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CAPLUS COPYRIGHT 2008 ACS on STN
| TITLE:
| Preparation of imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as PI-3 kinase inhibitors |
| INVENTOR(S):
| Ni, Zhi-Jie; Pecchi, Sabina; Burger, Matthew; Han, Wooseok; Smith, Aaron; Atallah, Gordana; Bartulis, Sarah; Frazier, Kelly; Verhagen, Joelle; Zhang, Yanchen; Iwanowicz, Ed; Hendrickson, Tom; Knapp, Mark; Merritt, Hanne; Voliva, Charles; Wiesmann, Marion; Legrand, Darren Mark; Bruce, Ian; Dale, James; Lan, Jiong; Levine, Barry; Costales, Abran; Liu, Jie; Pick, Teresa; Menezes, Daniel |
| PATENT ASSIGNEE(S):
| Novartis A.-G., Switz. |
| SOURCE:
| PCT Int. Appl., 236pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2007095588 A1 20070823 WO 2007-US62157 20070214
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, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN,
KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK,
MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO,
RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT,
TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
RW: AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE,
IS, IT, LT, LU, LV, 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, BW, GH,
GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM, AZ, BY,
KG, KZ, MD, RU, TJ, TM
ABSTRACT:
Title compds. represented by the formula I [wherein Q = O or S; X = CR3 or N; W = C or N; V = CR2, O or S; L1 = CR9 or N; L2 = CR6 or N; R1 = H, (un)substituted alkyl alkenyl, etc.; R2, R3, R7, R9 = independently H, (un)substituted alkyl, (hetero)aryl, etc.; R4-R6 = independently H, halo, cyano, etc.; R8 = H, (un)substituted alkyl, heterocyclyl, etc.; and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof] were prepd. as Phosphatidylinositol 3 (PI-3) kinase inhibitor. For example, reaction of N-(6-iodoimidazo[1,2-a]pyridin-2-yl)acetamide with 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3-(trifluoromethyl)pyridin-2 -amine gave II.bul.TFA in 21% yield. I showed PI3K inhibitory with IC50 value of less than about 10 .mu.M. Thus, I and their pharmaceutical compns. are useful for the prophylaxis or treatment of proliferative diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, phospholipid kinases, G-protein coupled receptors, and phosphatases.
Updated 1/25/2008 1:15:49 PM
