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1. (WO2007001455) HYDROPHOBIC POLYAMINE AMIDES AS POTENT LIPOPOLYSACCHARIDE SEQUESTRANTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/001455 International Application No.: PCT/US2005/041042
Publication Date: 04.01.2007 International Filing Date: 14.11.2005
IPC:
A61K 31/16 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
16
Amides, e.g. hydroxamic acids
Applicants:
MEDIQUEST THERAPEUTICS, INC. [US/US]; 22322 20th Ave. SE, Suite 100 Bothell, WA 98021, US (AllExceptUS)
THE UNIVERSITY OF KANSAS [--/US]; 1501 Wakarusa Drive Lawrence, KS 66049, US (AllExceptUS)
BURNS, Mark, R. [US/US]; US (UsOnly)
DAVID, Sunil, A. [IN/US]; US (UsOnly)
Inventors:
BURNS, Mark, R.; US
DAVID, Sunil, A.; US
Agent:
AMERNICK, Burton, A.; Connolly Bove Lodge & Hutz LLP 1990 M Street, N.W., Suite 800 Washington, DC 20036-3425, US
Priority Data:
60/627,08212.11.2004US
Title (EN) HYDROPHOBIC POLYAMINE AMIDES AS POTENT LIPOPOLYSACCHARIDE SEQUESTRANTS
(FR) AMIDES DE POLYAMINE HYDROPHOBES, SEQUESTRANTS PUISSANTS DES LIPOPOLYSACCHARIDES
Abstract:
(EN) Lysine-spermine conjugates with a long-chain aliphatic (C12-C20) substituent at R1 bind and neutralize bacterial lipopolysaccharides. These compounds reduce lethality in a murine model of lipopolysaccharide-induced shock, and may serve as novel leads for developing novel anti- lipopolysaccharide agents for the therapy of Gram-negative sepsis. These compounds are represented by the formula (I): wherein X is 0 or H, H; R is a hydrophobic C12-C20 chain and Y is -NH2 or -H; and pharmaceutically acceptable salts thereof and prodrugs thereof.
(FR) La présente invention concerne des conjugués lysine-spermine qui comportent un substituant aliphatique à chaîne longue (C12-C20) en R1 et qui se lient aux lipopolysaccharides bactériens et les neutralisent. Ces composés réduisent la létalité dans un modèle murin de choc induit par un lipopolysaccharide et ils peuvent servir de pistes innovantes pour la mise au point d'agents anti-lipopolysaccharide innovants dans le traitement de la septicémie à germes Gram négatif. Ces composés sont représentés par la formule (I) : dans laquelle X est 0 ou H, H ; R est une chaîne hydrophobe en C12-C20 et Y est -NH2 ou -H ; et par leurs sels et promédicaments pharmaceutiquement acceptables.
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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)
Also published as:
EP1817018JP2008519856CA2587344AU2005333545