JP2005504731A - ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造 - Google Patents

ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造 Download PDF

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JP2005504731A
JP2005504731A JP2002585380A JP2002585380A JP2005504731A JP 2005504731 A JP2005504731 A JP 2005504731A JP 2002585380 A JP2002585380 A JP 2002585380A JP 2002585380 A JP2002585380 A JP 2002585380A JP 2005504731 A JP2005504731 A JP 2005504731A
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compound
phenyl
gsk
pyrazolo
pyridazin
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JP2005504731A5 (enExample
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ハー， エルンスト テア
ロボルカ スウェンソン，
ジェレミー グリーン，
マイケル ジェイ． アーノスト，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
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JP2002585380A 2001-04-30 2002-04-29 ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造 Withdrawn JP2005504731A (ja)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US28736601P 2001-04-30 2001-04-30
US29709401P 2001-06-08 2001-06-08
US36189902P 2002-02-27 2002-02-27
PCT/US2002/013511 WO2002088078A2 (en) 2001-04-30 2002-04-29 INHIBITORS OF GSK-3 AND CRYSTAL STRUCTURES OF GSK-3β PROTEIN AND PROTEIN COMPLEXES

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JP2009229078A Division JP2010059162A (ja) 2001-04-30 2009-09-30 ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造

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JP2005504731A true JP2005504731A (ja) 2005-02-17
JP2005504731A5 JP2005504731A5 (enExample) 2005-07-21

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JP2002585380A Withdrawn JP2005504731A (ja) 2001-04-30 2002-04-29 ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造
JP2009229078A Pending JP2010059162A (ja) 2001-04-30 2009-09-30 ＧＳＫ−３のインヒビター、およびＧＳＫ−３βタンパク質およびタンパク質複合体の結晶構造

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US (4) US7390808B2 (enExample)
EP (3) EP2295550A3 (enExample)
JP (2) JP2005504731A (enExample)
AT (1) ATE433751T1 (enExample)
AU (1) AU2002259071A1 (enExample)
CA (1) CA2444882A1 (enExample)
DE (1) DE60232669D1 (enExample)
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019502674A (ja) * 2015-08-25 2019-01-31 ヒスタイド アクツィエンゲゼルシャフト 組織形成誘導用化合物及びその使用

Families Citing this family (66)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4122216B2 (ja) * 2000-09-19 2008-07-23 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド ＧＳＫ−３βタンパク質の特徴づけおよびその使用方法
MXPA04007697A (es) * 2002-02-06 2004-11-10 Vertex Pharma Compuestos de heteroarilo utiles como inhibidores de gsk-3.
JP2005532265A (ja) * 2002-02-11 2005-10-27 カイロン コーポレイション ヒトｇｓｋ３を結晶化するための方法およびその新規な結晶構造
WO2003068773A1 (en) * 2002-02-12 2003-08-21 Glaxo Group Limited Pyrazolopyridine derivatives
GB0207249D0 (en) * 2002-03-27 2002-05-08 Glaxo Group Ltd Novel compounds
CA2565308A1 (en) * 2003-05-06 2004-11-25 New Century Pharmaceuticals Albumin binding sites for evaluating drug interactions and methods of evaluating or designing drugs based on their albumin binding properties
BRPI0415185A (pt) * 2003-10-10 2006-11-28 Pfizer Prod Inc 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3
US20070043509A1 (en) * 2003-11-03 2007-02-22 Carter Daniel C Albumin binding sites for evaluating drug interactions and methods of evaluating or designing drugs based on their albumin binding properties
EP1723427A2 (en) * 2004-02-26 2006-11-22 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with glycogen synthase kinase 3 beta (gsk3b)
DE602005013670D1 (de) * 2004-05-21 2009-05-14 Inst Systems Biology Zusammensetzungen und verfahren zur quantifizierung von serumglykoproteinen
MX2007005120A (es) 2004-10-29 2007-07-16 Abbott Lab Nuevos inhibidores de cinasa.
WO2009126335A2 (en) * 2008-04-08 2009-10-15 University Of Florida Research Foundation, Inc. Ant2 inhibitor compounds and methods of use thereof
US20100016247A1 (en) * 2008-07-21 2010-01-21 Florida State University Research Foundation Using budding yeast to screen for inhibitors of aurora kinases
WO2010014253A2 (en) * 2008-08-01 2010-02-04 University Of Florida Research Foundation, Inc. Ant4 inhibitor compounds and methods of use thereof
US8492344B2 (en) * 2008-09-02 2013-07-23 University Of Florida Research Foundation PDK inhibitor compounds and methods of use thereof
WO2010075551A1 (en) * 2008-12-24 2010-07-01 Massachusetts Institute Of Technology Compositions of modulators of the wnt/beta-catenin pathway and benzamide and/or hydroxamic acid derivatives to treat bipolar disorder
WO2011019648A1 (en) * 2009-08-10 2011-02-17 Epitherix, Llc Indazoles as wnt/b-catenin signaling pathway inhibitors and therapeutic uses thereof
ES2835553T3 (es) 2009-08-10 2021-06-22 Biosplice Therapeutics Inc Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
CN102821607B (zh) * 2009-12-21 2014-12-17 萨穆梅德有限公司 1H-吡唑并[3，4-b]吡啶及其治疗应用
SI3311666T1 (sl) 2010-08-18 2021-09-30 Biosplice Therapeutics, Inc. Diketoni in hidroksiketoni, kot aktivatorji signalne poti katenina
EP2701510B1 (en) 2011-04-25 2017-02-15 Usher III Initiative Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
US20130018026A1 (en) 2011-07-14 2013-01-17 Latham Keith R Halogenated phenols for diagnostics, antioxidant protection and drug delivery
HRP20190281T1 (hr) 2011-09-14 2019-05-31 Samumed, Llc Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin
EP2825886A4 (en) * 2012-03-14 2015-11-18 Stephen Marx MEDIUM AND METHODS OF DIAGNOSIS AND THERAPY OF ILLNESSES
PH12017500997A1 (en) 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
PL2770994T3 (pl) 2012-05-04 2020-03-31 Samumed, Llc 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne
US8765762B2 (en) 2012-10-25 2014-07-01 Usher III, Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome
US9227976B2 (en) 2012-10-25 2016-01-05 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
PL2912038T3 (pl) * 2012-10-25 2019-02-28 Usher Iii Initiative, Inc. Pirazolopirydazyny oraz sposoby leczenia zwyrodnieniowych chorób siatkówki i utraty słuchu związanych z zespołem ushera
EP2943198B1 (en) 2013-01-08 2019-07-17 Samumed, LLC 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
PL2968249T3 (pl) 2013-02-22 2019-06-28 Samumed, Llc Gamma-diketony jako aktywatory szlaku sygnałowego Wnt/beta-kateniny
CA2945263A1 (en) 2014-04-09 2015-10-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
RS59797B1 (sr) 2014-08-20 2020-02-28 Samumed Llc Gama-diketoni za tretman i prevenciju starenja kože i bora
WO2016040188A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040181A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040185A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof
WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2016040182A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof
WO2016040193A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040190A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof
WO2016040184A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
WO2017024010A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024015A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023993A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023986A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof
US10350199B2 (en) 2015-08-03 2019-07-16 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
US10188634B2 (en) 2015-08-03 2019-01-29 Samumed, Llc 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
WO2017023972A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
US10285983B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof
US10231956B2 (en) 2015-08-03 2019-03-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10519169B2 (en) 2015-08-03 2019-12-31 Samumed, Llc 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10206909B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof
US10285982B2 (en) 2015-08-03 2019-05-14 Samumed, Llc 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10166218B2 (en) 2015-08-03 2019-01-01 Samumed, Llc 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
WO2017023984A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017023987A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
US10392383B2 (en) 2015-08-03 2019-08-27 Samumed, Llc 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof
WO2017023975A1 (en) 2015-08-03 2017-02-09 Samumed, Llc. 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof
WO2017032857A2 (en) * 2015-08-25 2017-03-02 Histide Ag Compounds for inducing tissue formation and uses thereof
WO2017032856A2 (en) * 2015-08-25 2017-03-02 Histide Ag Compounds for inducing tissue formation and uses thereof
KR20180080262A (ko) 2015-11-06 2018-07-11 사뮤메드, 엘엘씨 골관절염의 치료
ES2933109T3 (es) 2016-06-01 2023-02-02 Biosplice Therapeutics Inc Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida
CN110709082A (zh) 2016-10-21 2020-01-17 萨穆梅德有限公司 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途
KR102558716B1 (ko) 2016-11-07 2023-07-21 사뮤메드, 엘엘씨 단일-투여량, 즉시-사용가능한 주사용 제제
CN110914265B (zh) * 2017-05-15 2022-12-23 密歇根大学董事会 作为lsd-1抑制剂的吡咯并[2,3-c]吡啶和相关类似物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004509891A (ja) * 2000-09-22 2004-04-02 スミスクライン　ビーチャム　パブリック　リミテッド　カンパニー 抗糖尿病薬としてのピラゾロピリジンおよびピラゾロピリダジン

