AU2011245441B2 - Activators of human pyruvate kinase - Google Patents

Activators of human pyruvate kinase Download PDF

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Publication number
AU2011245441B2
AU2011245441B2 AU2011245441A AU2011245441A AU2011245441B2 AU 2011245441 B2 AU2011245441 B2 AU 2011245441B2 AU 2011245441 A AU2011245441 A AU 2011245441A AU 2011245441 A AU2011245441 A AU 2011245441A AU 2011245441 B2 AU2011245441 B2 AU 2011245441B2
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AU
Australia
Prior art keywords
oxo
sulfonamide
tetrahydroquinoline
alkyl
cancer
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Expired - Fee Related
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AU2011245441A
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English (en)
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AU2011245441A1 (en
Inventor
Douglas S. Auld
Matthew B. Boxer
Min Shen
Craig J. Thomas
Martin J. Walsh
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United States Department of Health and Human Services
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Government of the United States of America
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Publication of AU2011245441B2 publication Critical patent/AU2011245441B2/en
Priority to AU2015201398A priority Critical patent/AU2015201398A1/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16—Benzazepines; Hydrogenated benzazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2011245441A 2010-04-29 2011-04-26 Activators of human pyruvate kinase Expired - Fee Related AU2011245441B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2015201398A AU2015201398A1 (en) 2010-04-29 2015-03-17 Activators of human pyruvate kinase

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32915810P 2010-04-29 2010-04-29
US61/329,158 2010-04-29
PCT/US2011/033852 WO2011137089A1 (en) 2010-04-29 2011-04-26 Activators of human pyruvate kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2015201398A Division AU2015201398A1 (en) 2010-04-29 2015-03-17 Activators of human pyruvate kinase

Publications (2)

Publication Number Publication Date
AU2011245441A1 AU2011245441A1 (en) 2012-11-15
AU2011245441B2 true AU2011245441B2 (en) 2014-12-18

Family

ID=44280778

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2011245441A Expired - Fee Related AU2011245441B2 (en) 2010-04-29 2011-04-26 Activators of human pyruvate kinase

Country Status (6)

Country Link
US (2) US20130109672A1 (enExample)
EP (1) EP2563761A1 (enExample)
JP (1) JP2013525438A (enExample)
AU (1) AU2011245441B2 (enExample)
CA (1) CA2797694A1 (enExample)
WO (1) WO2011137089A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5756457B2 (ja) 2009-04-06 2015-07-29 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 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
DK2448581T3 (en) 2009-06-29 2017-03-13 Agios Pharmaceuticals Inc Therapeutic compositions and methods for their applications
PE20120693A1 (es) 2009-06-29 2012-07-04 Agios Pharmaceuticals Inc Compuestos heterociclos como moduladores de la piruvato cinasa m2 (pkm2)
US9221792B2 (en) 2010-12-17 2015-12-29 Agios Pharmaceuticals, Inc N-(4-(azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase M2 (PMK2) modulators
WO2012088314A1 (en) * 2010-12-21 2012-06-28 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
PT3406251T (pt) 2011-05-03 2024-01-24 Agios Pharmaceuticals Inc Ativadores da piruvato-cinase para utilização em terapia
WO2012151440A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
WO2013027168A1 (en) * 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013122897A1 (en) 2012-02-13 2013-08-22 Amgen Inc. Dihydrobenzoxazine and tetrahydroquinoxaline sodium channel inhibitors
US9051311B2 (en) 2012-03-09 2015-06-09 Amgen Inc. Sulfamide sodium channel inhibitors
NZ707778A (en) * 2012-11-08 2019-03-29 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
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
SG10201900631TA (en) 2014-08-01 2019-02-27 Nuevolution As Compounds active towards bromodomains
FR3030518B1 (fr) 2014-12-19 2018-03-23 Galderma Research & Development Derives sulfonamides en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
FR3030516B1 (fr) 2014-12-19 2019-12-27 Galderma Research & Development Derives sulfonamides bicycles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
MX384883B (es) 2015-06-11 2025-03-14 Agios Pharmaceuticals Inc Métodos para usar activadores de piruvato cinasa.
US10626087B2 (en) 2015-07-10 2020-04-21 Loyola University Of Chicago Indoline and tetrahydroquinoline sulfonyl inhibitors of dimetalloenzymes and use of the same
AR111295A1 (es) 2017-03-20 2019-06-26 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de piruvato quinasa (pkr)
EP3668513B1 (en) 2017-08-15 2021-11-10 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in treating blood disorders
WO2019043208A1 (en) * 2017-09-04 2019-03-07 F. Hoffmann-La Roche Ag DIHYDROQUINOLINONES
CN112105602A (zh) * 2018-03-01 2020-12-18 反应生物公司 基于喹啉和异喹啉的hdac抑制剂及其使用方法
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
US20200129485A1 (en) 2018-09-19 2020-04-30 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
SI4299135T1 (sl) 2019-06-18 2025-12-31 Pfizer Inc. Benzizoksazolni sulfonamidni derivati
MX2022003025A (es) 2019-09-19 2022-04-07 Forma Therapeutics Inc Activacion de la piruvato cinasa r.
DE102019129527A1 (de) 2019-10-31 2021-05-06 Forschungszentrum Jülich GmbH Inhibitoren für Bromodomänen
US20240000806A1 (en) * 2020-11-20 2024-01-04 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Methods and materials for inhibiting cb1 activity
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010042867A2 (en) * 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase

