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CAPLUS COPYRIGHT 2005 ACS on STN
| TITLE:
| Preparation of azabicyclic heterocycles as cannabinoid receptor modulators |
| INVENTOR(S):
| Yu, Guixue; Ewing, William R.; Mikkilineni, Amarendra B.; Pendri, Annapurna; Sher, Philip M.; Gerritz, Samuel; Ellsworth, Bruce A.; Wu, Gang; Huang, Yanting; Sun, Chongqing; Murugesan, Natesan; Gu, Zhengxiang; Wang, Ying; Sitkoff, Doree; Johnson, Stephen R.; Wu, Ximao |
| PATENT ASSIGNEE(S):
| USA |
| SOURCE:
| U.S. Pat. Appl. Publ., 196 pp. CODEN: USXXCO |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
US 2005143381 A1 20050630 US 2004-16135 20041217
WO 2005063761 A1 20050714 WO 2004-US42820 20041217
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, IS, IT, LT, 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
US 2005192278 A1 20050901 US 2004-15876 20041217
WO 2005061509 A1 20050707 WO 2004-US42542 20041220
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, IS, IT, LT, 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 present application describes compds. I [R1, R2 = halo, CN, alkyl, etc.; R3 = alkyl, alkenyl, cycloalkyl, etc.; R6 = H, alkyl, cycloalkyl, etc.; R7 is absent when double bond; or R7 = H, alkyl, cycloalkyl, etc.], pharmaceutical compns. comprising at least one compd. I and optionally one or more addnl. therapeutic agents and methods of treatment using the compds. I both alone and in combination with one or more addnl. therapeutic agents. Over 400 compds. I were prepd. E.g., a multi-step synthesis of II, starting from dibromopyridazinone, was given. Representative compds. I showed the CB-1 receptor binding Ki values in the range of 0.01 nM to 10000 nM.
Updated 5/10/2007 1:15:25 PM
