AU2003300447B2 - Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders - Google Patents

Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders Download PDF

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Publication number
AU2003300447B2
AU2003300447B2 AU2003300447A AU2003300447A AU2003300447B2 AU 2003300447 B2 AU2003300447 B2 AU 2003300447B2 AU 2003300447 A AU2003300447 A AU 2003300447A AU 2003300447 A AU2003300447 A AU 2003300447A AU 2003300447 B2 AU2003300447 B2 AU 2003300447B2
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disease
autoimmune
compounds
compound
protein
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AU2003300447A1 (en
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James F. Blake
Gregory F. Miknis
Jeffrey O. Saunders
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/101,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2003300447A 2002-12-30 2003-12-30 Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders Ceased AU2003300447B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2009243502A AU2009243502A1 (en) 2002-12-30 2009-12-03 Sulfhydantoins as Phosphate Isosteres for use as Phosphatase Inhibitors in the Treatment of Cancer and Autoimmune Disorders

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43757202P 2002-12-30 2002-12-30
US60/437,572 2002-12-30
PCT/US2003/041630 WO2004062664A1 (en) 2002-12-30 2003-12-30 Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders

Related Child Applications (1)

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AU2009243502A Division AU2009243502A1 (en) 2002-12-30 2009-12-03 Sulfhydantoins as Phosphate Isosteres for use as Phosphatase Inhibitors in the Treatment of Cancer and Autoimmune Disorders

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AU2003300447A1 AU2003300447A1 (en) 2004-08-10
AU2003300447B2 true AU2003300447B2 (en) 2009-09-03

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AU2003300447A Ceased AU2003300447B2 (en) 2002-12-30 2003-12-30 Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders
AU2009243502A Abandoned AU2009243502A1 (en) 2002-12-30 2009-12-03 Sulfhydantoins as Phosphate Isosteres for use as Phosphatase Inhibitors in the Treatment of Cancer and Autoimmune Disorders

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AU2009243502A Abandoned AU2009243502A1 (en) 2002-12-30 2009-12-03 Sulfhydantoins as Phosphate Isosteres for use as Phosphatase Inhibitors in the Treatment of Cancer and Autoimmune Disorders

Country Status (8)

Country Link
US (1) US7432292B2 (enExample)
EP (1) EP1594497B1 (enExample)
JP (1) JP4611751B2 (enExample)
AT (1) ATE432074T1 (enExample)
AU (2) AU2003300447B2 (enExample)
CA (1) CA2511818A1 (enExample)
DE (1) DE60327811D1 (enExample)
WO (1) WO2004062664A1 (enExample)

Families Citing this family (21)

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CA2463724A1 (en) * 2001-10-16 2003-04-24 Structural Bioinformatics Inc. Organosulfur inhibitors of tyrosine phosphatases
JP2006518738A (ja) * 2003-02-12 2006-08-17 トランス テック ファーマ,インコーポレイテッド 治療薬としての置換アゾール誘導体
WO2005035551A2 (en) 2003-10-08 2005-04-21 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
CA2551909C (en) * 2004-02-12 2011-10-11 Transtech Pharma, Inc. Substituted azole derivatives, compositions, and methods of use
US20060135773A1 (en) * 2004-06-17 2006-06-22 Semple Joseph E Trisubstituted nitrogen modulators of tyrosine phosphatases
JP2008505916A (ja) * 2004-07-09 2008-02-28 メタバシス・セラピューティクス・インコーポレイテッド チロシンホスファターゼの酸素/窒素複素環阻害剤
EP1841749A1 (en) * 2004-09-02 2007-10-10 Metabasis Therapeutics, Inc. Derivatives of thiazole and thiadiazole inhibitors of tyrosine phosphatases
EP1728790A1 (en) 2005-06-01 2006-12-06 Max-Delbrück-Centrum Für Molekulare Medizin Shp-2 inhibitors, pharmaceutical compositions comprising them and their use for treating phosphatase-mediated diseases
CA2630448A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,1,3-trioxo-1,2,5-thiadiazolidines and their use as ptp-ases inhibitors
WO2007067613A1 (en) * 2005-12-08 2007-06-14 Novartis Ag 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase)
UA94724C2 (en) * 2005-12-08 2011-06-10 Новартис Аг Thiadiazolidinone derivatives as antidiabetic agents
UA94921C2 (en) * 2005-12-08 2011-06-25 Новартис Аг 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors
US7723369B2 (en) * 2006-01-30 2010-05-25 Transtech Pharma, Inc. Substituted imidazole derivatives, compositions, and methods of use as PTPase inhibitors
BRPI0710182A2 (pt) * 2006-03-31 2012-08-07 Novartis Ag compostos orgÂnicos.
US9174969B2 (en) 2008-07-21 2015-11-03 University Of South Florida Indoline scaffold SHP-2 inhibitors and cancer treatment method
WO2011120902A1 (en) * 2010-03-29 2011-10-06 Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute For Biomedical Research Protein tyrosine phosphatase, non-receptor type 11 (ptpn11) and tumor initiating cells
WO2012041524A1 (en) 2010-10-01 2012-04-05 Max-Delbrück-Centrum Für Molekulare Medizin (Mdc) Hydrazonopyrazolones as protein tyrosine phosphatase inhibitors
EP2717911A1 (en) * 2011-06-06 2014-04-16 Novartis Forschungsstiftung, Zweigniederlassung Protein tyrosine phosphatase, non-receptor type 11 (ptpn11) and triple-negative breast cancer
CN103087166B (zh) * 2011-10-31 2014-03-05 中国科学院微生物研究所 一种钾氢泵蛋白及其编码基因和它们的应用
US9844535B2 (en) 2013-07-03 2017-12-19 Indiana University Research And Technology Corporation SHP2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors
AU2019290197B2 (en) * 2018-06-21 2023-08-24 Abbvie Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof

