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 PDFInfo
- Publication number
- 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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- RLJLXKXLYCEMMA-UHFFFAOYSA-N N#CC(C(NN=C1)=O)=C1c1ccccc1 Chemical compound N#CC(C(NN=C1)=O)=C1c1ccccc1 RLJLXKXLYCEMMA-UHFFFAOYSA-N 0.000 description 1
- HPHBOJANXDKUQD-UHFFFAOYSA-N NNC(CC#N)=O Chemical compound NNC(CC#N)=O HPHBOJANXDKUQD-UHFFFAOYSA-N 0.000 description 1
- OCHNFYUNDYIYRF-UHFFFAOYSA-N Nc1n[nH]c2c1c(-c1ccccc1)c(-c1ccccc1Cl)nn2 Chemical compound Nc1n[nH]c2c1c(-c1ccccc1)c(-c1ccccc1Cl)nn2 OCHNFYUNDYIYRF-UHFFFAOYSA-N 0.000 description 1
- OJUGVDODNPJEEC-UHFFFAOYSA-N O=CC(c1ccccc1)=O Chemical compound O=CC(c1ccccc1)=O OJUGVDODNPJEEC-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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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- A—HUMAN NECESSITIES
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- A61P11/06—Antiasthmatics
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- 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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- G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
- G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
- G16B15/00—ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
- G16B15/30—Drug targeting using structural data; Docking or binding prediction
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- C07K—PEPTIDES
- C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
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- G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
- G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
- G16B15/00—ICT specially adapted for analysing two-dimensional [2D] or three-dimensional [3D] molecular structures, e.g. structural or functional relations or structure alignment
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- Animal Behavior & Ethology (AREA)
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- Public Health (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
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- Zoology (AREA)
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- Biotechnology (AREA)
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- Bioinformatics & Computational Biology (AREA)
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- Psychiatry (AREA)
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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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005504731A true JP2005504731A (ja) | 2005-02-17 |
| JP2005504731A5 JP2005504731A5 (https=) | 2005-07-21 |
Family
ID=27403701
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (9)
| Country | Link |
|---|---|
| US (4) | US7390808B2 (https=) |
| EP (3) | EP2295550A3 (https=) |
| JP (2) | JP2005504731A (https=) |
| AT (1) | ATE433751T1 (https=) |
| AU (1) | AU2002259071A1 (https=) |
| CA (1) | CA2444882A1 (https=) |
| DE (1) | DE60232669D1 (https=) |
| MX (1) | MXPA03009957A (https=) |
| WO (1) | WO2002088078A2 (https=) |
Cited By (1)
| 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 (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1360286A2 (en) * | 2000-09-19 | 2003-11-12 | Chiron Corporation | Characterization of the gsk-3beta protein and methods of use thereof |
| WO2003066629A2 (en) * | 2002-02-06 | 2003-08-14 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| EP1504368A4 (en) * | 2002-02-11 | 2008-01-23 | Novartis Vaccines & Diagnostic | Method for crystallizing human gsk3 and novel crystal structure thereof |
| 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 |
| EP1627323A4 (en) * | 2003-05-06 | 2008-04-09 | New Century Pharmaceuticals | ALBUMIN FIXATION SITES FOR EVALUATING DRUG INTERACTIONS OR THE DEVELOPMENT OF MEDICAMENTS 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 |
| US20080050314A1 (en) * | 2004-02-26 | 2008-02-28 | Bayer Healthcare Ag | Diagnostics and Therapeutics for Diseases Associated With Glycogen Synthase Kinase 3 Beta (Gsk3b) |
| US20060141528A1 (en) * | 2004-05-21 | 2006-06-29 | Aebersold Rudolf H | Compositions and methods for quantification of serum glycoproteins |
| ATE554087T1 (de) | 2004-10-29 | 2012-05-15 | Abbott Lab | Neue kinaseinhibitoren |
| 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 |
