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Pub. No.:    WO/1996/004281    International Application No.:    PCT/US1995/009702
Publication Date: 15.02.1996 International Filing Date: 31.07.1995
Chapter 2 Demand Filed:    27.02.1996    
C07D 239/46 (2006.01), C07D 239/48 (2006.01), C07D 239/50 (2006.01), C07D 251/52 (2006.01), C07D 473/06 (2006.01), C07D 473/18 (2006.01), C07D 473/40 (2006.01), C07D 487/04 (2006.01)
Applicants: THE UNITED STATES OF AMERICA, represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US/US]; National Institutes of Health, Office of Technology Transfer, Box OTT, Bethesda, MD 20892-9902 (US) (For All Designated States Except US).
ARCH DEVELOPMENT CORPORATION [US/US]; The University of Chicago, 1101 East 58th Street, Chicago, IL 60637 (US) (For All Designated States Except US).
THE PENN STATE RESEARCH FOUNDATION, INC. [US/US]; 113 Technology Center, University Park, Pennsylvania 16802 (US) (For All Designated States Except US).
MOSCHEL, Robert, C. [US/US]; (US) (For US Only).
PEGG, Anthony, E. [US/US]; (US) (For US Only).
DOLAN, M., Eileen [US/US]; (US) (For US Only).
CHAE, Mi-Young [KR/US]; (US) (For US Only)
Inventors: MOSCHEL, Robert, C.; (US).
PEGG, Anthony, E.; (US).
DOLAN, M., Eileen; (US).
CHAE, Mi-Young; (US)
Agent: GAGALA, Bruce, M.; Leydig, Voit & Mayer, Ltd., Suite 4900, Two Prudential Plaza, 180 North Stetson, Chicago, IL 60601-6780 (US)
Priority Data:
283,953 01.08.1994 US
Abstract: front page image
(EN)The present invention provides AGT inactivating compounds such as substituted $i(O)?6¿-benzylguanines of formula (I) wherein 7- or 9-substituted 8-aza-$i(O)?6¿-benzylguanines, 7,8-disubstituted $i(O)?6¿-benzylguanines, 7,9-disubstituted $i(O)?6¿-benzylguanines, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidines, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidines, as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesion at the $i(O)?6¿-position of guanine, by administering to a mammal an effective amount of one of the aforesaid compounds, 2,4-diamino-6-benzyloxy-$i(s)-triazine, 5-substituted 2,4-diamino-6-benzyloxypyrimidines, or 8-aza-$i(O)?6¿-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions of the $i(O)?6¿-position of guanine.
(FR)La présente invention concerne des composés inhibant l'enzyme AGT qui sont des $i(O)?6¿-benzylguanines substituées de la formule (I), des 8-aza-$i(O)?6¿-benzylguanines substituées en 7 ou en 9, des $i(O)?6¿-benzylguanines disubstituées en 7 et 9, des 2-amino-5-nitro-6(4)-benzyloxypyrimidines substituées en 4(6) et des 2-amino-5-nitroso-6(4)-benzyloxypyrimidines substituées en 4(6), ainsi que des compositions pharmaceutiques comprenant de tels composés et un vecteur acceptable sur le plan pharmaceutique. La présente invention concerne en outre un procédé permettant d'améliorer la chimiothérapie dirigée contre les cellules tumorales chez les mammifères, utilisant un agent alkylant anticancéreux cytotoxique provoquant des lésions au niveau de la position $i(O)?6¿ de la guanine. Cette amélioration est obtenue en administrant au mammifère une quantité suffisante pour être efficace d'un des composés susmentionnés, de 2,4-diamino-6-benzyloxy-$i(s)-triazine, d'une 2,4-diamino-6-benzyloxypyrimidine substituée en 5 ou de 8-aza-$i(O)?6¿-benzylguanine, ainsi qu'une quantité suffisante pour être efficace d'un agent alkylant anticancéreux cytotoxique provoquant des lésions au niveau de la position $i(O)?6¿ de la guanine.
Designated States: AM, AT, AU, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LT, LU, LV, MD, MG, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TT, UA, UG, US, UZ, VN.
African Regional Intellectual Property Organization (KE, MW, SD, SZ, UG)
European Patent Office (AT, BE, CH, DE, DK, ES, 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)