AU2003215087B2 - Heteroaryl compounds useful as inhibitors of GSK-3 - Google Patents

Heteroaryl compounds useful as inhibitors of GSK-3 Download PDF

Info

Publication number
AU2003215087B2
AU2003215087B2 AU2003215087A AU2003215087A AU2003215087B2 AU 2003215087 B2 AU2003215087 B2 AU 2003215087B2 AU 2003215087 A AU2003215087 A AU 2003215087A AU 2003215087 A AU2003215087 A AU 2003215087A AU 2003215087 B2 AU2003215087 B2 AU 2003215087B2
Authority
AU
Australia
Prior art keywords
benzoimidazol
furazan
ring
nitrogen
disease
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.)
Ceased
Application number
AU2003215087A
Other languages
English (en)
Other versions
AU2003215087A1 (en
Inventor
Michael J Arnost
Jeremy Green
Scott L Harbeson
Vladimir Savic
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 AU2003215087A1 publication Critical patent/AU2003215087A1/en
Application granted granted Critical
Publication of AU2003215087B2 publication Critical patent/AU2003215087B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
AU2003215087A 2002-02-06 2003-02-06 Heteroaryl compounds useful as inhibitors of GSK-3 Ceased AU2003215087B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US35484302P 2002-02-06 2002-02-06
US60/354,843 2002-02-06
PCT/US2003/003655 WO2003066629A2 (en) 2002-02-06 2003-02-06 Heteroaryl compounds useful as inhibitors of gsk-3

Publications (2)

Publication Number Publication Date
AU2003215087A1 AU2003215087A1 (en) 2003-09-02
AU2003215087B2 true AU2003215087B2 (en) 2009-07-16

Family

ID=27734431

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003215087A Ceased AU2003215087B2 (en) 2002-02-06 2003-02-06 Heteroaryl compounds useful as inhibitors of GSK-3

Country Status (13)

Country Link
US (2) US20040034037A1 (OSRAM)
EP (2) EP1472245A2 (OSRAM)
JP (2) JP4656838B2 (OSRAM)
KR (1) KR20040084896A (OSRAM)
AU (1) AU2003215087B2 (OSRAM)
CA (1) CA2475633C (OSRAM)
ES (1) ES2437391T3 (OSRAM)
MX (1) MXPA04007697A (OSRAM)
NO (1) NO20043726L (OSRAM)
PL (1) PL372198A1 (OSRAM)
RU (1) RU2004126671A (OSRAM)
SG (1) SG159380A1 (OSRAM)
WO (1) WO2003066629A2 (OSRAM)

