-06-03 A. H. Robins Company, Inc. N-[(amino)alkyl]-1-pyrrolidine, 1-piperidine and 1-homopiperidinecarboxamides (and thiocarboxamides) with sulfur linked substitution in the 2, 3 or 4-position
IT1196195B (it) * 1984-07-20 1988-11-10 Minnesota Mining & Mfg Copulanti formatori di colorante cian ed elementi e procedimenti fotografici
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
JPS61129129A (ja) 1984-11-28 1986-06-17 Kureha Chem Ind Co Ltd 抗腫瘍剤
FI855180A7 (fi) 1985-01-18 1986-07-19 Nissan Chemical Ind Ltd Pyratsolisulfonamidijohdannainen, menetelmä sen valmistamiseksi ja sitä sisältävä rikkaruohomyrkky.
EP0246749A3 (en) 1986-05-17 1988-08-31 AgrEvo UK Limited Triazole herbicides
JPS6339875A (ja) 1986-08-05 1988-02-20 Nissin Food Prod Co Ltd ピリミジン誘導体
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
US4775762A (en) 1987-05-11 1988-10-04 The Dow Chemical Company Novel (1H-1,2,3-triazol-1-yl)pyridines
US5962490A (en) 1987-09-25 1999-10-05 Texas Biotechnology Corporation Thienyl-, furyl- and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin
DE3813885A1 (de) 1988-04-20 1989-11-02 Schering Ag 1-chlorpyrimidinyl-1h-1,2,4-triazol-3-sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als mittel mit herbizider, fungizider und pflanzenwachstumsregulierender wirkung
DE3813886A1 (de) 1988-04-20 1989-11-02 Schering Ag 1-triazinyl-1h-1,2,4-triazol-3- sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als mittel mit herbizider, fungizider und pflanzenwachstumsregulierender wirkung
US5220028A (en) 1988-10-27 1993-06-15 Nissan Chemical Industries, Ltd. Halogeno-4-methylpyrazoles
KR910021381A (ko) 1990-02-20 1991-12-20 모리 히데오 4-3급 부틸이미다졸 유도체, 및 이의 제조방법 및 용도
CA2036148A1 (en) 1990-06-29 1991-12-30 Hiroki Tomioka A 1-phenylimidazole derivative and its production and use
DK0565593T3 (da) 1990-12-31 1999-09-27 Monsanto Co Reducering af pesticidinteraktion i afgrøder
US5252590A (en) 1991-06-28 1993-10-12 Sumitomo Chemical Company, Limited 1-pyridylimidazole derivative
IT1252567B (it) 1991-12-20 1995-06-19 Italfarmaco Spa Derivati di 5-isochinolinsolfonammidi inibitori delle protein-chinasi
JPH0625177A (ja) 1992-07-09 1994-02-01 Nissan Chem Ind Ltd ピラゾール誘導体及び除草剤
JP3409165B2 (ja) 1993-04-28 2003-05-26 株式会社林原生物化学研究所 養毛剤とその製造方法
JP3719612B2 (ja) 1993-06-14 2005-11-24 塩野義製薬株式会社 ヘテロ環を含有する尿素誘導体
JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
IL115420A0 (en) 1994-09-26 1995-12-31 Zeneca Ltd Aminoheterocyclic derivatives
WO1996022287A1 (en) 1995-01-20 1996-07-25 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
FR2735127B1 (fr) 1995-06-09 1997-08-22 Pf Medicament Nouvelles piperazines heteroaromatiques utiles comme medicaments.
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
DE19541146A1 (de) 1995-10-25 1997-04-30 Schering Ag Imidazolderivate und deren Verwendung als Stickstoffmonoxid-Synthase-Inhibitoren
FR2744449B1 (fr) 1996-02-02 1998-04-24 Pf Medicament Nouvelles piperazines aromatiques derivees de cycloazanes substitues, ainsi que leur procede de preparation, les compositions pharmaceutiques et leur utilisation comme medicaments
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
JP2000504336A (ja) 1996-02-02 2000-04-11 ゼネカ・リミテッド 薬学製剤として有用なヘテロ環式化合物
JP2000510866A (ja) 1996-05-20 2000-08-22 ダーウィン・ディスカバリー・リミテッド Ｔｎｆとｐｄｅ―ｉｖのインヒビターとしてのキノリンスルホンアミド
US5843485A (en) 1996-06-28 1998-12-01 Incoe Corporation Valve-gate bushing for gas-assisted injection molding
DE19629335A1 (de) 1996-07-20 1998-01-22 Golden Records Ass Internation Karte aus Kunststoff
US6020357A (en) 1996-12-23 2000-02-01 Dupont Pharmaceuticals Company Nitrogen containing heteroaromatics as factor Xa inhibitors
