ATE232873T1 - Phosphonsaürederivate als ptp-1b-inhibitoren - Google Patents

Phosphonsaürederivate als ptp-1b-inhibitoren

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Publication number
ATE232873T1
ATE232873T1 AT99944200T AT99944200T ATE232873T1 AT E232873 T1 ATE232873 T1 AT E232873T1 AT 99944200 T AT99944200 T AT 99944200T AT 99944200 T AT99944200 T AT 99944200T AT E232873 T1 ATE232873 T1 AT E232873T1
Authority
AT
Austria
Prior art keywords
ptp
inhibitors
acid derivatives
phosphonic acid
encompasses
Prior art date
Application number
AT99944200T
Other languages
English (en)
Inventor
Yves Leblanc
Claude Dufresne
Zhaoyin Wang
Chun Sing Li
Jacques Y Gauthier
Michel Therien
Cheuk K Lau
Patrick Roy
Original Assignee
Merck Frosst Canada 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 Merck Frosst Canada Inc filed Critical Merck Frosst Canada Inc
Application granted granted Critical
Publication of ATE232873T1 publication Critical patent/ATE232873T1/de

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    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
    • H04MTELEPHONIC COMMUNICATION
    • H04M3/00Automatic or semi-automatic exchanges
    • H04M3/42Systems providing special services or facilities to subscribers
    • H04M3/42314Systems providing special services or facilities to subscribers in private branch exchanges
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
    • C07F9/3839Polyphosphonic acids
    • C07F9/3856Polyphosphonic acids containing halogen or nitro(so) substituents
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    • 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
    • C07F9/3839Polyphosphonic acids
    • C07F9/386Polyphosphonic acids containing hydroxy substituents in the hydrocarbon radicals
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    • 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
    • C07F9/3839Polyphosphonic acids
    • C07F9/3865Polyphosphonic acids containing sulfur substituents
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    • 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
    • C07F9/3839Polyphosphonic acids
    • C07F9/3869Polyphosphonic acids containing carboxylic acid or carboxylic acid derivative substituents
    • CCHEMISTRY; METALLURGY
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    • 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
    • C07F9/3882Arylalkanephosphonic acids
    • CCHEMISTRY; METALLURGY
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    • 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
    • C07F9/5537Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom the heteroring containing the structure -C(=O)-N-C(=O)- (both carbon atoms belong to the heteroring)
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    • 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
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
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    • 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
    • C07F9/6515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6518Five-membered rings
    • C07F9/65188Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
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    • 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
    • C07F9/6524Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
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    • 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
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/653Five-membered rings
    • C07F9/65306Five-membered rings containing two nitrogen atoms
    • C07F9/65318Five-membered rings containing two nitrogen atoms having the two nitrogen atoms in positions 1 and 3
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    • 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
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/653Five-membered rings
    • C07F9/65324Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
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    • 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
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
    • CCHEMISTRY; METALLURGY
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    • 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
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
    • C07F9/65392Five-membered rings containing two nitrogen atoms
    • C07F9/65395Five-membered rings containing two nitrogen atoms having the two nitrogen atoms in positions 1 and 2
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    • 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
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
    • C07F9/6541Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
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    • H04Q3/58Arrangements providing connection between main exchange and sub-exchange or satellite
    • H04Q3/62Arrangements providing connection between main exchange and sub-exchange or satellite for connecting to private branch exchanges
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    • HELECTRICITY
    • H04ELECTRIC COMMUNICATION TECHNIQUE
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Signal Processing (AREA)
  • Astronomy & Astrophysics (AREA)
  • General Physics & Mathematics (AREA)
  • Computer Networks & Wireless Communication (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Ink Jet (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT99944200T 1998-09-21 1999-09-21 Phosphonsaürederivate als ptp-1b-inhibitoren ATE232873T1 (de)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US10116498P 1998-09-21 1998-09-21
US12742099P 1999-04-01 1999-04-01
US09/398,356 US6174874B1 (en) 1998-09-21 1999-09-17 Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)
PCT/CA1999/000864 WO2000017211A1 (en) 1998-09-21 1999-09-21 Phosphonic acids derivatives as inhibitors of ptp-1b

Publications (1)

Publication Number Publication Date
ATE232873T1 true ATE232873T1 (de) 2003-03-15

Family

ID=27379139

Family Applications (1)

Application Number Title Priority Date Filing Date
AT99944200T ATE232873T1 (de) 1998-09-21 1999-09-21 Phosphonsaürederivate als ptp-1b-inhibitoren

Country Status (9)

Country Link
US (1) US6174874B1 (de)
EP (1) EP1115729B1 (de)
JP (1) JP2002526505A (de)
AT (1) ATE232873T1 (de)
AU (1) AU761596B2 (de)
CA (1) CA2344927A1 (de)
DE (1) DE69905476T2 (de)
ES (1) ES2192396T3 (de)
WO (1) WO2000017211A1 (de)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2372116A1 (en) * 1999-05-14 2000-11-23 Claude Dufresne Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1b (ptp-1b)
US6777433B2 (en) 1999-12-22 2004-08-17 Merck Frosst Canada & Co. Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
EP1244678A1 (de) 1999-12-22 2002-10-02 Merck Frosst Canada Inc. Phosphonsäurederivate als inhibitoren der protein tyrosin phosphatase 1b (ptp-1b)
JP2003518129A (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 タンパク質チロシンホスファターゼ1b(ptp−1b)のインヒビターとなるホスホン酸誘導体
EP1242431A1 (de) * 1999-12-22 2002-09-25 Merck Frosst Canada & Co. Aromatische phosphonate als protein tyrosin phosphatase 1b (ptp-1b) inhibitoren
EP1244677A1 (de) 1999-12-22 2002-10-02 Merck Frosst Canada Inc. Phosphonsäurediarylerivate als inhibitoren der protein tyrosin phosphatase (ptp-1b)
JP2003528106A (ja) * 2000-03-22 2003-09-24 メルク フロスト カナダ アンド カンパニー Ptp−1b阻害薬としての硫黄置換アリールジフルオロメチルホスホン酸類
US7163932B2 (en) 2001-06-20 2007-01-16 Merck Frosst Canada & Co. Aryldifluoromethylphosphonic acids for treatment of diabetes
US20040191926A1 (en) * 2001-09-26 2004-09-30 Zhong-Yin Zhang Ptp1b inhibitors and ligands
EP1446110A2 (de) * 2001-10-16 2004-08-18 Structural Bioinformatics Inc. Organoschwefel-hemmer von tyrosinphosphatasen
AU2002349705A1 (en) 2001-12-03 2003-06-17 Japan Tobacco Inc. Azole compound and medicinal use thereof
KR20050009744A (ko) * 2002-06-11 2005-01-25 시바 스페셜티 케미칼스 홀딩 인크. 모노- 및 비스아실포스핀 옥사이드의 다량체 형태
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
CN1747936A (zh) * 2003-02-12 2006-03-15 特兰斯泰克制药公司 作为治疗试剂的取代吡咯衍生物
US7141596B2 (en) 2003-10-08 2006-11-28 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
NZ548208A (en) * 2004-02-12 2010-09-30 Transtech Pharma Inc Substituted azole derivatives, compositions, and methods of use
WO2005114197A2 (en) * 2004-04-15 2005-12-01 Albert Einstein College Of Medicine Of Yeshiva University Activity-based probes for protein tyrosine phosphatases
US20060135773A1 (en) * 2004-06-17 2006-06-22 Semple Joseph E Trisubstituted nitrogen modulators of tyrosine phosphatases
WO2006017124A2 (en) * 2004-07-09 2006-02-16 Cengent Therapeutics, Inc. Oxygen/nitrogen heterocycle inhibitors of tyrosine phosphatases
EP1841749A1 (de) 2004-09-02 2007-10-10 Metabasis Therapeutics, Inc. Thiazol- und thiadiazolderivate als inhibitoren von tyrosinphosphatasen
US7691898B2 (en) * 2004-10-08 2010-04-06 Kotobuki Pharmaceutical Co., Ltd. Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia
US7504389B2 (en) 2004-11-15 2009-03-17 Ceptyr, Inc. Protein tyrosine phosphatase inhibitors and methods of use thereof
BRPI0707338A2 (pt) * 2006-01-30 2011-05-03 Transtech Pharma Inc derivados de imidazol, composições, e métodos substituìdos de uso como inibidores de ptpase
RU2462469C2 (ru) * 2007-01-26 2012-09-27 Канек Фарма Инк. Конденсированные ароматические дифторметанфосфонаты в качестве ингибиторов протеинтирозинфосфатазы ib (ptp-1b)
WO2009083275A1 (de) 2008-01-02 2009-07-09 Zeosys Gmbh Verfahren zur rückgewinnung halogenierter kohlenwasserstoffe
DE102014006224B4 (de) * 2014-04-30 2020-10-22 Chiracon Gmbh Verfahren zur Herstellung von 2-Aryl-2-Alkyl-malonsäuren
CN106631885B (zh) * 2016-09-28 2018-08-07 荆门医药工业技术研究院 一种制备4-甲醛肟基苯甲酸酯类衍生物的方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2381397A (en) 1996-04-19 1997-11-12 Novo Nordisk A/S Modulators of molecules with phosphotyrosine recognition units
CA2269659A1 (en) 1996-11-04 1998-05-14 Merck Frosst Canada & Co. Hydrolase binding assay

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Publication number Publication date
DE69905476D1 (en) 2003-03-27
AU761596B2 (en) 2003-06-05
CA2344927A1 (en) 2000-03-30
EP1115729B1 (de) 2003-02-19
ES2192396T3 (es) 2003-10-01
AU5724199A (en) 2000-04-10
EP1115729A1 (de) 2001-07-18
WO2000017211A1 (en) 2000-03-30
DE69905476T2 (de) 2003-12-24
JP2002526505A (ja) 2002-08-20
US6174874B1 (en) 2001-01-16

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