Families Citing this family (117)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE346064T1 (de) * 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
GB0206861D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Medicaments
GB0206860D0 (en) * 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
US20040002524A1 (en) * 2002-06-24 2004-01-01 Richard Chesworth Benzimidazole compounds and their use as estrogen agonists/antagonists
AU2003290346A1 (en) * 2002-12-24 2004-07-22 Biofocus Plc Compound libraries of 2,3-substituted pyrazine derivatives capable of binding to g-protein coupled receptors
JP2006516626A (ja) * 2003-01-28 2006-07-06 スミスクライン ビーチャム コーポレーション 化学的化合物
JP2006520794A (ja) * 2003-03-21 2006-09-14 スミスクライン ビーチャム コーポレーション 化合物
PL1636215T3 (pl) * 2003-05-23 2008-09-30 Basilea Pharmaceutica Ag Furazanobenzymidazole
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
TW200523262A (en) * 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
WO2005019190A2 (en) 2003-08-20 2005-03-03 Vertex Pharmaceuticals Incorporated (4 -amino -1,2, 5-oxadiazol-4-yl) -hetξroaromatic compounds useful as protein kinase inhibitors
US20070004771A1 (en) * 2003-10-06 2007-01-04 Glaxo Group Limited Preparation of 1,6,7-trisubstituted azabenzimidazoles as kinase inhibitors
DE102004010194A1 (de) 2004-03-02 2005-10-13 Aventis Pharma Deutschland Gmbh 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate, ihre Herstellung und Verwendung in Arzneimitteln
DE102004010207A1 (de) 2004-03-02 2005-09-15 Aventis Pharma S.A. Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
CA2573185A1 (en) 2004-07-14 2006-02-23 Ptc Therapeutics, Inc. Methods for treating hepatitis c
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7645881B2 (en) 2004-07-22 2010-01-12 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7674907B2 (en) * 2004-07-23 2010-03-09 Amgen Inc. Furanopyridine derivatives and methods of use
US8771754B2 (en) * 2004-09-17 2014-07-08 Vanderbilt University Use of GSK3 inhibitors in combination with radiation therapies
GB0422057D0 (en) * 2004-10-05 2004-11-03 Astrazeneca Ab Novel compounds
US20060204980A1 (en) * 2004-12-28 2006-09-14 Altieri Dario C Colorectal cancer therapies
US20080312223A1 (en) 2004-12-30 2008-12-18 Astex Therapeutics Limited Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases
US8110573B2 (en) 2004-12-30 2012-02-07 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases
AU2006218404A1 (en) * 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-phenyl benzamide derivatives as sirtuin modulators
RU2453540C2 (ru) 2005-04-21 2012-06-20 Лаборатуар Сероно С.А. 2,3-замещенные пиразинсульфонамиды в качестве ингибиторов crth2
CA2609980C (en) 2005-05-27 2015-10-13 Queen's University At Kingston Treatment of protein folding disorders
DE102005025225A1 (de) * 2005-06-01 2006-12-07 Sanofi-Aventis Deutschland Gmbh Verfahren zur Herstellung von 2-(2-Amino-pyrimidin-4-yl)-1H-indol-5-carbonsäure-derivaten
ES2431050T3 (es) * 2005-08-04 2013-11-22 Sirtris Pharmaceuticals, Inc. Benzotiazoles y tiazolopiridinas como moduladores de la sirtuína
US7855289B2 (en) * 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8093401B2 (en) * 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
AR055669A1 (es) * 2005-10-03 2007-08-29 Astrazeneca Ab Derivados de 3h - imidazo[4, 5 -b]piridina como inhibidores selectivos de gsk3, metodos e internediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la elaboracion de un medicamento para el tratamiento de enfermedades neurodegenerativas y mentales.
AR057525A1 (es) * 2005-10-03 2007-12-05 Astrazeneca Ab Compuestos inhibidores selectivos de gsk3 y un proceso para su preparacion
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
JP5474354B2 (ja) 2005-12-30 2014-04-16 アステックス、セラピューティックス、リミテッド 医薬化合物
US20090170812A1 (en) * 2006-06-23 2009-07-02 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
MX2008015923A (es) * 2006-06-29 2009-01-13 Hoffmann La Roche Derivados de bencimidazol, metodo para su produccion, su uso como agonistas fxr y preparaciones farmaceuticas que los contienen.
US20080249081A1 (en) * 2006-10-24 2008-10-09 Roger Olsson Compounds for the treatment of pain and screening methods therefor
EP2081892A4 (en) * 2006-11-17 2014-03-05 Donald F Weaver COMPOUNDS AND METHOD FOR THE TREATMENT OF PROTEIN DISAPPEARANCE
SG144809A1 (en) * 2007-01-11 2008-08-28 Millipore U K Ltd Benzimidazole compounds and their use as chromatographic ligands
UY30892A1 (es) * 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
CL2008001822A1 (es) * 2007-06-20 2009-03-13 Sirtris Pharmaceuticals Inc Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras.
GB0713259D0 (en) * 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
WO2009024825A1 (en) * 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
BRPI0815696A2 (pt) 2007-08-27 2016-06-21 Hoffmann La Roche composto derivados de benzimidazol, processo para a sua manufatura, composições farmacêuticas que os compreendem, metódo para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por agonistas de fxr e uso destes compostos.
MX2010004491A (es) 2007-10-25 2010-06-21 Astrazeneca Ab Derivados de piridina y pirazina utiles en el tratamiento de trastornos proliferativos celulares.
WO2009058348A1 (en) * 2007-11-01 2009-05-07 Sirtris Pharmaceuticals, Inc. Amide derivatives as sirtuin modulators
WO2009061453A1 (en) * 2007-11-08 2009-05-14 Sirtris Pharmaceuticals, Inc. Solubilized thiazolopyridines
AU2008323017B2 (en) 2007-11-15 2012-12-20 F. Hoffmann-La Roche Ag Methyl-benzimidazole derivatives
US7816540B2 (en) * 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
KR20110040958A (ko) * 2008-07-30 2011-04-20 온코세라피 사이언스 가부시키가이샤 벤조이미다졸 유도체 및 이를 유효성분으로 함유하는 글라이코겐 합성 카이네이즈-3 베타 저해제
