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Machine translation
1. (WO2001005779) METHOD OF DESIGNING TUBULIN POLYMERIZATION STABILIZERS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/005779 International Application No.: PCT/US2000/019524
Publication Date: 25.01.2001 International Filing Date: 17.07.2000
Chapter 2 Demand Filed: 24.01.2001
IPC:
C07C 233/58 (2006.01) ,C07C 233/87 (2006.01) ,C07C 235/14 (2006.01) ,C07C 271/22 (2006.01)
Applicants: ARAD, Dorit[IL/US]; US (UsOnly)
BOLLON, Arthur, P.[US/US]; US (UsOnly)
POLAND, Bradley, W.[US/US]; US (UsOnly)
YOUNG, David, C.[US/US]; US (UsOnly)
CYTOCLONAL PHARMACEUTICS, INC.[US/US]; 9000 Harry Hines Boulevard, Suite 621 Dallas, TX 75235, US (AllExceptUS)
Inventors: ARAD, Dorit; US
BOLLON, Arthur, P.; US
POLAND, Bradley, W.; US
YOUNG, David, C.; US
Agent: COOPER, Rod, C. ; Sidley Austin Brown & Wood 717 North Harwood, Suite 3400 Dallas, TX 75201-6507, US
HANSEN, Eugenia, S. ; Sidley & Austin Suite 3400 717 N. Harwood Dallas, TX 75201, US
Priority Data:
60/143,97315.07.1999US
60/171,89223.12.1999US
Title (EN) METHOD OF DESIGNING TUBULIN POLYMERIZATION STABILIZERS
(FR) CONCEPTION DE STABILISATEURS DE POLYMERISATION DE LA TUBULINE
Abstract:
(EN) A method for designing paclitaxel alternative compounds which stabilize the tubulin polymerization process has been found. These compounds in solution possess steric conformational properties of natural paclitaxel and are capable of binding to the tubulin protein at the same site where paclitaxel is known to bind. The compounds of the present invention stabilize tubulin polymerization in a way that is mechanistically equivalent to activity mechanism of paclitaxel. The compounds of the present invention have increased solubility, simpler synthesis, and the possibility for specificity and optimization due to the combinatorial reactions over natural paclitaxel.
(FR) L'invention concerne un procédé permettant la conception de composés de remplacement du paclitaxel, qui stabilisent le processus de polymérisation de la tubuline. Ces composés en solution présentent les caractéristiques de conformation stérique du paclitaxel naturel et sont capables de se fixer à la protéine de tubuline au même site de liaison que le paclitaxel. Ces composés stabilisent la polymérisation de la tubuline par un mécanisme correspondant au mécanisme d'activité du paclitaxel. Comparés au paclitaxel naturel, ces composés présentent une solubilité accrue, sont plus faciles à synthétiser et offrent des possibilités de réactions combinatoires permettant une spécificité et d'une optimisation.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)