RU2462469C2 - Конденсированные ароматические дифторметанфосфонаты в качестве ингибиторов протеинтирозинфосфатазы ib (ptp-1b) - Google Patents

Конденсированные ароматические дифторметанфосфонаты в качестве ингибиторов протеинтирозинфосфатазы ib (ptp-1b) Download PDF

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RU2462469C2
RU2462469C2 RU2009132092/04A RU2009132092A RU2462469C2 RU 2462469 C2 RU2462469 C2 RU 2462469C2 RU 2009132092/04 A RU2009132092/04 A RU 2009132092/04A RU 2009132092 A RU2009132092 A RU 2009132092A RU 2462469 C2 RU2462469 C2 RU 2462469C2
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bromo
methyl
compounds
pharmaceutically acceptable
difluoro
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RU2009132092/04A
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English (en)
Russian (ru)
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RU2009132092A (ru
Inventor
Джон КОЛУЧЧИ (CA)
Джон Колуччи
Мари-Клер УИЛСОН (CA)
Мари-Клер УИЛСОН
Юнсинь ХАНЬ (CA)
Юнсинь ХАНЬ
Клод ДЮФРЕН (CA)
Клод ДЮФРЕН
Мишель БЕЛЛЕЙ (CA)
Мишель Беллей
Чеук К. ЛАУ (CA)
Чеук К. ЛАУ
Кристофер БЭЙЛИ (CA)
Кристофер БЭЙЛИ
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Канек Фарма Инк.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576—Six-membered rings
    • C07F9/60—Quinoline or hydrogenated quinoline 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
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3834—Aromatic acids (P-C aromatic linkage)
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
RU2009132092/04A 2007-01-26 2008-01-24 Конденсированные ароматические дифторметанфосфонаты в качестве ингибиторов протеинтирозинфосфатазы ib (ptp-1b) RU2462469C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89770007P 2007-01-26 2007-01-26
US60/897,700 2007-01-26

Publications (2)

Publication Number Publication Date
RU2009132092A RU2009132092A (ru) 2011-03-10
RU2462469C2 true RU2462469C2 (ru) 2012-09-27

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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)

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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

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RU2074860C1 (ru) * 1989-06-21 1997-03-10 Лейрас Ой Производные метиленбисфосфоновой кислоты
WO2001070754A1 (en) * 2000-03-22 2001-09-27 Merck Frosst Canada & Co. Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
WO2006055525A2 (en) * 2004-11-15 2006-05-26 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof

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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
AU7705601A (en) 2000-07-25 2002-02-05 Merck & Co Inc N-substituted indoles useful in the treatment of diabetes
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RU2074860C1 (ru) * 1989-06-21 1997-03-10 Лейрас Ой Производные метиленбисфосфоновой кислоты
WO2001070754A1 (en) * 2000-03-22 2001-09-27 Merck Frosst Canada & Co. Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
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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
DK2114971T3 (en) 2015-08-31
ZA200904679B (en) 2010-04-28
EP2114971A4 (en) 2011-07-06
JP5570223B2 (ja) 2014-08-13
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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