AU2002259071A1 - Inhibitors of gsk-3 and crystal structures of gsk-3beta protein and protein complexes - Google Patents

Inhibitors of gsk-3 and crystal structures of gsk-3beta protein and protein complexes

Info

Publication number
AU2002259071A1
AU2002259071A1 AU2002259071A AU2002259071A AU2002259071A1 AU 2002259071 A1 AU2002259071 A1 AU 2002259071A1 AU 2002259071 A AU2002259071 A AU 2002259071A AU 2002259071 A AU2002259071 A AU 2002259071A AU 2002259071 A1 AU2002259071 A1 AU 2002259071A1
Authority
AU
Australia
Prior art keywords
gsk
protein
relates
inhibitors
methods
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.)
Abandoned
Application number
AU2002259071A
Other languages
English (en)
Inventor
Michael J. Arnost
Jeremy Green
Lovorka Swenson
Ernst Ter Haar
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 AU2002259071A1 publication Critical patent/AU2002259071A1/en
Abandoned legal-status Critical Current

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 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Physics & Mathematics (AREA)
  • Pulmonology (AREA)
  • Biophysics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Theoretical Computer Science (AREA)
  • Medical Informatics (AREA)
  • Evolutionary Biology (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Microbiology (AREA)
AU2002259071A 2001-04-30 2002-04-29 Inhibitors of gsk-3 and crystal structures of gsk-3beta protein and protein complexes Abandoned AU2002259071A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US28736601P 2001-04-30 2001-04-30
US60/287,366 2001-04-30
US29709401P 2001-06-08 2001-06-08
US60/297,094 2001-06-08
US36189902P 2002-02-27 2002-02-27
US60/361,899 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
AU2002259071A1 true AU2002259071A1 (en) 2002-11-11

Family

ID=27403701

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002259071A Abandoned AU2002259071A1 (en) 2001-04-30 2002-04-29 Inhibitors of gsk-3 and crystal structures of gsk-3beta protein and protein complexes

Country Status (9)

Country Link
US (4) US7390808B2 (enExample)
EP (3) EP1435957B1 (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
JP4656838B2 (ja) * 2002-02-06 2011-03-23 バーテックス ファーマシューティカルズ インコーポレイテッド Ｇｓｋ−３の阻害剤として有用なヘテロアリール化合物
WO2003068932A2 (en) * 2002-02-11 2003-08-21 Chiron Corporation 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
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
ATE369370T1 (de) * 2003-10-10 2007-08-15 Pfizer Prod Inc Substituierte 2h-(1,2,4)triazolo(4,3-a)pyrazine als gsk-3-inhibitoren
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)
WO2005114221A2 (en) * 2004-05-21 2005-12-01 The Institute For Systems Biology Compositions and methods for quantification of serum glycoproteins
CA2585934C (en) 2004-10-29 2013-09-10 Abbott Laboratories Novel pyrazolopyridine urea 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
WO2010014253A2 (en) * 2008-08-01 2010-02-04 University Of Florida Research Foundation, Inc. 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
WO2011019651A1 (en) 2009-08-10 2011-02-17 Epitherix, Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
BR112012002942A2 (pt) * 2009-08-10 2015-10-13 Epitherix Llc indazóis como inibidores da trilha de sinalização de wnt/b-catenina e empregos terapêuticos destes.
EP2464647B1 (en) 2009-08-11 2016-09-21 Bristol-Myers Squibb Company Azaindazoles as btk kinase modulators and use thereof
SMT201700581T1 (it) 2009-12-21 2018-01-11 Samumed Llc 1h-pirazolo[3,4-b]piridine e loro usi terapeutici
PL2605652T3 (pl) 2010-08-18 2018-04-30 Samumed, Llc Diketony i hydroksyketony jako aktywatory szlaku sygnalizacji kateninowej
CA2834049C (en) 2011-04-25 2018-05-22 Usher Iii Initiative, Inc. Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome
US8673269B2 (en) 2011-07-14 2014-03-18 Keith R. Latham 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
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
NZ629282A (en) 2012-05-04 2017-04-28 Samumed Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
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
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
CA2897400A1 (en) 2013-01-08 2014-07-17 Samumed, Llc 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof
PE20151721A1 (es) 2013-02-22 2015-12-07 Samumed Llc Y-dicetonas como activadores de la ruta de senalizacion de wnt/b-catenina
WO2015155738A2 (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
KR102165385B1 (ko) 2014-08-20 2020-10-15 사뮤메드, 엘엘씨 피부 노화 및 주름의 치료 및 예방을 위한 감마-디케톤
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
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
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
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
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
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
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
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
US10383861B2 (en) 2015-08-03 2019-08-20 Sammumed, LLC 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1H-pyrazolo[3,4-C]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
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
WO2017024021A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof
WO2017024026A1 (en) 2015-08-03 2017-02-09 Samumed, Llc 3-(1h-indol-2-yl)-1h-pyrazolo[3,4-c]pyridines 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
US10604512B2 (en) 2015-08-03 2020-03-31 Samumed, Llc 3-(1H-indol-2-yl)-1H-indazoles 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
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
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
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
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
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
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
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
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
CN109311956A (zh) 2015-08-25 2019-02-05 伊斯迪德股份公司 诱导组织形成的化合物及其应用
CN109311957A (zh) * 2015-08-25 2019-02-05 伊斯迪德股份公司 诱导组织形成的化合物及其应用
WO2017032857A2 (en) * 2015-08-25 2017-03-02 Histide Ag Compounds for inducing tissue formation and uses thereof
JP6982748B2 (ja) 2015-11-06 2021-12-17 バイオスプライス セラピューティクス インコーポレイテッド ２−（１Ｈ−インダゾール−３−イル）−３Ｈ−イミダゾ［４，５−ｃ］ピリジンおよびそれらの抗炎症的使用
SI3464285T1 (sl) 2016-06-01 2023-02-28 Biosplice Therapeutics, Inc. Postopek za pripravo N-(5-(3-(7-(3-fluorofenil)-3H-imidazo(4,5-C)piridin-2-il)-1H-indazol-5- il)piridin-3-il)-3-metilbutanamida
KR102593742B1 (ko) 2016-10-21 2023-10-24 사뮤메드, 엘엘씨 인다졸-3-카복사마이드를 사용하는 방법 및 wnt/b-카테닌 신호전달 경로 억제제로서의 그들의 용도
JP7630905B2 (ja) 2016-11-07 2025-02-18 バイオスプライス セラピューティクス インコーポレイテッド 単回用量の調整済み注射用製剤
EP3628044B1 (en) * 2017-05-15 2023-11-22 The Regents of The University of Michigan Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors