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4009022A (en) 1975-10-30 1977-02-22 Rohm And Haas Company Selective antagonists for triazine herbicides
US4886646A (en) 1988-03-23 1989-12-12 The United States Of America As Represented By The Administrator Of The National Aeronautics And Space Administration Hanging drop crystal growth apparatus and method
US5096676A (en) 1989-01-27 1992-03-17 Mcpherson Alexander Crystal growing apparatus
US5130105A (en) * 1990-10-23 1992-07-14 The United States Of America As Represented By The Administrator Of The National Aeronautics And Space Administration Protein crystal growth tray assembly
US5200910A (en) 1991-01-30 1993-04-06 The Board Of Trustees Of The Leland Stanford University Method for modelling the electron density of a crystal
AU3320193A (en) 1991-07-22 1993-02-23 Regents Of The University Of California, The Methods of designing specific affectors using three-dimensional conformation of enzyme/affector complex
US5221410A (en) * 1991-10-09 1993-06-22 Schering Corporation Crystal forming device
US5353236A (en) * 1992-04-23 1994-10-04 The Board Of Trustees Of The Leland Stanford University High-resolution crystallographic modelling of a macromolecule
US5453937A (en) 1993-04-28 1995-09-26 Immunex Corporation Method and system for protein modeling
US5400741A (en) 1993-05-21 1995-03-28 Medical Foundation Of Buffalo, Inc. Device for growing crystals
CA2279846C (en) 1997-02-07 2008-06-03 Princeton University Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
GB9721437D0 (en) * 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
US6162613A (en) * 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6387641B1 (en) * 1998-12-16 2002-05-14 Vertex Pharmaceuticals Incorporated Crystallized P38 complexes
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
JP4122216B2 (ja) * 2000-09-19 2008-07-23 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド ＧＳＫ−３βタンパク質の特徴づけおよびその使用方法
WO2002050254A2 (en) * 2000-12-18 2002-06-27 Smithkline Beecham P.L.C. Crystal structure of glycogen synthase kinase 3 beta
JP2005532265A (ja) * 2002-02-11 2005-10-27 カイロン コーポレイション ヒトｇｓｋ３を結晶化するための方法およびその新規な結晶構造
GB0206723D0 (en) * 2002-03-21 2002-05-01 Glaxo Group Ltd Novel compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004509891A (ja) * 2000-09-22 2004-04-02 スミスクライン　ビーチャム　パブリック　リミテッド　カンパニー 抗糖尿病薬としてのピラゾロピリジンおよびピラゾロピリダジン

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019502674A (ja) * 2015-08-25 2019-01-31 ヒスタイド アクツィエンゲゼルシャフト 組織形成誘導用化合物及びその使用
JP2022043261A (ja) * 2015-08-25 2022-03-15 ヒスタイド アクツィエンゲゼルシャフト 組織形成誘導用化合物及びその使用

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