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1. (WO1998052614) COMPOSITION AND METHOD FOR ENHANCING TRANSPORT ACROSS BIOLOGICAL MEMBRANES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1998/052614    International Application No.:    PCT/US1998/010571
Publication Date: 26.11.1998 International Filing Date: 21.05.1998
Chapter 2 Demand Filed:    18.12.1998    
IPC:
A61K 47/48 (2006.01), C07B 61/00 (2006.01)
Applicants: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY [US/US]; Stanford, CA 94305 (US) (For All Designated States Except US).
ROTHBARD, Jonathan, B. [US/US]; (US) (For US Only).
WENDER, Paul, A. [US/US]; (US) (For US Only)
Inventors: ROTHBARD, Jonathan, B.; (US).
WENDER, Paul, A.; (US)
Agent: POWERS, Vincent, M.; Dehlinger & Associates, P.O. Box 60850, Palo Alto, CA 94306-0850 (US).
VOSSIUS & PARTNER; Siebertstr. 4, 81675 München (DE)
Priority Data:
60/047,345 21.05.1997 US
Title (EN) COMPOSITION AND METHOD FOR ENHANCING TRANSPORT ACROSS BIOLOGICAL MEMBRANES
(FR) COMPOSITION ET PROCEDE PERMETTANT D'AMELIORER LES TRANSPORTS A TRAVERS DES MEMBRANES BIOLOGIQUES
Abstract: front page image
(EN)Methods and compositions for transporting drugs and macromolecules across biological membranes are disclosed. In one embodiment, the invention includes a method for enhancing transport of a selected compound across a biological membrane, wherein a biological membrane is contacted with a conjugate containing a biologically active agent that is covalently attached to a transport polymer. In one embodiment, the polymer consists of from 6 to 25 subunits, at 50 % of which contain a guanidino or amidino sidechain moiety. The polymer is effective to impart to the attached agent a rate of trans-membrane transport across a biological membrane that is greater than the rate of trans-membrane transport of the agent in non-conjugated form. The transport-enhancing polymers are exemplified, in a preferred embodiment, by peptides in which arginine residues constitute the subunits. Such a polyarginine peptide may be composed of either all D-, all L- or mixed D- and L-arginines, any may include additional amino acids. More preferably, at least one, and preferably all of the subunits are D-arginine residues, to enhance biological stability of the polymer during transit of the conjugate of its biological target.
(FR)L'invention concerne des procédés et des compositions permettant de transporter des médicaments et des macromolécules à travers des membranes biologiques. Dans une forme de réalisation, l'invention concerne un procédé qui améliore le transport d'un composé sélectionné à travers une membrane biologique. Ce procédé consiste à mettre en contact une membrane biologique avec un conjugué contenant un agent biologiquement actif qui est lié de manière covalente à un polymère transporteur. Dans une forme de réalisation, le polymère est constitué de 6 à 25 sous-unités, dont au moins 50 % contiennent une fraction de chaîne latérale guanidino ou amidino. Le polymère est efficace pour conférer à l'agent attaché une vitesse de transport transmembranaire à travers une membrane biologique qui est supérieure à la vitesse de transport transmembranaire de l'agent se présentant sous une forme non conjuguée.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)