Family Cites Families (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE508815A (enExample) * 1949-07-23
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
JPS569749A (en) * 1979-07-04 1981-01-31 Mitsubishi Paper Mills Ltd Preparation of lithographic plate
DE2948434A1 (de) 1979-12-01 1981-06-11 Hoechst Ag, 6000 Frankfurt 1-piperidinsulfonylharnstoffe und verfahren zu ihrer herstellung
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
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
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
JPH0667926B2 (ja) 1985-11-12 1994-08-31 旭化成工業株式会社 環状のイソキノリンスルホンアミド誘導体
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
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
BR9200951A (pt) 1991-03-21 1992-11-17 Hoffmann La Roche Compostos, processo para sua producao,preparacoes farmaceuticas e uso
IT1252567B (it) 1991-12-20 1995-06-19 Italfarmaco Spa Derivati di 5-isochinolinsolfonammidi inibitori delle protein-chinasi
US5891435A (en) 1993-04-16 1999-04-06 Research Corporation Technologies, Inc. Methods and compositions for delaying or preventing the onset of autoimmune disease
US5639600A (en) 1994-08-05 1997-06-17 The Regents Of The University Of California Diagnosis and treatment of cell proliferative disease having clonal macrophage involvement
DE69637380T2 (de) 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
JPH09286783A (ja) * 1996-02-19 1997-11-04 Fuji Photo Film Co Ltd 感熱記録材料及びジアゾ化合物
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
AR016551A1 (es) * 1997-07-30 2001-07-25 Smithkline Beecham Corp Derivados de 2-oxindol, composiciones farmaceuticas que los comprenden y el uso de los mismos para la manufactura de medicamentos
AR016384A1 (es) 1997-07-30 2001-07-04 Smithkline Beecham Corp Inhibidores de caspasas, composiciones farmaceuticas que comprenden dichos inhibidores de caspasas y uso de los inhibidores de caspasas para prepararun medicamento util para el tratamiento de apoptosis y desordenes asociados con excesiva actividad de la convertosa il-1 beta.
US7087648B1 (en) 1997-10-27 2006-08-08 The Regents Of The University Of California Methods for modulating macrophage proliferation using polyamine analogs
DE19755268A1 (de) * 1997-12-12 1999-06-17 Merck Patent Gmbh Benzamidinderivate
US6617171B2 (en) 1998-02-27 2003-09-09 The General Hospital Corporation Methods for diagnosing and treating autoimmune disease
PL351767A1 (en) 1999-02-09 2003-06-16 Dimensional Pharmaceuticals 3 Heteroaryl amidines, methylamidines and guanidines as protease 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
CO5170498A1 (es) * 1999-05-28 2002-06-27 Abbott Lab Biaril sulfonamidas son utiles como inhibidores de proliferacion celular
JP2003510278A (ja) 1999-09-30 2003-03-18 スミスクライン・ビーチャム・コーポレイション カスパーゼおよびアポプトシス
JP2003535847A (ja) * 2000-06-02 2003-12-02 スージェン・インコーポレーテッド 蛋白質キナーゼ/ホスファターゼ阻害剤としてのインドリノン誘導体
AR032885A1 (es) 2000-08-16 2003-12-03 Actelion Pharmaceuticals Ltd Bis-sulfonamidas, composiciones farmaceuticas, procedimiento para prepararlas y el uso de las mismas para la produccion de las composiciones farmaceuticas
DE60228233D1 (de) 2001-05-23 2008-09-25 Max Planck Gesellschaft Pyruvat-kinase als einem neuen zielmolekül
EP1492794B1 (en) 2002-03-28 2007-12-12 Eli Lilly And Company Piperazine substituted aryl benzodiazepines and their use as dopamine receptor antagonists for the treatment of psychotic disorders
ATE457025T1 (de) * 2002-05-23 2010-02-15 Cytopia Res Pty Ltd Kinaseinhibitoren
AU2003237532B2 (en) 2002-06-12 2009-07-30 Symphony Evolution, Inc. Human ADAM-10 inhibitors
GB0215650D0 (en) 2002-07-05 2002-08-14 Cyclacel Ltd Bisarylsufonamide compounds
WO2004076640A2 (en) 2003-02-25 2004-09-10 Ambion, Inc. Small-molecule inhibitors of angiogenin and rnases and in vivo and in vitro methods of using same
JP2005008624A (ja) * 2003-05-27 2005-01-13 Taiho Yakuhin Kogyo Kk テトラハイドロキノリン骨格を有するスルホンアミド誘導体およびその塩
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
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
