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

Info

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
Authority
JP
Japan
Prior art keywords
compound
phenyl
gsk
pyrazolo
pyridazin
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.)
Withdrawn
Application number
JP2002585380A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005504731A5 (https=
Inventor
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，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2005504731A publication Critical patent/JP2005504731A/ja
Publication of JP2005504731A5 publication Critical patent/JP2005504731A5/ja
Withdrawn legal-status Critical Current

Links

Images

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • G—PHYSICS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2299/00—Coordinates from 3D structures of peptides, e.g. proteins or enzymes
    • G—PHYSICS
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Biophysics (AREA)
  • Endocrinology (AREA)
  • Theoretical Computer Science (AREA)
  • Medical Informatics (AREA)
  • Evolutionary Biology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Microbiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Engineering & Computer Science (AREA)
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

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) EP1435957B1 (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)

* 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 (67)

* 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
EP1472245A2 (en) * 2002-02-06 2004-11-03 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
AU2003245700A1 (en) * 2002-02-12 2003-09-04 Glaxo Group Limited Pyrazolopyridine derivatives
GB0207249D0 (en) * 2002-03-27 2002-05-08 Glaxo Group Ltd Novel compounds
WO2004102151A2 (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 therir albumin binding properties
CA2541832C (en) * 2003-10-10 2009-11-24 Pfizer Products Inc. Substituted 2h-[1,2,4]triazolo[4,3-a]pyrazines as gsk-3 inhibitors
WO2005041895A2 (en) * 2003-11-03 2005-05-12 New Century Pharmaceuticals, Inc. 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)
ATE427499T1 (de) * 2004-05-21 2009-04-15 Inst Systems Biology Zusammensetzungen und verfahren zur quantifizierung von serumglykoproteinen
US7812166B2 (en) 2004-10-29 2010-10-12 Abbott Laboratories Kinase inhibitors
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
US20110230564A1 (en) * 2008-08-01 2011-09-22 University Of Florida Research Foundation Ant4 inhibitor compounds and methods of use thereof
WO2010027458A2 (en) * 2008-09-02 2010-03-11 University Of Florida Research Foundation, Inc. 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
EP2987487B1 (en) 2009-08-10 2020-10-07 Samumed, LLC Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
JP2013501792A (ja) * 2009-08-10 2013-01-17 サミュメッド リミテッド ライアビリティ カンパニー Ｗｎｔ／ｂ−カテニンシグナル伝達経路阻害剤としてのインダゾールおよびその治療的使用
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
EP2515655B1 (en) 2009-12-21 2015-08-05 Samumed, LLC 1h-pyrazolo[3,4-beta]pyridines and therapeutic uses thereof
ES2879314T3 (es) 2010-08-18 2021-11-22 Biosplice Therapeutics Inc Dicetonas e hidroxicetonas como activadores de la vía de señalización de catenina
WO2012148994A1 (en) * 2011-04-25 2012-11-01 Usher Iii Initiative Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
US20130017163A1 (en) 2011-07-14 2013-01-17 Latham Keith R Halogenated phenols for diagnostics, antioxidant protection and drug delivery
EP3473099A1 (en) 2011-09-14 2019-04-24 Samumed, LLC Indazole-3-carboxamides and their use as wnt/b-catenin signaling pathway inhibitors
US20150099645A1 (en) * 2012-03-14 2015-04-09 Stephen Marx 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
EP2770994B1 (en) 2012-05-04 2019-08-21 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
WO2014066835A1 (en) * 2012-10-25 2014-05-01 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
WO2014110086A2 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
RU2019104082A (ru) 2013-02-22 2019-04-10 СЭМЬЮМЕД, ЭлЭлСи γ-ДИКЕТОНЫ В КАЧЕСТВЕ АКТИВАТОРОВ WNT/β -КАТЕНИНОВОГО СИГНАЛЬНОГО ПУТИ
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
MX368248B (es) 2014-08-20 2019-09-25 Samumed Llc Gamma-dicetonas para tratamiento y prevencion de piel envejecida y arrugas.
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
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
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
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
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
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
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
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
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
US10206908B2 (en) 2015-08-03 2019-02-19 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof
US10226448B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-pyrrolo[3,2-C]pyridin-2-yl)-1H-pyrazolo[3,4-B]pyridines and therapeutic uses thereof
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles 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
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
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
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
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
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
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
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
US10226453B2 (en) 2015-08-03 2019-03-12 Samumed, Llc 3-(1H-indol-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
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
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
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
WO2017032857A2 (en) * 2015-08-25 2017-03-02 Histide Ag Compounds for inducing tissue formation and uses thereof
IL298067A (en) * 2015-08-25 2023-01-01 Histide Ag Compounds for inducing tissue formation and their uses
BR112018009252A2 (pt) 2015-11-06 2018-11-06 Samumed Llc tratamento da osteoartrite
LT3464285T (lt) 2016-06-01 2022-12-27 Biosplice Therapeutics, Inc. N-(5-(3-(7-(3-fluorfenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)- 3-metilbutanamido gamybos būdas
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
US10758523B2 (en) 2016-11-07 2020-09-01 Samumed, Llc Single-dose, ready-to-use injectable formulations
JP7352284B2 (ja) * 2017-05-15 2023-09-28 ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガン ＬＳＤ－１インヒビターとしてのピロロ〔２，３－ｃ〕ピリジン及び関連類似体
IL299695A (en) 2020-07-09 2023-03-01 Usher Iii Initiative Inc Treatment of cancer, inflammatory diseases and autoimmune diseases