DE19702988A1 (de) 1997-01-28 1998-07-30 Hoechst Ag Isoxazol- und Crotonsäureamidderivate und deren Verwendung als Arzneimittel und Diagnostika
CA2280515A1 (en) 1997-03-11 1998-09-17 E.I. Du Pont De Nemours And Company Heteroaryl azole herbicides
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
DE19743435A1 (de) 1997-10-01 1999-04-08 Merck Patent Gmbh Benzamidinderivate
US6106849A (en) 1998-01-21 2000-08-22 Dragoco Gerberding & Co. Ag Water soluble dry foam personal care product
GB9811427D0 (en) 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
WO2000012077A1 (en) 1998-09-01 2000-03-09 Bristol-Myers Squibb Company Potassium channel inhibitors and method
DE19841985A1 (de) 1998-09-03 2000-03-09 Schering Ag Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate
CN1326457A (zh) 1998-09-18 2001-12-12 巴斯福股份公司 作为激酶抑制剂的4－氨基吡咯并嘧啶
US6211182B1 (en) 1999-03-08 2001-04-03 Schering Corporation Imidazole compounds substituted with a six or seven membered heterocyclic ring containing two nitrogen atoms
US6492408B1 (en) 1999-07-21 2002-12-10 Boehringer Ingelheim Pharmaceuticals, Inc. Small molecules useful in the treatment of inflammatory disease
JP2003509412A (ja) 1999-09-17 2003-03-11 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子阻害剤
EP1216228B1 (en) 1999-09-17 2008-10-29 Millennium Pharmaceuticals, Inc. BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa
AU2001245353A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
US20010037689A1 (en) 2000-03-08 2001-11-08 Krouth Terrance F. Hydraulic actuator piston measurement apparatus and method
US6515013B2 (en) 2000-07-13 2003-02-04 Abbott Laboratories 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications
FR2817349B1 (fr) 2000-11-28 2003-06-20 Centre Nat Rech Scient Nouveau procede de criblage de modulateurs de la transcription bacterienne
JP2002193710A (ja) 2000-12-25 2002-07-10 Kumiai Chem Ind Co Ltd ピリミジン又はトリアジン誘導体及び農園芸用殺菌剤
DE10164711A1 (de) 2001-03-13 2002-10-17 Schebo Biotech Ag Verwendung von Zuckerphosphaten, Zuckerphosphatanalogen, Aminosäuren und/oder Aminosäureanalogen zur Modulation des Glycolyse-Enzym-Komplexes, des Malat Aspartat Shuttles und/oder der Transaminasen
EP1389194A2 (en) 2001-04-27 2004-02-18 Vertex Pharmaceuticals Incorporated Inhibitors of bace
WO2002089793A1 (en) 2001-05-07 2002-11-14 Smithkline Beecham Corporation Sulfonamides
US20040152648A1 (en) 2001-05-23 2004-08-05 Axel Ullrich Pyruvate-kinase as a novel target molecule
US6967212B2 (en) 2001-05-30 2005-11-22 Bristol-Myers Squibb Company Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
US7144883B2 (en) 2001-06-11 2006-12-05 Biovitrum Ab Bicyclic sulfonamide compounds
JP4083397B2 (ja) 2001-06-18 2008-04-30 株式会社ルネサステクノロジ 半導体集積回路装置
RU2283839C2 (ru) 2001-08-15 2006-09-20 Е.И.Дюпон Де Немур Энд Компани Ортозамещенные ариламиды, способ борьбы с насекомыми, композиция для борьбы с насекомыми, промежуточное соединение
JP2003081937A (ja) 2001-09-07 2003-03-19 Bayer Ag ベンゼンスルホンアミド誘導体
US7169788B2 (en) 2001-10-30 2007-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1472248A1 (en) 2002-01-17 2004-11-03 Eli Lilly And Company Modulators of acetylcholine receptors
WO2003073999A2 (en) 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Pini-modulating compounds and methods of use thereof
WO2003076400A1 (en) 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. New inhibitors of histone deacetylase
KR20040090978A (ko) 2002-03-13 2004-10-27 얀센 파마슈티카 엔.브이. 히스톤 디아세틸라제의 신규한 저해제로서의 설포닐-유도체
EP1501514B1 (en) 2002-05-03 2012-12-19 Exelixis, Inc. Protein kinase modulators and methods of use
GB0215775D0 (en) 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
CA2494962C (en) 2002-08-09 2011-06-14 Merck & Co., Inc. Tyrosine kinase inhibitors