| US20130039998A1 (en) * | 2008-12-24 | 2013-02-14 | University Of Washington | Compositions of modulators of the wnt/beta-catenin pathway and benzamide and/or hydroxamic acid derivatives to treat bipolar disorder |
| CN105037355B (zh) | 2009-08-10 | 2017-06-06 | 萨穆梅德有限公司 | Wnt信号传导途径的吲唑抑制剂及其治疗用途 |
| CN102595899A (zh) * | 2009-08-10 | 2012-07-18 | 埃皮瑟瑞克斯有限公司 | 作为wnt/b-联蛋白信号传导途径抑制剂的吲唑及其治疗用途 |
| US8846673B2 (en) | 2009-08-11 | 2014-09-30 | Bristol-Myers Squibb Company | Azaindazoles as kinase inhibitors and use thereof |
| LT3001903T (lt) | 2009-12-21 | 2018-01-10 | Samumed, Llc | 1h-pirazolo[3,4-b]piridinai ir jų terapinis panaudojimas |
| RU2592694C2 (ru) | 2010-08-18 | 2016-07-27 | СЭМЬЮМЕД, ЭлЭлСи | Дикетоны и гидроксикетоны в качестве активатора сигнального пути катенина |
| PL2701510T3 (pl) * | 2011-04-25 | 2017-07-31 | Usher Iii Initiative Inc | Pirazolopirydazyny oraz sposoby leczenia zwyrodnieniowych chorób siatkówki i utraty słuchu związanych z zespołem ushera |
| US20130017163A1 (en) | 2011-07-14 | 2013-01-17 | Latham Keith R | Halogenated phenols for diagnostics, antioxidant protection and drug delivery |
| IN2014CN02646A (https=) | 2011-09-14 | 2015-08-07 | Samumed Llc | |
| EP3173788A3 (en) * | 2012-03-14 | 2017-07-12 | Marx, Stephen | Means and methods for diagnostics and therapeutics of diseases |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| NZ629282A (en) | 2012-05-04 | 2017-04-28 | Samumed Llc | 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| 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 |
| 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 |
| CA2889537C (en) * | 2012-10-25 | 2017-12-12 | Usher Iii Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| 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 |
| DK2968249T3 (en) | 2013-02-22 | 2019-03-04 | Samumed Llc | GAMMA DIKETONS AS WNT / BETA-CATENIN SIGNAL ROAD ACTIVATORS |
| 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 |
| MA40454B1 (fr) | 2014-08-20 | 2020-01-31 | Samumed Llc | Gamma-dicétones pour le traitement et la prévention des rides et du vieillissement de la peau |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| US10463651B2 (en) | 2015-08-03 | 2019-11-05 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-indazoles and therapeutic uses thereof |
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| WO2017023996A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US10329309B2 (en) | 2015-08-03 | 2019-06-25 | Samumed, Llc | 3-(3H-imidazo[4,5-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]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 |
| WO2017023989A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023988A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017024003A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023980A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]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 |
| 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 |
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| WO2017024004A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
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| US11578110B2 (en) * | 2015-08-25 | 2023-02-14 | Histide Ag | Compounds for inducing tissue formation and uses thereof |
| WO2017032857A2 (en) * | 2015-08-25 | 2017-03-02 | Histide Ag | Compounds for inducing tissue formation and uses thereof |
| MX380092B (es) | 2015-11-06 | 2025-03-11 | Samumed Llc | Tratamiento de la osteoartritis. |
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| JP2019535672A (ja) | 2016-10-21 | 2019-12-12 | サミュメッド リミテッド ライアビリティ カンパニー | インダゾール−3−カルボキサミドの使用方法およびwnt/β−カテニンシグナル伝達経路阻害剤としてのそれらの使用 |
| MA46696A (fr) | 2016-11-07 | 2019-09-11 | Samumed Llc | Formulations injectables à dose unique prêtes à l'emploi |
| 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 |
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| 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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| DE60232669D1 (de) | 2009-07-30 |
| EP2295550A3 (en) | 2011-12-14 |
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| WO2002088078A3 (en) | 2004-05-06 |
| US8318467B2 (en) | 2012-11-27 |
| US7883881B2 (en) | 2011-02-08 |
| EP2295550A2 (en) | 2011-03-16 |
| JP2010059162A (ja) | 2010-03-18 |
| EP1435957A4 (en) | 2005-04-13 |
| WO2002088078A2 (en) | 2002-11-07 |
| EP2082743A3 (en) | 2010-03-03 |
| AU2002259071A1 (en) | 2002-11-11 |
| US20100227814A1 (en) | 2010-09-09 |
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