ATE433751T1 - Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen - Google Patents

Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen

Info

Publication number
ATE433751T1
ATE433751T1 AT02729056T AT02729056T ATE433751T1 AT E433751 T1 ATE433751 T1 AT E433751T1 AT 02729056 T AT02729056 T AT 02729056T AT 02729056 T AT02729056 T AT 02729056T AT E433751 T1 ATE433751 T1 AT E433751T1
Authority
AT
Austria
Prior art keywords
gsk
protein
relates
inhibitors
methods
Prior art date
Application number
AT02729056T
Other languages
German (de)
English (en)
Inventor
Haar Ernst Ter
Lovorka Swenson
Jeremy Green
Michael Arnost
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE433751T1 publication Critical patent/ATE433751T1/de

Links

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)
AT02729056T 2001-04-30 2002-04-29 Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen ATE433751T1 (de)

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

Publications (1)

Publication Number Publication Date
ATE433751T1 true ATE433751T1 (de) 2009-07-15

Family

ID=27403701

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02729056T ATE433751T1 (de) 2001-04-30 2002-04-29 Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen

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=)

Families Citing this family (68)

* 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
EP3341397B1 (en) * 2015-08-25 2024-12-18 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
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

Family Cites Families (22)

* 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
AU2001287898A1 (en) 2000-09-22 2002-04-02 Stephen Garland Pyrazolopyridines and pyrazolopyridazines as antidiabetics
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

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
JP2005504731A (ja) 2005-02-17
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

Similar Documents

Publication Publication Date Title
DE60232669D1 (de) Inhibitoren von gsk-3 und kristallstrukturen von gsk-3beta-protein und -proteinkomplexen
DE60331329D1 (de) Kristallstruktur des aurora-2 proteins und dessen bindungstaschen
WO2005105988A3 (en) Crystal structure of human jak3 kinase domain complex and binding pockets thereof
ATE211129T1 (de) Inhibitoren von beta-amyloid-protein-herstellung
DK1240337T3 (da) Fremgangsmåder og præparater til forlængelse af elimeneringshalveringstider af bioaktive forbindelser
WO2003059934A3 (en) Albumin fusion proteins
BR9909358A (pt) Composto, composição farmacêutica, e, processo para prevenção ou alìvio de complicações crÈnicas decorrentes de diabetes melito
NO20084362L (no) Difenylazetidinon derivater inneholdende kolesterol absorbsjonsinhibitor aktivitet
DE60027409D1 (de) Glykosylierte leptinzusammensetzungen und zugehörige verfahren
ATE327250T1 (de) Kristallstruktur von ribosomen und proteinsynthese-inhibitoren
WO2003085093A3 (en) Antibodies that specifically bind to gmad
WO2004090106A3 (en) Crystal structures of human pim-1 kinase protein complexes and binding pockets thereof, and uses thereof in drug design
WO2004013287A3 (en) Antibodies against c3a receptor
BRPI0407031A (pt) Composições e métodos para tratamento de câncer empregando igsf9 e liv-1
WO2005056785A3 (en) Crystal structure of interleukin-2 tyrosine kinase (itk) and binding pockets thereof
ATE423102T1 (de) 4-substituirte-5-cyano-1h-pyrimidin-6-(th)iones als als gsk-3-hemmer
Sumbul et al. Purification and characterization of high molecular mass and low molecular mass cystatin from goat brain
WO2004023270A3 (en) Crystal structure of angiotensin-converting enzyme-related carboxypeptidase
ATE496991T1 (de) Kristallstruktur von tak1-tab1
ATE555447T1 (de) Kristallstruktur der polo-like-kinase 3 (plk3) und bindungstaschen dafür
WO2004110367A3 (en) Sdr proteins from staphylococcus capitis and their use in preventing and treating infections
ATE412903T1 (de) Diagnostik- und therapie- verfahren von mit c5a rezeptor verbundenen krankheiten
WO2002072632A3 (en) Nucleic acids of the human abcc11 gene, vectors containing such nucleic acids and uses thereof.
WO2001037194A3 (en) Crystallizable compositions comprising a caspase-7
WO2005028506A3 (en) Crystal structure of fms-like tyrosine kinase

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties