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1. (WO2014186398) COMPOUNDS FOR INHIBITING DRUG-RESISTANT STRAINS OF HIV-1 INTEGRASE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/186398    International Application No.:    PCT/US2014/037905
Publication Date: 20.11.2014 International Filing Date: 13.05.2014
IPC:
A61K 31/4375 (2006.01), A61K 31/4704 (2006.01), A61K 31/496 (2006.01), A61K 31/5377 (2006.01), C07D 471/04 (2006.01), A61K 45/06 (2006.01)
Applicants: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES [US/US]; National Institutes of Health Office of Technology Transfer 6011 Executive Boulevard Suite 325, MSC 7660 Bethesda, MD 20852-7660 (US)
Inventors: ZHAO, Xue, Zhi; (US).
SMITH, Steven; (US).
METIFIOT, Mathieu, A.; (US).
JOHNSON, Barry; (US).
MARCHAND, Christophe; (US).
HUGHES, Stephen; (US).
POMMIER, Yves; (US).
BURKE, Terrence, R.; (US)
Agent: RUPERT, Wayne; Klarquist Sparkman, LLP One World Trade Center, Suite 1600 121 Sw Salmon Street Portland, OR 97204 (US)
Priority Data:
61/899,061 01.11.2013 US
61/824,306 16.05.2013 US
Title (EN) COMPOUNDS FOR INHIBITING DRUG-RESISTANT STRAINS OF HIV-1 INTEGRASE
(FR) COMPOSÉS POUR INHIBER DES SOUCHES RÉSISTANTES AUX MÉDICAMENTS D'INTÉGRASE DE VIH-1
Abstract: front page image
(EN)A method of inhibiting drug -resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH; Y is H or OH; each of Z1-Z5 is independently H or halogen; R4 is H, OH, NH2, NHR8, NR8R9 or R8; R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and R8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally- substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen to which R8 and R9 are attached form an optionally-substituted heterocycle.
(FR)La présente invention concerne un procédé d'inhibition d'intégrase de VIH-1 résistant aux médicaments chez un sujet comprenant l'administration à un sujet qui en a besoin d'une quantité thérapeutiquement efficace d'un composé de formule I, ou un sel ou ester pharmaceutiquement acceptable de celui-ci, ayant une structure : dans laquelle X est N, C(OH), ou CH; Y est H ou OH; chacun de Z1-Z5 est indépendamment H ou halogène; R4 est H, OH, NH2, NHR8, NR8R9 ou R8; R5, R6, et R7 sont chacun indépendamment H, halogène, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, ou R5 et R6 conjointement avec les atomes de carbone auxquels R5 et R6 sont liés forment un carbocycle facultativement substitué ou un hétérocycle facultativement substitué; et R8 et R9 sont chacun indépendamment H, alkyle facultativement substitué, alcényle facultativement substitué, alcynyle facultativement substitué, aryle facultativement substitué, cycloalkyle facultativement substitué, cycloalkylène facultativement substitué, hétérocycle facultativement substitué, amide facultativement substitué, ester facultativement substitué, ou R8 et R9 conjointement avec l'azote auquel R8 et R9 sont liés forment un hétérocycle facultativement substitué.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, IR, IS, JP, KE, KG, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, 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, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)