JP5837091B2 - 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 - Google Patents

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 Download PDF

Info

Publication number
JP5837091B2
JP5837091B2 JP2013544848A JP2013544848A JP5837091B2 JP 5837091 B2 JP5837091 B2 JP 5837091B2 JP 2013544848 A JP2013544848 A JP 2013544848A JP 2013544848 A JP2013544848 A JP 2013544848A JP 5837091 B2 JP5837091 B2 JP 5837091B2
Authority
JP
Japan
Prior art keywords
compound
pharmaceutically acceptable
alkyl
acceptable salt
pkm2
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
JP2013544848A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013545823A (ja
JP2013545823A5 (OSRAM
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，
シュンチー ヤン，
シュンチー ヤン，
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 JP2013545823A publication Critical patent/JP2013545823A/ja
Publication of JP2013545823A5 publication Critical patent/JP2013545823A5/ja
Application granted granted Critical
Publication of JP5837091B2 publication Critical patent/JP5837091B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2013544848A 2010-12-17 2011-12-16 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 Expired - Fee Related JP5837091B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201061424395P 2010-12-17 2010-12-17
US61/424,395 2010-12-17
PCT/US2011/065633 WO2012083246A1 (en) 2010-12-17 2011-12-16 Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators

Publications (3)

Publication Number Publication Date
JP2013545823A JP2013545823A (ja) 2013-12-26
JP2013545823A5 JP2013545823A5 (OSRAM) 2014-11-13
JP5837091B2 true JP5837091B2 (ja) 2015-12-24

Family

ID=45491789

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2013544848A Expired - Fee Related JP5837091B2 (ja) 2010-12-17 2011-12-16 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

Country Status (7)

Country Link
US (1) US9221792B2 (OSRAM)
EP (1) EP2651898B1 (OSRAM)
JP (1) JP5837091B2 (OSRAM)
CA (1) CA2821975A1 (OSRAM)
ES (1) ES2564952T3 (OSRAM)
MX (1) MX2013006900A (OSRAM)
WO (1) WO2012083246A1 (OSRAM)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2944788C (en) 2009-06-29 2023-08-22 Agios Pharmaceuticals, Inc. Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same
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
US9388164B2 (en) 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
JP6243918B2 (ja) * 2012-10-16 2017-12-06 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 Ｐｋｍ２調節因子およびそれらの使用方法
US9458132B2 (en) * 2012-11-08 2016-10-04 Agios Pharmaceuticals, Inc Therapeutic compounds and compositions and their use as PKM2 modulators
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
DK3448859T3 (da) 2017-03-20 2019-09-23 Forma Therapeutics Inc Pyrrolopyrrolsammensætninger som pyruvatkinase- (pkr) aktivatorer
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
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
WO2020198077A1 (en) 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
MX2022003254A (es) 2019-09-19 2022-04-18 Forma Therapeutics Inc Composiciones activadoras de piruvato cinasa r (pkr).
WO2022170200A1 (en) 2021-02-08 2022-08-11 Global Blood Therapeutics, Inc. 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
JP2025500499A (ja) 2021-12-21 2025-01-09 サイノハブ ファーマシューティカル カンパニー リミテッド ビス（アザニリリデン）スルホニル構造を含む化合物および医薬におけるその使用
WO2024245143A1 (zh) 2023-05-26 2024-12-05 赛诺哈勃药业（成都）有限公司 含二氮杂亚基磺酰结构化合物的药物组合物在治疗贫血相关疾病中的用途