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
JP3784076B2 (ja) 1997-02-07 2006-06-07 プリンストン ユニヴァーシティ 変性ヌクレオチド三燐酸基質を利用できる組み換えタンパクキナーゼ
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
JP4533534B2 (ja) 1998-06-19 2010-09-01 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 グリコーゲンシンターゼキナーゼ３のインヒビター
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2000036096A1 (en) * 1998-12-16 2000-06-22 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
WO2002024694A1 (en) * 2000-09-22 2002-03-28 Smithkline Beecham, P.L.C. Pyrazolopyridines and pyrazolopyridazines as antidiabetics
AU2002222274A1 (en) * 2000-12-18 2002-07-01 Smithkline Beecham Plc Crystal structure of glycogen synthase kinase 3 beta
WO2003068932A2 (en) * 2002-02-11 2003-08-21 Chiron Corporation 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
EP2082743A3 (en) 2010-03-03
US7666647B2 (en) 2010-02-23
US8318467B2 (en) 2012-11-27
DE60232669D1 (de) 2009-07-30
ATE433751T1 (de) 2009-07-15
EP1435957A4 (en) 2005-04-13
WO2002088078A3 (en) 2004-05-06
US20080262205A1 (en) 2008-10-23
US7390808B2 (en) 2008-06-24
WO2002088078A2 (en) 2002-11-07
JP2010059162A (ja) 2010-03-18
MXPA03009957A (es) 2005-07-25
EP1435957A2 (en) 2004-07-14
CA2444882A1 (en) 2002-11-07
US20030125332A1 (en) 2003-07-03
US7883881B2 (en) 2011-02-08
EP2295550A2 (en) 2011-03-16
US20110129896A1 (en) 2011-06-02
JP2005504731A (ja) 2005-02-17
US20100227814A1 (en) 2010-09-09
EP2082743A2 (en) 2009-07-29
EP2295550A3 (en) 2011-12-14
EP1435957B1 (en) 2009-06-17

Similar Documents

Publication Publication Date Title
AU2002259071A1 (en) Inhibitors of gsk-3 and crystal structures of gsk-3beta protein and protein complexes
WO2003092607A3 (en) Crystal structure of aurora-2 protein and binding pockets thereof
BG104819A (en) Substituted indolealkanoic acids
WO2003060071A3 (en) Albumin fusion proteins
ATE446313T1 (de) Muteine von tränen-lipocalin
WO2005077042A3 (en) Albumin fusion proteins
WO2003057144A3 (en) Change inhibitors of dipeptidyl peptidase iv
WO2001079444A3 (en) Albumin fusion proteins
WO2003085093A3 (en) Antibodies that specifically bind to gmad
DE60027409D1 (de) Glykosylierte leptinzusammensetzungen und zugehörige verfahren
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
AP2001002377A0 (en) Substituted phenoxyacetic acids.
WO2004035604A3 (en) Spleen tyrosine kinase catalytic domain:crystal structure and binding pockets thereof
WO2000069901A3 (en) Proteins with insulin-like activity useful in the treatment of diabetes
WO2005056785A3 (en) Crystal structure of interleukin-2 tyrosine kinase (itk) and binding pockets thereof
WO2005000205A3 (en) Methods and compositions for modulating serum cortisol levels
DE602004019500D1 (en) 4-substituirte-5-cyano-1h-pyrimidin-6-(th)iones als als gsk-3-hemmer
WO2002097046A3 (en) B7 related protein-2 molecules and uses thereof
WO2004023270A8 (en) Crystal structure of angiotensin-converting enzyme-related carboxypeptidase
WO2003094851A3 (en) 1,1- and 1,2-bisphosphonates as apoliprotein e modulators
WO2007146436A3 (en) Crystal structure of polo-like kinase 3 (plk3) and binding pockets thereof
WO2002072632A3 (en) Nucleic acids of the human abcc11 gene, vectors containing such nucleic acids and uses thereof.
WO2006091673A3 (en) Crystal structure of tak1-tab1
WO2003086301A3 (en) Antibodies that specifically bind to tr2

Legal Events

Date Code Title Description
MK6 Application lapsed section 142(2)(f)/reg. 8.3(3) - pct applic. not entering national phase