KR20170015566A (ko) 2008-11-10 2017-02-08 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
BRPI0922435A2 (pt) 2008-12-19 2018-09-11 Sirtris Pharmaceuticals Inc "composto de tiazolopiridina moduladores de sirtuina, composição farmacêutica compreendendo o mesmo e seu uso."
EP2376485B1 (en) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
UA106740C2 (uk) * 2009-01-30 2014-10-10 Глаксосмітклайн Ллс Кристалічний гідрохлорид n-{(1s)-2-аміно-1-[(3-фторфеніл)метил]етил}-5-хлор-4-(4-хлор-1-метил-1h-піразол-5-іл)-2-тіофенкарбоксаміду
EP2251010A1 (en) * 2009-05-08 2010-11-17 Sygnis Bioscience GmbH & Co. KG Use of thiabendazole and derivatives thereof for the therapy of neurological conditions
EP2430016B1 (en) * 2009-05-13 2020-04-01 University Of Virginia Patent Foundation Inhibitors of inv(16) leukemia
DE102009033208A1 (de) * 2009-07-15 2011-01-20 Merck Patent Gmbh Aminopyridinderivate
PL2459553T3 (pl) * 2009-07-27 2015-03-31 Basilea Pharmaceutica Ag Furazanobenzimidazole jako proleki do leczenia chorób nowotworowych lub autoimmunizacyjnych
WO2011022721A1 (en) * 2009-08-21 2011-02-24 Microbiotix, Inc Inhibitors of botulinum neurotoxins
AU2010314891A1 (en) 2009-11-06 2012-06-07 Vanderbilt University Aryl and heteroaryl sulfones as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
AU2011253021A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of ATR kinase
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 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 Ａｔｒキナーゼ阻害剤として有用な化合物
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 키나제의 억제제로서 유용한 화합물
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
JP2014510151A (ja) 2011-04-05 2014-04-24 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 Ａｔｒキナーゼ（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2723746A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) 2011-06-22 2014-09-08 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 Ａｔｒキナーゼ阻害剤として有用な化合物
EP2554662A1 (en) 2011-08-05 2013-02-06 M Maria Pia Cosma Methods of treatment of retinal degeneration diseases
EP2757884B1 (en) 2011-09-22 2022-07-27 Merck Sharp & Dohme LLC Pyrazolopyridyl compounds as aldosterone synthase inhibitors
EP2757882B1 (en) 2011-09-22 2020-11-04 Merck Sharp & Dohme Corp. Imidazopyridyl compounds as aldosterone synthase inhibitors
WO2013043520A1 (en) 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Triazolopyridyl compounds as aldosterone synthase inhibitors
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
KR102056586B1 (ko) 2011-09-30 2019-12-18 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 억제제를 이용한 췌장암 및 비소세포 폐암의 치료
BR112014007721B1 (pt) 2011-09-30 2022-11-01 Vertex Pharmaceuticals Incorporated Processos para preparar compostos úteis como inibidores de atr quinase
EP2751099B1 (en) 2011-09-30 2017-06-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2015515478A (ja) 2012-04-05 2015-05-28 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な化合物及びそれらの併用療法
RS61664B1 (sr) 2012-04-24 2021-04-29 Vertex Pharma Inhibitori dna-pk
US8999632B2 (en) 2012-10-04 2015-04-07 Vertex Pharmaceuticals Incorporated Method for measuring ATR inhibition mediated increases in DNA damage
JP6496246B2 (ja) 2012-10-05 2019-04-03 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． アルドステロンシンターゼインヒビター関連用途としてのインドリン化合物
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2015004803A (es) 2012-10-26 2015-08-14 Hoffmann La Roche Inhibidores de 1h-pirazol 3,4-disubstituida y tiazol 4,5-disubstituida de syk.
BR112015012454B1 (pt) 2012-12-07 2022-07-05 Vertex Pharmaceuticals Incorporated Compostos inibidores de atr quinase, seu uso e composição farmacêutica compreendendo os mesmos
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
SI3424920T1 (sl) 2013-10-17 2020-08-31 Vertex Pharmaceuticals Incorporated Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk
ES2768678T3 (es) 2013-12-06 2020-06-23 Vertex Pharma Compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inhibidor de la ATR quinasa, su preparación, diferentes formas sólidas y derivados radiomarcados de las mismas
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP6615791B2 (ja) 2014-06-05 2019-12-04 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 殺虫剤としての二環式化合物
ES2777608T3 (es) 2014-06-05 2020-08-05 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
KR20170016498A (ko) 2014-06-17 2017-02-13 버텍스 파마슈티칼스 인코포레이티드 Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법
CN115925679A (zh) 2014-12-24 2023-04-07 株式会社Lg化学 作为gpr120激动剂的联芳基衍生物
KR102678021B1 (ko) 2015-09-30 2024-06-26 버텍스 파마슈티칼스 인코포레이티드 Dna 손상제와 병용되는, atr 저해제를 포함하는 암 치료용 약제학적 조성물
EP3231434A1 (en) 2016-04-14 2017-10-18 Fundacio Centre de Regulacio Genomica Method of treatment of parkinsonism
WO2017216706A1 (en) 2016-06-14 2017-12-21 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
KR20190062485A (ko) 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
MX388196B (es) 2017-04-26 2025-03-19 Basilea Pharm Int Ag Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos.
US11331313B2 (en) 2017-05-22 2022-05-17 Whitehead Institute For Biomedical Research KCC2 expression enhancing compounds and uses thereof
CN109265451B (zh) * 2018-10-09 2022-07-15 中国药科大学 丁酰胆碱酯酶选择性抑制剂及其制备方法与用途
AU2020218366A1 (en) 2019-02-08 2021-09-16 Frequency Therapeutics, Inc. Valproic acid compounds and Wnt agonists for treating ear disorders
CN111454254B (zh) * 2020-04-26 2023-06-02 云白药征武科技(上海)有限公司 一种具有含氟取代基的苯并咪唑衍生物的制备及其应用
CN111423429A (zh) * 2020-05-19 2020-07-17 江西科技师范大学 苯并咪唑联呋咱类系列化合物及其合成方法
CN112920178A (zh) * 2021-01-29 2021-06-08 中国药科大学 具有苯并咪唑结构的化合物及其制备方法与用途
KR20250135234A (ko) * 2023-01-20 2025-09-12 파이로테크 (베이징) 바이오테크놀로지 컴퍼니, 리미티드 신규한 alpk1 억제제