RU2261246C1 (ru) 2004-04-15 2005-09-27 Общество с ограниченной ответственностью "Исследовательский Институт Химического Разнообразия" (ООО "Исследовательский Институт Химического Разнообразия") Замещенные 7-сульфонил бензо[b][1,4]диазепины (варианты), способы их получения (варианты), фокусированная библиотека и фармацевтическая композиция
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
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
WO2006055880A2 (en) 2004-11-16 2006-05-26 Genzyme Corporation Diagnostic pkm2 methods and compositions
ES2430569T3 (es) 2005-02-18 2013-11-21 Astrazeneca Ab Compuestos antibacterianos derivados de piperidina
EP1888558B1 (en) 2005-05-16 2011-10-05 Vertex Pharmaceuticals, Inc. Bicyclic derivatives as modulators of ion channels
AR054363A1 (es) 2005-05-23 2007-06-20 Astrazeneca Ab Compuestos que exhiben actividad moduladora en el receptor 5-hidroxi-triptamina 6
FR2887881B1 (fr) 2005-07-01 2009-10-09 Pierre Fabre Medicament Sa Inhibiteurs de proteines kinases
US7345178B2 (en) * 2005-08-04 2008-03-18 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
EP1965799A2 (en) 2005-12-22 2008-09-10 Merck & Co., Inc. Substituted piperidines as calcium channel blockers
EP1962851A2 (en) 2005-12-22 2008-09-03 SmithKline Beecham Corporation Compounds
WO2007076055A2 (en) * 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
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
US8987474B2 (en) * 2006-04-07 2015-03-24 University Of South Florida Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
WO2007120638A2 (en) * 2006-04-12 2007-10-25 President And Fellows Of Harvard College Methods and compositions for modulating glycosylation
DE602006014532D1 (de) 2006-07-11 2010-07-08 Sanofi Aventis N-Ä(1,5-diphenyl-1H-pyrazol-3-yl)methylÜsulfonamid-Derivate Antagonisten der CB1 Rezeptoren der Cannabinoide
TW200817319A (en) * 2006-08-10 2008-04-16 Astellas Pharma Inc Sulfonamide compound or salt thereof
CL2007003223A1 (es) 2006-11-10 2008-01-11 Wyeth Corp Compuestos derivados de piperidinil 4-arilsulfonamidas n-sustituidas, que actuan como moduladores de la proteina sfrp-1; proceso para preparar los compuestos; co mposicion farmaceutica que comprende a dichos copmpuestos y uso de los compuestos para preparar medicamentos para el tratamiento de enfermedades.
EP2132169A1 (en) 2007-03-05 2009-12-16 Biolipox AB New methylenebisphenyl compounds useful in the treatment of inflammation
WO2008124838A1 (en) * 2007-04-10 2008-10-16 University Of Maryland, Baltimore Compounds that inhibit human dna ligases and methods of treating cancer
WO2008130718A1 (en) 2007-04-23 2008-10-30 Atherogenics, Inc. Sulfonamide containing compounds for treatment of inflammatory disorders
WO2009025781A1 (en) 2007-08-16 2009-02-26 Beth Israel Deaconess Medical Center Activators of pyruvate kinase m2 and methods of treating disease
HUE025137T2 (en) * 2007-08-21 2016-01-28 Senomyx Inc Compositions are bitter taste blocking (blocking) compounds
WO2009036341A2 (en) * 2007-09-14 2009-03-19 The Regents Of The University Of Michigan Compositions and methods relating to hiv protease inhibition
JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体
AU2008345225A1 (en) * 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009084501A1 (ja) * 2007-12-27 2009-07-09 Asahi Kasei Pharma Corporation スルタム誘導体
GB0815947D0 (en) * 2008-09-02 2008-10-08 Univ Dundee Compounds
BR112012004149A2 (pt) 2009-08-25 2016-03-22 Abraxis Bioscience Llc terapia de combinação com composições de nanopartículas de taxano e inibidores de hedgehog
WO2011153359A1 (en) 2010-06-04 2011-12-08 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010042867A2 (en) * 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Boxer, M. B. et al, "Identification of activators for the M2 isoform of human pyruvate kinase Version 3", Molecular Libraries, 2009, pages 1-25. Retrieved from internet: http://www.ncbi.nlm.nih.gov/books/NBK56225/pdf/ml170.pdf *

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