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CAS indexed 446 chemical substances from this document. CAS subject entries for this document include: Antiviral agents; Human; Human immunodeficiency virus 1. | |
CAPLUS COPYRIGHT 2005 ACS on STN
| TITLE:
| Preparation and antiviral activity for HIV-1 of substituted azaindoleoxoacetylpiperazines |
| INVENTOR(S):
| Wang, Tao; Zhang, Zhongxing; Meanwell, Nicholas A.; Kadow, John F.; Yin, Zhiwei |
| PATENT ASSIGNEE(S):
| Bristol-Myers Squibb Company, USA |
| SOURCE:
| PCT Int. Appl., 367 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2002062423 A1 20020815 WO 2002-US455 20020102
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN,
CO, CR, CU, CZ, DE, DK, DM, DZ, EC, 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, PH, PL,
PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG,
UZ, VN, YU, ZA, ZM, ZW, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM
RW: GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW, AT, BE, CH,
CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, TR,
BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG
CA 2437524 AA 20020815 CA 2002-2437524 20020102
EP 1363705 A1 20031126 EP 2002-707413 20020102
R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE, MC, PT,
IE, SI, LT, LV, FI, RO, MK, CY, AL, TR
EE 200300359 A 20031215 EE 2003-359 20020102
BR 2002006636 A 20040225 BR 2002-6636 20020102
NZ 527193 A 20040528 NZ 2002-527193 20020102
JP 2004522755 T2 20040729 JP 2002-562428 20020102
BG 108021 A 20040430 BG 2003-108021 20030722
NO 2003003436 A 20031001 NO 2003-3436 20030801
ABSTRACT:
Title compds. Q(CO)nWCOA [Q = (un)substituted azaindolyl; W = (un)substituted piperazino; A = (un)substituted alkoxy, aryl, heteroaryl; n = 1, 2] were prepd. for use as antiviral agents, alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors, in the treatment of HIV and AIDS. Thus, 2-chloro-3-nitropyridine was cyclized with vinylmagnesium bromide to give 7-chloro-6-azaindole which was treated with ClCOCO2Me, followed by ester hydrolysis, amidation with (R)-3-methyl-1-benzoylpiperazine, and substitution with 4-FC6H4B(OH)2 to give the title compd. I which had an EC50 for HIV-1 in vitro of <1 .mu.M.
Updated 5/11/2007 11:38:34 AM