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1. WO2011106898 - METHODS AND SYSTEMS FOR PREPARING IRREVERSIBLE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES

Publication Number WO/2011/106898
Publication Date 09.09.2011
International Application No. PCT/CA2011/050126
International Filing Date 03.03.2011
IPC
C07F 9/38 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P-C bonds
38Phosphonic acids ; Thiophosphonic acids
A61K 31/661 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
661Phosphorus acids or esters thereof not having P-C bonds, e.g. fosfosal, dichlorvos, malathion
A61K 38/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
06Tripeptides
C07K 1/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
C07K 5/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
C07K 5/093 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
093the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07F 9/3882
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
38Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids ; , i.e. RP(=X)(XH)2 (X = S, Se)
3804not used, see subgroups
3882Arylalkanephosphonic acids
C07F 9/4056
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9Compounds containing elements of Groups 5 or 15 of the Periodic System
02Phosphorus compounds
28with one or more P—C bonds
38Phosphonic acids RP(=O)(OH)2; Thiophosphonic acids ; , i.e. RP(=X)(XH)2 (X = S, Se)
40Esters thereof
4003the acid moiety containing a substituent or a structure which is considered as characteristic
4056Esters of arylalkanephosphonic acids
C07K 5/0827
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
08Tripeptides
0827containing heteroatoms different from O, S, or N
C12Q 1/42
CCHEMISTRY; METALLURGY
12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS
1Measuring or testing processes involving enzymes, nucleic acids or microorganisms
34involving hydrolase
42involving phosphatase
Applicants
  • THE GOVERNORS OF THE UNIVERSITY OF ALBERTA [CA]/[CA] (AllExceptUS)
  • CAIRO, Christopher Warren [CA]/[CA] (UsOnly)
  • TULSI , Naresh Singh [AU]/[AU] (UsOnly)
  • DOWNEY , Alan Michael [CA]/[CA] (UsOnly)
Inventors
  • CAIRO, Christopher Warren
  • TULSI , Naresh Singh
  • DOWNEY , Alan Michael
Agents
  • OSLER, HOSKIN & HARCOURT LLP
Priority Data
61/310,08203.03.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) METHODS AND SYSTEMS FOR PREPARING IRREVERSIBLE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES
(FR) PROCÉDÉS ET SYSTÈMES POUR PRÉPARER DES INHIBITEURS IRRÉVERSIBLES DE PROTÉINES TYROSINES PHOSPHATASES
Abstract
(EN)
Described herein are the preparation and use of novel bromo- phosphonomethylphenylalanine amino acid derivatives (BrPmp) and BrPmp-containing peptides as specific, irreversible protein tyrosine phosphatase inhibitors, which are suitable for application in peptide synthesis. These derivatives are particularly advantageous since their synthesis is both easy and scalable, and they are suitable for peptide synthesis. The BrPmp derivatives described herein can be appropriately protected to allow for solid phase peptide synthesis (SPPS) and incorporation into peptides for preparation of protein tyrosine phosphatase inhibitors and inhibitor libraries. The peptides and peptide libraries can be used to identify new protein tyrosine phosphatase specific sequences and profile protein tyrosine phosphatase activity in cell lysates, diagnostic samples and biopsy samples.
(FR)
Cette invention concerne la préparation et l'utilisation de nouveaux dérivés de l'acide aminé bromophosphonométhylphénylalanine (BrPmp) et des peptides contenant lesdits BrPmp à titre d'inhibiteurs irréversibles, spécifiques, de protéines tyrosines phosphatases, qui se prêtent à une application en synthèse des peptides. Ces dérivés sont particulièrement avantageux dans la mesure où leur synthèse est à la fois facile et modulable, et où ils se prêtent à la synthèse des peptides. Les dérivés BrPmp ci-décrits peuvent être convenablement protégés pour permettre la synthèse de peptides en phase solide (SPPS) et leur incorporation dans des peptides pour la préparation d'inhibiteurs de protéines tyrosines phosphatases et de banques d'inhibiteurs. Les peptides et les banques de peptides peuvent être utilisés pour identifier de nouvelles séquences spécifiques des protéines tyrosines phosphatases et déterminer le profil d'activité desdites protéines tyrosines phosphatases dans des lysats cellulaires, des échantillons diagnostiques et des échantillons biopsiques.
Also published as
Latest bibliographic data on file with the International Bureau