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1. (WO2012108990) PEPTIDE-PHOSPHOLIPID CONJUGATES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/108990    International Application No.:    PCT/US2012/021819
Publication Date: 16.08.2012 International Filing Date: 19.01.2012
IPC:
A61K 38/10 (2006.01), A61P 9/10 (2006.01)
Applicants: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION [US/US]; 351 West 10th Street Indianapolis, IN 46202 (US) (For All Designated States Except US).
VAN NIEUWENHZE, Michael, S. [US/US]; (US) (For US Only).
TURNER, William, W. [US/US]; (US) (For US Only).
WITZTUM, Joseph, L. [US/US]; (US) (For US Only).
HARTVIGSEN, Karsten [DK/DK]; (DK) (For US Only)
Inventors: VAN NIEUWENHZE, Michael, S.; (US).
TURNER, William, W.; (US).
WITZTUM, Joseph, L.; (US).
HARTVIGSEN, Karsten; (DK)
Agent: KEYES, William, John; Klintworth & Rozenblat IP LLC 850 West Jackson Boulevard, Suite 660 Chicago, IL 60607 (US)
Priority Data:
61/440,231 07.02.2011 US
Title (EN) PEPTIDE-PHOSPHOLIPID CONJUGATES
(FR) CONJUGUÉS PEPTIDE-PHOSPHOLIPIDE
Abstract: front page image
(EN)The present invention provides a peptide-phospholipid conjugate of Formula 1: (l) wherein: X is selected from the group consisting of -CR1R2-, -NR 3_ -0-, -S-, and - S+(R3)-; Y is selected from the group consisting of a bond, alkyl, alkenyl, alkynyl, haloalkyi, alkoxyalkyi, hydroxyalkyi, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; Z is a peptide comprising 1 to 50 amino acids; R1 and R2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyi, alkoxyalkyi, hydroxyalkyi, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; and R3 is selected from the group con¬ sisting of alkyl, alkenyl, alkynyl, haloalkyi, alkoxyalkyi, hydroxyalkyi, aminoalkyl, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocy cloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl. The peptide-phospholipid conjugates of the invention are stable, have strong, specific binding with the CD36 macrophage receptor, and are soluble in aqueous media. The conjugates have also been shown to efficiently compete for binding of OxLDL to macrophages, and may therefore be used in the treatment and prevention of atherosclerosis.
(FR)La présente invention concerne un conjugué peptide-phospholipide de Formule 1 dans laquelle : X est choisi dans le groupe consistant en -CR1R2-, -NR3-, -O-, -S- et -S+(R3)- ; Y est choisi dans le groupe consistant en une liaison, alkyle, alcényle, alcynyle, haloalkyle, alcoxyalkyle, hydroxyalkyle, amino, éther, cycloamino, cycloéther, aryle, hétéroaryle, arylalkyle, hétéroarylalkyle, hydroxyaryle, aryléther, cycloalkyle, hétérocycloalkyle, hydroxycycloalkyle, halocycloalkyle et aminocycloalkyle; Z représente un peptide comprenant de 1 à 50 acides aminés ; R1 et R2 sont chacun indépendamment choisis dans le groupe consistant en hydrogène, alkyle, alcényle, alcynyle, haloalkyle, alcoxyalkyle, hydroxyalkyle, amino, éther, cycloamino, cycloéther, aryle, hétéroaryle, arylalkyle, hétéroarylalkyle, hydroxyaryle, aryléther, cycloalkyle, hétérocycloalkyle, hydroxycycloalkyle, halocycloalkyle et aminocycloalkyle ; et R3 est choisi dans le groupe consistant en alkyle, alcényle, alcynyle, haloalkyle, alcoxyalkyle, hydroxyalkyle, aminoalkyle, amino, éther, cycloamino, cycloéther, aryle, hétéroaryle, arylalkyle, hétéroarylalkyle, hydroxyaryle, aryléther, cycloalkyle, hétérocycloalkyle, hydroxycycloalkyle, halocycloalkyle et aminocycloalkyle.
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, QA, RO, RS, RU, RW, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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)