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1. (WO2010073126) COMPOUNDS USEFUL IN DELIVERING ANTI-NEOPLASTIC THERAPY AND DIAGNOSTIC IMAGING TO HYPOXIC CELLS AND METHODS OF USE THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/073126 International Application No.: PCT/IB2009/007980
Publication Date: 01.07.2010 International Filing Date: 22.12.2009
IPC:
C07H 15/26 (2006.01) ,A61K 31/7056 (2006.01) ,A61K 31/706 (2006.01) ,A61K 49/00 (2006.01) ,A61K 51/04 (2006.01) ,A61P 35/00 (2006.01) ,C07H 15/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15
Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
26
Acyclic or carbocyclic radicals, substituted by hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
7056
containing five-membered rings with nitrogen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706
containing six-membered rings with nitrogen as a ring hetero atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49
Preparations for testing in vivo
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
02
characterised by the carrier
04
Organic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15
Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
Applicants:
THE GOVERNORS OF THE UNIVERSITY OF ALBERTA [CA/CA]; Suite 400 8308-1114 Street Edmonton Alberta T6G 2E1, CA (AllExceptUS)
WEIBE, Leonard, Irving [CA/CA]; CA (UsOnly)
KUMAR, Piyush [CA/CA]; CA (UsOnly)
ZHENG, Weizhong [CA/CA]; CA (UsOnly)
Inventors:
WEIBE, Leonard, Irving; CA
KUMAR, Piyush; CA
ZHENG, Weizhong; CA
Priority Data:
61/139,66922.12.2008US
Title (EN) COMPOUNDS USEFUL IN DELIVERING ANTI-NEOPLASTIC THERAPY AND DIAGNOSTIC IMAGING TO HYPOXIC CELLS AND METHODS OF USE THEREOF
(FR) COMPOSÉS UTILES DANS L'ADMINISTRATION D'UNE THÉRAPIE ANTINÉOPLASIQUE ET EN IMAGERIE DIAGNOSTIQUE DE CELLULES HYPOXIQUES ET PROCÉDÉS POUR LES UTILISER
Abstract:
(EN) Conjugate compounds comprising saccharides coupled to bioreductively activated drugs that permeate cell membranes via specific hypoxia- upregulated transporters in hypoxic cells and retain cytotoxic and rediosensitizmg activities. They are expected to be bioreductively activated intracellularly, and bind selectively to subcellular macromolecules. The compounds have numerous applications in diagnostic imaging and the therapeutic management of hypoxic cells and tissues, (e.g. cancer). Formula (13) and Formula (31).
(FR) L'invention concerne des composés qui traversent les membranes cellulaires au moyen de transporteurs spécifiques positivement régulés par l'hypoxie dans des cellules hypoxiques, sont activés par bioréduction dans le milieu intracellulaire, et se lient sélectivement aux macromolécules subcellulaires pour présenter une accumulation spécifique de l'hypoxie dans des cellules hypoxiques. Du point de vie chimique, ces composés sont des saccharides couplés à des médicaments activés par bioréduction. Les composés ont de nombreuses applications en imagerie diagnostique et dans la prose en charge thérapeutique des cellules et des tissus hypoxiques (par exemple, en cas de cancer).
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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, 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, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, 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)