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
WO1993002209A1 (en) 1991-07-22 1993-02-04 The Regents Of The University Of California 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
AU755062B2 (en) 1997-02-07 2002-12-05 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
KR100581199B1 (ko) 1998-06-19 2006-05-17 카이론 코포레이션 글리코겐 신타제 키나제 3의 억제제
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
AU3114600A (en) 1998-12-16 2000-07-03 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
EP1504368A4 (en) * 2002-02-11 2008-01-23 Novartis Vaccines & Diagnostic Method for crystallizing human gsk3 and novel crystal structure thereof
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

Also Published As

Publication number Publication date
US7666647B2 (en) 2010-02-23
JP2010059162A (ja) 2010-03-18
EP2295550A2 (en) 2011-03-16
WO2002088078A3 (en) 2004-05-06
EP2082743A3 (en) 2010-03-03
US20030125332A1 (en) 2003-07-03
CA2444882A1 (en) 2002-11-07
DE60232669D1 (de) 2009-07-30
US7390808B2 (en) 2008-06-24
US20080262205A1 (en) 2008-10-23
EP2082743A2 (en) 2009-07-29
MXPA03009957A (es) 2005-07-25
AU2002259071A1 (en) 2002-11-11
EP1435957B1 (en) 2009-06-17
US20110129896A1 (en) 2011-06-02
US20100227814A1 (en) 2010-09-09
US7883881B2 (en) 2011-02-08
WO2002088078A2 (en) 2002-11-07
EP1435957A2 (en) 2004-07-14
EP2295550A3 (en) 2011-12-14
US8318467B2 (en) 2012-11-27
EP1435957A4 (en) 2005-04-13
ATE433751T1 (de) 2009-07-15

Similar Documents

Publication Publication Date Title
US7390808B2 (en) Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes
US8124392B2 (en) Crystal structure of Aurora-2 protein and binding pockets thereof
US7593820B2 (en) Crystal structure of human Janus Kinase 2 (JAK2) and uses thereof
Raaf et al. The catalytic subunit of human protein kinase CK2 structurally deviates from its maize homologue in complex with the nucleotide competitive inhibitor emodin
EP1518925A1 (en) Crystal of glucokinase protein, and method for drug design using the crystal
US7826982B2 (en) Method of identifying inhibitors using a 3-D structure of RAC-1 GTPASE
Raaf et al. First inactive conformation of CK2α, the catalytic subunit of protein kinase CK2
Hsu et al. Solution structure of the cytotoxic RNase 4 from oocytes of bullfrog Rana catesbeiana
US20070129281A1 (en) Pharmaceutical compounds
US20070276607A1 (en) Crystal structure and uses thereof
Chen et al. Structural and functional characterization of a 5, 10‐methenyltetrahydrofolate synthetase from Mycoplasma pneumoniae (GI: 13508087)
Anupriya et al. Homology modeling and in silico screening of inhibitors for the substrate binding domain of human Siah2: implications for hypoxia-induced cancers
Jiang et al. Elucidating Binding Selectivity in Cyclin-Dependent Kinases (CDKs) 4, 6, and 9: Development of Highly Potent and Selective CDK4/9 Inhibitors
Ruan et al. Fragment based discovery of a small molecule RhoGDI2 ligand HR3119 that inhibits cancer cell metastasis
US8440443B1 (en) MEK1 polypeptides
Dixit et al. Hierarchical Modeling of Activation Mechanisms in the ABL and EGFR Kinase Domains: Thermodynamic and Mechanistic
Townley Visualizing metabolic control: Crystal structures of fission yeast AMPK homologs with regulatory ligands
Wallis et al. Pharmaceutical compounds
Hari Investigating inactive conformations of protein kinases
Domain et al. Nocturnin (NOCT) helps the circadian clock to adjust metabolism according to day and night activity. NOCT is upregulated in early evening and it has been proposed that NOCT serves as a deadenylase for metabolic enzyme mRNAs. We present a 2.7-Å crystal structure of the catalytic domain of human NOCT. Our structure shows that NOCT has a close overall similarity to CCR4 deadenylase family members, PDE12 and CNOT6L, and to a DNA repair enzyme TDP2. All the key catalytic residues present

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20050428

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090331

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090626

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090703

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090730

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090806

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20090826

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20090902

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20090930

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20100922

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20110121