CA2501228A1 (en) 2002-10-24 2004-05-06 Sterix Limited Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 and type 2
WO2004073619A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
WO2004074438A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Ccr8 antagonists
US20070032418A1 (en) 2003-02-25 2007-02-08 Ambion, Inc Small-molecule inhibitors of angiogenin and rnases and in vivo and in vitro methods of using same
JP4629657B2 (ja) 2003-04-11 2011-02-09 ハイ・ポイント・ファーマスーティカルズ、エルエルシー １１β−ヒドロキシステロイドデヒドロゲナーゼ１型化活性化合物
EP1635832A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. Combination therapy for the treatment of diabetes
US6818631B1 (en) 2003-08-15 2004-11-16 Nippon Soda Co. Ltd. Fungicidal pyrimidine derivatives
US7247625B2 (en) * 2003-10-09 2007-07-24 Wyeth 6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators
US20080051414A1 (en) 2003-10-14 2008-02-28 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
US20050170316A1 (en) 2004-01-29 2005-08-04 Russell Bruce M. Toothbrush for detecting the presence of plaque
WO2005074946A1 (en) 2004-02-10 2005-08-18 Adenobio N.V. Stable and active complexes of adenosine and adenosine phosphates with aminoalcohols for the treatment of pulmonary artery hypertension, cardiac failure and other diseases
CA2556589A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
US7588779B2 (en) 2004-05-28 2009-09-15 Andrx Labs, Llc Pharmaceutical formulation containing a biguanide and an angiotensin antagonist
GB0412526D0 (en) 2004-06-05 2004-07-14 Leuven K U Res & Dev Type 2 diabetes
CA2577309C (en) 2004-06-24 2013-10-22 Temple University - Of The Commonwealth System Of Higher Education Alpha, beta-unsaturated sulfones, sulfoxides, sulfonimides, sulfinimides, acylsulfonamides and acylsulfinamides and therapeutic uses thereof
TW200606152A (en) 2004-07-02 2006-02-16 Tanabe Seiyaku Co Piperidine compound and process for preparing the same
FR2872704B1 (fr) 2004-07-12 2007-11-02 Laurent Schwartz Pluritherapie contre le cancer
EP2316458A1 (en) 2004-09-20 2011-05-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
JP2008514590A (ja) 2004-09-24 2008-05-08 アストラゼネカ・アクチエボラーグ ベンゾイミダゾール誘導体、それを含む組成物、その製造方法及びその使用
WO2006038594A1 (ja) 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. Ｎ型カルシウムチャネル阻害薬
US20070249625A1 (en) 2004-10-20 2007-10-25 Jakob Busch-Petersen Il-8 Receptor Antagonists
WO2006052546A2 (en) 2004-11-04 2006-05-18 Neurogen Corporation Pyrazolylmethyl heteroaryl derivatives
SE0402762D0 (sv) 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
WO2006055880A2 (en) 2004-11-16 2006-05-26 Genzyme Corporation Diagnostic pkm2 methods and compositions
JP2008526723A (ja) 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するピラゾール誘導体
US20100160304A1 (en) 2005-01-19 2010-06-24 Dainippon Sumitomo Pharma Co., Ltd Aromatic sulfone compound as aldosterone receptor modulator
WO2006087543A1 (en) 2005-02-18 2006-08-24 Astrazeneca Ab Antibacterial piperidine derivatives
SI1879877T1 (sl) 2005-05-03 2013-02-28 Ranbaxy Laboratories Limited Protimikrobna sredstva
DE112006002052A5 (de) 2005-05-18 2008-05-08 Forschungsverbund Berlin E.V. Nicht-Peptidische Inhibitoren der AKAP-PKA-Wechselwirkung
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
JP2009501705A (ja) 2005-07-05 2009-01-22 アストラゼネカ・アクチエボラーグ 新規化合物、その製造方法、中間体、医薬組成物、並びにアルツハイマー病、認知障害、統合失調症に伴う認識機能障害、肥満及びパーキンソン病のような５−ｈｔ６介在疾患の治療におけるそれらの使用
EA015937B1 (ru) 2005-08-26 2011-12-30 Мерк Сероно С.А. Производные пиразина и их применение в качестве ингибиторов pi3k
FI20055644A0 (fi) 2005-12-02 2005-12-02 Nokia Corp Ryhmäviestintä
JP2009521444A (ja) 2005-12-22 2009-06-04 メルク エンド カムパニー インコーポレーテッド カルシウムチャンネルブロッカーとなる置換ピペリジン
