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CAPLUS COPYRIGHT 2004 ACS on STN
| TITLE:
| Preparation of 1,1-dioxido-4H-1,2,4-benzothiadiazines as hepatitis C polymerase inhibitors and anti-infective agents |
| INVENTOR(S):
| Pratt, John K.; Betebenner, David A.; Donner, Pemela L.; Green, Brian E.; Kempf, Dale J.; Mcdaniel, Keith F.; Maring, Clarence J.; Stoll, Vincent S.; Zhang, Rong |
| PATENT ASSIGNEE(S):
| USA |
| SOURCE:
| U.S. Pat. Appl. Publ., 160 pp., Cont.-in-part of U.S. Ser. No. 285,714. CODEN: USXXCO |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
US 2004087577 A1 20040506 US 2003-410853 20030410
US 2004097492 A1 20040520 US 2002-285714 20021101
US 2004162285 A1 20040819 US 2003-625121 20030723
WO 2004041818 A1 20040521 WO 2003-US34707 20031031
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, EG, 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, NI, NO, NZ,
OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM,
TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW, AM, AZ, BY,
KG, KZ, MD, RU
RW: BW, GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW, AT, BE,
BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU,
MC, NL, PT, RO, SE, SI, SK, TR, BF, BJ, CF, CG, CI, CM, GA, GN,
GQ, GW, ML, MR, NE, SN, TD, TG
ABSTRACT:
Title compds. I [wherein A = monocyclic or bicyclic ring selected from hetero/aryl, cycloalkyl, cycloalkenyl, heterocyclyl; R1 = H, (un)substituted cycloalkyl/cyclo/alkenyl, alkoxycarbonyl/alkoxy/aryl/arylsulfonyl/arylsulfanyl/carboxy/cyano/heteroary l/alkyl, heterocyclyl, etc.; R2, R3 = independently H, cyano, halo, (un)substituted alkenyl, alkoxycarbonyl, alkyl, heteroaryl, etc.; CR2R3C = 5- or 6-membered ring selected from Ph, pyridinyl, pyrimidinyl, pyridazinyl, thienyl, furanyl, pyrazolyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, triazolyl, thiadiazolyl, tetrazolyl, cyclopentyl, and cyclohexyl; R4 = OH and derivs., halo, NH2 and derivs., etc.; R5 = independently CN, NO2, (un)substituted alk(en/yn)yl, hetero/aryl, arylsulfonyl, heterocyclyl etc.; n = 0-4; their pharmaceutically acceptable salts, stereoisomers, or tautomers] were prepd. as hepatitis C (HCV) polymerase inhibitors for treating related infections. Thus reacting Et 2-(1,1-dioxido-4H-1,2,4-benzothiadiazin-3-yl)acetate with ester II in THF in the presence of NaH at reflux for 3 h and neutralizing the title compd. III with NaOH in MeCN/H2O gave the sodium salt III.bul.Na. I inhibited HCV polymerase with IC50's in the range of 0.003 .mu.M to 500 .mu.M. I inhibited RNA replication with EC50 in the range of 0.01 .mu.M to > 100 .mu.M. I exhibited a cytopathic effect redn. with TC50's in the range of 16 .mu.M to > 100 .mu.M.
Updated 5/9/2007 2:39:28 PM
