JP5570223B2 - タンパク質チロシンホスファターゼ1b(ptp−1b)阻害剤としての縮合芳香族ジフルオロメタンホスホネート - Google Patents

タンパク質チロシンホスファターゼ1b(ptp−1b)阻害剤としての縮合芳香族ジフルオロメタンホスホネート Download PDF

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JP5570223B2
JP5570223B2 JP2009546627A JP2009546627A JP5570223B2 JP 5570223 B2 JP5570223 B2 JP 5570223B2 JP 2009546627 A JP2009546627 A JP 2009546627A JP 2009546627 A JP2009546627 A JP 2009546627A JP 5570223 B2 JP5570223 B2 JP 5570223B2
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pharmaceutically acceptable
compound
inhibitor
acceptable salt
agonist
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JP2010516715A (ja
JP2010516715A5 (enExample
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コルッチ,ジョン
ウィルソン,マリー−クレール
ハン,ヨンシン
ドゥフレスヌ,クロード
ベレイ,ミシェル
ラウ,チェク,ケイ
ベイリー,クリストファー
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カネック ファーマ インコーポレイテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/60Quinoline or hydrogenated quinoline ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/12Antidiuretics, e.g. drugs for diabetes insipidus
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808Acyclic saturated acids which can have further substituents on alkyl
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3834Aromatic acids (P-C aromatic linkage)
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2009546627A 2007-01-26 2008-01-24 タンパク質チロシンホスファターゼ1b(ptp−1b)阻害剤としての縮合芳香族ジフルオロメタンホスホネート Expired - Fee Related JP5570223B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US89770007P 2007-01-26 2007-01-26
US60/897,700 2007-01-26
PCT/CA2008/000172 WO2008089581A1 (en) 2007-01-26 2008-01-24 Fused aromatic ptp-1b inhibitors

Publications (3)

Publication Number Publication Date
JP2010516715A JP2010516715A (ja) 2010-05-20
JP2010516715A5 JP2010516715A5 (enExample) 2011-02-03
JP5570223B2 true JP5570223B2 (ja) 2014-08-13

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JP2009546627A Expired - Fee Related JP5570223B2 (ja) 2007-01-26 2008-01-24 タンパク質チロシンホスファターゼ1b(ptp−1b)阻害剤としての縮合芳香族ジフルオロメタンホスホネート

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Country Link
US (4) US8168815B2 (enExample)
EP (1) EP2114971B1 (enExample)
JP (1) JP5570223B2 (enExample)
KR (1) KR101568799B1 (enExample)
CN (1) CN102317296B (enExample)
AU (1) AU2008209296B2 (enExample)
BR (1) BRPI0806789B8 (enExample)
CA (1) CA2675142C (enExample)
DK (1) DK2114971T3 (enExample)
ES (1) ES2547386T3 (enExample)
IL (1) IL199742A (enExample)
MX (1) MX2009007911A (enExample)
NZ (2) NZ600947A (enExample)
RU (1) RU2462469C2 (enExample)
WO (1) WO2008089581A1 (enExample)
ZA (1) ZA200904679B (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008089581A1 (en) * 2007-01-26 2008-07-31 Merck Frosst Canada Ltd. Fused aromatic ptp-1b inhibitors
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
CA2870488A1 (en) * 2012-04-16 2013-10-24 Kaneq Pharma Inc. Fused aromatic phosphonate derivatives as precursors to ptp-1b inhibitors
WO2014141110A2 (en) * 2013-03-14 2014-09-18 Curadev Pharma Pvt. Ltd. Aminonitriles as kynurenine pathway inhibitors
WO2015127548A1 (en) 2014-02-28 2015-09-03 The Royal Institution For The Advancement Of Learning / Mcgill University Tc-ptp inhibitors as apc activators for immunotherapy
CN108159069A (zh) * 2018-01-26 2018-06-15 广东省微生物研究所(广东省微生物分析检测中心) 灰树花多糖f2在制备治疗高脂血症药物、预防或延缓动脉粥样硬化药物中的应用
WO2023220833A1 (en) * 2022-05-19 2023-11-23 Kanyr Pharma Inc. Combined inhibition of tyrosine phosphatases tcptp and ptp1b and pd-1 blockage immunotherapy in the treatment of cancer
WO2024123585A1 (en) * 2022-12-05 2024-06-13 Merck Sharp & Dohme Llc Substituted quinazoline derivatives and methods of use thereof

Family Cites Families (12)

* Cited by examiner, † Cited by third party
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FI83421C (fi) * 1989-06-21 1991-07-10 Huhtamaeki Oy Foerfarande foer framstaellning av farmakologiskt anvaendbara metylenbisfosfonsyraderivat.
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
US6174874B1 (en) * 1998-09-21 2001-01-16 Merck Frosst Canada & Co. Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)
JP2003518130A (ja) * 1999-12-22 2003-06-03 メルク フロスト カナダ アンド カンパニー 蛋白チロシンホスファターゼ1b(ptp−1b)阻害薬としてのホスホン酸誘導体
CA2402414A1 (en) * 2000-03-22 2001-09-27 Christopher Bayly Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
CA2495943C (en) 2002-08-29 2009-07-21 Merck & Co., Inc. Indoles having anti-diabetic activity
UA84050C2 (en) * 2004-01-30 2008-09-10 Медивир Аб Hcv ns-3-serine protease inhibitors
JP4922924B2 (ja) 2004-04-13 2012-04-25 メルク・シャープ・エンド・ドーム・コーポレイション Cetp阻害薬
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
WO2006055525A2 (en) 2004-11-15 2006-05-26 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof
WO2008089581A1 (en) * 2007-01-26 2008-07-31 Merck Frosst Canada Ltd. Fused aromatic ptp-1b inhibitors

Also Published As

Publication number Publication date
NZ600947A (en) 2012-12-21
AU2008209296B2 (en) 2012-12-20
JP2010516715A (ja) 2010-05-20
CN102317296B (zh) 2015-05-27
HK1165806A1 (en) 2012-10-12
US8481742B2 (en) 2013-07-09
CN102317296A (zh) 2012-01-11
US20120178679A1 (en) 2012-07-12
US8927526B2 (en) 2015-01-06
WO2008089581A1 (en) 2008-07-31
EP2114971B1 (en) 2015-06-17
RU2462469C2 (ru) 2012-09-27
DK2114971T3 (en) 2015-08-31
ZA200904679B (en) 2010-04-28
EP2114971A4 (en) 2011-07-06
EP2114971A1 (en) 2009-11-11
RU2009132092A (ru) 2011-03-10
AU2008209296A1 (en) 2008-07-31
BRPI0806789B1 (pt) 2020-01-28
CA2675142C (en) 2014-08-19
IL199742A (en) 2014-03-31
BRPI0806789A2 (pt) 2011-09-13
IL199742A0 (en) 2010-04-15
KR101568799B1 (ko) 2015-11-12
US20150045325A1 (en) 2015-02-12
US20130281365A1 (en) 2013-10-24
US9334295B2 (en) 2016-05-10
KR20090108102A (ko) 2009-10-14
MX2009007911A (es) 2009-07-31
NZ578296A (en) 2012-07-27
US8168815B2 (en) 2012-05-01
CA2675142A1 (en) 2008-07-31
ES2547386T3 (es) 2015-10-05
BRPI0806789B8 (pt) 2021-05-25
US20100022477A1 (en) 2010-01-28

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