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0406734A2 (en) * 1989-07-03 1991-01-09 Hoechst-Roussel Pharmaceuticals Incorporated 2-(Aminoaryl)indoles and indolines, a process for their preparation and their use as medicaments
US6130333A (en) * 1998-11-27 2000-10-10 Monsanto Company Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use

Family Cites Families (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US3935183A (en) * 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) * 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) * 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
DOP1981004033A (es) * 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102194L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
JPS58124773A (ja) * 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc ５−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5496826A (en) * 1994-09-02 1996-03-05 Bristol-Myers Squibb Company Pharmaceutical methods of using heterocyclic derivatives of N-phenylamides
WO1996014843A2 (en) * 1994-11-10 1996-05-23 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
IL117659A (en) * 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
AU6966696A (en) * 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6267952B1 (en) * 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
WO1999041253A1 (en) * 1998-02-17 1999-08-19 Tularik Inc. Anti-viral pyrimidine derivatives
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
EP1105394A1 (en) * 1998-08-21 2001-06-13 Du Pont Pharmaceuticals Company ISOXAZOLO 4,5-d]PYRIMIDINES AS CRF ANTAGONISTS
US6184226B1 (en) * 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
DE19920936A1 (de) * 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
NZ516348A (en) * 1999-06-23 2003-06-30 Aventis Pharma Gmbh Substituted benzimidazole
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
BR0104424A (pt) * 2000-02-05 2002-01-08 Vertex Pharma Composições de pirazol úteis como inibidores de erk
US20030004174A9 (en) * 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
EP1136099A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-(Indolylalkylamino)pyrimidone derivatives as GSK3beta inhibitors
EP1299381B1 (en) * 2000-06-28 2008-05-07 AstraZeneca AB Substituted quinazoline derivatives and their use as inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6610677B2 (en) * 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE346064T1 (de) * 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE335737T1 (de) * 2000-09-15 2006-09-15 Vertex Pharma Isoxazole und ihre verwendung als erk-inhibitoren
US6716851B2 (en) * 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) * 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
EP1347972A1 (en) * 2000-12-19 2003-10-01 Smithkline Beecham Plc Pyrazolo 3,4-c]pyridines as gsk-3 inhibitors
ATE354573T1 (de) * 2000-12-21 2007-03-15 Vertex Pharma ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
EP1373257B9 (en) * 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
US6642227B2 (en) * 2001-04-13 2003-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
US20030096813A1 (en) * 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
EP2295550A3 (en) * 2001-04-30 2011-12-14 Vertex Pharmaceuticals Incorporated Crystal structures of GSK-3beta protein and protein complexes and their use
AU2002308748A1 (en) * 2001-05-16 2002-11-25 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
JP4342937B2 (ja) * 2001-07-03 2009-10-14 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 ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
EP1441725A1 (en) * 2001-10-26 2004-08-04 Aventis Pharmaceuticals Inc. Benzimidazoles and analogues and their use as protein kinases inhibitors
DE60236322D1 (de) * 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
US7091343B2 (en) * 2002-03-15 2006-08-15 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
DE60314603T2 (de) * 2002-03-15 2008-02-28 Vertex Pharmaceuticals Inc., Cambridge Zusammensetzungen brauchbar als protein-kinase-inhibitoren
EP1485381B8 (en) * 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
EP1485380B1 (en) * 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
WO2003091246A1 (en) * 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
US7361665B2 (en) * 2002-07-09 2008-04-22 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
PL1636215T3 (pl) * 2003-05-23 2008-09-30 Basilea Pharmaceutica Ag Furazanobenzymidazole