BRPI0706654A2 (pt) 2006-01-20 2011-04-05 Smithkline Beecham Corp composição farmacêutica, método para tratar condições ou distìrbios em um mamìfero, uso de um composto, e, composto
JP2007238458A (ja) 2006-03-06 2007-09-20 D Western Therapeutics Institute Inc 新規なイソキノリン誘導体及びこれを含有する医薬
US20090054453A1 (en) 2006-03-17 2009-02-26 Lilian Alcaraz Novel Tetralins as 5-HT6 Modulators
MX2008012064A (es) 2006-03-23 2008-12-17 Amgen Inc Compuestos de amida 1-fenilsulfonil-diaza-heterociclica y sus usos como moduladores de hidroxiesteroide deshidrogenadas.
US8008481B2 (en) 2006-03-31 2011-08-30 Ericsson Anna M Indazole compounds
US8877791B2 (en) 2006-08-04 2014-11-04 Beth Israel Deaconess Medical Center, Inc. Inhibitors of pyruvate kinase and methods of treating disease
US20090247499A1 (en) 2006-08-21 2009-10-01 Fletcher Joan M Sulfonylated piperazines as cannabinoid-1 receptor modulators
WO2008026658A1 (ja) 2006-09-01 2008-03-06 Otsuka Chemical Co., Ltd. Ｎ－ピリジルピペリジン化合物、その製造方法及び有害生物防除剤
ES2435430T3 (es) 2006-10-16 2013-12-19 Thesan Pharmaceuticals, Inc. Pirazolil tienopiridinas terapéuticas
EP2086329B1 (en) 2006-10-26 2014-07-23 The Arizona Board of Regents on behalf of the University of Arizona Aquaporin modulators and methods of using them for the treatment of edema and fluid imbalance
HUP0600810A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
CA2913963A1 (en) 2006-12-08 2008-06-19 Millenium Pharmaceuticals, Inc. Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor
US7897776B2 (en) 2007-04-23 2011-03-01 Salutria Pharmaceuticals Llc Sulfonamide containing compounds for treatment of inflammatory disorders
MX2010000690A (es) 2007-07-18 2010-06-25 Janssen Pharmaceutica Nv Sulfonamidas como moduladores de trpm8.
SG183049A1 (en) 2007-07-20 2012-08-30 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
US8552050B2 (en) 2007-08-16 2013-10-08 Beth Israel Deaconess Medical Center Activators of pyruvate kinase M2 and methods of treating disease
EP2053045A1 (en) 2007-10-26 2009-04-29 Syngenta Participations AG Novel imidazole derivatives
KR20100101580A (ko) 2007-10-26 2010-09-17 신젠타 파티서페이션즈 아게 신규한 이미다졸 유도체
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
ES2620634T3 (es) * 2008-10-09 2017-06-29 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Activadores de piruvato quinasa humana
JP6067226B2 (ja) 2009-03-13 2017-01-25 アジオス ファーマシューティカルズ， インコーポレイテッド 細胞増殖関連疾患のための方法および組成物
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
EP2427441B1 (en) 2009-05-04 2016-12-14 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
WO2010130638A1 (en) 2009-05-14 2010-11-18 Evotec Ag Sulfonamide compounds, pharmaceutical compositions and uses thereof
CA2766873C (en) * 2009-06-29 2018-08-21 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
AR077292A1 (es) 2009-06-29 2011-08-17 Agios Pharmaceuticals Inc Derivados de piperazin - quinolin sulfonamidas y composiciones farmaceuticas
EP2477625A4 (en) 2009-09-14 2012-10-24 Phusis Therapeutics Inc PHARMACEUTICAL COMPOSITIONS AND FORMULATIONS COMPRISING PLECKSTRINE HOMOLOGY DOMAIN INHIBITORS AND METHODS OF USE
CN105153188B (zh) 2009-10-22 2018-06-01 法博太科制药有限公司 抗纤维化剂的稠环类似物
JP5967827B2 (ja) 2009-12-09 2016-08-10 アジオス ファーマシューティカルズ， インコーポレイテッド Ｉｄｈ変異体をもつことを特徴とする癌治療用の治療的活性化合物
JP2013525438A (ja) * 2010-04-29 2013-06-20 アメリカ合衆国 ヒトピルビン酸キナーゼ活性剤
CA2801074A1 (en) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US9328077B2 (en) 2010-12-21 2016-05-03 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
CN103608016A (zh) 2011-05-03 2014-02-26 安吉奥斯医药品有限公司 丙酮酸激酶激活剂在治疗中的用途
WO2013056153A1 (en) 2011-10-13 2013-04-18 Kung Charles Activators of pyruvate kinase m2 and methods of treating disease

