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

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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
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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
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Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE433751T1 publication Critical patent/ATE433751T1/de

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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
    • 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
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    • 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 or three-dimensional 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 or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment

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

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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 (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)
MX (1) MXPA03009957A (enExample)
WO (1) WO2002088078A2 (enExample)

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
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
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
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

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
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
EP1319001A1 (en) * 2000-09-22 2003-06-18 Smithkline Beecham Plc 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
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

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EP1435957A4 (en) 2005-04-13
JP2005504731A (ja) 2005-02-17
CA2444882A1 (en) 2002-11-07
AU2002259071A1 (en) 2002-11-11
US20080262205A1 (en) 2008-10-23
US20100227814A1 (en) 2010-09-09
US20030125332A1 (en) 2003-07-03
EP2082743A2 (en) 2009-07-29
EP2295550A3 (en) 2011-12-14
US7666647B2 (en) 2010-02-23
WO2002088078A2 (en) 2002-11-07
US7883881B2 (en) 2011-02-08
DE60232669D1 (de) 2009-07-30
US20110129896A1 (en) 2011-06-02
MXPA03009957A (es) 2005-07-25
US8318467B2 (en) 2012-11-27
WO2002088078A3 (en) 2004-05-06
US7390808B2 (en) 2008-06-24
EP2295550A2 (en) 2011-03-16
EP1435957A2 (en) 2004-07-14
EP2082743A3 (en) 2010-03-03
JP2010059162A (ja) 2010-03-18

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