Family Cites Families (138)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL76414C (OSRAM) 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
MY106533A (en) 1990-02-20 1995-06-30 Sumitomo Chemical Co A 4-tert.-butyl imidazole derivative and its production and use.
CA2036148A1 (en) 1990-06-29 1991-12-30 Hiroki Tomioka A 1-phenylimidazole derivative and its production and use
HUT65077A (en) 1990-12-31 1994-04-28 Monsanto Co Antidoted herbicides and process for combatting the phytotoxic action of herbicidal compounds
AU644297B2 (en) 1991-06-28 1993-12-02 Sumitomo Chemical Company, Limited A 1-pyridylimidazole derivative and its production and use
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
ES2303337T3 (es) 1995-01-20 2008-08-01 G.D. Searle Llc Inhibidores de la proteasa retroviral de bis-hidroxietilamino sulfonamida.
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
WO1997028128A1 (en) 1996-02-02 1997-08-07 Zeneca Limited Heterocyclic compounds useful as pharmaceutical agents
GB9602166D0 (en) 1996-02-02 1996-04-03 Zeneca Ltd Aminoheterocyclic derivatives
EP0912519A1 (en) 1996-05-20 1999-05-06 Darwin Discovery Limited Quinoline sulfonamides as tnf inhibitors and as pde-iv inhibitors
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
US6172005B1 (en) 1997-03-11 2001-01-09 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
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
SK3852001A3 (en) 1998-09-18 2003-03-04 Basf Ag 4-Aminopyrrolopyrimidines as kinase inhibitors
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
DE60040676D1 (de) 1999-09-17 2008-12-11 Millennium Pharm Inc BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa
NZ517828A (en) 1999-09-17 2003-10-31 Millennium Pharm Inc Inhibitors having activity against mammalian factor Xa
CA2401778C (en) 2000-02-29 2010-12-21 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
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
DE10112926B4 (de) 2001-03-13 2005-11-10 Schebo Biotech Ag Verwendung von Aminooxyacetat zur Tumorbehandlung
US20030095958A1 (en) 2001-04-27 2003-05-22 Bhisetti Govinda R. 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
CA2445653A1 (en) 2001-06-11 2002-12-19 Biovitrum Ab Substituted sulfonamide compounds, process for their use as medicament for the treatment of cns disorders, obesity and type ii diabetes
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
US7288554B2 (en) 2001-08-15 2007-10-30 E.I. Du Pont De Nemours And Company Ortho-substituted aryl amides for controlling invertebrate pests
JP2003081937A (ja) 2001-09-07 2003-03-19 Bayer Ag ベンゼンスルホンアミド誘導体
WO2003037252A2 (en) 2001-10-30 2003-05-08 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2003062235A1 (en) 2002-01-17 2003-07-31 Eli Lilly And Company Modulators of acetylcholine receptors
US20040180889A1 (en) 2002-03-01 2004-09-16 Pintex Pharmaceuticals, Inc. Pin1-modulating compounds and methods of use thereof
EA006707B1 (ru) 2002-03-13 2006-02-24 Янссен Фармацевтика Н. В. Сульфонилпроизводные в качестве новых ингибиторов гистон-деацетилазы
OA12790A (en) 2002-03-13 2006-07-10 Janssen Pharmaceutica Nv New inhibitors of histone deacetylase.
JP4901102B2 (ja) 2002-05-03 2012-03-21 エクセリクシス， インク． プロテインキナーゼモジュレーターおよびその使用方法
GB0215775D0 (en) 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
DE60334386D1 (de) 2002-08-09 2010-11-11 Merck Sharp & Dohme Tyrosinkinaseinhibitoren
AU2003274373A1 (en) 2002-10-24 2004-05-13 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
EP1615698B1 (en) 2003-04-11 2010-09-29 High Point Pharmaceuticals, LLC New amide derivatives and pharmaceutical use thereof
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
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
EP1720874A4 (en) 2004-02-24 2010-03-03 Bioaxone Therapeutique Inc 4-SUBSTITUTED PIPERIDINE DERIVATIVES
WO2005117591A2 (en) 2004-05-28 2005-12-15 Andrx Labs Llc Novel 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
US8058313B2 (en) 2004-06-24 2011-11-15 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
JP5149009B2 (ja) 2004-09-20 2013-02-20 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヒトステアロイル−ＣｏＡデサチュラーゼを阻害するためのピリダジン誘導体
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
US20100160324A1 (en) 2004-12-30 2010-06-24 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
WO2006087543A1 (en) 2005-02-18 2006-08-24 Astrazeneca Ab Antibacterial piperidine derivatives
CA2606804A1 (en) 2005-05-03 2006-11-09 Ranbaxy Laboratories Limited Antimicrobial agents
WO2006122546A1 (de) 2005-05-18 2006-11-23 Forschungsverbund Berlin E.V. Nicht-peptidische inhibitoren der akap-pka-wechselwirkung
GB0513702D0 (en) 2005-07-04 2005-08-10 Sterix Ltd Compound
CN101258135A (zh) 2005-07-05 2008-09-03 阿斯利康(瑞典)有限公司 新化合物、其制备方法、中间体、药物组合物和其在治疗5－ht6介导的疾病例如阿尔茨海默病、认知障碍、精神分裂症相关的认知缺损、肥胖和帕金森病中的用途
JP5226513B2 (ja) 2005-08-26 2013-07-03 メルク セローノ ソシエテ アノニム ピラジン誘導体及びその使用
FI20055644A0 (fi) 2005-12-02 2005-12-02 Nokia Corp Ryhmäviestintä
CA2633379A1 (en) 2005-12-22 2007-07-05 Merck & Co., Inc. Substituted piperidines as calcium channel blockers
CN101404987A (zh) 2006-01-20 2009-04-08 史密丝克莱恩比彻姆公司 磺酰胺衍生物在治疗代射和神经系统疾病中的用途
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
WO2007108742A1 (en) 2006-03-17 2007-09-27 Astrazeneca Ab Novel tetralins as 5-ht6 modulators
AU2007231594A1 (en) 2006-03-23 2007-10-04 Amgen Inc. 1-phenylsulfonyl-diaza heterocyclic amide compounds and their uses as modulators of hydroxsteroid dehydrogenases
CA2659956C (en) 2006-08-04 2016-01-05 Lewis C. Cantley Inhibitors of pyruvate kinase and methods of treating disease
WO2008024284A2 (en) 2006-08-21 2008-02-28 Merck & Co., Inc. Sulfonylated piperazines as cannabinoid-1 receptor modulators
JP5121717B2 (ja) 2006-09-01 2013-01-16 大塚アグリテクノ株式会社 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
CN101528752A (zh) 2006-10-16 2009-09-09 辉瑞产品公司 治疗性吡唑基噻吩并吡啶
WO2008052190A2 (en) 2006-10-26 2008-05-02 Flynn Gary A 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
CA2671502C (en) 2006-12-08 2017-01-24 Millennium 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
AU2008275927B8 (en) 2007-07-18 2014-08-14 Janssen Pharmaceutica N.V. Sulfonamides as TRPM8 modulators
PL2176231T3 (pl) 2007-07-20 2017-04-28 Nerviano Medical Sciences S.R.L. Podstawione pochodne indazolu aktywne jako inhibitory kinazy
US8552050B2 (en) 2007-08-16 2013-10-08 Beth Israel Deaconess Medical Center Activators of pyruvate kinase M2 and methods of treating disease
KR20100101580A (ko) 2007-10-26 2010-09-17 신젠타 파티서페이션즈 아게 신규한 이미다졸 유도체
EP2053045A1 (en) 2007-10-26 2009-04-29 Syngenta Participations AG Novel imidazole derivatives
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
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
EP2406389B1 (en) 2009-03-13 2019-05-08 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
EP2417123A2 (en) * 2009-04-06 2012-02-15 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
DK2427441T3 (en) 2009-05-04 2017-03-20 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
CA2944788C (en) 2009-06-29 2023-08-22 Agios Pharmaceuticals, Inc. Compounds, and compositions thereof, which modulate pyruvate kinase m2, and methods of making same
US20120189670A1 (en) 2009-09-14 2012-07-26 Kirkpatrick D Lynn Pharmaceutical compositions and formulations including inhibitors of the pleckstrin homology domain and methods for using same
IN2012DN03312A (OSRAM) 2009-10-22 2015-10-23 Fibrotech Therapeutics Pty Ltd
ES2642109T3 (es) 2009-12-09 2017-11-15 Agios Pharmaceuticals, Inc. Compuestos terapéuticamente activos para su uso en el tratamiento de cáncer caracterizados por tener una mutación de IDH
US20130109672A1 (en) 2010-04-29 2013-05-02 The United States Of America,As Represented By The Secretary, Department Of Health And Human Service Activators of human pyruvate kinase
EP2575815A4 (en) 2010-06-04 2013-12-25 Albany Molecular Res Inc GLYCIN TRANSPORTER 1 INHIBITORS, METHODS OF MAKING THE SAME, AND USES THEREOF
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

Also Published As

Publication number Publication date
WO2012083246A1 (en) 2012-06-21
HK1190405A1 (zh) 2014-07-04
ES2564952T3 (es) 2016-03-30
JP2013545823A (ja) 2013-12-26
MX2013006900A (es) 2013-10-17
EP2651898B1 (en) 2015-12-09
US9221792B2 (en) 2015-12-29
CA2821975A1 (en) 2012-06-21
EP2651898A1 (en) 2013-10-23
US20140073625A1 (en) 2014-03-13

Similar Documents

Publication Publication Date Title
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
JP5764555B2 (ja) 治療組成物および関連する使用方法
JP6362610B2 (ja) 治療用化合物及び組成物並びにｐｋｍ２調節剤としてのそれらの使用
EP2427441B1 (en) Pkm2 activators for use in the treatment of cancer
JP6092118B2 (ja) ニ環式ｐｋｍ２活性化剤
EP2922832B1 (en) Glutaminase inhibitors and methods of use
EP2922850B1 (en) Compounds and their methods of use
JP5989664B2 (ja) 治療用の化合物および組成物
JP2020019807A (ja) 化合物及びそれらの使用の方法
HK1190405B (en) Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
HK1170152B (en) Therapeutic compositions and related methods of use
HK1170152A (en) Therapeutic compositions and related methods of use
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

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140926

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140926

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150602

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20150604

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150902

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20150918

TRDD Decision of grant or rejection written
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20150918

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20151028

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20151104

R150 Certificate of patent or registration of utility model

Ref document number: 5837091

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees