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WO1997040017A3 - Modulators of molecules with phosphotyrosine recognition units - Google Patents

Modulators of molecules with phosphotyrosine recognition units Download PDF

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Publication number
WO1997040017A3
WO1997040017A3 PCT/DK1997/000166 DK9700166W WO9740017A3 WO 1997040017 A3 WO1997040017 A3 WO 1997040017A3 DK 9700166 W DK9700166 W DK 9700166W WO 9740017 A3 WO9740017 A3 WO 9740017A3
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WO
WIPO (PCT)
Prior art keywords
molecules
recognition units
modulators
proteins
organic compounds
Prior art date
Application number
PCT/DK1997/000166
Other languages
French (fr)
Other versions
WO1997040017A2 (en
Inventor
Henrik Sune Andersen
Niels Peter Hundahl Moeller
Peter Madsen
Original Assignee
Novo Nordisk As
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 Novo Nordisk As filed Critical Novo Nordisk As
Priority to JP09537609A priority Critical patent/JP2000511883A/en
Priority to AU23813/97A priority patent/AU2381397A/en
Publication of WO1997040017A2 publication Critical patent/WO1997040017A2/en
Publication of WO1997040017A3 publication Critical patent/WO1997040017A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/1131,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D249/14Nitrogen atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/34Oxygen atoms
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    • 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
    • C07D285/081,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • 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
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen 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
    • C07D417/06Heterocyclic 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
    • 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)
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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
    • C07F9/3882Arylalkanephosphonic acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)

Abstract

The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, micro-organisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of the general formula (I) (L)n--Ar1--R1--A, wherein (L)n, n, Ar1, R1 and A are defined as defined in the application.
PCT/DK1997/000166 1996-04-19 1997-04-17 Modulators of molecules with phosphotyrosine recognition units WO1997040017A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP09537609A JP2000511883A (en) 1996-04-19 1997-04-17 Modulators of molecules with phosphotyrosine recognition units
AU23813/97A AU2381397A (en) 1996-04-19 1997-04-17 Modulators of molecules with phosphotyrosine recognition units

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DK46496 1996-04-19
DK0464/96 1996-04-19

Publications (2)

Publication Number Publication Date
WO1997040017A2 WO1997040017A2 (en) 1997-10-30
WO1997040017A3 true WO1997040017A3 (en) 1997-12-11

Family

ID=8093850

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK1997/000166 WO1997040017A2 (en) 1996-04-19 1997-04-17 Modulators of molecules with phosphotyrosine recognition units

Country Status (4)

Country Link
JP (1) JP2000511883A (en)
AU (1) AU2381397A (en)
WO (1) WO1997040017A2 (en)
ZA (1) ZA973349B (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262044B1 (en) 1998-03-12 2001-07-17 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (PTPASES)
JP2002514636A (en) * 1998-05-12 2002-05-21 アメリカン・ホーム・プロダクツ・コーポレイション Phenyloxo-acetic acids useful for treating insulin resistance or hyperglycemia
US6166069A (en) * 1998-05-12 2000-12-26 American Home Products Corporation Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
US6489344B1 (en) 1998-06-19 2002-12-03 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US6503935B1 (en) 1998-08-07 2003-01-07 Abbott Laboratories Imidazoles and related compounds as α1A agonists
US6174874B1 (en) * 1998-09-21 2001-01-16 Merck Frosst Canada & Co. Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)
US6933272B1 (en) 1998-09-22 2005-08-23 Erik Helmerhorst Use of non-peptidyl compounds for the treatment of insulin related ailments
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
AU3073700A (en) * 1999-01-19 2000-08-07 Sankyo Company Limited Troglitazone-containing medicinal compositions for inhibiting apoptosis
WO2000063171A1 (en) 1999-04-20 2000-10-26 Meiji Seika Kaisha, Ltd. Tricyclic compounds
AU4738600A (en) 1999-05-14 2000-12-05 Merck Frosst Canada & Co. Phosphonic and carboxylic acid derivatives as inhibitors of protein tyrosine phosphatase-1b (ptp-1b)
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
US7115624B1 (en) 1999-09-10 2006-10-03 Novo Nordisk A/S Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
EP1214060A2 (en) * 1999-09-10 2002-06-19 Novo Nordisk A/S Method of inhibiting protein tyrosine phosphatase 1b and/or t-cell protein tyrosine phosphatase and/or other ptpases with an asp residue at position 48
JP2003518129A (en) 1999-12-22 2003-06-03 メルク フロスト カナダ アンド カンパニー Phosphonic acid derivatives acting 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
US6486141B2 (en) 1999-12-22 2002-11-26 Merck Frosst Canada & Co. Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B)
AU2336001A (en) 1999-12-22 2001-07-03 Merck Frosst Canada & Co. Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1b (ptp-1b)
AU2335801A (en) 1999-12-22 2001-07-03 Merck Frosst Canada & Co. Aromatic phosphonates as protein tyrosine phosphatase 1b (ptp-1b) inhibitors
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
CA2402414A1 (en) 2000-03-22 2001-09-27 Christopher Bayly Sulfur substituted aryldifluoromethylphosphonic acids as ptp-1b inhibitors
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
ES2166328B1 (en) * 2000-05-11 2003-09-16 Consejo Superior Investigacion HETEROCICLIC INHIBITORS OF ENZYME GSK 3 USEFUL IN THE TREATMENT OF NEURODEGENERATIVE AND HYPERPROLIFERATIVE PROCESSES
US6376524B1 (en) 2000-06-21 2002-04-23 Sunesis Pharmaceuticals, Inc. Triphenyl compounds as interleukin-4 antagonists
US6613903B2 (en) 2000-07-07 2003-09-02 Novo Nordisk A/S Modulators of protein tyrosine phosphatases (PTPases)
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
GB0021726D0 (en) 2000-09-05 2000-10-18 Astrazeneca Ab Chemical compounds
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
GB0113041D0 (en) 2001-05-30 2001-07-18 Astrazeneca Ab Chemical compounds
EP1448538A1 (en) 2001-11-15 2004-08-25 Eli Lilly And Company Peroxisome proliferator activated receptor alpha agonists
GB0205690D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
US7442697B2 (en) 2002-03-09 2008-10-28 Astrazeneca Ab 4-imidazolyl substituted pyrimidine derivatives with CDK inhibitory activity
GB0205688D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
GB0205693D0 (en) 2002-03-09 2002-04-24 Astrazeneca Ab Chemical compounds
PT1492780E (en) 2002-04-03 2012-04-11 Novartis Ag 5-substituted 1,1-dioxo-¬1,2,5 thiazolidine-3-one derivatives as ptpase 1b inhibitors
GB0225986D0 (en) * 2002-11-07 2002-12-11 Astrazeneca Ab Chemical compounds
GB0227813D0 (en) * 2002-11-29 2003-01-08 Astrazeneca Ab Chemical compounds
WO2004071448A2 (en) * 2003-02-12 2004-08-26 Transtech Pharma Inc. Substituted azole derivatives as inhibitors of protein tyrosine phosphatases
TW200505441A (en) 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
US7355049B2 (en) 2003-06-24 2008-04-08 Hoffmann-La Roche Inc. Biaryloxymethylarenecarboxylic acids as glycogen synthase activator
CA2532965C (en) 2003-07-22 2013-05-14 Astex Therapeutics Limited 3, 4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
WO2005035551A2 (en) 2003-10-08 2005-04-21 Incyte Corporation Inhibitors of proteins that bind phosphorylated molecules
TW200528101A (en) 2004-02-03 2005-09-01 Astrazeneca Ab Chemical compounds
AR047894A1 (en) 2004-02-25 2006-03-01 Wyeth Corp THIOPHEN DERIVATIVES AS INHIBITORS OF PROTEIN THYROSINE PHOSPHATASE 1B (PTPASA 1B); METHODS FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE TREATMENT OF DISEASES MEDIATED BY PTPASA 1B
WO2005114197A2 (en) * 2004-04-15 2005-12-01 Albert Einstein College Of Medicine Of Yeshiva University Activity-based probes for protein tyrosine phosphatases
US8293778B2 (en) 2004-07-27 2012-10-23 Roche Palo Alto Llc Heterocyclic antiviral compounds
GB0416730D0 (en) 2004-07-27 2004-09-01 Novartis Ag Organic compounds
MX2007000788A (en) 2004-07-27 2007-03-23 Hoffmann La Roche Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors.
US7524870B2 (en) * 2004-12-03 2009-04-28 Hoffmann-La Roche Inc. Biaryloxymethylarenecarboxylic acids as glycogen synthase activators
WO2006077424A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
US20090036435A1 (en) 2005-01-21 2009-02-05 Astex Therapeutics Limited Pharmaceutical Compounds
GB0507298D0 (en) 2005-04-11 2005-05-18 Novartis Ag Organic compounds
WO2007039177A2 (en) 2005-09-29 2007-04-12 Sanofi-Aventis Phenyl- and pyridinyl- 1, 2 , 4 - oxadiazolone derivatives, processes for their preparation and their use as pharmaceuticals
NZ566878A (en) 2005-09-29 2010-07-30 Sanofi Aventis Phenyl-and pyridinyl-1,2,4-oxadiazolone derivatives with phenyl group, processes for their preparation and their use as pharmaceuticals
CN101277956A (en) 2005-09-30 2008-10-01 阿斯利康(瑞典)有限公司 Imidazo [1,2-A] pyridine having anti-cell-proliferation activity
US20100056505A1 (en) * 2005-11-21 2010-03-04 Biogen Idec Ma Inc. Substituted Pyrazalones
TW200800978A (en) * 2006-03-23 2008-01-01 Otsuka Pharma Co Ltd Carbazole compound
WO2007115058A2 (en) * 2006-03-31 2007-10-11 Novartis Ag Thiadiazolidinone inhibitors of ptpase
CA2664794A1 (en) 2006-10-20 2008-05-02 Merck & Co., Inc. Substituted imidazoles as bombesin receptor subtype-3 modulators
MX2009004112A (en) 2006-10-20 2009-05-11 Merck & Co Inc Substituted imidazoles as bombesin receptor subtype-3 modulators.
CA2667003A1 (en) 2006-10-20 2008-05-02 Merck & Co., Inc. Substituted imidazoles as bombesin receptor subtype-3 modulators
CL2008000835A1 (en) 2007-03-23 2008-10-03 Icagen Inc Pfizer Ltd COMPOUNDS DERIVED FROM SULFONAMIDS, INHIBITORS OF THE CALCIUM CHANNELS; PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUND; AND USE OF THE COMPOUND FOR THE TREATMENT OF PAIN, IRRITABLE INTESTINE SYNDROME, CROHN DISEASE, TAQUIARRITM
CN101657433A (en) 2007-03-29 2010-02-24 弗·哈夫曼-拉罗切有限公司 Non-nucleoside reverse transcriptase inhibitors
WO2008157407A2 (en) * 2007-06-13 2008-12-24 University Of Virginia Patent Foundation Thiadiazole, oxadiazole and triazole derivatives for treating leukemia
MX2010006647A (en) 2007-12-26 2010-08-17 Sanofi Aventis Cyclic pyridyl-n-(1,3,4)-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals.
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US20110112147A1 (en) 2009-11-11 2011-05-12 David Robert Bolin Indazolone analogs as glycogen synthase activators
US20110112158A1 (en) 2009-11-11 2011-05-12 David Robert Bolin Benzisoxazole analogs as glycogen synthase activators
US7947728B1 (en) 2009-11-11 2011-05-24 Hoffmann-La Roche Inc. Indole and indazole analogs as glycogen synthase activators
US20110118314A1 (en) 2009-11-16 2011-05-19 Weiya Yun Piperidine analogs as glycogen synthase activators
US8039495B2 (en) 2009-11-16 2011-10-18 Hoffman-La Roche Inc. Biphenyl carboxylic acids and bioisosteres as glycogen synthase activators
US7939569B1 (en) 2009-12-01 2011-05-10 Hoffmann-La Roche Inc. Aniline analogs as glycogen synthase activators
US20110136792A1 (en) 2009-12-04 2011-06-09 David Robert Bolin Novel carboxylic acid analogs as glycogen synthase activators
RU2012139463A (en) * 2010-02-17 2014-03-27 Янссен Фармацевтика Нв AMINOTIAZOLES AS MODULATORS OF ACTIVITY OF PROTEINS RELATED TO ALPHA ESTROGEN RECEPTOR
US9505728B2 (en) 2012-03-09 2016-11-29 Inception 2, Inc. Triazolone compounds and uses thereof
CN104797573A (en) 2012-11-07 2015-07-22 卡鲁斯治疗有限公司 Novel histone deacetylase inhibitors and their use in therapy
WO2014099503A1 (en) 2012-12-20 2014-06-26 Inception 2, Inc. Triazolone compounds and uses thereof
WO2014181137A1 (en) 2013-05-10 2014-11-13 Karus Therapeutics Ltd Novel histone deacetylase inhibitors
CA2921420A1 (en) 2013-09-06 2015-03-12 Inception 2, Inc. Triazolone compounds and uses thereof
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
EP4076448A4 (en) 2019-12-20 2024-03-27 Tenaya Therapeutics, Inc. Fluoroalkyl-oxadiazoles and uses thereof
EP4333841A1 (en) 2021-05-04 2024-03-13 Tenaya Therapeutics, Inc. 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, hdac6 inhibitors for use in the treatment of metabolic disease and hfpef

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0193256A1 (en) * 1985-01-19 1986-09-03 Takeda Chemical Industries, Ltd. Thiazolidinedione derivatives, their production and use
EP0339549A2 (en) * 1988-04-25 1989-11-02 F. Hoffmann-La Roche Ag Tyr-peptide analogs
WO1991012003A1 (en) * 1990-02-09 1991-08-22 The Upjohn Company Use of insulin sensitizing agents to treat hypertension
EP0500337A1 (en) * 1991-02-22 1992-08-26 University Of Colorado Foundation, Inc. Composition containing aryl-substituted rhodanine derivatives for the treatment of type I diabetes
WO1995007694A1 (en) * 1993-09-15 1995-03-23 Sankyo Company, Limited Use of thiazolidinediones to prevent or delay onset of niddm
WO1996040113A2 (en) * 1995-06-07 1996-12-19 Sugen, Inc. Phosphatase inhibitors
EP0764632A2 (en) * 1995-09-21 1997-03-26 Eli Lilly And Company Selective beta3 adrenergic agonists

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0193256A1 (en) * 1985-01-19 1986-09-03 Takeda Chemical Industries, Ltd. Thiazolidinedione derivatives, their production and use
EP0339549A2 (en) * 1988-04-25 1989-11-02 F. Hoffmann-La Roche Ag Tyr-peptide analogs
WO1991012003A1 (en) * 1990-02-09 1991-08-22 The Upjohn Company Use of insulin sensitizing agents to treat hypertension
EP0500337A1 (en) * 1991-02-22 1992-08-26 University Of Colorado Foundation, Inc. Composition containing aryl-substituted rhodanine derivatives for the treatment of type I diabetes
WO1995007694A1 (en) * 1993-09-15 1995-03-23 Sankyo Company, Limited Use of thiazolidinediones to prevent or delay onset of niddm
WO1996040113A2 (en) * 1995-06-07 1996-12-19 Sugen, Inc. Phosphatase inhibitors
EP0764632A2 (en) * 1995-09-21 1997-03-26 Eli Lilly And Company Selective beta3 adrenergic agonists

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, No. 125:195654; & JP,A,08 157 461 (18-06-96). *
STN INTERNATIONAL, File CAPLUS, Accession No. 1996:543848, YANAGISAWA HIROAKI et al., "Preparation of (Azolylphenoxy)alkyl Aryl or Heterocyclyl Sulfone Derivatives Having Aldose Reductase-Inhibitory Activity as Hypolipidemics, Hypoglycemics and Antiobesity Agents". *
TETRAHEDRON LETTERS, Volume 33, No. 29, 1992, MARK S. SMYTH et al., "A General Method for the Preparation of Benzylic x,x-Difluorophosphonic Acids; Non-Hydrolyzable Mimetics of Phosphotyrosine", pages 4137-4140. *
TETRAHEDRON, Volume 52, No. 30, 1996, BIN YE et al., "Synthesis of a Difluorophosphonomethyl-Containing Phosphatase Inhibitor Designed from the X-Ray Structure of a PTP1B-Bound Ligand", pages 9963-9970. *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US7425557B2 (en) 1998-06-19 2008-09-16 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3

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