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US5512576A (en) * 1994-12-02 1996-04-30 Sterling Winthrop Inc. 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5541168A (en) * 1994-12-02 1996-07-30 Sterling Winthrop Inc. Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5550139A (en) * 1994-01-03 1996-08-27 The Wichita State University Serine protease inhibitors
US5556909A (en) * 1994-12-02 1996-09-17 Sanofi Winthrop Inc. Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives and compositions and method of use thereof
US5750546A (en) * 1994-12-02 1998-05-12 Sanofi Winthrop, Inc. 2-(2, 3, 5, 6-tetrafluoro-4-pyridyl)-1, 2, 5-thiadiazolidin-3-one 1, 1-dioxides and compositions and method of use thereof
AU2003224030A1 (en) * 2002-04-03 2003-10-13 Novartis Ag 5-substituted 1,1-dioxo-`1,2,5!thiazolidine-3-one derivatives as PTPase 1B inhibitors

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US5550139A (en) * 1994-01-03 1996-08-27 The Wichita State University Serine protease inhibitors
US5494925A (en) * 1994-12-02 1996-02-27 Sterling Winthrop Inc. 2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5512576A (en) * 1994-12-02 1996-04-30 Sterling Winthrop Inc. 2-substituted 1,2,5,-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5541168A (en) * 1994-12-02 1996-07-30 Sterling Winthrop Inc. Substituted 2-(phosphinyloxymethyl)-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
US5556909A (en) * 1994-12-02 1996-09-17 Sanofi Winthrop Inc. Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives and compositions and method of use thereof
US5750546A (en) * 1994-12-02 1998-05-12 Sanofi Winthrop, Inc. 2-(2, 3, 5, 6-tetrafluoro-4-pyridyl)-1, 2, 5-thiadiazolidin-3-one 1, 1-dioxides and compositions and method of use thereof
AU2003224030A1 (en) * 2002-04-03 2003-10-13 Novartis Ag 5-substituted 1,1-dioxo-`1,2,5!thiazolidine-3-one derivatives as PTPase 1B inhibitors

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Also Published As

Publication number Publication date
ATE432074T1 (de) 2009-06-15
EP1594497A1 (en) 2005-11-16
DE60327811D1 (de) 2009-07-09
US7432292B2 (en) 2008-10-07
JP4611751B2 (ja) 2011-01-12
US20040167187A1 (en) 2004-08-26
EP1594497B1 (en) 2009-05-27
CA2511818A1 (en) 2004-07-29
AU2003300447A1 (en) 2004-08-10
JP2006514960A (ja) 2006-05-18
AU2009243502A1 (en) 2009-12-24
WO2004062664A1 (en) 2004-07-29

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