Also Published As

Publication number Publication date
CA2822432A1 (en) 2012-06-28
JP2016153418A (ja) 2016-08-25
EP2655350A1 (en) 2013-10-30
WO2012088314A1 (en) 2012-06-28
MX2013007268A (es) 2013-12-06
CA2822432C (en) 2019-09-24
HK1190406A1 (zh) 2014-07-04
ES2569712T3 (es) 2016-05-12
JP2014500330A (ja) 2014-01-09
US20140011804A1 (en) 2014-01-09
MX336022B (es) 2016-01-06
US20160280697A1 (en) 2016-09-29
US9328077B2 (en) 2016-05-03
US20170369481A1 (en) 2017-12-28
US10087169B2 (en) 2018-10-02
EP2655350B1 (en) 2016-03-09

Similar Documents

Publication Publication Date Title
JP6092118B2 (ja) ニ環式ｐｋｍ２活性化剤
JP5764555B2 (ja) 治療組成物および関連する使用方法
JP5756457B2 (ja) ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法
JP5837091B2 (ja) ピルビン酸キナーゼｍ２（ｐｋｍ２）調節剤としての新規ｎ−（４−（アゼチジン−１−カルボニル）フェニル）−（ヘテロ−）アリールスルホンアミド誘導体
EP2427441B1 (en) Pkm2 activators for use in the treatment of cancer
TWI472522B (zh) 治療化合物及組成物
JP2016104814A (ja) 治療用の化合物および組成物
HK1190406B (en) Bicyclic pkm2 activators
HK1168842A (en) Pmk2 activators for use in the treatment of cancer
HK1168842B (en) Pmk2 activators for use in the treatment of cancer
HK1170152A (en) Therapeutic compositions and related methods of use
HK1170152B (en) Therapeutic compositions and related methods of use
HK1190405B (en) Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20141218

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20141218

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150917

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150929

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20151224

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160126

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160224

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160329

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160728

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161028

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170117

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170208

R150 Certificate of patent or registration of utility model

Ref document number: 6092118

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees