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CAPLUS COPYRIGHT 2006 ACS on STN
| TITLE:
| Preparation of [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia, other mental disorders, and central nervous system disorders |
| INVENTOR(S):
| Clark, Jerry D.; Davis, Jamie M.; Favor, David; Fay, Lorraine K.; Franklin, Lloyd; Henegar, Kevin E.; Johnson, Douglas S.; Nichelson, Brian J.; Ou, Ligong; Repine, Joseph Thomas; Walters, Michael A.; White, Andrew David; Zhu, Zhijian |
| PATENT ASSIGNEE(S):
| USA |
| SOURCE:
| U.S. Pat. Appl. Publ., 140 pp. CODEN: USXXCO |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
US 2005043309 A1 20050224 US 2004-900210 20040728
WO 2005019215 A1 20050303 WO 2004-IB2665 20040813
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, 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, NA, 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, US, UZ, VC, VN, YU, ZA, ZM, ZW
RW: BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM,
AZ, BY, KG, KZ, MD, RU, TJ, TM, AT, BE, BG, CH, CY, CZ, DE, DK,
EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PL, PT, RO, SE,
SI, SK, TR, BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE,
SN, TD, TG
ABSTRACT:
The authors prepd. [1,8]naphthyridin-2-ones and related compds. I [A = (CH2)mCH2, (CH2)mO, (CH2)mNH, or where one or two of the carbon or nitrogen atoms can be substituted, m = 2-5; D = N, C, CH, where when D = N, each carbon is covalently attached to D with a single bond; G = structure Q1, Q2; V, W = N, C, CH; ring L = satd. or unsatd. 5-, 6-, or 7-membered carbocyclic; Z and Q = independently N, C, CH, where at least one of Z and Q = N; X-Y = CH2CH2, CH:CH, CH2NH, NHCH2, N:CH, CH:N, OCH2, CH2O, or X-Y is substituted with R2, R3, R15, R16; R1 = H, COMe, C1-C3 alkyl; R2, R3, R15, R16 = independently H, halide, cyano, oxo, OH, COMe, C1-C4 alkyl, C1-C4 alkoxy; R4, R5 = independently H, halide, cyano, OH, COMe, C1-C4 alkyl, C1-C4 alkoxy; R6, R7 = independently H, Me; R8, R9, R10, R11, R12 = independently H, halide, COMe, C1-C4 alkyl, C1-C4 alkoxy, aryl, aryloxy; R13, R14 = independently H, halide, cyano, oxo, OH, COMe, C1-C4 alkyl, C1-C4 alkoxy] for treating central nervous system disorders and mental disorders including schizophrenia. Thus, reductive amination of 1-(2,3-dihydrobenzo[1,4]dioxin-5-yl)piperazine gave 7-[4-[4-(2,3-dihydrobenzo[1,4]dioxin-5-yl)piperazin-1-yl]butoxy]-3,4-dihydro -1H-[1,6]naphthyridin-2-one in 50% yield. The compds. were examd. for dopamine D2 receptor binding and D2 intrinsic activity.
Updated 5/16/2007 10:23:38 AM
