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1. (WO2011106898) METHODS AND SYSTEMS FOR PREPARING IRREVERSIBLE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2011/106898 International Application No.: PCT/CA2011/050126
Publication Date: 09.09.2011 International Filing Date: 03.03.2011
IPC:
C07F 9/38 (2006.01) ,A61K 31/661 (2006.01) ,A61K 38/06 (2006.01) ,C07K 1/00 (2006.01) ,C07K 5/00 (2006.01) ,C07K 5/093 (2006.01) ,C12Q 1/42 (2006.01) ,C40B 30/08 (2006.01) ,C40B 40/10 (2006.01) ,C40B 50/00 (2006.01) ,G01N 33/573 (2006.01) ,C12N 9/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
28
with one or more P-C bonds
38
Phosphonic acids (R-P(:O)(OH)2); Thiophosphonic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
661
Phosphorus acids or esters thereof not having P-C bonds, e.g. fosfosal, dichlorvos, malathion
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
06
Tripeptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
08
Tripeptides
093
the side chain of the first amino acid containing more carboxyl groups than amino groups, or derivatives thereof, e.g. Asp, Glu, Asn
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
Q
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES OR MICRO-ORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
1
Measuring or testing processes involving enzymes or micro-organisms; Compositions therefor; Processes of preparing such compositions
34
involving hydrolase
42
involving phosphatase
C CHEMISTRY; METALLURGY
40
COMBINATORIAL TECHNOLOGY
B
COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
30
Methods of screening libraries
08
by measuring catalytic activity
C CHEMISTRY; METALLURGY
40
COMBINATORIAL TECHNOLOGY
B
COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
40
Libraries per se, e.g. arrays, mixtures
04
Libraries containing only organic compounds
10
Libraries containing peptides or polypeptides, or derivatives thereof
C CHEMISTRY; METALLURGY
40
COMBINATORIAL TECHNOLOGY
B
COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
50
Methods of creating libraries, e.g. combinatorial synthesis
G PHYSICS
01
MEASURING; TESTING
N
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
33
Investigating or analysing materials by specific methods not covered by groups G01N1/-G01N31/131
48
Biological material, e.g. blood, urine; Haemocytometers
50
Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
53
Immunoassay; Biospecific binding assay; Materials therefor
573
for enzymes or isoenzymes
C CHEMISTRY; METALLURGY
12
BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
N
MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICRO-ORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
9
Enzymes, e.g. ligases (6.); Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating, or purifying enzymes
14
Hydrolases (3.)
16
acting on ester bonds (3.1)
Applicants:
CAIRO, Christopher Warren [CA/CA]; CA (UsOnly)
TULSI , Naresh Singh [AU/AU]; AU (UsOnly)
DOWNEY , Alan Michael [CA/CA]; CA (UsOnly)
THE GOVERNORS OF THE UNIVERSITY OF ALBERTA [CA/CA]; Suite 4000 10230 Jasper Avenue Edmonton, Alberta T5J 4P6, CA (AllExceptUS)
Inventors:
CAIRO, Christopher Warren; CA
TULSI , Naresh Singh; AU
DOWNEY , Alan Michael; CA
Agent:
OSLER, HOSKIN & HARCOURT LLP; Suite 1900 , 340 Albert Street Ottawa , Ontario K1R 7Y6, CA
Priority Data:
61/310,08203.03.2010US
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.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)