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0406734A2 (en) * 1989-07-03 1991-01-09 Hoechst-Roussel Pharmaceuticals Incorporated 2-(Aminoaryl)indoles and indolines, a process for their preparation and their use as medicaments
US6130333A (en) * 1998-11-27 2000-10-10 Monsanto Company Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
CAS registry number 293760-30-2 *
CAS registry number 309289-58-5 *
CAS registry number 328243-88-5 *
CAS registry number 328974-42-1 *
CAS registry number 332026-91-2 *
CAS registry number 333414-38-3 *
CAS registry number 339338-65-7 *
CAS registry number 384860-37-1 *

Also Published As

Publication number Publication date
NO20043726L (no) 2004-11-08
KR20040084896A (ko) 2004-10-06
SG159380A1 (en) 2010-03-30
AU2003215087A1 (en) 2003-09-02
WO2003066629A2 (en) 2003-08-14
WO2003066629A3 (en) 2003-10-30
CA2475633A1 (en) 2003-08-14
JP2010132697A (ja) 2010-06-17
JP2005526028A (ja) 2005-09-02
EP2322521A1 (en) 2011-05-18
PL372198A1 (en) 2005-07-11
US20040034037A1 (en) 2004-02-19
CA2475633C (en) 2013-04-02
EP1472245A2 (en) 2004-11-03
EP2322521B1 (en) 2013-09-04
JP4656838B2 (ja) 2011-03-23
US20070270420A1 (en) 2007-11-22
MXPA04007697A (es) 2004-11-10
ES2437391T3 (es) 2014-01-10
RU2004126671A (ru) 2005-04-10

Similar Documents

Publication Publication Date Title
AU2003215087B2 (en) Heteroaryl compounds useful as inhibitors of GSK-3
CA2513463C (en) Gyrase inhibitors and uses thereof
AU2002246754B2 (en) Pyrazole compounds useful as protein kinase inhibitors
JP4523271B2 (ja) プロテインキナーゼのインヒビターとして有用なチアゾール化合物
US10738041B2 (en) Ferroportin inhibitors
CA2577758C (en) Gyrase inhibitors and uses thereof
US8653088B2 (en) Compositions useful as inhibitors of protein kinases
AU2012240026A1 (en) Methods and compositions for treating neurodegenerative diseases
US20140066434A1 (en) Methods and Compositions for Treating Parkinson's Disease
AU2003245442A1 (en) 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase iv inhibitors for the treatment of bacterial infections
JP2005509592A (ja) プロテインキナーゼインヒビターとしての５−（２−アミノピリミジン−４−イル）ベンズイソキサゾール
HRP20010451A2 (en) 2-phenylbenzimidazoles and 2-phenylindoles, and production and use thereof
US9926318B2 (en) Tetracyclic autotaxin inhibitors
CN119219603A (zh) Sarm1酶活性抑制剂及其用途
US20110081316A1 (en) Pyrazole inhibitors of phosphatidylinositol 3-kinase
HK1065033B (en) Thiazole compounds useful as inhibitors of protein kinases
HK1087699B (en) Gyrase inhibitors and uses thereof

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
GM Mortgages registered

Name of requester: MACQUARIE US TRADING LLC

MK14 Patent ceased section 143(a) (annual fees not paid) or expired